PHARMACOLOGY

PHARMACOLOGY
PHARMACOLOGY
PHARMACOLOGY
PHARMACOLOGY
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PHARMACOLOGY
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PH{RMACOLOGY
PHARMACOLOGY
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PHARMACOLOGY
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AN'TIBIOTICS

L Penicillins
Mechamsm of Action
- baaericidal
- acl on penicillin binding protein to inhibit cell nali s.vnrhesis
Classif cation of Penicillins
1. Narural Penicillins
PeniciUin G - 1.2{0 million units IM or fV qd
Peniciliin V -- 250-500 mg po qid
Specrrum of Activiq'
- sueplococci. n onpenici ll inase saphyl ococci
- nonpenicillinase producing gonococci
- anaerobes(not Bacteroides)
2. Aminopenicillins
Ampicillin - 250-1000 mg PO, Ilvl- I\/ q4-6 hr
Amoxicillin - 250-500 me PO tid
Spearum of Acriin
- sueptococci. enterococci
- granl negatives(E. coli, P. nrirabilis. Shigella.
Salmonella)
3. Semi-srnthetic (penicillinase resisunt)
Methicillin Giacillin Dicloxacillin
Nafcillin Cloracillin
Spectrum of Activitl'
- staphvlococci (not MRSA)
- streplococcj
4 Expanded Specrmm (anti-pseudomonal peniciliins)
Carcenicillin Piperacillin Mezlocillin
Ticarcillin Azlocillin
Spectrum of Activiq'
- increasedgranr negative (Pseudomonas.Enterobaoer)
- sreptococci
- nol actire against Suph'r'lococci
5. Penicillin/3-lactamase lnhibirors
ticarcilli-n/clavulanicacid (Timentin) .- 3.1 gm IV q46hr
piperacillh/tazobacram (Zoqn) - 3.375-4.5 gm IV qShr
ampicillirVsulbactam(Unann) - 1.5-3.0 gnr IV q6fu
amoxicillin/clarulanic acid (Augmentin) - 875 mg po bid
Spectrum of Acrivitl'
- suphylococci (not MRSA)
- sueprococci
- enaerobes(ircluding Baoeroides)
- grun negatives (Pseudomonas.Enterobaoer)

Adverse Reactions
- h1'persensitivin - diarrbea
- neuuopenia - tralsient eleradon of LFT's
- Ouombocrropenia - high sodium (especialll'sith ticarcilli-n)
- mvoclonic seizures

114
IL - Ccpbalosporins.-
Mechanismof Action
- baaericidal
- inhili1i6pof cell s'aUs\Tlbesis
Agenu Available:

Cefazolin(Ancel) Cefoxiren(Mefoxin) lCefouxime(Clafoxin) lCefipime(Maxipime)

Cephalothin(Keflin) Cefurariime(ZinaceJ)
Cephapcrin(Cefa4vl) Cefoteun(Cefoun)
CephalexinCKeflix) Cefamandol(Mandel)
Cephadine(Ansper) Cefonicidft4onocid)
Cefadroxil@uricef) Ceforamide(Precef)
Cefaclor(Ceclor)
Ce$odoxime(Vantin)
Cefuroxirrre
axetil(Cefi
in)
| Cizorime(Cefizax)
| Ceftriaxone(Rocephin)
| CenaSOme(Fonaz)
| Moxalaaam(Maram)
| Cefoperazone{Cefobid)
| Cefixime(Suprax)
|

Spectrum of Actirity
I" Generation
- Suph'r'lococci. Sneprococci
- gram negati'r'es(E. coli, P. mirabilis, Shigella- Salmonella)
- anaerobes(nor Bacteroides)
2d Generation
- Supln'lococci (less active than l" generation)
- Snegococci (same as lo generation)
- more gram negative (ll. inlluenza horeus. Klebsiella- E.coli)
- anaerobes(cefotetan & cefoxitan aaiv'e agains Baoeroides)
3'd
Generation
'*,
lrfrT"?
'araerobes
ii."#frT?
f Tr"ffinrlf
46 Generatione
as earrier ae.ents
- grealer gram negauve coverage (including Pseudomonas)
Adverse Reaaions
- h1'persensitivi6' (cross reactir.iq' q'i1h PCN allerry S-|Syo)
- neutropenia
- diarrhea
- bleeding
- phJebitis q'ith IV adminisrrarion

m Otber B-Lactams
lmipenen/Cilasuti-o &imaxin) - 500 mg IV q6-Ehr
t*'*i1:Ti--::i::':9
mosl gntm posirive aerobes & anaerobes
gram negatives (including Pseudomonas)

Ad'erse*ffi#:"ffi"":':.

115
 Azueonem * l-2 gn fV q8h
Spectrum of Actiun
- eram negafive aerobes(Pseudomonas)
- not actiYeagains gram positiYeor aerobic organisms
Adverse Reactions
- no major side effeos

n/. Quinolones
Mechanism of Action
- bactericidal
- hhibits DNA gnase
Available Agents
Ciprofloxacin Lomefloxacin Trovafloxacin
Ofloxacin Levolloxacin Soerlloxacln
Enoxacin Sparfloxacin
Specrrum of Acriviq'
- Supbr'lococci (r'E MRSA)
- gram nep3tive bacilli (Pseudomonas)
- Enlerobaoer
Adverse reacuons
- GI (nausea. vonriting. diarrhea)
- insomnia
- headache
- setzures
- conrraindicated in children -- defeos in canilage
- drug interacdon n'irh rheophvlline & anracids

\/. Aminogll'cosides
Mecbanism of Action
- bactericidal - binds 30S bacterial n-bosometo inhibit prorein srnthesis

Available Agenls Daill Dosc Pcak(ug/ml) Trough(upy'ml)

Genuml'cin 3-5 mglkg qSh 4-10 2
Tobraml'cin 3-5 mgllcg qSh 4-10 2
Amikacin 15 mglkg q8b 20-30 10

*Check uough afier rhird dose

*dosing is nos' bei-ngrecommendedfor q 24 to decreasetoxicin' (able to do this due 10
po$anlibiotic effect of the medication)

Adverse Effeas
l. ototoxicity - irrwersible
2. nephroroxicir,r"- reversible
3. neuromuscularblockade

Srnergi'uitb PCN
Dose Genaml'cin 3mg/kg/da1'qSh or ql2h
Ad.lust dose to 2mgkglda:- in ESRD

116
 I
\t Sulfonamides - TrimcrhoprimSulfamelborazole(Bacrrim)
Mechanismof Action
I
- bacteriostatic
- sullamethoxazole+ inhibis folic acid production
- rnmelhoprim--+inhibitsbacterialdihl'drofolatereducrase
Dosage= I DS ublet bid
I
- trimetboprim 160mgisulfamerboxazole
- excellenloral absorption.
Specrum of Activjn'
800 mg
parenteralfornr rarelvused I
- Suphl'lococci(includingN,IRSA& MRSE)
- Streprococci
- gt'amnegarives@seudomanas) I
Adverse Reactions
- hvpersensitirin
- hemolltic anemia
I
- conrraindicareduith oral h1'poglvcemics& G6-pD deficjenc\.

\ZII. Macrolids
I
Mechanism of Action
- bacreriostatic
- binds -50sbaoerial rjbosome inhibiring prorein sur}esis I
Agenu Available
Enrluomycin (E-ruycin) - 250-500 nrg po qid
Azithromycin (Zirhromycin) - 500 mg l" day, 250 mg qd x 4 days
Clarirhroml'cin (Bioiin) - 250 mg po bid
I
Dintluomvcin (Drnabac) - 500 mg po qd
Specmrm of Activiqv
- Supbl'lococci & Srreprococci
J
- sortreanaerobes (not Baderojdes)
Adverse Reactions
- gasnoinresdnal (nausea & r'onaiting)
- heparoroxicin'
I
- thrombophJebitis n'irh IV infi:sion
- h1'persensitivin' ]

VII. Vancom_vcin
Mechanism of Action
- bactericidal
- inlu-bition of cell qzll srrrthesis
I
Dosage
- I gram fV ql2hl22.5(Crcl) + l50l = 24h requirement
T
- 125mg po qid for C. difficile colitis onlr.
- must monilor peaksand rrouE:hs
peak -- l5-30 mglml(ideal peak is bers..30-.10)
t
trough - < I0 mglml-(idealrroughis bem'. t0-12)
get pcaks/trougbsafter ffib dose
Specrum of Actiliq'
. MRSA & MRSE
l
- Suphl'lococci- Sueptococci,Enterococci
- gram posirive anaerobes(CIostridiurn-Cornrbacterium)
- nol acfivea-eainngram neeadves
t
117
t
I
 AdverseReacrions
- nephJoloxctn'
- ototoxicin' -- reversible
- red nran srndrome
- anaphvlactoidreacuonu4rerebl'lusunrine is releasedb-r'mast cells
- due lo npid IV infusion
- entherna & pruritis especialll'of upper lorso. neck and face
- treatmenl: antilusumines

DL Clindaml'cin
Mechanism of Action
- bacreriostatic- inhibits nanslation br' 50s baoerial ribosome
Dosage
- 600-900 mg IV qSlt
- 300 mg po bid+id

Spectmm of Actiriq'
- Suphylococci. Sueptococci
- anaerobes(Bacteroi des)
Adverse Rqrctions
- pseudonrerrrbranouscoliti s
- diarrhea- naus€a

)L Tctracl'clines
Arzilable Agents
Minocvcline - 100 mg p ql2-24h
Doxl'q'cline - 100 mg po ql2-24h
Tetraq'cline - 250-500 mg po qid
Specu-umof Activin'
- Supbl'lococci. StrePococci
- some gram negatives and anaerobes
- rare organisms @. burgdorferi. Acrinomyces, M. Marinum)
Adverse Reacnons
- gastrointestinal ffi666n
- rash & photosensitiun'
- $aining ofbones and teeth

Xl. Rifampin
Dosage .. 300 mg Po bid
Spectrum of Aair"it-r'
- Suphi'lococci. StrePtococci
- lr{1'cobacteria
- some gram negatives (Neisseria. HaemophiJus)
Adverse Reacrions
- red discolorarion of bo$'fluids (uri-ne. E:lrs. contacl lenses)
- skin rash
- flu-like s\TnDloms

XIL Melronidazole (FlaS'l)

Dosage
- 500 mg po tid
- intravenous- 15 mglkg load 7.5 mg/kg q6-8h
Spefl.rum of Acririn'
- gr?m negarive anaerobes@acteroides)

118
 - -AdverseReaaions-
- nreullic taste/dn' moutlr
- antabuse reacdon
- seizures in natients u'itlr b/o seizures

Sursical Pronhr'laris
== Goal is to provide adequatedrug level prior to and during the surgical procedure

lndications:
- prolonged surgery (>2 hours)
- use of implanls (screws,k-wires, proslheses,elc.)
- trauma surgery
- immunocompromrsed parients
- SBE risks

Selection of Agents:
- active against most conrnroncausativeorganism (Suph1'lococcusaureus)
- long half life
- intravenous admi nistration
- antibiotic level should be nu>iimal at incision
Specific Agens.
Cefazolin I grant fV
C[ndamvcin 600 mg IV
Vancomycin I gram IV

M isccllancous lnformalion

Antibiotics for MRSA

- r'ancoml'cin
- minoq'cline
- ciprofl oxaci n/rifampin
- bacrim/rifampin

Di sul fi ram/Anrabuse R eacti on

- nausea.vomiting diarrbea
- occurs uith concurrenr ingestion of EIOH and certain antibiotics
- relared with rhe MMT sidechain present on some antibiotics
- specitrc drugs:
moxalacum cefomandol
cefoperazone cefoletan
metronidazole

Antibi oti c Associated Di arrhea

2 Tlpes:
I . overgron'th of C. difficile (xeudomembrarous coliris)
2. alteration of inresdnal microbial population
Charaoeristics:
- can be causedb'anl'antibioucs
- clindam-"-cin is most conrmon cause
- occurs u'ith oral or parenteral adminisranon
- indeoendenl of dose or duration of ueatment

119
 Treatment--
- discontinue antibiotic il possibie
- no anridiarrheal agents(allows toxin to accumulate)
- fluid and elecuolrre suppon
- antibiotic therapr'
metronjrtqTole500 mg q8h
vancomvcm 125 mgpo q6b

A N T I F U N G AA
L GENTS

SYSTEMIC
A m p h o t e r i c r nB lmidazoles Terbinafrne Flucytocine
Nystatin Miconazole Griseofulvin
Ketoconazole
Triazoles
Itraconazole
Fluconazole
TOPICAL
Amphotericin lmidazoles Naftifine Specl/lc
Nystatin Miconazole Terbinafine C i c l o o r o xO l a m i n e
Clotrimazole Haloprogen
Ketoconazole Tolnaftate
Econazole lodochlorhydroxyquin
Oxiconazole Nonspecific
Sulconazole W h i t f i e l d ' sO i n t m e n t
l.tndecylenicacid
C a s t e l l a n i ' sP a i n t

POLYENES

M e c h a n i s mo f a c t i o n : F U N G I S T A T I C .
B i n d s i r r e v e r s i b l yw i t h e r g o s t e r o l( p r i n c i p a ls t e r o l i n t h e f u n g a l c e l l m e m b r a n e ) .
T h i s r e s u l t s i n a l t e r e dm e m b r a n e p e r m e a b i l i t y ,l e a k a g eo f i n t r a c e l l u l a rc o n s t i t u e n t s a, n d
c e l l d e a t h . O t h e r p o s s i b l em e c h a n i s m si n c l u d eo x i d a t i v em e m b r a n ed a m a g e a n d
e n h a n c e m e n to l c e l l m e d i a t e d i m m u n i t v .

