2. Dapoxetine Hydrochloride
6. Dapoxetinum [inn-latin]
7. Dapoxetina [inn-spanish]
8. Ly 210448
14. Benzenemethanamine, N,n-dimethyl-alpha-(2-(1-naphthalenyloxy)ethyl)-, (+)-
15. Dapoxetine [inn]
17. Priligy (tn)
20. Kutub, Priligy, Duratia
38. 129938-20-1 (hydrochloride)
|Molecular Weight||305.421 g/mol|
|Hydrogen Bond Donor Count||0|
|Hydrogen Bond Acceptor Count||2|
|Rotatable Bond Count||6|
|Exact Mass||305.178 g/mol|
|Monoisotopic Mass||305.178 g/mol|
|Topological Polar Surface Area||12.5 A^2|
|Heavy Atom Count||23|
|Isotope Atom Count||0|
|Defined Atom Stereocenter Count||1|
|Undefined Atom Stereocenter Count||0|
|Defined Bond Stereocenter Count||0|
|Undefined Bond Stereocenter Count||0|
|Covalently Bonded Unit Count||1|
For the treatment of premature ejaculation.
Treatment of premature ejaculation (PE) in men 18 to 64 years of age
Dapoxetine is a selective serotonin reuptake inhibitor currently undergoing trials through Alza (under license from GenuPro, a collaboration between Eli Lilly and PPD). Dapoxetine is a short-acting SSRI drug currently being considered for approval by the Food and Drug Administration (FDA) for the treatment of premature ejaculation in men, which would make it the first drug approved for such treatment. Despite two clinical trials finished in 2006, experts doubt it will be approved by the FDA soon because SSRIs come with undesirable side-effects after long-term use, such as psychiatric problems, dermatological reactions, increase in body weight, lower sex-drive, nausea, headache, upset stomach and weakness, thus not significantly outweighing the benefit of premature ejaculation medication versus the risks. By contrast with SSRIs approved for depression, which take 2 weeks or longer to reach steady-state concentration, dapoxetine has a unique pharmacokinetic profile, with a short time to maximum serum concentration (about 1 h) and rapid elimination (initial half-life of 1-2 h).
G - Genito urinary system and sex hormones
G04 - Urologicals
G04B - Urologicals
G04BX - Other urologicals
G04BX14 - Dapoxetine
Initial half-life of 1-2 hours.
The drug's mechanism of action is thought to be related to inhibition of neuronal reuptake of serotonin and subsequent potentiation of serotonin activity. The central ejaculatory neural circuit comprises spinal and cerebral areas that form a highly interconnected network. The sympathetic, parasympathetic, and somatic spinal centers, under the influence of sensory genital and cerebral stimuli integrated and processed at the spinal cord level, act in synergy to command physiologic events occurring during ejaculation. Experimental evidence indicates that serotonin (5-HT), throughout brain descending pathways, exerts an inhibitory role on ejaculation. To date, three 5-HT receptor subtypes (5-HT(1A), 5-HT(1B), and 5-HT(2C)) have been postulated to mediate 5-HT's modulating activity on ejaculation.