17 Glycopeptides, Fusidans, Lipopeptides, Bacitracin, Mupirocin Flashcards
Which are the glycopeptide drugs?
- Vancomycin
- Teicoplanin
- Dalbavacin
- Telavancin
What is the mechanism of action and the antibacterial spectrum of glycopeptides?
Mechanism of action:
-
Cell wall synthesis inhibitor:
- Binding to the d-Ala-d-Ala terminus ==> inhibition of the transglycolase
Antibacterial spectrum:
- Gram (+) bacteria (Staphylococcus aureus, MRSA/E, enterococci, Corynebacterium jeikum, Clostridium difficile)
- Its activity against penicillin-sensitive bacteria is lower than that of penicillins
What are the indications for vancomycin?
Pharmacokinetics?
Adverse effects?
Indication:
- Serious infections caused by:
- MRSA/MRSE
- Ampicillin resistant enterococci (in combination with gentamycin)
- Severe pseudomembranous colitis not responding to metronidazole (–> oral administration)
- Monitoring of serum concentration is strongly recommended in case of risk (administration together with aminoglycosides)
- Narrow therapeutic range
Pharmacokinetics:
- Elimination via the kidney
- Poor penetration into the CNS
- Never given in bolus to avoid the histamine release
Adverse effects:
- Nephrotoxicity, rarely ototoxicity
- Red man syndrome for Vancomycin (histamine release)
Teicoplanin, glycopeptide!
Same antibacterial spectrum, slower elimination, less toxicity (no monitoring)
Dalbavacin, glycopeptide!
- Half-life: 6-11 days, 1x/week for two weeks
-
Indication:
- MRSA/VRSA infection
- Skin and soft tissue infection
Telavacin, glycopeptide!
- Dual action: as vancomycin + change the membrane potential, the membrane permeability
- Indication: nosocomial pneumonia (if nothing else is acting)
- Nephrotoxicity – higher risk than with vancomycin
What is fusidans?
Mechanism of action?
Spectrum?
…
Mechanism of action:
- Inhibits the translocation by acting on the elongation factor
Spectrum:
- Gram (+) bacteria (staphylococci)
- No action against gram (-)
Pharmacokinetics:
- Oral, parenteral and topical
- Good distribution, but not into CSF
Indication:
- Serious staphylococci infection
- Cutaneous infections
- Osteomyelitis
- Pneumonia
- Septicemia
- Wound infection
- Endocarditis
- Superinfected cystic fibrosis
Adverse effects:
- GI
- Hepatotoxicity
What are the lipopeptides?
Drug?
Mechanism of action?
Spectrum?
…
Drug:
- Daptomycin
Mechanism of action:
- Cell wall inhibitor:
- Binds cell membrane via Ca2+-dependent insertion causing depolarization and increased K+ efflux ==> cell death!
- Bactericidal
- Binds cell membrane via Ca2+-dependent insertion causing depolarization and increased K+ efflux ==> cell death!
Antibacterial spectrum:
- MRSE
- Polyresistant gram (+) cocci
Indication:
- Complex skin infections and skin structure infections
- Staph Aureus bacteremia
- Including right-sided endocarditis
Administration:
- IV infusion 1x/day
Adverse effects:
- Myopathy
- Increase of creatinine kinase
-
Contraindications:
- Pulmonary infections as it is inactivated by surfactant
What is bacitracin?
Mechanism of action?
Spectrum?
Administration?
Adverse effects?
Mechanism of action:
- Cell wall inhibitor:
- Interferes with dephosphorylation of the lipid carrier transferring peptidoglycan
Antibacterial spectrum:
- Gram (+) bacteria
Administration:
- Topical
- Sometimes in combination with neomycin or polymyxin
Adverse effects:
- Nephrotoxic
What is mupirocin?
Mechanism of action?
Spectrum?
Pharmacokinetics?
Indication?
Adverse effects?
Mechanism of action:
- Protein synthesis inhibitor
- Inhibits isoleucyl tRNA synthesis
Spectrum:
- Gram (+) bacteria (resistant staphylococci)
Pharmacokinetics:
- Topical application
- Poor absorption
Indication:
- Dermatology (impetigo)
Adverse effects:
- Nephrotoxicity!
