Dapotin 30

• Persistent or recurrent ejaculation with minimal sexual stimulation before, on, or shortly after penetration and before the patient wishes.
• Marked personal distress or interpersonal difficulty as a consequence of PE.
• Poor control over ejaculation.

Dapoxetine is rapidly absorbed with maximum plasma concentrations (Cmax) occurring approximately 1-2 hours after tablet intake. The absolute bioavailability is 42%. More than 99% of Dapoxetine is bound in-vitro to human serum proteins. The active metabolite Desmethyl dapoxetine (DED) is 98.5% protein bound. Dapoxetine appears to have a rapid distribution with a mean steady state volume of distribution of 162 L.

Dapoxetine is extensively metabolized to multiple metabolites primarily through the following biotransformational pathways: N-oxidation, N-demethylation, Naphthyl hydroxylation, Glucuronidation and Sulfation. There was evidence of presystemic first-pass metabolism after oral administration. The metabolites of the Dapoxetine were primarilly eliminated in urine as conjugates. Dapoxetine has a rapid elimitaion and the terminal half life is approximately 19 hours.

Adult men (18 to 64 years of age): The recommended starting dose for all patients is 30 mg, taken as needed approximately 1 to 3 hours prior to sexual activity. The maximum recommended dosing frequency is once every 24 hours. If the effect of 30 mg is insufficient and the side effects are acceptable, the dose may be increased to the maximum recommended dose of 60 mg. Dapoxetine may be taken with or without food.

Children and adolescents: Dapoxetine should not be used in individuals below 18 years of age. Elderly (age 65 years and over): Safety and efficacy of Dapoxetine have not been established in patients age 65 years and over as limited data are available in this population.

Patients with renal impairment: Caution is advised in patients with mild or moderate renal impairment. Dapoxetine is not recommended for use in patients with severe renal impairment.

Patients with hepatic impairment: Dapoxetine is contraindicated in patients with moderate and severe hepatic impairment

PDE5 inhibitors: Tadalafil did not affect the pharmacokinetics of Dapotin. Sildenafil caused slight changes in Dapotin pharmacokinetics, which are not expected to be clinically significant. However, Dapotin should be prescribed with caution in patients who use PDE5 inhibitors due to possible reduced orthostatic tolerance.

Tamsulosin: Concomitant administration of single or multiple doses of 30 mg or 60 mg Dapotin to patients receiving daily doses of Tamsulosin did not result in changes in the pharmacokinetics of Tamsulosin. However, Dapotin should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.

Warfarin: There are no data evaluating the effect of chronic use of Warfarin with Dapotin; therefore, caution is advised when Dapotin is used in patients taking Warfarin chronically.

Ethanol: Concomitant use of alcohol and Dapotin could increase the chance or severity of adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. Combining alcohol with Dapotin may increase these alcohol-related effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Dapotin.

• Patients with known hypersensitivity to Dapoxetine Hydrochloride.
• Patients with significant pathological cardiac conditions (such as heart failure (NYHA class ll-IV), conduction abnormalities (second- or third-degree AV block or sick sinus syndrome) not treated with a permanent pacemaker, significant ischemic heart disease or significant valvular disease.
• Concomitant treatment with monoamine oxidase inhibitors (MAOIs), thioridazine, or within 14 days of discontinuing treatment with MAOIs, thioridazine. Similarly, MAOIs, thioridazine should not be administered within 7 days after Dapoxetine has been discontinued.
• Concomitant treatment with serotonin reuptake inhibitors [selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs)] or other medicinal/herbal products with serotonergic effects or within 14 days of discontinuing treatment with these medicinal/herbal products.

Ethanol: Combining alcohol with Dapotin may increase alcohol-related neurocognitive effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Dapotin.

Syncope: Possibly prodromal symptoms such as nausea, dizziness, lightheadedness, palpitations, asthenia, confusion and diaphoresis generally occurred within the first 3 hours following dosing and often preceded the syncope. Patients need to be made aware that they could experience syncope at any time with or without prodromal symptoms during their treatment with Dapotin.

Orthostatic hypotension: An orthostatic test should be performed before initiating therapy. In case of a history of documented or suspected orthostatic reaction, treatment with Dapotin should be avoided.

Haemorrhage: There have been reports of bleeding abnormalities with SSRIs. Caution is advised in patients taking Dapotin, particularly in concomitant use with medicinal products known to affect platelet function (e.g., atypical antipsychotics and phenothiazines, acetylsalicylic acid, nonsteroidal anti-inflammatory drugs [NSAIDs], anti-platelet agents) or anticoagulants (e.g., warfarin), as well as in patients with a history of bleeding or coagulation disorders.

PDE5 inhibitors: The pharmacokinetics of Dapotin (60 mg) in combination with Tadalafil (20 mg) and Sildenafil (100 mg) were evaluated in a single dose crossover study. Tadalafil and Sildenafil did not affect the pharmacokinetics of Dapotin.

Tamsulosin: Dapotin should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.

Withdrawal effects: Clinical trial in subjects with PE designed to assess the withdrawal effects of 62 days of daily or as needed dosing with 60 mg Dapotin showed no evidence of withdrawal syndrome.