Dapoxetine CAS129938-20-1 Treatment of impotence and premature ejaculation Erectile dysfunction

Dapoxetine

Category:

Other chemical correlation

dapoxetine is a chemical with a density of 1.081g/cm3.) As a new rapid SSRI with a short half-life and belongs to selective serotonin reabsorption inhibitors (SSris), it is used to treat premature ejaculation and erectile dysfunction in men, with an effective rate of 98%.

Dapoxetine is absorbed quickly and can reach effective blood concentration quickly. The tissue is widely distributed, and the concentration of drug in nerve tissue is close to that in blood.

Chinese name

Dapoxetine

English name

Dapoxetine

Molecular weight

305.4134

CAS login number 119356-77-3

density

1.081 g/cm3

Molecular formula

C21H23NO

2. Dapoxetine package insert information

Chinese alias: Dapoxetine; (S-(+) -n, n-dimethyl-A -[2-(naphthoxy) ethyl] benzoylamine

English name :Dapoxetine

Phenylpropan-1-amine; (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

Physicochemical property

Appearance and properties: white to off-white crystalline powder

Density: 1.081g /cm

Boiling point :454.4ºC at 760mmHg

Flash point :132.6ºC

Refractive index :1.607

Vapor pressure :1.91E-08mmHg at 25°C[1]

Clinical use

dapoxetine is a new rapid SSRI with a short half-life and belongs to selective serotonin reabsorption inhibitors (SSris), which is used to treat premature ejaculation in men.

Usage and dosage

30-60mg each time

Dosage and usage

One capsule should be taken orally 1-3 hours before delivery.

efficacy

A new drug to treat premature ejaculation in men.

Suitable for people

Premature ejaculator

Not suitable for use

Minors, pregnant women and lactating women are prohibited.

Matters needing attention

(1) Patients with recent stroke and heart attack, low blood pressure, or certain rare hereditary eye diseases and retinitis pigmentosa are contraindicated.

(2) This product shall not be used with NO donor (such as any short-acting or long-acting nitrates).

(3) Patients with a history of severe cardiovascular disease who are not suitable for sexual activity and severe liver damage should not use this product.

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

(5) This product combined with amlodipine 5mg or 10mg orally had an accumulative antihypertensive effect, with an additional reduction of 1.1kPa(8mmHg) in systolic blood pressure and 0.9kPa(7mmHg) in diastolic blood pressure with other antihypertensive agents, respectively.

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

Related clinical research

Random test

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

SSRIs have been identified as the most effective treatment for PE among all therapeutic drug classes. Newer SSRIs agents show promise by acting more rapidly, having a shorter half-life and a lower incidence of side effects. The FDA will likely approve some of the new agents under study, and the number of patients treated with SSRIs for PE is expected to increase in the near future.

Dapoxetine can be absorbed quickly and reach effective blood concentration quickly, with peak time of 1.4 -- 2.OH. The peak blood concentration of Dapoxetine 30 and 60mg was 297 and 498ng·mL 1 ', respectively, showing dose correlation [2,]. The distribution volume was 2IL·kg 1 ', the tissue distribution was wide, the drug concentration in nerve tissue was close to that in blood, the absolute bioavailability was 42%, the protein binding rate was 9%, and the metabolites were about 40 through various pathways (cyp50, FMol), the main metabolites were demethyldapoxetine and Dapoxetine N oxide. The excretion of dapoxetine was rapid, and the blood concentration of a single dose of Dapoxetine dropped to about 5% of the peak concentration within 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 blood concentration was reached with mild accumulation (about 1.5 times) after continuous administration for 4 days. The pharmacokinetic characteristics of Dapoxetine were dose-dependent and time-invariant, and were not affected by multiple doses, as were its major metabolites. The study showed that Cmax and AUC were similar in young and old people, and food reduced the absorption rate of Dapoxetine by 11%(398 vs. 443ng·mL), Tm prolonged 3omin, but AUC was not affected.

Phase II clinical trial

The Phase II trial evaluated the efficacy and safety of Dapoxetine 60mg, 10omg and placebo in the treatment of PE using a multicenter, double-blind, randomized, controlled, and crossover trial. The study included 166 patients (aged 18-65 years, average IELT 1.olmin, single fixed heterosexual partner > 6 months) Participants were divided into three groups. They were given Dapoxetine 60, 100mg, or placebo 1 to 3 hours before sexual activity, and their IELT was measured by a stopwatch of their sexual partner. 130 patients completed the trial, which showed a significant increase in IELT at all doses of dapoxetine compared with placebo (P< 0.0001). The mean pre-trial IELT was 1.0lmin, and the end point IELT of the 100mg, 60mg and placebo groups were 3.20, 2.94 and 2.05min, respectively. The first dose was effective. 0.00 1. The incidence of nausea was 5.6%, 16.1% and 0.7%, respectively. Of the 10 patients who dropped out of the trial due to adverse reactions, 9 were in the 100mg group, so the maximum dose of dapoxetine in the Phase 1 trial was 60mg