Glycopeptide antibiotics dr. johan
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Transcript of Glycopeptide antibiotics dr. johan
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