Pharmacokinetics of oral doses of telmisartan and nisoldipine, given alone and in combination, in patients with essential hypertension

Milica Bajcetic; Ralf A Benndorf; Daniel Appel; Edzard Schwedhelm; Friedrich Schulze; Daniel Riekhof; Renke Maas; Rainer H Böger

doi:10.1177/0091270006297225

Pharmacokinetics of oral doses of telmisartan and nisoldipine, given alone and in combination, in patients with essential hypertension

J Clin Pharmacol. 2007 Mar;47(3):295-304. doi: 10.1177/0091270006297225.

Authors

Milica Bajcetic¹, Ralf A Benndorf, Daniel Appel, Edzard Schwedhelm, Friedrich Schulze, Daniel Riekhof, Renke Maas, Rainer H Böger

Affiliation

¹ Institute of Experimental and Clinical Pharmacology and Toxicology, Clinical Pharmacology Unit, University Hospital Hamburg-Eppendorf, Martinistrasse 521, D-20246 Hamburg.

PMID: 17322141
DOI: 10.1177/0091270006297225

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.

Publication types

Randomized Controlled Trial
Research Support, Non-U.S. Gov't

MeSH terms

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 / pharmacokinetics*
Benzimidazoles / therapeutic use
Benzoates / adverse effects
Benzoates / pharmacokinetics*
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
Hypertension / drug therapy*
Male
Middle Aged
Nisoldipine / adverse effects
Nisoldipine / pharmacokinetics*
Nisoldipine / therapeutic use
Single-Blind Method
Telmisartan
Time Factors

Substances

Angiotensin II Type 1 Receptor Blockers
Benzimidazoles
Benzoates
Calcium Channel Blockers
Nisoldipine
Telmisartan