Pharmacokinetics and safety of a single oral dose of once-daily alfuzosin, 10 mg, in male subjects with mild to severe renal impairment.
The effect of renal impairment on the safety and pharmacokinetics of a once-daily formulation of alfuzosin, 10 mg, was evaluated. In an open, single-dose study, 26 volunteers, ages 18 to 65 years, were classified as having normal renal function (n = 8) or mild (n = 6), moderate (n = 6), or severe (n = 6) renal impairment. Mean Cmax values increased by a factor of 1.20, 1.52, and 1.20 in subjects with mild, moderate, or severe renal impairment, respectively, compared with controls. Values for AUC(0-infinity) were 1.46, 1.47, and 1.44, respectively. The t(1/2z) was increased only in the group with severe renal impairment. Emergent vasodilatory adverse events were reported by 4 of 26 subjects. No discontinuations due to adverse events occurred. Laboratory parameters were satisfactory in all groups. In conclusion, once-daily alfuzosin, 10 mg, could be safely administered to patients with impaired renal function, and dosage adjustment does not seem necessary.
Marbury
Thomas C
TC
Orlando Clinical Research Center, Orlando, Florida, USA.
Blum
Robert A
RA
Rauch
Clémence
C
Pinquier
Jean-Louis
JL
D000284:Administration, Oral; D000293:Adolescent; D000317:Adrenergic alpha-Antagonists / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D000328:Adult; D000368:Aged; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D006801:Humans; D007262:Infusions, Intravenous; D007279:Injections, Subcutaneous; D007668:Kidney / Q000503:physiopathology; D007674:Kidney Diseases / Q000378:metabolism* / Q000503:physiopathology; D008297:Male; D008875:Middle Aged; D011799:Quinazolines / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects; D013997:Time Factors
D000317:Adrenergic alpha-Antagonists; D003692:Delayed-Action Preparations; D011799:Quinazolines; D018340:Receptors, Adrenergic, alpha-1; C047638:alfuzosin