Dapoxetine-ZZ pills 30mg, 10pcs

Composition

1 film-coated tablet contains:

Active ingredient:

dapoxetine hydrochloride-33.6 mg (based on dapoxetine) – 30 mg;

excipients (core):

lactose monohydrate (milk sugar) – 44.0 mg;

croscarmellose sodium (primellose) – 4.0 mg,

microcrystalline cellulose 102-14.9 mg,

colloidal silicon dioxide (aerosil) – 2.5 mg,

magnesium stearate-1.0 mg;

excipients (shell):  3 mg (hypromellose-1.64 mg; polysorbate-80 (twin-80) – 0.46 mg; talc – 0.46 mg; titanium dioxide E 171-0.31 mg; iron oxide yellow dye E 172-0.13 mg).

Pharmacological action

Pharmacotherapy group: treatment of premature ejaculation

ATX code: G04BX14

Pharmacological properties

Pharmacodynamics

Dapoxetine is a powerful selective serotonin reuptake inhibitor (SSRI) with a half-maximum inhibition (IC50) concentration of 1.12 nM, which is metabolized in the body to the main metabolites – desmethyldapoxetine (IC50

The mechanism of action of dapoxetine in premature ejaculation is associated with inhibition of serotonin reuptake 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, urethral and bladder neck muscles, causing their coordinated contraction to achieve ejaculation. Dapoxetine affects the ejaculation reflex at the supraspinal level in the lateral parahigantocellular nuclei, increasing the latent period and reducing the duration of reflex impulse of motor neurons of the perineal ganglia. The stimulus that triggers ejaculation is generated in the spinal reflex center, which is controlled through the brainstem by several brain nuclei, including the preoptic and paraventricular.

Pharmacokinetics

Suction

Dapoxetine is rapidly absorbed, and the maximum concentration in blood plasma (Cmax) is reached 1-2 hours after taking the drug. Absolute bioavailability is 42% (range 15-76%) and exposure (AUC and Cmax) increases proportionally to the dose in the range from 30 mg to 60 mg. After repeated oral use, the AUC of dapoxetine and its active metabolite desmethyldapoxetine increases by approximately 50% compared to the AUC values after a single dose.

The intake of fatty foods moderately reduces the Cmax of dapoxetine (by 10%) and increases the AUC (area under the concentration-time curve) and the time to reach the maximum concentration in blood plasma by 12%. These changes are not clinically significant. The drug Dapoxetine-SZ can be taken regardless of food intake.

Distribution

More than 99% of dapoxetine binds to plasma proteins in vitro. The active metabolite, desmethyldapoxetine, binds to plasma proteins by 98.5%. Dapoxetine is distributed throughout the body with an average equilibrium volume of distribution of 162 liters.

Metabolism

In vitro studies suggest that dapoxetine is metabolized by many liver and kidney enzymes, especially CYP2D6, CYP3A4 and flavin-containing monooxygenase (FM 01) of the kidneys. In a clinical study that examined the metabolism of 14C-dapoxetine, dapoxetine was extensively metabolized after oral use mainly by N-oxidation, N-demethylation, naphtho group hydroxylation, glucuronidation, and addition of a sulfo group. After oral use, signs of presystemic metabolism in the liver were found. The main components circulating in the blood plasma were intact dapoxetine and dapoxetine-N-oxide. In vitro studies have shown that dapoxetine-N-oxide is inactive. In addition, desmethyldapoxetine and didezmethyldapoxetine were detected in an amount of less than 3% of the total amount of circulating dapoxetine metabolites. An in vitro study found that desmethyldapoxetine is comparable in activity to dapoxetine, and didezmethyldapoxetine is approximately 2 times less active than dapoxetine. The exposure (AUC and Cmax) of unbound desmethyldapoxetine was 50% and 23% of unbound dapoxetine, respectively.

Deduction

Dapoxetine metabolites are mainly excreted by the kidneys in the form of conjugates. Dapoxetine is not detected unchanged in the urine. After oral use, the initial (dispositional) half-life of dapoxetine is approximately 1.5 hours, the plasma level is less than 5% of the peak concentration 24 hours after use, and the final half-life is about 19 hours. When taken daily, the final half-life is approximately 19 hours.

