Giáo Trình Môn Hóa Dư C

MC LC
Chng I: Ha dc i cng
Chng II:
Chng III
Chng IV
Chng V
Chng VI
Chng VII
Chng VIII
Chng IX
Chng X
Chng XI
Chng XII
Chng XIII
Chng XIV
Chng XV
CHNG I
HA DC I CNG
I. nh ngha mn hc
Ha dc l mn hc s nghin cu v cng thc ha hc, tnh cht l ha, mi lin quan
gia cu trc ha hc v tc dng dc l ca cc hp cht dng lm thuc.
Ngoi ra, c mt s khi nim khc v mn hc
Ha dc l mt ngnh ha hc th hin cao s kt hp gia ha hu c v sinh ha, ha
tin hc, dc l, sinh hc phn t, ton thng k v ha l.
II. V tr mn hc
i vi sinh vin dc, ha dc l mn hc nghip v dc. Cc mn c s ca ha
dc l ha v c, ha hu c, ha l, ho phn tch, vi sinh, k sinh trng, sinh ha,
bnh hc.
III. Mc tiu mn hc
Sau khi hc xong mn ny, ngi hc c th:
Trinh bay va giai thich c c ch tac du ng, ap du ng i u tri cua cac thu c a i di n
trong tng nhom.
ng dng ca kim nghim trong sn xut ch phm thuc.
Phn tich c tac du ng khng mong mu n va c tin h cua thu c bi t cach phong
va x tri.
K c cac n thu c ung nguyn t c, ung chuyn mn, ung phap li.
IV. Cc kin thc cn nm khi hc mn ha dc
Mt phn t c tc dng sinh hc c th mang hai thnh phn cu to chnh: khung phn
t v nhm chc (quyt nh kiu tc dng sinh hc)
Mt phn t c tc dng sinh hc c th mang hai nhm chc: nhm c tc dng (nhm
c hot tnh) v nhm nh hng (c kh nng thay i tnh cht l ha ca phn t).
Nhm mang hot tnh thng l nhng nhm nguyn t khng thay i, l phn c coi
l cn thit c tc dng c hiu.
Nhm c hot tnh gn vo gc khc nhau, c th c tc dng khc nhau.
S thay i gc gn i khi c th to tc dng khc nhau.
S thay i v tr gn c th lm thay i hn tc dng.
V tr, khong cch gia cc nhm hot ng, hinh th phn t u nh hng n hot
tnh ca thuc.
S th v bin i cc nhm chc
S tc dng sinh hc ca thuc c coi l do ton b phn t quyt nh. Ty nhin, khi
thay th hoc bin i nhm chc ca nguyn t cng lm nh hng n hot tnh ca
thuc. C th cc nhm chc sau:
- Cc hp cht hydrocarbon cha no c hot tnh mnh hn hp cht no, kh nng
phn ng cao.
- Halogen: lm tng hot tnh, cng hot lc v c tnh ca thuc. Trong ,
hot tnh ph thuc vo bn cht halogen, cng hot lc v c tnh ph thuc
vo s lng v v tr halogen c gn. Halogen gn vo vng thm v no lm
tng c tnh.
Vd: CHCl3 (Cloroform): gy m
CHBr3 (Bromoform): tr ho
CHI3 (Idoform): st khun
- Oxygen: ty thuc nhm chc nng cha oxy
+ -OH alcol: tng hot tnh. Tc dng gy ng tng t alcol bc I-III v gim khi
tng cc nhm OH alcol.
+ -OH phenol: tng hot tnh v c tnh. Phenol th hin tnh kh trng, hot tnh
tng ln theo s lng nhm OH.
- Aldehyd, ceton, carboxyl: tng tnh cht dc lc
- Nitrogen: cc nhm cha N thng tng tc dng ca thuc
- Nhm amino: tng c tnh ca phn t.
- Cc gc alkyl: thay i tc dng ca thuc trong c th.
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- Cc nhm thiol (-SH): d b oxy ha, tc dng vi kim loi v cc hp cht lin kt
kp. Thng dng lm thuc gii c v khi u
Thay i cc nhm gn vo nhn benzene
Khi thm nhp vo c th, benzene kch thiachs mnh vo trung tm vn ng c th
dn n ng c v t vong.
- Alkyl, halogen: tng c tnh
- Hydroxyl: thuc st trng.
- Aldehyde v ceton thm lm tng c tnh.
- Nhm carboxyl: gim c tnh
- Nhm amin, hoc kh nitrobenzene to thnh anilin. Cc cht ny gy c cho
thn kinh trung ng v h tun hon nhng ng thoi c tc dng h nhit gim
au.
S ph thuc ca hot tnh sinh hc i vi tnh cht l ha ca dc cht.
TNH CHT L HA KH NNG THAM GIA VO CC PHH
CU TO HA HC
TC DNG SINH HC
V. Ni dung bi hc:
- Tn khoa hc, tn thng mi
- Cng thc: cu to, phn t.
- iu ch:
- c tnh (tnh cht l ha):
o L tnh:
o Ha tnh:tnh cht ca khung c bn, nhm chc, phn t
- Kim nghim (cc pp xc nh cht lng thuc): nhm nh tnh, xc nh tinh khit,
nh lng hm lng hot cht. Gm:
o nh tnh:
Cc p hh c hiu(2-3 p): xc nh khung, nhm chc, phn t.
Cc pp vt l-ha l: ph (hng ngoi IR; t ngoi UV)
Sc k: SKLM (TLC), sc k kh (GC), sc k hiu nng cao (HPLC).
o nh lng: xc nh hm lng thnh phn c hot tnh trong thuc.
- Cng dng- cch dng:
o Tc dng (tnh cht dc l): chnh, ph
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o Ch nh:
Cng dng: cn c vo tc dng dc l ca thuc.
Cc bnh tt c ch nh dng (k n).
o c tnh v tai bin:
o Tng tc thuc v tng k:
o Liu dng-cch dng:
o Bo qun:
- T lng gi.
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CHNG II
THUC KHNG SINH
MC TIU
1.V c cng thc cu to chung ca cc nhm khng sinh, mi lin quan gia cu trc v tc
dng ca cc nhm khng sinh.
2.Trnh by tnh cht l ha ng dng trong kim nghim ca mt s khng sinh.
3. Hng dn s dng cc thuc khng sinh an ton, hp l, hiu qu.
NI DUNGN BI HC:
Da vo cu trc ha hc c th chia cc nhm khng sinh sau:
1. Khng sinh beta-lactam.
2. Khng sinh Aminoflycosid.
3. Khng sinh tetracycline.
4. Cloramphenicol v dn cht.
5. Khng sinh Macrolid.
6. Khng sinh Lincosamid.
7. Khng sinh Polypeptid.
8. Cc khng sinh khc: Rifamycin., Quinolon
A. CC KHNG SINH NHM -LACTAM

1. Cu trc
L nhm khng sinh ln nht k c tc dng tr bnh ln tn lng sn xut v doanh s.
Cu trc: khng sinh thuc h - lactam l nhng khng sinh c cu trc azetidin-2-on (cn
c gi l vng - lactam) mt amid vng 4 cnh.
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D vng azetidin-2-on thng lin kt vi mt d vng khc:
- Azetidin-2-on + thiazolidincu trc penem (nhm penicillin). Trong nhm ny cn c cc

cht tng ng vi penicillin mang cu trc penem, carbapenem v oxapenem (nhn
clavam).
- Azetidin-2-on + dihydrothiazincu trc cephem (nhm cephalosporin). Trong nhm ny

cn c nhng cht tng ng vi cephalosporin mng cu trc oxacephem v carbacephem.
- Azetidin-2-on ng ring rcu trc monobactam
2. Quan h cu trc v tc dng:

Hot tnh khng khun ca nhng khng sinh h - lactam ph thuc vo:
- S nguyn vn ca vng - lactam
- S hin din ca mt nhm chc c tnh acid trn N hoc C
- S hin din ca nhnh bn acylamin
- S kt hp d vng - lactam vi mt d vng khc cng nh cu dng ca hai hoc nhiu
cacbon bt i ng vai tr quan trng trong hot tnh khng khun.
3. C ch tc dng
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c ch hot ng ca transpeptidase
1. NHM PENICILLIN
Nm 1929, A. Flemming phn lp ra benzyl penicillin t mi trng nui cy Penicillium

notatum; nhng n nm 1949 cht ny c a vo ng dng trn lm sng. Nm 1957,
ngi ta tch c 6APA, m u cho mt lot cc khng sinh penicillin bn tng hp ra i.
Tn cc cht lun c ui t illin
1.c im chung:
1.1 Tnh cht vt l:
- Cc penicillin di dng mui hoc dng acid l nhng bt trng khng mi khi tinh khit.
- Ph UV a s cc nhm R acyl ha trn 6APA u l vng thm nn cho ph hp thu

vng UV c th ng dng c.
- Ph IR: vng 16000-18000 cm-1
1.2. Tnh cht ha hc:
Tnh acid (nhm -COOH t do):
Cc penicillin c kh nng to mui natri v kali tan trong nc, trong khi cc mui kim
loi nng (mui Cu+ ) th khng tan hoc kch thch s phn hy.
Cc penicillin cng c kh nng to mui vi cc amin:
+ To cc penicillin thy gii chm nh: procain penicillin ( tc ng ko di t 24-48h),

benzathin penicillin (tc ng ko di t 2-4 tun).
* Ch :
Mt s c tnh base nh nhm aminosid v cc alkaloid khi trn chung vi penicilin s gy

kt ta.
Cc penicillin c kh nng to este vi alcol: Gii phng chm hot cht.
Tnh khng bn ca vng beta lactam:
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+ S phn hy trong mi trng kim: Mi trng pH > 8 m vng
+ S hin din ca mui kim loi nng
+ S alcol phn v amino phn
+ S phn hy trong mi trng acid
Ngoi ra vng beta lactam c th m bi lactam tit ra t vi khun.
1.3. Phn ng mu phn bit cc penicillin v cephalosporin
Tin hnh: 2mg/ng nghim, thm 1 git nc lm m;
Thm 2ml TT formaldehyd/H2SO4 96%, trn u: Xem mu.
t ng nghim vo cch thy 100o C; quan st i mu /1 pht
Quan st i mu: Khc nhau gia cc cht -lactam.
Bng: Thay i mu ca cc -lactam trong 1 pht
Mu penicillin th TT Formol/H2SO4 (t0 TT Formol/H2SO4 (1000

phng) C/1 pht)
Amoxicillin Khng mu Vng sm
Benzathin penicillin G Khng mu Nu
Ampicillin Khng mu Vng sm
Penicillin G Khng mu Nu
Cephalexin Vng nht Vng sm
Cephaloridin nu
Cephalothin nu
Cloxacillin Vng xanh lc Vng m
Flucloxacillin Vng xanh lc Vng
Penicillin V Nu Nu sm
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1.4. Cc phng php nh lng penicillin:
Phng php vi sinh: L kinh in, p dng cho khng sinh.
Hm lng: Tnh theo n v quc t (UI = Unit Internationale)
- Penicillin G, th trn chng t cu vng: 1UI = 0,6 g penicillin G natri tinh khit =
0,627g penicillin G kali tinh khit (1mg penicillin G natri tng ng 1667 UI);
Phng php o Hg:
- Thy phn penicillin th/NaOH; to phng/15 pht;
- Trung ha bng HNO3; thm m pH 4,6;
- Chun bng Hg(NO3)2 0,02M; o in th (Cp in cc Hg (I) sulfat-Pt)
Xc nh penicillin ton phn bng o iod:
- Thu phn penicillin nh o Hg; Acid ha bng HCl 1N;
- Thm 10ml d.d.I2 0,01 N; y bnh 15 pht;
- Chun iod d bng natri thiosulfat 0,01N; h tinh bt.
Cc phng php vt l: HPLC,....
Tc dng:
* C ch tc dng: thuc c ch to vch ca vi khun gram dng, mt s vi khun gram

m. Khng tc dng vi mt s trc khun gram m, trc khun lao, virus,....
- cc vi khun khng li cc khng sinh -lactam bng cch tit ra cc -lactam c tc dng
m vng -lactamtheo phn ng i nhn vo C=O, lm mt tc dng ca khng sinh.
- Cc khng sinh Penicillin l cc khng sinh t c, ngoi tr d ng.
2.Phn loi penicillin v iu ch:
* Cng thc chung:
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Da vo ngun gc c th sp xp penicillin thnh 3 nhm sau:
2.1 Penicillin nhm I:
Khng sinh tc dng dit khun
Nhm ny c ph tc dng hp, ch yu tc dng trn vi khun gram dng ( lin cu, ph
cu, t cu tit -lactam).
Thuc tc dng tt nht vo giai on phn chia ca vi khun, km tc dng trn vi khun
trng thnh.
c im hot tnh:
- D b -lactamase ph hy. Thi gian bn thi ngn (~1 h).
- Penicillin G (TN): Khng bn/acid, ch dng ng tim.
- Penicillin V v dn cht: Bn/acid, ung c.
* Mt s penicillin dng trong iu tr
1. PENICILLIN G KALI (NATRI)
Tn khc: Benzylpenicillin kali (natri).
1.1. Cng thc:
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1.2. iu ch: Nui cy Penicillium notatum v Penicillium khc.
Tnh cht: Bt kt tinh trng, v ng, mi penicillin; ht m .D tan trong nc. Dung dch,
nu n nh pH = 5,5-6,0 v nhit 15C, c th dng c trong vng 24h.
nh tnh:(xem bng)
nh lng: Bng php o thy ngn
Hot lc: Tnh bng UI
1.3. Ph tc dng: in hnh ca penicillin nhm I:
Ch yu trn gram (+)
+ lu cu v mng no cu (gram -)
Khng bn trong mi trng acid, khng dng ng ung; ch tim bp (IM) hoc truyn
tnh mch (IV). t1/2 =1 h.
1.4. Ch nh, cch dng v liu lng:
- Nhim khun gram (+): h hp v phi, mng no, khp, mng tim, ty xng, nhim trng
mu, bch hu, than v.v;
Lu, giang mai: NL, tim IM: 200 000-1 triu UI/ln; 3-4 ln/24 h.
- Vim mng no, nhim trng mu c th tim ti 2 triu UI/ln.
Tr em, ty theo tui, tim 1/3 n 1/2 liu ngi ln. Bng 12-penicillin/dh Penicillin G-tip
Dng bo ch: L bt pha tim: 200.000; 500.000 v 1.000.000 UI.
Bo qun: nhit thp; trnh m.
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Penicillin G c thi gian bn thi ngn, phi tim nhiu ln trong ngy. V vy, ngi ta
nghin cu ch to ra cc mui ca penicillin G c tc dng ko di nh penicillin G
benzathin, penicillin G procain v.v
2. PENICILLIN G BENZATHIN
2.1 Cng thc:
2.2. Tnh cht: Bt kt tinh mu trng. Kh tan trong nc; tan trong ethanol. 900 mg
penicillin G benzathin tng ng 720 mg penicillin G.
2.3. Ch nh: Tng t penicillin G, nhng u tin cho cc mc ch:
- Duy tr iu tr hn ch s ln tim penicillin G/24 h.
- Nhim lin cu, lu, giang mai (tr giang mai no).
Liu dng:
Thp khp, thp tim do lin cu: Tim bp su: 1.200.000 UI/4 tun, hoc 600.000 UI/ln 2
ln/thng
Cp: phi tim penicillin G natri nhng ngy u; tip sau duy tr bng tim hn dch
penicillin G benzathin.
- Lu, giang mai: Tim bp su liu duy nht 2.400.000 UI.
Dng bo ch:
L bt 600.000 UI; 1.200.000 UI v 2.400.000 UI; km ng nc ct 2; 4 v 8 ml tng ng.
ng tim 10 ml hn dch: 600.000 UI/liu v 1.200.000 UI/liu. Lc mnh to hn dch ng

u trc khi tim.
CC: Ngi mn cm vi penicillin. Khng tim tnh mch.
Bo qun: nhit < 30oC.
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2.2 Penicillin nhm II:
L cc penicilin BTH, cht u tin l meticillin, vi c trng l khng -lactamase, nn

nhm ny cn c gi l "nhm M".
Nhm ny c dng trong cc trng hp nhim t cu vng tit penicillase khng

khng, c bit trong cc lnh vc tai, mi, hng, ph qun phi, da, m mm, nhim trng
mu, vim ni tm mc.
ISOXAZOLYPENICILLIN
Cng thc chung:
X=F FLUCLOXACILLIN
Cu trc chung v cng dng:
- Do c nhn isoxazol mang 2 nhm th phenyl v methyl v tr ortho i vi v trni CO-

, nn cn tr khng gian i vi penicillin.
- Do tc dng ht in t ca nhn isoxazol nn bn vi acid nn hp thu tt hn khi ung.
- S c mt ca cc nguyn t halogen lm tng hp thu khi ung v tng hot tnh
Ph tc dng: Nh penicilin nhm I. Hot lc mnh hn hn Penicillin G i vi cc chng

t cu tit penicillinase
c im:
- Khng b -lactamase phn hy (do gc R cng knh).
- Meticillin khng bn/H+, ch tim; d/c oxacillin ung c.
- Thi gian bn thi: t1/21 h (penicilin nhm I).
Ch nh: Thay th khi penicilin nhm I b vi khun khng
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Tc dng khng mong mun:
- Meticilin gy vim thn, chy mu tan huyt, gim bch cu.
- Cc d/c oxacillin gn halogen c vi thn kinh, thn v gan
2.3 Penicilin nhm III:
Gm nhng penicillin bn tng hp c c do s thay th trn C ca chc carboxamid

penicillin G mt nhm amin.
L cc cht c ph tc dng rng ln nhiu loi vi khun gram dng, vi khun gram m v
vng bn trong ng tiu ha. c dng iu tr cc bnh nhim trng ng h hp,
tit niu, sinh dc v nhim khun mu.
* Cc ch phm dng trong iu tr: Ampicillin, Amoxicillin, Cacbenicillin, Azlocillin
2.3.1. AMPICILLIN
Cng thc: C16H25N3O7S
iu ch: 6APA c acyl ha bi D-glycin
Tnh cht:
- Bt kt tinh trng, khng mi; tn ti di dng trihydrat bn nhit phng.
- Tan tng i trong nc, khng tan trong aceton, alcol, du bo.
nh tnh:
- Ph IR
- Sc k lp mng
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- Phn ng vi thuc th fromandehyd/H2SO4: cho mu vng nu.
- Phn ng vi thuc th Fehling cho mu tm.
nh lng:
- Phng php chun in th chun in th vi dung dch chun o Hg(NO3)2.
- Phng php o thy ngn.
Cng dng:
Trong mi trng nc, phn t phn cc nh mt acid amin do Ampicillin bn vng

trong mi trng acid. D b ph hy bi tc nhn kim
S phn cc ca phn t lm tng tnh thm qua mng t bo vi khun gram m, nn tc dng
tt trn vi khun gram m.
Cch dng-liu dng:
ng ung
Liu dng thng thng: NL: 500mg, 4 ln/ ngy; tim bp 2g/24h.
Dng s dng: tim, ung. C th kt hp vi Sulbactam ( cht c ch betalactam) m

rng ph khng khun tn mm khng.
2.3.2. AMOXICILLIN
Cng thc: C16H19N3O5S.3H2O ( ch khc Ampicillin l c nhm OH v tr para ca nhn

phenyl)
Tnh cht:
- Bt kt tinh trng, v ng.
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- m cao v nhit >370C nh bt li n bn
Kim nghim: tng t nh ampicillin
Cng dng:
L dn cht ca Ampicillin, nn tc dng ging Ampicillin, nhng hp thu nhiu hn v t

nng cao hn cc dch tit ng h hp.
Cch dng:
C th kt hp vi acid clavuclanic (cht c ch betalactam) m rng ph khng khun

trn nhng mm khng.
Liu dng thng thng: NL, ung 500mg cch 8h; tim bp 2g/24h.
2. NHM CEPHALOSPRIN
Nm 1948, ln u tin ngi ta trch c cephalosporin C t mi trng nui cy

Cephalosporium acremonium, nhng mi n nm 1961 cu trc ca cephalosporin C mi
c xc nh.
2.1.Cu trc:
R1,R2: thay i, X=S hoc O
iu ch: Tt c cc khng sinh cephalosporin c s dng trong iu tr l nhng phn t

bn tng hp. Chng l dn xut acyl ha ca 7ACA, mang cu trc 3 - cephem hp cht
c tc dng sinh hc.
Trong 7ACA, c 2 carbon bt i u c cu hnh R, hu nh l nguyn nhn lm cho cc

cephalosporin c tnh hu huyn kh mnh.
Ngoi ra cng bn tng hp t penicillin bng cch m vng thiazollidinyl ca penicillin gn

thm mt nhm CH2 v tr 2 sau bin vng penem thnh vng cephem.
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Tnh cht:
Tnh cht vt l:
Dng bt kt tinh th trng hoc c mu nh, khng mi hoc c mi thong nh.
Ph UV: cu trc cephem cho 2 hp th 220nm v 260nm.
Ph IR: nh penicillin.
Tnh cht ha hc:
Tnh khng bn ca vng betalactam.
Tnh acid (do c nhm COOH).
Da vo tnh acid c th nh lng cc cephalosporin bng phng php chun trong mi

trng khan.
nh tnh: o UV, cc phng php sc k.
nh lng: iod, UV, HPLC.
Cng dng:
C ch tc dng: tng t nh penicllin.
Khng thuc: V c bn vi khun khng thuc ging nh penicillin v c khng cho.
Da vo kh nng khng -lactam v ph khng khun, c th chia cc Cephalosporin thnh

4 th h khc nhau sau:
CEPHALOSPRIN TH H I:
c im:
- L cc hp cht khng bn b thy phn bi beta-lactam, gm: Cephalothin, Cephaloridin,

Cephalexin, Cephadroxin.
- Tc dng mnh trn vi khun gram dng, yu vi khun gram m, khng tc dng vowuis trc
khun gram m
Ch nh chung:
- Thay th cc penicillin b khng bi t cu, lin cu tr trng hp bnh do cu khun rut, vim
mng no do mang no cu.
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- Phng nhim khun trong v sau phu thut mt s trng hp.
CEPHALEXIN
Bit dc: Kflex, Keforal
Tnh cht: Bt kt tinh mu trng, mi c trng.
Tan trong nc, d tan trong NaOH long, khng tan trong dung mi hu c.
nh tnh:
- Phn ng mu phn bit: vng nht/ vng m.
- Ph IR hoc sc k, so vi chun.
nh lng: bng HPLC.
Cng dng:
- Bn vi acid, d hp thu khi ung, khng b nh hng bi thc n do c cu trc theo m hnh
ca ampicillin.
- Tc dng ch yu vi lin cu khun beta-lactam tan huyt, t cu, E.coli.
Ch nh v liu dng:
Nhim khun h hp, xng khp, ng niu, da, m mm do vi khun nhy cm.
NL: ung 1g/ln4 ln/24h.
Dng bao ch: vin nang 0,25 v 0,50g
Tc dng khng mong mun: c vi thn, cnh bo c vi gan.
Bo qun: nhit thp.
CEPHALOSPORIN TH H II:
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Gm cc dn cht khng cc beta-lactam nh: Cephamandol, Cefuroxim,...
c im:
Bn vng vi beta-lactam do gc R2= -OCH3, hoc R1= C6H5-CH- c tc dng gim s sinh ra
beta-lactam ca vi khun.
Do cu truc khng gian (=N-O-R), lm cn tr beta-lactam, ng thi lm tng tc dng trn cc vi

khun gram (-).
Ch nh chung: Dng iu tr cc nhim khun nng do t cu, trc khun gram m ym kh,
phng nhim khun mt s trng hp phu thut.
CEFUROXIM NATRI
Bit dc: Kefurox, Zinacef
Cng thc: C16H15N4NaO8S; ptl: 446,37
Tnh cht:
Bt kt tinh mu trng, tan trong nc, rt t tan trong ethanol, thc t khng tan trong ether.
nh tnh:
- Phn ng thuc HCHO/H2SO4 c mu nu nht.
- o []D20 = +59 n +600
- Tp lin quan xc nh bng HPLC.
nh lng: Bng HPLC.
Cng dng: c ph khng khun in hnh ca cephalosporin th h II, t nng cao trong dch
no ty.
Ch nh: Vim mng no, t cu vng, bnh lu, vim ng h hp di,...
CD-LD: Ch yu tim bp, tnh mch; liu 0,75-1,5g/ ln3 ln/ ngy.
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Dng bo ch: L bt pha tim 0,75g; 1g.
CEPHALOSPORIN TH H III:
c im:
Gm cc thuc tc dng mnh hn vi cc chng gram (-), kh nng huyt tn vi cc b phn tt

hn
Khng beta-lactam ca vi khun gram (-), trc khun m xanh.
Ch nh chung:
- Vim mng no do H. Influenzae.
- iu tr nhim khun nng do vi khun ng rut gram (-).
CEFOTAXIM NATRI
Bit dc: Claforan
Cng thc: C16H17N5O7S2
2.1.1. Tnh cht: Bt kt tinh mu trng;
D tan trong nc; tan trong methanol; kh tan trong dung mi hu c.
hp th nh sng
Ha tan 20,0 mg ch phm trong nc v pha long thnh 100,0 ml vi cng dung mi. Pha
long 10,0 ml dung dch thu c thnh 100,0 ml bng nc. Gi tr A(1%, 1 cm) 235 nm
phi t 360 n 390, tnh theo ch phm lm kh.
nh tnh:
Cho phn ng B trong php th Phn ng mu ca cc penicilin v cephalosporin.
Ch phm cho phn ng ca natri.
nh lng: HPLC
19
Cng dng:
- C ph khng khun rng vi nhiu vi khun gram (-), (+) v c tc dng vi cc vi khun
tit ra beta-lactam, R3 khng bn d chuyn thnh -CH2OH t tc dng, t hp thu theo
ng ung dng ng tim.
2.2.4. Ch nh- liu dng:
- Nhim cc vi khun nhy cm: no, nhim khun huyt, vim mng trong tim, vim mng
no.
Tim IV: NL, 1-2g/ ln3-6 ln/24h.
- Lu: Tim IM liu n 1g ( km thuc t).
- Phu thut: Tim 1-2g trc phu.
2.2.5. CC: Mn cm, thiu nng thn, ri lon mu
Bo qun: Trnh m v nh sng.
CEPHALOSPORIN TH H IV:
L thuc tc dng rng hn th h III, tc dng mnh nht trn chng gram (-) v bn vng hn
vi cc beta-lactam nn hiu qu iu tr cao hn vi cc th h trc
Ch phm: Cefepim.
I. NHM KHNG SINH AMINOGLYCOSID (A.G).
Khng sinh u tin l Streptomycin do Wasksman (1944) tm ra, sau l neomycin (1949),
Kanamycin.
L nhm khng sinh quan trng trong vic iu tr cc bnh nhim trng trm trng do vi
khun gram (-).
1. Cu trc: 2 phn
- Phn aglucon hay genin l cc hp cht cha vng cyclitol (poliancol vng).
20
vng cyclitol (poliancol vng)
Sau y l mt s cu trc mt s aglucon chnh ca cc aminoglycosid: Streptidin,

Streptamin, 2-Deoxistreptamin (DOS)
- Phn ng: Gm cc ng c amin hoc khng c amin 6 hoc 5 cnh. Sau y l cu

trc ca mt s thnh phn ng ch yu.
Cu trc cc khng sinh ch yu ca nhm aminoglycozid c th thy trong hnh sau:
Streptomycin Gentamicin
21
Neomycin Amikacin
2. Ngun gc:
T mi trng nui cy Micromonospora (M.); Streptomyces (S.)
Tnh cht l ha:
- Aminosid thn nc do phn ng, tnh base do c nhm amin
-To mui vi acid, vi mui sulfat d tan trong nc.
- Bn pH gn trung tnh.
- To phc mu tm vi ninhydrin
nh lng:HPLC hoc pp vi sinh; pp Complexon
C ch tc dng:
c ch qu trnh tng hp protein
Vi khun khng thuc li bng cch to ra cc enzym ph hy khng sinh lm mt hiu lc ca

khng sinh.
3. Ph tc dng: Ch yu trn vi khun gram (-); m rng sang gram (+).
Mt s c th nhy cm:
+ Streptomycin: Rt nhy cm vi Mycobacterium (lao, phong).
+ Aminosid th 4,6 v th 4,5-deoxy-2 streptamin:Tc dng trn hu ht cc chng vi khun

gy bnh thuc c hai gram VK, tr vi lin cu (km penicillin).
+ Paromomycin: Tc dng trn amip v sn rut (KST).
Hp thu:Khng hp thu qua nim mc ng tiu ha.
Thi tr: 70-90% qua ng thn-nc tiu.
22
c tnh: Hai tc dng bt li ch yu khi dng ko di:
+ Tc ng xu trn thn kinh thnh gic, gy ic kh hi phc.
+ Kch ng ng thn, nng gy hoi t.
4. Tc dng khng mong mun khc: Mn cm thuc, gim th lc...
Dn cht th 4,5-deoxy-2 streptamin c cao nht;
5. Chng ch nh: bng ng tim.
Mt s ch phm
STREPTOMYCIN SULFAT
Cng thc: C21H39N7O12
Ngun gc: T mi trng nui cy Streptomyces griseus (1943).
c im: C 3 trung tm base; 1 nhm aldehyd; v tr 1,3 l guanin.
Tnh cht: Bt mu trng, v ng, ht m mnh.
- D tan trong nc, kh tan trong cc dung mi hu c.
- Dung dch nc khng bn (nhanh b kt ta bi base).
nh tnh:
- un si streptomycin trong NaOH: gii phng NH3 (guanin).
- un soio vi thuc th Fehling: kt ta Cu2O mu nu (tnh kh).
- un si streptomycin trong NaOH cho maltol, to mu tm vi FeCl3.
23
ng dng nh tnh v th tinh khit bng o quang, so vi chun.
- Sc k, so vi chun.
- Hm lng streptomycin B3%
nh lng:
Phng php vi sinh: Hot lc 720 UI/1mg cht th.
Hm lng sulfat: 18,2-21,5% (pp Complexon III, qua BaCl2 chun).
Ch nh: Phi hp iu tr lao
Liu dng: tim bp 1-2g/24h; chia 2 ln. L bt ch pha khi dng.
Tc dng khng mong mun: chung ca aminosid.
Bo qun: Trnh m; nhit thp. Thuc c hn dng.
AMIKACIN SULFAT
Cng thc: C22H43N5O13. 2H2SO4
Ngun gc: bn tng hp t Kanamycin (aminosid tStreptomyces kanamyceticus).
Tnh cht: Bt kt tinh mu trng hoc gn nh trng.
D tan trong nc; khng tan trong alcol, aceton.

Ph tc dng: Nhy cm nht nh Mycobactarium tuberculosis (trc khun lao).
24
Khng hu ht enzym phn hy aminosid ca vi khun.
Tuy nhin, khi dng vn tun th cc nguyn tc s dng aminosid.
Ch nh: Thay th gentamycin, tobramycin tr nhim khun nng. Phi hp tr lao.
Liu dng: tnh theo amikacin base.

