About: Telavancin     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Telavancin is a semi-synthetic derivative of vanocymycin that has bactericidal activity against Methicillin-resistant Staphylococcus aureus (MRSA is an important pathogen causing hospital-acquired pneumonia (HAP) worldwide) and other gram-positive bacteria. FDA approved on September 11, 2009. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Laohavaleeson S, Kuti JL, Nicolau DP: Telavancin: a novel lipoglycopeptide for serious gram-positive infections. Expert Opin Investig Drugs. 2007 Mar;16(3):347-57. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17302529 # Rubinstein E, Corey GR, Stryjewski ME, Kanafani ZA: Telavancin for the treatment of serious gram-positive infections, including hospital acquired pneumonia. Expert Opin Pharmacother. 2011 Dec;12(17):2737-50. doi: 10.1517/14656566.2011.633511. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22077833 # Zhanel GG, Calic D, Schweizer F, Zelenitsky S, Adam H, Lagace-Wiens PR, Rubinstein E, Gin AS, Hoban DJ, Karlowsky JA: New lipoglycopeptides: a comparative review of dalbavancin, oritavancin and telavancin. Drugs. 2010 May 7;70(7):859-86. doi: 10.2165/11534440-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20426497 # Wong SL, Goldberg MR, Ballow CH, Kitt MM, Barriere SL: Effect of Telavancin on the pharmacokinetics of the cytochrome P450 3A probe substrate midazolam: a randomized, double-blind, crossover study in healthy subjects. Pharmacotherapy. 2010 Feb;30(2):136-43. doi: 10.1592/phco.30.2.136. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20099988 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Terminal elimination half-life = 8 ± 1.5 hours (with normal renal function) (en)
http://linked.open...ugbank/indication
  • Treatment of complicated skin infections caused by gram-positive bacteria like methicillin-susceptible or -resistant Staphylococcus aureus, vancomycin-susceptible Enterococcus faecalis, and Streptococcus pyogenes, Streptococcus agalactiae, or Streptococcus anginosus group. (en)
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Title
  • Telavancin (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Telavancin is a bactericidal lipoglycopeptide that is active against a broad range of gram-positive bacteria. Telavancin prevents polymerization of N-acetylmuramic acid (NAM) and N-acetylglucosamine (NAG) and cross-linking of peptidoglycan by binding to D-Ala-D-Ala. As a result, inhibition of bacterial cell wall synthesis occurs. Furthermore, telavancin disrupts membrane potential and cell permeability as a result of the lipophillic side chain moiety. This additional bactericidal mechanism is what sets telavancin apart from vancomycin. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Urine with >80% as unchanged drug and <20% as hydroxylated metabolites (with dose of 10mg/kg); Feces (<1%) (en)
http://linked.open.../drugbank/synonym
  • TD-6424 (en)
  • Vibativ (en)
http://linked.open...umeOfDistribution
  • Vss, healthy subjects, 10 mg/kg = 0.14 L/kg (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • >90% to serum albumin in a concentration independent manner (despite being highly protein bound, antimicrobial activity of telavancin is not affected) (en)
http://linked.open...ogy/drugbank/salt
  • (en)
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http://linked.open...ugbank/IUPAC-Name
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http://linked.open...ugbank/absorption
  • Telavancin demonstrates linear pharmacokinetics at doses between 1 and 12.5 mg/kg. Furthermore, 24 hours post-infusion of a dose of 7.5 to 15 mg/kg, activity against MRSA and penicillin-resistant Streptococcus pneumonia can still be observed. The trough concentration at this point of time is approximately 10 μg/mL. Telavancin also has poor bioavailability and must be administered over 30-120 minutes IV. Cmax, healthy subjects, 10 mg/kg = 93.6 ± 14.2 μg/mL; AUC (0- ∞), healthy subjects, 10 mg/kg = 747 ± 129 μg · h/mL; AUC (0-24h), healthy subjects, 10 mg/kg = 666± 107 μg · h/mL; Time to steady state = 3 days; (en)
http://linked.open.../affectedOrganism
  • Gram-positive Bacteria (en)
http://linked.open...casRegistryNumber
  • 372151-71-8 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • Cl, healthy subjects, 10 mg/kg = 13.9 ± 2.9 mL/h/kg (en)
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http://linked.open...bank/Rule-of-Five
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http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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