Pharmacokinetics of dapoxetine in specific patient populations

Race

A single dose of dapoxetine 60 mg did not reveal a statistically significant difference in the indicators among the representatives of the Caucasian race, the Black race, the Latin Americans and the representatives of the Mongolian race. Comparison of the pharmacokinetics of dapoxetine in Caucasians and Japanese showed higher Cmax and AUC values in the latter (by 10-20%) due to lower body weight. A higher level of systemic exposure is unlikely to cause a significant difference in the clinical effect. Elderly patients (65 years and older)

Analysis of a clinical pharmacology study with a single dose of dapoxetine 60 mg did not reveal a significant difference in pharmacokinetic parameters (Cmax, AUC_0-∞, Tmax) in healthy elderly men and healthy younger men.

In patients with impaired renal function

, there was no clear increase in the AUC of dapoxetine with a decrease in renal function. The AUC of dapoxetine in patients with severe renal impairment was approximately 2 times higher than in patients with normal renal function. Data on the use of the drug in patients with severe renal impairment are limited. The pharmacokinetics of dapoxetine have not been studied in patients requiring hemodialysis.

In patients with impaired liver function

In patients with mild hepatic insufficiency, the Cmax of unbound dapoxetine decreased by 28%, and the AUC did not change. Cmax and AUC of the active fraction (the sum of unbound fractions of dapoxetine and desmethyldapoxetine) decreased by 30% and 5%, respectively. In patients with moderate hepatic insufficiency, the cmax of unbound dapoxetine usually does not change (decreases within 3%), the AUC increases by 66%. The cmax of the unbound active fraction of dapoxetine was unchanged, and the AUC was increased by 2 times.

In patients with severe hepatic insufficiency, the cmax of unbound dapoxetine was reduced by 42%, and the AUC of unbound dapoxetine was increased by approximately 223%. The cmax and AUC of the active fraction changed similarly.

CYP2D6 polymorphism

The concentration of dapoxetine in blood plasma after a single dose of Dapoxetine-SZ at a dose of 60 mg in patients with low CYP2D6 activity was higher than in patients with high CYP2D6 activity (Cmax by about 31%, AUC_{0 –∞} – about 36%). Similarly, the cmax of desmethyldapoxetine in patients with low CYP2D6 activity was increased by 98%, and the AUC_{of 0 –∞} was increased by 161%. The cmax of the active fraction of Dapoxetine-SZ was increased by about 46%, and the AUC was increased by about 90%. This increase may be accompanied by an increased frequency and severity of dose-dependent adverse events. When using Dapoxetine-SZ in patients with low CYP2D6 activity, special attention should be paid to the safety of concomitant use of other drugs that may inhibit dapoxetine metabolism, such as moderate-acting CYP3A4 inhibitors and strong CYP3A4 inhibitors.

Indications

The drug Dapoxetine-SZ is intended for the treatment of premature ejaculation in men aged 18 to 64 years.

Dapoxetine-SZ can only be used in patients who meet the following criteria: :

• intravaginal ejaculation delay time (IVSE) < 2 minutes;
• permanently or recurrent ejaculation with minimal sexual stimulation before, during, or shortly after sexual penetration, and the coming sooner desired by the patient;and
• expressed personal distress or difficulties in interpersonal relationships due to premature ejaculation;
• poor control of ejaculation;
• the onset of premature ejaculation in the majority of attempts at sexual intercourse in the last 6 months.

The drug Dapoxetine-SZ should be used only in the mode of reception as needed before the intended sexual activity. The drug Dapoxetine-SZ should not be used to delay ejaculation in men who do not have a confirmed diagnosis of premature ejaculation.

Use during pregnancy and lactation

The drug Dapoxetine-SZ is not intended for use in women. Animal studies have not shown any direct or indirect negative effects on fertility, pregnancy, or embryo/ fetus development.

Contraindications

-Hypersensitivity to dapoxetine and / or to any auxiliary substance in the preparation.