1,3mg tng ng 1mg amikacin base
NL, TE c th tim bp 5mg/kg/8h; 3 ln/24h. t 7-10 ngy.
Bo qun: trnh m.
II. KHNG SINH NHM MACROLID
Khng sinh macrolid u tin c pht minh nm 1950 l picromycin, k sau l vo

nm 1952 li tm ra erythomycin mt khng sinh macrolid quen bit nht v quan trng nht
ngy nay. Cc khng sinh loi ny ch yu tc dng trn gram (+).
1. Cu trc chung: Cc macrolid bao gm hai phn: aglucon ( hoc genin) v phn ng.
- Phn aglucon l vng lacton ln gm 12 n 16 nguyn t to thnh vng 12 n 16 cnh,

cc nhm th trn vng c th oxo, hydroxyl, metoxy, ankyl ( ch yu l metyl) formyl-metyl
ni i v ni i lin hp. Nhm th formyl- metyl c trng cho cc macrolit c vng 16
nguyn t (16 cnh), cc nhm hydroxyl trong cc phn t cc hp cht thin nhin thng
c axyl ho ( vi cc nhm axetyl, izopropanoyl, isobutanoyl, n-axyl...).
- Phn ng: gm cc ng trung tnh (glucoz) v ng amin ( aminoglucoz). Cc ng

amin a li tnh baz cho phn t macrolid, cc ng bao gm : desosamin, cladinoz,
Oleandroz, mycaroz, forosamin, mycaminoz.
25
Tnh cht l ha:
- Bt mu trng, v ng
- dng base thn nc, d tan trong dung mi hu cowgiups cho vic chit Macrolid t mi
trng nui cy.
- Dng mui vi cc acid hu c tan trong nc nhng khng bn, d kt ta tr li.
- Hp thu UV nh tnh, nh lng.
- Vng lacton ln d b m vng trong mi trng pH acid hoc kim.
- Phn ng vi thuc th acid HCl, H2SO4 cho phn ng mu (nh tnh).
2. Ph tc dng:
- Cc khng sinh macrolid c ph tc dng tng i hp, nhy cm vi cc vi khun.
- Gram dng: T cu, ph cu, lin cu, trc khun than, bch cu.
- Gram m: Lu cu, mng no cu.
- Trn mt s vi khun khc: Mycoplasma, Rickettsiae, Chlamydiae...
- Khng nhy cm vi phn ln vi khun Gram m, nht l cc vi khun gy bnh ng

rut do khng sinh kh vt qua mng t bo vi khun v ni bo.
3. C ch tc dng:
- Ngn cn sinh tng hp protein
26
- Ngn cn gn kt ca tRNA - ngn cn mc xch peptid.
4. Lin quan cu trc tc dng
- Phn t c tc dng nu cha c hai thnh phn ( aglucon ln thnh phn ng hoc
amino-ng.
- Vi cc macrolid c vng 14 th khi este ho nhm OH, hidrazon ho, oxy ho khng lm
thay i tnh cht tc dng.
- Nhm dimetylamino l iu kin tin quyt cho tc dng khng sinh.
ERYTHROMYCIN
Bit dc: Erymax, Retcin
Cng thc:
Erythromycin Cngthc phn t R1 R2
A C37 H67 NO13 OH CH3
B C37 H67 NO12 H CH3
C C36 H65 NO13 OH H
Dc dng: Hn hp Erythromycin A, B, C (ch yu l A)
Tnh cht:
Bt mu trng hay hi vng hoc tinh th khng mu hay mu hi vng, hi ht m.
27
t tan trong nc ( tan gim i khi nhit tng), d tan trong ethanol 96%, tan trong
methanol.
nh tnh:
- To mu xanh tm vi HCl c
- Sc k: cho 3 thnh phn Erythromycin A, B, C.
nh lng: Pp vi sinh hoc HPLC. Hot lc: 830 UI/mg.
Ch nh:
Nhim khun nhy cm: ni tng, h hp, tuyn tin lit,....
Khp do vi khun ym kh.
Liu dng: NL, ung 1g/ln2-3 ln/24h. TE, uoongs1/2 liu ngi ln.
Mui hoc este tnh theo liu erythromycin.
CC: Thiu nng gan, d ng vi Erythromycin.
Bo qun: ng trong bao b kn.
III. KHNG SINH NHM TETRACYCLIN
y l khng sinh ph rng, c tc dng km khun, t tc dng dit khun.
1. Cu trc chung: u l khng sinh c 4 vng 6 cnh, l dn xut ca octahydronaphtacen.
Cc tetracyclin khc nhau cc nhm th khc nhau t R1...R6
2. Ngun gc: ly t Streptomyces aureofaciens (clotetracyclin, 1947), hoc bn tng hp.
3. c im ha- ha tnh:
28
Tnh cht:
Bt kt tinh mu vng. Tan trong nc, kh tan trong ethanol 96%, thc t khng tan trong
aceton, tan trong dung dch kim hydroxyd v carbonat. Dung dch trong nc b c khi
yn do to thnh kt ta tetracyclin.
- Pht hunh quang vng trong nh sng UV.
- Hp th UV vi nhiu cc i hp th.
- Nhm -OH vng D l phenol, cho phc mu vi FeCl3.
- Tnh kh: B bin mu chm khi tip xc lu vi khng kh, nh sng; kh thuc th
Fehling (cho kt ta Cu2O mu nu).
- Lng tnh: Dimethylamin (4) tnh base; cc nhm -OH tnh acid.
- To phc bn vi cc ion kim loi a tr: Fe3+, Zn2+, Cu2+...
+ Cc chelat to thnh c mu.
+ V tr lin kt vi ion kim loi thay i theo pH.
+ c bit to mu vi ZnCl2, mi tetracyclin cho mu ring: clotetracyclin (),

oxytetracyclin (tm), tetracyclin (vng)...
C th dng phn ng ny phn bit s b cc tetracyclin.
- Trong pH acid xy ra chuyn cu hnh, gi l "epi ha":
Cc nhm -CH3 v -N(CH3)2 (4) lin kt a p, gim hot lc.
Ur, phosphat, citrat, acetat xc tc cho s chuyn ny.
Tuy nhin khi v pH thch hp, cu trc tr v bnh thng, hot tnh khng sinh tr li:
Nh vy cc tetracyclin khng bn trong khng kh, nh sng.
Mt hot tnh mi trng qu kim hoc qu acid.
nh lng: Phng php vi sinh v HPLC.
29
C ch tc dng: c ch qu trnh tng hp protein ca vi khun
Lin quan cu trc v tc dng: cc nhm th v cu hnh phn t nh hng ti hiu lc ca

khng sinh.
Cc yu t lm tng hot tnh:
- Vng A/B cu hnh cis.
- Nhm N(CH3)2 lin kt mi c hot tnh, nu chuyn sang lin kt thi hot lc mt tc
dng 90%.
- Cc nhm th: -Cl, NO2 (7), OH (1) lm tng hot tnh.
Cc yu t lm gim hot tnh:
- Nhm th -Cl (9), -NH2 (7)
- pH>8, vng C ca mt s khng sinh Tetracyclin b ph hy; nhm Cl (7) thc y nhanh s
phn hy ny.
4.Ph tc dng:
Tc dng c hiu trn vi khun gram (-), gram (+)
Tc dng c hiu vi phy khun t
Tc dng vi virus ln: mt ht, ho g.
5.Ch nh:
- Bnh t, bnh do trc khun gram dng.
- St hi qui.
- Vim ph qun
- Vim tuyn tin lit mn tnh ( dng Doxycyclin).
- Bnh do virus.
6. CC:
- Tr em di 8 tui
- Ph n c thai v cho con b.
- Bnh gan, thn mn tnh.
30
7. Tng tc:
- Mt s ion kim loi to chelat vi Tetracyclin, nn khng dng vi cc ch phm c ion kim
loi: thuc khng acid ti d dy, ch phm st, thuc ty mui.
- Khng dng phi hp vi ch phm ca sa.
- Tetracyclin tc dng km khun, khoonng phi hp vi nhm -lactam.
Mt s ch phm:
TETRACYCLIN HYDROCLORID
Cng thc: C22H24N2O8HCl
Ngun gc: T mi trng nui cy Streptomyces viridifaciens.
Tnh cht:
Bt kt tinh muvng. Tan trong nc, khtan trong ethanol 96%, thc t khng tan trong
aceton, tan trong dung dch kim hydroxyd v carbonat.Dung dch trong nc b c khi
yn do to thnh kt ta tetracyclin.
nh tnh:
- Pht hunh quang vng di n UV (tm dung dch ln giy).
- Dung dch cho kt ta vi tt alkaloid (tnh base).
- un si dung dch trong thuc th Fehling: kt ta Cu2O ( nu).
- To mu vi FeCl3 v H2SO4 m c.
- Sc k, so vi chun.
nh lng: pp vi sinh hc hoc HPLC
Ph tc dng v ch nh: nh phn chung.
31
Liu dng: NL, ung 250-500mg/ln/6-8h.
TE8 tui, ung 5-10mg/kg/12h.
Dng bo ch: vin nang; thuc m 1-3% (bi ngoi).
Bo qun: Trnh nh sng.
IV. KHNG SINH NHM AMPHENICOL
Lch s: c Bartez v Ehrlich ng thi phn lp ra t mi trng cy x khun

Venezuelea nm 1948 do loi Streptomyces Venezuela. Sau cht ny c nhiu x khun
khc sn sinh ra. Sn phm hin c trn th trng u do tng hp ha dc.
Hai thuc c s dng:
1. Cu trc: Chloramphenicol (levomycetin) c thc t s dng, m theo cu trc ca n thuc

v nitrophenylalkylamines.
a: p-nitrobenzen
b: 2-aminopropandion-1,3
c: dicloroacetyl
Vi nt v cu trc v ng phn: C 2 C* (C1 & C2) =>22 ng phn. ng phn c hot

tnh l D(-)-treo, D(+)-treo khng c hot tnh. 2 ng phn Erytro c c tnh nn cn loi
b.
32
Thay i nhm th thay i hot tnh khng sinh:
- Thay i lm gim hoc mt hot tnh:
+ Thay p-nitro bng m-, o-nitro; thay -NO2 bng cc nhm th CN, NH2, CONH2...
+ Thay phenyl bng nhn khc; thay i mch thng.
- Thay i cn gi hot tnh:
+ Thay -NO2 bng Me-SO2- (methylsulfonyl), tc dng gn nh cloramphenicol; gim

tc dng ph (Thiamphenicol).
+ Thay -NHCOCHCl2 (dicloacetamid) bng -NHCOCF3.
3. c im l-ha tnh
Gc quay cc ring thay i theo dung mi:
[]D20 = + 19.50(dung dch 5%/ethanol)
- 250 (dung dch 5%/ethylacetat)
Hp th UV:max = 276-278 nm (theo dung mi H2O; H2SO4 0,1N; NaOH 0,1N).
tan: Kh tan trong nc (2,5 mg/ml); tan d trong cc dung mi hu c: methanol,

ethanol, aceton, ethylacetat..
Nhit nng chy: 149-1530C.
4. Ha tnh:
Nhm nitro thm:
Kh ha nhm nitro thnh amin thm bc nht, to mui diazoni v to phm mu azoic vi
naphtol.
33
Kh ha tng phn nhm nitro bi Zn / CaCl2 to N-arylhydroxylaminchuyn thnh dn
cht hydroxamic (khi tc dng vi benzoyl clorid)to phc vi Fe+++ cho mu tm.
un nng vi dung dch NaOH, mu vng xut hin, sau chuyn thnh mu cam.
Do nhm dicloacetyl:
Khi un nng cloramphenicol vi KOH, thu c dung dch cha ion Cl- cho phn ng trm
hin vi AgNO3/HNO3.
Phn ng FUJIWARA ROSS c trng cho nhm gem-diclo: un cch thy

cloramphenicol vi pyridin v NaOH, mu xut hin.
Do nhm alcol bc nht:
Phn ng to este vi cc acid tng ng este palmitat, stearat khng ng, khng tan trong
ncdng cho tr em este succinat, glicinat tan c dng lm thuc tim.
nh lng:
a. Quang ph UV: o max = 278 nm (nc); E1cm1%= 279
b. o nitrit: phn ng kh Ar-NO2 Ar-NH2 bng H (Zn/H+)Ar-NH2 + NaNO2 +

2HCl[Ar-N+N] Cl- + NaCl + 2 H2O
o in th, cp in cc Pt-calomel (hoc Ag/AgCl).
c. Cc phng php khc: Clo ton phn; HPLC
5. Ph tc dng: Nhy cm ch yu VK gram (-).
- Km hm vi khun.
- Dit khun: H. influenzae, Strep. Pneumoniae, N. meningitidis, Salmonella (thng hn).
Ch : Trong iu tr thng hn, liu dng tun theo th t:
Thp > Trung bnh > liu thng thng
Trnh VK cht nhiu cng lc lng ni c t cao gy t vong.
V. KHNG SINH NHM QUINOLON
34
Cu trc chung: l dn cht ca acid 1,4-dihydro-4-oxo-quinolein-3-carboxylic v tr 8 c th
lN
R thng l piperazine.
Lin quan gia cu trc ha hc v tc dng:
Quan trng l cc nhm th gn vo 1, 6, 7, 8.
+ V tr 1: R cho cc cht c tc dng tt l cc gc C2H5; -C3H7, -CH-CH3, -OCH3, c bit
+ V tr 6: Lun mang (6)-F cho cc fluoroquinolon l thuc th h II.
+ V tr 7: L gc piperazinyl-1 th s cho cc cht c tc dng tng ng k v c tc dng

tt trn trc khun m xanh. Cc cht th h II u mang gc ny. thuc mi c gc gm
h hai vng gn vo (7).
+ Hot tnh tng, gim tnh khng ca vi khun gram (+) nu v tr 8 gn F hoc OCH3
Phn loi:
Da trn ph khng khun ca n, quinolon c chia thnh nhiu th h nh:
35
Quinolon th h th nht: L cc cht khng gn F (tr flumequin); bao gm cinoxacin,
flumequine, nalidixic acid, oxlinic, ch c dng trong iu tr ng tit niu (UTI) khng
bin chng. Hin nay vic s dng thuc ny b hn ch do vi khun khng thuc.
Quinolon th h th hai: L cc cht c gn F (gi l fluoroquinolone) v tr s 6; bao gm

ciprofloxacin, enoxacin, fleroxacin, lomefloxacin Tc dng mnh trn c vi khun gram (-)
v (+).
C ch tc dng: c ch ADN-gyrase; l enzym tham gia qu trnh tng hp acid nhn ca vi

khun.
Ch nh iu tr chung:
Nhim khun ng tit niu v vim tuyn tin lit, acid nalixilic, norfloxacin,
ciprofloxacin, ofloxacin, tc dng ging nhau, tng t nh trimethoprim sulfamethoxazol
Bnh ly theo ng tnh dc
Bnh lu: ung liu duy nht ofloxacin hoc ciprofloxacin. Nhuyn h cam: 3 ngy
ciprofloxacin.
Cc vim nhim vng chu hng: ofloxacin phi hp vi khng sinh chng vi khun k kh (
clindamycin, metronidazol)
Nhim khun ng tiu ha: do E.coli, S. typhi, vim phc mc trn bnh nhn phi lm
thm phn nhiu ln.
Mt s ch phm:
ACID NALIDIXIC
Bit dc: Negram, Nelidic
Cng thc: C12H12N2O3
Acid 1- ethyl-7-methyl-1,4-dihydro-4-oxo-1,8-naphtyridin-3-carboxylic
Ngun gc:
36
Acid nalidixic (negram) c pht hin mt cch tnh c vo nm 1962 trong qu trnh iu
ch thuc st rt cloroquin. Sau , ngi ta cng a vo s dng mt s thuc tng t nh
puram, purin, eracine... Hin nay, vic s dng nhng thuc ny b hn ch do vi khun
khng thuc cao.
Tnh cht l ha:
C dng bt tinh th trng hoc vng nht, thc t khng tan trong nc, tan trong methylen
clorid, t tan trong aceton, alcol; tan trong cc dung dch hydroxyd kim long.
T = 230.
Phng php kim nghim dc cht:
nh tnh, nh lng: (tham kho ti liu).
*Tc dng:
Acid nalidixic l thuc khng khun ph rng, tc dng hu ht cc vi khun a kh Gram (-),
E.coli, Proteus, Klebsiella.
Enterobacter thng nhy cm vi thuc.
Nhim khun ng tit niu cp v mn tnh do vi khun ng rut Gram (-).
Cc cu khun ng rut ( Enterococcus) v Staphylococcus saprophyticus, nguyn nhn

ch yu gy vim ng tit niu
* Ch nh iu tr:
Nhim trng ng tiu di cp hay nhim trng ti pht khng bin chng. L trc trng,
tiu chy do nhim trng.
* Chng ch nh:
Nhy cm vi nalidixic acid. Tin cn co git. Tr < 3 thng.
* Liu lng:
- Ngi ln 2 vin x 4 ln/ngy.
- Thiu nin > 30 kg 1 - 2 vin x 4 ln/ngy.
- Tr em 50 mg/kg/ngy. Ung vo bui sng & chiu.
* Bo qun: trong bnh kn nhit 15-30.
37
CIPROFLOXACIN HYDROCLORID
Bit dc: Ciflox, Ciprobay
Cng thc: C17H18FN3O3. HCl.H2O; ptl: 385,82
Dng dng mui d tan trong nc, c th dng pha tim.
Tnh cht:
Dng bt kt tinh mu hi vng, tan trong nc, t tan trong methanol, khng tan trong aceton.
nh lng: bng HPLC.
Cng dng:
- Tc dng hu ht trn vi khun gram (-) gy bnh, k c trc khun m xanh, tc dng vi t cu
vng, t cu gram (-) Chlamydia, lin cu.
- Sinh kh dng ng ung 70-80%.
Ch nh:
Nhim khun ng tit niu v m mm, vim ng h hp, vim khp, tiu chy, mc lu cu,
bnh do Salmonella, chn lc iu tr nhim khun do Campylobacter.
VI. KHNG SINH LINCOSAMIN
c im chung:
- L khng sinh c ngun gc t thin nhin: Lincomycin (1962) t Streptomyces linconenses hoc
bn tng hp: Clidamycin (BTH t lincomycin).
Cu trc chung: l cu trc amid gia aminoacid v ng amin.
38
Aminoacid ng vng c tnh base, to mui vi acid; dng mui vi HCl d tan trong nc, n
nh thng dng dng pha tim.
Nhm OH phn ng amin c th phn ng vi acid to ester.
Tnh cht:
- Dng mui vi HCl rt d tan trong nc.
- Sn phm sau khi thy phn trong dung dch HCl; tc dng vi natrinitroprusiat v Na2CO3,
xut hin mu tm.
nh lng: pp vi sinh vt
Tc dng:
Tng t nh khng sih nhm Macrolid nhng c mt s c im
- Nhy cm vi Clostridium perfringens, nhng khng nhy cm vi vi khun rut Clotridium

dificile.
- Dng thay th khng sinh bera-lactam khi b khng bi Stapylococcus aureus.
LINCOMYCIN HYDROCLORID
Bit dc: Lincosin, Lincogin
Cng thc: C18H34N2O6S.HCl.H20; ptl: 461,01
39
Tnh cht:
Bt kt tinh mu trng, gn ng, d tan trong nc, ethanol, kh tan trong nhiu dung mi hu c.
nh tnh, nh lng: xem phn chung.
Cng dng:
Nhim khun ym kh bng, vng chu, gn khp, thay th khng sinh beta-lactam trong iu
tr vi khun gram (+).
CD-LD:
Ngi ln Tim bp 0,5g/ ln2 ln/ ngy.
Tim tnh mch: pha ch phm vi dung dch NaCl 0,9% hoc dung dch Glucose 5%.
Ngi ln 600mg/12h.
Dng bo ch: Thuc tim ng ng 300mg v 600mg/2ml.
CHNG II. THUC IU TR NM
MC TIU:
1. K tn v trnh by c ch tc dng ca cc nhm thuc dng trong iu tr nm, cc thuc

thng dng trong mi nhm v ch nh dng ca mi thuc.
2. Trnh by c cng thc cu to, cc tnh cht l ha v ng dng cc tnh cht trong
kim nghim cc thuc c hc trong bi.
NI DUNG BI HC
I. I CNG:
40
Bao gm cc bnh nm ca biu b da, lng, tc, mng, nim mc cc hc t nhin
C khong 35 loi nm gy bnh da
Tn bnh thng c t theo v tr gy bnh
Nm gy bnh ngoi da thuc cc ging sau:
+ Microsporum: gy bnh tc, lng, da nhn
+ Epidermophyton: gy bnh da trn, mng
+ Trichophyton: gy bnh tc, da trn, mng
+ Candida: gy bnh da, mng, nim mc.
Nm ni tng: mu, phi,mng tim,....
Hu ht u c din bin mn tnh. (Tr bnh gy ra do Phycomycetes v Nocardia). Mm

bnh k sinh trung trong t, xm nhp vo c th qua ng h hp hoc da b tn thng
(Tr Candida sp)
II. THUC IU TR NM
Da vo cu trc ha hc c th chia thuc iu tr nm thnh cc nhm sau:
1. Khng sinh chng nm:
1.1 Cu to: l cc cht phn t ln thuc nhm khng sinh nm polyen ( l Macrolid vng
ln, 1 lacton vng cha nhiu dy ni i).
Theo kch thc vng chia thng 2 nhm:
+ Polyen 26 cnh: Natamycin.
+ Polyen 38 cnh: Nystatin, Amphotericin B.
Tt c cc khng sinh ny u cha ng deoxyaminohexon lin kt vi glucosid. Ch khc

nhau v s lng dy ni i trong vng lacton.
Ngoi ra, Griseofulvin l khng sinh chng nm c cu trc khung.
1.2 Tc dng chung:
Lin kt vi sterol trn mng t bo nm, lm thay i thm ca mngtiu dit nm.
1.3 Mt s ch phm:
41
GRISEOFULVIN
Bit dc: Fulvicin, Grisactin
Cng thc: C17H17ClO6
Ngun gc: Griseofulvin c sinh tng hp t penicillium griseofulvun
Tnh cht: Bt mn, ng knh ht 4 m, tng kem, khng mi.
Tan t trong nc; tan va trong ethanol, tan trong du m.
nh tnh:
Ha tan 5mg ch phm/1ml H2SO4 m c; thm 5mg kalidicromat (bt mn), trn u:
mu vang.
Hp th UV: MAX 291 v 325nm.
nh lng:o quang ph UV
Tc dng:
Hm nm biu b, hot lc thp trn nm men. Phi dng ko di thi gian tip xc km
hm nm, nn hin ny thuc ny t c s dng do thoiwg gian tc dng lu v c thay
bng thuc khng nm tt hn.
Ch nh:
Griseofulvin c dng iu tr cc bnh nm da, tc v mng, bao gm nm da thn, nm

da chn, nm da i, nm ru, nm da u v nm mng do cc loi Trichophyton,
Microsporum hoc Epidermophyton nhy cm gy ra
Liu dng- cch dng:
NL: 0,5-1g/24h, ung 1 ln hay chia 2 ln
TE: 5-10mg/kg/24h. Nn n nh trc khi ung.
42
t 8 tun (nm tc, da), 6-12 thng (nm mng chn, tay).
Dng bao ch: vin 250-500mg; Hn dch ung 125mg/5ml.
CC: bnh gan, ri lon mu v ty sng.
NYSTATIN
Bit dc: Mycostatin, Mykinac, Nilstat
Cng thc: cu trc polyen macrolid
Ngun gc: T mi trng nui cy Streptomyces noursei.
Tnh cht: Bt mu vng sng, mi c trng. D b bin mu bi nh sng.
Tan t trong nc; tan trong ethanol; khng tan trong ether, cloroform.
Hp th UV: max 291, 305, 319nm.
nh tnh:
Trn 2mg cht th vi 0,1ml HCl m c: mu nu.
Tc dng; dit nhiu loi nm biu b v nm men.
L thuc u tay c s dng tr nm Candida albicans.
Ung khng hp thu; bi khng ngm qua davaf nim mc.
43
Ch nh:
D phng v iu tr nhim nm Candida da v nim mc (ming, ng tiu ha, m o).
Liu dng:
NL: 2-3 vin/ ln3-4 ln/ngy.
TE: 2-8 vin/ngy2-4 ln/ngy. Ty theo tui.
Ung cch xa ba n.
2. Nhm azol: Imidazol v Triazol.
2.1 c im:
Imidazol v triazol u thuc nhm azol chng nm, c cng c ch v cng ph tc dng.
Triazol dng ng ton thn chm b chuyn ho v t tc dng trn tng hp sterol ca
ngi hn l imidazol. V vy, cc dn xut mi u phn ln l t triazol ch khng phi t
imidazol.
Vic tm ra azol (1980) l mt bc tin quan trng trong nghin cu thuc chng nm.
Nhn triazol Nhn imidazol
Cc azol c ch enzym cytochrom P450 ca nm nn lm gim tng hp ergosterol ca vch

t bo nm, km hm s ln ln v pht trin ca nm.
Cu to ha hc, tt c cc hp cht thuc nhm ny, phi cha nhn imidazol hoc 1,2,4-
triazol v c tnh base. Cc hp cht c tnh khng nm mnh phi cha 2 n 3 nhn thm,
trong t nht 1 nhn b th bi halogen ( F,Cl).
2.2. Mt s ch phm:
CLOTRIMAZOL
Bit dc: Lotrimin, Canesten.
Cng thc: C22H17ClN2
44
1-[(2-chlorophenyl)-diphenylmethyl]imidazole
Tnh cht: Bt mu trng vng nht; c th dng v nh hnh.
D tan trong ethanol, cloroform, ethyl acetat; tan va trong nc.
nh tnh:
- 10 mg/3 ml acid sulfuric c: Xut hin mu vng nht.
Thm 10 mg HgO + 20 mg NaN02, trn, yn: vng vng nu.
- Hp th UV: MAX 262 v 265 nm (HC1 0,1 M/methanol).
- Sc k hoc ph IR, so vi chun.
nh lng:
Phng php acid-base/CH3COOH khan; HClO40,1M;
Ph tc dng: Phong b cc loi nm gy bnh:
Hu ht nm men Candida, Malaseezia furfur...
Nm biu b: Epidermophyton, Microsporum, Trichophyton, Tinea sp.
Nhy cm nht nh vi vi khun.
DH: Bi da, nim mc thuc t ngm su.
Ch nh:
- Nhim nm da, mng, hu mn: Bi kem 1%; 2-3 ln/24 h.
- Nm m o: t 1 vin thuc n 500 mg.
45
Dng bo ch: Kem 0,1-1% clotrimazol base; thuc n 500 mg.
Bo qun: Trnh nh sng. nhit 5-25 C.
KETOCONAZOLE
Bit dc: Fungarest; Nizoral
Cng thc:
Tnh cht: Bt kt tinh mu trng, khng mi;
Khng tan trong nc; tan nh trong ethanol v methanol.
Ha tnh: Tnh base; tnh kh.
nh tnh: Ph IR hoc sc k, so vi ketoconazol chun.
nh lng: Acid-base/acid acetic khan; HCIO4 0,1 M; o th.
Tc dng: Dit a nm: da, mng, nim mc; nm men ton thn.
Candida albicans (tiu ha, sinh dc).
Ung hp thu tt; t1/2 8 h. Thi tr ch yu qua ng mt-rut.
C ch tc dng: Thuc phong b sinh tng hp mng t bo nm.
Ch nh- cch dng v liu dng:
- Nm ng h hp, tiu ha. ung cng thc n:
NL: 0,2-0,4 g/ln/24 h; ti a 1 g/24 h. TE: 50-100 mg/ln/24 h.
- Nm mng, da, nim mc: Kem 2%; bi 2-3 ln/ngy.
46
- Nm da u, nm tc: X phng gi u 1-2 %; gi 2 ln/tun.
Dng bo ch: Kem 2%; x phng gi u 1-2%; Vin 200 mg.
Tc dng KMM:
Ung gy nn, tiu chy (cn ung cng thc n).
Ketoconazol cn tr sinh tng hp hormon v thng thn.
Vim gan vng da sau 2 tun ung ketoconazol lin tc.
Triu chng khc: au u, mt ng, st nh, s nh sng...
Chng ch nh: Ph n mang thai; suy gan, mn cm thuc.
Ngi suy gim min dch nhim nm: HIV...
3. ALLYLAMIN V HP CHT LIN QUAN
Cc allylamin c ch vic sinh tng hp ergosterol gian on u tin trong vic tng hp
n, ngha l s epoxy ha squanlen thnh squanlen epoxit. Squalen epoxit sau bin thnh
lansosterol ->14-demethyllansosterol-> ergosterol. Squalen khng b bin i s tch t li v
lm tn hi mng t bo nm. Kt qu, nm b tiu dit.
Khc vi cc thuc khng nm loi azol, cc allylamin khng c ch cc enzym cytochrom

