Key words Tamsulosin
Benign prostatic hyperplasia
Springer Online Journal Archives 1860-2000
Chemistry and Pharmacology
Abstract Objective: This study was performed to estimate whether the pharmacokinetics and safety of tamsulosin, an α1A-adrenoceptor antagonist for the treatment of symptomatic benign prostatic hyperplasia (BPH), are influenced by impaired renal function. Methods: In an open-label study design, the plasma concentration profile of 0.4 mg tamsulosin p.o. was studied in age-matched groups of male subjects with normal (n = 10), moderately impaired (n = 10), and severely impaired (n = 8) renal function after single-dose administration and in steady state, i.e. after 21 days of multiple-dose administration. Results: The AUC of total, but not of unbound, tamsulosin was correlated to creatinine clearance and α1-acid glycoprotein plasma levels, and was found to be significantly higher in both groups of subjects with impaired renal function than in controls after single- and multiple-dose administration. However, the pharmacokinetics of total and unbound tamsulosin were comparable for both trial periods. Conclusions: Impaired renal function increases total tamsulosin plasma concentration by approximately 100% after single-dose administration and in steady state. Since active unbound drug levels are not affected, no dose modification is required in symptomatic BPH patients with renal impairment.
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