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MISCELLANEOUS CHEMOTHERAPEUTIC AGENTS, MISCELLANEOUS CHEMOTHERAPEUTIC…
MISCELLANEOUS CHEMOTHERAPEUTIC AGENTS
MISCELLANEOUS CHEMOTHERAPEUTIC AGENTS
Vancomycin
MOA
inhibits synthesis of bacteria cell wall phospholipids
inhibits peptidoglycan polymerization
binds to D-Ala-D-Ala side chain of precursor pentapeptide
prevents transglycosylation step in peptidoglycan polymerization
weakening cell wall
damaging the underlying cell membrane
Resistance
1) Plasmid-mediated changes in permeability
2) Decreased binding of vancomycin to receptor molecules
Uses / Spectrum
Tricyclic glycopeptide
Against multiple drug-resistant organisms:
MRSA & Enterococci
Wide variety of Gram+ve
Pharmacokinetics
Slow IV infusion: 60-90mins - for systemic infections & prophylaxis
NOT orally absorbed
Inflammation allows penetration to meningitis
Metabolism of drug is minimal
90-100% excreted by glomerular filtration
Adverse effects
Infusion site - Inflammation of vein: Fever, Chills, Phlebitis
Rapid infusion - Histamine release: Flushing, Shock
Patient with renal failure - Drug accumulation: Dose-related hearing loss
Ototoxicity
Nephrotoxocity - Restricted for TOPICAL application
Teicoplanin
Treat serious infections - Gram+ve bacteria:
Methicillin-resistant S. aureus & E. faecalis
Glycopeptide antibiotic (similar spectrum to Vancomycin)
MOA: inhibit bacteria cell wall synthesis
Quinupristin/Dalfopristin
Adverse effects
Venous irrigation
Arthralgia
Myalgia
Hyperbilirubinemia
Interactions
inhibit cytochrome P450 isoenzyme
concomitant administration with drugs that are metabolized by CYP450 - TOXICITY
Interact with Digoxin
MOA
Bactericidal - long post antibiotic effect
binds to separate site of 50S ribosomal subunit, forming stable ternary complex
synergistically interrupt protein synthesis
Uses / Spectrum
derived from Streptomycetes
combination Quinupristin/Dalfopristin - 30:70
Against Grma+ve cocci
Against those resistant to other antibiotics:
Vancomycin-resistant Enterococcus faecium (VRE)
Primary use for E. fascium infections
Fusidic acid
Inhibit Bacteria protein synthesis
Against Gram+ve: Staphylococcus sp. & Corynebacterium sp.
Only TOPICAL for:
boils
folliculitis
sycosis barbae
cuteneous infections
Linezolid
Pharmacokinetics
Completely absorbed on oral administration
widely distributed
metabolites may hv antimicrobial activity
Excreted in renal & non-renal routes
metabolites excreted through urine
Adverse effects
generally well-tolerated
GI upset, nausea, diarrhea
Headache
Rashes
Thrombocytopenia - 2% for use >2 weeks
MOA
inhibits bacteria protein synthesis
binds on 50S ribosomal subunit, interfere translocation
Uses & Spectrum
Combat/ Against resistant Gram+ve organisms:
Methiciline- & Vancomycin-resistance Staphylococcus
Vancomycin-resistant Enterococci faecium
Vancomycin-resistant Enterococci faecalis
Penicillin-resistant Streptococci
Corynebacterium species
Listeria monocytogenes
Mycobacterium tuberculosis - moderateactive
Cidal against - Streptococci & Clostridium perfringes (Bactericidal)
Polypeptide antibiotics
Clinical used agents: Polymyxin B, Colistin, Bacitracin, Tyrothricin
Low molecular weight
Powerful bactericidal
Restricted due to toxicity
Clindamycin
Side effects
Rashes, Urticaria
Abdominal pain, Diarrhoea
Pseudomembranous enterocolitis caused by overgrowth of Clostridium difficile
Uses
Abdominal pain associated trauma - Bacteroides fragilis
Pelvic & Lung abscesses - Bacteroides fragilis
combined with Pyrimethamine for Toxoplasmosis in AIDS patient
combined with Primaquine for Pneumocystis carinii
Pharmacokinetics
oral route
well-distributed into all body fluids, EXCEPT CSF
at adequate levels, not achieve in brain
penetrate into bones
undergoes extensive oxidative metabolism to inactive products
excreted into bile or urine by glomerular filtration
Drug interactions
Potentiate neuromuscular blockers
Mutual antagonism with Erythromycin & Chloramphenicol at ribosomal level
MOA & Spectrum
Binds to 50S ribosomal subunit
inhibits protein synthesis
active against anaerobic bacteria - Bacteroides fragilis
against most Gram+ve cocci