Glycopeptide and other antibiotics

Dr. Johan

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

Glycopeptides Vancomycinobtained from the fungus streptomyces

orientalis

effective against Gm+ve Cocci, MRSA, Corynebacterium diphtheria, enterococcus fecalis, clostridium tetani and C. PerfringensMOA

Bactericidal, acts by inhibiting cell wall synthesis

Binds to terminal end of peptidoglycan pentapeptide and inhibits addition of amino acids

GlycopeptidesGiven 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

glycopeptidesUses: 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.

Glycopeptides Telavancin, Dalbavancin, OritavancinSecond gen glycopeptides TelavancinExhibits rapid bactericidal activity t1/2 8 hrs.more potent than vancomycin

against MRSA (approved by FDA) DalbavancinExtremely long acting with half life of

6-11 daysOnce weekly for skin, soft tissue and

catheter related infections. ( Pending FDA approval)

Glycopeptides OritavancinPrevents transglycosylation and

transpeptidation during cell wall synthesis

Effective against VRS & VREPhase IV trial for skin, soft tissue and

MRSA infections.

Glycopeptides TeicoplaninSimilar to vancomycin - acts by cell

wall synthesis inhibition Bactericidalstaphylococci can develop resistance.More active than vancomycin against

enterococci but equally effective against MRSA

Can be given safely IMHalf life about 50 hrs.Occasional bronchospasm.

Glycopeptides Ramoplanin

Analogue of teicoplanin.Oral administrationUsed for treating C. difficile induced

PMC and to eliminate VRE from gut.

Miscellaneous group DaptomycinLipopeptide 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

Adverse effects-GI disturbances, rash, headache and rarely muscle discomfort/weakness.

Used in MRSA and vancomycin resistant skin and soft tissue infections.

Miscellaneous group BacitracinEffective 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

Miscellaneous group FosfomycinPhosphonic acid derivative.BactericidalStaph. 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.

Miscellaneous CycloserineEffective against G+ve and G-ve

bacteria.Second line drug in TBCan cross BBB and placenta.Half life is 10 hrsAdv effects - dose related CNS side

effects. folate and B12 deficiency.

Elevated serum aminotransferases levels

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