Clarithromycin (Clarithromycin)
Synonyms
Binoklar (Bangladesh), Klabaks (India), Klatsid (France, Italy), Klatsid CP (UK), Fromilid (Slovenia)
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Macrolides (Antimicrobial drugs)
Release form of the drug
Film-coated tablets, 250 mg; 500 mg film-coated tablets, 500 mg retard
Por. liof. for inhalation of 500 mg
Por. yelled for suspensions. 1.5 g; 2.5 g; 125 mg / 5 ml
Gran. yelled for suspensions. 125 mg / 5 ml
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Well absorbed when taken orally, the bioavailability is 55%. Peak plasma concentration after oral administration of 500 mg is achieved after 2-3 h of 1,77- and 1,89 mg / l. At regular ingestion maximum equilibrium concentration (Cx) unchanged medicament and its metabolite after 2-3 days in plasma was 2.4 ± 0.7 and 0.7 ± 0.2 mcg / ml, respectively. Eating slows down the absorption without affecting the Cmax and bioavailability. The plasma protein binds to 65-75%; when the plasma concentrations above 1 mg / ml of free fraction of drugs increases.
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The concentration of clarithromycin in secretions (saliva apart) and significantly higher than serum tissues: 39 times in the liquid lining the bronchial mucosa; 8.8 times in the lung tissue perilymph and the middle ear; 27.5 and 3.1 times in the bronchial mucosa and bronchial secretions, respectively; 1.5 times in the sinuses and 33.1 times in tonsils. However, the highest concentrations - v471i 16.4 times higher than whey - are in the lysosomes of alveolar macrophages and polymorphonuclear leukocytes. Tissue tropism of clarithromycin and defines a substantial volume of distribution (Vd), reaching 3.5 l / kg. The medicament passes through the placenta, but not the blood-brain barrier into breast milk. T1 / 2 when administered 3.7 hours, increasing with increasing dose.