Glycopeptide antibiotics dr. johan

1. Glycopeptide and other antibiotics
Dr. Johan

2. Antibiotics inhibiting cell wall synthesis
Glycopeptides:
I. Vancomycin
II. Dalbavancin, Oritavancin, Telavancin (DOT)
III. Teicoplanin and Ramoplanin
IV. Daptomycin
V. Bacitracin
VI. Fosfomycin
VII.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
 t1/2 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. aureus, 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