P450, enzym tham gia sinh tng hp hormon steroid v chuyn ha thuc.
NAFTIFIN HYDROCLORID
Bit duc : Naftin
Cng thc: C21H21N.HCl
N-methyl-N-(3-phenyl-2-propenyl)-l-naphtalen methanamin hydroclorid
47
Tnh cht:
Bt kt tinh trng, tan trong cc dung mi phn cc nh ethanol, dicoromethan.
Ha tnh ca naftifin l tnh base ca nhm methylamin, hp th bc x t ngoi ca nhn

thm, ha tnh ca dy ni i v ha tnh ca acid hydroclorid kt hp.
nh, tnh nh lng dng phng php o quang ph hp th t ngoi, ngoi ra c th

nh lng bng phng php o acid trong mi trng khan hoc bng phng php o
kim trong mi trng ethanol.
Cng dng:
iu tr nm da chn, nm da i, nm da thn, nm ru, nm da u, nm da nhiu mu hay

nm mt tri.
Dng dng : Kem 1% ; gel 1%.
CHNG III: THUC CHNG VIRUS
I. I CNG:
Virus l cc tc nhn gy bnh truyn nhim c kch thc nh cha thnh phn acid nucleic
(ADN hoc ARN) c bao bc bn trong mt lp o protein.
Virus khng c cu trc t bo v khng c b my chuyn ha ring. Chng l nhng vt k

sinh bt buc, s dng qu trnh chuyn ha ca t bo vt ch m chng ly nhim nhn
ln.
Virus thng c phn loi thnh virus ADN v virus ARN, ty thuc vo bn cht thnh
phn acid nucleic ca chng. Hai phn nhm ln ny cn c chia thnh khong 6 phn
48
nhm nh phn chia cc virus da trn cc acid nucleic chui n hay chui kp v cch thc
th hin chc nng ca chng trong qu trnh sao chp.
CC VIRUS GY BNH
Virus c th ly nhim hu ht nh tt c cc vi sinh vt sng, v gy bnh ph bin ngi.
1. Virus ADN: thng thm nhp vo nhn t bo vt ch v iu khin qu trnh to ra virus

mi.
Mt s bnh m virus ADN gy ra: poxvirus (u ma), herpesvirus (thy u, zona, herpes
mi v mt, st tuyn), adenovirus (vim hng, vim kt mc), v cc papillomavirus (cc
loi mn cc).
2. Virus ARN: Thng iu khin qu trnh to ra virus mi m khng c s lin quan ca nhn
t bo (ngoi tr virus cm v mt s chng virus khc).
Mt s bnh m virus ARN gy ra: orthomyxovirus (cm), paramyxovirus (si, quai b, bnh
truyn nhim ng h hp), virus rubella (si c),...
Retrovirus ARN (nh HIV, virus gy bnh bch cu t bo T) c cha enzym phin m
ngc xc tc qu trnh to bn sao ADN ca ARN virus. Bn sao ADN ny c tch hp
vo b gen ca t bo vt ch v iu khin qu trnh to ra cc virus mi.
PHNG V IU TR DO VIRUS
Cc bin php phng nga nh: ci thin v sinh, ci thin ngun nc sinh hot, cch ly
bnh nhn, kh trng tit trng dng c v mi trng, dit tc nhn trung gian truyn bnh...
c p dng thch hp trong tng bnh, tng v dch.
Nhng bin php k trn gp phn ng k gii quyt bnh virus, nhng vic thc hin i
hi nhiu cng sc v tin ca. Bin php dit tc nhn trung gian truyn bnh l mt bin
php phng dch hu hiu.
Phng nga v iu tr bng phng php ha hc
Vaccin l nhng yu t gy min dch, chng b mt c lc nhng khng mt tnh khng

nguyn.
Hin ny chng ta sn xut ra mt s vaccin phng bnh do virus gy ra nh: bi lit, si,
di, vim no, u ma, vim gan.
Tuy nhin cn nhiu bnh do virus gy ra cha c vaccin hu hiu. V th ngoi nghin cu
cc vaccin, th chng ta cng cn nghin cu cc thuc c tc dng iu tr bnh do virus.
II. THUC KHNG VIRUS
49
Khc vi vi khun, cc virus k sinh bt buc bn trong t bo sng, chng khng c chuyn
ha v s sao chp ca virus hon ton nm trong t bo ch nn chng khng nhy cm vi
cc khng sinh thng dng. Do mt thuc iu tr c hiu cho virus phi t c
nhng yu cu sau :
-Thuc phi xm nhp c vo trong t bo, c bit l cc t bo b nhim virus.
-Thuc ngn cn qu trnh tng hp ra cc virus nhng khng hoc t nh hng n hot
ng ca t bo .
Hin ny chng ta sn xut c cc thuc iu tr cc bnh cm, bnh do herpes virus,

bnh AIDS hay vim gan B.
Qu trnh nhn ln ca virus trong t bo ch c th chia 5 giai on:
+ Hp th
+ Ci v
+ Tng hp
+ Lp rp
+ Phng thch
Da vo qu trnh nhn ln v pht trin ca virus m thuc tc dng ln tng giai on .
Da vo cu to ha hc c th chia thnh cc nhm thuc sau:
Cc dn cht kiu nucleosid nh: zidovudin, didanosin, stavudin,....
Dn cht ca guanin: acyclovir, ganciclovir,...
Cc dn cht ca adamantan nh: amantadin, rimantadin,...
Mt s cht khc nh: 9-cloro tibo, foscarnet,...
III. MT S THUC:
1. ZIDOVUDINE (AZT)
(Azidothymidin)
1.1. Bit dc: Novo-AZT; Retrovir.
1.2.Cng thc: C10H13N5O4
50
1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione[1]
1.3 Tnh cht: Bt kt tinh mu trng nh nu/ v nh hnh.
Bin mu trong nh sng.
Tan nh trong nc, tan trong alcol.
nh tnh: Ph IR hoc sc k, so vi chun.
nh lng: HPLC, so vi chun.
1.4 Tc dng: Zidovudine c ch s tng hp ADN virus t ARN b gen virus.
Hp thu khi ung
Sinh kh dng: 50-70%; t1/2=1h.
1.5 Ch nh: nhim HIV1 khi lng CD4 c s lng 500/ml.
NL, ung 200-300mg/4h
TE 3 thng tui, ung 150 mg/6h.
Ch : th mu 1-2 ln/thng iu chnh liu.
1.6. TDKMM: C c tnh cao nh gy bun nn, nn, au u mt ng, c bit gy thiu
mu, gim bch cu do c ch ty xng (gp 50% bnh nhn).
khc phc tnh trng , phi lun phin dng mt s thuc cng nhm.
1.7.CC: Dng thuc chng phn bo. Suy ty, thiu mu v suy thn.
Dng bo ch: vin nang 100; 150; 300mg.
2. LAMIVUDINE (3TC)
2.1 Bit dc: Combivir; Lamzidivir.
51
2.2 Cng thc: C8H11N3O3S
4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
2.3.Tnh cht: Lamivudine l mt mu trng n trng tinh th rn vi ha tan khong 70

mg mi ml trong nc 20 C.
2.4. Tc dng: c ch sao chp ngc laoij INTI. Nhy cm HIV, vim gan B.
Hp th nhanh sau khi ung.
Sinh kh dng: 80-87%; t1/2=5-7h.
Thuc vo c bo thai v sa m.
2.5.Ch nh:
- Phi hp vi Zidovudin (AZT) tr HIV.
NL,TE 2 tui; ung lu di
- Vim gan B mn tnh:
NL, ung 100-150mg/24h; cn c s theo di ca thy thuc.
2.6.CC:
Lng bch cu thp; TE 12 tui; ph n mang thai 3 thng u.
Thn trng: Dng thuc Lamzidivir i vi ph n cho con b.
Suy gan, thn, ngi mang thai.
Ch : Trc khi dng Lamivudin tr vim gan B th cn kim tra HIV.
Dng bo ch: vin 100 v 150mg.
52
3. GANCICLOVIR NATRI
3.1.Cng thc:
Natri 2-amino-9-(1,3-dihydroxypropan-2-yloxymethyl)purin-6-olate
3.2.Tnh cht: Bt kt tinh mu trng.
Tan trong nc, dung dch khng bn.
Tc dng: Nh acylclovir
Ung km hp thu; ch truyn. Tc dng trn c ADN t bo vt ch
3.3.Ch nh:
- Nhim Herpes simplex.
- Nhim, phng nhim Cytomegallovirus (EBV) do suy min dch: HIV giai on AIDS; ho
tr liu ung th, ghp c quan,...
Liu dng:
iu tr khi u:
Tim truyn tnh mch chm trong 1 gi, vi tc khng i: 5 mg/kg, 12 gi/ln, dng
trong 14 - 21 ngy, sau iu tr duy tr.
Khng dng ng ung khi iu tr khi u.
iu tr duy tr:
Tim truyn tnh mch chm trong 1 gi: 5 mg/kg/ngy, 1 ln/ngy, dng trong 7 ngy/tun
hoc 6 mg/kg/ngy, dng 5 ngy/tun.
Ung: 1000 mg, 3 ln/ngy, ung vo ba n hoc 500 mg/ln, 6 ln/ngy, cch nhau 3
gi/ln, cng vi thc n
3.4.TDKMM: Ch yu trn h thng mu, gim bch cu; tiu cu; thiu mu.
3.5.CC: Ph n c thai v cho con b.
53
Trnh tip xc vi da, nim mc
Thn trng: Suy thn, ri lon cng thc mu.
Bo qun nhit di 300C.
CHNG IV: THUC TC DNG TRN NG TIU HA
MC TIU
1. Trnh by cc nguyn nhn chnh v cc tc nhn gy lot d dy t trng; t ; k tn cc

nhm thuc dng trong iu tr lot d dy- t trng.
2. Trnh by c ch nh dng ca cc thuc nhun trng v ty, cc thuc iu tri bnh

tiu chy.
NI DUNG BI HC
Trong chng ny, chng ti s trnh by 3 phn:
- Thuc iu tr lot d dy, t trng.
- Thuc nhun trng v ty.
- Thuc iu tr tiu chy.
A. THUC IU TR LOT D DY T TRNG

1. NGUYN NHN BNH SINH VIM LOT D DY T TRNG
D dy hot ng c bnh thng nh s cn bng gia hai qu trnh: Qu trnh hy hoi

nim mc v qu trnh bo v nim mc. Khi c s mt cn bng gia hai qu trnh ny m
trong qu trnh hy hoi chim u th hn dn n lm tn hi hoc lm mt cht liu
nim mc d dy gy vim lot d dy t trng (VLDDTT)
Qu trnh hy hoi nim mc: l qu trnh to bi cc yu t c kh nng n mn, hy hoi

nim mc d dy t trng:
l acid hydrocloric (HCl) v pepsin trong dch v. tiu ha thc n, d dy tit dch v
gm cc men tiu ha (ch yu l pepsin); cc cht v c (HCl, cc ion Na+, Mg2+, K+,
SO42-); cht nhy v yu t ni ti. Song chnh HCl v pepsin li l yu t n mn nim
mc d dy.
l s nhim vi khun Helicobacter pylori (Hp).
54
l nhng cht t ngoi a vo nh: ru, thuc khng vim khng steroid (NSAID),
cc steroid, s cng thng (stress), cng ph giao cmcng lm tng tit dch v.
Qu trnh bo v nim mc: l qu trnh to bi cc yu t c kh nng bo v nim mc d

dy t trng:
l cht nhy v Natri bicarbonat (NaHCO3) c t bo tit nhy nm ri rc trn khp

nim mc d dy tit ra.
l prostaglandin do c th tit ra c tnh bo v nim mc bng cch kch thch t bo

nhy sn sinh ra cht nhy v NaHCO3.
2. CC THUC DNG TRONG IU TR LOT D DY T TRNG
C th chia thuc dng trong iu tr VLDDTT thnh hai nhm ln:
Nhm tc ng vo qu trnh hy hoi tc dng theo c ch lm hn ch qu trnh bi tit

dch v.
Nhm tc ng vo qu trnh bo v tc dng theo c ch tng cng yu t bo v.
2.1. THUC C TC DNG LM GIM YU T GY LOT
2.1.1. Thuc khng acid (Antacid)
Thng l cc hp cht v c c tnh base yu c kh nng trung ha acid dch v nng pH d

dy ln xp x 4. Thuc hin nay ang c dng l nhm hydroxyde (Al(OH)3), magnesi
hydroxyde (Mg(OH)2) hoc cc mui nhm, magnesi dng phosphat, carbonat, trisilicat
NHM HYDROXYD GEL
Cng thc: Al(OH)3
Tnh cht:
L tnh:
Hn hp nht, trng, c th c mt lng nc nh tch ra khi yn; khng c lm

phenolphthalein.
Ha tnh:
Hydroxyd nhm c tnh cht lng tnh, ngha l tan c trong dung dch kim v acid.
- Ly 5 ml ch phm, thm t t acid hydrochloric long, dung dch tr nn trong:
Al(OH)3+ 3HC1 AlCl + 3H2O.
55
- Ly 2 ml ch phm, thm 2 ml dung dch natri hydroxyd 10%. Lc. Hn dch tr nn trong:
Al(OH)3 + NaOH > NaA1O2 + 2H2O
xc nh s c mt ca nhm v hm lng ca n trong nhm hydroxyd gel, tin hnh

nh sau: Ha tan hn dch trong mt lng acid hydrochloric long va . Thm alizarin v
ammoniac, to ta mu khng tan trong acid acetic.
* nh lng:
Bng phng php o complexon, mi trng m acetate pH 4,8. Cho d dung dch chun
EDTA v chun lng d bng dung dch chun km sulfat; ch th dithison
1 ml dung dch EDTA 0,05M tng ng vi 3,9 mg Al(OH)3.
Cng dng:
Ch nh iu tr lot d dy- t trng; chng tng phosphate mu, gim triu chng kh tiu.
Khng dng cho tr nh v c nguy c ng c do nhm; c bit tr em ang b mt nc v

tr b suy thn.
Tc dng ph: Gy to bn v gy thiu phosphat mu.
Liu dng:
Ngi ln: vin nhai 0,5-1,0g; HD: 320-640mg,ngy 4 ln
Tr em: HD 320mg,ngy 3 ln
Bo qun: nhit phng, ng trong chai l kn.
Nhm tc ng vo s bi tit acid dch v
2.1.2 Thuc khng th th H2
Cc thuc tc ng vo receptor H2 ti thnh TB dd, tranh chp vi histamin ngn chn s

bi tit HCl.
Gm cc thuc: Cimetidin; Famotidin; Nizatidin; Ranitidin
Cu trc ha hc chung: c 1 d vng 5 cnh, 1 mch nhnh CH2-S-CH2-CH2-R
Ch nh iu tr chung:
* Phng v iu tr lot d dy, t trng.
* Phng v iu tr chng nng, n kh
56
tiu do tng acid d dy.
* iu tr hi chng Zollinger-Ellison; bnh
tng tit acid.
* iu tr bnh hi lu thc qun d dy.
CIMETIDIN
Bit dc: Peptol; Tagamet
Cng thc:
TN KH: 1-cyano-2-methyl-3- [2 - [(5-methyl-1H-imidazol-4-yl) metylsulfanyl] ethyl]

guanidin
Tnh cht:
L tnh:
Bt kt tinh, trng hoc hu nh trng, mi kh chu. Nng chy khong 139C-144 C;

pKa 6,8. Cimetidin t tan trong nc, tan trong ethanol, kh tan trong chloroform, khng tan
trong ether v dicloromethan; tan trong cc acid v c long. Ha tnh:
Cimetidin c tnh base, hp th mch bc x t ngoi, ng dng cc tnh cht
ny trong kim nghim v pha ch cimetidin.
- Ha cimetidin trong nc to hn dch c. Thm acid hydrochloric, hn dch tr nn trong.

Thm tip acid silicovolframic, to ta.
- nh lng cimetidin bng phng php o acid trong.mi trng khan, dung mi acid
acetic, ch th o in th, dung dch chun acid percloric. Trong phng php nh lng
ny, 1 phn t cimetidin phn ng vi 1 phn t acid percloric (BP 2001).
- Dung dch ch phm 0,001 trong acid sulfuric 0,2M c 1 cc i hp th 218 nm vi

hp th ring 650 n 705.
57
- iu ch dng mui hydroclorid d tan trong nc pha dung dch tim, dung dch ung v
cng l ch phm c dng.
Cng dng:
Ch nh dng nh cc thuc khng th th H2 ni chung.
Liu lng mt ln khong 300 mg; ngy 3 n 4 ln.
Tc dng ph:
- Khc vi cc thuc khng th th H2 khc, cimetidin c ch mnh h enzyme cytochrom

P450 v P448 oxydase gan nn lm chm s chuyn ha ca mt s thuc.
- C tc dng khng androgen nn c th gy chng to v n ng khi dng trn 1 thng.
- C tc dng lm tng kh nng bo v nim mc d dy v lm lnh vt lot do stress.
Dng bo ch:
Vin nn 200,300,400,800mg
Dung dch tim 200mg/ml
Bo qun: ng trong l kn, trnh nh sng.
CC THUC KHNG TH TH H2 CNG NHM
Cng thc cc thuc khng histamin
T/C l, ha, nh tnh, nh lng:
tng t cimetidin.
Cng dng: tng t cimetidin
So snh mt s thuc:
58
Thuc Hot lc Liu Tc dng ph
Cimetidin 1 300mg x3-4 ln/ngy c ch P450 lm gim chuyn ha mt s
thuc; khng androgen
Ranitidin 10 150mg x 2 ln/ngy t tc dng ph hn so vi cimetidin
Famotidin 3 20mg x 2 ln/ngy t tc dng ph hn so vi cimetidin
2.1.3 Thuc c ch bm proton
Gm: omeprazol, lansoprazol, pantoprazol, rabeprazol, esomeprazol. Cc cht ny l dn xut

benzimidazol, s dng dng tin dc khng c hot tnh v tr thnh dng c hot tnh ti
pH = 5.
Bm proton l khu cui cng a acid vo d dy c thc hin bi cc enzym H+ /K+

ATPase (bm proton). Cc thuc c tc dng c ch enzym ny c gi l thuc c ch
bm proton.
Cu trc ha hc chung: u l dn xut benzimidazol, v tr 2 gn nhm th 2- pyridin

methyl sulfanil, chng khc nhau cc nhm th gn vo cc v tr R1, R2,R3, R4.
59
TC chung:
+ Bt kt tinh trng hoc hu nh trng, kh tan/H2O.
+ Nhn thm: Hp th UV (nh tnh, nh lng).
+ Rt d b phn hy trong mi trng acid.
+ Tnh acid: H v tr 1, ch phm dd mui natri.
+ Tnh base: Nhn pyridin, nh tnh, nh lng.
Cng dng chung:
+ iu tr lot d dy, t trng. Ngoi tc dng chng tit acid, cc
hp cht ny cn c tc dng dit H.pylori.
+ Dng trong tt c cc trng hp cn gim tit acid.
OMEPRAZOL
Bit dc: Prilosec; Losec
ptl: 345,4
Tn KH: 5- methoxy-2[[(4-methoxy-3,5-dimethypyridin-2-yl)methyl]sulfinyl]-1H-
benzimidazol
Tnh cht:
L tnh:
Bt kt tinh trng hoc hu nh trng. Nng chy khong 155c vi s phn hy pKa 3,97
(N ca nhn pyridine) v 8,7 (N-H ca nhn benzimidazol). Omeprazol rt kh tan trong
nc, kh tan trong acetonev isopropanol, tan trong dicloromethan, methanol v ethanol.
n nh ca dung dch omeprazol ph thuc pH. Trong mi trng acid, omeprazol nhanh
chng b phn hy ; trong mi trng kim, omeprazol kh vng bn.
60
Ha tnh:
Omeprazol va c tnh acid, va c tnh base., hp th mnh bc x t ngoi. Cc tnh cht

ny c ng dng trong nh tnh, nh lng v trong pha ch omeprazol
- Ha ch phm vo nc to hn dch c. Thm acid hydrochloric. Lc. Hn dch tr nn

trong. Dung dch ny cho phn ng to ta vi mt s thuc th chung ca alcaloid.
- Ha ch phm vo nc to hn dch. Thm dung dch natri hydroxyd 10%. Lc. Hn dch
tr nn trong. Trung ha kim d, dung dch s to mui kt ta hoc c mu vi mt s ion
kim loi nng.
- nh lng omeprazol bng phng php do kim, dung mi ethanol, ch nh o in th.
- Dung dch ch phm 0,002% trong dung dch natri hydroxyd 0,1N bc sng t 230 nm
n 350 nm c hai cc i hp th 276 nm v 305 nm. T s hp th 305 nm so vi
hp th 276 nm bng 1,6 n 1,8.
Cng dng: Ch nh dng nh cc thuc c ch bm proton ni chung.
Liu thng dng 20mg/ln/ngy.
Vin nang gii phng mun; vin nn gii phng mun omeprazol magnesi.
2.1.4. Thuc dit H. Pylory
S dng cc khng sinh nh: Tetracyclin, Amoxicllin, Clarythromycin, Metronidazol (hc trong
bi khng sinh).
2.2. THUC TC DNG LM TNG YU T BO V
Bao gm cc thuc c tc dng kch thch tng sinh lp cht nhy trn nim mc d dy hoc bao
che ch lot. Do vy, thuc c tc dng ngn nga acid tip xuacs vi ch lot, c th t phc
hi ch lot.
Sucralfat (Aluminium sucrose sulfat)
Bit dc: Ulcar, Carafate
Cng thc: C12H6O11[SO3.Al2(OH)5+]8.16H2O
61
TnKH: 3,4,5,6-tetra-(polyhydroxyaluminium)-D-glucopyranosylsulfat-2,3,4,5-(tetra-
(polyhydroxyaluminium)-D-fructofuranosid sulfat
Tnh cht:
Sulcralfat hu nh khng tan trong nc; tan trong cc acid c v cc dung dch hydroxyd
kim loi kim c.
C ch tc dng:
+ Gii phong Al3+
+ Gc sulfat cn li b polime ha to gel nhy dnh, bao bc lot.
+ Lin kt lm mt hot tnh ca pepsin v acid mt
+ Bo v t bo: kch thch nim mc tit prostanglandin, cht nhy
Cng dng:
Kch thch to cht nhy, ng thi hp th pepsin v mui mt lm gim tc dng gy lot.
Phng v iu tr lot dd-tt.
Liu dng: 1g/ln, ngy vi ln
BISMUTH SUBSALICYLAT
Bit dc:Bismatrol, Bismed
Cng thc:C7H5BiO4
62
PTL:362,11
L tnh: Tinh th nh, hnh lng tr, khng tan/nc, ethanol, tan/acid v c (phn hy).
Ha tnh: d b thy phn to acid salicylic v bismuth hydroxyd.
- Thy phn = dd kim, lc. Acid ha dch lc thu c acid salicylic (cho phn ng vi
FeCl3 to mu tm).
- Ta thu c sau khi thy phn v lc (bismuth hydroxyd): ha tan
trong dd HCl. Thm NH3 to ta trng khng tan/ dd kim, tan/ dd
acid.
2NH3
Bi(OH)3 + 3HCl = BiCl3 Bi(OH)2Cl + 2NH4+ + 2Cl-
- nh lng: v c ha, nh lng = pp o Complexon (CT vng xylenol, mu

tmvng).
Tc dng:
- Lm gim nhu ng rut, tng hp thu cht lng v cht in gii rut: iu tr a chy.
- C tc dng khng khun, k c H.pylori; lm gim c
t E.coli.
- Kch thch to cht nhy, natri bicarbonat, to phc hp lycoprotein bao ly ch lot.
Ch nh:
- iu tr lot d dy, t trng.
- iu tr v phng a chy.
B. THUC NHUN TRNG V TY
Thuc nhun trng c dng iu tr to bn do lm gia tng v lm d dng s bi xut

phn bng cch gia tng nhu ng rut v/hoc lm mm cht cha trong rut.
63
Phn loi:
Thuc nhun trng c hc: Methylcellulose (Citrucel), Polycarbophil (Mitrolan, fibrall,

fibercon,), Psyllium (Metamucil, konsyl, fiberal),...
Thuc nhun trng thm thu: Mui magie, Mui natri,...
Thuc nhun trng kch thch: Bisacodyl, Phenolphtalein,...
Thuc nhun trng lm mm phn: Docusat natri (Colace, Doxinate), docusat canxi (Surfak),
docusat kali (Dialose).
Thuc nhun trng lm trn: Du khong
MT S CH PHM:
BISACODYL
Bit dc: Dulcolax; Bisacolax; Bisco-Lax; Deficol; Laxit; Theralax
Cng thc:
4,4'-(2-pyridylmethylen) diphenyl diacetat
iu ch: Ngng t 2-pyridincarboxaldehyd vi phenol, xc tc acid sulfuric to 4,4-(2-

pyridin methylen) diphenol (I). Ester ha (I) bng anydrid acetic v natri acetate khan to
bisacodyl.
Tnh cht:
L tnh:
Bt kt tinh trng hoc hu nh trng; cc ht ch yu c ng knh di 50 m. Nng chy

khong 131C-135C. Bisacodyl rt kh tan trong nc, hi tan trong ethanol, kh tan
trong ether, d tan trong chloroform, tan trong cc dung dch acid v c long.
Ha tnh:
64
Ha tnh ca bisacodyl l tnh base, d b thy phn v hp th bc x t ngoi. Cc tnh cht
ny c dng nh tnh v nh lng bisacodyl.
- un ch phm vi dung dch natri hydroxyd 10%. Chia dung dch lm 3 phn.
+ Phn 1: Acid ha bng dung dch acid hydroloric long. Thm dung dch st (II) clorid.
Dung dch c mu tm.
+ Phn 2: Trung ha bng acid hydrochloric. Thm dung dch bc nitrat trong ammoniac.
un nng. To ta en.
+ Phn 3: Trung ha bng acid sulfuric long. Lc. Thm ethanol v acid sulfuric vo dch
lc. un nng, to ethyl acetate c mi thm.
- Cho mt t ch phm vo nc, lc, khng tan. Thm vi git acid hydrochloric long v
lc, tan hon ton,
- nh lng bng phng php o acid trong mi trng khan, dung mi acid acetic, cht
chun acid percloric, ch th l-naphtolbenzein hoc o in th.
- Dung dch ch phm 0,002% trong dung dch natri hydroxyd 0,1 N trong methanol, vng
sng t 230 nm n 350 nm c mt cc i hp th 248 nm vi hp th ring 632 n 672.
Trong mi trng chloroform, bc sng ny, hp th ring l 148.
Cng dng:
- Kch thch cc ngn dy thn kinh cm gic trn nim mc rut nn lm tng nhu ng rut.
- Dng iu tr to bn, lm sch rut trc khi phu thut, soi hoc chiu chp trc trng.
- Do gy kch ng d dy nn dng bo ch l vin bao tan rut vin t trc trng; dung
dch tho tht.
Liu dng:
Ngi ln ung 10-30 mg. t trc trng 10 mg.
Tr em t 6 tui tr ln 5 mg.
Dng bo ch:
Vin bao tan trong rut 5 mg; thuc n 5 mg hoc lOmg . Dung dch tho tht 5 ml hoc
30 ml cha 10 mg.
Dng vin bao tan rut: Khng dng cho tr em di 6 tui v kh nut c vin.
Khng ung cng sa hoc antacid v s lm thuc tan trong d dy gy kch ng.
65
MAGNESI SULFAT
Cng thc: MgS04.7H20 ptl: 246,47
iu ch:
Trung ha megnetri carbonat hoc magnesi oxyd bng acid sulfuric
MgC03 + H2S04 = MgS04 + C02 +H20
Tnh cht:
Tinh th nh, khng mu, v. mn mt, hi ng; thng hoa trong khng kh m, kh,
100c, mt nm phn t nc. ung dch trong nc c phn ng trung tnh vi giy qu.
Magnesi sulfat d tan trong nc, glycerin; t tan trong ethanol.
nh tnh:
Xc nh ion sulfat bng thuc th bng clorid; ion magnesi bng thuc th diamoni
hydrophosphat.
nh lng:
Bng phng php o complexon, cht chun EDTA, ch th en eriocrom T, dung dch m
ammoniac pH 10.
Cng dng
- Khi ung c tc dng gy nhun trng do hai nguyn nhn: Do khng hp thu khi ung nen
ht nc vo trong long rut cn bng thm thu; kch thch gii phng cholecystokinin-
pancreozymin nn gy tch t cc cht in gii v cht lng vo trong rut non, lm tng th
tch v tng kch thch s vn ng ca rut. Ung 10-15 g ha tan trong mt cc nc.
trinh bun nn khi ung do c v ng, c th pha trong nc chanh ung.
- Khi tim (tnh mch, bp) c tc dng chng co git trong nhim c mu ph n mang
thai; iu tr non; gim magnesi mu.
C. THUC IU TR TIU CHY
a chy l bnh do nhim khun, nhim c, km hp thu, km tiu ha, do khi u, do ri

lon chc nng rut, do d ng...V vy, iu tr a chy, ngoi vic iu tr nguyn nhn
66
gy bnh th phi iu tr c triu chng v b sung nc v cc cht in gii mt. Trong
trng hp a chy nng, i vi tr em v ngi gi, cn truyn dung dch cc cht in gii.
lm ngng a chy, ung Loperamid; Diphenoxylat, Bismuth subsalicylat cng c tc

dng tt.
I. ORS (ORAL REHYDRATION SALTS)
y l hn hp mui v ng dng b li lng nc v cht in gii mt.
1. Tnh cht:
Bt mu trng, d tan trong nc.
Thnh phn ORS lun c NaCl; KCl; Glucose; NaHCO3 (hoc natri citrat) vi s lng
khc nhau ty mi cng thc. Khi dng, ha tan trong mt lng nc ghi trn nhn, ung
mi ln mt t.
nh tnh cc thnh phn:
Xc nh s c mt cc thnh phn trong hn hp:
Ha tan bt vo nc:
- Ion natri: Tc dng vi magnesi uranyl acetate to ta mu vng, hnh mt nhn.
Na++ Mg[(U02)3(CH3COO)8] = NaMg[(U02)3(CH3COO)'9].9H2O
- Ion kali: Tc dng vi nitrat cobalnitrit to ta vng.
2K+ + Na3[Co(N02)6] = K2Na[Co(N02)6]
- Ion clorid: Tc dng vi thuc th bc nitrat to ta trng, ta tan trong dung dch
ammoniac.
Cl- + AgNO3 = AgCl + NO3-
AgCl + 2NH4OH = [Ag(NH3)2]+Cl- + H20
Ion hydrocarbonat: Acid ha dung dch ri un si, kh bay ln lm c nc vi trong.
HC03- + H+ = C02 +H20
- Ion citrate: Tc dng vi calci clorid v un nng to ta trng. Ta tan trong acod
hydrochloric.
- Glucose: Kim ha dung dch ri thm dung dch ng (II) sulfat v un nng, to ta .
67
nh lng:
nh lng ion natri, kali bng phng php o pht x nguyn t; ion clorid bng phng
php o bc; ion citrat bng phng php o acid trong mi trng khn; ion bicarbonate
bng phng php o acid trong mi trng nc; glucose bng phng php o gc quay
cc hoc o iod.
2.Cng dng: Dng b li lng mui v nc mt.
DIPHENOXYLAT HYBROCLORID
1. Bit dc: Lomotil; Lonox; Logen; Lomonate.

2. Cng thc:
ethyl 1-(3-cyano-3,3-diphenylpropyl)-4-phenylpiperidine-4-
carboxylate;hydrochloride
3.Tnh cht:
L tnh:
Bt kt tinh trng hoc hu nh trng, khng mi hoc hu nh khng mi; kh tan trong
nc v isopropanol; hi tan trong ethanol, acetone; d tan trong chloroform v
dicloromethan; thc t khng tan trong ether v hexan.
Nng chy 220C vi s phn hy,
Ha tnh:
Ha tnh ca diphenoxylat hydroclorid l ha tnh ca nhm chc ester, ha tnh nhn

thm, tnh base ca nhn piperidin v ha tnh cu acid hydrochloric kt hp. Cc tnh cht
ny c dng trong nh tnh, nh lng v bo ch diphenoxylat.
un ch phm vi dd NaOH3O% v iod to iodoform (CHI3) mi
c bit.
Tc dng vi TT alcaloid cho ta hoc mu c trng.
68
Tc dng vi dd AgNO3 to ta trng.
nh lng = pp o acid/ mt khan hoc pp o quang.
4.Cng dng
Lm gim s vn ng ca rut; iu tr a chy cp v mn tnh.
Liu dng:
Ngi ln v tr em trn 12 tui: ung lc u 5 mg (2 vin) hoc 10 ml dung dch (2,5 mg/5
ml); ngy 4 ln.
iu tr duy tr, ngy ung mt ln 5 mg.
Dng bo ch:
Vin nn 2,5 mg cha thm 0,025 mg astropin sulfat hoc dung dch ung, trong 5 ml dung
dch cha 2,5 mg diphenoxylat v 0,025 mg atropine sulfat.
Khng dng cho tr em di 12 tui do nguy c suy h hp.
LOPERAMID HYDROCLORID
Thuc khng nhu ng rut
1. Bit dc: Imodium; Kaopectate II; Loperacap
2. Cng thc:
P.t.l.: 513,5
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-
diphenylbutanamide;hydrochloride
3.Tnh cht:
L tnh:
69
Bt kt tinh rt nh hoc v nh hnh, mu trng hoc trng hi vng. Nng chy khong
225c vi s phn hy.
Loperamid hydrochloric t tan trong nc, tan trong ethanol, d tan trong methanol.
Ha tnh:
Ha tnh ca loperamid l ha tnh ca nhm chc amid, tnh base ca nhn piperidinm ha
tnh ca nhn thm v ha tnh ca acid hydrochloric kt hp. ng dng cc tnh cht ny
nh tnh, nh lng v pha ch loperamid.
un ch phm vi dd kim gii phng dimethylamin lm xanh giy qu v c mi c bit.
Tc dng vi TT alcaloid cho ta hoc mu c trng.
Tc dng vi dd AgNO3 to ta trng.
nh lng = pp o acid/ mt khan hoc pp o quang. Cng c th nh lng = pp o

kim/dung mi ethanol, dd chun NaOH 0,1N, ch th o th.
4. Tc dng
Lm chm nhu ng rut nn lm chm cc cht di chuyn trong rut v vy ko di thi gian
hp thu nc v cc cht in gii nn tng c ca khi phn. c ch nhu ng rut
nhanh chng (1 gi) v ko di.
Ch nh
Tiu chy cp khng chuyn bit, tiu chy mn tnh ngi ln.
Liu mi ln 2 n 4 mg; ngy khng qu 16 mg.
5.Tc dng ph:
Do thuc lm gim nhu ng ca rut nn lm ng nc trong rut v do lm trm

trng thm s mt nc v cc cht in gii, c bit tr em. Mt khc, loperamid cn c
tc dng c ch thn kinh trung ng kiu opioid. V vy, thn trng khi dng loperamid cho
tr em v ngi gi.
Dng bo ch: Vin nn 2 mg, vin nang 2 mg; dung dch ung 1 mg/5 ml.
70
CHNG V: HORMON V CC HP CHT TNG T
MC TIU
1. V c khung hoc cng thc chung ca mi nhm thuc (nu c); cng thc cu to ca
cc cht trong chng.
2. Trnh by c cc tnh cht l ha v cc php th nh tnh, nh lng; tc dng v

cng dng ca moi thuc c th.
NI DUNG BI HC:
I. I CNG
1. Khi nim:
Hormon l nhng cht ha hc do mt nhm t bo hoc mt tuyn ni tit bi tit vo mu

ri c mu a n cc t bo hoc cc m khc trong c th v gy ra cc tc dng sinh l
ti .
2. Phn loi:
Da vo bn cht ha hc c 3 loi hormon c bn:
Hormon steroid: l nhng hormon c cu trc ho hc ging cholesterol v hu ht c

tng hp t cholesterol nh hormon v thng thn, tinh hon, bung trng v rau thai.
Hormon dn xut t acid amin l tyrosine: hormon ca tuyn gip (T3, T4), hormon ca ty
thng thn (adrenalin v noradrenalin).
Hormon peptid: a s nhng hormon cn li thuc nhm ny nh hormon vng di i,

hormon tin yn, hormon tuyn cn gip, hormon tu ni tit.
Ngoi ra cn c hormon dng eicosanoid: cc hormon a phng, mi c khm ph gn

