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Drug Interactions Montelukast at a dose of 10 mg once daily dosed to pharmacokinetic steady state: ° did not cause clinically significant changes in the kinetics of a single intravenous dose of theophylline (predominantly a cytochrome P450 1A2 substrate). Text Continues Below
° did not change the pharmacokinetic profile of warfarin (primarily a substrate of CYP 2C9, 3A4 and 1A2) or influence the effect of a single 30-mg oral dose of warfarin on prothrombin time or the INR (International Normalized Ratio). ° did not change the pharmacokinetic profile or urinary excretion of immunoreactive digoxin. ° did not change the plasma concentration profile of terfenadine (a substrate of CYP 3A4) or fexofenadine, its carboxylated metabolite, and did not prolong the QTc interval following co-administration with terfenadine 60 mg twice daily. Montelukast at doses of 100 mg daily dosed to pharmacokinetic steady state: ° did not significantly alter the plasma concentrations of either component of an oral contraceptive containing norethindrone 1 mg/ ethinyl estradiol 35 mcg. ° did not cause any clinically significant change in plasma profiles of prednisone or prednisolone following administration of either oral prednisone or intravenous prednisolone. Phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40% following a single 10-mg dose of montelukast. No dosage adjustment for SINGULAIR is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with SINGULAIR. Pharmacodynamics Montelukast causes inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD4 in asthmatics. Doses as low as 5 mg cause substantial blockage of LTD4 -induced bronchoconstriction. In a placebo-controlled, crossover study (n= 12), SINGULAIR inhibited early-and late-phase bronchoconstriction due to antigen challenge by 75% and 57%, respectively. Page: << Prev | 1 | 2 | 3 | 4 | 5 | Next >>
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