N Y S T A T I N( M y c o s t a t i n N , ilstat,)
- c r e a m ,o i n t m e n t ,p o w d e r
apply to affecledarea BID
- i n h i b i t sc e l l m e m b r a n e s t e r o l b i o s y n t h e s i s
- e s s e n t i a l l yn o a b s o r p t i o nw i t h o r a l f o r m - u s e d t o t r e a t o r a l e s o p h a g e a al n d
Gl
c an d i d i a s i s
- i n d i c a t e ds p e c i f i c a l l yf o r C a n d i d a
A M P H O T E R I C I NB ( f u n g i z o n e )
- l o t i o n ,o i n t m e n t ,a n d c r e a m i n 3 / o c o n c e n t r a t i o n
. a p p l y t o a f f e c t e da r e a s B I D - Q l D
-derivedfrom StreptomycesNodosus
- a c i i v ea g a i n s ts a p r o p h y t e sa n d y e a s t
- o r a l f o r m o o o r l va b s o r b e d

120
 - _._us€d_intravenously--for_potentiallyJife_threaiening
deeprnycottc
i n f e c t i o n s / s y s t e miiucn g e m i a
D o s e :O . 2 5 m g / k g l d a yi n f u s e ds l o w l yo v e r6 h o u r s( i m p o r t a ntto m o n i t o rB U N / C R )
W i t h i n c r .o f C r t o > 3 . 0s w i t c ht o l i p o p h i l i cA m p h o t e r i c i Bn (Amphotec)
S i d e E f f e c t sG : l d i s t r e s sf,e v e r .c h i l l s ,h e a d a c h e sh,y p o t e n s i o nh,y p o k a l e m i a ,
h y p o m a g n e s e m iaan, e m i at,h r o m b o p h l e b i t li isf,e rf a i l u r e r, e n a lf a i l u r e
Drug Reactions:
Aminogylcoside &sC y c l o s p o r i nsey: n e r g i s t inc e p h r o t o x i c i t y
C o r t i c o s t e r o i d&sK * d e p i e t i n gd r u r e t r c sm: a y p o t e n t i a t eh y p o k a l e m i a ,
nypomagnesemta

AzOLES

lmidazoles and Triazoles

M e c h a n i s mo f a c t i o n :F U N G I S T A T I C
- i n h i b i tg r o w t ho f f u n g i b - vi n t e r f e r i n w
g i t h c e l l m e m b r a n ee r g o s t e r obl i o s y n t h e s i s
b y p r e v e n t i n gt h e
i 4 - a l p h a - d e m e t h y t a t ioof nl a n o s t e r o l
- r n a yi n h i b i tc y t o c h r o m ec p e r o x i d a t i vaen d o x i d a t i v e n z y m e sr e s u l t i n gi n
Increased
i n t r a c e l l u l a rp e r o x i d eg e n e r a t r o n
- e f f e c t i v ea g a i n s td e r m a t o p h y t e s s, a p r o p h y t e s c, a n d i d aa n d s o m e g r a m p o s i t i v e
bacteria
. m a n y h a v e a n t i - i n f l a m m a t o r ya c t i v i t y

SYSTEMICA7 OLES- I MID NOLES:

M I C O N A Z O L E( M o n i s t a t l V )
- N O o r a l p r e p a r a t i o na v a i l a b l e
- i n t r a v e n o u so r i n t r a t h e c a l
Dose: 2O0-36OOmg/dayin 3 divided doses
S i d e E f l e c t s :G l d i s l r e s s ,p h l e b i t i s ,s e i z u r e s ,t r e m o r s , a n e m i a , h y p o n a t r e m i a ,
th rombocytopenia,ca rdiac dysrhythmias
D r u g ! n l e r a c t i o n s :m a y i n h i b i t m e t a b o l i s mo f S u l l o n o l u r e a s C , o u m a d i n ,p h e n y t o i n

KETOCO NAZOLE (Nizoral)

-well absorbed I
-99% bound to plasma protein
- r e a c h e s s k i n v i a b l o o d s t r e a ma n d e c c r i n es w e a t g l a n d s
- e x c r e t e d p r e d o m i n a n t l yt h r o u g h b i l e ( f e c e s5 7 / o , u r i n e l 3 % )
I n d i c a t i o n s : b l a s t o m y c o s i sc, o c c i d i o m y c o s i sp, a r a c o c c i d i o m y c o s i s ,
h i s t o p l a s m o s i s ,c h r o n i c m u c o c u t a n e o u sc a n d i d i a s i s s, u p e r f i c i a ld e r m a t o p h y t e
infections I
D o s e : 2 0 0 ' 4 0 0 m g / d a y l o r 2 - 8 w e e k s( s u p e r f i c i a li n f e c t i o n s )8 . i 8 m o n t h s
(onychornycosis)
S i d e E f f e c t s :M a n y ! m o r e c o m m o n S E ' s i n c l u d eG l d i s o r d e r s . I
L e s sc o m m o n S E ' s : h e p a t o t o x i c i t yC , N S d i s o r d e r s( H A , d i z z i n e s s )a, d r e n a l
i n s u f f ci i e n c y , g y n e c o m a s t i a i,m p o t e n c e ,t h r o m b o c y t o p e ni a , a n e r n i a ,
leukopenia
' a s y m p l o m a t r ce i e v a t i o ni n l i v e rt r a n s a m i n a s e o s c c u r i n 2 . 7 O / oo f p a t i e n t s I

r21
 Di u e I nt -tclib ns : Ah1ac rds, F|2-BIOekeTs,Rif emFi n;1 sdn i azi d;P he nytoi n ;
t e r f e n a d i n eA
, stemizoleC , h l o r d i a z e p o x i d eC, o u m a d i n ,C y c l o s p o r i n I, n s u l r n ,
A m p h o t e r i c i nB , C o r t i c o s t e r o i d sA, l c o h o i

SYSTEMICAZOI.ES-IRJAZOTES:
-Iriazolering may be responsiblefor increasedpotency, decreasedtoxicity, and wider
specttum ol aclion of these agents

ITRACONAZOLE(Sporanox)
- r a p i d l ya b s o r b e d
-lipophilic
-only O.2/s free drug in the plasma
- " r e s e r v o i r "e f f e c t - t h e r a p e u t i cl e v e l sp e r s i s t i n s k i n / n a i l s / h a i rf o l l i c l e sf o r w e e k s
after discontinuairon of
t h e r a p y ;d e t e c t e di n t o e n a i l sf o r 6 m o n t h s a f t e r c e s s a t i o no f t h e r a p y
- h e p a t i cm e t a b o l r s m - l i v el ru n c t i o n t e s t s ( L F T ' s )s h o u l d b e m o n i t o r e d r e g u l a r l y
-excretionu : n n e ( 3 5 . 2 / ) a n d f e c e s( 5 4 . 1 / o )
-not removed by hemodialysis
l n d i c a t i o n s :b l a s t o m y c o s r sh, i s t o p l a s m o s i sa, s p r i g i l l o s i sd, e r m a t o p h y t e
onychomycosis

C o n t r ai n d i c a t i o n s :
-coadministratiow n i t h T e r f e n a d i n eA
. s t r e m i z o l eT
, r i a z o l a m ,A n d
Midazolam
- a v o i di n p r e g n a n c ya n d i n n u r s i n g m o t h e r s -d o s e d e p e n d e n tm a t e r n a l
toxicity and embryotoxicity

lT RACONAZOLE(Sporanox)-continued

Dose: {or onychomycosis 2OOmgpo BID {or 7 days, then frrst week of each
m o n t h f o r 3 - 4 m o n t h s ( i e . P u l s ed o s i n g )
OR
ZOOmg/daylor 3 months

lor tinea pedis l OOmg/day for thirty days

- c l i n i c a lc u r e r a l e a p p r o x . 6 0 - 7 O 7 om ; y c o l o g i cc u r e r a t e a p p r o x . 7 4 / o i
approx- 75/6 relapserate
S i d e E f l e c t s( i n c i d e n c e7 - I 2 . 5 V ) : G l d i s o r d e r s ,H A , d i z z i n e s s ,d i z z i n e s s ,
m a l a i s e ,m y a l g i a ,r a s h , p r u r i t i s , f e v e r , i d i o s y n c r a t i ch e p a t i t i s ,v a s c u l i t i s ,
e d e m a ,H T N , o r t h o s t a t i ch y p o t e n s i o n ,h y p o k a l e m t a g, y n a c o m a s t i a ,
imootence
- e l e v a t i o no f L F T ' s i n O . 3 / s - 5 / so 1 p a t i e n t s -u s u a l l yt r a n s i e n t
Drug lnteractions:
-decreaseltraconazole/evels.'Rifampin, I soniazid,Phenobarbitol,
C ar b i m a z e p i n e ,P h e n y t oni ,
H2 Blockers
-increasesdrug concentrationsof: Warfarin, Digoxin, Cyclosporin,Oral
Hypoglycemics

FLUCONAZOLE(Diflucan)
- i n t r a v e n o ufso r m a v a i l a b l e
-hydroPhilic
-more than 9O7oof ingested dose is absorbed

122
 - . o n l y - 7 J t o b o u n d t o p l a s m a - p r o t e i n sm , a j o r i t y - o fc i r c u l a i i n gd r u g t n f r e e i o r m
- n o s i g n i f i c a n tf i r s t p a s s m e t a b o l i s m ,u n l i k eo t h e r a z o l e s
. p r i r n a r i l ye x c r e t e dt h r o u g ht h e k i d n e y :u n c h a n g e d( 8 O % )m e t a b o l i t e s( 1 1 % )
- h t g h c o n c e n t r a t r o n isn t h e s t r a t u m c o r n e u m a n d s w e a t
- d e t e c t e di n s k r n 1 0 d a y s a f t e r c e s s a t i o no f t h e r a p y
l n d i c a l i o n s v: a g r n a al n d o r o p h a r y n g e a l / e s o p h a g ecaaln d i d i a s i sc, r y p t o c o c c a l
meningitis
Dose: lor onychomycosis 1 50.3OOmg/weekfor 6-12 months
lor linea pedis 150 mglweek for 4 months
if creatinrne c l e a r a n c e> 5 0 m 1 / m i nt h e n g i v e f u l l d o s e
i f c r e a t i n i n ec l e a r a n c ei s 2 1 t o 5 0 m l l m i n t h e n g i v e h a l f d o s e
i f c r e a t i n i n ec l e a r a n c ei s 1 1 t o 2 0 m l / m i n t h e n g i v e 1 / 4 d o s e
-clinical cure rate approx. 60/o; mycologic cure rale 65/o
S i d e E f l e c G : G l d i s o r d e r s ,H A , r a s h , i n c r e a s e dL F T ' s
Drus Interactions:
-lncreasesdrug levelsof: Warfann, Cyclosporine,Theophyline, oral
h y p o g l y c e m i ca g e n t s
-increasesFluconazole levels:Rifampin
- P h e n v t o i nm e t a b o l i s mi n h i b i t e d

TOPICAL ATOLES:

M I C O N A X O L EN I T R A T E( M i c a t i n ,M o n i s t a t )
-2lo cream, aerosol, powder, solution
- a p p l y t o a f f e c t e da r e a s B I D

C L O T R I M A Z O L E( L o t r i m i n , M y c e l e x )
- 7 / o c r e a m , l o t i o n ,s o l u t i o n
- a p p l yt o a f f e c t e da r e a s B I D

KETOCONAZOLE(Nizoral)
-2/o cream
- a p p l yo n c e d a i l Y
- a v o i di n p t s w i t h s u l f i t e s e n s i t i v i t y

ECONAZOLENITRATE(SPectazole)
'1/o cream
- a p p l yo n c e o r t w i c e d a i l y
-may be effectiveagainst some g+ bacteria

OXICONAZOLE N ITRATE(Oxistat)
-)./o cream, lotion
- a p p l yo n c eo r t w i c e d a i l y
- m a y b e e f l e c t i v ea g a i n s ts o m e g + b a c t e r i a
S U L C ON A Z O L EN I T R A T E( E x e l d e r m )
- 7 / o c r e a m ,s o l u t i o n
- a p p l yt o a f f e c t e da r e a s B I D

C L O T RI M A Z O L EA N D B E T A M E T H A Z O N E ( L o t r i z o n ec r e a m )
- a p p l yt o a f f e c t e da r e a s B I D
- f o r m o r e i n f l a m m a t o r yd e r m a t o p h y t ea n d y e a s t i n f e c t i o n s

* s t r n g i n g , b u r n i n g ,i t c h i n g ,b l i s t e r i n ga, n d c o n t a c td e r m a t i t i sc a n o c c u r w i t h a n y t o p i c a l
a n t i fu n g al *

r23
 ATLYLAMINES

M e c h a n i s m o f a c t i o n : F U N G I C I D A vL s . d e r m a t o p h y t e s
- p o t e n t r n h i b i t i o no { e r g o s t e r osl y n t h e s i sb y s e l e c t i v ei n h i b i t i o no f s q u a l e n e
epoxrdase
- l a c k o f e r g o s t e r o lc a n i n t e r f e r ew i t h t h e i n t e g r i t ya n d g r o v r r t o
hf the fungal
cellwall
- s q u a l e n ee p o x i d a s ei n h i b i t i o nc a u s e ss q u a l e n ea c c u m u l a t i o nt h a t m a y b e
f u n g i c i d aI
- w e a k e n sc e l l m e m b r a n e a n d c a u s e sc e l l d e a t h
- e f l e c t i v ea g a i n s ts o m e g r a m p o s i t i v ea n d g r a m n e g a t i v eb a c t e r i a

N A F T I F I N E( N a f t i n e )
. 7 / o c r e a ma n d g e l
- a p p l y t o a f t e c t e da r e a s B I D
- l i p o p h i l i c -b i n d s w e l l t o t h e s t r a t u m c o r n e u m a n d p e n e t r a t e si n t o h a i r f o l l i c l e s
- h a s a n t i - r n f l a m m a t o r yp r o p e r t i e s

