| Description | PE
is the most common form of male sexual dysfunction affecting 20-40% of
men globally at some point in their lives. Ejaculation is a reflex
comprising different sensory pathways, motor centers, and nerve
pathways. This ejaculatory reflex has been shown to be controlled
primarily by serotonin and dopamine. Dapoxetine is a short-acting SSRI.
It is differentiated from the existing SSRI treatments for PE by the
fact that it can be administered on an as-needed basis. In healthy
subjects, dapoxetine is rapidly absorbed after oral administration with a
peak plasma concentration (Tmax) occurring between 1.4 and 2 h.
Dapoxetine
also showed statistically significant improvements in perceived control
over ejaculation, PE-related personal distress, and other
patient-reported outcomes in all five trials. Dapoxetine treatment was
generally well tolerated, with low incidences of discontinuation
syndrome, sexual dysfunction, and treatment-emergent mood symptoms. The
most common adverse events with dapoxetine included nausea, diarrhea,
headache, dizziness, and somnolence. |
| Chemical Properties | Off-white Cryst |
| Originator | Lilly (US) |
| Uses | Selective serotonin reuptake inhibitor (SSRI) |
| Uses | Dapoxetine
hydrochloride is a short-acting novel selective serotonin reuptake
inhibitor marketed for the treatment of premature ejaculation in men.
Premature ejaculation (PE) is the most common male sexual disorder,
estimated to affect up to 30% of men. D |
| Uses | A selective serotonin reuptake inhibitor |
| Brand name | Priligy |
| Chemical Synthesis | Dapoxetine
can be synthesized in four chemical steps starting from R-1phenyl-
1,3-propanediol via selective tosylation of the primary hydroxy group
with p-toluenesulfonyl chloride, triethylamine and 4-(dimethylamino)
pyridine (DMAP), and subsequent condensation with 1naphthol by means of
sodium- or lithium hydroxide to yield R-3-(1naphthyloxy)-
1-phenylpropanol as the key intermediate. Conversion of the alcohol
group to the corresponding mesylate with methanesulfonyl chloride,
triethylamine, and DMAP, followed by treatment with dimethylamine
affords dapoxetine, which is then acidified to its hydrochloride salt. |
China
