Brands of Telithromycin in Kenya
No brand is available
Mechanism of Action:
Telithromycin blocks protein synthesis 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 domain V binding site of telithromycin. Telithromycin may also inhibit the assembly of nascent ribosomal units.
Telithromycin belongs to the ketolide class of antibacterials and is structurally related to the macrolide family of antibiotics. Telithromycin concentrates in phagocytes where it exhibits activity against intracellular respiratory pathogens. In vitro, telithromycin has been shown to demonstrate concentration-dependent bactericidal activity against isolates of Streptococcus pneumoniae (including multi-drug resistant isolates [MDRSP]).
Telithromycin is a semi-synthetic erythromycin derivative. It is created by substituting a ketogroup for the cladinose sugar and adding a carbamate ring in the lactone ring. An alkyl-aryl moiety is attached to this carbamate ring. Furthermore, the carbon at position 6 has been methylated, as is the case in clarithromycin, to achieve better acid-stability.
It was patented in 1994 and approved for medical use in 2001
INDICATIONS:
Telithromycin is indicated for the treatment of community-acquired pneumonia (of mild to moderate severity) due to Streptococcus pneumoniae, (including multi-drug resistant isolates [MDRSP]), Haemophilus influenzae, Moraxella catarrhalis, Chlamydophila pneumoniae, or Mycoplasma pneumoniae, for patients 18 years old and above.
DOSAGE AND ADMINISTRATION:
The dose of Telithromycin is 800 mg taken orally once every 24 hours, for 7–10 days.
CONTRAINDICATIONS
Telithromycin is contraindicated in patients with myasthenia gravis. Exacerbations of myasthenia gravis have been reported in patients and sometimes occurred within a few hours of the first dose of telithromycin. Reports have included fatal and life-threatening acute respiratory failure with a rapid onset and progression.
Telithromycin is contraindicated in patients with previous history of hepatitis and/or jaundice associated with the use of Telithromycin, or any macrolide antibiotic.
Telithromycin is contraindicated in patients with a history of hypersensitivity to telithromycin and/or any , or any macrolide antibiotic.
Concomitant administration of Telithromycin with cisapride or pimozide is contraindicated
Concomitant administration of Telithromycin and colchicine is contraindicated in patients with renal or hepatic impairment.
ADVERSE DRUG REACTIONS:
Most common side-effects are gastrointestinal, including diarrhea, nausea, abdominal pain and vomiting. Headache and disturbances in taste also occur. Less common side-effects include palpitations, blurred vision, and rashes. Prolonged QTc intervals may also be caused by telithromycin.
Rare but severe side-effects were initially reported in March 2006, involving damage to the liver. Three different incidents were reported: one case of temporary drug-induced hepatitis, one ending in a liver transplant, and one ending in death.
Reporting of suspected adverse reactions:
The PPB Department of Pharmacovigilance was set up with a vision to develop, implement and continuously upgrade an appropriate system for detecting, reporting, and monitoring adverse drug reactions (ADRs) and other relevant problems with medicines in Kenya. The department strives to ensure the safety and efficacy of pharmaceutical products in Kenya.
Reporting suspected adverse reactions after authorization of the medicinal product are important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals/ Patients are encouraged to report any suspected adverse reactions via Pharmacovigilance Yellow Form, pv@pharmacyboardkenya.org or clicking below button:
Clinical | Pharmacokinetic data
Pregnancy Category: C (Risk not ruled out)
Routes of Administration: Oral
Bioavailability: 57%
Protein Binding: 66% to 79%
Metabolosim: Hepatic (50% CYP3A4-mediated)
Onset of Action: Not Available
Elimination Half life: 10 hours
Excretion: Biliary and renal
Legal Status | Dosage forms & Strengths
Prescription Category:
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Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
Dosage Forms | Strengths:
Drug Indentifiers:
Drug Images
References/ Citation:
Telithromycin