T E R B I N A F I N E( L a m i s i l )
Topical:
-7/o cream
- a p p l y t o a f f e c t e da r e a s B I D
Systemic:
- l i p o p h i l i c -h t g h c o n c e n t r a t i o n sf o u n d i n s t r a t u m c o r n e u m , h a r r , a n d s e b u m
-7O-9OV,of oral dose is absorbed
- s i g n i f i c a n tf i r s t p a s s m e t a b o l i s m
- B O % o r a l d o s e ( m e t a b o l i t e s )e x c r e t e di n u r i n e
- d r u g l e v e l se x c e e d i n gt h e M I C f o r d e r m a t o p h y t e sp e r s i s t sl o r 2 1 o 3 w e e k sa f t e r
c e s s a t i o no f t h e r a p y
l n d i c a t i o n s :o n y c h o m y c o s i sd u e t o d e r m a t o p h y t e s
Dose: lor onychomycosis: 25O mg/day ior 12 weeks
lor tinea pedis: 25O mg/day tor 2-6 weeks
- d e c r e a s ed o s e i n l i v e r d y s f u n c t i o na n d w h e n c r e a t i n i n ec l e a r a n c ei s
<5Oml/min
- m y c o l o g i cc u r e r a t e 7 O / o ; m y c o l o g i ca n d c l i n i c a lc u r e - 3 8 / o ; 8 5 / o p t s w i t h
no relapse
S i d e E f l e c t s :h e p a t i c d y s f u n c t i o n( r a r e ) , G l d i s o r d e r s ,H A , s k i n r e a c t i o n s / r a s h ,
f a ' t i g u e ,l o s s o f t a s t e , v i s u a ld i s t u r b a n c e s ,n e u t r o p e n r a
- a v o i di n p r e g n a n c ya n d n u r s i n g m o t h e r s

D r u g I n l e r a c t i o n s :l e s s p o t e n t i a lf o r d r u g i n t e r a c t i o n st h a n A z o l e s
- Terbina{in e cl earance increased by: Ri{am pin (7 OO/), P he nobarbitaI
.Terbinafineclearancedecreasedby: Cimetidine (33/o), Terfenadine(16%)

MISCELLANEOUS
AGENTS
SYSTEMIC:

F L U C Y T O S I N E( A n c o b o n )
M O A : i n h i b i t s R N A s y n t h e s i si n s u s c e p i i b l e{ u n g i c o n t a i n i n gt h e e n z y m ec y t o s i n e
oermease
- t y p i c a l l yu s e d i n c o m b i n a t i o nw i t h A m p h o t e r i c i nB
U s e s : s y s t e m i cm y c o s i s ,c a n d i d i a s i s
D o s e : 5 0 - 1 5 O m g / K gp o i n d i v i d e dd o s e s e v e r y 6 h o u r s

1 1 A
 S i d e e f l e c t s :G l d i s t r , e s sC, N Sd i s o r d e r s - ( l - ' l A , d i z z i n e s s ) ' s rkai ns h i a b n o r m a l - l i v e r
f u n c t i o n ,b o n e m a r r o w p p r e s s i o nr,e n a lf a i l u r e ,c a r d i a ca r r e s t ,r e s p t r a t o r ya r r e s t
s u

GRISEOFULVIN ( G r i f u l v i nF, u l v i c r nG, risactin)

MOA: FUNGISTATIC
- i n h i b i t sc e l l m i t o s i sa n d n u c l e t ca c i d s y n t h e s t s
- p o s s i b l yi n h i b i t s c h i t i n s y n t h e s i s
- h a s a n t i - i n f l a m m a t o r yp r o p e r t i e s
- e f f e c t i v ea g a r n s tr e c a l c i t r a n ts k i n , h a i r , a n d n a i l i n f e c t i o n sc a u s e d b y
oermatophytes
- n o t e f f e c t i v ea g a i n s t c a n d i d a
- r e a c h e ss t r a t u m c o r n e u m b y s w e a t i n ga n d d i f f u s i o n
- n o t r e c o m m e n d e di n P r e g n a n c Y
- c o n t r a i n d i c a t e di n h e p a t i cd i s e a s ea n d p o r p h y r i a
D o s e : 5 O O m gp o Q D ; 3 3 0 ' 3 7 5 m g p o Q D ( u l t r a m r c r o s i z e )
Side Eflects: ManY!
- m o r e c o m m o n i n c l u d e :G l d i s t r e s s ,H A
. l e s sc o m m o n r n c l u d e :C N S d r s o r d e r s u , r i n a r y d i s o r d e r s ,c u t a n e o u s
d i s o r d e r s ,n e u t r o p e n i a A , r t h r a l g i a s ,l i v e r d y s f u n c t i o n
D r u g l n t e r a c i i o n s :b a r b i t u r a t e s ,c o u m a d i n ,o r a l c o n t r a c e p t i v e sc, y c l o s p o r i n e ,
alcohol

TOPICAL:

H A L O P R O G E N( H a l o t e x )
- F U N G I C I D A aL g a i n s t d e r m a t o p h y t e s C
, andida
- s y n t h e t i c7 / o c r e a m a n d s o l u t i o n
- a p p l y t o a f l e c t e da r e a s B I D

C T C L OP R O X O L A M I N E( L o p r o x )
.FUNGICIDAL
, . b l o c k st r a n s p o r to f a m i n o a c i d s i n t o t h e f u n g a lc e l l a n d w e a k e n sf u n g a lc e l l
memDrane
- e f l e c t i v ea g a i n s td e r m a t o p h y t e s c, a n d i d a a n d s o m e b a c t e r i a
-l/o cream, lotion
- a p p l y t o a f f e c t e da r e a s B I D
- h a s a n t i ' i n f l a m m a t o r yp r o p e r t i e s

M I S C EL L A N E O U ST O P I C A LA G E N T S( c o n t i n u e d )

TOLNAFTATE (Tinactin, Aftate)

.FUNGICIDAL
-i n h ib i t s s q e al e n e e P o x i d a s e
- r n h i b i t sg r o w t h o f h Y P h a e
- l r m i t e dt o d e r m a t o P h Y t e s
- s y n t h e t i cI / o g e l , p o w d e r ,c r e a m , a e r o s o l
- a p p i y t o a f f e c t e da r e a s B I D

U N D E C Y L E N I CA C I D ( D e s e n e x ,C r u e x )
.FUNGISTATIC
- c r e a m ,o i n t m e n t , p o w d e r ,s p r a y p o w d e r
- a p p l yt o a f f e c t e da r e a sB I D

t25
W H I T F I E L DOS INTMENT
- 1 2 % b e n z o i ca c i d ( F U N G l s r A T t ca) n d6 / o s a l i c y t i a
c c i d( k e r a t o t y t i c )
' c a u s e sd e s q u a m a t t oonf k e r t t n t z eedp i d e r m tcso n t a i n i nfgu n g a lo r g a n i s m s

C A S T E L L A NPI A I N T( f u c h s i np, h e n o lr e s o r c i n oal ,c e t o n eS, P a l c o h o4l O B ,p u r i f i e dw a t e r )

- t o p i c aal n t i f u n g adlr y i n ga g e n t
- a p p l y1 - 3 t r m e sd a i l y

LOCAL AA'ESTEETICS

Mechanismof Aclion
a. surface charge theory:
- l o c a l b r n d st o r e c e p t o ri n t h e N a c h a n n e li n n e r v e
membrane
- N a c h a n n e li s b l o c k e d
- d e c r e a s ei n r a t e a n d d e g r e eo f d e p o l a r i z a t r o n
- l a c k o f d e v e l o p m e n to f a c t i o n p o t e n t i a l
- c o n d u c t i o nb l o c k a d e
b- membraneerpansion:
- a b i l i t yo f u n - i o n i z e dc o m p o u n d st o p o s s e s sa n e s t h e t i c
activitv
- a l t e r e dc o n f i g u r a t i o no l t h e m e m b r a n e
- d e c r e a s e dd i a m e t e ro f t h e N a c h a n n e l
. i n h i b i t i o no f N a i n f l u x / c o n d u c t i o nb l o c k a o e
c diffusion:
-diffusionof LA depends on degree of ionization
- L A e x i s t a s u n c h a r g e dm o l e c u l ea n d c h a r g e d
cations
-proportion depends on pKa of LA and pH of solution
- g o v e r n e db y H e n d e r s o n - H a s s e l b a l cehq u a t r o n
pH = pKa + log base/cation
- a s p H d e c r e a s e se q u i l i b r i u m s h i f t s l o w a r d c a t i o n
w h i c h b i n d st o r e c e p t o r
- a s p H i n c r e a s e se q u i l i b r i u m s h i f t s l o w a r d b a s e w h i c h
c a u s e sm e m b r a n e
e x p an s l o n

Pharmacology
E s t e r sa n d A m i d e s

plasma esterase u n s t ab l e r a r e ( p ar a - a m r n o b e n z o iacc i d )

A m i d e h e p a t r ce n z y m e stable very rare

Characteristics:
l . L i p i dS o l u b i l i t y
- L A t h a t a r e l i p i d s o l u b l ep e n e t r a t en e r v e m e m b r a n e
readily
-they have a greater potency
2 . P r o t e i nB i n d i n g
- i n f l u e n c e sd u r a t i o n o f a c t i o n
. a g e n t so f s h o r t d u r a t i o n b i n d p o o r l v

126
 3 p[1 -defineithe
p H a t w h i a ht h e b a s t a n d c a t i o ni o r m sa r e e q u a l
- a g e n t sw i t h a p K ac l o s e rt o i i s s u ep H h a v ea r a p i do n s e t
4 . In t r t n s i cV a s o d i l a t oArc t t v t t y
- i n f l u e n c epso t e n c y / d u r a t t oonf a c t i o n
- t n c .i n v a s o d i l a t o
a rc t i v i t y= i n c .i n v a s c u l aar b s o r p t l o n
- l e s sL Aa v a i l a b l feo r n e r v eb l o c k a d e
Agents:
L5 I LKS
1 . C o c a t n e - a d d i c t l voen, l y v a s o c o n s t r i c t o ru, s e d a s t o p r c a la n e s t h e t t c
2 . P r o c a i n e - w e a pk o t e n c yd u e r a p i d h y d r o l y s i s u , sedfor infiltratton
anesthesra
3 . C h l o r p r o c a i n e - r a p iodn s e t ,l e s s t o x r c ,u s e d i n o b s t e t r i c a lc a s e s
4.f elracaine-slow o n s e t , i n c t. o x i c i t y ,u s e d f o r s p i n a l a n e s t h e s t a
AMIDES
l . L i d o c a i n e - r a p iodn s e t ,u s e d r n r e g i o n a lt,o p i c a la n e s t h . ,a n t i a r r y t h m r c
2.Mepivacaine-use f odr i n f i l t r a t i o np, e r i p h e r a bl l o c k ,e p i d u r a l
3 . P r i l o c a i n e - l e a st ot x i c , u s e d f o r i n t r a v e n o u sr e g i o n a la n e s t h . ,
4 . B u p i v i c a i n e - l o ndgu r a t i o n ,u s e d i n c h r o n i cp a i n ,e p i d u r a l( l a b o r )
5 . E t i d o c a i n e - r a p iodn s e t ,i n t e n s em o t o r b l o c k a d e
6 . R o p i v a c a r n e - r a p ci dl e a r a n c e , s h o r t ehr a l f - l i f et h a n b u p i v .

Toxicity
cNs cvs
lnitial events I n i t i a le v e n t s
Tin itus hypertension/ta c hycard ta
lightheadedness I n t e r m e d i a t ep h a s e
confusion m y o c a r d i a ld e P r e s s i o n
E x c i t a t r o np h a s e d e c r e a s e dc a r d i a c o u t p u t
t o n i c - c l o n i cc o n v u l s i o n s mild hypotension
D e p r e s s i o np h a s e TerminalPhase
unconscrousness p e r i p h e r a lv a s o d i l a t i o n
g e n e r a lC N S d e p r e s s r o n p r o { o u n dh y p o t e n s i o n
r e s p i r a t o r ya r r e s t sinus bradycardta
conduction de{ects
v e n t r i c u l a ra r r y t h m i a s
c i r c u l a t o r yc o l l a p s e
M a x i m u m R e c o m m e n d e dD o s e s

Drug Conc. mE/kg mg/70kg

mg/7okg
(7) Pll(EPi) PL(EPI) PL(EPI)
chlorprocaine 3.OO 11(14) 77O(9BO) 25(33)
Irdocarne 1.O0 4(7) 280(490) 28(50)
lidocaine 1.50 4(7) 2BO(490) 19(33)
lidocaine 2.00 4(7) 280(490) 14(25)
mepivacaine 2.O0 4(7) 280(490) 14(25)
prilocaine 3.00 7(8.5) 500(600) l7(2O)
bupivacaine 0.75 2.5(3.2) 1'75(225) 23(30)
erroocaine 1.O0 6(8) 420(560) 42(56)
etrdocaine 1.50 '(8)* (560) ' (37)
* e t i d o c a t n e 1 . 5 n o t a v a i l a b l ew r t h o u te p t n e p h r t n e
* d o s e s r n p a r e n t h e s e sa p p l y w n e n e p r n e p h r r n eS u g l m l r s a d d e d t o s o l u t t o n

t27
 --
AliEinat'iveagent5:---
BENZYLALCOHOLO.9/o:
I n d i c a t e dw i t h p a t i e n t sw i t h a m r d e / e s t earl l e r g i e s
F o r u s e r n s h o r t l a c e r a t r o n sa n d s u p e r f r c i awl o u n d s

GLTICOCORTICOIDS

G l u c o c o r t i c o i dasr e t h e m o s t p o w e r f ubl u t a l s ot h e m o s tt o x r cc l a s sof drugs

usedfor the
t r e a t m e n to f i n f l a m m a t o rcyo n d i t i o n s T
. h e i n v e s t i g a t i oann d u s e o f glucocorticoids began
a l m o s tf i f t y y e a r sa g o ,y e t m a n yc o n t r o v e r s i esst i l l l e m a i nr e g a r d i n gt h e i r
c l i n i c a lu s e s .
r i s k sa n d b e n e f i t s .

