Telavancin

DB06402

small molecule approved

Deskripsi

Telavancin is a semi-synthetic derivative of vanocymycin that has bactericidal activity against Methicillin-resistant Staphylococcus aureus (MRSA) and other gram-positive bacteria. MRSA is an important pathogen capable of causing hospital-acquired pneumonia (HAP), ventilator-associated pneumonia (VAP), and skin and subcutaneous tissue infections among others.

Struktur Molekul 2D

Berat 1755.65
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Terminal elimination half-life = 8 ± 1.5 hours (with normal renal function)
Volume Distribusi Vss, healthy subjects, 10 mg/kg = 0.14 L/kg
Klirens (Clearance) Cl, healthy subjects, 10 mg/kg = 13.9 ± 2.9 mL/h/kg

Absorpsi

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 ?g/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 ?g/mL; AUC (0- ?), healthy subjects, 10 mg/kg = 747 ± 129 ?g · h/mL; AUC (0-24h), healthy subjects, 10 mg/kg = 666± 107 ?g · h/mL; Time to steady state = 3 days;

Metabolisme

Metabolism of telavancin does not involve the cytochrome P450 enzyme system. Primary metabolite is called THRX-651540, but the metabolite pathway has not been identified.

Rute Eliminasi

Urine with >80% as unchanged drug and <20% as hydroxylated metabolites (with dose of 10mg/kg); Feces (<1%)

Interaksi Obat

1086 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Telavancin.
Ardeparin The therapeutic efficacy of Ardeparin can be decreased when used in combination with Telavancin.
Heparin The therapeutic efficacy of Heparin can be decreased when used in combination with Telavancin.
Enoxaparin The therapeutic efficacy of Enoxaparin can be decreased when used in combination with Telavancin.
Sulodexide The therapeutic efficacy of Sulodexide can be decreased when used in combination with Telavancin.
Semuloparin The therapeutic efficacy of Semuloparin can be decreased when used in combination with Telavancin.
Danaparoid The therapeutic efficacy of Danaparoid can be decreased when used in combination with Telavancin.
Dalteparin The therapeutic efficacy of Dalteparin can be decreased when used in combination with Telavancin.
Tinzaparin The therapeutic efficacy of Tinzaparin can be decreased when used in combination with Telavancin.
Nadroparin The therapeutic efficacy of Nadroparin can be decreased when used in combination with Telavancin.
Bemiparin The therapeutic efficacy of Bemiparin can be decreased when used in combination with Telavancin.
Parnaparin The therapeutic efficacy of Parnaparin can be decreased when used in combination with Telavancin.
Reviparin The therapeutic efficacy of Reviparin can be decreased when used in combination with Telavancin.
Dofetilide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Dofetilide.
Citalopram The risk or severity of QTc prolongation can be increased when Telavancin is combined with Citalopram.
Anagrelide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Telavancin is combined with Valproic acid.
Terfenadine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Terfenadine.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Grepafloxacin.
Quinine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Quinine.
Sotalol The risk or severity of QTc prolongation can be increased when Telavancin is combined with Sotalol.
Erlotinib The risk or severity of QTc prolongation can be increased when Telavancin is combined with Erlotinib.
Toremifene The risk or severity of QTc prolongation can be increased when Telavancin is combined with Toremifene.
Cisapride The risk or severity of QTc prolongation can be increased when Telavancin is combined with Cisapride.
Imatinib The risk or severity of QTc prolongation can be increased when Telavancin is combined with Imatinib.
Astemizole The risk or severity of QTc prolongation can be increased when Telavancin is combined with Astemizole.
Thioridazine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Trovafloxacin.
Mifepristone The risk or severity of QTc prolongation can be increased when Telavancin is combined with Mifepristone.
Flupentixol The risk or severity of QTc prolongation can be increased when Telavancin is combined with Flupentixol.
Cocaine The risk or severity of methemoglobinemia can be increased when Telavancin is combined with Cocaine.
Quinidine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Quinidine.
Procainamide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Procainamide.
Pimozide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Pimozide.
Amiodarone The risk or severity of QTc prolongation can be increased when Telavancin is combined with Amiodarone.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Telavancin is combined with Arsenic trioxide.
Escitalopram The risk or severity of QTc prolongation can be increased when Telavancin is combined with Escitalopram.
Domperidone The risk or severity of QTc prolongation can be increased when Telavancin is combined with Domperidone.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Sparfloxacin.
Halofantrine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Halofantrine.
Bepridil The risk or severity of QTc prolongation can be increased when Telavancin is combined with Bepridil.
Paliperidone The risk or severity of QTc prolongation can be increased when Telavancin is combined with Paliperidone.
Lithium cation The risk or severity of QTc prolongation can be increased when Telavancin is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Temafloxacin.
Zuclopenthixol The risk or severity of QTc prolongation can be increased when Telavancin is combined with Zuclopenthixol.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Tetrabenazine.
Dronedarone The risk or severity of QTc prolongation can be increased when Telavancin is combined with Dronedarone.
Nilotinib The risk or severity of QTc prolongation can be increased when Telavancin is combined with Nilotinib.
Iloperidone The risk or severity of QTc prolongation can be increased when Telavancin is combined with Iloperidone.
Vandetanib The risk or severity of QTc prolongation can be increased when Telavancin is combined with Vandetanib.
Romidepsin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Romidepsin.
Asenapine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Asenapine.
Artemether The risk or severity of QTc prolongation can be increased when Telavancin is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Lumefantrine.
Vemurafenib The risk or severity of QTc prolongation can be increased when Telavancin is combined with Vemurafenib.
Eliglustat The risk or severity of QTc prolongation can be increased when Telavancin is combined with Eliglustat.
Ribociclib The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Telavancin.
Glasdegib The risk or severity of QTc prolongation can be increased when Telavancin is combined with Glasdegib.
Deutetrabenazine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Deutetrabenazine.
Macimorelin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Telavancin is combined with Terodiline.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Telavancin.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Telavancin.
Erythromycin The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Telavancin.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Telavancin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Telavancin.
Ranolazine The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Telavancin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Telavancin.
Methadone The risk or severity of QTc prolongation can be increased when Methadone is combined with Telavancin.
Diltiazem The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Telavancin.
Clozapine The risk or severity of QTc prolongation can be increased when Telavancin is combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Telavancin.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Telavancin.
Promazine The risk or severity of QTc prolongation can be increased when Promazine is combined with Telavancin.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Telavancin.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Telavancin.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Chlorpromazine is combined with Telavancin.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Telavancin.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Telavancin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Telavancin.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Telavancin.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Telavancin.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Telavancin.
Chloroquine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Telavancin.
Efavirenz The risk or severity of QTc prolongation can be increased when Efavirenz is combined with Telavancin.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Telavancin.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Telavancin.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Telavancin.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Telavancin.
Dolasetron The risk or severity of QTc prolongation can be increased when Dolasetron is combined with Telavancin.
Roxithromycin The risk or severity of QTc prolongation can be increased when Roxithromycin is combined with Telavancin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Telavancin.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Telavancin.
Loperamide The risk or severity of QTc prolongation can be increased when Loperamide is combined with Telavancin.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Telavancin.
Ondansetron The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Telavancin.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Telavancin.

Target Protein

Neuronal acetylcholine receptor subunit alpha-2 CHRNA2
Neuronal acetylcholine receptor subunit alpha-3 CHRNA3
Corticotropin-releasing factor receptor 1 CRHR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17302529
    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.
  • PMID: 22077833
    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.
  • PMID: 20426497
    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.
  • PMID: 20099988
    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.

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Sekuens Gen/Protein (FASTA)

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