Description
Trade name:
Andopoxetine
Compound:
Each tablet contains:
Dapoxetine 60 mg
Auxiliary components:
Lactose monohydrate, microcrystalline cellulose, carboxymethylcellulose, aerosil, magnesium stearate, titanium dioxide, polyethyleneglycol 6000, talc.
Properties:
Dapoxetine is a potent selective serotonin reuptake inhibitor (SSRI) with a half-maximal inhibition concentration (IC50) of 1.12 nM, metabolized in the body to the main metabolites – desmethyldapoxetine (IC50<1.0 nM) and didesmethyldapoxetine (IC50=2.0 nM), equally or less active (dapoxetine-N-oxide (IC50=282 nM)).
The mechanism of action of dapoxetine in premature ejaculation is associated with the inhibition of the reuptake of serotonin by neurons, followed by an increase in the effect of the neurotransmitter on pre- and postsynaptic receptors.
The mechanism of ejaculation is regulated mainly by the sympathetic nervous system. In rats, postganglionic sympathetic nerve fibers innervate the seminal vesicles, vas deferens, prostate gland, urethral muscles, and bladder neck, causing their coordinated contraction to achieve ejaculation. Dapoxetine affects the ejaculation reflex at the supraspinal level in the lateral paragigantocellular nuclei, increasing the latency period and decreasing the duration of reflex impulses of the perineal ganglia motor neurons. The stimulus that triggers ejaculation is generated in the spinal reflex center, which is controlled via the brainstem by several brain nuclei, including the preoptic and paraventricular nuclei.
Indications:
The drug is intended for the treatment of premature ejaculation in men aged 18 to 64 years.
The drug can only be used in patients who meet the following criteria:
– intravaginal ejaculation deferred time (IVDET) <2 min;
– persistent or regular ejaculation after minimal sexual stimulation before, during or shortly after sexual penetration, and occurring earlier than the patient desires;
– marked personal distress or difficulty in interpersonal relationships due to premature ejaculation;
-poor ejaculation control;
– the occurrence of premature ejaculation in most attempts at sexual intercourse over the past 6 months.
Dapoxetine should only be used as needed before anticipated sexual activity. It should not be used to delay ejaculation in men who do not have a confirmed diagnosis of premature ejaculation.
Method of administration and dosage:
The recommended starting dose for all men is 30 mg, taken 1-3 hours before expected sexual intercourse. If the 30 mg dose is not effective and well tolerated (no moderate to severe adverse reactions or prodromal symptoms that may precede syncope), the dose can be increased to the maximum recommended dose of 60 mg, taken 1-3 hours before sexual intercourse. The frequency and severity of adverse reactions increases with the 60 mg dose.
Contraindications:
– hypersensitivity to dapoxetine and/or to any excipient in the drug;
– severe heart disease;
– concomitant use of MAO inhibitors and dapoxetine within 14 days after discontinuation of the MAO inhibitor;
– concomitant use of selective serotonin reuptake inhibitors (SSRIs);
– serotonin and norepinephrine reuptake inhibitors and tricyclic antidepressants; other drugs with serotonergic action – concomitant use with strong CYP3A4 inhibitors;
– moderate and severe liver failure;
– severe renal failure;
– age under 18 years and over 64 years (due to the lack of data on the efficacy and safety of dapoxetine in these patient populations);
– lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
– history of syncope;
– history of manic state or severe depression;
– the presence of diagnosed or suspected orthostatic hypotension;
-in patients with mania/hypomania or bipolar disorder.
Precautions:
Concomitant use of dapoxetine with alcohol may enhance its effects on the central nervous system and may also increase neurocardiogenic adverse reactions such as syncope, thereby increasing the risk of accidental injury. Therefore, patients should be advised to abstain from alcohol while taking dapoxetine.
Side effects:
Psychiatric disorders: common – anxiety, agitation, restlessness, unusual dreams, decreased libido.
From the nervous system: very often – dizziness, headache; often – drowsiness, impaired concentration, tremor, paresthesia.
From the organ of vision: often – blurred vision; uncommon – mydriasis, eye pain, visual impairment.
From the organ of hearing and labyrinth: often – ringing in the ears; uncommon – vertigo.
From the cardiovascular system: often – hot flashes (skin hyperemia), increased blood pressure.
From the respiratory system: often – nasal congestion, yawning.
From the digestive system: very often – nausea.
Storage method:
Store at temperatures not exceeding 30 degrees.