GlucocorticoidStructure
- c o r t i s o n ei s t h e m a i n e n d o g e n o ugsl u c o c o r t i c o i d
- s t r u c t u r ei s a 2 1 c a r b o ns t e r o i dh o r m o n e
- synthesized lrom cholesterol
- activitydependson siructure
' s t r u c t u r ed e t e r m i n e sp o t e n c y
and raie of absorption
' c o r t l s o n ea n d p r e d n i s o n ea r e i n a c t i v e
u n t i l c o n v e r l e dt o c o r t i s o l a n d
prednisolone

H y o o t h al a m i c P i t u i t a r yA d r e n a lA x i s
- regulales cortisol secretion
- basal induced glucocorticoid release
- 20 mg/day
- d i u r n a l - i n c r e a s e di n e v e n i n ga n d m o r n i n g
- stress induced glucocorticoid release
- cold, exercise,infection,surgery
- H P A a x i s s u p p r e s s i o n= a d r e n a li n s u f f i c i e n c y
- d u e t o i n c r e a s e de n d o g e n o u so r e x o g e n o u s
grucocorticoid
- s y m p t o m s o f a d r e n a li n s u f f i c i e n c v
- n a u s e a ,U B p , h y p e r k a l e m i a ,C V
collapse
- s u r g i c a ls t r e s sd o s i n g
.for pt's on > 7.5 mg/day of prednisone
for I month
- hydrocortisonelO0 mg lV for
total 3OO mg
Mechanism of Aciion
- w o r k t h r o u g h t h e s y n t h e s i so l o t h e r c o m p o u n d s
' r e g u l a t e st r a n s c r i p t i o na n d u l t i m a t e r yp r o t e i n
synthesis
- m e c h a n i s mo f a c t i o n i m p o r t a n t b e c a u s e :
I t a k e s h o u r s f o r a c l i n i c a lr e s p o n s e
2. action is indirect :+ causes many unwanted side effects

Metabolic Effects
g l u c o c o r t i c o i d sp r o t e c t t h e g l u c o s ed e p e n d a n tt i s s u e s ( b r a i n& h e a r t )
C ar b o h y d r a t e M e t ab o l i s m
- i n c r e a s eg l u c o n e o g e n e s i s
- d e c r e a s e p e r i p h e r a lg l u c o s eu p t a k e
Lipid Metabolism
- i n c r e a s e s l i p o l y s i s+ i n s u l i n r e l e a s ea n d g l u c o n e o g e n e s i s

128
ProtCin Metbbolism
- d e c r e a s e ss y n t h e s i sa n d t n c r e a s e sb r e a k d o w ni n m u s c l e
' i n c r e a s e si r e e p l a s m a a m l n o a c l o s
Fluids and ElectrolYtes
- sodium andwater retenllon
-hYPokalemia
B o n e& C a t c i u mM e t a b o l i s m
' d e c r e a s eisn t e s t i n acl a l c i u ma b s o r p t l o n
' i n h i b i t so s i e o b l a sftu n c t r o n
Connective Tissue
' d e c r e a s ecso l l a g e nf o r m a t t o n
' i m p a i r sg r a n u l a t i o 'nt t s s u feo r m a t t o n

S Y s t e m i cG l u c o c o r t i c o i d s
Theraoeutic Efiqcts
1 . A n l i - r nl fa m m a t o r Y
' m o d u l a t o r so i i n f l a m m a t t o n
- i n h i b i t p r o s t a g l a n d r ns y n t h e s t s
- i n h i b i t sC O X ' 2
-inhibrtscytokrne,adhesionmolecule'chemotacticfactorprod'
' d e c r e a s e sv a s c u l a rp e r m e a b i l i t y
- cellular effects
-|ncreases#ofneutrophilsbutdecreasesaccumu|ationatsiteso{
i n f l am r n a t t o n
.decreases#otmacrophages,|ymphocytes,eosinophils,basophi|s
2. lmmunosuPPressive
' c e l l u l a r> h u m o r a l
- c t r c u l a t i n gl y m p h o c y t e sa n d m o n o c y t e sd e c r e a s e
' r n h i b i tn a i u i a l k i l l e r a n d T ' c e l l p r o l i f e r a t i o n
- eflective againstacute graft relectton
3. Antr'asthmatic protein called
s epromoting production o{ a
- i n h i b i t sl i P o o x Y g e n aby
ItPocorttn
' i n h i b i t s p r o d u c t i o no f l e u k o t r r e n eC 4 & D 4 = S R S ' A
' d e c r e a s e sb r o n c h i o l ei n f l a m m a t r o n
P h ar m a c o k i n e t t c s
.absorbedora||y,intramuscuIar|y,intrasynovia||y,topica||y
- m e t a b o l l z e dr n t h e l t v e r ,e x c r e t e di n t h e u r t n e

D o s r n gR e e t m e n s
1 . D a i l YH r g hD o s e
' > 1 5 m g P r e d n i s o nd ea i l Y
' l i f et h r e a t e n i n ga u t o i m m u n ed i s e a s e s
2. PulseMethYlPrednisol-one
' 1 g r a m l V o v e r4 5 m i n u t e s
- u s e da s l a s t r e s o r t t h e r a P Y
3 . D a i l YL o w D o s e
' < 1 5 m g P r e d n i s o n ed a i l Y
' m o s t c o m m o n d o s i n gs c h e d u l e
' u s e df o r i n f l a m m a t o r ya r t h r i t t c p r o c e s s e s
4 . A l t e r n a t eD a YD o s t n g
- less side ef{ects
- u s u a l l Yl e s s e f f e c t l v e

t29
D r u gl n t e r a c t t o n s
i n c r e a s eS t e r o i dC l e a r a n c e
- p h e n y t o i nr,i f a m p i n b, a r b i t u a t e sc,a r D a m z e p t n e
Decrease Steroid M e t a b o l i s m
- k e t o c o n a z o le s, t r o g e n - c o n t a i n o i nr ga l c o n t r a c e p t i v e s
Other Effects
o" 'jJl
. :j:,'"",3:"'fi:,:il i:? l""l?
i ., ",,I hypogIycemcs

A d v e r s eR e s o o n s e s
A d v e r s er e s p o n s e st o t h e r a p e u t i cu s e s o f g l u c o c o r t i c o i d a s r e m a i n l yd u e t o
prolonged exposure to high doses. Most adverse effectsare dose related and a short
c o u r s e ( 2 w e e k s )e v e n a t h i g h d o s e sg i v e sa l o w r i s k . A l t h o u g ht h r e s h h o l dd o s e s a r e
v a r i e d l o r i n d i v i d u a lp a t i e n t s ,s t u d r e sh a v e s h o w n t h a t a l l p a t i e n t sr e c e i v i n g3 0 m g o i
p r e d n i s o n ed a i l y l o r a t h r e e m o n t h d u r a t i o n w i l l e x p e r r e n c e a d v e r s er e s p o n s e s .

Very Common Frequent

- osteoporosis ' mYoPathY
- i n c r e a s e da p p e t i t e - a v a s c u l a rn e c r o s i s
- centripetal obesity - hypertension
- r m p a i r e dw o u n d h e a l i n g 'edema
- i n c r e a s ei n i e c t i o nr i s k ' t h i n , f r a g i l es k i n
- HPAaxis suppresston ' cataracts

Uncommon Rare
- glaucoma - pancreatitis
. b e n i g n i n t r a c r a n i a lh y p e r t e n s i o n - hirsituism
- peptic ulcerdisease -panniculiiis
- h y p o k a l e m t ca l k a l o s t s - rmpolence

Comoarisoo n f V a r i o u sS t e r o i d s
Glucocorticoid Potency D a i l yD o s e ( m g )
ShorlActrng
Cortrsone(Cortone) 0.8 50' lOO
Hydrocortisone(Hydrocortonne) I 50' 1O0
lnlermediateActine
Prednisone(Orasone) 4 10' 20
P r e d n i s o l o n e ( D e l t a ' C o r t e f )4 70'20
Methyprednisolone(Medrol) 5 1O-20
Triamcinalone 5 5-2O
LongActine
D e x a m e t h a s o n e ( D e c a d r o n )3 0 0.75- 3.0
Paramethasone(Haldrone) 10 4 '6
Betamethasone(Celestone) 30 0.6 - 3

130
 T
L o c a lC o r t i c o s t e r o i d s
- M a x i m i z e l o c a le f f e c t sa n d m i n r m l z es y s i e m l ca d v e r s ee f f e c t s c
T
Contraindicattons
lndrcattons
- r h e u m a t o i da r t h r i t i s
. g o u ta n d P s e u d o g o u t
. s e r o n e g a t i vaer t h r i d i t i e s
- i n f e c t o u sa r t h r i t i s
- bacteremta
- p e r i a r t i c u l acre l l u l i t t s
t
- a c u t et r a u m a t i ca r t h r i t i s
. osteoarthritis
- S L Ea n d M C T D
- osteochondra
- jointprothests
- allergy
t rla c t u r e
I
- tendonitis/bursitls - osteomyelitts
. n e r v ee n t r a p m e nst y n d r o m e s
- p l a n t a rf a s c i i t i s
- b a c t e r i ael n d o c a r d i t i s
- severaldays beloreyointsurgery T
- i n t r al e s i o n a l / d e r mI a

A d v e r s eR e s o o n s e s
I
- p o s t r n 1 e c t i ofnl a r e ' d u e t o c r y s t a ld e p o s i t r o ni n t h e j o i n t
. c o r t i c o s l e r o i da r t h r o p a t h y- s i m i l a rt o C h a r c o to s t e o a r t h r o p a t h y
- i a t r o g e n i ci n f e c t i o n' v e r y t a r e
I
. t e n d o n r u p t u r e . o n l y i i i n j e c t e dd i r e c t l yi n t o t e n d o n o u ss u b s t a n c e
- i a c i a l . [ l u s h i n g- m o r e c o m m o n w i t h t r i a m c t n a l o n e
- skin atroPhY/dePigmentatton
. p e r i a r t i c u l a cr a l c i f i c a t i o n - e s p e c i a lilny D I P J ' sa n d P I P J ' so f f t n g e r s / t o e s
I
- s y s t e m t ca b s o r P t i o n
- m a s k s s i g n s o f i n { e c t i o n( J e d e m a ,e r y t h e m a ,c a l o r , d o l a r ) t
j
T o p i c a lS t e r o i d s
P h a r m a c o l o g i cA c t i o n s
l. Anti'inflammatorY
vasoconstriction in the skin
s t a b i l i z e sl Y s o s o m am l embrane
I
p r e v e n t sc o n v e r s i o no f m e m b r a n e p h o s p h o l i p i d st o a r a c h i d o n r ca c i d s
2 . D e r m a lA t r o P h Y
i n h i b i t s f i b r o b l a s tp r o l i i e r a t i o n
I
i n h i b i t s d e p o s r t r o no { c o n n e c t i v et i s s u e c o l l a g e n
3 . I n h i b i t sM i t o s e si n E P i d e r m t s
D i s o r d e r sL e s s
I
D i s o r d e r sR e s p o n s i v et o T o p i c a lS t e r o i d s
Resoonsive

erythematosts
a t o P i cd e r m a t i t i s d i s c o i dl u p u s
I
p s o r i a s i so f p a l m s a n d
s e b o r r h e i cd e r m a t i t i s
soles
l i c h e ns t m P l e xc h r o n i c u s necrobiosts I
I rp o i d i c a d i ab e t l c o r u m
a l l e r g r cc o n t a c td e r m a t i t i s ( l a tpeh a s e s )
r r r i t a n td e r m a t i t i s ( l a i p
eh a s e s )
n u m u l ar e c z e m a t o u sd e r m a t i t i s
s ar c o i d o s i s
l i c h e ns t r i a t u s
pemPhigus
I
vitiligo
s t a s i sd e r m i t i t i s
o s o r i a s i so f f a c e a n d g e n i t a l i a
g r a n u l o m aa n n u l a r e
t
1 - 1
I
t
lJr
p o t e n c vC i a s i e i o f T o o i c aS l teroiOs
G r o u P s| & l i
- h i g hp o i e n c y
- s h o r tt e r m t h e r a P Y
- n o t r e c o m m e n d efdo r g e n e r a l i z edde r m a t o s e sc,h r o n i ct h e r a p y t, a c e o f
i ntertri ginoustheraPY
G r .I e x a m p l e sb: e t a m e t h a s o ndet p r o p t o n a fO e ' O 5 / oc, l o b e t a s o l
d i p r o p i o n a t eO . O 5 l o
- G r .l l e x a m p i e s :b e t a m e t h a s o nder p r o p r o n a 0 t e. 0 1 / 6 ,t l u o c i n o n i d.eO 5 / o ,
desoximetasone .2570
G r o u P sl l l , l V ,V
- mediumPotencY
- r e c o m m e n d el o d r t r u n k ,e x t r e m i t i e ss,c a l p
- u s ew i t h c a u t r o ni n g e n e r a l t z edde r m a l c s e s
. G r .l l l e x a m p l e s t: r r a m c i n a l o n0e. 5 / oo i n t m e n t b, e t a m e t h a s o n0e. 0 1 / o
cream
G r . l V e x a m p l e s t: r i a m c i n a l o n0e. 1 / e o i n t m e n t b, e t a m e t h a s o nOe. O 2 5 %
otntment
. G r .V e x a m p l e s t: r i a m c i n a l o n0e. 1 / o c r e a m ,h y d r o c o r t i s o nvea l e r a t e
o.2%
G r o u P sV l & V l l
- low potency
- r e c o m m e n d e dl o r l a c e , a x i l l a , n e c k , g r o i n
. G r . V l e x a m p l e s : f l u m e t h a s o n eO . 0 3 / oc r e a m , d e s o n i d eO . O 5 %c r e a m
- G r . V l l e x a m p l e s : h y d r o c o r t i s o n e1 / o c r e a m , d e x a m e t h a s o n eO . O 4 l o
cream