y, nh prostaglandin, leucotrien.
II. HORMON NHM STEROID

1. HORMON SINH DC NAM
Cc cht ny c gi l androgen. Hai hormon t nhin chnh l testosteron v 5-

hydrotestosteron. Testosteron c hot tnh mnh c.
Ch phm:
71
TESTOSTERON PROPIONAT
Bit dc : Testolin, Androfort, Agovirin
Cng thc : C22H32O3; pttl: 344,5
Tn khoa hc : 3 -on-17 p-hydroxyl-4-androsten propionate
Tnh cht:
Bt kt tinh mu trng, khng mi, bn vwngnx khng kh, khng tan trong nc; tan trong
du,cn; d tan trong cloroform, benzen.
Nhit nng chy 119-1230C.
nh tnh:
- Phn ng vi H3PO4/EtOH (2/1), un 5, lnh, +HOOC-CHO (acid glyoxylic) tm,

hunh quang .
- Phn ng Zimmerman (mu tm)
- To hydrazon vi phenylhydrazin hoc 2,4-dinitrophenylhydrazin.
- Phn propionat: dch thy phn tc dng vi hydroxylamin to natri propionohydroxamat;

thm FeCl3 c mu gch:
- Ph IR; Gc quay cc ring = 83-90o
- UV (+): TLC (th tp), T, lng
nh lng: php o ph UV
Cng dng:
Ung khng c tc dng do b ph hy gan.Thng dng tim bp, tc dng ko di (24 h)
72
- iu tr thay th thiu nng sinh dc nam, ri lon chc nng sinh dc, lit dng
- Cho n: iu tr ung th v, d con, bung trng, ri lon kinh nguyt
- Tc dng tng dng (tng ng ha protid).
Dng thuc: Dung dch tim trong du: 25mg hoc 50mg/ml
METHYLTESTOSTERON
Cng thc:
Tnh cht l, ha-T/L
- Phn ng Zimmerman
- Phn ng to hydrazon
- Phn ng oxi ha
- Ph IR c trng
- Gc quay cc ring
- UV(+): TLC, HPLC (nh tnh, th tinh khit, nh lng)
Cng dng: bn gan so vi testosteron (c th ung)
- Tng t testosteron propionat cho nam gii.
- Phi hp estrogen iu tr ri lon kinh nguyt, a kinh, cc triu chng tin mn kinh,
long xng sau mn kinh.
73
2. HORMON SINH DC N
2.1.Cc Estrogen:
Ngun gc: nhau thai, bung trng tit ra
Cc ch phm:
Cc estrogen t nhin: Estron, Estradiol, Estriol, este: Estropipat, Estradiol monbenzoat.
Cc estrogen bn tng hp:Ethinylestradiol.
ESTRADIOL MONOBENZOAT
Bit dc: Benzo - gynoestryl, Progynon-depot
Cng thc: C25H28O5; ptl: 376,5
Tn khoa hc: 3,17-dihydroxy-1,3,5-(10)-estratrien-3-benzoat
* Tnh cht:
Bt kt tinh trng, kh tan/ nc (tr estropiat), tan nhiu/dm hu c.
C nhiu C bt i l 1 pp th t,l, th tinh khit.
C ni i lin hp in thp th UVTLC, o UV, HPLC t,l.
Hp th as t ngoi: ph IR c trng.
C nhm OH phenol: p vi FeCl3: xanh.
P oxy ha bng H2SO4 hoc hh thuc th c trng cho mu hunh quang c trng.
Cng dng:
Dng este (3)-benzoat bn (kha -OH phenol), c dc ng hc thch hp, gii phng dn
estradiol trong c th.
74
Estradiol monbenzoat c hiu lc iu tr hn estron hoc estropipat (l mui ca este sulfat
ca estron vi piperazin). Do bn v mt s dn cht chuyn ha ca estradiol vn c tc
dng nn estradiol monobenzoat c tc dng ko di (vi ngy).
Ch nh:
Dng iu tr thay th sau mn kinh, thiu nng bung trng, sau ct bung
trng. Thay cho estron hoc estropipat trong hu ht cc trng hp.
Dng di dng tim bp pha trong ethyloleat hoc trong ester thch hp hoc trong du .
Thng nng 0,1%, ng ng lmg hoc 5mg.
Liu dng: Ty theo trng hp c th, v d
Cc ri lon sau mn kinh, chng long xng sau mn kinh.... th dng 5mg/ln/3-4 tun .
Dng di dng vin (thng vin 0, lg mg) ung vi liu 0,3-0,6mg/24 gi, ty trng
hp.
2.2.Cc estrogen bn tng hp
c im chung: Bn hn i vi tc dng chuyn ha, tc dng mnh hn v thng ko di

hn, nhng tc dng khng mong mun thng hay gp hn v mnh hn.
ETHINYLESTRADIOL
Bit dc: Estinyl; Progynon; Estigyn
Cng thc: C20H24O2; pttl: 296,41.
Tn khoa hc: 17a-ethynylestradiol
iu ch: Bn tng hp theo phn ng
75
Estron Ethinylestradiol
Tnh cht
Ch phm dng bt tinh th c mu t trng n kem. Khng tan trong nc , tan trong
alcol,ether, cloroform , trong dung dch hydroxyd kim loi kim.
nh tnh
Phn ng mu vi H2SO4 (lg ch phm/ 1 ml EESO4 c): cho mu cam, soi di n

UV 365 c hunh quang xanh , pha long bng nc (thm 10ml) c mu tm v c ta mu
tm.
nh lng:
Da vo phn ng to mui bc vi AgNO3, gii phng HNO3, nh lng HNO3 bng

NaOH 0,1N, xc nh im kt thc bng in th k.
Cng dng
Ngn cn tc dng ca enzim chuyn ha gan ln phn t nn gi c tc dng mnh theo

ng ung .
Khi tim th tc dng ca n tng ng vi estradiol nhng nu dng theo ng ung

th tc dng ca ethinylestradiol mnh gp 15-20 ln estradiol.
Ethinylestradiol c tc dng chng rng non liu tng i thp, v phi hp vi

progestin chng th thai dng theo ng ung.
Ch nh:
iu tr thay th sau mn kinh: 0,01-0,02 mg/24 gi (cng vi progestin). Vi ch nh ny

th estrogen t nhin c a chung hn.
N thiu nng sinh dc, ung th tuyn tin lit, ung th v ( ph n mn kinh) 0,l-lg/ln-3
ln X 24 gi.
76
Trong thuc trnh thai phi hp: ethinylestradiol- levonorgestrel.
Dng thuc:
Vin 0,02mg, 0,05mg (dng iu tr ung th); cc vin trn ba pha cha ethinylestradiol.
1.2 Cc progestin
Hormon t nhin l progesteron, do do hong th tit ra v c nhiu trong thi k thai nghn do
nhau thai tit ra. Cc cht bn tng hp bn hn c tc dng mnh hn, ko di v dng c theo
ng ung.
V cu trc ha hc chng c khung pregnan.
PROGESTERON
Bit dc: Lutein
Cng thc :
Tn khoa hc : Pregn-4-ene-3,20-dione
Tnh cht:
Ch phm c dng bt kt tinh trng, khng tan trong nc, tan trong du,alcol, ether,
cloroform. Chy 126-13lC.
nh tnh:
Phn ng Zimmerman ca chc ceton: cho mu tm Phn ng to hydrazon
Phn ng to dioxim progesteron, kt ta, ly ta kt tinh li trong methanol, o chy

c 134C -137C.
o ph UV
77
o ph IR
nh lng:
Cn ta hoc o quang
HPLC l phng php ph bin.
Cng dng:
L hormon chnh ca c th. Dng iu tr thay th cho nhng trng hp : thiu nng vt
th vng, ri lon kinh nguyt, v kinh, au khi hnh kinh, chy mu t cung, cc c quan
sinh dc km pht trin, km hot ng, v sinh, vi liu trung bnh 5-10mg/24 gi, phi hp
vi estrogen.
c bit phng sy thai: tim bp 25g/24 gi, lin tc hoc 25-100mg (nu cn c th
tng)/ln X 2 ln/tun.
Ung th ni mc t cung : dng liu cao.
Dng thuc :
Dung dch tim trong du 5mg/ml, 25mg/ml, 10mg/ml, 50mg/ml, hn dch tim trong nc
10mg/2ml, cng c dng vin ung hoc ngm 50mg.
3. HORMON V THNG THN
Phn loi
Tuyn thng thn nm trn thn v chia lm 2 phn l phn li (sinh ra adrenalin,
noradrenalin) v phn v sinh ra cc hormon steroid. Theo tc dng sinh l, c chia thnh 2
nhm chnh:
3.1. Cc glucocorticoid :
Tc dng-ch nh: Ngoi tc dng thay th hormon, 3 tc dng chnh c ng dng trong iu
tr l:
- Chng vim.
- Chng d ng.
- c ch min dch.
Mt s ch phm
78
HYDROCORTISON ACETAT
Bit dc : Cortef, Colifoam...
Tnh cht
Dng bt tinh th trng hoc hu nh trng. Thc t khng tan trong nc, kh tan trong
ethanol v methylen clorid.
nh tnh:
o ph IR, so vi ph chun
Phn ng mu vi H2SO4 c trong ethanol (tt) cho mu nu m dn v hunh quang

xanh, sau khi thm nc mu nht dn v mt hunh quang.
Th gc acety: thy phn bng H3PO4.
Cng dng
Hydrocortison c hp thu tt theo ng ung, nng mu cc i sau khong 1 gi.
Khi tim bp , hydrocortison v cc ester tan trong lipid ca n khuch tn chm.

Hydrocortison v ester ca n c hp thu qua da nht l cc vng da mng v sch.
Ch nh, cch dng:
Phi hp vi udrocortison acetat iu tr thiu nng thng thn, suy thng thn ( bnh
Addison) hoc sau cn ct thng thn. Thiu nng ung 20mg vo bui sng v 10mg vo
bui chiu ti.
Tnh trng d ng mnh nh hen nng v c tnh , sc liu: 100-500mg/ lnx 3-4 ln/24 gi.
Chun b cho phu thut ngi thiu nng thng thn : lOOmg/ln X 3-4 ln/ 24 gi.
Gim dn sau 5 ngy ti liu duy tr : 20-30mg/24 gi.
Chng vim
Dng dng:
79
Vin nn 5,10,20mg, hn dch l 5ml cha 125 mg hydrocortison acetat, dung dch, dng ng
25mg, l00mg.
DEXAMETHASON
Bit dc: Dexadron, Dexaxon, Decacort..
Cng thc: C22H29FO5; ptl: 392,5
Tnh cht:
Bt trng, khng mi. Tan trong aceton, ethanol. Dng dng photphas hoc acetat
Dng bo ch: Vin nn mu trng ng hay mu vng, hm lng 500 mg nh tnh: Nghin
mn 2 vin, ly bt vin chia lm 2 phn
1. Phn ng vi thuc th fehling:
Cho 1 phn bt vin vo ng nghim. Thm lml ethanol v 5 git tt fehling. un nng , xut
hin ta mu vng cam
2. Phn ng vi formaldehyd:
Cho 1 phn bt vin vo ng nghim. Thm lml formaldehyd/H2S04 c. Lc k: xut hin

mu vng. un cch thy 1 pht: chuyn sang mu nu ti
nh lng:
o 238,5 nm t dung dch c nng chnh xc khong 0,001% trong ethanol 96%.
Cng dng:
- Dexamethason c tc dng glucocorticoid (chng vim) gp gn 7 ln prednisolon v 25 ln

cortison.
80
- Dexamethason khng c hot tnh chuyn ha mui khong ( khng gi Na v nc), dng
thun li cho cc trng hp nh thiu nng thn, tim, cao huyt p... Khi ung d c hp
thu, thi gian bn hy sinh hc ( huyt tong) khong 36-54 gi. Vy dexamethason c tc
dng ko di.
- Vi hot tnh mnh, ko di, khng gi mui-nc, dexamethason l mt thuc chng vim,
chng d ng dng rng ri, ngoi ra c nhng ch nh cn thit khc ca mt glucocorticoid
bn tng hp.
- Dexamethason c dng di dng cc ester acetat, isonicotinat, natri phosphat, trong

dexamethason acetat v dexamethason natri phosphat ph bin hn c.
Cch dng:
- Chng vim, chng d ng, chn on hi chng Cushing ( da trn cc tc dng chn v
thng thn), dng ng ung (dng alcol) vin nn ( 0,5; 0,75; 4;
5mg/vin): 0,5-10mg/24 gi/ ln hoc chia vi ln.
- Cc trng hp bnh khng nng hoc khng khn cp dng hn hp tim.
- Cc trng hp bnh nng hoc cn phi thuyn gim nhanh nh u no, ph no, sc dng
dung dch tim.
- Cha hen ph qun (ester natri phosphat): xt vo hng v ht vo.
- Vim mi d ng hoc cc dng vim mi: phun dung dch ( 0,04%, 0,1%)
- Dng ngoi dng kem, m (0,1 %)
- Dung dch nh mt hoc m tra mt (0,05-0,1%).
PREDNISOLON
Bit dc: Prednisol, Hydrocortancyl.
Cng thc:
81
Tnh cht:
Bt kt tinh trng, dng khan d ht m, rt kh tan trong nc, tan trong ethanol, methanol, hi
tan trong aceton. Nhit nng chy so vi s phn hy l 227-2300C.
nh tnh:
- Dng ph IR, TLC
- Phn ng mu vi H2SO4 c: sau 5 pht c mu m v hunh quang nu di nh n

UV365, pha long mu nht dn c hunh quang vng di n UV365, c ta bng mu xm.
nh lng:
o UV max= 243,5nm, o nng chnh xc khong 0,002% trong ethanol 960.
Cng dng: ch nh nh phn chung.
3.2. Cc mineralocorticoid:
Tc dng lm tng ti hp thu Na+, tng thi tr K+ c th dn n: tng th dch, tng huyt
p v mt kim.
cng l tc dng ph khi dng iu tr thay th thiu nng hoc suy thng thn.
DESOXYCORTICOSTERON ACETAT
Bit dc: Cortin, Deoxycorton
Tnh cht:
82
Bt kt tnh mu trng hoc kem nht, thc t khng tan trong nc, tan trong acol v
du m.
nh tnh:
- o ph UV.
- o mu.
Cng dng: Tc dng glucocorticoid khng ng k, phi hp vi hydrocorticoid hoc
cortison iu tr thiu nng, suy thng thn.
Liu dng: IM 5mg/ln3 ln/tun.
II. HORMON C CU TRC PEPTID
L hormon ca tuyn yn ( oxytocin), hormon tuyn ty (insulin, glucagon,..).
OXYTOCIN
Bit dc: Pitocin, Syntocinon
Cng thc :
Oxytocin l mt nonapepid vng, c iu ch bng phong php tng hp ha hc hoc

phn lp t thy sau tuyn yn ca sc vt khe mnh.
Tnh cht:
Bt kt tinh trng hoc hu nh trng, d ht m, rt d tan trong nc, trong acid acetic
long v ethanol. nh tnh v nh lng oxytocin, dng phng php sc k lng hiu
nng cao vi detector 220nm.
Cng dng:
Nh tn gi, oxytocin c tc dng tr oxytocic. Oxytocin c tc dng kch thch c trn

t cung v tuyn v ; c tc dng lm gin c trn thnh mch mu khi dng liu cao.
Ch nh dng thc ; gy sy thai, iu tr chy mu sau khi sinh.
83
Dng thuc tim 10 n v/ml. Ngoi ra, do c tc dng kch thch c trn tuyn v gip cho
vic tit sa c d dng (khng c tc dng to sa) nn cn c dng phun vo 2 l
mi trc khi cho b. Dng dung dch bm vo mi 40n v/ml. lg oxytocin tng ng
vi 600 n v quc t.
INSULIN
Insulin c tng hp cc t bo p ca tuyn ty t preproinsulin, mt polypeptid mch

n gm 110 acid amin. Sau , n b tch mt 24 acid amin cui cng to thnh
proinsulin. Lc , phn t cun li v to thnh ba cu ni disulfid. Di tc dng ca
enzim endopeptidase, proinsulin bin thnh insulin cha 51 acid amin, sp xp thnh 2 chui
A v B, trong chui B c 1 cu ni disufid ni chui, gia 2 chui c 2 cu ni disulfid; phn
t lng khong 5800.
Tnh cht:
Bt trng hoc hu nh trng, thc t khng tan trong nc, trong ethanol v ether. Insulin
tan trong cc acid v c long v trong cc dung dch long ca cc hydroxyd kim loi kim
vi s phn hy.
nh tnh v nh ing bng phng php sc k lng hiu nng cao vi detector V 214
nm.
Cng dng:
Insulin c tc dng iu ha s d tr v chuyn ha ca hydrat cacbon, protein v cc cht

bo. Tc dng ny ch yu xy ra gan, cc c v cc t chc bo.
Insulin lm tng vic s dng cc cht bo, protein v hydrat cacbon cc m, kch thch
vic tng hp protein v cc acid bo t do, c ch vic gii phng cc acid bo t do ra khi
m m.
Insulin lm tng vic vn chuyn glucose hot ng vo c v mng t bo cht bo, lm tng
vic bin glucose v acid bo t do trong t bo thnh cc dng d tr thch hp (glycogen v
triglycerid tng ng).
gan, insulin lm tng vic bin i glucose gan thnh glycogen v lm gim s cung cp
glucose t gan.
Ch nh:
iu tr bnh i tho ng v cc bin chng ca n nh i tho ng typ 1, i tho

ng typ 2 (khi cc iu tr khc khng c hiu qu), v iu tr i tho ng khi ph n
mang thai.
84
Dng bo ch: Thuc tim, hm lng 100 n v hoc 500 n v/ml.
III. HORMON C CU TRC AMINOACID (HORMON NHM AMIN).
1. Hormon tuyn gip
Tuyn gip tit ra 2 hormon chnh l thyroxin hay cn gi l levothyroxin (trong phn t c
gn 4 nguyn t iod), v triodothyronin cn gi l liothyronin (trong phn t gn 3 nguyn t
iod). Do cu trc ha hc ging nhau nn tnh cht l ha hc ging nhau, v tc dng,
liothyronin tc dng nhanh hn, hp thu qua ng tiu ha tt hn v hot lc mnh hn
levothyroxin.
NATRI LEVOTHYROXIN
Bit dc : Eltroxin, Levo-T, Levothroid, Levoxyt, Synthroid
Cng thc: C15H10I4NaO4; ptl: 799,0
Hin nay, Levothyrixin c iu ch bng phng php tng hp ha hc.
Tnh cht:
L tnh:
Bt hu nh trng hoc vng hi nu hoc bt kt tinh nh, khng mi, khng v, kh tan
trong nc v ethanol, thc t khng tan trn ether. Natri levothyroxin tan trong dung dch
long ca cc hydroxyd kim loi kim.
Gc quay cc ring: -5 n -6
Ha tnh: ha tnh ca levothyroxin l ha tnh ca mt amino acid, ha tnh ca hp cht iod

hu c, ha tnh ca nhm -OH phenol v ha tnh ca nhn thm.
Cho ch phm vo nc, lc, khng tan. Thm dung dch natri hydroxyd long, lc, tan hon
ton.
85
Cho ch phm vo chn s, thm acid sulfuric ri un nh, hi mu tm bc ln. Ch phm
sau khi v c ha cho phn ng c trng ca ion natri.
Tc dng vi thuc th ninhydrin to mu tm.
nh tnh:
Bng phng php o ph hp th t ngoi trc tip hoc sau khi tch bng sc k lng hiu
nng cao.
Cc ch phm levothyroxin phi bo qun trnh nh sng.
Cng dng:
Ch nh dng iu tr thiu nng tuyn gip. Ngoi ra, levothyroxin cn c dng

phng v iu tr bu gip, phng v iu tr carcinom tuyn gip.
Dng bo ch: Vin nn, dung dich tim hoc bt pha tim.
2.Cc thuc khng gip trng
Cc cht ny thuc dn cht ng vng ca thioure nh dn cht 2- thioimidazol v cc dn

cht 2- thiouracil. C ch tc dng ca cc hp cht ny ging nhau, c th chng ngn cn
vic gn iod vo cc cht tin thn to ra levothyroxin hoc liothyronin. Cu trc ha hc
chung ca chng nh sau:
Thioure 2- thioimidazol 2- thiouracil
PROPYLTHIOURACIL
Bit dc: Propyl-Thiracyl
Cng thc: C7H10N2OS; ptl: 170,2
86
Tnh cht
L tnh:
Bt kt tinh hoc tinh th trng hoc hu nh trng, v ng, rt kh tan trong nc, kh tan
trong ether; hi tan trong ethanol, tan trong c dung dch hydroxyt kim. im chy 217c
n 221C.
Ha tnh:
Ha tnh ca propylthiouracil l tnh acid, hp th bc x t ngoi.
xc nh lu hunh trong ch phm, em voomcow ha nc brom v un si ri xc

nh ion sulfat to thnh.
Ch phm kh tan trong nc, thm dung dich NaOH long, to thnh dung dch.
nh lng bng phng php o kim, dung mi l nc, ch th o in th.
nh tnh bng sc k lp mng, cht hp ph silicagel hoc bng so snh ph hng ngoi vi
cht chun.
Di dng mui vi kim loi kim , ch phm to ta hoc mu vi cc ion kim loi nng
hoc kim loi mu.
Cng dng:
Ch nh dng iu tr u nng tuyn gip. Do phn b vo sa m v vo nhau thai km

hn methimazol nn thun tin dng vi ph n c thai v ph n ang trong thi k cho con
b.
Dng bo ch: Vin nn 50mg, 100mg.
87
CHNG VI: THUC TC DNG TI CC C QUAN H HP
MC TIU HC TP
Sau khi hc xong bi ny, sinh vin c th:
1- Trnh by c cc nhm thuc iu tr ho, cc uru khi s dng thuc ho; cc nhm thuc
iu tr hen.
2- Trnh by c cng thc cu to, tnh cht, nh tnh, nh lng, cng dng, liu dng ca
mt s thuc iu tr ho, hen, long m.
NI DUNG BI HC
I. I CNG
Ho l phn x rt phc tp c tnh bo v nhm loi tr cc cht nhy, cht kch thch ra khi
ng h hp.
Ho cn l mt trong nhng triu chng ca mt s bnh vim nhim ng h hp nh
nhim lnh, vim hng, vim ph qun, vim phi...
Cc thuc ho tc ng theo c ch trung ng hay ngoi bin:
- Thuc tc ng trung ng: Do c ch trung tm ho lm tng ngng ho. Thuc nhm
ny c cc dn xut opioid (codein, dextromethophan, levopropoxyphen, noscapin ) v nhiu
cht khc.
- Thuc tc ng ngoi bin lm gim nhy cm ca receptor vi cc cht kch thch:
thng l cc cht bay hi nh menthol, camphor...
Cc lu khi s dng thuc ho:
- Thuc ho ch l thuc iu tr triu chng, do khng nn dng thuc ho mt cch ba bi
m cn phi bit nguyn nhn gy ho c cch x tr thch hp.
- Khng dng thuc ho qu lu (thng ch dng trong vi ngy)
- Trong iu tr ho thng kt hp vi cc thuc long m.
Thuc long m
Tc dng: Tng tit dch, gim qunh dch tit ph qun lm long dch nhy kh qunh
bm ng h hp.
Gm cc thuc: Bromhexin, terpin hydrat, acetylcystein...
88
Thuc cha hen:
Tc dng: gin c trn ph qun, m rng ng dn kh d th.
Gm:
Thuc cng giao cm: adrenalin, ephedrine, sabutamol, terbutalin, isoprenalin,
phenylpropanolamin ... ( hc trong bi thuc tc dng ln h thn kinh giao cm v ph
giao cm)
- Thuc nhm corticoid: prednisolon, belomethason...( s hc trong bi hormon v cc hp
cht tng t)
- Mt s thuc khc nh theophyllin, aminophyllin (dn cht xanthin), alimemazin (khng
histamin ).
II. THUC DNG TRONG IU TR:
1. Thuc ho:
Thuc giam ho trung ng
Thu c c ch trc ti p trung tm ho hanh tuy.
CODEIN (Neo codion, Terpin Gonnon, Acopin)
Tinh ch t: Tinh th khng mau, ho c b t k t tinh mau tr ng, khng mui, d tan trong cloroform
va ethanol 96%.
Kho tan trong nc. Tan trong nc si va ether.
nh tnh:
- So ph hng ngoi vi chun
- o ph t ngoi ( c cc i hp th 284 nm)
- Cho phn ng vi thuc th chung ca alkaloid
- Thm lml acid sulfuric v 2 git dung dch st III clorid 2% vo lOmg ch phm, un
nng trn cch thy s xut hin mu xanh lam, thm acid nitric c chuyn sang mu .
89
nh lng:
- Codein base v mui ca n c th nh ng bng acid perclorid 0,1 M trong mi
trng khan, ch th tm tinh th
- Dng mui c th nh lng bng dung dch NaOH hoc nh lng trong mi
trng khan.
Tc dng: Lm gim ho do c ch trung tm ho, lm m c kh tng xut m.
Ch nh : Ho khan gy m t ngu, cac chng au nhe va va.
Tc dng khng mong mun: to bn, bun ng, hoa mt, lam am c kho t ng ra ngoai, dng
lu di c th gy dung np v l thuc thu c.
Chng ch nh : Mn cam, hen suyn, suy h hp, b nh gan, tr em di 5 tui, ph n c thai
v cho con b.
Liu dng:
Ngi ln : 10 50 mg chia 3 ln/ngy.
Tr em t 5 tui: 5 15 mg/ngy.
DEXTROMETHORPHAN (Thorphan, Atussin, Decolsin)

Cng thc: C18H25NO.HBr.H2O
Tin
h ch t: B t k t tinh g n nh tr ng, d tan trong ethanol 96%, hi tan trong nc, khng tan
trong ether.
nh tnh:
- SKLM hoc ph IR
- Phn ng ca ion bromid.
nh lng:
Phng php trung ha: ha tan ch phm vo hn hp gm 5ml dung dch acid HC1 0,0 IN
v 20ml ethanol 96%. Chun bng dung dch NaOH 0,1N. Xc nh im kt thc bng
phng php o in th.
90
Tc dng: c ch trung tm ho tng t codein, it phan ng phu va it tr m tro ng nh codein,
gy bu n ng nhe , khng gy nghin thuc, t gy to bn so vi codein.
Ch nh: Ho khan do cm cm, cm lnh, vim ph qun.
Chng ch nh: Tr em di 24 thng, ph n c thai hoc ang cho con b.
Liu dng:
Ngi ln: 10 30 mg/ngy. T i a 120mg/ngay.
Tr em 6 12 tu i : 5 15 mg/ngy. T i a 60mg/ngay.
BROMHEXIN HYDROCLORID
Bit dc: Aparsonin
Cng thc: C14H21Br2ClN2
N(2-amino-3,5-dibromophenyl methyl) N-methyl cyclohexylamin hydroclorid.

Tnh cht:
L tnh: Bt kt tinh mu trng. Tan t trong nc, ethanol.
Ha tnh: Tnh kh, b oxy ho cho sn phm mu.
nh tnh:
- Phn ng ca amin thm I: phn ng diazo ha
- Cho phn ng ca ion clorid.
- Ph IR hoc SKLM; so vi bromhexin chun.
nh lng: Phng php acid-base trong mi trng ethanol 96%; cht chun NaOH 0,1 M;
ch th o in th.
Cng dng: Bromohexin lm lng dch tit ph qun, d long m, du ho, trong c th
chuyn ha thnh ambroxol pht huy tc dng. c ch nh trong cc trng hp vim cp
v mn tnh thanh qun, kh qun, ph qun, phi; ho khan.
Liu dng: Ngi ln ung ngy 2-3 ln, mi ln 4mg. Tim bp hoc tnh mch chm 8-24
mg chia lm 4 ln ( ha vi dung dch glucose).
ACETYL CYSTEIN
Tn khc: N-Acetylcystein
Cng thc:C5H9NO3S
ptl: 163,2
91
Acid (R)-2-acetamido-3-mercaptopropanoic
Tnh cht:
L tnh: Bt kt tinh trng hoc tinh th khng mu.
D tan trong nc, ethanol; khng tan trong cloroform, ether.
Ha tnh: Tnh kh do -SH.
nh tnh:
- Ph IR hoc sc k, so vi cht chun.
- o chy: t 104 n 110c.
- Thm 0,05 ml dung dch natri nitroprussiat ( 50g/l ) v 0,05 ml ammoniac c vo 0,5 ml
dung dch ch phm 5%, xut hin mu tm m.
nh lng: Ha ch phm vo nc v dung dch HC1 long, lm lnh, thm dung dch KI
v nh lng bng dung dch iod 0,05M.
Cng dng:
- Lm lng dch nhy ng h hp.
- Bo v t bo gan khng c paracetamol.
- Tiu cht nhy trong bnh nhy nht, vim ph qun cp, ph qun-phi mn di dng
ung, xng kh dung hoc nh ti ch ( dung dch acetyl cystein 10- 20%)
- Bo v t bo nhu m gan khi dng liu cao paracetamol
Thn trng: Hen ph qun (do thuc gy co tht ph qun, nght mi).
Ch nh: Tiu cht nhy trong mucoviscidosis, bnh l h hp c m nhy, v lm sch
thng quy trong m kh qun.
Qu liu paracetamol.
Dng ti ch trong iu tr hi chng kh mt kt hp vi tit bt thng cht nhy.
3. THUC IU TR HEN PH QUN
3.1. AI CNG
Hen ph quan v m t lm sang c nh ngha l hi chng tt nghn ng h hp c
tnh thun nghch v ti din. Cn hen c c trng bi cc triu chng nh kh th, kh
kh, mt nhc km theo ri lon xut tit m di. Cc triu chng ny c th ko di t 5
10 pht, c khi hng gi hay c ngy khng dt. Sau cc cn kh th s gim dn v h t
h n, bnh nhn c th tr li trng thi bnh thng.
92
V m t sinh li b nh co th xem hen suyn la m t b nh vim ma n tinh ng h h p co
s hoa t hoa cac t bao ba ch c u, a i thc bao, dng bao, lympho baolam giai phong ra cac
ch t trung gian hoa ho c (histamin, leucotrien, prostaglandin, protease, cytokin, PAF) tham
gia vao phan ng vim va co th t ph quan, trong o co vai tro quan tro ng cua leucotrien
trong b nh chng hen.
Cn hen co th do di ng (bu i, ph n hoa, lng vu, thc ph m) ho c khng do di ng
(nhim khu n, r i loa n n i ti t, g ng sc, dung thu c khang vim NSAID).
3.2. THUC TR LIU HEN PH QUAN
3.2.1. Nguyn tc
Da vo hai nguyn tc chnh
Tr liu khng vim
Tr liu bng cc thuc lm dn ph qun
2.2.2. Thuc dn ph qun
THEOPHYLINE (Theostat, Nuelin SA).
Ch yu dng theophylin gii phng chm iu tr d phng v kim sot hen v m.
Trong cn hen nng, theophylin c dng phi hp vi cc thuc cng 2 hoc corticoid
lm tng tc dng gin ph qun.
Cng thc: C7H8N4O2
Tnh cht: Bt kt tinh mu trng, v ng nh, khng mi. Kh tan trong nc, chloroform,
tan nh trong ether, ethanol, tan trong dung dch hydroxyd kim.
nh tnh:
- Phn ng murexit (phn ng chung cho cc dn cht xanthin ): theophyllin + HC1 + H 202
.un trn ni cch thy n cn, ngui. Thm 1-2 git NH3 s xut hin mu hng
m, thm NaOH long s mt mu.
93
- Ha tan bo ha theophyllin vo dung dch NaOH long, thm dung dch CoCl2: cho kt ta
mu trng nh hng.
nh lng: phng php acid-base trong mi trng khan.
Tc dng: trc tip gin c trn ph qun v mch mu phi. c dng lm gim triu
chng v phng nga hen ph qun.
Tc dng ph: nhp tim nhanh, lon nhp, bn chn, bun nn, nn, au u, mt ng, run;
co git l du hiu xc nh trng thi qu liu.
Chng ch nh: Lot d dy t trng tin trin, ri lon chuyn ha porphyrin, ng kinh
khng kim sot c.
Liu dng: ban u 4-6 mg/ kg/ ln, sau tng dn. Ti a: 24mg/kg/ngy ( di 9
tui ); 20 mg/kg/ngy (9-12 tui ); 18mg/kg/ngy (12-16 tui ); 13kg/mg/ngy (16
tui tr ln).
CHNG VII: VITAMIN V MT S CHT DINH DNG
Mc tiu:
Sau khi hc xong bi ny, snh vin c th:
1- Trnh by c nh ngha, vai tr ca vitamin i vi sc khe con ngi, phn loi

