-2%
Plezer is prescribed for the management of premature ejaculation (PE) in adult men aged 18 to 64 years. It is particularly suitable for individuals experiencing one or more of the following conditions:
- Frequent or recurrent ejaculation occurring with minimal stimulation, before, during, or soon after penetration, and earlier than desired.
- Significant personal distress or interpersonal relationship issues resulting from premature ejaculation.
- Lack of control over the timing of ejaculation.
- Dapoxetine is not approved for individuals under 18 years of age.
The primary mechanism by which Dapoxetine exerts its effect in premature ejaculation is through selective inhibition of serotonin reuptake. This action enhances the activity of serotonin at both presynaptic and postsynaptic receptors, which is believed to delay ejaculation.
Human ejaculation is governed by the sympathetic nervous system, originating from spinal reflex centers influenced by the brainstem, especially the medial preoptic and paraventricular nuclei.
Dapoxetine is rapidly absorbed, with peak plasma concentration typically occurring within 1–2 hours after oral administration. Its absolute bioavailability stands at approximately 42%. In plasma, over 99% of Dapoxetine binds to serum proteins, while its active metabolite, desmethyl dapoxetine, is 98.5% protein-bound. The drug demonstrates extensive tissue distribution, with a steady-state volume of distribution of around 162 liters.
Dapoxetine undergoes metabolism via several pathways, including N-oxidation, N-demethylation, hydroxylation of the naphthyl ring, glucuronidation, and sulfation. It is subject to significant first-pass metabolism, and its metabolites are primarily eliminated through the urine in conjugated forms. It is rapidly cleared from the system, with a terminal half-life of around 19 hours.