T o p i c aI V e h i c l e s
1. Ointment
- a l m o s t p u r e g r e a s ew i t h v e r y l i t t l e w a t e r
- m o s l o c c l u s i v ea n d h Y d r a t i n g
- providesgrealer steroid effect
- u s €o n d r y r a s h , p a l m s a n d s o l e s ;n o t f o r u s e o n w e t r a s h
2. Cream
- g r e a s ew i t h m o r e w a t e r
- steroid eflect weaker
- use lor drY rash
3. Lotion
- l i t t l e g r e a s ew i t h m o r e w a t e r
- steroid ef{ect weaker
, xilla, groin
- u s e o n s c a l p ,t o e i n t e r s p a c e s a
4. Solution
- o i l y l i q u i d o f a l c o h o l( p r o p y l e n eg l y c o l )
- steroid eflect strong
- t a i r l y d r y i n g- b u r n s o n d r y , c r a c k e d s k t n
- u s e o n s c a l p ,l o e i n t e r s p a c e s a , x i l l a ,g r o i n
5. Gel
- s t e r o r de t f e c ti s a s s t r o n g a s i n a n o t n t m e n t
- may use underocclusion
- very drYing
- u s e o n s c a i p ,i o e i n t e r s p a c e s a , x i l l a ,g r o i n

152
 )
\
SEDATNT H\?NOT] CS/SLEEP]\[fDI CAT]ONS
;
\
1. TEN,IAZEPAM( RESTORIL )
CLASS : benzodiazepam hlpnotic
DOSAGE : l-5-30mg po HS prn insomnia )
N{ETABOLISM:b@tic
EXCRETION:renal
\I/ARNINGS : 1. do not usedurirg pregnanq'
2. combinedeffeas u'ith ETOH and CNSdepressanrs
3. potentialfor ahrse
7
2.T?.IAT,c,LAM ( EALCTON ) \
CL.ASS: triazolobenzodiazepine lxpnoric
DOSAGE:0.1254.25mgpoHS prn iruomnia
METABOLISM : hepanc
)
EXCRETION;renal
'fr/ARNINGS; l. do nol useduringpregnanq'
2. '<elouer dosesi-nel&rl1'parients
3. nuy causebeluvioraichenees
4. combinedefleqsnith ETOH andCNSdepressanl<
5. potentialfor abuse
:
3. FI-I'RAZEPAM ( DAL]VIANE )
CLASS : bcnzodiazepamh)pnobc agenl )
DOSAGE: 15-30mg po HS prn inrcmnia
METABOLISM : hepadc t
EXCRETION: renal
U/ARNINGS: 1. donotus€duingpregnanc\'
2. combinedeflefls $'i$ ETOH and CNS depressans
3. potentialfor abr:se
.1.do not usein childrenu-rrderI 5 r'earsof aee

4. ESTAZOLAM(PROSOM )
CLASS: rriazolobenzodiazepine hypnotic
DOSAGE : 1-2 mgpo HS prn insomma I
N{ETABOLISM:heptic ( rapidir smokers)
EXCRETION:retul
WARNINGS: l. do nol us€duringpregnanct- 2

2. combi-nedeflectsu'ith ETOH and CNS deoressans ;

3. potentialfor abuse

5. DOXYLAT{INE SUCCINATE( IJNISOM )

CLASS : et}anolamineatrtihisarrlille
DOSAGE: 25 mgPoHS Pn insomnia
Ir{ETABOLISM : beParic
EXCRETION. renal
WARNINGS: l. shouldonl)'be takenal be'ftime
2. combinedeflectsu'ith ETOH and CNS &pressans
6. ZOLPIDE}{ TARTRATEI AJ\{BIEN)
CLASS : norr-berzodrazepxrehipnouc
DOSACE : 5-J0mg po Hs prn rnrcmma
METABOLISM:hepabc
EXCRETIOI' :renal
WARNINGS : l. usereduced dosaeentth elderh'
2 combinedefects-"rrfrETOH and Cl{S depressanrs
3. potentialfor abuse

ANTI-PRURITUSAND POTENTTATIONOF NARCOT]CS

I. DIPHENH}DRAMINE ( BENADRYL )
CLASS . arttilrisami:re
ADULT DOSAGE : 25-50 po tidgid prn prurirus
PEDS DOSAGE : 12.5-25 mg po tidgid prn pruritus
METABOLISM : lrepatic
EXCRETION :renal
WARNINGS : L use loser dosesin children and elderh'
2. addiuve effectsuitlt ETOH a:rd CNS depressalrs
3. do not glve lo ptienu uking MAO inhjbirors

2 PROMETHAZNE ( PMNERGAN )
CLASS : plrenothiazinederivitive u'itlr antihisunune. sedative.antinroriotr sickless- antientetic. and
anti cholinergrc effecrs
ADULT DOSAGE : 12-5-25mg bv deepIM inlection q 6-8 }tr
PEDS DOSAGE : I2.5 nrg ['deep IM in-ieflion q 6{ }ir
METABOLISM: hepatic
EXCRET]ON : renal
WARNINGS : l. conrairs sodium nreubisulfre ( ? alJergr')
2. avoid intra-anerial injecrion
3. rnterxif es and prolongs eflects of CNS depressans and sedative b'rpnotics
4. nuf interactu'ith MAO inhjbrton

3. }IYDROXYZNE HCL ( ATARAXN/ISTARIL )

CLASS : piperazine derived antihisanrilre
DOSAGE: 25 mg po tidqid prn pruritus ( ATARAX )
50-100 mg IM q 46 hr prn prn ( \ISTARIL )
METABOLISM : hepatic
EXCREnON: biljary
\\/ARNINGS . l. potentiatjon of narcoticsand CNS depressants
2. do not give lo nursrng mofrers
3. induration/serile abecessesat iniecdon sircs

134
 ANTTE]\MTICS

1. CYCLIZINE HCL ( MAREZTNE )

CLASS: piperazirederivedantilrisanrue
DOSAGE: 50 mg po q a4 iu
METABOLISM : b"?ads
EXCRETION:renal
WARNINGS : l. combrnedefecrcu'irh ETOH and CNSdepressanrs
2. rna]'causehi'potensonespecialll'afler surgen'

2. DIMEN}ryDRINATE ( DRAMAMINE )
CLASS : etlranolamineantihisramine
DOSAGE: 50-100mg po q.1-6lu
50mgIMqa4hr
N,IETABOLISM :heptic
EXCRETION:rerul
WARNINGS : l. combinedeffeasu'ith ETOH and CNSdspressanrs
2. useu'ith caurionif hison. of serztuedisorders

3. PROCHLORPERAZINE( COMPAZINE )
CLASS : pbenothiazinederjratjve
DOSAGE. 5-10mgpotid-qid
I
25 mg supppr bid
5-10mg ['de€p IM injectionq 34 hr
METABOLI5I4 ; lrpatic
EXCRET]ON:renal
WARNINGS: l. do nol usern children( s\mporns similiarro Rete'ssrndrome)
2. snongexu-aptramidalsideeflecrs
3. m4v causeonlosatic blporension

4. TRI 4ETIJOBEI.IZAN{IDE HCL ( TIGAN )

CLASS: cenu-all1'aainganoerneoc
DOSAGE: 250 mgpo tidaid
200 mg supppr tidgid
200 mg IM tid-qid
METABOLISM: hepatic
EXCRETION : renal andbifian'
WARNINGS: l. do nol us€i-uchijdren
2. do not useu'ith ETOH
3. Parkinson-like smpoms
4. suppositories contair berzrcaine

J PRON,IETHA.ANE( PMNERGAN )
CL.ASS:phenorhiazinederirzdveuitlt antilustarmne.
sedad'r,e.
altimouon sicloess.antienretic.and
antichoiinergic efecrs
DOSAGE: 12.5-25mg b' deepIM injectionq 6$ Hr
METABOLISM : hepatic
EXCRETION:renal
\\/ARNbIGS : SEEPRE\f]OUSDESCRIPION

lJf

I
 ODFh-ISETRONX& ( Z0FRr$t I
CLASS . seroronin5III-3 recep{oranugorus
DOSAGE : 4 mg fV prn nausean'omlnrng
METABOLISM :hepatic
EXCRETION:renal
WARMNGS : RELATI\EL'I'NEW UTTH FEW AD\ERSE EFEECTSINCLIMCAL TRTALS
? HeparicToxioq

]. }ELLOW PHENOLPHT}IALEN AND DOCUSATE CALCILIM ( DOX]DA}{ )

CLASS : irritalt larativey'soolsofiener
DOSAGE : I -2 capsulepo q d4\'up ro onen,eek
WARNINGS : ( sameasfor COLACEDIALOSE )

2. CASANTHRANOLANDDOCUSATE SODTUM( PERTCOLACE

)
CLASS : irritent laxaritdsool sofiener
DOSAGE : l-2 capsr.rles po HS
l5-30 mL lqrup) po HS
WARNINGS : sameasfor COLACE/DIALOSE

.3 DOCUSATESODILM ( COLACf,, DIALOSE )

CLASS :surbqan stoolsofiener
DOSAGE: 50-200mgpo q dal,( COLACE)
100mg po Cd4,- rid ( DIATOSE)
\\/ARNINGS : l. do nol uses'irlr mineraloil
2. do not useu'itlr abdolrriralpairt. rnlsea or vonrinine

4 CASCARASAGRADA
O-ASS : irritant laxarive
DOSAGE: 325mg po HS

5 CALCILIM POLYCARBOPHIL( FTBERCON.FTBf,RALI- MrrRor-AN

)
CLASS : hrlk fonrring fi-berlararive
DOSAGE: 2 ubs up ro gid ( FIBERCON)
I rabq dq'- qrd( FIBERALL)
2 tabsqid or prn ( MITROLA].] )
I. sbouldtr uken u'ith firll glassof uater lo prevenlchoking( ublerscan su,ellin rhroarif nottaken.*"jtlr
at leas 8 ounzesofuater )
2. slrouldbetakenI hourbeforeor 2 lrous afierrerracvcline-tike antibiotics

6. PSYLLIUM lryDROpHILlC MUCILT OID ( hIETAI\'UCL )

CLASS . hrlk forming run:ral tlrerapeuricfrber
DOS-AGE. araiableil porvden packzu,granuJes. anduafen
( seePDR for prescnbinginforrnarion)
WARNINGS: l. patienrsrDavhavean allergr'ropsr'lliruu
2. conu-aindicared nirh inresdnalobsructionandfecalimmcdon

7. SENNA CONCENTRATE( SEIYEXOT)

CLASS : irritant larative

136
 I
DOSAGE;2'tabs po q d4', preferablvHS I
l0-15 nrl- (s\Tup)po q da)'.preferablvHS
I rq) (gnnuies) po q daf',preferablvHS
I sr4:posiro4'prq d4, preferabll'HS
I
S. SENNA CONCENTRATEAND DOCUSATESODIUM( SENEXOT-S)
CLASS' ffi tqnl laxative/stool
DOSAGE:2tabsPoqda)'
soflener
I
9. BISACODYI- ( DI.ILCOLAX )
CLASS : irritart laxatire
DOSAGE: lGl5 mg Poq da]'
I
I suprposto4'prq d4

10.DO].i'T FORGET PRLINEJUJCEI ! ! !

I
ANTTDIARRHEAL AGEI\TS T
NATURAL BFI I.ADONNA ALKALOIDS \UTrH PHENTOBARBITOL ( BELLATAL
CLASS : artticltolrergidaltispastlodic
) I
DOSAGE : l-2 ubs Po ddqid
U/ARNINGS : I. additi'r'e etrects u'ith ETOH and CNS depressans
2. poential for ahrse I
D]CYCI,OMINE HCL ( BENT-YL )
CLASS . antichollrergidantispasrtrodic I
DOSAGE : 80 mg/d4'po in 4 divided doses
WARNINGS . l. contraindicatrons:
- obsm)fiive uropathl'
- obstructive diseaseof tle GI u-ao
- ssvere ulcerative coljtis
t
- rdluri esophagitis
- gJaucoma
- rras}enia gravis
l
- nursrng nrotlrers
2. use u'it-b caution in patients n"ith autonomic neuroparhy. heEtic or renal drsease.
HTN. CAD. and CIIF.
r
HYOSCYAMINE ( CYSTOSPAZ )
CLASS : ParaqmParholltic agent
t
DOSAGE : I -2 ubs po grd ( feu'er if rteeded)
WARNINGS : l. contraurdcadons :
- gaucoma
- obsmrcr^'e uropatlt't'
l
- perahtic ileus
- mvastbeniagrarx

t
1 a F 1
1 3/

I
 4. GLYCOPIRROLATE ( ROBINIIL-)---
CLASS : antichoiinergicagenr
DOSAGE : I ub po tid
WARNINGS: l. conuarndicarions :
- autononricneuropat}t'r'
- hepaticor renal drsese
- ulcerarirccolios
- hlpertlnroidisnr
- hiaralherniau'jt} esophageal
rellui

5. DIPHENOXYLATE Hc- AND ATROPINESUI-FATE( LOMOTIL )

CLASS : antidiarrheaVanticholinergic agenl
DOSAGE:2 ubpo gid
WARNIINGS: 1. fluid andelecro\remoniroringamus
2. do not "sefor anu'bioucassmiarcddiarrhea
3. rna)'inreradq'jrh barbirurares.
rranquilizen.EToR andlvc-Aoinlubiron

6. KAOLIN AND PECTIN( XAOPECTATE )

CLASS : antidiarrhealagenr
DOSAGE : capsules, chesablerabs,andliguid p'eps

7. LOPERAMIDE HCL ( rhr}roDruM )

CLASS : antidiarrlrealageur
DOSAGE : 4 mg po foilos,edby 2 mg afier cachunformedsool

8. PrNK BISN4UTII(PEPTOBTSMOL)

ANALGESICS

l. Morphile suUate
- adult dosage- 5-20mgq a hr SC-IM (alsoslou'I\)
- l0-20rugq .t hr recralll'
- pediarricdosage - 0.1{.2mg q hr SC-IM
- metabolism- Iirer
- excretion- kidnq'
- antidore- nelslsns - (Narcan)- O.4-2mgq 2-3 min IV-n,oSC up ro 0.1mg/kgIV

MS Conun - 15,30.60-100-200mg in controlledreleaseublersu'irlr200mgtablersonJl'being

usedin
patientsq'ith tolerance
shouldtitratedoseon aDeven' 12 hourinrcn'al suning uith l5mg q 12 hr po

