Pharmacokinetics of tamsulosin in subjects with normal and varying degrees of impaired renal function: an open-label single-dose and multiple-dose study.
OBJECTIVE
This study was performed to estimate whether the pharmacokinetics and safety of tamsulosin, and alpha(1A)-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 alpha(1)-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 trail 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.
Wolzt
M
M
Klinische Pharmakologie, Allgemeines Krankenhaus Wein, Austria.
Fabrizii
V
V
Dorner
G T
GT
Zanaschka
G
G
Leufkens
P
P
Krauwinkel
W J
WJ
Eichler
H G
HG
D000317:Adrenergic alpha-Antagonists / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D001794:Blood Pressure / Q000187:drug effects; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D013449:Sulfonamides / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D000077409:Tamsulosin
D000317:Adrenergic alpha-Antagonists; D013449:Sulfonamides; D000077409:Tamsulosin