– Severe heart diseases (for example, NYHA Class II-IV chronic heart failure, cardiac conduction disorders (atrioventricular conduction block or sinus node weakness syndrome); diagnosed coronary heart disease; heart valve diseases.

– Concomitant usSimilarly, these medications should not be taken within 7 days of discontinuation of dapoxetine.

Drugs acting on the central nervous system

The use of dapoxetine concomitantly with drugs acting on the central nervous system (for example, antiepileptic drugs, antidepressants, neuroleptics, anxiolytics, sedative hypnotics) in patients with premature ejaculation has not been studied. Therefore, it is recommended to exercise caution if the simultaneous use of these drugs is necessary.

Effect of other drugs on the pharmacokinetics of dapoxetine

Studies using human liver, kidney, and intestinal microsomes in vitro have shown that dapoxetine is primarily metabolized by CYP2D6, CYP3A4, and flavin-containing monooxygenase 1 (FM 01). Therefore, inhibitors of these enzymes can reduce the clearance of dapoxetine.

CYP3A4 Inhibitors

Strong CYP3A4 inhibitors

Ketoconazole 200 mg twice daily for 7 days increased the Cmax and AUC_{of 0 –∞} dapoxetine (60 mg once) by 35% and 99%, respectively. Taking into account the proportion of unbound dapoxetine and desmethyldapoxetine, the Cmax of the active fraction (the sum of unbound dapoxetine and desmethyldapoxetine) in the presence of strong CYP3A4 inhibitors can increase by about 25%, and the AUC can double. This increase in the Cmax and AUC of the active fraction can be significantly more pronounced in a subpopulation of patients who do not have a functionally active CYP2D6 enzyme, for example, in weak CYP2D6 metabolizers, as well as when taking strong CYP2D6 inhibitors at the same time.

Thus, the use of dapoxetine concomitantly with strong CYP3A4 inhibitors, for example, ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nelfinavir and atazanavir is contraindicated.

Moderate CYP 3A 4 inhibitors

Concomitant use with moderate-acting CYP3A4 inhibitors, such as erythromycin, clarithromycin, fluconazole, amprenavir, fosamprenavir, aprepitant, verapamil, or diltiazem, may significantly increase the degree of systemic exposure to dapoxetine and desmethyldapoxetine, especially in patients with low CYP2D6 activity. These two measures apply to all patients, except for those who, according to the results of geno-or phenotyping, were assigned to the group of active metabolizers of CYP2D6. Patients who belong to the group of active metabolizers of CYP2D6, with the simultaneous use of dapoxetine and a strong inhibitor of CYP3A4, a maximum dose of 30 mg is recommended. They should exercise caution when concomitantly using dapoxetine at a dose of 60 mg and a moderate CYP3A4 inhibitor.

Strong inhibitors of CYP2D6

Fluoxetine 60 mg/day for 7 days increased the Cmax and AUC_{of 0 –∞} dapoxetine (60 mg once) by 50% and 88%, respectively. Taking into account the proportion of unbound dapoxetine and desmethyldapoxetine, the Cmax of the active fraction (the sum of unbound dapoxetine and desmethyldapoxetine) in the presence of strong CYP2D6 inhibitors can increase by about 50%, and the AUC can double. This increase in Cmax and AUC of the active fraction is close to what is expected in patients with low CYP2D6 activity and may lead to an increase in the frequency and severity of dose-dependent adverse reactions. Therefore, caution is recommended when increasing the dose of dapoxetine to 60 mg in patients receiving active CYP2D6 inhibitors and in patients with low CYP2D6 activity.

Phosphodiesterase 5 (PDE5)inhibitors

A cross-sectional single-dose study examined the pharmacokinetics of dapoxetine taken at a dose of 60 mg concomitantly with tadalafil (20 mg) or sildenafil (100 mg). Tadalafil did not affect the pharmacokinetics of dapoxetine. Sildenafil caused small changes in the pharmacokinetics of dapoxetine: an increase in AUC_{0– ∞} and Cmax (by 22% and 4%, respectively), which is considered clinically insignificant. Dapoxetine should be used with caution in patients taking PDE5 inhibitors due to the potentially reduced tolerability of orthostatic hypotension. Concomitant use of dapoxetine with PDE5 inhibitors may lead to orthostatic hypotension. The efficacy and safety of dapoxetine in patients with premature ejaculation and erectile dysfunction, while taking dapoxetine and PDE5 inhibitors, have not been studied.

