Telithromycin
- Atc Codes:J01FA15
- CAS Codes:191114-48-4#173838-31-8
- PHARMGKB ID:191114-48-4#173838-31-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Ketek; Belgium: Ketek; Cyprus: Ketek; Czech Republic: Ketek; Estonia: Ketek; Finland: Ketek; France: Ketek; Germany: Ketek; Greece: Ketek; Hungary: Ketek; Ireland: Ketek; Italy: Ketek; Latvia: Ketek; Lithuania: Ketek; Netherlands: Ketek; Poland: Ketek; Portugal: Ketek; Romania: Ketek; Slovakia: Ketek; Slovenia: Ketek; Spain: Ketek; Sweden: Ketek; UK: Ketek.
North America
Canada: Ketek; USA: Ketek.
Latin America
Brazil: Ketek; Mexico: Ketek.
Asia
Japan: Ketek.
Drug combinations
Chemistry
Telithromycin: C~43~H~65~N~5~O~10~. Mw: 812.00. (1) Erythromycin, 3-de[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]-; (2)(3aS,4R,7R,9R,10R,11R,13R,15R,15aR)-4-Ethyl-11-methoxy-3a,7,9,11,13,15-hexamethyl-1-[4-[4-(pyridin-3-yl)-1H-imidazol-1-yl]butyl]-10-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]octahydro-2H-oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetrone. CAS-191114-48-4; CAS-173838-31-8 (2004).
Pharmacologic Category
Antibacterials; Macrolides; Ketolides. (ATC-Code: J01FA15).
Mechanism of action
Inhibits bacterial protein synthesis by binding to two sites on 50 S ribosomal subunit. Also alters secretion of IL-1-α and TNF.
Therapeutic use
Treatment of community-acquired pneumonia (mild-to-moderate) caused by susceptible strains of Streptococcus pneumoniae (including multidrug-resistant isolates), Haemophilus influenzae, Chlamydophila pneumoniae, Moraxella catarrhalis, and Mycoplasma pneumoniae.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies of telithromycin in pregnant women. Excretion in breast milk unknown (use with caution in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to telithromycin, macrolide antibiotics, or any component of the formulation. Myasthenia gravis. History of hepatitis and/or jaundice associated with telithromycin or other macrolide antibiotic use. Concurrent use of cisapride or pimozide.
Warnings and precautions
May prolong QTc interval, leading to risk of ventricular arrhythmias. Avoid in prolongation of QTc interval due to congenital causes, history of long QT syndrome, uncorrected electrolyte disturbances (hypokalemia or hypomagnesemia), significant bradycardia (<50 bpm), or concurrent therapy with QTc-prolonging drugs (e.g. class Ia and class III antiarrhythmics). Avoid use in prior history of confirmed cardiogenic syncope or ventricular arrhythmias while receiving macrolide antibiotics or other QTc-prolonging drugs. Acute hepatic failure and severe liver injury, including hepatitis and hepatic necrosis (leading to some fatalities) reported. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. May cause loss of consciousness (possibly vagal-related). May cause severe visual disturbances (e.g. changes in accommodation ability, diplopia, blurred vision). Life-threatening (including fatal) respiratory failure occurred in myasthenia gravis (use contraindicated). Use with caution in renal impairment; severe impairment (CrCl <30 mL/minute) requires dosage adjustment.