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The cytochrome P-450 enzyme system, specifically 2C8 and 3A4, have been shown to be involved in the N-dealkylation of repaglinide to M2 and the further oxidation to M1. Metabolites do not contribute to the glucose-lowering effect of repaglinide. Repaglinide appears to be a substrate for active hepatic uptake transporter organic anion transporting protein OATP1B1. C-repaglinide as a single, oral dose, approximately 90% of the radiolabel was recovered in the feces and approximately 8% in the urine. Only 0.1% of the dose is cleared in the urine as parent compound. The major metabolite M2 accounted for 60% of the administered dose. Less than 2% of parent drug was recovered in feces. The pharmacokinetic parameters of repaglinide obtained from a single-dose, crossover study in healthy subjects and from a multPrandinle-dose, parallel, dose-proportionality 0.5, 1, 2 and 4 mg study in patients with type 2 diabetes are summarized in the following table: These data indicate that repaglinide did not accumulate in serum. Clearance of oral repaglinide did not change over the 0.5 - 4 mg dose range, indicating a linear relationshPrandin between dose and plasma drug levels. Repaglinide AUC after multPrandinle doses of 0.25 to 4 mg with each meal varies over a wide range. Co-administration of both gemfibrozil and itraconazole with PRANDIN resulted in a 19-fold higher repaglinide AUC and prolonged repaglinide half-life to prandin precio en mexico 6.1 hr. Plasma repaglinide concentration at 7 h increased 28.6-fold with gemfibrozil co-administration and 70.4-fold with the gemfibrozil-itraconazole combination see CONTRAINDICATIONS, PRECAUTIONS : DRUG INTERACTIONS. Fenofibrate : Co-administration of 200 mg fenofibrate with a single dose of 0.25 mg repaglinide after 5 days of once daily fenofibrate 200 mg resulted in unchanged AUC and Cmax values for both drugs. Ketoconazole : Co-administration of 200 mg ketoconazole and a single dose of 2 mg PRANDIN after 4 days of once daily ketoconazole 200 mg resulted in a 15% and 16% increase in repaglinide AUC and Cmax, respectively prandin precio en mexico. The increases were from 20.2 ng/mL to 23.5 ng/mL for Cmax and from 38.9 ng/mLhr to 44.9 ng/mLhr for AUC.

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