Effect of dapoxetine on concomitant medications

Tamsulosin

Single and repeated use of dapoxetine at doses of 30 mg and 60 mg to patients receiving tamsulosin daily did not lead to a change in the pharmacokinetics of the latter. At the same time, the frequency of orthostatic hypotension also did not change, which was the same when taking tamsulosin alone and in combination with tamsulosin with dapoxetine 30 mg or 60 mg. Dapoxetine should be used with caution in patients taking alpha-blockers because of their potentially reduced tolerance to orthostatic hypotension.

Drugs metabolized by CYP2D6

Multiple doses of dapoxetine (60 mg / day for 6 days) increased the Cmax and AUC_{of 0-∞} desipramine (50 mg once) by 11% and 19%, respectively, compared to desipramine alone. Dapoxetine can similarly increase the plasma concentrations of other drugs metabolized by CYP2D6. The clinical significance of this is likely small.

Drugs metabolized by CYP3A

Repeated use of dapoxetine (60 mg / day for 6 days) reduced the AUC_{of 0-∞} midazolam (8 mg once) by approximately 20% (range from -60% to +18%). The clinical significance of this phenomenon in most patients is probably low. However, an increase in CYP3A activity may have clinical significance in some patients who are simultaneously taking drugs that are mainly metabolized by CYP3A and have a narrow therapeutic index.

Drugs metabolized by CYP2C19

Repeated use of dapoxetine (60 mg / day for 6 days) did not lead to inhibition of omeprazole metabolism (40 mg once). Dapoxetine is unlikely to affect the pharmacokinetics of other CYP2C19 substrates.

Drugs metabolized by CYP 2C9

Repeated use of dapoxetine (60 mg / day for 6 days) did not affect the pharmacokinetics and pharmacodynamics of glibenclamide (5 mg once). Dapoxetine is not expected to affect the pharmacokinetics of other CYP2C9 substrates.

Warfarin and drugs that inhibit blood clotting and / or platelet function.

There are no data on the effects of long-term use of warfarin simultaneously with dapoxetine. Caution is recommended when prescribing dapoxetine to patients taking warfarin for a long time. In the pharmacokinetic study, multiple doses of dapoxetine (60 mg/day for 6 days) did not affect the pharmacokinetics and pharmacodynamics (PV and INR) of warfarin (25 mg once). There have been cases of abnormal bleeding when used concomitantly with SSRIs.

Ethanol

A single dose of ethanol (0.5 g / kg or approximately 2 doses) did not affect the pharmacokinetics of dapoxetine (60 mg once) and vice versa. However, concomitant use of dapoxetine and ethanol increases drowsiness and significantly reduces alertness in patients ‘ own assessment. Pharmacodynamic measurements of cognitive impairment (digital attention speed test, digital character replacement test) also revealed the presence of an additive effect with simultaneous use of dapoxetine and ethanol. Concomitant use of ethanol and dapoxetine increases the frequency and severity of such adverse reactions as dizziness, drowsiness, slow reflexes, and changes in judgment. It can also increase neurocardiogenic adverse reactions, such as the frequency of syncope, which increases the risk of accidental injury. Therefore, patients should be advised to refrain from taking alcohol during treatment with dapoxetine.

How to take, course of use and dosage

Inside. The tablet should be swallowed whole, washed down with at least one full glass of water. The drug Dapoxetine-SZ can be taken regardless of food intake.

Do not start taking the drug with a dose of 60 mg

Adult males from 18 to 64 lt

The recommended starting dose for all men is 30 mg; this dose is taken 1-3 hours before the intended sexual intercourse. If the 30 mg dose is insufficiently effective and well tolerated (there are no moderate or severe adverse reactions or prodromal symptoms that may precede syncope), the dose can be increased to the maximum recommended 60 mg taken 1-3 hours before sexual intercourse. The frequency and severity of adverse reactions increases when taking the drug at a dose of 60 mg.

