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.
Klinische Pharmakologie, Allgemeines Krankenhaus Wein, Austria.
M
M
Wolzt
V
V
Fabrizii
G T
GT
Dorner
G
G
Zanaschka
P
P
Leufkens
W J
WJ
Krauwinkel
H G
HG
Eichler
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