This product is intended for the treatment of male patients with premature ejaculation (PE) aged 18 to 64 years who meet
This product can only be purchased with a prescription from a urologist or male doctor.
Main ingredient: Dapoxetine hydrochloride.
Chemical name: (+)-(S)-N,N-dimethyl-α-[2-(1-naphthyloxy)ethyl]-benzylamine hydrochloride
Chemical structural formula: http://x1.webres.medlive.cn/drugref/ChemPreparationDetail/201509091157240914.png
Molecular formula: C21H23N0.HCL
Molecular weight: 341.88
This product is a gray film-coated tablet, white or almost white after removing the coating.
This product is suitable for the treatment of male premature ejaculation (PE) patients aged 18 to 64 who meet all of the following conditions:
Persistent or repeated ejaculation of the penis before, during, or shortly after insertion, and before sexual satisfaction is achieved due to only minimal sexual stimulation; and significant personal distress or interpersonal distress caused by premature ejaculation (PE) Communication obstacles; and poor ejaculation control.
30mg, 60mg (calculated as C21H23N0).
oral. The tablets should be swallowed whole. It is recommended that patients take the medication with at least a full glass of water. Patients should try to avoid injuries caused by prodromal symptoms such as syncope or dizziness.
1. Adult male (18 to 64 years old)
The recommended first dose for all patients is 30 mg, which needs to be taken about 1 to 3 hours before sex. If the effect is not satisfactory after taking 30 mg and the side effects are still within the acceptable range, the dosage can be increased to the maximum recommended dose of 60 mg. The recommended maximum dosage is once every 24 hours.
This product can be taken before or after meals (see section on pharmacokinetics).
If doctors choose this product to treat premature ejaculation, they should evaluate the risk and benefit reported by the patient in the first 4 weeks after using the drug, or evaluate the patient's risk-benefit balance after using the drug for 6 doses and decide whether to continue to use this product for treatment.
Seniors (65 years and older)
The safety and efficacy of this product in the population of patients 65 years and older have not been evaluated. The main reason is that the data on the use of this product in this population is extremely limited (see the section on pharmacokinetics).
Children and adolescents
This product is not for use in people under 18 years of age.
Patients with kidney injury
Patients with mild or moderate renal impairment do not need to adjust the dose when taking this product, but they should be taken with caution. This product is not recommended for patients with severe renal impairment (see the pharmacokinetics section).
Patients with liver injury
Patients with mild liver injury do not need to adjust the dose when taking this product; this product is forbidden to be used in patients with moderate and severe liver injury (Child-pugh C) (see the pharmacokinetics section).
Clinical trial data
The safety of this product was evaluated in 6081 patients who had premature ejaculation and participated in five double-blind, placebo-controlled clinical trials. Among these evaluated subjects, 4222 patients received this product. Among them, 1615 cases received 30 mg of this product as needed, and 2607 received 60 mg of this product, either on-demand or once a day.
Syncope (characterized by loss of consciousness) has been reported in clinical trials, and the event is considered to be drug-related. Most of the cases occurred within 3 hours after the administration, after the first administration or during the research-related operations performed in the clinic (such as blood draw, upright movement, and blood pressure measurement), it often occurs before syncope Prodrome.
Orthostatic hypotension has been reported in clinical trials
The most common (≥5%) adverse drug reactions in clinical trials include headache, dizziness, nausea, diarrhea, insomnia, and fatigue. The most common events leading to discontinuation include nausea (2.2% of subjects in the product-treated group) and dizziness (1.2% of subjects in the product-treated group).
Table 1 lists adverse drug reactions with an incidence of> 1% among subjects in the product treatment group in these trials.
This product is forbidden to be used in patients who are known to be allergic to dapoxetine hydrochloride or any excipients.
This product is forbidden to be used in patients with obvious pathological conditions of the heart (such as heart failure (NYHA grade II-IV), conduction abnormalities not treated with permanent pacemakers (grade 2 or 3 atrioventricular block or sick sinus syndrome) Sign), obvious myocardial ischemia and valvular disease]
This product can neither be used together with monoamine oxidase inhibitors (MAOIs), nor can it be used within 14 days after the treatment with monoamine oxidase inhibitors is stopped. Similarly, monoamine oxidase inhibitors should not be used within 7 days after discontinuing Piligen (see the Drug Interactions section).
This product can neither be used together with thioridazine, nor can it be used within 14 days after thioridazine treatment is stopped. Similarly, thioridazine should not be taken within 7 days after discontinuing Pligen (see the Drug Interactions section).
This product is prohibited from taking ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nafenavir, atazanavir and other strong cytochrome P450 3A4 inhibition at the same time For the patient.
This product is forbidden to be used in patients with moderate and severe liver damage.
Using Biligen may cause fainting or dizziness.
-If the patient has possible prodromal symptoms, he should immediately lie down so that the head is lower than other parts of the body, or sit down and place the head between the knees until the symptoms disappear.
Patients should be warned to avoid situations that may cause injury in the event of syncope or other central nervous system (CNS) effects, including driving or operating dangerous machinery.
The simultaneous use of this product with alcohol may aggravate alcohol-related neurological effects, and may also aggravate the adverse reactions of the nervous and cardiovascular system (such as syncope), and therefore increase the risk of accidental injury; therefore, it is recommended that patients should avoid taking this product Take alcohol.
See the instructions for details.
Medication for pregnant and lactating women
Women are not suitable for using this product.
