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Concept
Teicoplanine
Résumé
Teicoplanin is an antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and Enterococcus faecalis. It is a semisynthetic glycopeptide antibiotic with a spectrum of activity similar to vancomycin. Its mechanism of action is to inhibit bacterial cell wall synthesis.
Teicoplanin is marketed by Sanofi-Aventis under the trade name Targocid. Other trade names include Ticocin marketed by Cipla(India).
Oral teicoplanin has been demonstrated to be effective in the treatment of pseudomembranous colitis and Clostridium difficile-associated diarrhoea, with comparable efficacy with vancomycin.
Its strength is considered to be due to the length of the hydrocarbon chain.
Teicoplanin is produced by so-called "rare" actinobacterium Actinoplanes teichomyceticus ATCC 31121, belonging to the Micromonosporaceae family. Biosynthetic pathway leading to teicoplanin, as well as the regulatory circuit governing the biosynthesis, were studied intensively in recent years allowing to construct an integrated model of the biosynthesis.
Teicoplanin targets peptidoglycan synthesis making it an effective antimicrobial against Gram-positive bacteria including Staphylococci and Clostridium spp. The following represents MIC susceptibility data for a few medically significant pathogens:
Clostridium difficile: 0.06 μg/ml - 0.5 μg/ml
Staphylococcus aureus: ≤0.06 μg/ml - ≥128 μg/ml
Staphylococcus epidermidis: ≤0.06 μg/ml - 32 μg/ml
Teicoplanin (TARGOCID, marketed by Sanofi Aventis Ltd) is actually a mixture of several compounds, five major (named teicoplanin A2-1 through A2-5) and four minor (named teicoplanin RS-1 through RS-4).
All teicoplanins share a same glycopeptide core, termed teicoplanin A3-1 — a fused ring structure to which two carbohydrates (mannose and N-acetylglucosamine) are attached. The major and minor components also contain a third carbohydrate moiety — β-D-glucosamine — and differ only by the length and conformation of a side-chain attached to it.
Source officielle
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