Dapoxetine (Dapoxetinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Potency regulators

Included in the formulation
  • Priligi®
    pills inwards 
    Berlin-Chemie, AG     Germany
  • Primaxetine®
    pills inwards 
    OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC     Russia
    • АТХ:

    G.04.B.X.14   Dapoxetine

    G.04.B.X   Other drugs for the treatment of urological diseases

    Pharmacodynamics:

    It is assumed that the mechanism of action of dapoxetine in premature ejaculation is associated with inhibition of reuptake of serotonin by neurons, followed by an increase in the action of the neurotransmitter on pre- and postsynaptic receptors. The mechanism of ejaculation is regulated mainly by the sympathetic nervous system. Postganglionic sympathetic nerve fibers innervate the seminal vesicles, the vas deferens, the prostate, the urethra and the neck of the bladder, causing their coordinated contraction to achieve ejaculation. Dapoxetine affects the ejaculation reflex, increasing the latent period and decreasing the duration of the reflex impulse of the motoneurons of the perineal ganglia. Stimulus, which starts ejaculation, is generated in the spinal reflex center, which is controlled through the brain stem by several nuclei of the brain, including the preoptic and paraventricular.

    Pharmacokinetics:

    Quickly absorbed. The maximum concentration in the blood plasma (Cmax) is achieved 1-2 hours after taking the drug. Bioavailability ranges from 15 to 76%. The connection with plasma proteins is 98.5%. Metabolized in the liver, excreted by the kidneys in the form of conjugates. The half-life is 19 hours.

    Indications:

    Premature ejaculation in men aged 18 to 64 years.

    ICD-10

    V.F50-F59.F52.4   Premature ejaculation

    Contraindications:

    - severe blood diseases;

    - severe heart disease (eg, NYHA class II-IV heart failure, cardiac conduction abnormalities (AV block of grade 2-3) in the absence of a permanent pacemaker, severe coronary heart disease or valve apparatus damage);

    - simultaneous administration of monoamine oxidase inhibitors;

    - hypersensitivity;

    - simultaneous administration of serotonin reuptake inhibitors (selective serotonin reuptake inhibitors, serotonin reuptake inhibitors and norepinephrine and tricyclic antidepressants) and other drugs that have a serotonergic effect (for example, L-tryptophan, triptans, tramadol, linezolid, lithium, preparations of St. John's wort (Hypericum perforatum) and within 14 days after discontinuation of these medications;

    - age younger than 18 years;

    - simultaneous administration with inhibitors of CYP3A4 (ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nelfinavir, atazanavir);

    - kidney and liver diseases;

    - simultaneous administration with thioridazine;

    - lactose intolerance.

    Carefully:

    - age over 65;

    - mild or moderately severe renal dysfunction.

    - simultaneous use with drugs that affect platelet aggregation, and with anticoagulants due to the risk of bleeding.

    Pregnancy and lactation:

    Not intended for women.

    Dosing and Administration:

    For oral administration. The tablet should be swallowed whole, washed down with one full glass of water. The drug can be taken regardless of food intake.

    In a dose of 30 to 60 mg (depending on the health and age of the patient) once a day.

    Side effects:

    From the nervous system: anxiety, anxiety, decreased libido, unusual dreams, agitation, depression, nervousness, pathological thinking, anorgasmia, drowsiness, impaired concentration, tremor, paresthesia, lethargy.

    From the side of the organ of vision: blurred vision, pain in the eye area, visual impairment.

    From the cardiovascular system: "hot flashes", bradycardia, lowering of arterial pressure, systolic hypertension, cessation of sinus node activity.

    From the respiratory system: yawning, nasal congestion.

    From the gastrointestinal tract: nausea, vomiting, diarrhea, constipation, indigestion, bloating, dry mouth.

    On the part of the reproductive system: absence of ejaculation, erectile dysfunction, anorgasmia in men, paresthesia of the genital organs.

    From the skin and subcutaneous tissue: hyperhidrosis, cold sweat, itching.

    Other: increased blood pressure, increased heart rate, weakness, irritability, asthenia, a sense of anxiety, malaise.

    Overdose:

    In general, the symptoms of overdose with selective serotonin reuptake inhibitors include serotonergic reactions, including drowsiness, gastrointestinal disorders (nausea, vomiting), tachycardia, tremor, agitation and dizziness.

    If necessary, in case of an overdose, standard maintenance therapy should be performed. Because of the significant binding of the drug to plasma proteins and a large volume of distributiondapoxetine hydrochloride, forced diuresis, dialysis, hemoperfusion and blood transfusion are unlikely to be effective. The specific antidote is unknown.

    Interaction:

    Taking the drug simultaneously with serotonergic drugs (including inhibitors monoamine oxidase, L-tryptophan, triptans, tramadol, linezolid, selective serotonin reuptake inhibitors, serotonin and norepinephrine seizure inhibitors, lithium and St. John's wort preparations (Hypericum perforatum) may increase the incidence of serotonergic side effects.

    Alcohol enhances the effect of the drug on the nervous system (dizziness, drowsiness, slowing reflexes, changing judgments).

    Taking the drug with CYP2D6 inhibitors increases the systemic effect of the drug.

    Thioridazine prolongs the QTc interval, which is accompanied by ventricular arrhythmia. Dapoxetine inhibits the enzyme CYP2D6, and, apparently, inhibits the metabolism of thioridazine. It is expected that the resulting increase in the level of thioridazine will increase the elongation of the QTc interval.

    Do not allow simultaneous reception with monoamine oxidase inhibitors.

    A drug dapoxetine It should not be taken simultaneously with active inhibitors of CYP3A4, for example,ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nelfinavir and atazanavir, as they increase the concentration of dapoxetine in the blood plasma.

    Special instructions:

    Impact on the ability to drive and other mechanical means

    When taking the drug, attention, memory, and dizziness can be disturbed, so you should stop driving and controlling other complex mechanisms during intake.

    Instructions
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