Rats or rabbits receiving up to 100 mg/kg (rat) or 75 mg/kg (rabbit) of this product have not found evidence of teratogenicity, embryo toxicity or fetal toxicity. Based on the current limited observational data from clinical trial databases, there is no evidence that taking dapoxetine will affect the mother's pregnancy. At present, there has not been a sufficient number of well-controlled studies on pregnant women.
It is not clear whether dapoxetine or its metabolites can be secreted in human milk.
This product should not be used for people under 18 years of age.
The safety and efficacy of this product in patients aged 65 years and older have not been evaluated. The main reason is that the data on the use of this product in this population is extremely limited.
The analysis of the clinical pharmacology study of a single dose of 60 mg dapoxetine hydrochloride showed that there was no significant difference in pharmacokinetic parameters (Cmax, AUCinf, Tmax) between healthy elderly men and healthy young men.
Possibility of interaction with monoamine oxidase inhibitor oxidase
In patients taking a selective serotonin reuptake inhibitor plus a monoamine oxidase inhibitor (MAOI), severe (sometimes fatal) reactions have been reported. These reactions include high fever, rigidity, myoclonus, spontaneous Neurological instability is accompanied by possible rapid fluctuations in vital signs and changes in mental state, including quarterly excitement and development of delirium and coma. Recently, a selective serotonin reuptake inhibitor was discontinued and a monoamine oxidase inhibitor was started These reactions have also been reported in patients treated with drugs, and some cases have features similar to neuroblocker malignant syndromes. 1. Possibility of interaction with monoamine oxidase inhibitors In patients taking a selective serotonin reuptake inhibitor and a monoamine oxidase inhibitor (MAOI) at the same time, there have been severe (sometimes fatal) reactions Reported that these reactions include high fever, rigidity, myoclonus, autonomic instability with possible rapid fluctuations in vital signs and changes in mental state, including extreme excitement and development of delirium and coma. These reactions have also been reported in patients who recently discontinued a selective serotonin reuptake inhibitor and started using a monoamine oxidase inhibitor. Some cases show features similar to neuromuscular blocker malignant syndrome. The combined use of selective serotonin reuptake inhibitors and monoamine oxidase inhibitors in animal models shows that these drugs may have a synergistic effect in raising blood pressure and inducing behavioral excitement. Therefore, this product cannot be combined with monoamine oxidase inhibitors. It cannot be used within 14 days of stopping the monoamine oxidase inhibitor. Similarly, monoamine oxidase inhibitors cannot be used within 7 days of stopping this product. (See taboo section)
2. Possibility of interaction with thioridazine
Thioridazine alone can prolong the QTc interval, which is accompanied by severe ventricular arrhythmia. Some drugs that can inhibit cytochrome P450 2D6 isoenzymes, such as Perigen, can inhibit the metabolism of thioridazine and lead to an increase in the concentration of thioridazine, which will increase the effect of prolonging the QTc interval.
This product cannot be combined with thioridazine, nor can it be used within 14 days of stopping thioridazine. Similarly, thioridazine cannot be used within 7 days of stopping this product. (See taboo section)
3. Medicines/herbal medicines with serotonin effect
Like other selective serotonin reuptake inhibitors, Pligen is compatible with drugs/herbals with serotonin effects (including monoamine oxidase inhibitors, L-tryptophan, triptan, tramadol, linezolid, The combined use of selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, lithium agents, and Hypericum perforatum extract (Hypericum) may cause serotonin effects. This product cannot be combined with other selective serotonin reuptake inhibitors, monoamine oxidase inhibitors or other drugs/herbal medicines with serotonin-related effects. Nor can it be used within 14 days after stopping these medicines/herbal medicines. Similarly, these medicines/herbal medicines cannot be taken within 7 days of stopping this product. (See taboo section)
Central nervous system active drugs
The combination of this product and CNS active drugs has not been systematically evaluated in patients with premature ejaculation. Therefore, if it is necessary to use this product with such drugs, the patients should be treated with caution.
The effect of combination drugs on dapoxetine
In vitro studies conducted in human liver, kidney and intestinal microsomes indicate that dapoxetine is mainly metabolized by cytochrome P450 2D6, cytochrome P450 3A4 and flavin-containing monooxygenase 1 (FMO1), so inhibitors of these enzymes may be Reduce the clearance rate of Dapoxetine.
Powerful cytochrome P450 3A4 inhibitor
Ketoconazole (200 mg twice a day for 7 days) can increase the CMAX and AUCINF of dapoxetine (60 mg single dose) by 35% and 99%, respectively. Taking into account the effects of free dapoxetine and desmethyl dapoxetine, if you take a strong CYP3A4 inhibitor, the active part (the sum of free dapoxetine and desmethyl dapoxetine) is the largest blood drug The concentration may be
Increased by about 25%, AUC may be doubled. Such an increase will be obvious in some patients, mainly including the lack of cytochrome CYP2D6 functional enzymes, namely cytochrome CYP2D6 weak metabolizers or combined use of strong cytochrome P2D6 inhibitors patient.
Therefore, this product is contraindicated in patients taking ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nafenavir, atazanavir and other patients at the same time.
Moderate cytochrome P450 3A4 inhibitor
Taking moderate cytochrome P450 3A4 inhibitors at the same time, such as erythromycin, clarithromycin, fluconazole, amprenavir, furosanavir, aprepitant, verapamil and diltiazem, may also increase Exposure to dapoxetine and desmethyldapoxetine, especially those with weak metabolizers of cytochrome CYP2D6. Therefore, in combination with any of the above drugs, the maximum dose of this product is limited to 30mg, and it is recommended to use it with caution.