Pharmacokinetics of dapoxetine, a new treatment for premature ejaculation: Impact of age and effects of a high-fat meal.
Dapoxetine is being developed as a treatment for premature ejaculation and has demonstrated rapid absorption and elimination in previous pharmacokinetic studies. Two open-label studies were conducted in healthy men: a parallel-group pharmacokinetic and safety study in young and elderly men and a randomized crossover food-effect study. Maximal plasma dapoxetine concentrations (C(max)) were similar in young and elderly men (338 and 310 ng/mL, respectively), as were the corresponding area under the plasma concentration versus time curve (AUC) values (2040 and 2280 ng x h/mL, respectively). When coadministered with food, C(max) was reduced by 11% (398 vs 443 ng/mL in the fed and fasted states, respectively), and the peak was delayed by approximately 30 minutes, indicating that food slowed the rate of absorption; however, systemic exposure to dapoxetine (ie, AUC) was not affected by food consumption. Thus, age or consumption of a high-fat meal has only a modest impact on dapoxetine pharmacokinetics in healthy men.
Dresser
Mark J
MJ
ALZA Corporation, 1900 Charleston Road, Building M11-4, Mountain View, CA 94043, USA. mdresser@alzus.jnj.com
Kang
Dongwoo
D
Staehr
Peter
P
Gidwani
Shalini
S
Guo
Cindy
C
Mulhall
John P
JP
Modi
Nishit B
NB
D000293:Adolescent; D000328:Adult; D000368:Aged; D000375:Aging / Q000502:physiology*; D001596:Benzylamines / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D018592:Cross-Over Studies; D004041:Dietary Fats / Q000494:pharmacology*; D004542:Ejaculation / Q000187:drug effects*; D005502:Food; D006801:Humans; D008297:Male; D008875:Middle Aged; D009281:Naphthalenes / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*
D001596:Benzylamines; D004041:Dietary Fats; D009281:Naphthalenes; C080598:dapoxetine