Peringatan Keamanan

LD50>2000 mg/kg (PO in rats). Adverse effects are similar to those of clarithormycin and erithromycin and include diarrhea, nausea, vomiting, loose stools, abdominal pain, flatulence and dyspepsia. It may also cause dizziness, headache and taste disturbances.

Telithromycin

DB00976

small molecule approved

Deskripsi

Telithromycin, a semi-synthetic erythromycin derivative, belongs to a new chemical class of antibiotics called ketolides. Ketolides have been recently added to the macrolide-lincosamide-streptogramin class of antibiotics. Similar to the macrolide antibiotics, telithromycin prevents bacterial growth by interfering with bacterial protein synthesis. Telithromycin binds to the 50S subunit of the 70S bacterial ribosome and blocks further peptide elongation. Binding occurs simultaneously at to two domains of 23S RNA of the 50S ribosomal subunit, domain II and V, where older macrolides bind only to one. It is used to treat mild to moderate respiratory infections.

Struktur Molekul 2D

Berat 812.018
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Main elimination half-life is 2-3 hours; terminal elimination half-life is 10 hours
Volume Distribusi * 2.9 L/kg
Klirens (Clearance) -

Absorpsi

Absolute bioavailability is approximately 57%. Maximal concentrations are reached 0.5 - 4 hours following oral administration. Food intake does not affected absorption.

Metabolisme

Hepatic - estimated 50% metabolized by CYP3A4 and 50% metabolized independent of cytochrome P450

Rute Eliminasi

The systemically available telithromycin is eliminated by multiple pathways as follows: 7% of the dose is excreted unchanged in feces by biliary and/or intestinal secretion; 13% of the dose is excreted unchanged in urine by renal excretion; and 37% of the dose is metabolized by the liver.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1122 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Telithromycin.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Telithromycin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Telithromycin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Telithromycin.
Alfentanil The serum concentration of Alfentanil can be increased when it is combined with Telithromycin.
Buspirone The metabolism of Buspirone can be decreased when combined with Telithromycin.
Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Telithromycin.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Telithromycin.
Disopyramide Telithromycin may increase the QTc-prolonging activities of Disopyramide.
Estazolam The serum concentration of Estazolam can be increased when it is combined with Telithromycin.
Pimozide The risk or severity of QTc prolongation and ventricular arrhythmias can be increased when Telithromycin is combined with Pimozide.
Quinine The serum concentration of Quinine can be increased when it is combined with Telithromycin.
Quinidine The metabolism of Quinidine can be decreased when combined with Telithromycin.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Telithromycin.
Rilpivirine The serum concentration of Rilpivirine can be increased when it is combined with Telithromycin.
Terfenadine The serum concentration of Terfenadine can be increased when it is combined with Telithromycin.
Triazolam The serum concentration of Triazolam can be increased when it is combined with Telithromycin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Telithromycin.
Colchicine The metabolism of Colchicine can be decreased when combined with Telithromycin.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Telithromycin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Telithromycin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Telithromycin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Telithromycin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Telithromycin.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Telithromycin.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Telithromycin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Telithromycin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Telithromycin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Telithromycin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Telithromycin.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Telithromycin.
Itraconazole The metabolism of Telithromycin can be decreased when combined with Itraconazole.
Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Telithromycin.
Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Telithromycin.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Telithromycin.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Telithromycin.
Vintafolide The serum concentration of Vintafolide can be increased when it is combined with Telithromycin.
Vincamine The serum concentration of Vincamine can be increased when it is combined with Telithromycin.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Telithromycin.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Telithromycin.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Telithromycin.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Telithromycin.
Cymarin The serum concentration of Cymarin can be increased when it is combined with Telithromycin.
Proscillaridin The serum concentration of Proscillaridin can be increased when it is combined with Telithromycin.
Lanatoside C The serum concentration of Lanatoside C can be increased when it is combined with Telithromycin.
Gitoformate The serum concentration of Gitoformate can be increased when it is combined with Telithromycin.
Peruvoside The serum concentration of Peruvoside can be increased when it is combined with Telithromycin.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Telithromycin.
Dicoumarol The serum concentration of Dicoumarol can be increased when it is combined with Telithromycin.
Phenindione The serum concentration of Phenindione can be increased when it is combined with Telithromycin.
Coumarin The serum concentration of Coumarin can be increased when it is combined with Telithromycin.
Tioclomarol The serum concentration of Tioclomarol can be increased when it is combined with Telithromycin.
4-hydroxycoumarin The serum concentration of 4-hydroxycoumarin can be increased when it is combined with Telithromycin.
Fluindione The serum concentration of Fluindione can be increased when it is combined with Telithromycin.
Clorindione The serum concentration of Clorindione can be increased when it is combined with Telithromycin.
Magnesium sulfate The risk or severity of QTc prolongation and hypotension can be increased when Telithromycin is combined with Magnesium sulfate.
Methsuximide The risk or severity of QTc prolongation and hypotension can be increased when Telithromycin is combined with Methsuximide.
Xylometazoline The risk or severity of QTc prolongation and hypotension can be increased when Telithromycin is combined with Xylometazoline.
Fasudil The risk or severity of QTc prolongation and hypotension can be increased when Telithromycin is combined with Fasudil.
Ziconotide The risk or severity of QTc prolongation and hypotension can be increased when Telithromycin is combined with Ziconotide.
Anagrelide The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Anagrelide.
Clemastine The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Valproic acid.
Sotalol The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Sotalol.
Thioridazine The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Trovafloxacin.
Cocaine The risk or severity of methemoglobinemia can be increased when Telithromycin is combined with Cocaine.
Procainamide The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Procainamide.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Arsenic trioxide.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Sparfloxacin.
Lithium cation The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Temafloxacin.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Tetrabenazine.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Telithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Telithromycin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Telithromycin.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Telithromycin.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Telithromycin.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Telithromycin.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Telithromycin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Telithromycin.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Telithromycin.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Telithromycin.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Telithromycin.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Telithromycin.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Telithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Telithromycin.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Telithromycin.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Telithromycin.
Mesoridazine The risk or severity of QTc prolongation can be increased when Mesoridazine is combined with Telithromycin.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Dimenhydrinate.
Papaverine The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Papaverine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Ofloxacin.
Flecainide The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Flecainide.
Probucol The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Probucol.

Target Protein

23S ribosomal RNA

Referensi & Sumber

Synthesis reference: Suhas Sohani, Mandar Deodhar, Nishant Patel, Manish Patel, Mahesh Davadra, Vinodhamar Kansal, "Process for the Preparation of Telithromycin." U.S. Patent US20070260066, issued November 08, 2007.
Artikel (PubMed)
  • PMID: 16481451
    Clay KD, Hanson JS, Pope SD, Rissmiller RW, Purdum PP 3rd, Banks PM: Brief communication: severe hepatotoxicity of telithromycin: three case reports and literature review. Ann Intern Med. 2006 Mar 21;144(6):415-20. Epub 2006 Feb 15.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Ketek
    Tablet, film coated • 400 mg/1 • Oral • US • Approved
  • Ketek
    Tablet, film coated • 400 mg/1 • Oral • US • Approved
  • Ketek
    Tablet, film coated • 300 mg/1 • Oral • US • Approved
  • Ketek
    Tablet • 400 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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