Tuesday, June 7, 2011

Info two

Omeprazole is effective for preventing formation of peptic ulcers with concomitant therapy non-steroidal anti-inflammatory drugs (even inhibitors of COX - 2 selective group).

Nexium - of acid medication, use it in the form of granules, coated inside. Esomeprazole is rapidly absorbed, C max reached in plasma after about 60-120 minutes after internal use. Bioavailability after the adoption of a single dose of 40 mg - 64%, increasing to 90% in case of re-admission. At a dose of 20 mg, respectively, the absolute bioavailability of 50%, 68%.
Plasma proteins bind 97% of active ingredient. With simultaneous administration of esomeprazole and food does not change antisecretory effect, but the absorption may be delayed.

Biometabolizm most of esomeprazole occurs when the enzyme CYP 2S19, the rest of the - isomer of the enzyme: CYP 3A4, all reactions occur with participation of cytochrome P450. The half-life of approximately 70 minutes after the second dose of esomeprazole 24 hours later. Eliminated by the kidneys completely in the interval between taking the drug does not accumulate in the body when taking 1 every 24 hours. A smaller part of esomeprazole is excreted in the feces. Metabolites of the drug have no effect on the secretion of hydrochloric acid. Less than 1% of esomeprazole is eliminated unchanged by the kidneys. Metabolism of esomeprazole is not changed in the case of elderly patients (71-80 years). Women have a higher value of AUC, than men (30%) for dose selection for patients of both sexes are not affected. Particular group of patients are poor metabolisers - people whose metabolism is due only to the influence of CYP 3A4.U weak metabolisers figures AUC (average per day) to 100% higher than in those who have expressed activity and isomer (extensive metabolisers) - enzyme CYP 2C19. The choice of doses for one or the other group of persons is not affected. Of metabolism of esomeprazole in patients with liver failure is not revealed. The rate of biotransformation is reduced only at the expressed infringements, which leads to an increase in AUC 2-fold. Due to this, is recommended to use for such patients the dose of esomeprazole that is equal to 20 mg per day.



Not conducted studies to identify the metabolism of esomeprazole in patients with renal insufficiency. Because the kidneys are not eliminated in the active substance and metabolites, the biotransformation of violations should not be expected. The studies in adolescence - the effect of options and the maximum concentration of omeprazole in blood plasma from 12 years are the same as in patients of adult age.

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