MSIR flmmediarerelease)- l5.30mgrabletsor a solurjonof 5mg/lrrJ

- sbouJdtitrare dose5-30mgq 4 hr pO is a good suning poirl

Morph:neDerivarives:
l. OnmorphoneHCL (Numorphan)
- arhll dosage- L0-l.5nrg q 4-6 hr SC.IN4
or 0.5mg 46 IV
2. Hvdromorphone HCL @ilaudid)
- adult dosage- 24mgq a5 hr PO
- 2rngq 44 hr SC
- 3mg q6-8 hr Recrally

138
 I
2.-M ethl'lm orphine SO4or?O1,(Codeire)

- adult dosage- l550mg q a hr PO.IIvLSC

- pediarncdosage > I )'earold:0.5mg/kgq44 PO.SC
- ureubolisnt- liver
- excretjon- hdnel'andsomeliver
I
- antidore - narcanas above

- Compoundsconuining Coderne
I
NAME CODEINE (mg) ASA (mg) ACETAMINOPHEN (mg)
I
T1'lenol#2 I-5 300
Trlenol #3
Tr,lenol#-1
T1'VCodEiixir
30
60
12
300
300
120
T
Enrpracet#3 30 300
Enrpracel#-1
Empin #2
60
15
300
325
I
Emprin #3 30 325
Enrprin #4 60 325
I
Codeine Derival:r'es:
l. OxvcodoneHCL (
- heparanons and Dosages
a. Percmet (5mg oxlcodone. 325mg acetaminophen)
- l-2 q 44lu PO
b. T'r'lox (5mg ox1'codone-500m9 aceraminophen)
-lq6hrPO
t
c. Percodan(4.5nrg on'codone. 0.38nrg orycodone rereplrthalate.325 nrg
aspirin)
-iq6PO
I
d Percodan Demi (pediatric)
- l/2 the strengrh of regular percodan
- 1/2 tab q 6 for children > 12 1,earsold
I
- l/4 tab q 6 for children 6-12 r'ears old
e. Oxycontin (controlled release)
- analgesiaonsel u'jthin one hour
- su-starned releaseover l2 hours
r
- titrate ever]' I -2 da1's.if nec€ssan'
- increasedoseb1' 25-50ohas necessan'.do nol increase dose frequenq
- nlal g!\/e on'contin inuuediale releasefor breakrluough pain
5
- suppliedin 10.20.a0.80mg rableu taken every l2 hours

I
t
T
139
l
 -Hvdrocodone
2.

Preparationsand Dosases

NAME IIDROCODONE tmg) ACETAN{INOPHEN (mg) ASA (mg)

Lortab 2.5 2.5 500

Lortab,5 5.0 500
Lortab 7.5 t.) 500
Lonab liquid 2.5 I2()
Lonad ASA 5.0 500
Lorcet r 0.0 650
H1'drocet 5.0 500
Vicodin 5.0 500
Vicodin ES t-) 750

-- Dosagesgeneralll'should nol exceed40mg of Hvdrocodone

3 hopoxlphene HCl-inapq'late (Dan'on / Dan'on-N)

- adult dosage - Dan'on 65mg q 4 hr PO
- Dan'orr-N l00nrg q 4 lu PO
or l0mg/mj suspal l0nrj q 4 hr PO
- metabolism - liver
- excretion - lddnel
- antidote - narcan as above
- hepararions:
l. Dan'on cornpound (32mg dan,on- 389nrg ASA 32.1mg cafleine)
2. Dan'on u'ith ASA (65m9 dan'on. 325m9 ASA)
3. Dan'on-N 50 (50mg dan,on-N, 325mg aceumi-nophen)
4. Dan'on-N I00 ( 100 darvou-N. 650urg acetanrinophen)

*r Ma)'be p'r'en to coderndmorphine alJerpc palients

.1. Pentazocjne HCl/lacute Oahvin / Talu'in lnj)
- adult dosage- 50mg q 3a hr PO, 30mg q 3-4 hr IM.SC.IV
- contraindicatedin children under l2
- nterabolisnt - liver
- excrerion - kjdnel'
- anridote - narcon as above
- Prepararions.
l. Tals'in compound(l2.5mg pcntazocine.325mg ASA)
-2tabq6hrPO
2. Talacen (25n9 pentrzocire. 650ng acetaminophen)
- I qa hrPO
3. Taluin Inj *(caution uith SC route - urav causeskin
rlenpgs /sclerosisl;
- 30mg q 3{ br IV.SC.IM
4 Taluin Nx *(contains Naloxone - an antagonis u'hjch
has no aflect at 0.5nrg PO hou'ever. it does lrave ar narcotc antagonis affect if
g:r'en fV al this
dosage - tbus prevenrilg abuse)*
- 50nrg penrarocine. 0.5rng rreloxone
- I q 3-4 po (mav be rncreased to 2 tabs if necded)

i40
 l* All-Talu'in-products m2\'c;ruse u'it-bdras',duelo an anugonisuc aflect tou'ard morphine and
demerol regardlessoftle preseuceofnaloxone

*t lr4a)'be used in morphine and codeineallergic patrenrs

5. Meperidine HCL (Demerol)

- adult dosage - 50-l50mg q 3a hr PO.Ilvt-SC
- l5-35nrg/lu IV in divided dosesor slou'dnp
- pediamc dosage- l.5mg/irg q 3{ hr PO.IM (singJedose nor ro exceed l00mg)
- meubolism - hver
- excretion - lcidnev
- antidote - narqln
- rruscellaneous- lr{av be given u'ith 25-50mg of Phenerganor Vistirit in
order lo decreaseLbe
dose and not Joseeflect.
** This drug should not be pven lo diah'sis patienrsdue
ro irs meubolire nor berng djaliazableand. rhis
metabobte mav induce seizures.

- Prepararions:
I. Mepergan(25m9/rnlmeperidine.2\mg/nn promethazine)
- adulr- 25-50rngq 3-5 IM
- children- 0.5mg/bq 3-4 iM

2. lr4eperganFortis (50mg meperidine. 25mg prometlazine)

-adult-Iqa-6PO

6. Butorphanol (Stadol)
- adull dosage- lutg q 3{ lu IV
2mgq3-4hriM
- lmg puflup I nostril q 3-a hr
- pediaric dosage- contraindicared in parients ulder l8
- meubolism - liver
- excredon - kidnq'
- anudote - narcan as above
7. Non-narcoric agents n.itb Narcoric-iile pa.inrelief
A. Ketoralac Ooradol)
- adulr dosage- 60rng loading dose ilren 30nrg q 6 hr IM
- lOmg q a-6 hr PO
* onl)' for up ro 5 da1'smat' this
be us€d
* This drug is a NSAID and lus all tlre sanreprecautions.

*' Gen eral hecauti ons/Contrai ndicati ons for these Medi cati
ons
-check PDR if 1'ouare going lo us€ these drugs arrd the folloning appl)'
l. compromised respiraton' funcrron
2. bilia:-r' raa $'sfunction
3. increasedCSF pressure
4. hepanc or renal djsease
5. recenl use of CNS depressa-nts
6. Tblroid disease
7. recentuse of MAO inhibiton
8. nursi-ngmotben
9. be alvare of acetaminophen and aspirin conraining conrpounds and tlteir relau.i'e
conrraindrcations

141
 r.*ON=tiAR CO Tt e7 N O N r\*SAID

-TRAMADOL HCL (uluam)

CLASS . 2nalgesiccenrrallr.aoing
DOSE : 50 - 100mg po q I - 6 hrs.
max dose: 400mgi da1'
METABOLITFD: liver
CLEARED: renal
WARNINGS : crearinineclearance< 30ml/min : dose:50 -l00mg po q l2 hrs
crrbosispt. dose: 50mgpo q 12 hrs.
nlal polenbaleseizurerisk uith otler medications
associatedqidr man.r'G.l. complaints

N O N STER OIDAL ANTIINFL{.]\[\I-A TOR}' DR L]GS

Pharmacologl
. With r-lreexceprionof nabunrelone.all NSAIDs are n.eak acids.
. Acidic enr"jronmenlof somach / proxmal small inresune
' NSAIDs - nonionized lipophilic sute allou'ing for rapid and complere absorption
. Mosr NSAIDs reach peak plasma concentralions- three hours.
. Stea{' stateplasma concentrationsare achievedin 3--shalf lives.
. Exensit'ell bound lo plasma proteins (98-99o/o)
. snull volume of distriburion. (l-2o/oof the drug is ..free'.)
. PalicDts s'ith hepatic d-r'sfunctionna1'require doseaheratrons.
. Sulindac and Nabumetone- prodrugs (convened in the liver ro active form)
. Mosl NSAIDs uldergo hepaticbiotransformation eirher through the c\rochrome pt50 s_\,srem
or glucuronide conjugation
. Elimjnation is predominantlv tlrougb the kidnel'alrhougb some NSAIDs c"n be eliminated eirlrer
paniall-r or rorallv through the biliarl' rract (e.g.. Sulindac. Indomethacin)
o Flatjentsu'jtb renal failure conjugated metabobres ca-naccumulare and be reabsorbed and
reconverted lo the acrive drug.
. Differencesin NSAID half-life generalll'reflect differencesin renal clearance
. The aciditl' of inflamed snovial tissueallou's for increasedp€nelrarion inlo jolnts and a larger
ponion of ulbound drug in qr:oorial fluid
. Joint concentralionsof NSAIDs u'ill remain consunl even uJren senxn concentratiorx flucru:rte.

Ilcchanism of Action
. NSAJDs possessanaleesic-anripvreric.and anti-injlanrmaron' eflects.
. The exao mechanismof action is nol known.
. Therapeutic eflea is Otoughtto be due to the inhibition of prosaglandin (PrG) s1'ntbesis
fyel for
ntanv NSAIDs tlre dose required lo suppressprosugJandrn srnthesis is lower than the doseneededro
produce ann -inllammatory effecrs.)
Prostaglandins:
. Sensitizenociceptorsto the eflects of brad.r,kinin-hisumine and other substances.
r Raise the set point rn tlre ht'pothalamic thermoreguiarory c€nler rhere[' causirg feyer.
r Effects on idlarnrnation are not completell'urdemood
. Some PGs causea direct vasodilatjon and are t-houghtto potenriare t}le eflecrs of brad.r'kinin and
lusamire on blood vesselsresrJnng ir increasedvascu-larpermeabibtl'. r'asodilaudon and edema.
. PGs are t}e brproducu of aracbidonic acid metabolism

142
 t
. Stored in phospholipidsof cell membranes
I
. Liberated ['phospholipases in responselo norious srrmull
.
.
r
Meubolized throug.hc1'cloorl'genase or lipor-r'gcnase.
Leukotrienes are the endproductsof the lipoxt'genasepathuar'.
proslaglandins, prostacl'clin. and thromboranes are tle en@roduos of the o'cloox)'genas€
t
pathuar'.

Cvclrrcrvpenase: nvo disinct forms of the q'clooxl'genase(COX) enzvme.

1. COX-I
. expressedin nrosl tlssuesincluding the Gl tract. krdneys. and blood vessels.
2. COX-2
.
' induced
usuall]'uadetecuble

I
f'oprori'e
i;ili'tr'f:#:ir* :,nmiyJ;i;'.",rffii,
Nabu:netone.Celebrex Vioxr) are associatedu,itl less side eflects.
T
ARA CIIADONI C ACID CASCADE I
PEOSPBOLIPDS

I
I
I
A2
lPhospholipase I
I I
ARACEIDOMC ACII)

Cvcloowgenase
(coxr&:)
T
cYcl-rc
ENDOPERO}fDASES
s-HPETE
1
t
Tbronoboranes Leukotrieoes
I
Prosracl'clin

I
I
I
143
I
I
 PG&
o \/asodilator
o Bronchodilator
o Sensirizespain receplors
o Raises set point in h)'pothalamic thermoregularon' cenrer
o Sumujales GI mucus secretion

@
o Vasoconsrrictor
o Stimujates GI Mucus Secretion

Pr0$acvclin

PGI,
o Vasodilator
o lnhibits platelet aggregaion
o Inhibits gastric acid secretion

Thromboxane

TXA.
o Promotes platelet aggregation

Advcrsc Effeos of NSAIDs

l. Gasrointestinal

. lrlost cornmon side eflect of NSAIDs. (10-20.000 people each vear die fiom NSAID induced GI
conrplications).
. Mosl complicadons involve damageto the mucosal laver and include
. indigestron
. difluse gastritis
. erosions
. ulcerations
. severeGI hemorrhage.
. fusk factors for rhe development of NSAID induced Gl complicauons
. prior hisory of ulcer disease
. advanced age
. cigarene smoking
. alcohol abuse
. high dose/multiple NSAIDs
. concomitant comcosleroid use.
. The relationshjp ur'tb Hebcobacter$'lori is rrnk-neql.
(NSAID i-nducedulcerationscan be trisologicalll drsinguished from H. RJori ulcers.
Addirionalll'. tbe majoritl'of H. h'lori ulcers occur in the duodenum and are
s\mptom2tic- u'bereas mos NSAID ulcers occur in the a:rtru::r of tbe slorn:ch ald are
asrmptonradc.)
. NSAIDs have a dual insult on the GI rao- topical and s1-scmic

144
 l
Tonicaj (direct an{ indrrecl eflect.)
. direct eflecl
due ro rhe rranspon of rhe lipophilic drug into the gasric mucosal cell u'here thq' are
"rdpped" in the cell (Ion Trappirg).
converled back to tlre ioruzed form n'hich becomes
The nrenrbranepernreabilrn'of the nrucosalcell is then altered leading to an influi of
ven'acidic ga$ric juic€ back into lhe mucosalcell (Back Diffusion).
r indirecl cffect

Svslemic
occurs front lhe reflu of bile containing aaive nretabolites. l
' rcsur
"Tf,,:',HtiffiTfi."tri#,iilH:fi,,,
enecrrhq
n,u"ac)lopro,ecrir,e
srimulatemucusr;roducrionand secrerion.simulate HCO3- secretion"inhibit acid
t
secrelion inhibit Gasrrin secretion and enhancemucosal blood floq'.
Various nrerlrodshave been ernplovedin anenrptiug to decreasetlre incidence of GI
Side efleos. Mos are directed at reducing the topical eflea on the mucosa and
ha'r'eno q'stemic eflect (e.g.. buflenng- enteric coatirg prodrugs. nonacidic
T
NSAIDs. adnrinisrrariouuidt food). Therefore. dresenretltods are nlel u'ith linrited
success. The use of qroprotective agenls {e.g.. Mtsoprostol. H2 blockers) has
proven lo be more efl:cacious. SomeNSAIDs are associatedu'itlr less GI side
T
eflects becausethev are rlrougJrtto be less polenl irilribitors of GI prosug:laltdins.

