Glycopeptide antibiotics dr. johan

Glycopeptide antibiotics dr. johan

1. Glycopeptide and other antibiotics Dr . Johan

2. Antibiotics inhibiting cell wall synthesis Glycopeptides : Vancomycin Dalbavancin , Oritavancin , Telavancin (DOT) Teicoplanin and Ramoplanin Daptomycin Bacitracin Fosfomycin Cycloserine Miscellaneous group

3. Glycopeptides Vancomycin obtained from the fungus streptomyces orientalis effective against Gm+ve Cocci , MRSA, Corynebacterium diphtheria, enterococcus fecalis , clostridium tetani and C. Perfringens MOA Bactericidal , acts by inhibiting cell wall synthesis Binds to terminal end of peptidoglycan pentapeptide and inhibits addition of amino acids

4. Glycopeptides Given IV 2gm in divided doses Bacterial resistance can develop so use judiciously to Pts having PMC. Adverse reactions: Local thrombophlebitis, generalized cutaneous reactions (Red Man syndrome) and auditory damage Mainly eliminated by the kidney – use with caution in renal damage

5. glycopeptides Uses: used in penicillin and cephalosporin resistant infections, MRSA and E.fecalis infections Adequately controls acute staphylococcal enterocolitis and pseudomembranous colitis Vancomycin + gentamicin = synergistic effect useful in enterococcal endocarditis.

6. Glycopeptides Telavancin , Dalbavancin , Oritavancin Second gen glycopeptides Telavancin Exhibits rapid bactericidal activity t 1/2 8 hrs. more potent than vancomycin against MRSA ( approved by FDA) Dalbavancin Extremely long acting with half life of 6-11 days Once weekly for skin, soft tissue and catheter related infections. ( Pending FDA approval)

7. Glycopeptides Oritavancin Prevents transglycosylation and transpeptidation during cell wall synthesis Effective against VRS & VRE Phase IV trial for skin, soft tissue and MRSA infections.

8. Glycopeptides Teicoplanin Similar to vancomycin - acts by cell wall synthesis inhibition Bactericidal staphylococci can develop resistance . More active than vancomycin against enterococci but equally effective against MRSA Can be given safely IM Half life about 50 hrs. Occasional bronchospasm.

9. Glycopeptides Ramoplanin Analogue of teicoplanin . Oral administration Used for treating C. difficile induced PMC and to eliminate VRE from gut.

10. Miscellaneous group Daptomycin Lipopeptide antibacterial Binds to the bacterial plasma membrane causing membrane depolarization and release of intracellular ions – causes cell damage Spectrum similar to Vancomycin and includes MRSA, VRSA and VRE . Excreted by kidney

11. Adverse effects -GI disturbances, rash, headache and rarely muscle discomfort/weakness. Used in MRSA and vancomycin resistant skin and soft tissue infections.

12. Miscellaneous group Bacitracin Effective against Gm+ve organisms like, streptococci, staphylococci, pneumococci and enterococci. Corynebacterium , gonococci, meningococci , Cl. Tetany , treponema and H.influenzae are highly sensitive. Topical antibiotic used as antiseptic Do not develop resistance Adverse effects : Marked nephrotoxicity

13. Miscellaneous group Fosfomycin Phosphonic acid derivative. Bactericidal Staph. a ureus , streptococci, enterobacteriaceae , H. influenzae and neisseria are susceptible. Synergistic effect with penicillins , cephalosporins and aminoglycosides. 3g oral dose is used to treat UTIs in women. Adv effects: GI distress, skin rash, exacebration of asthma and cholestatic jaundice.

14. Miscellaneous Cycloserine Effective against G+ve and G- ve bacteria. Second line drug in TB Can cross BBB and placenta. Half life is 10 hrs Adv effects - dose related CNS side effects. folate and B12 deficiency. Elevated serum aminotransferases levels

15. Summary Cell wall synthesis inhibitors Active against gram + ve cocci Mostly used for skin, soft tissue infections & PMC What you have to know from this topic: A/E of vancomycin - VSAQ Uses of glycopeptide antibiotics- VSAQ Name few glycopeptide & lipopeptide antibiotics- VSAQ