What Is Dapoxetine?

Dapoxetine is a chemical used to treat premature ejaculation in men. The total effective rate of dapoxetine was 98%.

Chinese name: Dapoxetine
English name: Dapoxetine
Molecular weight: 305.4134

CAS Registry Number: 119356-77-3
Density: 1.081g / cm3
Molecular formula: C21H23NO

Dapoxetine Basic Information

Chinese name

Chinese alias: Daboxetine; (S-(+)-N, N-dimethyl-a- [2- (naphthyloxy) ethyl] benzylamine

English name: Dapoxetine

English alias: (1S) -N, N-dimethyl-3-naphthalen-1-yloxy-1-phenylpropan-1-amine; Priligy; Dapoxetina; Dapoxetinum; CAS number: 119356-77-3

Molecular formula: C ₂₁ H ₂₃ NO

Molecular weight: 305.41300

Exact mass: 305.17800

PSA: 12.4000

LogP: 4.91160

Structural formula:

Physicochemical properties of dapoxetine

Appearance and properties: white to off-white crystalline powder

Density: 1.081 g / cm ³

Boiling point: 454.4ºC at 760mmHg

Flash point: 132.6ºC

Refractive index: 1.607

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

Dapoxetine Dapoxetine related drug label information

Dapoxetine clinical use

Dapoxetine is a new type of fast SSRI with short half-life. It is a selective serotonin reuptake inhibitor (SSRI) and is used to treat male premature ejaculation.

Dapoxetine dosage

30-60mg each time

Dapoxetine dosage and usage

Take one capsule 1-3 hours before.

The efficacy of dapoxetine

New medicine for treating male premature ejaculation.

Dapoxetine is suitable for the crowd

Patients with premature ejaculation

Dapoxetine should not be taken

Minors, pregnant women, lactating women are prohibited.

Dapoxetine precautions

(1) Patients with recent stroke and heart attack, hypotension or some rare hereditary eye diseases and pigmented retinitis are contraindicated.

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

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

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

(5) This product has a cumulative antihypertensive effect when administered orally with 5 mg or 10 mg of amlodipine. Patients' systolic and diastolic blood pressures have an average additional reduction of 1.1 kPa (8 mmHg) and 0.9 kPa (7 mmHg). .

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

Clinical studies of dapoxetine

Random test

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

Of all the therapeutic drug categories, SSRIs have been determined to have the best effect on PE. Newer SSRIs have a faster effect, shorter half-life, and lower incidence of side effects, showing promise. The US FDA will likely approve some new formulations being studied, and it is expected that the number of patients treated with SSRIs for PE will continue to increase in the near future.

Dapoxetine is absorbed quickly and can reach the effective blood concentration quickly. The peak time is 1.4-2.oh. The peak blood concentrations of single-dose dapoxetine 30 and 60mg are 297 and 498ng · mL-1 ', respectively. Relevance [2,]. The volume of distribution is 2IL · kg-1 '; the tissue is widely distributed, and the drug concentration in the nervous tissue is close to the blood drug concentration; the absolute bioavailability is 42%; the protein binding rate is 9%. It is metabolized by multiple pathways (cyp50, FMol), with up to 40 metabolites. The main metabolites are desmethyl dapoxetine and dapoxetine-N oxide. Dapoxetine is excreted quickly. The blood concentration of a single dose of dapoxetine drops to about 5% of its peak concentration within 24 hours. Its excretion is divided into two phases. About 20h. Steady-state blood drug concentration was reached after 4 days of continuous administration, with slight accumulation (about 1.5 times). The pharmacokinetic characteristics of dapoxetine are dose-dependent and time-invariant, and are not affected by multiple doses, and its main metabolites are also not affected by multiple doses. Studies have shown that Cmax and AUC are similar in young and old people. Food can reduce the absorption rate of dapoxetine, its Cmax is reduced by 11% (398 vs. 443ng · mL), and Tm is extended by 3omin, but AUC is not affected.

Phase II clinical trial

A multi-center, double-blind, randomized, controlled, and crossover trial was used to evaluate the efficacy and safety of dapoxetine 60mg, 10omg, and placebo for PE in a phase II clinical trial. The study involved 166 patients (aged 18-65 years old, average IELT 1.olmin, single fixed heterosexual partner> 6 months), divided into 3 groups, taking dapoxetine 60 1-3 hours before sexual activity. , 100 mg, and placebo. IELT was determined by a sexual partner using a stopwatch. A total of 130 patients completed the trial, and the results showed that all doses of dapoxetine significantly increased the IELT compared with placebo (P <0.0001). The average IELT before the trial was 1.0 lmin, and the endpoints for the 100 mg, 60 mg, and placebo groups were 3.20, 2.94, and 2.05 min, respectively, and the first dose was effective. The two treatment groups were p <0.00 1 compared with the placebo group. The incidence of major adverse reactions nausea was 5.6%, 16.1%, and 0.7%, respectively. Of the 10 patients who withdrew from the trial due to adverse reactions, there were 9 patients in the 100 mg group. Therefore, the maximum dose of dapoxetine in the phase 1 clinical trial was 60 mg.

Phase III clinical trials are to verify the effectiveness and safety of taking dapoxetine on time and in patients with moderate to severe PE. Two 12-week, multicenter, randomized, double-blind, controlled, balanced trials were conducted at 121 trial sites across the United States. 2614 patients received placebo (n = 870), dapoxetine 30mg (n = 874), and 60mg ( n = 870), taking medication 1-3h before sexual activity, the main endpoint was to measure IELT with a stopwatch. The number of completed trials was 627 in the placebo group, 676 in the 30 mg group, and 610 in the 60 mg group. The results showed that compared with placebo, all doses of dapoxetine significantly prolonged IELT (P <0001), and the first dose was effective. Before the trial, the placebo, 30 mg and 60! N9 groups were (0.90 ± 0.47), (0.92 ± 0.50), and (0.91 ± 0.48) min, respectively, and the endpoints after 12 weeks were (1.75 ± 2.21), (2:78 ± 3.48) and (3.32 ± 3.68) min. Therefore, taking time-consuming dapoxetine 30 and 60 mg is effective for patients with moderate to severe PE and is well tolerated. The main adverse reactions were nausea and headache.

Common adverse reactions of dapoxetine are nausea, diarrhea, dizziness, and headache. In the Phase 1 clinical trial, the incidence of nausea was the highest, reaching 20% in the 60 mg group, with 10% of patients discontinuing the trial, dizziness of 6.2%, and diarrhea of 6.8%. Single-dose 3omg and 6omg adverse reaction rates were 26.2% and 40.5%, and multiple doses were 45.2% and 40.5%, respectively. Diarrhea, nausea, and dizziness were more common than dg. The incidence of ds was similar to that of single-dose Most are mild to moderate adverse reactions. No serious adverse events such as the cardiovascular system, liver and blood system were found.

There are no reports of interactions between dapoxetine and other drugs. In the pharmacokinetic study of dapoxetine and phosphodiesterase inhibitors teldanafil and sildenafil, and ethanol, although sildenafil increased the AUC of dapoxetine by 2%, it was not clinical Significance; and there is no obvious pharmacokinetic interaction between ethanol and dapoxetine ^[2] .