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Tetracycline
Chloramphenicol
Macrolide
Lactone ring + deoxy
sugar
Quinolone
MOA
-irreversible, cidal
-passive diff via porin
across OM
-O2-dep transport
-30S
-conc dep
-reversible
-passive diff & active
-30S
-prevent tRNA bind to
A site
-reversible, static
-50S
-inhibits peptidyl
transferase
-inhibits peptide bond
formation
PK
A: hydrophilic (IM/IV)
D: x cross BBB
M: E: glomerular filtration
-significant PAE
A: PO (--food, cation,
alkaline), IV
D: calc tissue,
placenta
M: enterohepatic
E: U&B
A: prodrug hydrolysed
D: CSF
M: glucuronyl
transferase
E: renal secretion
(90%)
-usually cidal
-G-ve: block DNA
gyrase (transcription,
repair, replication)
-G+ve: block
topoisomerase IV
(separation of
replicated DNA)
A: PO, IV
D: wide
M: liver
E: secretion, filtration
Clinical
uses
-aerobic, G-ve
-sepsis
-bact endocarditis
-tualraemia, plague
-TB
-infected burns
-cholera
-severe acne
-mixed resp infections
-periodontal
-H. pylori
-M. pneumonia,
chlamydiae,
rickettsiae
-for life-threatening,
serious infections
-bacterial meningitis
-rickettsial infections
-eye infections
-irreversible, cidal
-50S
-inhibit elongation of
peptide bond
(interfere initiation
complex formation,
blocks ribosome
translocation)
A: PO (ester, enteric
coating, stearate)
D: placenta, x cross
BBB
M: enterohepatic
E: U- 5% active
B- 95%
-strep & staph
infections
-syphilis
-whooping cough, CAP
-orodental infections
-prophylaxis for bact
endocarditis
SE
-ototoxicity
-acute renal failure
-nondepolarising
neuromuscular
blockade
-BM disturbance
(anaemia, erythroid
suppression)
-GIT
-Gray Baby Syndrome
-arthropathy,
tendinitis
-nausea, diarrhea
-avoid in pregnant
-avoid in prolong QR/
pt receiving
antiarrhythmia
-photosensitivity
Lincosamine
Vancomycin
Glycopeptide
Metronidazole
Sulfonamide
PABA analog
Trimethoprim
Structure
Structure
-GIT infections
(infectious diarrhea,
enterobact)
-resp infections (TB,
URTI, LRTI)
-GUT infections (UTI,
STD)
MOA
=macrolides
=-lactam
-cidal
-static
-inhibit
dihydropteroate
synthetase
-static
-inhibit dihydrofolate
reductase
-cidal
-reacts with bact DNA
(inhibits replication,
fragmentize existing
DNA)
A: PO, IV, rectal
D: wide
M: liver
E: U
PK
A: PO, IV
D: plasma protein
bound, x cross BBB
M: liver
E: U&B
A: PO
D: CSF, placenta,
protein-bound
M: liver (variable)
E: glomerular filtration
A: PO
D: CSF
M:
E: U
Clinical
uses
-sepsis
-AAPC, MRSA
-endocarditis (+AG)
-antiprotozoa
-anaerobes
-periodontitis, ANUG
-oral non-absorbable
(inflammatory bowel
disease)
-topical ( bact
conjunctivitis,
trachoma, burn
wounds)
SE
AAPC (suppress
normal flora, allow
Clostridium difficile
overgrow, produce
exotoxin A&B, colon
tissue necrosis
-HS (flushing,
hypotension,
tachycardia)
-phlebitis
-nephrotoxicity,
ototoxicity
Structure
Penicillin
-lactam (6-aminopenicillanic
acid) + R
MOA
-mimic D-Ala-D-Ala
-disulfiram-like effect
-nausea, headache,
metallic
-oral candidiasis
-potentiates warfarin
effect
Monobactam
Monocyclic -lactam
ring
Carbapenem
-antifolate effect ( BM
depression,
megaloblast anaemia,
leuko- &
granulocytopenia, HS)
-TMP-SMZ
(=sulfonamide, GIT
upset, HS)
Cephalosporin
Thiazolidine ring +-lactam ring +
R1 + R 2
=-lactam
Clinical
uses
SE
A: PO, IM
D: placenta; bone& CSF when
inflamed
M: liver insignificant
E: active tubular secretion (90%),
GFR, as active molecule,
inhibited by probenecid
Natural: G+ve, clostridium,
spirochete, G-ve anaerobe
Antistaph: staph with lactamase
Aminopen, antipseudo: UTI, LRTI,
sinusitis, otitis, pen-resistant
pneumococci, pseudomonal
infections
A: IV
D: CSF
M:
E:
A: IV
D:
M: dehydropeptidase
I (inhibited by
cilastatin)
E:
A: PO (*1st), IV (most)
D: good
M:
E: active secretion except
ceftriaxone (bile)
-mixed aerobic
+anaerobic
-pseudomonal
infections
--lactamase
producing
enterobacter
-phlebitis
-GIT disturbances,
skin rash, rxn at
infusion site
-seizures in renal
failure