Patients who receive Dapoxetine-SZ at a dose of 30 mg accompanied by symptoms of orthostatic hypotension should not increase the dose of the drug to 60 mg. The drug should be taken no more than once a day. The maximum daily dose with good tolerability is 60 mg.

A doctor who prescribes Dapoxetine-SZ for the treatment of premature ejaculation should evaluate the risk and benefit of using the drug after the first 4 weeks of treatment or at least after taking the first 6 doses and determine the risk-benefit ratio to decide whether further treatment with Dapoxetine-SZ is appropriate.

Data on the efficacy and safety of dapoxetine for more than 24 weeks are limited.The clinical need for continuation of therapy and the benefit / risk ratio of Dapoxetine-SZ should be evaluated at least every 6 months.

Patients with impaired renal function

For patients with mild or moderate renal insufficiency, no dose adjustment is required, but caution is recommended. The drug Dapoxetine-SZ is not recommended for patients with severe renal insufficiency.

Patients with impaired liver function

Dapoxetine-SZ is contraindicated in patients with moderate to severe hepatic insufficiency (Child-Pugh class B and C).

Elderly patients (65 years and older)

The efficacy and safety of dapoxetine in patients 65 years and older have not been established.

Patientswith low CYP 2D6 isoenzymeactivity and patients taking concomitant CYP2d6 signal inhibitors

Caution should be exercised when increasing the dose of Dapoxetine-SZ to 60 mg in patients with low activity of the CYP2D6 isoenzyme or in patients taking Dapoxetine-SZ simultaneously with strong inhibitors of the CYP2D6 isoenzyme.

Patients receiving strong or moderately active inhibitors of the CYP3A4 isoenzyme

Concomitant use of Dapoxetine-SZ with strong inhibitors of the CYP3A4 isoenzyme is contraindicated. When Dapoxetine-SZ is co-administered with moderately active inhibitors of the CYP3A4 isoenzyme, the dose of the drug should be reduced to 30 mg, and caution should also be exercised.

Overdose

Cases of overdose are not described.

Taking dapoxetine in a dose of up to 240 mg (2 doses of 120 mg with an interval of 3 hours) it did not cause any unexpected adverse reactions. In general, symptoms of SSRI overdose include serotonergic reactions, including drowsiness, gastrointestinal disorders (nausea, vomiting), tachycardia, tremor, agitation, and dizziness.

In case of overdose, standard maintenance therapy should be used, if necessary. Due to the significant binding of the drug to plasma proteins and the large volume of distribution of dapoxetine, forced diuresis, dialysis, hemoperfusion and blood transfusion are unlikely to be effective. The specific antidote is unknown.

Description

Tablets, film-coated from light yellow to yellow in color, round, biconvex. On a cross-section, the tablet core is white or almost white in color.

Special instructions

General information

Dapoxetine can only be used in patients with premature ejaculation who meet the criteria specified in the section “Indications for use”. Dapoxetine should not be used in men who have not been diagnosed with premature ejaculation. The safety of using the drug in men without premature ejaculation has not been established, there are no data on delayed ejaculation.

Use with narcotic drugs

Patients should not take dapoxetine together with narcotic drugs. Concomitant use of dapoxetine with narcotic drugs with serotonergic activity, such as ketamine, methylenedioxymethamphetamine (MDMA), and lysergic acid diethylamide (LSD), can lead to potentially serious reactions, including, but not limited to, arrhythmia, hyperthermia, and serotonin syndrome. Concomitant use of dapoxetine with sedatives, such as opiates or benzodiazepines, may increase drowsiness and dizziness.

Application with ethanol

Concomitant use of dapoxetine with alcohol may increase its effects on the central nervous system, and may also increase neurocardiogenic adverse reactions such as syncope, thus increasing the risk of accidental injury. Therefore, patients should be advised to refrain from taking alcohol while taking dapoxetine.

Fainting

Patients should avoid potentially traumatic situations, in particular driving vehicles or mechanisms, in the event of syncope or its prodromal symptoms, such as dizziness or pre-syncope (see the section “Side effects”). Patients treated with dapoxetine were more likely to have prodromal symptoms, including nausea, dizziness/ fainting, and increased sweating, compared to patients treated with placebo.