CuoDrolectivc Agcnts
l
l. Misoorostol (C\lotec)-
.
o
.
PGE analogue
prolecu BOTII Ge gasric and duodenal mucosa I
Side effeos: Diarrhea- most colrunon
. lncreasesurerine contractilin- AVOID in pregrrancr'(spont. abonion)

2. lU receptor anuPonists (Cimetidine. Ranilidine- Famotidine)

I
.
.
Block histamine induced releaseof acid from panetal cells
effective in protecting tle duodenal mucos:l I
3. Sucralfate (Carafate)
.
.
Neuralized stomach acids
m?I stimulate PG antlesis
I
' ir:eflective

4. Prilosec t
l*a-st G a-strotoric NSAIDs
1. Nabuntetone(Relafen)
. onll'nonacidic NSAID
I
. prodrug

2.
. SelectiveCOX-2 inhibitor
Etodolac (Lodine)
I
3. Cboline I4agrresium Saliq'late Orilisate)
1. Salsalate(Disalcid)
.
.
BotI Trilisare and Salsalateare nonacenlated saliq'lates
Less potent inhibiton of PG's
I
5. Celebrex
. COX-2inhibitor t
1 A <
t - J
I
I
 2. Fenal

. hosugandrns have several imponant roles in tlre kidnei'

' reeulate vascular lone
. nraintain GFR
. enhancc sodium and saler excreuon
. stimulate Renin secretion
The efTectof renal prostaglandins is negligible in normal circumstances.
Renal Side eflects:
. Acule Renal Failure (ARF)
. fusk factors for the developmenlof ARF include conditions that rcsult in decreased
blood volume (liver disease.diuretjc therapl'. nephrotic srndrome. congesnvehean
failure, sepsis.etc.). S1'stemiclasrconstriction rccurs in tbese circumstancesto mainuin
blood pressure. Rernl PGs are srnthesized ou dernand and plal' a coulterreguJalon role
anenuadng the decrcasein renal blood floq'and GFR thar u'ould ot-beru'iseoccur if t-be
vasoconstrictive forces u'ere left unopposed O-her risk faoors in parients s-ilb norrral
blood volurte include contrasl induced nepluoparhr'.cluonic renal failure. and advanced
age.
. intemitial nephritis
. proteinuria
. nephrotic s-rndrome
. abnormabtresof sodiunr-potassiurn and nater homeostasis

I{asl Ncnhroloxic NSAIDs

l. Nabumetone(Relafen)
2. Etodolac O-odjne)
3. Sulindac (Cliroril)
1. Choline Ntaglesium Saliqlate Orilisate)
5. Salsalate@isalcid)
6. Celebrex (Cox-2 inhibitor)

3. Bronchorrulmonan'
asthma craccrbation.
. Tbe degreeof prosuglandin inhibition correlaleslo the polential for inducing bronchospasn.
. PGF4 is a bronchodilator a:rd stabilizes bistqmi-nestores in mast cells.
. Grealer leukotriene production
e Theorericalll'. rhe inhibirion of n'clooxl,genasealso funnels grealer
atnounls of arachadonjcacid tfuoug} rhe liporl,genase patrnzl' resulung
in. Manv of the leukorienes are bronchoconstrjoors (LTCI and function
as slou' reacting substancesof ananhr.laxes.
. For this rcason NSAJDs rhat inhibir botlr rhe crclooxl'genase and
lipoxl'ge nase (I)- clofenac- K etoprofen) patlru'a'r'sare c on sid ered safcr
ageors
. Paficnts sitb nasal poll'ps. asbma. and nonallergic rhjnitis are al increasedrisk to develop NSAID
induced bronchospasrns.

146
 T
4. Cardiova.scular t
. AnFna
. M'r'ocardid ischcmia
. Lrukotriene D:l (LTDI) is a potent coronan anen' \'asoconsrrictor. Its production mav be
enhancedb' NSAIDs b.r'shunting arachadonjc acid th;oug} the lipoxl'genase parhual'.
I
. Can increase blood pressure througtr its actions on lhe kidnel'. blood vessels. and from Ote increased
sait inuke associatedu'ith sonreNSAIDs. t
5. Bcmatologic
. imrrair platelel aggeeation
. inhibiung tle producuon of tlromborane ,A2 (TXA2)
I
. Aspirin irre'r'ersiblvacen'lalescvclooxlgenase and its eflect lasts for the life of the platelet
(8-12 davs). Plateletslack a nucleusand are unableto srnthesizea new enzvnre. All olher
NSAIDs reversiblv inhibjt q'clooxl'genase and t}eir eflect persrss for the rime rhat efleclrve
serum NSAID conceDtrzttions are present. Therefore. lo ensure rerurn of normal platelet
I
fir:rction aspirin should be discontinued 8-I2 davs prior to surgen'. Other NSAIDs should be
discontinued4-5 half lives prior lo $uBen' (Piroricam becauseof its long half Iife requires
8-10 da1'sfor completereversal).
I
. Blcrrd dvscrasias- rare effecls of NSAID use
. leadine causeof death aftributed to NSAID treras\'.
. Aplasrc alemia
I
' Agranulocrrosis
.
.
Hemol]'uc anemia
Thromboqloperua
(Aplanic anemia and agranuJocvtosisis utore frequentlv irnplicated u'ith Plrenrlbulqroue and
I
Indometlracinuse.)
I
6. Ilcnatic
A transient asmptomatjc elevation jn serum transaminasescan occur in up to I5% of NSAID
rreated patients. Possiblemechanismsfor hepatocellular inlun' include drug hlpersensitivrrv and rhe
I
formetjon of reactive i,ntermediatemetabolites. hrazoles, proprionic acids and irdole deri.r'ativesshot'
rhe grearestpropensin'for severeliver damage zuch as hepatitis and cholestasis. Diclofenac has also been
reponed to be relarivelv hepaloloxrc. I
7. Ccntral ncn'ous svslcm
. Headaches
I
. lndomcthacin causesdose related beadachessecondan'to its cerebral vasoconstrictive

. Tinnirus
eflecu.
I
. Confusion
o
.
lrntabili['
lnsomnia
I
o Pizz jasg5
. Jdros_rrecraticasepticmeningltis
(mosr likelr a h1'persensitirin'reactjon) has been associatedu'jth lbuprofen- Tolurentin and
Sulindac used il patienu nith SLE or otler collagen vascular djseases
I
of theseeflecrsare reversible$'ith discontinuation of t}e drus
The nraiorin'
I

1 4 1
I - t
I
I
 -
8-. AEicular Caitil@e
NSAIDs are ven' effective in rreatingioint inJlammarionbecauseof their abilin ro gain acc€ssto
srnorial fluid hou'ever lhere is evidencethat thel mal acrualll conrriburero ioint destrucrion. There is
conflictrng information regarding tbe role of NSAIDs rn prevenrrngor producurg caniJagedesrructjon.
Throupfr the inhibition of prosugl3nrlin5 ald cenain inflanrmaron'cells NSAIDs prevent carriJage
desructron Hou'ever. NSAIDs mav inhibit cenain asrrectsof carrilape reoair bv reducins the s\nthesis of
hlaluronic acid and glvcosaminoe]vcaru

DRUG INTERACTIONS
l. \4'arfarin
Warfarin is highlv bound to plasma proteins and is rapidll'displaced bv NSAIDs. The active
"free"
level of \\'arfarin is then increased Tbe combinarion of NSAID induced plarelet inhibiuon and the
\\/arfarin induced inlu..birjonof the coaguJationsvslem predisposesrheseindi.riduals ro seriousbleeding
cpisodesgranicularl'r'Gl bleedsdue ro rhe effecrof NSAIDs on rhe somach!).

2. Anticpilcpfic agcnts
Arazole NSAIDs interfere uith the nteubobsm of Phenrroin producing increasedplasma
concentralions and increasethe likelihcnd of toxjcin. Additionallv Phenrroin and Vaiproic acid are
hjghlf'prolern bourd u'hich can be easill'displacedbl NSAIDs

3. Corticosreroids
Conicoseroids increaselhe rale of sabo'late clearanceand reduceirs plasma concentration.
Contbiruuon Corticosteroid/NsAlD Orerapvconsiderabll increasesthe risli of GI side efleas.

4. Probcnecid
Probenecid increasesthe plasma concenualion of NSAIDs bv reducing their renal excrelion-
compcting for albumin binding sites. and competing for liver glucuronidarion enz\Tnes.

5. E-r'pogl.r'ccmicagcnts
Sulfonvlureasare hig}Iv bound to plasma proreins ard can be displacedfiom their binding sires
bl NSAIDs leadrng to a dangeroush1'pogl1'cemic evenl. SalioJares have a hvpoglycemic effeo
tbemseh'es. $razole NSAIDs can also inljbil rhe metabolism of sulfonylureas.

6. Antihl'perleosive agenls
NSAIDs can antagoni"e anti-b1'penersiveagenls througl several mechanisrns; most cagse
sodium and uzler retention- suppressionof plasma renin. suppressionof adrennl ;ggsplsrs. and impaired
prosraglandin s\T1hesrs.

7. Lithium
Lithium is almost entirelv eUminatedthroug} the bdnev and its clearanceis significanth'
reduced Qv the coadministration of an NSAID.

8. Itelhotrexale
Metlrouerate is predominantlv elimjnated throug-brhe kidnevs and its clearancers reducedbrl the
coadmini sradon of NSNDs.

9. Dieoxin
NSAIDs increaseserum Digorin levels br decreasingirs renal clearance.

148
 t
Salicttlntes Entenc coaled 8lmg a000mg/da1'
325m9
500 mg
in divided doses
I
Salsalate Disalcid
Salflex
500mg
750mg
3000m9/da1'
J dir,doses I
CholineMg* Trilisate 500mg 2000-3000mg/da1'
Salicvlate 750mg
J000mg
rn div doses
I
Trilisateliquid 500mg/5mJ peds-50mg/kglda1'

DiJlunisal Dolobid 250m9

500m9
-500-l500mg/da1'
in d:r'doses
l500mg T
h,razoles
Phenr'lbutazone l00mg 100m9/da1'
in di.r.doses
400mg t
lndoh:actic acids
lndomethacin lndocin 25mg
50mg
75-J50mg/da1'
rn dirided doses
200mg I
50mgsuppos

lndocir SR
25mgl5nrJsusp
75mg I
Sulindac Clinoril l50mg 3O0-100rny'dal 4OOmg {
200rng in dirided doses
h,rrolocaic Acids
Tolmentir: Tolectin 200mg
600mg
600-l8O0mg/dav
in div doses:pediau-
l800mg I
Tolecdn DS 400m9 l5-30m8/lgldav
Proprionic Acids
Ibuprofen Motrin
Rufen.Nuprin
IBU 200mg
300mg
1200-3200mg/day
in div doses
3200ng
I
Adyil 400mg
600mg
800mg
t
Childrenslr4otrin l00mg/5nrJ 2}-aomgkgldal. a0mg/kg/da
]'
I
ChildrensAdvil susDension

Naproxen Naprosn 25Omg 500-l500mg/da1' l500mg

I
1*ec=availin 375m9(ec) in div doses:
enlenccoated) -s0Qmg(ec)
l25mg/5urJ
susoension
ped:arrjc-
t0mg,&g/dar l5mgilg I
Naproxen
Sodrunr
Anaprox 275 mg
.Anaprox DS/AIev'e 550/220mp
500-l l00mpda1'
ir divided doses
l375mg t
r49
l
T
 hoprionic Acids
connnued Ketoprofen Orudis 25mg 100-300mg/dar' 300mg
5Omg in dn'doses
75mg
Oruiail l00mg ir singJeor
(ernrelease) l5Omg divided doses
200mg

Fenoprofen r.Nalfon 200mg 1200-3200mg/dar' 3200mg

300m9 in div doses
600mg

Flurbiprofen Ansaid 5Omg 200-300mg/rt"-r' 300mg

I 00nrg in div doses

Oxaprozin Dalpro 600mg 600-l200mg/da1' l800mg

or
in one or dn' doses 26mglkg
Phenl:lacaic Aci.fu
Diclofenac Na" Voluren 25mg
5Omg 100-20ttmgidav 200mg
75mg in div doses
Diclofenac IC Cau-Ilam -50mg
Anthronilic Acids
lr{eclofenamate Irdec)omen 5Omg 200{00m9/dar' 400mg
sodium lOOmg in div doses
Oxicoms
Piroxicam Feldene lOmg l0-20m9/da1' 2Omg
20mg
Nopthvlolkonones
Nabumetone Relafen 500mg 1000-2000mg/dal 2000m9
750m9 in one or trvo doses
Tatahydroindoles
Etodolac Lodine 200mg 800-l200mg/dar' l200mg
300m9 in div doses
400mg
500mg
Pvrrolopvrrok
Xetorolac Toradol l5mgrmJ gngte ctose:
Trometlnmine 30mgimJ <651'o60mgIM: 30mgIV
X5y'o. renalfailure.or
<50kg-30mgIM; l5mg IV
mulnple dose:
<65yo-30mgq6h IIWTV l2Omg
>651'o.renal failure. or
<50k9- l5mg q6b Ilvl/TV 60mg
** fV bolus>15 seconds
lOmg lOmgq6h 4Omg
*]rllaxmun Durati on ofuse is 5 Dars PO, INL ADd IV

150
 I

)
T a b l e sa n d F o r m u l a s
C r e a t i n i n eC l e a r a n c e= (Leankg) (140- age)(0.85 if 'femate)