vitamin, tnh cht chung ca mi nhm vitamin, tn cc vitamin ca mi nhm.
2- Trnh by c ngun gc, cng thc cu to, tnh cht, nh tnh, nh lng, cng dng
ca mt s vitamin.
3- Trnh by c tnh cht, cng dng ca mt s cht dinh dng thng dng.
Ni dung:
I. I CNG
1.1. NH NGHA
Vitamin l nhm cc hp cht c phn t lng tng i nh, c tnh cht l ha khc nhau
nhng c bit cn thit cho hot ng sng ca bt k c th sinh vt no.
Vitamin cn cho c th sng vi lng rt nh xp x 0,1-0,2g (trong khi cc cht dinh dng
khc khong 600g) v c vai tr nh cht xc tc.
Cho n nay c c 30 loi vitamin, xc nh c cu trc ha hc, kho st v tnh
cht vt l, tnh cht ha hc cng nh tc dng sinh hc ca chng.
1.2. PHN LOI
94
Cn c vo tnh tan, ngi ta phn vitamin ra thnh hai nhm:
Vitamin tan trong nc: vitamin nhm B v C.
- Cc loi vitamin tan trong nc xc tc v tham gia vo qu trnh lin quan vi s gii
phng nng lng (nh oxi ha kh, phn gii cc cht hu c) trong c th.
- Trong cu trc ha hc u c cha nguyn t N.
- Tnh cht: d b base v nhit phn hy.
- C th khng d tr, khi lng cung cp d d o thi ra ngoi c th qua thn, nn cn b
sung hng ngy.
Vitamin tan trong du: A, D, E, K.
- Cc loi vitamin tan trong cht bo (du) tham gia vo cc qu trnh hnh thnh cc cht
trong cc c quan v m.
- Trong cu trc ha hc khng cha nguyn t N. Nhin chung c cu trc phc tp v 1
vitamin thng tn ti nhiu dng.
- Tnh cht: bn vi nhit, base nhng d b oxy ha di tc dng ca nh sng, khng kh,
tia t ngoi, v cc tc nhn oxy ha khc.
- c d tr trong gan, m m cung cp dn cho c th nn khng cn thit phi b sung
hng ngy nhng phi b sung nh k.
- Khi hp thu bt buc phi c acid mt l cht nh ha, do phi ung thuc trong ba n (
ung lc no).
1.3. VAI TR SINH HC
Vitamin tc dng nh mt coenzym (vitamin nhm B) gp phn vo nhiu phn ng ca
enzym chuyn ha cc cht glucid, lipid, protid thnh nng lng cn thit cho hot ng
t bo.
V d:
Vitamin B1 tham gia chuyn ha hydrocarbon.
Vitamin B2 tham gia chuyn ha protid, lipid.
Vitamin tc ng chng oxy ha: vitamin A, C, E.
Vitamin tc ng nh mt hormon: vitamin A, D.
1.4. NGUN CUNG CP
- Thin nhin: M ng vt (gan c bin); c, qu, l ti sng.
95
- Sn xut bng tng hp sinh hc, ha hc.
MT S VITAMIN
VITAMIN A (RETINOL)
Bit dc: Arovit, Avibon
Ngun gc
ng vt (retinol): du gan c thu, b, sa, lng trng.
Thc vt (tin vitamin A carotene): c rt, c chua, gc, bu, b
iu ch: Trong cng nghip, vitamin A c sn xut t hai ngun nguyn liu l gan c bin
(c thu, c mp, c voi,...) v ha cht qua con ng tng hp ha hc.
Cng thc: Vitamin A khng phi l mt cht m l tn chung ch nhiu cht c hot tnh
sinh hc tng t nhau. Cht thng c gi l vitamin A l retinol c cng thc nh sau:
Tnh cht
Tinh th mu hi vng, d b oxy ha, bn vi acid, kim v nhit.
Ha tnh:
- Do c dy ni i nn vitamin A d b oxy ha; khng vng bn trong khng kh, nh sng,
khi c mt cc cht bo hoc du b hay d b oxy ha.
- Phn ng Carr- Price:
To phc mu xanh lam vi SbCl3/cloroform, mt mu nhanh.
- Nhm alcol (cui mch nhnh) to ester vi acid (bo); dng ester vitamin A bn vng hn
dng t do.
nh lng: pp UV-VIS.
Tc dng
To sc t th gic nhn trong ti.
Bit ha v duy tr biu m.
96
Gip pht trin xng, pht trin phi thai, tng trng tr em.
Tng cng chc nng min dch v gim nhim khun.
Triu chng thiu
Qung g, kh kt mc, vt bitot trn cng mc, tng sng ha nang lng.
Triu chng tha.
Triu chng: chng mt, bun nn, ban , da trc vy (cp tnh).
Triu chng: au xng, rng tc, tng p lc ni s, gan lch to (mn tnh).
Ch nh
Thiu vitamin A: qung g, kh mt.
Bnh v da: trng c, vy nn.
Ung th v cc bnh nhim trng.
Cch dng liu dng
Ty theo bnh, cng thiu vitamin A v theo tui.
Ung, tim bp: ngi ln v tr em > 8 tui: 5.000 10.000 IU/ngy x vi tun
Tr < 8 tui: 2.000 5.000 IU/ngy x vi tun.
VITAMIN D (CALCIFEROL)
Bit dc: Aldevit, Vitasterol, Vigantol.
Ngun gc
Ni sinh: 7dehydrocholesterol (tin vitamin D/da) UV
cholecalciferol (D3).
T nhin: du gan c thu, m ng vt, b, sa, lng trng (D3).
Tng hp: t ergosterol c trong nm, men bia.
iu ch: Vitamin D c iu ch bng cch chiu bc x t ngoi c bc sng thch hp vo
cc sterol tng ng.
Cng thc: V mt ha hc vitamin D l dn xut ca sterol,hai dng ph bin quan trng nht l
vitamin D2 v D3.Cc vitamin ny c to thnh t cc provitamin (tien vitamin) tng ng .
Vitamin D2 t ergosterol Vitamin D3 t 7-Dehydro cholesterol.
97
Tnh cht
L tnh:
Tinh th hnh kim, khng mu, khng mi, khng v, khng tan trong nc, tan trong dung
mi hu c, du, cht bo. B phn hy bi nh sng, acid.
Ha tnh:
- Phn ng vi thuc th SbCl3/cloroform: cho mu vng cam
- Hp th bc x t ngoi, MAX 265 nm (do c dy ni i trong phn t).
nh tnh:
- Phng php UV-VIS.
- Phn ng mu: khi cho dung dch vitamin D trong chloroform tc dng vi SbCl3,H2SO4.
nh lng: pp quang ph UV-VIS, HPLC.
Tc dng
Vitamin D2, D3 c hydroxyl ha ti gan, thn thnh Calcitriol l dng c hot tnh:
- Tng Ca2+ huyt (tng calci rut, huy ng Calci t xng vo mu, ti hp thu calci v
phosphat).
- Tc ng trn xng, biu b v t bo bit ha (tng thnh lp xng, bit ha biu b, c
ch tng sinh v cm ng bit ha t bo c tnh).
Triu chng thiu
Tr em: ci xng (xng bin dng), c km pht trin.
Ngi ln: nhuyn xng.
Triu chng tha
Calci huyt cao, tiu nhiu, mt nc, lo u, nn ma, nu ko di calci lng ng m mm
gy si thn, tng huyt p.
Ch nh
98
Phng v tr bnh ci xng tr em.
Tr nhuyn xng ngi ln.
Nhc nng tuyn cn gip.
H calci huyt.
VITAMIN E (TOCOFEROL)
Bit dc: Ephynal, Tocomin, Aquasol E.
Ngun gc
C nhiu trong du ht thc vt (m, lc, u nnh, hng dng)
Ngoi ra cn c torng gan b, lng trng, cy xanh.
Cng thc:
Tt c cc cht c hot tnh vitamin E u cha 1 nhn chroman, v tr 2 c nhm CH3, v tr
6 c nhm OH, v tr 2 cn c gc phytyl hoc 1 gc khng no (C16H17); s lng v v tr cc
nhm -CH3 gn vo nhn chroman l khc nhau.
Tnh cht
L tnh: Cht lng snh, mu vng sng, khng mi, khng v; khng tan trong nc, tan
trong du v dung mi hu c.
Ha tnh:
- Tnh kh ( nhm hydroxyphenol) : Phn ng mu vi tc nhn oxy ha (HNO 3), cc ion

kim loi...
V d: vi HNO3 hoc FeCl3 cho mu vng v :
o-Tocopherolquinon (mu ) p-Tocopherolquinon (mu vng)

- Tnh acid.
99
- Tham gia phn ng th vo v tr ortho hoc para nu cc v tr con t do.
nh tnh:
- Phn ng to phm mu azo khi tc dng vi mui diazoni.
- Ph UV-VIS trong khong 230-350nm.
- Tc dng vi FeCl3 to -tocoferylquinon c mu vng.
nh lng:
- Phng php o ceri, ch th diphenylamine ( khng mu sng mu xanh).
- Phng php o UV-VIS, HPLC.
Tc dng
Chng oxy ha, bo v mng t bo khi s tn cng ca gc t do nhm trnh thnh lp sn
phm c ca s oxy ha.
Triu chng thiu
Thn kinh v c: yu c, tht iu, rung git nhn cu, mt cm gic au v xc gic.
Tr non: Thiu mu tiu huyt, chy mu tm tht.
Ch nh
iu tr v d phng thiu vitamin E.
Dng ti ch lm m da v ngn tc dng ca tia UV.
Phng sy thai, v sinh, thiu nng to tinh trng.
Ri lon kinh nguyt, tin mn kinh.
Cn th.
Tr thiu mu tiu huyt v chy mu tm tht tr non.
VITAMIN K
Tn khc: Vikasol, Menadion
Vitamin K l mt trong nhng yu t tham gia vo qua trnh ng mu. Vitamin k l nhng
dn xut ca naphtoquinon, c hai loi:
- Vitamin K1 dng du vng nht, kt tinh - 200C, nhnh bn ch cha 20 nguyn t

carbon.
100
2-methyl-3-phytyl 1,4-naphthoquinon
- Vitamin K2 tinh th nng chy 520C, cu to nhnh bn cha 30-45 nguyn t carbon.
2- methyl-3-all-trans-famesylgeranylgeranyl-1,4-naphthoquinon.
Mch thng (3) c s n v isopren thay i, tu thuc chng vi khun sinh.
Tnh cht:
L tnh:
Vitamin K khng tan trong nc ch tan trong cht bo v cc dung mi nh ete, ru,
benzen, axeton. B phn hy nhanh di tc dng ca tia t ngoi do cu trc quinon b bin
i, ngoi ra n cng b phn hy nhanh chng khi un nng trong mi trng kim.
Ha tnh: ca nhn thm v nhm quinolon.
nh tnh: ph UV-VIS; phn ng mu.
nh lng: pp o ceri; HPLC.
Cng dng:
Vitamin K cn thit cho vic to thnh prothrombinogen v cc yu t gy ng mu khc
gan. c dng :
- Phng v iu tr bnh thiu vitamin K.
- Phng chy mu tr s sinh, phng chy mu sau phu thut v phng gim prothrombin
mu do dng thuc.
VITAMIN B1 (Thiamin)
Bit dc: Biamine, Betaxin.
Cng thc:
Ngun gc:
Vitamin Bi c trong thc n ngun gc thc vt cng nh ng vt; n c nhiu trong men
bia, trong cc ht ng cc, ch yu l cm v trong cc ht cc cy h , trong khoai ty,
c chua, hoa qu, trong tht, gan, trng, sa...
Vitamin B1 c iu ch bng phng php tng hp ho hc.
Tnh cht:
101
L tnh: Thiamin hydroclorid l bt kt tinh mu trng, v ng nh, mi thm c trng. D
tan trong nc; tan trong methanol, glycerol; kh tan trong dung mi hu c.
Ha tnh:
- Tnh base do dn xut pyrimidin c 3 nit trong phn t.
- Tnh khng bn trong mi trng base (do trong vng thiazol c nhm nit bc 4).
nh tnh:
- Trong NaOH, thm cht oxy ha (H202, kali ferricyanid...),to thiocrom, pht hunh quang
mu xanh l di tia UV:
Dung dch trong nc cho ta vi cc thuc th chung alcaloid.
nh lng:
Phng php mi trng khan, da vo tnh base ca thiamin.
Quang ph UV; o hunh quang, HPLC...
Vai tr sinh hc ca vitamin B1:
- Co-enzym (thiaminpyrophosphat carboxylase) trong chu trnh Kreb chuyn ha glucid.
- iu ha ng huyt bng hot ha hoc c ch hot tnh insulin mu.
- Tng hot tnh ca cht truyn t thn kinh
Thiu vitamin B1: Chuyn ha glucid b ngng tr, tch lu acid cetonic, gy vim dy thn
kinh, gim dn truyn thn kinh, teo c, ph n (triu chng beri-beri).
Ch nh: Phng v iu tr bnh thiu vitamin B.
VITAMIN B6 (piridoxal, piridoxamin, piridoxin)
Vitamin B6 c tch ra dng tinh th t nm men v cm go nm 1938. Cu to ca

vitamin B6 c cng nhn sau khi c tng hp nm 1939. Vitamin B6 c nm, men bia,
gan, tht b.
Cng thc: C8H11O3N.HCl; ptl: 205,64
Tn KH: 5-Hyroxy-6-methylpyridin-3,4-yl)dimethanol hydroclorid.

Tnh cht:
Piridoxin, tinh th khng mu, v hi ng, v ha tan tt trong ru v nc. Cc dng
vitamin B6 u bn khi un nng trong dung dch axit v kim nhng khng bn khi c mt
cht oxi ha.
Ha tnh:
- C tnh lng tnh: tnh base (c nhn pyridine), tnh acid (do c nhm OH phenol).
- Tnh kh (do c nhm OH ca phenol).
102
- D tham gia vo phn ng th vo v tr s 6.
nh tnh:
- Pyridoxin to phc vi acid boric (pyridoxamin v pyridoxamin khng cho phn
ng).
- Tc dng vi mui diazoni to phm mu azo.
- Tc dng vi Fe3+ to mu .
- Dng cc phn ng mu
- Phn ng xc nh gc clorid: tc dng vi AgNO3 to ta trng vn.
- Sc k lp mng, ph IR; so vi chun.
nh lng:
Acid-base/ acid acetic khan; HCIO4 0,1 M; o in th.
Quang ph UV: Pyridoxin.HCl / HC1 0,1 M; o 290 nm.
Khi thiu vitamin B6 s xut hin mt s bnh ngoi da, bnh thn kinh, st cn, rng lng,
tc
Ch nh:
- Pyridoxin c dng phng v iu tr bnh thiu vitamin B6. Biu hin ca thiu
vitamin B6 l tn thng mt, mi, ming km theo vim li, vim mng; gy co git;
sng, khp c tay; thiu mu.
- Pyridoxin c dng phng vim dy thn kinh ngoi vi do dng isoniazid, lm thuc
gii c trong ng c cycloserin.
Dng bo ch: Vin 25; 50; 100; 250 v 500 mg; Thuc tim 100 mg/ml.
Vin phi hp vitamin B1, B6 v B12.
Ch : Gim hiu lc ca levodopa khi khng c cht c ch dopa decarboxylase i km
(pyridoxal l co-enzym ca enzym ny).
VITAMIN B12 (COBALAMIN)
Gm : Cyanocobalamin, hydroxocobalamin v.v...

Cng thc:
103
X = CN : Cyanocobalamin
X = OH : Hydroxocobalamin
Trong cng thc c 2 phn:
- Phn cobalamin: gm 4 nhn pyrol hydrogen ha, gia cc nhn l nguyn t cobalt ha
tr 3.
- Phn nucleotide: gm 5,6-dimethylbenzimidazol ester ha bi acid phosphoric.
Hai phn ny ni vi nhau qua cu isopropanol.
Ngun gc:
Vitamin B12 c trong tht, trng, sn phm b, sa, gan. Vi khun sng trong lng rut
ngi, ng vt tng hp c vitamin B12. Nhiu loi vi sinh vt khc cng tng hp c
vitamin B 12
Hin nay vitamin B12 c iu ch bng phng php ln men.
Tnh cht: Bt kt tinh mu ti; phn hy chm ngoi khng kh, nh sng. Tan trong
nc, alcol; khng tan trong aceton, ether. Dng khan vitamin B12 rt d ht m v c th
hp ph n 12% nc.
nh tnh:
- Hp th UV: MAX 278; 361 v 547-559 nm; (2,5 mg/100 ml nc)
- Sc k lp mng, so vi cyanocobal chun.
nh lng: Quang ph uv, o E 361 nm.
Tc dng:
Vitamin B12 cn cho s hot ng bnh thng ca cc t bo, c bit l t bo tu xng,
thn kinh v ng tiu ho. Ngoi ra tham gia vo qu trnh chuyn ha cc cht trong c
th (protid, lipid), tng sc khng v bo v c th.
Thiu vitamin B12 gy ra cc bnh l:
- Thiu mu nguyn hng cu khng l, thiu mu c tnh.
- Tn thng ty xng khng hi phc.
- Thoi ha thn kinh lm gim hoc mt tr nh; nng hn c th b ri lon tm thn: o
gic, hoang tng...
104
Ch nh: phng v iu tr bnh thiu vitamin B12, thiu mu u sc hng cu to, vim dy
thn kinh, gi ct b 1 phn d dy.
Ch : khng dng cho bnh nhn ung th, mn cm vi thuc, thiu mu cha r nguyn
nhn.
Liu dng: 50-1000g/ln
VITAMIN C (ACID ASCORBIC).
Tn ti trong thin nhin di dng axit ascobic, axit dehidroascocbic v dng lin kt
ascocbigen, chnh l dng lin kt ca vitamin C vi polypeptit.
Vitamin C l mt dn xut ca ng glucoz.
Bit dc: Cevit, Ascorvit,...
Cng thc:
Ngun gc:
Vitamin C c nhiu trong rau qu nh cam, chanh, du, c chua, rau ci. Trong cc loi ng
cc, trng hoc tht hu nh khng c vitamin C.
Ngy nay vitamin c c iu ch bng tng hp ha hc.
Tnh cht:
Bt kt tinh mu trng, v chua. Bt kh bn trong khng kh, dung dch nc d b bin mu
trng nh sng.
D b oxy ha chuyn thnh ma nu khi tip xc v ion kim loi, mi trng kim. D tan
trong nc; tan trong ethanol, glycerin; khng tan trong dung mi hu c, du bo.
Ha tnh:
- Tnh acid: do hiu ng cm ng vi nhm carbonyl lm cho hydro ca nhm OH v tr 3
tr nn linh ng.
- Tnh kh.
nh tnh:
- Phn ng vi FeSO4, to mui st (II) ascorbat, mu xanh tm:
105
- Phn ng trc tip vi AgN03, cho mu nu v gii phng Ag.
- Lm mt mu nu ca iod trong mi trng acid sulfuric long.
- Xc nh MAX 243 nm v []D20.
nh lng:
Php o iod: Dung dch chun l dung dch iod 0,05 M; ch th h tinh bt
CH2OH CH2OH
Acid ascorbic Acid dehydroascorbic

.
Tc dng: Vitamin C c nhng tc dng sau:
- Duy tr tnh n hi thnh mch mu.
- Tng hp thu Fe2+ to hng cu; tng tnh khng nhim khun.
- Tng bn lin kt t chc xng-khp, rng, da, nim mc.
- Liu cao: h glucose huyt, km hm t bo ung th.
Khi c th b thiu vitamin C s xut hin cc triu chng nh chy mu chn rng, chy mu
cc l chn lng hoc c quan ni tng. Vitamin C cn lin quan n s hnh thnh cc
hoocmon ca tuyn gip v tuyn thng thn. Vitamin C rt cn thit cho c quan tng
sc khng v chng li cc hin tng chong, ng c bi ha cht cng nh c t ca
vi trng.
Ch nh:
- Phng v iu tr thiu vitamin c (bnh Scorbut)
- Phi hp iu tr chn thng, nhim khun, ung th.
- Thiu mu nhc sc: ung km thuc Fe (II).
Dng bo ch: vin nn, vin nhai,vin si, dung dch ung, siro, vin nang gia phng ko
da, dung dch tim
Tc dng ph: Lm dng vitamin c c th gy kch ng ng tiu ha, gy si oxalat thn,
si mt.
Bo qun: ng trong bao b kn; trnh nh sng, khng kh.
MT S CHT DINH DNG

Gm: Glucose, NaCl, KCl, st (II) sulfat, calci clorid,...
GLUCOSE
Tn khc: Dextrose
106
Cng thc: C6H12O6.H2O; ptl: 198,2.
Tn KH: D-(-) Glycopyranose monohydrat

Tnh cht: Bt kt tinh trng, v ngt nh. D tan trong nc v cn thp , kh tan trong
dung mi hu c.
Ha tnh: L mt polyalcol v l mt ng kh.
nh tnh:
- Kt ta Ag vi AgN03/amoniac.
- Phn ng vi thuc th Fehling.
- Vi phenylhydrazin: to glucosazon c dng tinh th hnh cnh thng, mu vng.
nh lng:
Phng php o gc quay cc:
Php o iod: Iod oxy ha glucose thnh acid gluconic:
I2 + NaOH NaOI + NaI + H2O
R-CHO + NaOI R-COOH + NaI (R = CH2OH-(CHOH)4-)
Cng dng:
- Cung cp cht dinh dng c kh nng chuyn ha nhanh cho c th; dng duy tr tm thi
th tch ma.
- Dng iu tr sc cho bnh nhn b bnh tm thn sau khi dng insulin.
Dng bo ch: Dung dch glucose ng trng 5% v cc dung dch u trng 10%, 20%,
25%, 30%, 50%.
NATRI CLORID(NaCl)
iu ch:
Ly t mui m hoc bc hi nc bin c mui n. Tinh ch mui n t tiu chun mui
dc dng.
Tnh cht:
Bt tinh th mu trng, khng mi, v mn. D tan trong nc, t tan trong ethanol, khng tan
trong cc dung mi hu c. pH dung dch nc 6,8-7,2.
nh tnh: Cho phn ng ca ion Cl- v Na+:
- Dung dch trong hc cho kt ta AgCl vi thuc th AgN03.
- t trn ngn la khng mu: nhum vng ngn la.
107
- Trn phin knh hin vi, t 1-2 git Natriclorid long(0,2-0,5%) .Lm bay hi nng n
kh, ngui, thm 1-2 git thuc th streng: xut hin ta vng nht, lp lnh.
Khi soi di knh hin vi thy cc tinh th hnh mt nhn c hiu
nh lng: Bng phng php o bc.
AgNO3 + NaCl - NaNO3 + AgCl
Cng dng:
Natri clorid rt cn thit cho c th. Ch phm dc dng l dung dch NaCl ng trng
(0.9%) v cc dung dch NaCl u trng 2%, 5%, 20%...
- Dung dch NaCl ng trng:
+ Duy tr tm thi th tch huyt tng
+ Dng lm dung mi a nhiu loi thuc vo trong c th bng ng truyn tnh mch
+ Dng lm cht tht tho, ra vt thng.
- Dung dch NaCl u trng: Lm gim ph gic mc khi b vim hoc ph kt mc
Bo qun: Trnh m.
CHNG VIII: THUC TIM MCH

Mc tiu:
1. Trnh by c thuc iu tr 4 bnh tim- mch: Lon nhp tim, suy tim, au tht ngc,
tng huyt p.
2. Trnh by cng thc, iu ch, tnh cht l-ha, phng php nh tnh v nh lng, cng
dng ca cc thuc in hnh ca mi nhm thuc.
NI DUNG BI HC:
A. I CNG:
Cc thuc iu tr bnh tim l nhng thuc trong chng mc nht nh c tc dng gip cho
tim phn no tr v trng thi bnh thng ca n. Cc thuc tc dng ln tim c phn
thnh bn loi chnh nh sau:
1. Thuc chng lon nhp tim.
2. Thuc tr tim.
3. Thuc chng au tht ngc.
4. Thuc chng tng huyt p.
I. THUC CHNG LON NHP
Khi s co bp, phi hp ca cc c tim khng ng u s gy ra lon nhp tim. Lon nhp
tim c hai loi: p nhanh hoc p chm hn.
Cc thuc dng trong iu tr: Thuc c tc dng iu ha tim v chng suy tim.
Da vo c ch tc dng chia thnh 4 nhm sau:
108
- Nhm I: Thuc c ch knh Na+ hay cn gi l cc thuc n nh mng: Quinidin,
Procainamid,...
- Nhm II: Thuc chn -adrenergic (thuc hy giao cm): Propanolol, Aternol,...
- Nhm III: Thuc lm gim lu thng K+ , lm gim dn truyn in tim: Aminodaron,
Bretylum,...
- Nhm IV: Thuc phong b knh Calci: Verapamil,...
MT S CH PHM
QUINIDIN SULFAT
Bit dc: Cardioquin Knidin
Cng thc: (C20H24N2O2)2.H2SO4.2H2O
ptl: 782,95
Tn khoa hc:6 -methoxy cinchonan-9-ol sulfat (2:1) dihydrat
iu ch: Chit xut t v canhkina, theo qui trnh chit alcaloid.
Tnh cht:
L tnh:
Bt kt tinh hnh kim, mu trng, v rt ng; b bin mu khi lu ngoi khng kh v
nh sng. Tan trong ethanol; kh tan trong nc, chloroform; khng tan trong ether. [a]D =
+275C n + 290 C.
Ha tnh: tnh base v d b oxy ha (do nhm vinyl).
nh tnh:
-Hunh quang: Pha quinidin sulfat vo dung dch H2S04 long, cho hunh quang xanh l trong
nh sng uv.
-Phn ng Thaleoquinin (phn ng chung ca cc alcaloid Cinchona): Dung dch quinidin, thm
nc Br2 tip theo thm ammoniac: xut hin mu hng chuyn nhanh sang xanh lc.
-Dung dch cho phn ng ca ion S04- (kt ta BaS04 vi BaCl).
-Sc k lp mng, so vi quinidn sulfat chun.
nh lng:
Phng php acid-base trong dung mi acid acetic khan; dung dch chun HGIO 0,1 M;
ch th o in th.
Cng dng: Tc dng lm gim tnh chu kch thch ca c tim nn lm gim nhp tim; ngoi
ra thuc cn tc dng h nhit.
109
Ch nh: Lon nhp tim, c bit lon nhp tim tm nh.
Liu dng: Ngi ln, ung 100-200 mg/8 gi.
Ch : ung trc ba n. Khng dng cho bnh nhn mch chm, ph n c thai, cc trng
hp nhim khun cp.
Tc dng khng mong mun: H huyt p do tim b phong b.
PROCAINAMID HYDROCLORID
Tn khc: Novocainamid hydroclorid.
Cng thc: C13H21N3O.HCl; ptl: 271,79
Tn khoa hc: 4-amino-N-[2-(diethylamino) ethyl]-benzamid hydroclorid.

