Dapoxetine hydrochloride powder

AASraw is with synthesis and production ability from gram to mass order of Dapoxetine hydrochloride powder (129938-20-1), under CGMP regulation and trackable quality control system.

Dapoxetine hydrochloride is a short-acting novel selective serotonin reuptake inhibitor marketed for the treatment of premature ejaculation in men. Premature ejaculation (PE) is the most common male sexual disorder, estimated to affect up to 30% of men. Dapoxetine hydrochloride is an analytical reference standard that is categorized as a selective serotonin reuptake inhibitor. It provides improvement in several parameters related to premature ejaculation in clinical trials. This product is intended for research and forensic applications.

Product Description

 

Dapoxetine hydrochloride anaesthesia powder video

 

 


 

I.Raw Dapoxetine hydrochloride anaesthesia powder basic Characters:

 

Name: Dapoxetine hydrochloride
CAS: 129938-20-1
Molecular Formula: C9H7ClN2O5
Molecular Weight: 258.62
Melt Point: 175-179°C
Storage Temp: -20°C Freezer
Color: White crystalline powder

 


Dapoxetine is an organic compound of the class of selective inhibitors of serotonin reuptake but without anti-depressant effect. The drug is specifically developed to treat premature ejaculation in adult males between the ages of 18 and 64 who meet all of the following criteria:

1. Continuous or repeated ejaculation of the penis before, during, or shortly after insertion into the vagina, and only prior to the lack of sexual satisfaction;

2. Significant personal distress or interpersonal barriers due to premature ejaculation (PE);

3. Poor ejaculation control ability.

Chemical properties of Dapoxetine

Dapoxetine hydrochloride tablet is a gray film-coated tablet, which is white or off-white after removal of the coating.

Main ingredient: Dapoxetine hydrochloride.

IUPAC Name: (1S)-N,N-dimethyl-3-naphthalen-1-yloxy-1-phenylpropan-1-amine

 

Dapoxetine HCL powder Chemical Structure:

1. 2D Structure: https://pubchem.ncbi.nlm.nih.gov/image/imagefly.cgi?cid=71353&width=500&height=500

2. 3D Conformer: https://pubchem.ncbi.nlm.nih.gov/compound/Dapoxetine#section=3D-Conformer

Molecular formula: C21H23NO

Molecular Weight: 305.421 g/mol

CAS: 119356-77-3

 

Simple description of Dapoxetine

At present, there is no specific regulation for the treatment of male premature ejaculation with dapoxetine hydrochloride tablets. There is no specific regulation for how long the drug is used for treatment. It depends on the severity of the symptoms of premature ejaculation. The treatment difficulty is different. The medicine time cannot be generalized. However, the drug can improve the symptoms of premature ejaculation, so patients can take medication according to their own symptoms.

Dapoxetine is primarily intended for the treatment of 18 to 64 year old male premature ejaculation (PE) patients who meet all of the following conditions, including:

1. The penis is minimally small before, during, or shortly after insertion into the vagina, and before sexual satisfaction. Sexual stimuli are continuous or repeated ejaculation;

2. Significant personal distress or interpersonal barriers due to premature ejaculation (PE);

3. Poor ejaculation control.

 

Dapoxetine is already been approved as a pharmaceutical in Europe and the United States as having high effect on treatment of premature ejaculation. When taking dapoxetine, serotonin, a substance in the brain, is secreted. This serotonin is a substance that burns the excitement of the brain or brings about a relaxing effect. The tension and excitement are solved, the effect of adrenaline is also reduced, so that ejaculation timing can be delayed.

Dapoxetine hydrochloride can effectively inhibit 5-HT reuptake and increase the concentration of 5-HT in the synaptic cleft by inhibiting the 5-HT transporter. Studies have shown that dapoxetine centrally inhibits ejaculation reflex, and the giant cell lateral nucleus is an essential brain structure. When the concentration of dapoxetine is high, the monoamine protein transport system can be inhibited, and the reuptake of dopamine is also inhibited. Dapoxetine increases the latency of pudendal motor neuron reflexes and improves sexual function.

How long it takes for dapoxetine hydrochloride tablets to be effective is not generalized. Treatment depends on the severity of the symptoms of premature ejaculation. The difficulty of treatment is different, and the time of taking the medicine is different.

 

Action mechanism of Dapoxetine

The mechanism of action of dapoxetine in the treatment of premature ejaculation may be related to the inhibition of the reabsorption of serotonin by neurons, thereby affecting the potential difference of neurotransmitters acting on receptors before and after cell synapses.