Inormal > 80] ( 7 2 ) ( s t a b l ec r e a t r n r n e )

W t . - [ ( a c t u a l - i d e a l )x 4 O / o ] + i d e a l b o d y w e i g h l

ldeal Bodv Weisht: T

S t a r l a t h e i g h to f 5 ' 0 " e q u i v .t o 1 0 0 l b s .
- tor males addTlbs./ inch >5ft
- f o r f e m a l e sa d d 5 l b s . / i n c h > 5 f t

)
B o d - vS u r { a c eA r e a ( B S A ) = s q u a r e r o o t o f I h e i e h t ( c m ) x w e r q h tGs)l
[rn m?] 3600.
F
L

Therapeutic Drug Levels

Drgoxin O . 5 - 2 . 2n g / m l
G e n t a m i c i np e a k 4-6 mg/ml
G e n t a m i c i nt r o u g h 7 -2 mg/ml
>
L i d o c ai n e I - 5 mglml
Lithium O . 5- 1 . 5 m e q / m l
P h e n o b a r b i t Ia 15- 40 mg/ml
,
Phenytoin 1 0 - 2 0 m g /m l
b
Theophylltne 1 0 - 2 0 m g /m l
T o b r a m y c i np e a k 4 - 6 mg/ml
T o b r a m y c i nt r o u g h 7 -2 mg/ml
>
V a n c o m y c i np e a k 18- 40 mg/ml
F
V a n c o m y c i nt r o u g h 5- 10mg/ml

Antidotes
Torin Antidote
r'
A c e t am i n o p h e n N . A c e t y l e y s t e r n( m
e ucomyst)
)
Benzodiazepine Flumazenii

r51
 -
Tbxiii- Antidote
H e p ar i n Protamrne
Warfarin V i t a m i nK
Narcotics N al o x o n e
N a r c o l i c - T y p e A n a l e e s i cC o m o a r i s o n s

Drup E q u i - A nlag e s i c Duration Drug Equi-Analgesic Duration

Roule Dose(MG) (HR) R o u t e D o s e( M G ) (HR)

(agonists) ( m i x e d a g o n i s t- a n i a g o n i s t s )
Morphine B u t o r p h a n o l( S t a n d o l )
rM t0 4 - 5 lM 2 3 - 4
A t r
PC 30-60
R 6 0 4 - 5

H y d r o m o r p h in e ( D i l au d i d ) B u p r e n o p hni e ( B u p r e n e x )
rM 1.5 4 - 5 tM 0.3- 0.6 4 . 6
PO 4.7.5 4 . 5
R 6 4 - 5
N a l b u p h r n e( N u b a i n )
tM t0 3 . 5
(agonists) mired agonist - antagonists)
L e v o rp h an o l ( L e v o - D r o m o rna)
rM 2 4-6 P e n t a z o c a i n e( T a l w i n N x )
P O 4 4-6 PO 180 2 - 4
Oxycodone
PO 30 3 - 4

Methodone
tM 10 4 - 6
PO 20 4 . 6

M e p e r i d i n e( D e m e r o l )
rM lo0 2 - 4
PO 300 2-4

Codeine
rM 130 3 - 5
PO 200 3 - 5

t52
 t
R e l a t i v e P o l e n c i e s a n d E q u i v a l e n tD o s e so f C o r l i c o s i e r o i d s (

A p p r o xE
. quiv. Relalrve Relative Duratron
Dose" Anti-inflam Sodium of Action
Glucocorticoid Potenc_v Potency Retaining T 1/2 (hrs)
(s)
Short-actrng
Cortisone
H-vdrocortisone ZU
0.8
l
0.8
1
8-t2
6 - tz
t
In t e r m e d i a t e - a c t i n g ( l )
Prednisone
Prednisolone
5
5
4
4
0.8
0.8
1Z - 5b
12-36
I
M e t h y l p r e d n r s o l o n e4 5 n q
Trramcinolone 4 tv r v
n
t2-36
lz - 50
I
L o n g - a c t i n(gL )
Betamethasone
D e x am e t h a s o n e
0.6
0.6
?
2
n
5
n
0
36- 54
36- 54 I
" T h e s e d o s e r e l a t i o n s h i p sa p p l y o n l y t o o r a l o r i n l r a v e n o u sa d m i n i s t r a t i o n ;
d r f f e r g r e a t l y w h e n i n j e c t e di n t r a m u s c u l a r l yi n t o j o i n t s p a c e s .
r e l a i i v e p o t e n c i e sm a v
t
T o p i c a l C o r t i c o s l e r o i dP o t e n c y

Potency
Level
Drug Slrength Polency
Level
Drug Strength
t
High LOW :
Befnethasone 0.0506 Fluocinolone 0.010a
(Drpolene,Dipasone) (Synar)

Triancinolone
acetonide
(KendogHP,Anstocorl-HP)
0.5% valerate 0.010,6
Eeta.nethasone I
Desoximetasone
[tropicrt)
0.253h
Jnancinolone
(KenaloglLP,
acetonide0.02504
Aristocorl-LP) I
I nlermediate
(Lidex)
Fluocinonide 0 05%
VeryLow I
Betanehasone 0.10k Hydoco'rtisone 2 SYo
(Valisone)

Desoximebsone 0.05% Ftydocrtisone 1.00%

I
I
flropicorl-LP)

Desonide 0.050/6 Hydocortisone 0.5o/5

flndesilon)

Triancinolone
(Kenalog,
acetonid€
Aristocort)
0.050/6
I
t
I
153
t
 SrjbStanceS
w h i c h m a y d i s c o l o ru r i n e

Black/Brown/Dark Red
Cascara Chloroquine Amrnopyrine Daunorubicin
F e r r o u ss a l t s F e r r o u ss u l f a t e Doxorubinicin lbuprolen
Furazolidone lvlethocarbamol ldarubrcrn Oxyphenbutazone
M e t r o n i d a z o r eN r t r o r u r a n t o i n phenyrbutazone p h e n y t o r n( p r n k )
Quinine Senna phenothiazines phensuxrmide
Riiamprn Senna
Blue Oranee/yellow
M e t h y l e n eb l u e Triamterene Acetanilid Heparrn
Phenazopyridine Rifampin
Blue./Green Sulfasalazrne Warfarin
Amitriptyline Indigotindisulfonate
M e l h y l e n eb l u e Resorcinol
Tolonium

Drugs which may discolorfeces

Black Green
Acetazolamide Aluminum
Hydroxide lndomethacin Meoroxyprogesterone
Aminophylllne Amphetamine
Amphotericin
B Bismuth
salts yellow
Chlorpropamide Clindamysin Senna
Corticosleroids Cyclcophosphamide
Black pink,rRed
Cytarabine Digitalis Anticoagulants Aspirin
Ethacrynic
Acrd Fenoussarts Banum Hepann
Fluorouracil Hydnalazrne oxyphenbutazone phenylbutazone
Hyorocortrsone lodideconlaining
drugs Tetrarycline
synrp
lvlelphalan Methyprednosolone
Methytrexele Phenlephrine Orange,/Red
,
Potassium
salts prednisolone phenazopyndrne
Rifamprn
Procabazine Sulfonamides_
@
Tet'zcycline The<phy'line Aluminum
Hydroxide Anilbiotics
(po)
Thiotepa Triamcinlone Banum
Warfann

154
 I
Blue - --
Chloramphenicol biue
Methylene
I
Drug-Lab Test lnterferences
I
Test
SerumALT/AST
M a y i n c r e a s er e s u l t s
Erythromycin
Methydopa
M a y d e c r e a s er e s u l t s
I
S e r u mB i l l r u b i n Ascorbicacid
Dextran
Epinephrine
I
Methyldopa
Rifampin
I
Serum Calcium H y d r al a zi n e Aspirin Heparin

Urine Catecholamines Acetaminophen

S u l fr s o x a z o l e

l o d i n e c o n t a i n i n g R a d i o c o n t r a s tM e d i a
I
Chloral Hydrate
Epinephrine
Erythromycin
Labetalol
I
Levooopa
Methenamine
Methydopa
I
Tetracyclines
Triamterene
I
Serum Cholesterol Aspirin Nitrates
Corticosteroids
Phenothiazines
Vitamin D T
Serum Creatinine Cefoxitin (Jaffe method)
Flucytosine I
Urine Glucose Ascorbic acid
Cephalosporins
Levadopa
( C l i ni t e s t )
Ascorbic acid
Cephalosporins
Levadopa
( C l i n i s t i x ,T e s t - T a p e )
t
Urine Ketone
N a l i d i x i cA c i d

Levadopa
I
Mesna
Phenazopyridine
Salicylates T
Methicillin Cytarabine
CSFProtein
Phenothiazines
Sullonamides
J
Serum Protein Phenazopyridine
l
I
155
I
 Urine Protein -aminogglycosides-
M a g n e s i u m S u l f a t e( L a r g el V d o s e s )
Nafciilin
Phenazopyridrne
Tolbutamide
Tolmeniin

Serum Thyroxrn Heparin Heparin

Blood UreaNitrogen ChloralHydrate C h l o r a mp h e n i c o l S t r e p t o m y c i n

SerurnUricAcid A s c o r b i cA c i d
Catleine
Theophylline
Levadopa

D r u g s t h a t c a n c a u s ef e v e r
Mosi common Lesscommon
Amphoiericin Allopurinal lbupro{en
Cephalosporins Antihistamines L - A s p ar a g i n a s e
Halothane Atropine ptopurine
6-lr4erca
Interferon Azathioprine Methoclopramide
lodides Barbituraates Nifedipine
lsoniazid Benztropine N i t r o fu r a n t o r n
Levothyroxine Bleomycin Para ldehyde
Methyldopa Carbamazepine PGE2
Muromonab - CD3(OKT3) Chlorambucil Procarbazine
Penicillins Cimetidine Q u i n i n es u l f a t e
Phenytoin Cisplatinum Ri{ampin
P r o c ai n a m i d e Clofibrate Ritodrine
Quinidine Cytarabine Salicylates
S t r e p t o k i n as e D au n o r u b i c i n Streptomysin
Urokinase Diazoxide Sulrndac
Vaccines Doxorubicin Streptozocin
Vancomycin F o l i cA c i d Tetracycline
Haloperidol Triamterene
H y d r al a z i n e T r i fl u o p e r a z r n e
Hydroxyurea

156
Druos-Causinqllversg
1 . D r u q l n d u c e d A o l a s t i cA n e m i a Clindamycin Phenolhiazines

Acelazolamide Oral Antidiabelics Clomipramine Phenylbutazone

Antihistamines oxyphenbulazone Dapsone Phenyloin

CarbamazePine Penicillamine Desirpramine Primidone

ChloramPhenicol Phenobarbital Doxycycline Procainamide

Chloroqutne Phenothiazines EthacrynicAcid ProPanolol

Chlorothiazide Phenytoin Ethrosuximide ProhYthiouracil

GoldSafts Propyllhiouracil Fenoprofen Pyrimelhamine

lndomelhacin Ouinidine Flucytosisne Ouinine

Melhimazole Sullonaamides Gentamicin RifamPin

2. Druo lnducedAoanulocvlosis Gold salts StrePtomycin

Acetaminophen lsoniazzid Griseofulvin Sulfa Antibiotics

Acelazolamide Levodopa Hydralazine ThiazideDiuretics

Allopurinal Lincomycin HydroychloroquineTocainide

Para-Aminosalicylic Meprobamale lbuprofen Tolbutamide

Acid
B-Laclam Antibiotics Methazolamide lmipramine VancomYcin

BenzodiazePines Methimazole Indomelhacin

Brompheniramine Melhyldopa 3. Druo lnduced HemolwicAnemia

Carbarnazepine Melronidazole a. lmmune Hemolytic Anemia

Captopril Nilrofuranloin Acelaminophen Methyldopa

Chloramphenicol oxyphenbulazone Para-Aminosalicylic Methysergide

Acid
Chlorpropamide Penicillamine Cephalosporins Penicillins

Cimelidine Penlazocine Chlorpromazine Probenecid

Chlorpropamide Procainamide

a . l m m u n e H e m o l Y t i cA n e m i a ( c o n t i n u e d )
Hydralzine Quinidine Cylophosphamide Phenytoin
HCTZ Quinine Cytarabine Primadone

lbuprofen Rifampin 5 -F l u o r o d e o x y u r i d i nPey r i m e t h a m i n e

lsonrazid Sullonamides 5-Fluorouracil Sulfasalzine

LevoOopa Strepiomycin Hydroxyurea Triamterene

M e l e n a m t cA c i d Tetracycline 6-Mercaptopurine Trimethiprim

l l ^ l ^ H ^ l ^ a
r v r g r P tr d r d r l Tolbutamide Methotrexate Vinblastine

Methadone Triamterene

r57
b . O x i d a t i t e H E m b - | t t i eA n e m i a 5 . D r u g l n d u c e dT h r o m b o c y t o p e n i a

A s c o r b i cA c i c j Menadiol A c e t a z o l a m r c jHey d r o c h l o r o t h r a z t c j e

Aspirrn M e t h y l e n eB l u e Allopurinol lsoniazid

Benzocaine Nitrolurantoin Amrnoglutethimrde Meclofenamate

C h l o r a m p h e n r c o l N i t r ou
f razone P a r a - A m t n o s a l i c y l r cM o r p h t n e
Acid
Chloroquine Phenazopyridine Amrinone Penicciltn

Dapsone cephalothin Phenylbutazone

S al a z o s u l f a p y r i d i n e Chlorothrazrde Phenytoin

Diazoxide Crmeirdtne Procainamtde

Desipramine Quinidine
Drazepam Quinrne
4 . D r u p l n d u c e dM e s a l o b l a s t i cA n e m i a D r u q l n d u c e d T h r o m b o c y l o p e n i a( c o n t )
P a r a - A m r n o s a l i s y l i cN e o m Y s i n Digitoxin Rifampin
Acid
Azathioprine Nitro{urantoin Fu r o s e m i d e Sulfisoxazole

Chloramphenicol Oral Contraceptives H e p ar i n Trimethoprim

Colchicine Phenobarbital

I )Li