Tnh cht:
L tnh: Bt kt tinh mu trng, khng mi; b bin mu khi tip xc lu vi khng kh, nh
sng. Rt tan trong nc, ethanol; kh tan trong nhiu dung mi hu c. Nng chy 166-
170C.
Ha tnh: tnh base v tnh kh do cc nhm amin bc I v III.
nh tnh:
-Nhm amin thm bc I: Phn ng to phm mu nit (nh procain).
-Dung dch cho phn ng ca ion C1- (phn HC1).
-Hp th UV/Dung dch lmg/100ml NaOH 0,1M cho max 273 nm.
-Sc k lp mng, so vi procainamid hydroclorid chun.
nh lng:
Bng php o nitrit, theo phn ng to mui diazoni ca amin thm bc I:
Ar-NH2 + NaNO2+2HC1 Ar-[N+N]Cl- + NaCl + 2H20
Cng dng: Tc dng trn c tim nh quinidin; ngoi ra cn tc dng gy t nh.
Ch nh: Lon nhp tim.
Liu dng: Ngi ln, ung: lon tht: 6mg/kg/3 gi; lon nh: 0,5-l,0g/2-6 gi.
Ch : khng s dng cho bnh nhn suy tim nng, hen ph qun.
VERAPAMIL HYDROCLORID
Bit dc: Arpamy; Cardibeltin
Cng thc:
110
Tn khoa hc:5-[2-(3,4-dimethoxyphenyl) ethyl] methylamino-2-(3,4- dimethoxyphenyl)-2-
isopropylvaleronitril hydroclorid.
iu ch:
Ngng t homoveratronitril () vi isopropyl bromide; tip n l-bromo-3- cloropropan, to
hp cht (II); cho (II) phn ng vi 3,4 dimethoxy 2-phenyl-N- methylethylamin (III) thnh
verapamid racemic. Kt tinh trong dung dch HC1 long cho verapamil hydroclorid
Tnh cht:
Bt kt tinh mu trng hoc gn nh trng. Tan trong nc, chloroform; hi tan trong
ethanol; hu nh khng tan trong ether. Nng chy khong 144 c.
nh tnh:
- Dung dch 20mg trong 100ml HC1 0,1M cho 2 cc i hp th 229 v 278 nm.
- Sc k lp mng hoc ph IR, so vi verapamil hydroclorid chun.
nh lng:
Phng php acid-base: Chun bng HC1O4 0,1 M trong dung mi acid acetic khan; ch
th o in th.
Cng dng: Tc dng chn knh Ca+ lm gim s co bp ca c tim, lm chm nhp tim, t nh
hng n thn kinh thc vt.
Ch nh: Lon nhp tim.
Liu dng: ung 80 mg/ln X 3-4 ln/24 gi.
Tim tnh mch chm 2-10 mg/ln.
Dng bo ch: ng tim 5 mg/2ml vin 40 va 80 mg.
Tc dng khng mong mun: H huyt p qu mc do gin mch ngoi vi.
II. THU C TR TIM
Thuc tr tim l nhng thuc c tc dng lm tng lc co bp ca c tim, dng trong cc

trng hp suy tim. Cc thuc c chia lm 2 nhm:
Thuc loi glycosid c ch nh trong suy tim mn.
Thuc khng phi glycosid dng trong suy tim cp tnh.
1. Cc glycoside tr tim (thin nhin)
+ Tt c u c ngun gc t thc vt.
111
+ Cu trc gn ging nhau: Phn ng gn vi phn genin qua lin kt glycoside.
- Phn Genin ( Aglycol): c cu trc Steroid lin kt vi R1 l vng lacton 5 hoc 6 cnh v
tr C17.
- Phn Ose l cc ng him nh: Digitoxose, Ramnose,..
+ C cng c ch tc dng.
Hin ch cn digoxin v digitoxin c dng lm sng.
DIGITOXIN
Tn khc: Digitoxosid.
Ngun gc: Glycosid t l cy Digitalis purpurrea (dng a hong ta) v Digitalis
lanata(dng a hong lng).
Cng thc:
Tnh cht:
Bt kt tinh mu trng, khng mi. Tan trong nc; d tan trong ethanol, chloroform.
nh tnh:
-Ha tan vo ethanol 60%, thm vi git acid dinitrobenzoic v vi git NaOH long xut hin
mu tm.
112
-Dung dch trong acid acetic khan c FeCl3, khi cho tip xc vi H2SO4 m c xut hin mu
xanh.
-SKLM, so vi digitoxin chun.
nh lng:
Phng php o quang, theo phn ng to mu gia digitoxin vi dung dch natri picrat kim; o
495 nm. Tin hnh ng thi vi digitoxin chun,
Ch nh: Suy tim. ung pht huy tc dng chm, ko di 14 ngy.
Liu dng:
Ngi ln, ung liu u 0,6 mg; sau 3-6 gi ung tip 0,2-0,4 mg cho n khi t tng liu 1,6
mg/1-2 ngy; duy tr, ung 0,05-0,3 mg/24 gi.
Ch : Thuc c c tnh cao, cn iu chnh liu ph hp cho tng bnh nhn.
Bo qun: Trnh nh sng; thuc c bng A
2. Cc thuc tr tim khng phi loi digitalis
V sao phi nghin cu tm cc thuc tr tim khng phi l digitalis?
Do glycosit tr tim c c tnh cao, vng iu tr hp.
tch ly trong c th cao.
Do glycosit tr tim ch iu tr c bnh tim mn tnh, khng dng c cho ngi b bnh
tim cp tnh.
Do cc thuc tng hp cn t c cc tiu ch sau:
Chi phi mt cch hiu qu cc triu chng lm sng ca bnh suy tim.
Thuc c th dng theo ng ung.
c tnh thp hn, t tch ly trong c th hn.
Khng th hin tc dng ph khi phi dng thuc trong thi gian di.
Ko di c cuc sng ca ngi bnh.
Tc dng: Tng lc bp c tim , gin mch.
C ch tc dng: Phong b phosphodiesterase khng chn lc.
Gm: Amrinon, milrinon v flosequinan:
Flosequinan Amrinon Milrinon
AMIRINON
Bit dc: Inocor; Wincoram
Tn khoa hc: 5-Amino-(3,4-bipyridin)-6(lH)-on
Tnh cht:
113
Bt mu vng nht; b bin mu trong nh sng, khng kh. Tan t trong methanol, kh tan tng
nc, tng tan pH 4; khng tan trong chloroform.
Cng dng:
Tng lc bp c tim, tng nhp tim v gin mch. Dng iu tr suy tim thi hn ngn, thay th
cc thuc chng suy tim khc khi cn.
Ch nh: Suy tim, iu tri thi hn ngn
Liu dng: Tim chm tnh mch 750 ug/kg/2-3 pht.
Ti a 10 mg/24 gi.
Dng bo ch: Thuc tim 5 mg/ml.
Tc dng khng mong mun: H huyt p, ccm au ging au tht ngc.
III. THUC CHNG AU THT NGC

Cc thuc iu tr (theo c ch tc dng) c chia thnh bn loi:
Loi iu tr cn au, gin mch: cc este nitrat v nitrit hu c. Loi thuc ny c.
Nhm c ch knh canxi: c tc dng lm gim mch, gim cng nng, nhp p ca tim,
gim s co bp ca tim.
Nhm thuc phong to recptor adrenergic: c tc dng iu tr, cng c, gim cng nng
ca tim, tit kim s dng oxi ca tim, c ch trao i cht.
Nhng nhm khc: c tc dng tng cng dng chy ca mch vnh.
Mt s thuc c th
NITROGLYCERIN
Bit dc: Trinitrin
Cng thc:
nh tnh, nh lng:
Phn ng to mu gia HNO3 vi acid phenolsulfonic, qua cng an:
- Trong mi trng acid acetic, cc nitrat hu c phn hy ra HNO3.
HN03 nitro ha acid phenoldisulfonic cho mu vng cam; chuyn sang vi ammoniac d
to mui amoni nitrophenolsulfonat.
R-O-NO2 + H2O/CH3COOH -> R-OH + HNO3
114
+ NH4OH
- Dng phn ng mu cho mc ch nh lng:
Sau khi to mu , o hp th 405 nm; so snh vi chun l dung dch KNO3 0,1335
g/500 ml, to mu theo cng phn ng.
Tc dng:
Cc nitrat hu c gii phng NO trc tip gy gin ng mch, k c ng mch vnh, iu
ha lng mu v tim.
Danh mc thuc: Nitroglycerin, isosorbit nitrat, pentaerythritol tetranitrat....
DILTIAZEM
c im cu to v tnh cht ha l:
Tn khoa hc: 1,5-Benzothiazepin-4(5H)-one,3-(acetyloxy)-5- [2-(dimethylamino)ethyl]-2,3-

dihydro-2-(4-methoxyphenyl), monohydrochlorid
Tnh cht vt l, ha hc:
- Bt kt tinh hoc tinh th nh mu trng, khng mi.
- Nhit nng chy: T 207,50 C n 212,00 C.
- H s phn b: Log P(octanol/nc) = 2,79.
- Dng mui tan tt trong nc, v acid formic, it tan trong ethanol, khng tan trong ether.
Dng base tan tt trong cloroform, ether. Do khi chit DTZ trong huyt tng bng
phng php chit lng lng nn kim ha chuyn sang dng base ri chit bng dung
mi hu c khng phn cc nh cloroform, diclormethan, diethyl ether, n-hexan
- Dng dc dng thng kt hp vi 1 phn t acid hydrocloric nn c th
nh lng DTZ theo phng php chun bc nitrat.
- Ph hp th UV-Vis: nh hp th trong dung dch acid H 2SO4 0,2M l 236 nm, trong
dung dch kim l 237 nm. Do vi dng nguyn liu v ch phm c th nh lng bng
cch o trc tip ph hp th UV hoc HPLC vi detector UV.
Tc dng:
Lm gin mch vnh, lm chm nhp tim, h huyt p. Thuc c s dng trong iu tr au
tht ngc v tng huyt p.
115
2. Thuc phong b bta-adrenergic
C ch: tc dng chng au tht ngc lin quan n vic c ch - receptor ca tim, khng
lin quan n tc dng n nh mng v gy t ti ch, lm gim cng nng ca tim, tit kim
s dng oxi cho c tim, c ch qu trnh trao i cht ca c tim.
Khng dng cho ngi c suy tht tri, v c th gy try tim mch t ngt. Khng nn
ngng thuc t ngt v c th gy hin tng bt li lm nhi mu c tim, t t.
Cc thuc s dng:
Practolol Acebutolol Atenolol

3. Cc thuc c tc dng chng au tht ngc khc
Thuc t tho mc: khelline v visnadine
Thuc tng hp: carbocromum, amiodarone, dipyridamole
khelline dipyridamole
Bng 1.2. Mt s thuc dng trong iu tr au tht ngc.
Tn cht Cng thc Cng dng, liu dng
Bepridil - Phng au tht ngc
- Chng lon nhp tim
NL, ung 200-400
mg/24 gi
Carbocromen - Phng au tht ngc

NL, ung 225-900
mg/24 gi
Imolamin - Phng au tht ngc

NL, ung 90 mg/24 gi
116
Lidoflazin - Phng au tht ngc
(phong b knh calci)
NL, ung 180 mg/24 gi
IV. THUC CHNG TNG HUYT P

Thuc iu tr tng huyt p (HA) c phn loi theo c ch tc dng gm cc nhm:
1. Thuc phong b knh calci lm h huyt p.
2. Thuc tc ng h thng rennin-angiotensin.
3. Thuc chng tng huyt p tc ng trung ng.
4. Thuc gin mch trc tip lm h huyt p.
Cc thuc dng trong iu tr
1. Thuc phong b knh calci lm h huyt p (cc CEB)
Cu trc ha hc chung: u l dn xut ca 1,4-dihydropyridin.
Da vo cu trc ha hc chia thnh 2 phn nhm:
- Nhm I: Dn cht nitro ( trong cu trc ha hc cha nhm NO2).
- Nhm II: Dn cht khng nitro ( trong cu trc khng cha nhm NO2).
Lin quan cu trc v tc dng:
- Cc thuc nhm ny u c tc dng phong b knh Calci c trn trong mch mu, gy
gin mch, h huyt p.
- Cu trc 1,4-dihydropyridin quyt nh n tc dng ca thuc. Trong nhm =NH (1)
ng vi tr quan trng.
- Cc nhm ester 3,5 nh hng n hot lc gin mch
- V tr nhm th phenyl nh hng n hiu lc tc dng: ortho> meta> para.
117
Mt s thuc c th:
NIFEDIPIN
Bit dc: Adalat; Cordicant
Cng thc: C17H18N2O6 ptl: 346,34
Dimethyl -l,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl) pyridine-3,5-dicarboxylat

Tnh cht:
Bt kt tinh mu vng nht; b bin mu khi tip xc nh sng bc song ngn. Khng tan
trong nc; tan trong ethanol, methanol, ether.
nh tnh: Kh ha nhm nitro thnh amin thm bc I ri lm phn ng diazo ha.
nh lng: pp o Ceri, HPLC.
Cng dng: Tc dng phng b knh Ca2+ lm gin mch, h huyt p.
118
Ch nh: Tng huyt p. Ngi ln, ung 10-30 mg/ln X 3 ln/24 gi.
Ch : bnh nhn suy gan, ph n mang thai, cho con b.
Bo qun: Trnh nh sng
2. Thuc tc ng h thng rennin-angiotensin:
Da vo c ch tc dng chia thnh 2 nhm:
- Thuc c ch enzyme chuyn angiotensin: Enalapril, Captopril,...
- Thuc i khng th th angiotensin II: Losartan, Valsartan,...
(Vit tt ACET= Angiotensin converting enzyme inhibitors).
Mt s thuc c th:
ENALAPRIL MALE AT
Bit dc: Enaladil; Renitec.
Cng thc: C20H28N2O5.C4H4 O4 ptl: 492,52
Tn khoa hc: l-[N-[l-(ethoxycarbonyl)-3-phenylpropil]-L-prolin butenedioat.

iu ch:
Ngng t acid benzylyruvic (I) vi dipeptid L-ala-L-pro (II) to hp cht trung gian imin;
kh bng cyanoborohydrua natri trong mi trng acid, to hn hp ng phn R,s
analaprilat (III); tch ly ng phn s bng sc k; to ester vi ethanol, sau to mui vi
acid maleic:
Tnh cht: bt kt tinh mu trng, tan t trong nc, tan trong ethanol, methanol.
nh tnh: Ph IR ph hp vi enalapril maleat chun.
nh lng: Phng php HPLC.
Cng dng:
Mt tin thuc ACEI chng tng huyt p. Hp thu ng tiu ha, vo c th thy phn
chc ester gii phng enalaprilat l dng hot tnh.
Ch nh:
Tng huyt p; phi hp iu tr suy tim.
Ngi ln, ung 5 mg/ln/24 gi; iu tr suy tim, ung 2,5 mg/ln/24 gi.
Dng bo ch: Vin 5 v 10mg.
Ch : khng dng bnh nhn hp ng mch thn, hp ng mch ch nng.
3. Thuc chng tng huyt p tc ng trung ng
- Dn cht kiu cathecholamin: Methyldopa
- Dn cht imidazol: Clonidin v cc cht tng t.
Mt s thuc c th:
119
METHYLDOPA
Tn khc: Alpha-methyldopa; 1-Methyldopa.
Cng thc: C10HI3NO4.1,5 H20
ptl: 238,20
Tn khoa hc: 3-Hydroxy- a -methyl-L-tyrosin sesquihydrat.

Tnh cht:
L tnh: Bt kt tinh mu trng, ti trng nh vng hoc dng tinh th khng mu. Tan t
trong nc, ancol, tan t do trong acid v c long; khng tan trong ether.
Dung dch 40 1 g/ml HC1 0,1 M cho cc i hp th 281 nm.
Ha tnh: D b oxy ha bi oxy khng kh, nh sng; lng tnh (acid amin).
nh tnh:
- Trn methyldopa vi vi git dung dch tricetohydriden trong H2 S04 c: xut
hin chm mu hng m; thm nc chuyn sang mu vng.
- Cho mui mu tm vi st (II) tartrat pH 8,5 (phenol).
nh lng: Bng cc phng php:
- Acid-base trong acid acetic khan; HCLO40,l M; o in th.
- o quang sau khi to mu vi st (II) tartrat; o 520 nm. IV.3.1.6 Cng dng: Thuc
tc ng trung ng lm h huyt p.
Ch nh: iu tr tng huyt p vi liu ung 250 mg/ln 2-3 ln/24 gi.
Tc dng khng mong mun: Bun ng, trm cm, mt mi.
CLONIDIN HYDROCLORID
Bit dc: Dixarit; Catapres.
Cng thc:
120
Tn khoa hc: 2-[(2,6-Diclorophenyl)amino]-2-imidazolin hydroclorid.
iu ch:
Oxy ha dicloro-2,6-N-formyl aniline (I) thnh dn cht dicloroimin (II); cho (II) phn ng
vi ethylendiamin; ng vng cho clonidin base; kt tinh dng hydroclorid trong dung dch
HC1.
Tnh cht
Bt kt tinh mu trng, khng mi, v ng; bn ngoi khng kh, nh sng v nhit. Tan
trong nc, ethanol; kh tan trong chloroform.
nh tnh:
- Hp th UV: Dung dch 30 mg trong 100 ml Cl 0,01 M cho hai cc i hp th 272 v
279 nm; tr s hp th ring 18 v 16, tng ng.
- Sc k lp mng, so vi clonidin hydrolorid chun.
nh lng:
Phng php acid-base trong ethanol 96%; dung dch NaOH 0,1 M trong ethanol; ch th o
in th (nh lng theo phn HC1).
Cng dng: Tc dng vo trung tm vn mch lm h huyt p.
Ch nh: Tng huyt p; d phng v iu tr chng au na u.
Liu dng: Ngi ln ung 0,1 mg/ln X 2 ln/ 24 gi.
Bo qun: Trnh nh sng
4. Cc thuc gin mch lm h huyt p:
L cc thuc trc tip lm gin mch theo cc c ch khc nhau; hiu lc ca
thuc ty thuc vo s nhy cm ca thnh mch. Thng cc thuc ny ch dng
phi hp trong phc iu tr tng huyt p.
Danh mc thuc: Natri nitroprusiat, hydralazin, nitropoxid, diazoxid, minoxidil....
NATRI NITROPRUSIAT
Tn khc: Natri nitroferricyanid
Cng thc: Na2Fe(CN)5 NO.2H2O
iu ch: Ha tan kali ferocyanid vo dung dch HNO3 50%; un si trong 1 gi. Sau khi
lm ngui, lc loi KNO3; trung ha dch lc bng Na2CO3; lm bay
121
hi nc kt tin.
Tnh cht:
Tinh th mu nu- nht; rt tan trong nc; tan nh trong ethanol; b phn hy chm trong
dung dch
Dung dch nc, thm thuc th natri sulit: xut hin mu tm .
Cng dng:
Vo c th gii phng NO gy gin mch ngoi vi, gim sc cn mch lm h huyt p. Thi
hn tc dng rt ngn; khong an ton hp.
Ch nh:
Ch dng truyn tnh mch chm, lin tc cp cu trong trng hp nhi mu c tim cp v
suy tim.
Truyn 50 mg, pha trong 400-1000 ml dung dch glucose 5%
Dng bo ch: L bt pha tim 50 mg; ch pha khi dng.
Tc dng khng mong mun: Tng nhp tim, bun nn, rung c; h huyt p.
IV. THUC LI TIU
1. THUC LI TIU THM THU

L nhng cht d tan trong nc, c lc hon ton qua cu thn, rt t ti hp th ng
thn v tr v mt dc l; v vy, khi dng liu cao, n lm tng thm thu ca dch lc
trong ng thn v do n lm gim s ti hp thu nc; tng lng nc tiu. Hin nay,
trong nhm ny c 4 thuc c dng l glycerin, isosorbit, mannitol v ur.
MANNITOL
Bit dc: Osmitrol.
Cng thc: C6H14O6 ; ptl: 182,17.
Tnh cht
L tnh:
Bt kt tinh trng, khng mi, v hi ngt. Nng chy 165C-168C. Mannital d tan trong
nc, rt kh tan trong ethanol, thc t khng tan trong ether v lipid.
Ha tnh:
Ha tnh ca mannitol l ha tnh ca mt polyalcol nn:
- Ha tan c hydroxyd ng (II) hoc hydroxyd st (III): Cho 0,5 ml dung dch st (III)
clorid vo 1 ml dung dch bo ha mannitol trong nc, thm 0,2 ml dung dch natri
122
hydroxyd 5 M. Lc. Dung dch vn trong D tham gia phn ng ether ha hoc ester ha: Tc
dng vi anhydride acetic c pyridine xc tc to kt ta hexaacetyl mannitol; ta nng chy
123C
Da vo phn ng ny nh tnh v nh lng mannitol bng cch xc nh ch
s ester ha..
Cng dng:
Do khng tan trong du nn mannitol khng khuch tn qua rut vo mu; phi dng ng
tim tnh mch. Liu cho ngui ln t 50-200 g/24 gi.
Ch nh dng:
Tng li tiu thi c.
Duy tr chc nng to nc tiu trong trng hp suy thn cp, hoi t ng thn, thiu niu
sau m, sau chn thng
Lm gim ph no, tr tng nhn p.
Dng bo ch: Dung dch t 5% n 25%; tim truyn tnh mch.
2. CC THUC C CH CARBONIC ANHYDRASE
ACETAZOLAMID
Bit dc: Diamox; Dazamid.
Cng thc:
Tnh cht:
L tnh:
Bt kt tinh trng, khng mi, khng v; t tan trong acetone; kh tan trong ethanol; rt kh
tan trong nc; thc t khng tan trong ether, chloroform
Ha tnh:
Ha tnh ca acetazolamid l ha tnh ca nhm acetamid; sil-fonamid v d vng thiadiazol.
l tnh acid, tnh base (pKa~7,4 v 9,1, d b thy phn, hp th mnh bc x t ngoi.
Cng dng:
Do khng c tc dng li tiu khi iu tr lu di, li c tc dng ph c hi nn ngy nay,
acetezolamid khng dng lm thuc li tiu m ch dng iu tr bnh glocom v iu tr
bnh ng kinh. Ngoi ra, acetazolamid cn c dng phng v iu tr chng say khi
leo ni v lm kim ha nc tiu gip cho vic o thi mt s thuc c tnh acid yu ra
khi c th v chng to si thn ( si acid, si cystin).
Ch nh
iu tr tng nhn p.
123
iu tr nhim kim chuyn ha.
Kim ho nc tiu gip thi tr mt s cht: Acid uric, Aspirin
iu tr ng kinh.
3. THIAZID V CC THC LI TIU CHNG THIAZID
HYDROCHLOROTHIAZID
Bit dc: Hydro-diuril; Apo-Hydro; Diuchlor H; Esidrix; Hydro-D; Hydro- Chlor, Oretic.
Cng thc:
Tn khoa hc:6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazin-7-sulfonamid-1,1-dioxyd
Tnh cht:
L tnh:
Bt kt tinh trng hoc hu nh trng, khng mi, nng chy khong 268C vi s phn hy;
pKa2 9,2.
Hydrochlorothiazide t tan trong nc, methanol; d tan trong cc dung dch kim,
dimethylformamid; khng tan trong ether, chloroform.
Ha tnh:
Hydrochlorothiazid c tnh acid yu, tnh base yu, d b thy phn v hp th mnh bc x
t ngoi. Nhng tnh cht c ng dng trong nh tnh, nh lng hydrochlorothiazide.
Hydrochlorothiazide d tan trong cc dung dch kim, tc dng vi mt s mui to mui
mi kt ta hoc c mu.
Cng dng: Ch nh dng nh cc thiazid ni chung l iu tr bnh tng huyt p v lm
thuc li tiu.
Dng bo ch: Vin nang 12,5 mg; vin nn 25 mg, 50 mg v 100 mg. Dung dch ung 10mg
v 10 mg/ml.
4. THUC LI TIU MNH - THUC LI TIU TC DNG TRN QUAI
HENLE.
Nhm ny gm nhng hp cht c cu trc hc hc rt khc nhau. Cc hp cht hu c thy
ngn cng thuc nhm ny, song do c vi tim thn v nhiu nhc im khc nhau nn
ngy nay khng dng.
FUROSEMID
Tn khc: Frusemid
Bit dc: Lasix; Furoside; Myrosemid; Novosemide; Uritol.
Cng thc:
124
Tn khoa hc: Acid-4-chloro-5-sulfamoyl-2-[(2-furanylmethyl) amino]benzoic.
Tnh cht:
L tnh:
Bt kt tinh trng hoc hu nh trng, khng mi, khng v; khng bn vng vi nh sng,
nhng vng bn ngoi khng kh; chy khong 210C vi s phn hy; pKa 3,9. Furosemid
thc t khng tan trong nc, tan trong acetone, kh tan trong ether,, hi tan trong ethanol,
tan trong methanol v rt d tan trong dimethylformamid; tan trong cc dung dch kim
long.
Di tc dng ca nh sng, furosemid bin mu dn.
Ha tnh:
Ha tnh ca furosemid l ha tnh ca nhm carboxylic, ca nhm sulfonamide, ca nhn
thm v ca nhm amin thm, ng dng cc ha tnh ny nh tnh, nh lng furosemid
v iu ch mui d tan trong nc.
Cng dng: iu tr bnh tng huyt p; iu tr ph v chng tng calci mu.
Dng bo ch: Vin nn 20; 40 v 80 mg. dung dch ung 8 mg; 10 mg/ml. Thuc tim
10mg/ml.
5. THUC LI TIU GI KALI
Tt c cc thuc li tiu k trn u c tc dng lm tng s o thi ion kali qua nc tiu.
Tuy nhin, c mt s cht thuc 3 nhm cu trc ha hc khc nhau, c tc dng li tiu, li
c tc dng lu gi ion kali. Cc thuc ny c gi chung l thuc li tiu gi kali.
AMILORID HYDROCLORID
Bit dc: Midamor.
Cng thc:
C6H8C1N70.HC1.2H20 ptl: 302,12

Tnh cht:
L tnh:
Bt mu xanh hi vng, khng mi; nng chy khong 240c. Amilorid hydroclorid t tan
trong nc (1 g tan trong 200ml nc) v ethanol, thc t khng tan trong chloroform v
ether.
Ha tnh:
125
Amilorid c tnh base, d b. thy phn, c bit trong mi trng kim; d b oxy ha (c
bit trong mi trng kim v khi tip xc vi nh sng); hp th mnh bc x t ngoi. Cc
tnh cht c ng dng trong nh tnh v nh lng amilorid.
Cng dng:
Amilorid hydroclorid ch yu c dng kt hp vi cc thuc li tiu khc ( nh thuc tc
dng trn quai Henle hoc thiazid) lm tng s o thi ion natri v nc ra khi c th.
Cc thuc ny cng c th dng mt mnh iu tr ph nh do suy tim sung huyt hoc x
gan, hi chng thn h hoc iu tr bnh tng huyt p.
CHNG IX: THUC TC DNG LN THN KINH GIAO CM V PH GIAO

CM
Mc tiu:
1- Trnh by c c im tc dng ca cc thuc kiu giao cm, hy giao cm, kiu ph
giao cm v hy ph giao cm.
2- Trnh by c cng thc cu to, tnh cht, nh tnh, nh lng, cng dng, liu dng
ca mt s thuc kiu giao cm, hy giao cm, kiu ph giao cm, hy ph giao cm.
Ni dung:
A. I CNG
H thn kinh thc vt gm 2 h: h thn kinh giao cm (h Adrenergic) v ph giao cm
(cholinergic) phn b ti cc c trn v cc tuyn.
Cht gy cn tr tc dng ca adrenalin l thuc hy giao cm (hay chn giao cm), cn
thuc gy cn tr tc dng ca acetylcholine l thuc hy ph giao cm (hay chn ph giao
cm).
1. Thuc tc dng kiu giao cm:
Thuc tc dng kiu giao cm hay cng giao cm c tc dng kch thch cc dy thn kinh
giao cm, gy tc dng:
- Tng nhp tim, co mch, tng huyt p.
- Gim co tht c trn, gin c ph qun.
- Gin ng t, gim tit dch ngoi tit.
V cu trc ha hc, hu ht cc thuc c tc dng cng giao cm l dn cht ca
phenylethylamin.
126
C th chia cc cht cng giao cm ra thnh 2 nhm:
- Nhm 1: Gm cc cht nh adrenalin, noradrenalin, dopamine, salbutamol, terbutalin,
dobutamin ... Cng thc c nhm - OH chc phenolic nn km bn. Nhm ny c tc dng
cng giao cm mnh, tc dng ngn.
- Nhm 2: Gm cc thuc nh ephedrine, norephedrin, amphetamine...Cng thc khng c
nhm chc - OH phenolic nn vng bn hn, c tc dng cng giao cm yu nhng lu hn.
2. Thuc tc dng hy giao cm:
Tc dng: phong b th th ca adrenalin v phong b ngn si giao cm.
Cu trc: gm:
- Dn cht ca acid lysergic ( ergotamine, ergometrin...)
- Dn cht ca phenylethanolamin ( sotalol, labetol)
- Dn cht ca aryloxypropanolamin ( atenolol, acebutolol, propranolol, timolol...)
- Dn cht ca guanidine (guanetidin)
- Dn cht ca aminoacid (methyldopa)
II. THUC TC DNG LN THN KINH PH GIAO CM
1. Thuc tc dng kiu ph giao cm:
- Lm gim hot ng ca h tim mch, gin mch gy h huyt p.
- Tng co tht c trn, co ng t.
- Tng tit dch ngoi tit.
Phn loi: gm 2 nhm:
- Thuc tc dng ph giao cm gm mt s este ca cholin vi acid acetic, acid carbonic nh
acetylchoin, methacholin, betanecol, carbacholin v mt s alkaloid nh muscarin,
pilocarpin, arecholin, nicotin,lobelin.
- Thuc khng cholinesterase khng thun nghch gm cc alkyl phosphate, mt s alkaloid
nh physostigmin.
2. Thuc tc dng hy ph giao cm:
Cc cht ch yu l cc alkaloid c nhn tropan (nh atropine, scopolamine) v mt s cht
tng hp hay bn tng hp .(nh homatropin, tropicamid)
Cu trc ha hc chung ca cc thuc hy ph giao cm c nhng yu t ging cu
trc acetylcholine, l:
- Amin bc 3 hoc bc 4 to trung tm cation
- Phn vng nh vo acyl to nn gc c ch
- Mch trung gian ni 2 phn trn.
V vy chng c tc dng i khng tranh chp vi acetylcholine v cc thuc cng ph
giao cm khc.
B. MT S THUC
I.Thuc tc dng kiu giao cm
ADRENALINE HYDROCLORID
Tn khc: Epinephrin, Levoepineprin
Cng thc: C9H13NO3 HCl
127
Tnh cht:
L tnh: Bt kt tinh mu trng hoc trng ng; d chuyn mu hoc nu di tc dng
ca nh sng, khng kh. Ch phm t tan trong nc v ethanol; tan trong cc dung dch
hydroxyd kim.
Ha tnh : tnh kh. Sn phm oxy ha chnh l Adrenocrom.
nh tnh:Dng phn ng oxy ha bi cc thuc th : mui st III, iod, kali iodat...
nh lng: Bng phong php acid-base trong mi trng acid acetic khan; cht chun
l HC1O4 0,1M; ch th o in th.
Cng dng, ch nh:
- Lm tng nhp tim, tng lu lng tim, co mch do lm tng huyt p.
- Lm gin ph qun, lm d th, dng cha hen ph qun.
- Lm co,cc ng mch nh:
+ Dng cho vo cc dung dch thuc t ko di tc dng ca thuc t
+ Gim xung huyt nim mc khi vim mi, vim xoang, vim kt mc...
+ Lm gim ng t: dng iu tr glocom v kim tra nhn p.
Dng dng- liu dng:
- Dung dch tim 0,1%. Tim bp hoc tim di da trung bnh 0,2 - 0,5 mg/ ln, ti a
lmg/ln, 2mg/24h.
- Dng vin: liu gp i liu tim
Bo qun: Trong chn khng, trnh nh sng.
SALBUTAMOL SULFATE
Tn khc: Albuterol sulfat
Cng thc:
Tn KH: [2-( 1,1 -Dimethyl)ethylamino-1 - r4-hvdroxv-3 -(hydroxymethyl)

phenyljethanol] sulfat.
Tnh cht: Bt kt tinh mu trng, v ng nh; bin mu chm trong khng kh, nh sng.
D tan trong nc (1 g/4 ml); tan trong ethanol, cloroform, ether.
128
nh tnh:
- Vi thuc th oxy ha (HNO3, FeCl3): mu hng.
- Dung dch trong nc cho phn ng ca ion SO42-
- Cc php th vt l: ph UV; sc k....
nh lng: Phng php acid-base trong mi trng acid acetic khan; cht chun l
HCIO4 0,1 M ; ch th o in th.
Cng dng: Cng dng chnh l iu tr hen co tht ph qun, kh th gin on v cn
hen ko di. Ngoi ra cn dng chng non
Dng bo ch: Vin 4 mg; Kh dung 100 g/liu; thuc tim 0,05 mg/ml, 0,2mg/ml,
0,5mg/ml; thuc n 1mg.
Bo qun: Trnh nh sng, khng kh.
NAPHAZOLINE HYDROCLORID
Bit dc: Naphathyzin, Rhinyl,...
Cng thc:
Tn KH: 2-(Naphth-l-ylmethyl)-2-imidazolin hydroclorid.

Tnh cht: Bt kt tinh mu trng, v ng, khng mi.Tan trong nc, ethanol
96%, khng tan trong ether.
Ha tnh: Tnh base do vng imidazolin.
nh tnh:
- Hp th UV: MAX = 270; 280; 287 v 291 nm (o trong mi trng acid Hydroclorid 0,01M
trong khong t 230 n 350).
- Ha ch phm vo methanol, thm dung dch natri nitroprusiat 5% v dung dch NaOH 2%;
yn 10 pht, thm dung dch NaHC03: xut hin mu tm.
- Dung dch nc cho phn ng ca ion Cl-
nh lng: Phng php acid-base trong mi trng ethanol 96%; cht chun NaOH 0,1
M; ch th o in th.
Cng dng:
- Thuc c tc dng cng giao cm, c bit l tc dng gy co mch lm tn mu.
Naphazolin khng kch ng v dung np tt.
- Dng lm tn mu, chng sung huyt, chng vim nim mc mt, mi, tai, hng. iu
tr vim mi cp, mn tnh; vim xoang cp v mn tnh, vim thanh qun, ph n thanh qun
do d ng, do chiu tia X, sung huyt nim mc sau phu thut.
- Dng ko di tc dng ca thuc t khi gy t b mt nim mc mi, ming, thanh qun:
thm 3-4 git dung dch 0,1% vo 1 ml dung dch thuc t.
129
II. Thuc tc dng hy giao cm
ATENOLOL
Tn khc: Tenormin
Cng thc:
Tn khoa hc: 4-[2-(Hydroxy-3-isopropylaminopropoxy)phenyl] acetonid.

Tnh cht: Bt kt tinh mu trng; nng chy 152-155C.
Tan nh trong nc; tan trong ethanol, methanol; khng tan trong ether.
Ha tnh: Tnh base do nhm amin bc II. un si trong dung dch NaOH to kh NH3 (thy
phn acetamid).
nh tnh:
- Hp th UV: MAX = 275 v 282 nm
- SKLM hoc ph IR, so vi atenolol chun.
nh lng:
Phng php acid-base trong mi trng acid acetic khan; cht chun HCIO4 0,1 M ; ch
th o in th.
Tc dng - ch nh: Thuc chn , lm gim lu lng tim v tnh co bp ca c tim. c
ch nh trong iu tr cn au tht ngc, lon nhp tim, bnh cao huyt p...
Liu dng: ngi ln 1 ngy ung 100mg.
Chng ch nh: mch chm di 50 nhp/ pht, tr em di 16 tui.
PROPRANOLOL HYDROCLORID
Tn khc: Dociton; Inderal
Cng thc:
TnKH: l-Isopropylamino-3-napht-l-yloxypropan-2-ol hydroclorid .

