fast SSRI Sex Enhancement Powder Dapoxetine For Anxiety CAS 119356-77-3

fast SSRI Sex Enhancement Powder Dapoxetine For Anxiety CAS 119356-77-3

The basic information

Chinese name: dapoxetine

S-(+)-N, N-dimethyl-A -[2-(naphthoxy) ethyl] benzylamine

English name: Dapoxetine

(1S)-N,N-dimethyl-3-naphthalen-1-yloxy-1-phenylpropan-1-amine; Priligy; Dapoxetina;Dapoxetinum; CAS no. : 119356-77-3

Molecular formula: C21H23NO

Molecular Weight: 305.41300

Accurate mass: 305.17800

PSA: 12.47000

LogP: 4.91160

Formula:

Physical and chemical properties

Appearance and properties: white to off-white crystalline powder

Density: 1.081 g/cm3

Boiling point: 454.4 ° C at 760mmHg

Flash: DHS 132.6 C

Index of refraction: 1.607

1.91E-08mmHg at 25°C [1]

Drug label information related to dapoxetine

Clinical use

Dapoxetine (Dapoxetine), as a new fast SSRI with short half-life, is a selective serotonin reuptake inhibitor (SSRI), which is used to treat premature ejaculation in men.

Usage.

Every 30 to 60 mg

Dosage and Usage

One tablet should be taken orally within the first 1-3 hours.

efficacy

A new drug for male premature ejaculation.

Suits the crowd

In patients with premature ejaculation

Shall not take

Minors, pregnant women and lactating women are prohibited.

Matters needing attention

(1) Patients with recent stroke and heart attack, hypotension, or some rare inherited eye diseases and retinitis pigmentosa are contraband.

(2) This product is forbidden to be used in combination with NO donors (such as any kind of short-acting or long-acting nitrate drugs).

(3) This product is contraindant in patients with previous history of severe cardiovascular disease and is not suitable for sexual activity or severe liver damage.

(4) Use with caution in patients with severe renal damage, active peptic ulcer and hemorrhagic disease.

(5) This product combined with amlodipine 5mg or 10mg orally has a cumulative hypotensive effect, and the average additional reduction of systolic and diastolic blood pressure in patients is 1.1kPa(8mmHg) and 0.9kPa(7mmHg) with other antihypertensive agents.

(6) Stop taking other drugs when taking this product.

Related clinical studies

Random test

Of 166 randomized patients (mean age 23 to 64 years), 130 completed the study. The mean baseline IELT before treatment was 1.01 minutes. IELT was 2.94 minutes after 60 mg dose, 3.20 minutes after 100 mg dose, and 2.05 minutes after placebo, a significant difference. The most common adverse reaction was nausea. Nine of the 10 patients who discontinued treatment due to adverse reactions received 100 mg. The study concluded that two weeks of treatment with dapoxetine significantly improved PE as assessed by IELT at the first dose.

SSRIs have been identified as having the best efficacy in the treatment of PE among all therapeutic classes. Newer SSRIs, with their faster action, shorter half-life and lower incidence of side effects, show promise. The U.S. Food and Drug Administration (FDA) is likely to approve a number of novel agents under study, and an increasing number of patients are expected to be treated with SSRIs for PE in the near future.

Dapoxetine is quickly absorbed and can quickly reach the effective plasma concentration with the peak time of 1.4-2.OH. The peak plasma concentrations of single dose of dapoxetine 30 and 60mg are 297 and 498ng·mL 1 ', respectively, showing a dose correlation [2,]. The drug concentration of nerve tissue is close to that of blood drug concentration; the absolute bioavailability is 42%; the protein binding rate is 9%. It is metabolized by multiple ways (CYP50, FMOL), and there are about 40 kinds of metabolites, the main metabolites are demethyl dapoxetine and dapoxetine-N oxide. The plasma concentration of a single dose of dapoxetine decreased to about 5% of the peak concentration after 24h, and the excretion was divided into two phases, the initial phase TL /2 was about 1.4h, and the final phase TL /2 was about 20h. The steady state plasma concentration was reached after 4d of continuous administration, with slight accumulation (about 1.5fold). Studies have shown that the absorption rate of dapoxetine is decreased by 11%(398 vs 443ng·mL) and Tm is prolonged by 3omin, but AUC is not affected by food.

Phase II Clinical Trial

The Phase II clinical trial was a multicenter, double-blind, randomized, controlled, and crosstalk study to evaluate the efficacy and safety of dapoxetine 60mg, 10omg, and placebo in the treatment of PE. 166 patients (age 18-65 years, IELT mean 1.olmin, single fixed heterosexual partner >; IELT was measured by the sexual partner using a stopwatch. The participants were divided into three groups and given dapoxetine 60,100 mg or placebo 1 to 3 hours before sexual activity. A total of 130 patients completed the trial, which showed a significant increase in IELT compared with placebo at all doses of dapoxetine (P&L; 0.0001). The mean pre-trial IELT was 1.0lmin, and the endpoints of the 100mg, 60mg and placebo groups were 3.20, 2.94 and 2.05min, respectively, and the first dose was effective. 0.00 1. The incidence of major adverse events, nausea, was 5.6%, 16.1%, and 0.7%, respectively. Of the 10 patients who withdrew from the trial due to adverse events, 9 were in the 100mg group, so the maximum dose of dapoxetine used in the phase 1 trial was 60mg.

The phase III clinical trial was designed to verify the efficacy and safety of dapoxetine for on-demand and on-time administration in patients with moderate to severe PE. In two 12-week multicentre, randomized, double-blind, controlled balance trials at 121 sites across the United States, 2614 patients received placebo (n=870), dapoxetine 30mg(n=874), and dapoxetine 60mg(n=870) one to three hours before sexual activity. The primary endpoint was measured by a stopwatch. The number of people who completed the trial was 627 in the placebo group, 676 in the 30mg group, and 610 in the 60mg group. The results showed that all doses of dapoxetine significantly prolonged IELT compared with placebo (P&L; 0001), and the first dose is effective. Pretrial placebo, 30mg and 60! IELT n9 groups respectively (0.90 + / - 0.47), (0.92-0.50) and (0.91 + 0.48) min, 12 weeks after the finish (1.75 + / - 2.21), respectively (" 8 + / - 3.48) and (3.32 + / - 3.68 min. Therefore, dapoxetine 30 and 60mg on time is effective and well tolerated in patients with moderate to severe PE. The major adverse reactions were nausea and headache.

The common adverse reactions of dapoxetine were nausea, diarrhea, dizziness and headache. In the phase 1 trial, nausea was highest at 20% in the 60mg group, with 10% of patients discontinued, dizziness was 6.2%, and diarrhea was 6.8%. The incidence of adverse reactions in single dose of 3OMG and 6OMG was 26.2% and 40.5%, respectively, and that in multiple doses was 45.2% and 40.5%, respectively. The occurrence of diarrhea, nausea and dizziness in DL was more common than that in DG. The incidence of adverse reactions in DS was similar to that in single dose, and most of them were mild to moderate. No serious adverse events, such as cardiovascular system, liver or blood system, were found.

There have been no reports of dapoxetine interacting with other drugs. In the pharmacokinetic studies of dapoxetine and phosphodiacetase inhibitors tetanafil and sildenafil, as well as ethanol, although sildenafil increased the AUC of dapoxetine by 2%, it had no clinical significance. There was no significant pharmacokinetic interaction between ethanol and dapoxetine.