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Raw Dapoxetine Powder CAS 129938-20-1

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Raw Dapoxetine Powder CAS 129938-20-1

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Molecular Formula: C9H7ClN2O5
Molecular Weight: 258.62
Melting Point: 175-179°C
Storage Temp: -20°C Freezer
Color: White crystalline powder

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Dapoxetine Powder Briefing

Dapoxetine Powder used for the treatment of premature ejaculation (PE) in men. Dapoxetine is a treatment designed specifically for men who have problems with premature ejaculation.

Dapoxetine Powder 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:

2. 3D Conformer:

Molecular formula: C21H23NO

Molecular Weight: 305.421 g/mol

CAS: 119356-77-3

Simple description of Dapoxetine Powder

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 Powder 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 Powder 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 Powder 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 Powder

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).

Use of Dapoxetine Powder

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.

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.

Dosage of Dapoxetine Powder

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.

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