Tnh cht: Bt kt tinh mu trng, khng mi, v ng. Tan trong nc v ethanol;
kh tan trong dung mi hu c.
130
nh tnh:
- Hp th UV: MAX 290 v 319 nm (nc-methanol).
- Ph IR hoc sc k, so vi propranolol hydroclorid chun.
- Dung dch nc cho phn ng ca ion Cl-
nh lng:
Phng php acid-base trong mi trng ethanol 96%; cht chun NaOH 0,1 M; ch th o
in th.
Tc dng- ch nh:
Propranolol c tc dng phong b th th (1, 2).
c ch nh trong iu tr au tht ngc, tng huyt p, ri lon nhp tim (nhp tim nhanh,
nh trng ngc, ngoi tm thu, rung tim), gii c thuc cng giao cm.
Chng ch nh: Hen ph qun, suy tim, mch chm (di 50 nhp/pht).
GUANETHIDIN MONOSULFAT
Cng thc:
Tn KH: l-(2-Perhydroazocin-l-yl) guanidin monosulfat (2:1)

Tnh cht: Bt kt tinh mu trng; nhit nng chy khong 250C. D tan trong nc; kh
tan khng tan dung mi hu c.
Ha tnh: Tnh base; d b thy phn gii phng NH3.
nh tnh:
- Phn ng mu: Dung dch trong NaOH c, thm -naphtol. Thm tng git, va lc, natri
hypoclorid: ta mu hng, lu chuyn sang mu tm .
- un si trong dung dch NaOH: NH3 (xanh qi ).
- Dung dch nc cho kt ta vi thuc th chung alcaloid.
- Cho phn ng ca ion sulphat.
nh lng: Phng php acid-base trong mi trng acid acetic khan; cht chun HC1O4
0,1 M; ch th o in th.
Tc dng - ch nh: Guanethidin lm gim hot ng ca tim, gin mch, h huyt p ko
di. c ch nh cho ngi cao huyt p, glocom mn n thun gc m.
Liu dng: Tun u, t 10-15 mg/ ngy, sau tng dn ti 30-50 mg/ngy.
Chng ch nh: U t bo a crom (ty thng thn), glocom cp, suy mch vnh, nhi mu
c tim.
III. Thuc tc dng kiu ph giao cm

ACETYLCHOLIN CLORID
131
Bit dc: Covochol, Miochol,...
Cng thc:
Tn khoa hc: 2-Acetyloxy-N,N,N-trimethyl ethanaminium clorid

Tnh cht: Bt kt tinh mu trng, d ht m, mi c trng, v ng mn. Tan nhiu trong
nc, ethanol; hu nh khng tan trong ether. D b hng do nhit, kim, nht l dung dch
(thy phn).
nh tnh :
- o nhit nng chy.
- Phn ng ca ion Cl-.
nh lng:
- Phng php nh lng ion clorid bng phn ng thy phn nhm acetyl trong mi trng
kim.
- Phng php nh lng nit bng phng php Kjeldahl.
Cng dng: Lm gin mch trong vim tc ng mch chi hoc iu ha nhp tim trong cn
nhanh tim kch pht.
Liu dng: tim di da hoc tim bp 0,05-0, lg/ln, ngy tim 1-2 ln. Pha trc khi dng
(do ch phm khng bn trong dung dch nc).
PHYSOSTIGMIN SALICYLAT
Cng thc:
Tnh cht: Tinh th rt nh, khng mu, khng mi. nhit 15C, ch phm tan trong
100 phn nc, trong 24 phn ethanol 95, t tan trong ether.
nh tnh:
- Ha cht th vo ammoniac, bc hi dung dch thu c cn mu xanh nc bin. Ha cn
vo cn, cho thm acid acetic s c mu v c hunh quang, hunh quang ny tng ln khi
cho thm nc.
- Sc k lp mng, so vi physostigmin salicylat chun.
132
- Dung dch trong nc, thm FeCl3 5% cho mu tm (salicylat).
nh lng: phng php acid-base trong mi trng acid acetic-cloroform; dung dch chun
HClO4 0,1 M; ch th o th.
Tc dng - ch nh: phong b cholinesterase, c c tnh cao. Ch phm c s dng
trong nhn khoa iu tr glocom, ngoi ra cn c dng iu tr chng nhc c v lit
rut.
Thng dng dung dch 0,5-1% nh mt. C th dng ung v tim di da
Liu dng: ung 1mg/ln, 3mg/24h; tim 0,5mg/ ln, lmg/24h.
Pha trc khi dng.
NEOSTIGMIN BROMID
Tn khc: Synstigmin bromid; Philostigmin bromid
Cng thc:
Tn KH: (3-Dimethylcarbamoyloxyphenyl) trimethylammonium bromid

Tnh cht: Bt kt tinh mu trng, khng mi, v ng. D tan trong nc (1 g/0,5 ml); tan
trong ethanol.
nh tnh:
- Hp th UV: MAX 260 v 266 nm (H2SO4 0,5 M).
-Thy phn trong KOH to phenol (II) cho phm mu cam (III) vi acid p-
diazobenzensulfonic (I):
- Dung dch nc cho phn ng ca ion Br-.

nh lng: v c ha ri nh lng nit ton phn di dng NH3
Tc dng - ch nh: Neostigmin l cht tng hp t c hn physostigmin, c tc dng
phong b cholinesterase. c ch nh trong cc trng hp glocom hay gin ng t , co
mch ngoi vi, gim chc nng c trn (to bn, chng bng, lit rut- bng quang sau m).
Ngoi ra cn dng gii c mt s thuc nh thuc lm mm c, thuc hy ph giao cm.
IV. Thuc tc dng hy ph giao cm
133
ATROPIN SULFAT
Tn khc: Atropisol
Cng thc:
Tn KH: 1H, 5H-Tropan-3-ol ()-tropat sulfat (2:1) monohydrat

Tnh cht: Tinh th khng mu hoc bt kt tinh mu trng, khng mi, v ng.
D tan trong nc, ethanol, glycerin; khng tan trong ether, cloroform.
nh tnh:
- un cch thy n kh atropine trong HNO3 c; cho vi git dung dch KOH
3%/methanol; xut hin mu tm (phn ng Vitali):
- Cho kt ta vi thuc th chung alcaloid.

- Dung dch nc cho phn ng ion SO42- (vi BaCl2).
- Ph IR hoc sc k; so vi atropin sulfat chun.
nh lng:
- Phng php acid-base trong mi trng acid acetic khan; cht chun HCIO4 0,1 M; ch
th o in th.
- Ha mt lng ch phm cn chnh xc vo hn hp ethanol-cloroform trung tnh ri
chun bng dung dch NaOH 0,1 N, ch th phenolphthalein.
- nh lng atropine sulfat trong dung dch tim c th dng phng php o mu da vo
phn ng ca atropin vi acid picric to thnh atropine picrat c mu vng.
Tc dng ch nh: phong b h M. c dng :
- Chng co tht, dng ct cn hen ph qun, cha ho.
- Gim au do co tht c trn trong cc trng hp au bng do vim lot d dy, t trng, co
tht rut v ng tit niu.
- Gii c morphin, thuc cng ph giao cm, ng c cht ln hu c.
Dng bo ch: Vin 0,4 mg; ng tim 0,25 mg/ml; Dch mt 0,5-3%.
134
Liu ti a: ung 3mg/ 24h,2mg/ ln, tim di da lmg/ln, 2mg/ 24h
Ng c: Liu cao gy ng c, triu chng:
- St cao, nn, mt nh hng, o gic, mn khng d ng;
- Try tun hon, h hp c th t vong.
Tr em nhy cm hn: mt n hi co-gin c, lit no.
Gii c: Bng thuc muscarinic, acetylcholin...(tc dng i khng).
CHNG XI: THUC GIM AU V THUC H NHIT, GIM AU, CHNG

VIM.
Mc tiu:
1- Trnh by c tc dng, ch nh v phn loi thuc gim au loi opioid.Trnh by c
cng thc, tnh cht, cng dng, liu dng ca mt s thuc gim au opioid.
2- Trnh by c c ch tc dng v cc cu trc ha hc thuc gim au, h st, chng
vim khng steroid. Trnh by c cng thc cu to, tnh cht, cng dng, liu dng ca
mt s thuc gim au, h st khng steroid.
Ni dung:
Thuc gim au l cc thuc c tc dng lm gim hoc lm mt cm gic au cho bnh
nhn.
Phn loi cc nhm thuc gim au:
+Gim au mnh (gim au loi opiod).
+Gim au h nhit gim au chng vim
A. CC THUC GIM AU MNH (thuc gim au loi opiod):
Tc dng - ch nh:
Tc dng:
- c ch trung tm au, nng cao ngng au; lm gim hoc mt au (khng p ng kch
thch).
- To cm gic khoan khoi, tng chu thuc; tng liu v l thuc khi dng ko di (nghin).
Do gi l "thuc gim au gy nghin".
Ch nh:
- Con au d di: Chn thng, phu thut, ung th ...
- Mt s thuc c dng cha ho.
Phn loi:
135
Theo cu trc ha hc c th chia ra cc nhm sau:
1. Morphin v cc cht lin quan: Morphin, heroin, hydromorphon, oxomorphon, code in,
levophanol, detromethophan...
Cng thc chung:
2. Cc opiod tng hp khc:

Cc thuc tng hp trn c s n gin b khung ca morphine
Mc ch: tm kim hp cht c tc dng gim au nh morphine nhng khng gy nghin
v khng c ch h hp, c cu trc n gin hn.
Cc hp cht thuc b khung morphinan(I): cc hp cht c cu trc ging morphine nhng
t hn morphine 1 vng do A. Gm: Cyclorphan, Butorphanol,...
Cc hp cht thuc b khung benzomorphan(II): L cc hp cht c cu trc morphinan
thiu vng C c iu ch ra t nhng nm 1947-1955. Gm: pentazocine, phenarocine,....
Cc hp cht cha khung phenyl- piperidin(III): pethidine, Fentanyl,...
Cc hp cht cha khung phenyl propyl amin(IV): Methadone, Phenadoxone,...
3. Cht i khng opioid: Naloxone, Nalorphine, Nalmefene, Naltrexone

Cc cht ny tranh chp vi morphin ti receptor morphinic. Mt s cht va c tnh khng
morphin va c hot tnh ca morphin (v d nh nalorphin).
Tn v bit dc (2-265) Hot tnh morphinic Hot tnh khng morphine
Nalorphine 1 1
Naloxone 0 10-30
Natrexone
Levalorphane 0,8 3
Cyclazocine 4 4,5
Cyprenorphine 10 35
Mt s thuc:
MORPHINE HYDROCLORID
136
Bit dc: Epimor, Morphitec.
Cng thc:
Tn KH: 3,6-Dihydroxy-4,5--epoxy-7,8-dehydro-17-methyl morphinan.HCl

iu ch: ngi ta chit xut morphin t thuc phin
Tnh cht:
L tnh: Bt kt tinh trng hoc tinh th hnh kim, khng mu. D bin mu; mt nc trong
khng kh kh. Tan trong nc, glycerin, dung dch kim mnh; kh tan trong ethanol 96%.
Ha tnh: Tnh kh (do -OH phenol + dy ); tnh base.
nh tnh:
+ Cho ta vi cc thuc th chung ca alkaloid
+ Tnh kh: Vi Kali fericyanid to kali ferocyanid, cho mu xanh l vi Fe3+.
+ Phn ng ca OH phenol: To mu xanh tm vi FeCl3.
+ Dung dch cho phn ng ca ion Cl-.
+ Hp th UV: MAX 285 nm (dung dch nc).
+ Sc k hoc ph IR, so vi chun.
nh lng: Acid-base/CH3COOH; dung dch chun HCIO4 0,1M; ch th o in th.
Dc ng hc: ung pht huy tc dng chm hn tim. Thuc vo c bo thai, sa m v
no.
Ch nh: Morphin c ch nh trong nhng trng hp au d di nh au do si mt,
ung th giai on cui, nhi mu c tim, au do phu thut.... Trong phu thut, morphin
c dng gy m, gim au, gim lo lng. Ngoi ra cn c dng trong cc trng hp
mt ng do au, tiu chy.
Ngi ln: Tim di da 10 mg/ln; c th ti 100 mg/24 h.
Tr em > 5 tui: tim di da 2-10 mg/24 h.
- c ch trung tm h hp lm nhp th chm v su.
- Gy nghin sau khi dng thuc vi ngy n 1 tun.
- Bun nn, gim nhu ng rut dn n to bn, chn n.
Ng c: Liu cao lm mt tri gic, lit trung tm h hp gy t vong.
Gii c: Bng thuc i khng opioid: naloxon ...
Chng ch nh:
- Tn thng hoc phu thut s no.
- Suy h hp; thiu nng gan, thn.
137
- Ph n c thai v thi k cho con b; tr em < 5 tui.
Bo qun: Trnh nh sng. Bo qun theo ch thuc gy nghin.
PETHIDINE HYDROCLORID
Tn khc: Meperidine hyroclorid
Ngun gc: opiat tng hp.
Cng thc: C15H22ClNO2
Tn KH: N-Methyl-4-phenyl-4-carbethoxy piperidin hydroclorid

Tnh cht:
L tnh: Bt kt tinh mu trng, v chua ng; bin mu trong nh sng. D tan trong nc,
ethanol; t tan trong ether.
Ha tnh: Tnh kh; base.
nh tnh:
- Dung dch trong nc cho phn ng Cl-
- Dung dch trong nc cho ta vi dung dch acid picric.
- Ph IR hoc SKLM, so vi pethidin hydroclorid chun.
- Hp th UV: MAX 251; 257 v 263 nm.
nh lng: Acid-base/Et-OH 96%; dung dch chun NaOH 0,1M; ch th o in th.
Tc dng - Ch nh: Gim au km morphin 6-8 ln, t gy ng, t co c trn. c dng
thay th morphin chng cn au d di. Ngoi ra thuc hay c dng gy tin m,
iu tr glocom cp, nhi mu c tim cp.
Liu dng:
- Ung hay t hu mn : 25-50 mg/ ln X 1-3 ln/ ngy
- Tim bp hoc tim di da : 250mg/ 24 h
Dng bo ch: ng tim 25; 50, 75, 100 mg/ml. Vin nn 50, lOOmg. Thuc n 100 mg
Tc dng khng mong mun: Gy nn, chng mt, ra nhiu m hi. Qa liu gy try h
hp, tun hon.
Gii c morphin bng cc thuc i khng opioid: Naloxon...
Bo qun: Trnh nh sng; bo qun theo ch thuc gy nghin
FENTANYL CITRAT
138
Bit dc: Sublimaze; Leptanal
Cng thc:
Tn KH: N-(l-Phenethyl-4-piperidyl) propionanilid citrat (1:1)

Tnh cht: Bt kt tinh trng, khng mi, bn trong khng kh.Tan trong nc (1 g/40 ml);
tan nh trong ethanol; kh tan trong ether.
nh tnh:
- Ph IR, UV
- Phn ng ca citrat
nh lng: Bng acid perclorid trong mi trng khan.
Cng dng:
Fentanyl c tc dng gim au mnh hn morphin khong 100 ln nhng ngn hn, t1/2= 4 h.
c ch nh gim au trong phu thut, tin m, tng tc dng ca thuc m, phi hp vi
haloperidol kt hp tc dng gim au vi tc dng an thn.
Liu dng:
- Tim phu thut: tim bp 0,05 0,1 mg trc khi m
- Gim au sau phu thut: tim bp nh trn, sau 1-2 h c th tim nhc li Dng ho ch:
ng tim 0,05 mg/ml; 2 v 10 ml.
Tc dng khng mong mun: c th gy co c, h huyt p tm thi, kch ng ch tim.
Qa liu s c ch h hp; gii c bng naloxon.
Chng ch nh: Mang thai; ngi suy h hp, tun hon.
Bo qun: Theo ch thuc gy nghin.
NALOXONE HYDROCLORID
Bit dc: Nalone
Cng thc:
Tn KH: 3,14-Dihydroxy-4,5-epoxy-N-allyl morphinan-6-on
139
Tnh cht: Bt kt tinh mu trng; bin mu trong nh sng, khng kh.Tan trong nc, acid
long v kim mnh; tan nh trong ethanol; khng tan trong cloroform, ether.
Ha tnh: Tnh base, tnh kh.
nh tnh: - Ph IR hoc SKLM, so vi chun.
- Phn ng ca ion Cl-
nh lng: Acid-base/Et-OH 96%; dung dch chun NaOH 0,1 M; ch th o in th.
Tc dng - ch nh: Khng opioid bng phong b cnh tranh trn receptor. Tim IV pht
huy tc dng sau 2 pht, ko di 1-4 h (ph thuc liu). Thuc c dng khc phc tc
dng c ch thn kinh trung ong ca thuc gim au opioid.
Liu dng: - Ngi ln: tim IV 0,4-2 mg/ln; nhc li sau 2-3 h.
- Tr em: tim IV: 10 g/kg/24h
- Tim sau phu hy tc dng ca thuc gim au: 100-200 g.
Dng dng: ng tim 0,4 mg/ lml; 0,04 mg/ lml (cho tr em)
Tc dng ph: Liu iu tr t c biu hin ng k.
B. THUC GIM AU, H ST, CHNG VIM

(NSAID = Nonsteroidal Anti-inflammatory Drugs)
I. I CNG
L loi thuc c tc dng h st, gim au, chng vim khng c cu trc steroids. Khc vi
cc thuc opiat, NSAIDs l thuc gim au ngoi vi v khng c tc dng gy nghin. Nhng
thuc tiu biu ca nhm ny gm c aspirin, ibuprofen, diclofenac, v naproxen c s
dng rng ri trong iu tr t lu. Paracetamol (acetaminophen) c tc dng chng vim
khng ng k, nhng li c tc dng h st v gim au rt tt, nn i khi vn c xp
trong nhm ny.
C ch tc dng: do c ch COX lm gim tng hp PG do lm gim qu trnh gy st
nn c tc dng h st.
Hai loi COX:
- COX-1 thnh d dy, thnh mch, thn.
- COX-2 t chc m tn thng
Cc thuc gim au, h st, chng vim truyn thng c tc dng ln COX-1 v COX-2.
Thuc th h mi c ch chn lc COX-2, hn ch tc dng ph.
Thuc khng tc ng ln nguyn nhn gy st nn ch c tc dng iu tr triu chng.
II. Phn loi:
Da vo cu trc ha hc, chia thnh cc nhm sau:
- Cc dn cht ca acid salicylic: Natri salicylat, methyl salicylat, salicylamid...
- Dn cht ca pyrazolon: antipyrin, phenylbutazon.
- Dn cht ca aniline: paracetamol, phenacetin...
- Dn cht ca acid indol v inden acetic: indomethacin, etodololac...
- Dn cht ca acid aryl propionic: ibuprofen, naproxen...
- Dn cht ca acid anthranilic: acid mefenamic, acid meclofenamic...
140
- Dn cht ca acid aryl acetic: diclofenac, ketorolac...
- Cc oxycam: piroxicam, meloxicam...
- Cc cht khc: Celebrex, nimesulid.
III. Mt s thuc:
ASPIRIN
Tn khc: Acid acetylsalicylic
Bit dc: pH 8; Aspgic
Cng thc:
Tn khoa hc: Acid-2-acethoxybenzoic

Tnh cht:
L tnh: Bt kt tinh mu trng, khng mi hoc mi dm nh. Thy phn chm khng kh
m. Kh tan trong nc; d tan trong ethanol 96%; tan trong ether, cloroform; tan trong cc
dung dch kim hydroxyd v carbonat.
Ha tnh: Tnh acid.
nh tnh:
- Thy phn aspirin bng dung dch.NaOH 10%; kt ta bng H2SO4.
Phn ta cho mu xanh tm vi FeCl3 5% (acid salicylic).
COONa OH COOH OH
+H2O, NaOH, to HCl

Trung ha dch lc, thm FeCl3 5%: mu hng- (acetat)
- Xc nh acid salicylic: tc dng vi FeCl3 to phc mu nu.
- Xc nh acid acetic: tc dng vi alcol ethylic trong mi trng acid to ethyl acetat c
mi thm.
- Ph IR, so vi acid acetylsalicylic chun.
nh lng: Acid-base/ethanol-nc; dung dch chun NaOH 0,1 M; ch th
phenolphtalein.
141
Cng dng: Aspirin c ch COX -1, 2 ng thi gy gin mch ngoi vi tng thot nhit. C
tc dng gim au, h nhit, tng thi tr acid uric qua nc tiu.
Aspirin c ch nh trong cc trng hp:
- au u do cm st; au mnh my.
Ngi ln ung 0,3-0,9 g/ln/4-6 h; ti a 4 g/24 h.
Tr em < 6 tui ung 50-65 mg/kg/4-6 h.
- Huyt khi (tiu cu tp kt gy cc mu ng):
Ngi ln ung 0,5-1 g/ln X 3 ln/24 h.
Hn ch dng aspirin cho tr em do thn kinh cha n nh.
- Dung dch ASA, bi tr hc lo, lang ben, nm da khc.
Dng bo ch: Vin bao tan trong rut 100; 250 v 500 mg.
Thuc phi c ung vo lc no.
- c ch tim, thng phi hp vi thuc tr tim
- Kch ng d dy, do hay dng cc mui hoc dng bo ch c bit
Chng ch nh: Vim lot d dy-t trng; chy mu kh cm.
Thuc khng dng khi ang ung aspirin: Chng ng mu, hng thn, NSAID v
glucocorticoid (GC).
METHYL SALICYLAT
Bit dc: Salonpas; Mialgin
Cng thc: C8H8O3
Tn KH: 2-Hydroxybenzoat methyl

Tnh cht: Cht lng khng mu hoc vng cam, mi c trng; b bin mu
khi tip xc vi nh sng. T trng (25C) = 1,84. Kh trn ln vi nc, trn ln vi ethanol
(96%), du bo.
Tc dng- ch nh: Gim au khp, c, bong gn... D thm qua biu b vo su bn trong
pht huy tc dng. Methyl salicylat c s dng bo ch cc dng thuc dng ngoi: xoa
bp khi au c, khp, bong gn, au lng, cng c, v d:
Methyl salicylat 25%/du lc: bi 3-4 ln/ngy.
Bng dnh Salonpas (methyl salicylat 15%): dn ch au.
Tc dng khng mong mun: Bi lin tc, liu cao s hi th gic do gii phng alcol
methylic trong c th, d ch l dng ngoi.
142
PARACETAMOL
Tn khc: Acetaminophen
Cng thc:
Tn KH: p-Hydroxyacetanilid
Tnh cht:
L tnh: Bt kt tinh trng, v ng nh; bin mu chm trong nh sng, khng kh.
Kh tan trong nc; tan trong ethanol, dung dch kim.
Ha tnh: Tnh kh (-OH phenol)
nh tnh:
- Dung dch trong nc cho mu xanh tm vi FeCl3 5% (-OH phenol).
- Thy phn,gii phng p-hydroxyanilin v acid acetic;
+Acid acetic: c mi chua
+ p-hydroxyanilin cho phn ng c trng ca amin thm I (phm mu nit);
- Ph IR hoc SKLM, so vi paracetamol chun.
- Hp th UV: MAX 250 nm (Et-OH); 257 nm (NaOH 0,1 M)
- Phn ng phn bit vi phenacetin: un paracetamol vi dung dch HC1 thy phn, thm
thuc th Kali bicromat th c ta mu tm (khc vi phenacetin l khng chuyn sang mu
hng)
nh lng:
Quang ph UV: o 257 nm (NaOH 0,1 M).
o nitrit
Cng dng:
Paracetamol c tc dng gim au, h nhit. Thi gian bn hy 1-4 h. Tc dng gim au
mnh v ko di hn aspirin. Kh nng gy kch ng ng tiu ha thp hn aspirin.
Hp thu khi ung; sn phm chuyn ha c vi gan
Paracetamol c ch nh trong cc trng hp st, au u, dy thn kinh, au c, thp
khp.
Liu dng:
- Ngi ln ung 0,3-0,6 g/ln/4-6 h; ti a 4 g/24 h.
- Tr em < 5 tui ung 60-250 mg/ln.
Dng bo ch: vin nn, vin nang 0,1; 0,2 v 0,5 g paracetamol, vin si, vin t...
Chng ch nh: Suy gan, thn; mn cm vi paracetamol.
Ng c paracetamol: Khi ung > 10 g paracetamol trong 24 gi.
Triu chng xut hin chm bao gm ti nht, bun nn, au bng, chn n. Ng c gan:
hn m, ph no, c th ti t vong.
Gii c: Tim hoc ung antidote: acetylcystein, methionin.
(ch hiu qa trong vng 15 h sau khi xut hin ng c).
INDOMETHACIN
143
Bit dc: Dolcidium; Indocin
Cng thc: C19H16ClNO4; ptl: 357,8
TnKH: Acid l-(4-clorobenzoyl)-5-methoxy-2-methylindol-3-yl acetic

Tnh cht:
L tnh: Bt kt tinh mu trng nh vng; bin mu trong nh sng. Khng tan trong nc;
tan trong ethanol, aceton; b thy phn trong dung dch kim. Bn pH < 7,
Ha tnh: Tnh acid yu.
nh tnh:
- Ph IR hoc SKLM, so vi chun
- Hp th UV: MAX 318 nm (Me-OH/HCl)
- Dung dch trong ethanol thm hydroxylamine, thm tip HC1 v dung dch FeCl3 cho mu
hng tm.
nh lng:
- Acid-base/aceton-nc; dung dch chun NaOH 0,1 M; ch th phenolphtalein.
- Quang ph UV hoc HPLC
Cng dng: Indomethacin c tc dng chng vim, gim au mnh; h st l th yu. Hp
thu ng tiu ha v trc trng, km hp thu tr s sinh. c ch nh trong cc trng
hp:
- au mnh my, xng khp, thn kinh...
Ngi ln ung 25-50 mg/ln; 2-3 ln/24 h.
- Bnh gout: ung 100 mg/ln; tip sau 50 mg/ln X 3 ln/24 h.
Dng bo ch: Vin nang 25; 50 v 75 mg; thuc n 50 mg.
Tc dng khng mong mun: chng mt, nhc u, vim lot d dy t trng.
Chng ch nh: vim lot d dy t trng, ngi c thai, cho con b.
Bo qun: Trnh nh sng
DICLOFENAC NATRI
Bit dc: Difenac; Voltaren
Cng thc:
144
Tn KH: 2-(2,6-Dicloroanilino) phenylacetat natri
Tnh cht:
L tnh: Bt kt tinh mu trng, ht m; bin mu trong nh sng. Tan trong nc, methanol,
ethanol; t tan trong aceton.
Hp thu tt ng tiu ha, trc trng; thi gian bn hy 1-2 h.
Ha tnh: Tnh kh (amin II); dung dch trong nc cho pH kim.
nh tnh:
- Ph IR hoc SKLM, so vi chun.
- Dung dch trong methanol, thm HNO3 c: Mu nu.
- Cho phn ng ca ion Na+.
nh lng: Phng php acid-base
Cng dng: Diclofenac natri c tc dng chng vim, gim au, h st
c ch nh trong cc trng hp au do vim khp, tht lng, au thn kinh, au bng
kinh....
Ngi ln: ung 75-150 mg/24 h; chia 3 ln ; t trc trng 100 mg/ln.
Tim IM su, chm: 75 mg/ln; 1-2 ln/24 h; t 2 ngy.
Tr em: ung hoc t trc trng 1-3 mg/kg/24 h; chia 2-3 ln. Bi ti ch gim au: Thuc
m 10%.
Dng bo ch: Vin 25; 50 v 75 mg; ng tim 75 mg; Kem 10%.
Chng ch nh: lot d dy, suy t bo gan, suy thn
CHNG XII: THUC TR BNH DO K SINH TRNG
Mc tiu:
1. Trnh by c cc thuc iu tr giun, sn thng dng bao gm tn thuc, cng thc cu
to, cc tnh cht l ha v ng dng cc tnh cht trong kim nghim, ch nh dng ca
mi thuc.
2. Trnh by c cc thuc iu tr bnh st rt thng dng bao gm tn thuc, cng thc
cu to, ch nh dng ca mi thuc.
3. Trnh by c cc thuc iu tr l amp v trichomonas thng dng bao gm tn thuc,
cng thc cu to, cc tnh cht l ha , ch nh dng ca mi thuc.
Ni dung:
A. THUC CHNG ST RT
I. i cng:
Mui Anophen k sinh trng st rt (dng thoa trng) tuyn nc bt. Khi t ngi thoa
trng vo mu ti gan, tin hnh sinh sn v tnh lm v cc t bo gan.
Giai on tin hng cu
- Loi facirarum: tt c cc loi k sih trng xm nhp vo mu
145
- Loi vivax v malaria, 1 phn k sinh trng vo mu, 1 phn s vo t bo gan v sinh sn
tip (th ngoi hng cu), giai c ny ko di nhiu thng v nhiu nm l nguyn gy ra st
rt ti pht ngi bnh.
T gan, KST vo mu,chng xm nhp vo t bo hng cu. KST tip tc sinh sn v tnh v
ph v hng cu gii phng hng lot KST cng vi c t ca chng chnh l nguyn
nhn gy st. Sau chng tip tc n cc hng cu khc :
- Faciparum, vivax, oval l 48h (st cch nhit).
- Malaria l 72h (gy st cch 2 ngy).
Mt s KST khng vo hng cu m chuyn thnh cc th hu tnh l giao t c v giao t
ci to thnh th giao t. Khi mui Anophen ht vo d dy ca chng, mui ci KST pht
trin v sinh sn hu tnh c th mui to ra thoa trng v tip tc chu k.
Trong 4 loi KST gy st rt, th loi faciparum gy st rt c t l cao nht v c tnh.
* Phng st rt:
- Dit mui v trnh mui t.
- Nng cao sc khng ca c th.
- Ung thuc phng: Thng p dng khi chun b i vo vng st rt. cn ung theo ng
ch nh.
Phn loi thuc st rt:
Da vo v tr tc dung ca thuc trn qua trnh sinh sn v tnh ca loi Plasmodium trong
c ngi, c th chia cc thuc thanh nhm sau:
1. Thuc ct cn st rt:
L nhm thuc c tc dungnj dit th v tnh ca KSTSR trong hng cu, ngn chn c
cc cn st. Khng tc dng vi st rt vi cc thi k khc.
Thuc in hnh: Quinin Cloroquin, Artemisinin.
2. Thuc chng ti pht (thuc iu tr tit cn):
Dit KSTSR thi k ngoi gng cu v tiu dit cc giao t con li .
Thuc in hnh: Primaquin, Plasmoquin.
3. Thuc phng st rt:
Ngn chn v tiu dit KSTSR thi k tin hng cu.
Thuc in hnh: Pyrimethamin.
4. Thuc chng ly lan:
Dit giao t hoc lm ung giao t ca KSTSR (lm mt kh nng giao phi ca giao t
trong c th mui).
Thuc in hnh: Primaquin, Plasmoquin.
II. Mt s thuc iu tr st rt c th:
CLOROQUIN PHOSPHAT
Bit dc: Aralen, Resochin.
Cng thc:
146
Tn KH: 7-Cloro-4-[(4-diethylamino-l-methylbutyl)amino] quinolin phosphat
iu ch: Ngng t 4,7-dicloroquinolein vi N,N-diethylamonopentylamin
Tnh cht: Bt kt tinh trng, khng mi, v ng.
D tan trong nc, khng tan trong ethanol.
nh tnh:
- Ph IR hoc sc k, so vi cloroquin phosphat chun.
- Hp th UV: MAX 220; 235; 256; 329 v 342nm (nc).
- Dung dch nc cho kt ta vng vi amoni molypdat (PO43-).
nh lng: Acid-base/acid acetic khan; HC14 0,1M; o in th.
Tc dng: Dit th phn lit p. falciparum, p. vivax; giao t p. vivax.
Ung, hp thu nhanh v gn nh hon ton. T1/2 khong 4 tun.
Ch nh: Liu dng tnh theo cloroquin base.
- D phng: ung trc 1-2 tun + trong vng + 6 tun sau ra khi.
NL, ung 300mg/ln/tun. TE, ung 5-8 mg/kg/ln/tun.
- Ct cn st: NL, ung ngy u 600 mg/6-8 h > 300 mg
> Ngy th hai + th ba: 300 mg/ln/24 h. (3 ngy).
TE, ung 10 mg/kg/6 h; tip sau rt i mt na.
Cp: tim IM 200-250 mg/6 h (thuc tim cloroquin hydroclorid).
Phi hp vi cc thuc tr st rt khc (tr vi quinin).
Tc dng khng mong mun: Gim th lc, thnh lc; lon cng thc mu. cn theo di th
lc sut thi gian iu tr bng cloroquin.
ARTEMISININ
Ngun gc: Chit t cy Thanh cao (hao) hoa vng {Artemisia annua L. , h Hoa cc-
Asteriaceae). Lng sn. Trung quc: Qinghaosu
Cng thc: Sesquiterpen vi lin kt peroxide trung tm.
147
Tn KH: Octahydro-3,6,9-trimethyl-3,12-epoxy-12i-pyrano[4,3-j]-l,2- -benzodioxepin-10(3
H)-on.
Tnh cht: Bt tinh th hnh kim khng mu, v hi ng.
Cu peroxid d b phn hy, mt hot tnh.
Khng tan trong nc; tan trong ethanol, d ha v dung mi hu c khc.
nh tnh
- Ph IR hoc SKLM, so vi artemisinin chun.
-Vi KI, gii phng I2, lm xanh tinh bt (peroxid).
nh lng: Quang ph UV; o 292 nm (Et-OH + NaOH 0,05 M).
Ph tc dng: Th phn lit p. falciparum v p. vivax .
D vo thn kinh trung ng, hiu qa vi st rt c tnh (th no).
Ct cn nhanh v ti pht nhanh. Thi hn tc dng ngn.
Hp thu khi ung hoc t trc trng.
Ch nh:
- Ct cn p. falciparum v p. vivax, k c th no: t 4-5 ngy.
NL, ung ngy u 1 g/ln X 2 ln /24 h; ngy sau 500 mg/ln.
Thuc n: ngy u 1,25 g; tip sau 0,75 g/ngy; t 2-3 ngy.
Phi hp vi primaquin, pyrimethamin v sulfadoxin lm sch nhanh KST v trnh ti
pht.
Dng bo che: Vin nang 250 mg; thuc n 0,75 g.
Kch ng ng tiu ho: bun nn, nn, au bng, tiu chy; nhc u, chng mt, hoa mt.
Thng nh v thong qua.
Bo qun: Trnh nh sng, khng kh. ch mt.
* Cc dn cht ca artemisinin:
T artemisinin, bn tng hp ra artesunat, artemether, arteether, l cc dn cht c hiu lc
dit KST cao hn artemisinin.
Artesunat: To mui tan trong nc vi NaHC3; tim bp, tim tnh mch. Artemether,
arteether: Tan trong du; ch dng tim bp.
ARTESUNAT
L ester ca artemissinin vi acid succinic.
Cng thc:
148
Tnh cht: Bt kt tinh mu trng, mi nh. Kh tan trong nc; tan trong aceton, cloroform,
ethanol; d tan trong kim, dicloromethan.
nh tnh:
- Ph IR hoc SKLM, so vi chun.
- Trn vi cloroform, cch thy ti gn cn; ngui, thm vanilin 2%/H2S04: Mu .
nh lng:
Quang ph UV; o 289 nm; so vi chun (Et-OH + NaOH 0,1M).
ph tc dng: Tng t artemisinin.
Ch nh: Tng t artemisinin.
Liu dng (WHO):
Ngy u: 4 mg/kg/24 h > 2 mg/kg/24 h; t 6 ngy.
Phi hp vi primaquin: ung 4 mg/kg/24 h; t 3 ngy.
Dng bo ch: Vin 200 mg, l bt pha tim, km NaHC03; pha khi dng.
Bo qun: Trnh nh sng v nhit cao.
B. THUC IU TR BNH GIUN SN
I. i cng
Giun sn k sinh thuc ng vt a bo. Bnh giun sng ngi rt ph bin trn th gii.
Trn 2 t ngi l vt ch ca cc loi giun sn khc nhau v s lng ny ngy cng tng do
di dn, du lch, tng din tch t canh tc, pht trin c sn di nc... V vy, thuc dng
iu tr giun sn l v cng quan trng.
Phn loi thuc iu tr giun sn:
Da vo hnh th k sinh trng chia thuc tr giun sn thnh 2 nhm:
- Thuc tr giun: Tc dng trn KST trong rut ( Mebendazol, Albendazol,...), ngoi rut
(Diethylcarbamazin, Ivermectin).
- Thuc tr sn: Tc dng sn rut (Niclosamid, Quinacrin), ngoi rut (Cloroquin,
Praziquantel).
II. Mt s thuc c th:
ALBENDAZOL
Bit dc: Zentel; Albenza
149
Cng thc:
Tn KH: 5-Propylthio-1H-benzimidazol-2-yl carbamatmethyl
Tnh cht: Bt kt tinh trng-vng nu; bin mu trong khng kh, nhssng. Kh tan trong
nc, ethanol; d tan trong acid formic m c.
Ha tnh: Tnh base; carbamat khng bn vi m v nhit (thot C02).
nh tnh:
Ph IR hoc sc k, so vi chun.
un si ch phm vi dung dch natri hydroxyd long. Acid ha dung dch gii phng kh
cacbonic lm c nc vi trong.
nh lng: Bng phng php o acid trong mi trng khan, dung mi l hn hp acid
acetic v acid formic khan, ch th o in th.
Tc dng- ch nh:
Albendazol c tc dng dit giun lng rut, giun di tr t chc; sn nang. c ch nh trong
cc trng hp:
- Nhim giun kim, mc, a, xon rut:
NL, TE > 2 tui, ung lc i liu n 400 mg; nhc li sau 3 tun.
- Nhim sn nang: 3 t 28 ngy; khong cch t 14 ngy.
Ngi > 60 kg, ung 400 mg/ln; 2 ln/24 h.
Ngi < 60 kg, ung 7,5 mg/kg/ln; 2 ln/24 h.
- Phi hp tr giun xon c: ung cng liu giun rut, cng thc n m.
Dng bo ch: Vin 200 v 400 mg.
Tc dng khng mong mun: Hay gp ri lon tiu ho, au u, bun nn.
150
Chng ch nh: Mang thai 3 thng u, tr em < 2 tui; d ng thuc.
MEBENDAZOL
Bit dc: Vermox, Fugacar.
Cng thc:
Tn KH: N-(5-Benzoyl-li/-benzimidazol-2-yl) carbamat methyl
Tnh cht: Bt mu trng- vng nht, nh; bin mu trong khng kh, nh sng. Tan trong
acid formic m c; hn hp isopropanol-acid formic.Khng tan trong nc, ethanol,
chloroform.
nh tnh:
- Phn ng mu: Trn 10mg mebendazol vi 5ml ethanol 96%, thm lml dd dinitrobenzen
1% pha trong ethanol 96% v lml dd NaOH 2M, trn u: xut hin mu vng m.
- Hp th UV:
Dung dch 1: Ha tan 30mg mebendazol vo 2rnl acid formic > 76%, pha long bng
isopropanol thnh 100ml
Dung dch 2: Ly 2,5ml dung dch 1, pha long bng isopropanol thnh l00ml.
o hp th ca d.d.2 khong sng 230-320nm, mu trng l dung dch acid formic