The cases of syncope observed in clinical trials, characterized as loss of consciousness, with bradycardia or sinus node arrest in patients with Holter monitoring, were attributed to vasovagal origin, and most of them occurred within the first 3 hours after use, after the first dose, or were associated with medical procedures (blood sampling, changes in body position, blood pressure measurement). Possible prodromal symptoms, such as nausea, dizziness, pre-syncope, palpitations, asthenia, confusion and increased sweating, were also usually observed in the first 3 hours after taking the drug and often preceded syncope. Patients should be informed that syncope with or without prodromal symptoms may occur at any time during dapoxetine treatment. The doctor should inform the patient about the importance of sufficient water load and about recognizing prodromal signs and symptoms to reduce the risk of serious injury in the event of a possible fall due to unconsciousness. If possible prodromal symptoms appear, the patient should immediately lie down so that the head is lower than the torso, or sit with the head between the knees and remain in this position until the symptoms disappear. In case of syncope or other adverse reactions from the central nervous system, the patient should be warned about the need to avoid potentially traumatic situations, including driving a car and other mechanisms.

Patients at risk of heart disease

Patients with cardiovascular diseases were not included in clinical trials of dapoxetine. Patients with organic diseases of the heart and blood vessels (for example, obstruction of the ejection of blood from the heart, damage to the valvular apparatus, carotid artery stenosis, coronary artery atherosclerosis) have an increased risk of undesirable cardiovascular consequences of syncope of cardiac and other origin. However, there is currently insufficient data to determine whether this risk extends to vasovagal syncope in patients with cardiovascular disease.

Orthostatic hypotension

Before starting therapy, the doctor should conduct a thorough medical examination, including finding out the history of orthostatic events, as well as an orthostatic test (measuring blood pressure and heart rate in a sitting or standing position). In case of confirmed or suspected orthostatic reactions in the anamnesis, dapoxetine therapy should be avoided.

Cases of orthostatic hypotension have been reported in clinical studies. The doctor should inform the patient in advance that if possible prodromal symptoms, such as dizziness, appear immediately after getting up, you should immediately lie down so that your head is lower than your torso, or sit with your head between your knees and remain in this position until the symptoms disappear. In addition, the patient should be informed about the need to avoid getting up abruptly after lying down or sitting for a long time.

Moderate CYP 3A 4 inhibitors

Caution should be exercised when using dapoxetine concomitantly with moderate CYP3A4 inhibitors (erythromycin, clarithromycin, fluconazole, amprenavir, fosamprenavir, aprepitant, verapamil, diltiazem), and the dose of the drug should be reduced to 30 mg.

Strong CYP2D6 inhibitors

Caution is recommended when increasing the dose of dapoxetine to 60 mg in patients receiving strong CYP2D6 inhibitors and in patients with low CYP2D6 activity, as this may increase the level of systemic exposure to the drug with a corresponding increase in the frequency and severity of dose-dependent adverse reactions.

Suicide/ suicidal thoughts

In short-term studies, antidepressants, including SSRIs, compared with placebo significantly increased the risk of suicidal thoughts and suicidality in children and adolescents with major depressive disorder and other psychiatric disorders. In short-term studies, there was no increased risk of suicidality when taking antidepressants compared to placebo in adults over 24 years of age. In clinical trials of dapoxetine for the treatment of premature ejaculation, there were no clear data on the occurrence of suicidal thoughts during treatment, evaluated using the Columbia Classification Algorithm for Suicide Assessment (C-CASA), the Montgomery-Asberg Depression Rating Scale, or the Beck Depression Questionnaire.

Mania

Dapoxetine should not be used in patients with a history of mania / hypomania or bipolar disorder, and if symptoms of these diseases appear, the drug should be discontinued.

Convulsions

Due to the ability of SSRIs to lower the seizure threshold, dapoxetine should be avoided in patients with unstable epilepsy, and the drug should be discontinued if seizures occur. Patients with controlled epilepsy should be closely monitored.