Dapoxetine is effective for premature ejaculation because it has the effect of increasing the concentration of serotonin that suppresses excitation in the brain.

Serotonin is usually reabsorbed from the synapse, but by taking dapoxetine it inhibits reabsorption and suppresses serotonin.

Serotonin suppresses dopamine that amplifies pleasure, anxiety, and adrenaline that comes out when you are nervous, so you can lengthen the time to ejaculate.Dapoxetine is effective for premature ejaculation because it has the effect of increasing the concentration of serotonin that suppresses excitation in the brain.

Serotonin is usually reabsorbed from the synapse, but by taking dapoxetine it inhibits reabsorption and suppresses serotonin.
Serotonin suppresses dopamine that amplifies pleasure, anxiety, and adrenaline that comes out when you are nervous, so you can lengthen the time to ejaculate.

Human ejaculation is mainly mediated by the sympathetic nervous system. The reflex pathway of ejaculation is derived from the spinal reflex center, which is mediated by the brainstem, which is initially affected by many brain nuclei (medial preoptic nucleus and hypoventricular paraventricular nucleus).

 

Dapoxetine HCL Pharmacokinetics

After oral administration, dapoxetine is rapidly absorbed and reaches a maximum plasma concentration (Cmax) after approximately 1-2 hours. The absolute bioavailability is 42% (range 15-176%). After a single oral administration of 30 mg and 60 mg of dapoxetine in the fasting state, peak plasma concentrations (297 ng/ml and 498 ng/ml, respectively) were reached after 1.01 and 1.27 hours, respectively. Ingestion of a high-fat diet can moderately reduce the Cmax (10%) of dapoxetine and moderately increase AUC (12%), while also slightly delaying the peak concentration of dapoxetine; however, high fat intake Diet does not affect the extent of absorption. None of these changes have clinical significance. Bentley can be served with or without meals.

After administration of the human body by intravenous injection, the estimated early, middle, and terminal half-lives of dapoxetine are 0.10, 2.19, and 19.3 hours, respectively.

The metabolites of the excreted dapoxetine are mainly cleared by urine in the conjugate situation. No active substance was detected in the urine. Dapoxetine is rapidly cleared, and the evidence is the bottom of the blood concentration 24 hours after administration (less than 5% of the peak concentration). The daily dose of dapoxetine is very small. The terminal half-life of oral administration is approximately 19 hours. The half-life of desmethyl dapoxetine is similar to that of dapoxetine.

 

Use of Dapoxetine

Treatment of male patients with premature ejaculation (PE)

Dapoxetine hydrochloride tablets can effectively enhance ejaculation control ability; significantly improve sexual life satisfaction; effectively prolong ejaculation latency.

While using medication, patients can also use some small measures to improve the symptoms of premature ejaculation, adjust the mood, strengthen communication between husband and wife, rational diet, strengthen physical exercise, daily running, and participate in a physical activity every week. It is also a good choice to play football and play basketball to enhance physical fitness and relieve psychological stress.

 

Dosage of Dapoxetine

The dosage of dapoxetine hydrochloride tablets is oral, and the tablets should be swallowed intact; patients are advised to take at least one full cup of water for medication; patients should try to avoid injuries caused by prodromal symptoms such as syncope or dizziness.

The amount of dapoxetine hydrochloride tablets recommended for all patients in adult males (18 to 64 years old) is 30 mg and needs to be taken about 1 to 3 hours before sexual life. If the effect is not satisfactory after taking 30mg and the side effects are still within the acceptable range, the dosage can be increased to 60mg of the maximum recommended dose.

The recommended maximum dose is used every 24 hours.
The elderly (aged 65 and over) This product has not been evaluated in 65 years and the safety and efficacy in patients over the crowd used, the main reason for the data on this product for use in this population is extremely limited in patients with mild renal impairment or Patients with kidney damage do not need to adjust the dose when taking this product, but should take it with caution. This product is not recommended for patients with severe kidney injury.

 

Dapoxetine Indications:

This product is intended for the treatment of male patients with premature ejaculation (PE) between the ages of 18 and 64 who meet all of the following conditions: the penis continues until it is inserted into the vagina, during or shortly after insertion, and before the sexual gratification is achieved, only due to minimal irritation. Or repeated ejaculation; and significant personal distress or interpersonal barriers due to premature ejaculation (PE); and poor ejaculation control.

(1) Adult males (18 to 64 years old)

Recommend a first dose of 30 mg for all patients and need to take about 1 to 3 hours before sex. If the effect is not satisfactory after taking 30mg and the side effects are still within the acceptable range, the dosage can be increased to 60mg of the maximum recommended dose. The recommended maximum dose is used every 24 hours. This product can be taken before or after a meal.

