1. Pharmacokinetics of oral doses of telmisartan and nisoldipine, given alone and in combination, in patients with essential hypertension.
- Author
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Bajcetic M, Benndorf RA, Appel D, Schwedhelm E, Schulze F, Riekhof D, Maas R, and Böger RH
- Subjects
- Administration, Oral, Aged, Angiotensin II Type 1 Receptor Blockers adverse effects, Angiotensin II Type 1 Receptor Blockers pharmacokinetics, Angiotensin II Type 1 Receptor Blockers therapeutic use, Area Under Curve, Benzimidazoles adverse effects, Benzimidazoles therapeutic use, Benzoates adverse effects, Benzoates therapeutic use, Biological Availability, Calcium Channel Blockers adverse effects, Calcium Channel Blockers pharmacokinetics, Calcium Channel Blockers therapeutic use, Dizziness chemically induced, Dose-Response Relationship, Drug, Drug Interactions, Drug Therapy, Combination, Edema chemically induced, Female, Half-Life, Headache chemically induced, Humans, Male, Middle Aged, Nisoldipine adverse effects, Nisoldipine therapeutic use, Single-Blind Method, Telmisartan, Time Factors, Benzimidazoles pharmacokinetics, Benzoates pharmacokinetics, Hypertension drug therapy, Nisoldipine pharmacokinetics
- Abstract
This randomized, single-blind, parallel-group study was performed to assess pharmacokinetic interactions potentially occurring during concomitant use of telmisartan and nisoldipine. Patients with essential hypertension (n = 37) were treated with once-daily doses of telmisartan, nisoldipine, or their combination for 6 weeks. The regimen was started at low dose with an increase of dosage after 3 weeks of treatment. AUC(ss) (132%; P < .01) of telmisartan applied in doses of 80 mg was significantly higher after concomitant application with nisoldipine (10 mg), whereas CL/f(ss) (-54%; P < .05) and Vz/f(ss) (-72%; P < .05) were significantly lower. Regarding pharmacokinetic parameters of nisoldipine, significant differences between treatment groups were not detected. In conclusion, the results of this study strongly suggest that concomitant treatment with nisoldipine enhances telmisartan bioavailability in hypertensive individuals. Larger crossover trials will have to establish these observations and investigate whether interaction of both drugs affects telmisartan efficacy and tolerability in clinical use.
- Published
- 2007
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