0,05% trong isopropanol: 2 cc i hp th 247nm v 312nm
- Ph IR hoc sc k, so vi chun.
nh lng:
- Acid-base/acid acetic + formic; HCIO4 0,1 M; o in th.
-Quang ph UV: o 247nm (acid formic + isopropanol)
Tc dng: c hiu tr giun lng rut; giun xon c.
151
C ch tc dng: c ch khng thun nghch ti hp thu glucose, gy teo giun. Hp thu rt
km rut, tng hp thu trong thc n nhiu m .
Ch nh: Nhim giun ng tiu ha: ngi ln v tr em ln hn 2 tui, ung:
- Nhim giun kim : liu n 100 mg/ln; nhc li sau 2-3 tun.
- Nhim giun a, giun mc: 100 mg/ln X 2 ln/24 h; t 3 ngy.
C th ung liu n 500 mg.
- Nhim giun xon c: Cng liu giun a, ung cng thc n giu m.
Dng bo ch: Vin 100 v 500 mg.
Tc dng khng mong mun: Hay gp ri lon tiu ho, au u, bun nn.
Chng ch nh: Mang thai 3 thng u, tr em < 2 tui; d ng thuc.
NICLOSAMID
Bit dc: Niclocide; Yomesan
Tn KH: 5-Cloro-N-(2-cloro-4-nitrophenyl)-2-hydroxybenzamid
iu ch: Cho t t PCl vo dung dch xylen ang si cha acid 5-clorosalicylic
v 2-cloro-4-nitroanilin vi t l mol nh nhau. un nng tip 3 gi. ngui niclosamid kt

tinh. Kt tinh li t ethanol.
Tnh cht: Bt tinh th mn, mu kem; bin mu ngoi nh sng. Khng tan trong nc; tan
nh trong ethanol, aceton.
nh tnh:
Kh bng:Zn/HCl (cch thy) ->
- Amin thm I: cho phn ng to phm mu nit.
152
-Acid salicylic: To mu tm vi Fe3+
Ph IR hoc sc k, so vi chun.
nh lng:
Bng phng php o kim, dung mi l hn hp aceton v methanol, cht chun

terbutylammonium hydroxyd 0,1M, ch th o in th.
Kh ha thnh nhm amin thm, nh lng bng php o nitrit.
Tc dng: Vi hu ht sn dy k sinh lng rut. Hp thu rt t rut.
C ch tc dng: c ch hp thu glucose khi thuc tip xc vi u sn.
Ch nh: Nhim sn rut. Ngi ln, ung:
Nhim sn b, sn c: ung 1 g; sau 1 gi ung tip 1 g.
Nhim sn ln: ung liu duy nht 2 g.
Nhim sn ln: Ngy u ung 2 g; 5 ngy tip ung 1 g/24 h.
Tr em: Ty theo tui, ung 1/4 -1/2 liu ngi ln.
Cch dng: Sau ba sng, nhai nt vin thuc trc khi nut; km thuc ty mui nh
magnesi sulfat d tng sn ra ngoi.
Dng bo ch: Vin 0,5 v 1 g.
Tc dng khng mong mun: Bun nn, nn, au bng, ri lon tiu ha.
C. THUC DIT AMIP, TRNG ROI
I. i cng
* L amip
Do amip Entamoeba hystolytica gy ra i trng.
* Vng i amip v gy bnh
Th kn (bn ngoi)
153
- au qun bng, lin tc mun i ngoi (5-10 ln/ngy).
- i nhiu ln, t phn, cht nhy c ln mu, mi. Mt mi.
II. THUC CHNG L AMIP
METRONIDAZOLE
Bit dc: Flagyl; Klion
Cng thc:
Tn KH: 2-(2-Methyl-5-nitroimidazol-l-yl) ethanol
iu ch: Cho 1 lng d nhiu ethylen clorohydrin ngng t vi 2-methy-5- nitroimidazol

bng cch un nng . Tch clorohydrin tha, chit cn bng nc, kim ha dch chit ri
chit bng cloroform. Bc hi dch chit cloroform c metronidazol th. Kt tinh li t
ethylacetat.
Tnh cht: Bt kt tinh mu trng hi vng nu, khng mi, v ng. Kh tan trong nc v
dung mi hu c.
nh tnh:
Tnh base: Tan trong acid v c long; to ta vi thuc th alcaloid Tin hnh th: Ha tan
0,lg cht th vo 4ml acid sulfuric 3%; thm 2m acid piric 1%: xut hin ta mu vng.
154
Phn ng ca nitro thm: Kh bng H mi sinh thnh amin thm I, sau to phm mu
nit.
Tin hnh:
+ ng nghim 1: un nng trn ni cch thy trong 5-10 pht hn hp gm: l0mg cht th,
l0mg km bt, lml nc v 0,5ml HC1 long, ngui, lc ly dch lc. Thm 1-2 git
NaN02 0,1M vo dch lc, trn u.
+ ng nghim 2: Ha tan khong 0,lg -naphtol vo 2ml NaOH long .
t t dch ng 2 vo ng 1: xut hin mu .
Phn ng mu: Ha 10mg cht th vo 2ml NaOH 10%, un nh: hn hp c mu tm ,

mu chuyn sang vng khi acid ha bng HC1 long.
nh lng:
Acid-base/acid acetic khan; HCIO4 0,1 M; o in th.
Quang ph UV: o 277 nm (HC10,1 M).
Tc dng: Dit amip, trng roi (Trichomonas vaginalis), vi khun ym kh. Hp thu ng
tiu ha, sinh kh dng 100%. ti/2 (HT) = 8 h.Thuc vo c bo thai v sa m.
Ch nh:
- L amip trong v ngoi lng rut, ung l ng ch yu:
Ngi ln: 500-750 mg/ln X 3 ln/24 h; t 5 ngy.
Tr em: 1/4 n 1/2 liu ngi ln, ty theo tui.
Nng: Truyn 500-750 mg/ln X 3 ln/24 h; t 5 ngy.
- Nhim T.vagnalis sinh dc: ung 2 g/24 h hoc t thuc n; 2 ngy.
- Phi hp iu tr lot d dy-t trng do H. pylori (xem phc ).
Dng bo ch: Vin 250 mg; n 500 mg; Thuc tim 500 mg/100 ml.
Tc dng khng mong mun: Bun nn, chn n, kh ming, v kim loi.
Thn trng: Ph n mang thai v thi k cho con b.
155
CHNG XIII: THUC KHNG HISTAMIN H1
Mc tiu hc tp:
1. V c cu trc chung ca thuc khng histamin H1. Nu c cch phn loi theo cu
trc ha hc v s lin quan gia cu trc v tc dng ca thuc khng histamin H1.
2. V c cng thc cu to, nu tnh cht l ha v ng dng php th kim nghim; tc
dng v cng dng ca cc thuc trong ni dung bi hc.
NI DUNG BI HC:
I. I CNG:
Histamin l cht ni sinh, to ra t Histidin, c vi tr sinh l nht nh.
Histamin trong c th tn ti 2 dng: dng t do c hot tnh v dng lin hp (Protein-

histamin) khng c hot tnh (gi tr Trong t bo mast).
Do tc ng khc nhau (khng nguyn) i vi c th, lm cho histamin v cc cht trung

gian dng lin hp c gii phng thnh dng t do theo c ch khng nguyn- khng th
v gy ra tnh trnh bnh l l D ng.
Histamin gn vo th th H1 c nhiu thnh mch, c trn rut, t cung, kh qun, ph

qun v cc t chc mi da,...
D ng, triu chng:
- Ni m ay, ph n, sung huyt, mt...
- Hen xuyn (co tht ph qun).
- au bng, bun nn, nn (co tht c trn tiu ha).
- Chy nc bt, nc mt... (tng tit).
Tc nhn gy d ng: Cht l, phn hoa, tri lnh,....
156
Tc dng dc l ca histamin.
Tim: Co c trn, gin mao mch; (ung b phn hy).
Tng tnh thm, lm mt huyt tng + protein.
mt, da nng, h HA; tng tit (nc bt, nc mt...).
S dng: Thm d chc nng mt s thuyn ni tit (tim 0,5 mg).
II. THUC CHNG D NG
1. Thuc phong b th th H1 (Gi tt: Khng histamin H1)
Phn loi:
1. Theo cu trc ha hc:
1. D/c ethanolamin: Diphenhydramin . HCl

R1
CH-O-CH2CH2-N
R2
2. D/c ethylendiamin: Tripelennamin . HCl

R1
N-CH2CH2-N
R2
3. D/c propylamin: Dexclopheniramin maleat

R1
CH-CH2CH2-N
R2
4. D/c phenothiazin: Promethazin . HCl
5. D/c piperazin: Cyclizin . HCl
6. D/c piperidin: Diphenylpyralin. HCl
Lin quan cu trc v tc dng:
157
- Cc thuc v hnh thc cu to c bn u c nhm aminoethyl guioongs histamin.
- Dn cht gn halogen thng lm tng hot tnh , v tr u tin l para ca nhn phenyl.
III.MT S CH PHM:
Dn cht propylamin
CLORPHENIRAMIN MALEAT
Cng thc:
Tn KH: 3-(p-Clorophenyl)-3-(2-pyridyl) N,N-dimethylpropylamin maleat
iu ch: Xem sch HD I.
Tnh cht: Bt kt tinh mu trng, khng mi.
Tan trong nc, ethanol, cloroform; tan t trong ether, benzen.
nh tnh:
Ph IR hoc SKLM, so vi chun.
Hp th UV: MAX 265 nm (HCl 0,1 M)
Acid maleic: Tch phn clopheniramin base (NaOH);
Dch lc (acid maleic): un cch thy vi nc Br2 v thuc th resorcinol/H2SO4c: Mu

xanh lam.
nh lng: Acid-base/CH3COOH khan; HClO4 0,1 M; o in th.
Tc dng: Khng histamin th h I; khng cholinergic, an thn.
Chnh, liu dng:
- D ng (chung ca thuc khng histamin H1); shock phn v.
- Phi hp vi thuc gim au h nhit (vin Decolgen,...).
158
- Vi clorpheniramin maleat: NL, ung 4 mg/4-6 h; ti a 24 mg/24 h; vin g/p chm: 1
vin/ln. C th tim IM, di da, IV chm: 10-20 mg/24 h.
- TE, theo tui: 1-2 mg/ln: 2 ln/24 h; ti a 6-12 mg/24 h.
- Vi dexclopheniramin maleat: NL, ung 2 mg/4-6 h.
Dng bo ch: Vin 2; 4; 8 v 12 mg; vin g/p chm 8 v 12 mg.
Tc dng KMM: Chung ca thuc khng histamin H1, th h I.
Chng C: Nh phn chung. Hen cp; tr s sinh. Bo qun: Trnh nh sng.
Dn cht ethanolamin
DIPHENHYDRAMIN HYDROCLORID
Cng thc:
Tn KH: 2-(Diphenylmethoxy)-N,N-dimethylethylamin hydroclorid
Tnh cht: Bt kt tinh trng, khng mi.
D tan trong nc, alcol v cloroform, khng tan trong ether.
nh tnh: Ph IR, SKLM
- Ph/ mu: Thm H2SO4 vo 0,5 ml d.d.5%: Vng m; thm 15 ml nc + 5 ml cloroform,

lc: Lp cloroform mu tm.
nh lng: Acid-base/ethanol 96%; NaOH 0,1 M; o in th.
Tc dng: Khng histamin hiu lc cao; chng nn, ho; an thn. Thi hn t/d 4 - 6 h;
Thuc thm nhp nhau thai, sa m.
Ch nh:
159
- Nn do say tu xe; mt ng do ri lon thn kinh nh: NL, ung: 25-50 mg/ln 3-4 ln/24
h. Tim (IV hoc IM su): 10-50 mg/ ln. TE, ung 6,25-25 mg/ln 3-4 ln/24 h. Ti a
300 mg/24 h (cho c ngi ln, tr em).
- Phi hp vi thuc ho, thuc gim au h nhit.
- Bi da tr nga dng: Kem 1-2%: bi 3-4 ln/ngy.
Dng b/c: Vin 12,5-50 mg; thuc tim 10 v 50 mg/ml; Kem 1- 2%.
Tc dng KMM:Ri lon tiu ho, h hp, tim mch, th gic.
Chng C:Mn cm vi thuc, tr s sinh; hen ph qun cp.
Dn cht phenothiazin
PROMETHAZIN HYDROCLORID
Cng thc:
Tn KH: 10-[(2-Methyl-2-dimethylamino)ethyl] phenothiazin hydroclorid
iu ch: Xem HD I.
Tnh cht:Bt mu trng, khng mi. Kch ng da, nim mc.
Bin mu/khng kh, nh sng (xanh). D tan trong nc, tan trong alcol; kh tan/dm hu
c.
Ha tnh: Base; tnh kh (nhn phenothiazin, amin III).
nh tnh: Ph IR hoc SKLM
- Ha tan vo HNO3c: Mu hng.
160
- Dung dch/nc kt ta vi thuc th chung alcaloid.
nh lng: Acid-base/ethanol 96%; NaOH 0,1M; o in th.
Tc dng: Khng histamin H1; an thn, gy ng, chng nn.
Ung, t trc trng: Hp thu tt; tc dng ko di > 12 h.
Ch nh: Ung, tim IV, tim IM su, t trc trng:
- D ng: NL: 12,5-25 mg/ln 4-6 ln/24 h; TE: 1/2 liu NL.
- Kh ng: NL: 25-50 mg; TE ung 1/2 liu ngi ln.
- Nn: NL: IM, t 12,5-25 mg/ln; TE: 0,25-0,5 mg/kg/4-6 h.
- Tin m: Ung ti hm trc 50 mg (NL) v 12,5-25 mg (TE).
Dng bo ch: Vin, thuc n: 12,5; 25 v 50 mg; Siro 6,25 v 25 mg/5 ml; thuc tim 25
v 50 mg/ml.
Tc dng KMM:Ng g, lon th, kh ming, b i.
161
THUC AN THN, GY NG, CHNG NG KINH
MC TIU HC TP:
1. Nu c khi nim v thuc gy ng, an thn v chng ng kinh.

2. Trnh by c phn loi, cu to ha hc, tnh cht l ha v tc dng chung ca nhm
dn cht acid barbituric, benzodiazepin v thuc chng ng kinh.
3. Trnh by cng thc cu to, phng php iu ch, tnh cht l ha, ng dng tnh cht
trong pha ch, bo qun, kim nghim v ch nh ca cc thuc trong bi hc.
NI DUNG
Thuc ng l thuc c ch thn kinh trung ng, to ra trng thi bun ng v a dn n

gic ng tng t nh gic ng sinh l.
Thuc an thn l thuc lm gim kch thch thn kinh trung ng, gim qu trinh hng phn
v no.
Thuc cha ng kinh l thuc c kh nng loi tr hoc lm gim tn s mc trm trng
ca cc cn ng kinh v cc triu chng tm thn km theo cn ng kinh.
I. THUC AN THN, GY NG:

Da vo cu trc ha hc chia thnh 3 nhm:
- Dn cht ca acid barbituric: Phenobarbital, Barbital,...
- Dn cht ca benzodiazepin: Diazepam, Nitrazepam,...
- Cc dn cht khc: Glutethimid,...
1. Dn cht acid barbituric:

c im:
- H ca nhm -NH- linh ng do ng gia cc nhm =C=O mang tnh acid (gi l acid
barbiturric).
- Acid barbituric ch c tnh an thn nh;
- Cc dn cht th v tr 5 (v i khi 3) c cc tc dng c ch thn kinh TW, to gic
ng, an thn, gin c hoc gy m:
Cu trc chung:
162
Bng: Mt s thuc dn cht acid barbituric
Tn thuc R1 R2 Tc dng chnh

Barbital -Et -Et Gy ng
Pentobarbital -Et -CH(CH3)- C3H7 Gy ng
Phenobarbital -Et -Ph Gy ng; Gin c
Butobarbital -Et -C4H9 Gy ng
Secobarbital -CH2-CH=CH -CH(CH3)- C3H7 Gim au; Gy ng
Ng c: Xy ra khi dng qu liu:

- Ng li b; th yu; huyt p tt;
- Cp cu khng kp thi s t vong do lit h hp.
Gii c:
- S cu: Gy nn; ung cht hp ph (than hot, lng trng trng)
- a ti bnh vin gii c; km vt chng lin quan ng c.
+ Tht ra ng tiu ha loi ht thuc cn d.
+ Tim thuc tr tim, th oxy, chng toan huyt.
Tnh cht ha hc chung:
- Tnh acid nn tan trong NaOH
- To mui vi cc ion Men+ (Ag+; Co++; Cu++...)

V d: Vi AgNO3, cc ion Na+ thay bng cc ion Ag+
163
Phn ng c trng ca cc barbiturat:
Barbiturat/Me-OH +CoCl2v CaCl2 mu tm
- un trong d.d. NaOH c gii phng NH3 (xanh qu ): (PTPU)
Cc phn ng ring: nhm th (5)
- Ph: th -Br; -NO3...
- Dy (-CH=CH- ; -C C- ...): tnh kh; gn iod..
nh lng:
Phng php acid-base, theo cc k thut sau:
- Trong dung mi ethanol-nc:
- Trong dung mi DMF: dung mi base lm tng phn ly, acid yu acid mnh; d pht
hin im tng ng bng ch th mu hoc o th.
- p dng cho mui mononatri: N=M (ch cn 1H)
MT S THUC C TH:
PENTOBARBITAL
Tn khc: Gardenal, Luminal.
Cng thc: C11H18N2O3; ptl: 226.27
Tn khoa hc: Acid 5-Ethyl-5-(1-methylbutyl) barbituric

Tnh cht:
Dng acid
+ Bt kt tinh mu trng, v ng nh; bn trong khng kh;
164
+ Kh tan trong nc lnh; tan trong Et-OH v cc dung mi hu c; tan trong dung dch
NaOH, KOH (to mui).
nh tnh:
+ Cc phn ng ha hc chung
+ p/ c trng barbiturat
+ Phn ng mu: un cch thy hn hp pentobarbital + vanilin/ acid sulfuric c: Mu
nu.
+ Ph IR hoc SKLM, so vi chun.
nh lng: Bng mt trong cc k thut ni phn chung.
Ch nh:
- Mt ng, cng thng: dng dng acid hoc mui mononatri.
Ng: NL, ung 100 mg trc lc i ng. AT: ung 20 mg/ln 3 ln/24 h; Tr em, ung 2-6
mg/kg/24 h.
- Tin m, dng thuc tim pha t mui mononatri
Bo qun: Trnh m; thuc hng thn (loi IV).
PHENOBARBITAL
Tn khc: Gardenal, Luminal
Cng thc:
Tn KH: Acid 5-ethyl-5-phenyl barbituric

Tnh cht: Tng t pentobarbital
nh tnh:
+ Cc phn ng chung: tng t pentobarrbital
+ Cc phn ng ring do gc th phenyl (5): Th Br; to mu hng vi thuc th
formol/H2SO4. nh lng: Acid-base, theo cc k thut ni phn chung.
Tc dng: Gy ng, gin c. Ch nh v liu dng:
+ Mt ng, cng thng thn kinh: NL, ung 100-300 mg trc lc i ng.
+ ng kinh, co c: NL, ung 50-100 mg/ln 2-3 ln/24 h.
+ Tin m: Tim/ truyn d.d. phenobarbital mononatri, liu gy ng.
Nhc im: Liu gin c gn vi liu gy ng. 600 mg/24 h.
165
2. Dn cht benzodiazepin:
Cu trc: l dn cht ca 1,4-benzodiazepin.
Tc dng:
- An thn: khc phc triu chng lo u, cng thng, bn chn.
- Gy ng: Dng cc trng hp kh ng, hay thc gic, dy qu sm khng ng li
c..
Ngoi ra con tc dng gin c vn.
- Sn phm chuyn ha cn hot tnh: Clorazepat, Diazepam, Flurazepam.
- Sn phm chuyn ha khng cn hot tnh: Lorazepam, Oxazepam,...
Cc php th dng trong nh tnh:
- Phn ng to mu, hunh quang c trng (Diazepam cho hunh quang mu xanh lc
khi ha tan vi H2SO4 ).
- Phn ng cc nhm th khc nhau nh NO2, gc phenyl,...
- Cc pp vt l: Ph IR, UV,...
Cc phng php nh lng:
Cc thuc dn cht benzodiazepam u l cc base hu c, dng dng base hoc mui
hydroclorid, kh nng hp th UV.
nh lng bng pp acid-base:
MT S THUC C TH:
NITRAZEPAM
Tn khc: Benzalin, Calssmin.
Cng thc: C15H11N3O3; ptl: 281.3
Tn kh: 7-nitro-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one.
Tnh cht: Bt kt tinh mu vng nht; nng chy 226-2300C. Hu nh khng tan trong
nc, tan nhiu trong dung mi hu c thng thng.
166
nh tnh, nh lng: nh phn chung.
Cng dng:
- Gy ng, km gin c vn mc trung bnh, ko di gic ng 6-8h.
- Mt ng, khc phc co c ngoi mun.
Cch dng-liu dng: ung trc lc i ng 5-10mg; TE v ngi gi ung liu ngi
ln.
THUC IU TR GIUN SN
MC TIU HC TP:
1. Trnh by c cc cch phn loi thuc iu tr giun sn.
2. Trnh by cng thc cu to, tnh cht l ha, cng dng ca cc thuc iu tr giun
sn thng dng.
NI DUNG
1. Bnh sn v phn loi thuc iu tr giun sn:
Bnh giun sn:
L bnh nhim l bnh nhim k sinh vt
167

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MC LC

Da vo cu trc ha hc c th chia cc nhm khng sinh sau:

1. Khng sinh beta-lactam.

2. Khng sinh Aminoflycosid.

3. Khng sinh tetracycline.

5. Khng sinh Macrolid.

6. Khng sinh Lincosamid.

7. Khng sinh Polypeptid.

8. Cc khng sinh khc: Rifamycin., Quinolon

A. CC KHNG SINH NHM -LACTAM

L nhm khng sinh ln nht k c tc dng tr bnh ln tn lng sn xut v doanh s.

- Azetidin-2-on + thiazolidincu trc penem (nhm penicillin). Trong nhm ny cn c cc

- Azetidin-2-on + dihydrothiazincu trc cephem (nhm cephalosporin). Trong nhm ny

- Azetidin-2-on ng ring rcu trc monobactam

2. Quan h cu trc v tc dng:

Nm 1929, A. Flemming phn lp ra benzyl penicillin t mi trng nui cy Penicillium

Tn cc cht lun c ui t illin

1.1 Tnh cht vt l:

- Ph UV a s cc nhm R acyl ha trn 6APA u l vng thm nn cho ph hp thu

- Ph IR: vng 16000-18000 cm-1

1.2. Tnh cht ha hc:

Tnh acid (nhm -COOH t do):

Cc penicillin cng c kh nng to mui vi cc amin:

+ To cc penicillin thy gii chm nh: procain penicillin ( tc ng ko di t 24-48h),

Mt s c tnh base nh nhm aminosid v cc alkaloid khi trn chung vi penicilin s gy

Cc penicillin c kh nng to este vi alcol: Gii phng chm hot cht.

Tnh khng bn ca vng beta lactam:

+ S hin din ca mui kim loi nng

+ S alcol phn v amino phn

+ S phn hy trong mi trng acid

Ngoi ra vng beta lactam c th m bi lactam tit ra t vi khun.

1.3. Phn ng mu phn bit cc penicillin v cephalosporin

Tin hnh: 2mg/ng nghim, thm 1 git nc lm m;

Thm 2ml TT formaldehyd/H2SO4 96%, trn u: Xem mu.

t ng nghim vo cch thy 100o C; quan st i mu /1 pht

Quan st i mu: Khc nhau gia cc cht -lactam.

Bng: Thay i mu ca cc -lactam trong 1 pht

Mu penicillin th TT Formol/H2SO4 (t0 TT Formol/H2SO4 (1000

Amoxicillin Khng mu Vng sm

Benzathin penicillin G Khng mu Nu

Ampicillin Khng mu Vng sm

Cephalexin Vng nht Vng sm

Cloxacillin Vng xanh lc Vng m

Flucloxacillin Vng xanh lc Vng

Phng php vi sinh: L kinh in, p dng cho khng sinh.

Hm lng: Tnh theo n v quc t (UI = Unit Internationale)

Phng php o Hg:

- Thy phn penicillin th/NaOH; to phng/15 pht;

- Trung ha bng HNO3; thm m pH 4,6;

- Chun bng Hg(NO3)2 0,02M; o in th (Cp in cc Hg (I) sulfat-Pt)

Xc nh penicillin ton phn bng o iod:

- Thu phn penicillin nh o Hg; Acid ha bng HCl 1N;

- Thm 10ml d.d.I2 0,01 N; y bnh 15 pht;

- Chun iod d bng natri thiosulfat 0,01N; h tinh bt.

Cc phng php vt l: HPLC,....

* C ch tc dng: thuc c ch to vch ca vi khun gram dng, mt s vi khun gram

- Cc khng sinh Penicillin l cc khng sinh t c, ngoi tr d ng.

2.Phn loi penicillin v iu ch:

* Cng thc chung:

2.1 Penicillin nhm I:

Khng sinh tc dng dit khun

- D b -lactamase ph hy. Thi gian bn thi ngn (~1 h).

- Penicillin G (TN): Khng bn/acid, ch dng ng tim.