Pharmacokinetics of dapoxetine hydrochloride in healthy Chinese, Japanese, and Caucasian men.
Dapoxetine is a short-acting selective serotonin reuptake inhibitor developed for the on-demand treatment of premature ejaculation and is approved in some European Union countries, as well as Mexico and Korea, for this indication. The pharmacokinetics of dapoxetine 30 mg and 60 mg in healthy Chinese (single dose), Japanese, and Caucasian men (single and multiple dose) were assessed in 2 studies. In the 3 ethnic groups, dapoxetine was rapidly absorbed following oral administration, with peak plasma concentrations evident approximately 1 hour after dosing, independent of dose, dosing frequency (single or multiple dosing), or ethnicity. Dapoxetine was eliminated in a biphasic manner with an apparent mean terminal half-life of 14 to 17 hours. There was a dose-proportional increase in dapoxetine maximum plasma concentration (C(max)) and area under concentration-time curves (AUCs). The single-dose pharmacokinetic parameters of dapoxetine metabolites were also similar for the 3 ethnic groups, as were the pharmacokinetics of dapoxetine and its metabolites following single and multiple dosing in Caucasian and Japanese men. Dapoxetine was well tolerated by all 3 ethnic groups.
Thyssen
An
A
Johnson & Johnson Pharmaceutical Research & Development, Division of Janssen Pharmaceutica, NV, Turnhoutseweg 30 B-2340 Beerse, Belgium. athyssen@its.jnj.com
Sharma
Om
O
Tianmei
Si
S
Aquilina
Joseph W
JW
Vandebosch
An
A
Wang
Shean-Sheng
SS
Mudumbi
Ramagopal
R
Hsiao
Hsiu-Ling
HL
D000328:Adult; D044466:Asian People; D001596:Benzylamines / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000652:urine; D002681:China / Q000208:ethnology; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D006207:Half-Life; D006801:Humans; D007564:Japan / Q000208:ethnology; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D009281:Naphthalenes / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000652:urine; D017367:Selective Serotonin Reuptake Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D006113:United Kingdom; D014481:United States; D044465:White People; D055815:Young Adult
D001596:Benzylamines; D009281:Naphthalenes; D017367:Selective Serotonin Reuptake Inhibitors; C522496:dapoxetine-N-oxide; C080600:di-desmethyldapoxetine; C080599:mono-desmethyldapoxetine; C080598:dapoxetine