If the doctor chooses this product to treat premature ejaculation, he should evaluate the risk and the patient’s reported benefit for the first 4 weeks after the drug is used, or evaluate the patient’s risk-benefit balance after using the 6-time treatment dose and decide whether to continue using the product.

(2) The elderly (65 years and older)

Research has not yet assessed the safety and efficacy of this product in patients aged 65 and over. The main reason for this is that the data on the use of this product in this population is extremely limited.

(3)Children and young people

This product is not intended for use by people under the age of 18.

One tablet at a time can be taken indefinitely. The drug needs to be taken on an empty stomach. It is better to drink tea before use well before this medicine is best to do a comprehensive inspection system, depending on their illness in a doctor or pharmacist told and security arranged for the drug in order to avoid improper use of drugs, but not arbitrarily increase the frequency of drug use during You must follow the doctor’s arrangements and embarrassment.

 

Dapoxetine Overdose

In general, symptoms of overdose of a selective serotonin reuptake inhibitor include serotonin-mediated adverse effects such as lethargy, gastrointestinal dysfunction such as nausea and vomiting, excitement, tremor, dizziness and tachycardia. In the case of overdose, standard support measures should be taken as needed. There are currently no specific antidote to this product.

 

Dapoxetine HCL Precautions

1. General precautions. Dapoxetine is only used for male patients with premature ejaculation. The safety of Dapoxetine in men who do not have premature ejaculation is not clear. At the same time, there is no data on the effect of Dapoxetine on delaying ejaculation in this population. It is recommended that patients should not take Beverly and “entertainment drugs” at the same time because the effect is unknown and serious adverse events may occur.

2. Patients are advised not to take stimulating psychotropic drugs while taking it.

3. Avoid taking alcohol when taking Dapoxetine.

4. Use Dapoxetine may cause syncope or dizziness

5. Also take moderate cytochrome P450 3A4 inhibitors like erythromycin, clarithromycin, fluconazole, verapamil and diltiazem.

6. Take strong cytochrome P450 2D6 inhibitor or known cytochrome P450 2D6 Patients with weak metabolism should be cautious when increasing the dose to 60 mg, as this may lead to increased exposure, which may eventually lead to higher dose-dependent adverse reactions and severity.

7. Beneficial should not be used for mania/ Patients with a history of hypomanic or bipolar disorder, at the same time, any patient with symptoms of the above-mentioned disease should be discontinued with Dapoxetine.

8. Because selective serotonin reuptake inhibitor may lower the threshold of epilepsy Value, any patient with seizures should be discontinued, and patients with unstable epilepsy should avoid using Dapoxetine.

9. Dapoxetine should not be used in people under the age of 18.

10. Not recommended For patients with severe kidney damage, patients with mild or moderate renal impairment should be used with caution. Like other selective serotonin reuptake inhibitors, the use of Dapoxetine is associated with some eye reactions. For example, pupil dilation and eye pain. Patients with elevated intraocular pressure or risk of angle-closure glaucoma should be used with caution.

 

Dapoxetine HCL powder Prohibited

1. Dapoxetine is forbidden for patients known to be allergic to dapoxetine hydrochloride or any excipients.

2. Dapoxetine is forbidden for patients with obvious pathological conditions in the heart [eg heart failure (NYHA II-IV), no Abnormal conduction with permanent pacemaker therapy (grade 2 or 3 atrioventricular block or sick sinus syndrome), significant myocardial ischemia and valvular disease]

3. Dapoxetine neither with monoamine oxidase inhibitors (MAOIs) ) It should not be used together within 14 days after the treatment of monoamine oxidase inhibitors was stopped. Similarly, monoamine oxidase inhibitors should not be used within 7 days of discontinuation of Bili (see drug interactions).

4. Dapoxetine can neither be used with thioridazine nor after thiodazine treatment is stopped. Used within days. Similarly, thioridazine should not be taken within 7 days after discontinuation of Dapoxetine (see the drug interaction section).

5. Dapoxetine is banned from taking ketoconazole, itraconazole, ritonavir, saquin Patients with strong cytochrome P450 3A4 inhibitors such as nave, telithromycin, nefazodone, naffenavir, and atazanavir.

6. Dapoxetine is prohibited for patients with moderate and severe liver injury.

 

Dapoxetine HCL powder Conclusion

When using dapoxetine hydrochloride tablets, it should be administered under the guidance of a physician, which can improve the symptoms of the disease and at the same time better serve the drug.

 


 

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