Esomeprazole undergoes a complete metabolism involving cytochrome P450. The main part is metabolized with the participation of specific polymorphic isoenzyme SYR2S19, with the formation of hydroxylated metabolites of esomeprazole and desmetilirovannye. Metabolism by the rest of the isoenzyme CYP3A4; with the formation of sulfo esomeprazole - the main metabolite in plasma is determined.
The parameters below reflect mainly the nature of the pharmacokinetics in patients with elevated isoenzyme CYP2C19. Total plasma Cl after a single dose of the drug - about 17 l / h, with repeated receptions - 9 l / h. T1 / 2 - 1.3 h after repeated dosing one time per day. AUC increases with repeated administration. This increase is time-and dose-dependent, which is due to lower metabolism in the first passage through the liver, as well as reduce systemic clearance, probably due to the fact that esomeprazole and / or sulfo inhibit isoenzyme CYP2C19.
With a daily intake of 1 time per day esomeprazole is completely removed from the plasma during the interval between doses, the trend towards accumulation of the drug is not indicated.
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