This document summarizes various antibiotics that inhibit cell wall synthesis, including glycopeptides like vancomycin, dalbavancin, telavancin, teicoplanin, and ramoplanin. It also discusses the lipopeptide daptomycin and other antibiotics such as bacitracin, fosfomycin, and cycloserine. The antibiotics covered are primarily effective against gram-positive cocci and are commonly used to treat methicillin-resistant Staphylococcus aureus (MRSA), skin and soft tissue infections, and pseudomembranous colitis.

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