Admission for children and adolescents under 18 years of age

The use of dapoxetine in patients younger than 18 years and older than 65 years is contraindicated, as there are no clinical data on the efficacy and safety of dapoxetine in these patient populations.

Concomitant depression and / or psychiatric disorders

If the patient has signs and symptoms of depression before starting the use of dapoxetine, it is necessary to conduct an examination to exclude the presence of undiagnosed depressive disorder. Dapoxetine should not be taken concomitantly with antidepressants, including SSRIs and serotonin and norepinephrine reuptake inhibitors. It is not recommended to stop treatment for depression or anxiety before starting treatment with dapoxetine. Dapoxetine is not intended for the treatment of psychiatric disorders (for example, schizophrenia or depression), and it should not be taken by men with these diseases, since this cannot exclude an increase in the symptoms of depression. You should immediately inform your doctor of any disturbing thoughts or feelings, and if signs and symptoms of depression appear during treatment, dapoxetine should be discontinued.

Bleeding

Cases of bleeding have been reported with SSRIs. Caution is recommended when taking dapoxetine concomitantly with medications that affect platelet function (for example, atypical antipsychotics, phenothiazines, acetylsalicylic acid, nonsteroidal anti-inflammatory drugs (NSAIDs), anticoagulants (for example, warfarin)), as well as in patients with a history of bleeding or clotting disorders.

Impaired renal function

Dapoxetine is not recommended for patients with severe renal insufficiency, and caution should be exercised in patients with mild or moderate renal insufficiency.

Withdrawal syndrome

There is evidence that abrupt discontinuation of long-term SSRIs used to treat chronic depressive disorders leads to the following symptoms: decreased mood, irritability, agitation, dizziness, sensitivity disorders (for example, paresthesia in the form of electric shock), anxiety, confusion, headache, drowsiness, emotional instability, insomnia, hypomania.

In a clinical study conducted to evaluate the effect of “withdrawal” of dapoxetine after 60 days of taking a dose of 60 mg daily in patients with premature ejaculation, no signs of “withdrawal”syndrome were found. After switching patients to placebo, only minor withdrawal symptoms were observed after daily dapoxetine use, in the form of mild to moderate insomnia and dizziness.

Other types of sexual dysfunction

Patients with other types of sexual disorders, including erectile dysfunction, should be carefully evaluated by a doctor before starting treatment. Dapoxetine should not be used in patients with erectile dysfunction receiving PDE5 inhibitors.

Medicinal products with vasodilating properties

Dapoxetine should be used with caution in patients taking medications with vasodilating properties (such as alpha-blockers and nitrates) due to the possible decrease in orthostatic tolerance.

Visual disturbances

Against the background of the use of dapoxetine, such undesirable reactions from the visual organ as mydriasis and pain in the eyes were noted. Dapoxetine should be used with caution in patients with elevated intraocular pressure or at risk of developing angle-closure glaucoma.

Influence on the ability to drive vehicles and mechanisms

Dapoxetine has a minor or moderate effect on the ability to drive vehicles and maintain mechanisms. When taking dapoxetine, cases of dizziness, impaired attention, fainting, blurred vision, drowsiness are described. The patient should be warned to avoid situations where injury may occur, including driving vehicles and maintaining machinery. Concomitant use of alcohol and dapoxetine may increase alcohol-related neurocognitive effects and may also increase the risk of neurocardiogenic adverse reactions such as syncope, which in turn increases the risk of injury. Therefore, patients should be advised to avoid concomit Formic acid spiritus consumption when using Dapoxetine-SZ.

Form of production

Film-coated tablets,30 mg and 60 mg

4,6,8,10 tablets in cell contour packages.

20 tablets each in polymer cans of the BP type made of low-pressure polyethylene with lids made of high-pressure polyethylene or in polymer bottles made of low-pressure polyethylene with lids made of high-pressure polyethylene.

Each jar, bottle,1 cell contour package of 4,6,8,10 tablets, or 2 cell contour packages of 6 tablets, or 2,3 cell contour packages of 10 tablets, together with the instructions for use, is placed in a cardboard pack.

Storage conditions

In a place protected from light, at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Dapoxetine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets