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QuickView for Telithromycin (compound)


PubChem
Name: telithromycin
PubChem Compound ID: 11693521
Molecular formula: C43H65N5O10
Molecular weight: 812.004 g/mol
DrugBank
Identification
Name: telithromycin
Name (isomeric): DB00976
Drug Type: small molecule
Brand: Ketek
Category: Anti-Bacterial Agents, Ketolides
CAS number: 191114-48-4
Pharmacology
Indication: For the treatment of <i>Pneumococcal</i> infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.
Pharmacology:
Telithromycin is a ketolide antibiotic which has an antimicrobial spectrum similar or slightly broader than that of penicillin. It is often used as an alternative in patients who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including mycoplasma. Telithromycin prevents bacterial grow...
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Mechanism of Action:
Telithromycin acts by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against gram-positive cocci (e.g. Streptococcus pneumoniae) in the presence of resistance mediated by methylases (erm genes) that alter the binding site at domain V. Telithromycin may also inhibit the a...
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Absorption: Absolute bioavailability is approximately 57%. Maximal concentrations are reached 0.5 - 4 hours following oral administration. Food intake does not affected absorption.
Protein binding: 60 - 70% bound primarily to human serum albumin
Biotransformation: Hepatic - estimated 50% metabolized by CYP3A4 and 50% metabolized independent of cytochrome P450
Route of elimination: 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.
Half Life: Main elimination half-life is 2-3 hours; terminal elimination half-life is 10 hours
Toxicity: 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.
Affected organisms: Enteric bacteria and other eubacteria
Interactions
Food interaction:
Take without regard to meals.
Drug interaction:
CarbamazepineCo-administration may cause decreased Telithromycin and increased Carbemazepine plasma concentrations. Consider alternate therapy.
IxabepiloneTelithromycin may reduce clearance of Ixabepilone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ixabepilone if Telithromycin is initiated, discontinued or dose changed.
SufentanilTelithromycin may reduce clearance of Sufentanil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sufentanil if Telithromycin is initiated, discontinued or dose changed.
NelfinavirNelfinavir may increase the plasma concentration of Telithromycin. Consider alternate therapy or monitor therapeutic/adverse effects.
NitrendipineTelithromycin may reduce clearance of Nitrendipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nitrendipine if Telithromycin is initiated, discontinued or dose changed.
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Targets


Enzymes