Effect of age and gender on azimilide pharmacokinetics after a single oral dose of azimilide dihydrochloride.
Azimilide is a new class III antiarrhythmic drug that blocks K+ channels. To determine the effects of age and gender on azimilide pharmacokinetics, a single 150-mg oral dose was administered to 66 healthy volunteers in a 3 x 2 factorial design (age groups of 18-40, 41-64, and > or = 65 years). Blood and urine were analyzed for azimilide and metabolites. The single dose was well-tolerated. Azimilide was 94% plasma protein-bound, and binding was not affected by age or gender. Age does not affect azimilide pharmacokinetics. The renal clearance of azimilide was significantly higher in women than in men (19%), but oral clearance did not differ between genders. Although the maximum azimilide concentration (Cmax) was 27% higher in women, time to maximum concentration or area under the azimilide concentration-time curve were not different from those for men. Body weight-adjusted Cmax did not differ between genders. Dosing adjustments based on either age or gender are not required.
Corey
A
A
Clinical Pharmacology and Pharmacokinetics Department, Procter & Gamble Pharmaceuticals, Cincinnati, OH 45242-1434, USA.
Agnew
J
J
Bao
J
J
Bryson
P
P
Comer
P
P
Griffith
S
S
Li
J
J
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000367:Age Factors; D000368:Aged; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D006827:Hydantoins; D007093:Imidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D048289:Imidazolidines; D008297:Male; D008875:Middle Aged; D010879:Piperazines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D012737:Sex Factors
D002121:Calcium Channel Blockers; D006827:Hydantoins; D007093:Imidazoles; D048289:Imidazolidines; D010879:Piperazines; C086123:azimilide