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ANDOPOKSETİN (Andropoxetine)

tablets

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ANDOPOXETINE      30 mg; 60 mg coated tablets

ANDOPOXETINE

International non-patented name: Dapoxetine

 

Composition

Active substance: 1 tablet contains 30 mg or 60 mg of dapoxetine (dapoxetine hydrochloride

in the picture).

Excipients: lactose monohydrate (dried spray), microcrystalline cellulose (Avisel

PH 102), croscarmellose sodium, colloidal silicon dioxide, magnesium

stearate.

Cover:                 30 mg- hydroxypropylmethylcellulose E5, polyethylene glycol 6000,

titanium dioxide, edicol, quinoline yellow (47005).

60 mg – hydroxypropylmethylcellulose E15, polyethylene glycol 6000,

titanium dioxide.

 

Description

The 30 mg film-coated tablets are yellow, round-coated tablets, embossed on one side with the lowercase letter "a" on both sides.

60 mg film-coated tablets are white round film-coated tablets, engraved with a small letter "a" on one side and slightly raised on both sides.

 

Pharmacotherapeutic group

Urological remedy.

ATC code:G04BX14.

pharmacological properties

Pharmacodynamics

 Dapoxetine is a potent selective serotonin reuptake inhibitor (SRI) with an IC50 of 1.12 nM, while its main metabolites desmethyldapoxetine (IC50 < 1.0 nM) and didemethyldapoxetine (IC50 = 2, 0 nM) are equivalent or less potent (dapoxetine-N-oxide (IC50 = 282 nM)). The ejaculatory pathways initially originate from the spinal cord reflex center through the influence of nuclei in the brain (medial preoptic and paraventricular nuclei) on the brainstem. The mechanism of action of dapoxetine during early ejaculation is related to the inhibition of neuronal reuptake of serotonin as a result of the increased effect of neurotransmitters on pre- and postsynaptic receptors. 

Pharmacokinetics

Being asked

Dapoxetine is rapidly absorbed and has maximum plasma concentrations (Cmax) approximately 1-2 hours after taking the tablets. Absolute bioavailability is 42% (range 15-76%). After a single oral administration of dapoxetine in doses of 30 mg and 60 mg on an empty stomach, the maximum concentrations were 297 ng/ml and 498 ng/ml, respectively. After multiple dosing, AUCs for both dapoxetine and the active metabolite desmethyldapoxetine (DED) were increased by approximately 50% compared to single dose AUCs.

Eating fatty foods moderately decreases dapoxetine Cmax (10%) and increases AUC (12%) and slightly delays the maximum plasma concentration of dapoxetine.

These changes are not clinically significant. Andopoxetine can be taken with or without food.

Distribution

More than 99% of dapoxetine is bound to human plasma proteins in vitro. Desmethyldapoxetine (DED), the active metabolite, is 98.5% protein bound. The average steady-state volume of distribution of dapoxetine is 162 L.

Biotransformation:

In vitro studies show that dapoxetine is metabolized by multiple hepatic and renal enzymes, mainly CYP2D6, CYP3A4, and flavin monooxygenase (FMO1). In clinical studies studying the metabolism of 14C-dapoxetine, it has been shown that after oral administration, dapoxetine is metabolized to numerous metabolites mainly by the following biotransformation pathways: N-oxidation, N-dimethylation, hydroxylation of naphthyl groups, glucuronidation and sulfuration. After oral administration, the first signs of presystemic metabolism were observed in the liver.

Intact dapoxetine and dapoxetine-N-oxide are the major components circulating in plasma. Dapoxetine-N-oxide has been shown to be inactive in in vitro studies. Additional metabolites such as desmethyldapoxetine and didesmethyldapoxetine account for less than 3% of the total circulating drug-related substances in plasma. Dismethyldapoxetine has been shown to be comparable in activity to dapoxetine in in vitro studies, and dismethyldapoxetine has 50% the potency (activity) of dapoxetine. The unconjugated AUC and Cmax of dapoxetine are approximately 50% and 23%, respectively.

Elimination

Metabolites of dapoxetine are mainly excreted in urine in the form of conjugates.   Unchanged active substance was not detected in urine. After oral administration, the initial (disposition) half-life of dapoxetine is approximately 1.5 hours, with a maximum concentration of less than 5% in a 24-hour period, and the terminal half-life is approximately 19 hours. The terminal half-life of desmethyldapoxetine is approximately 19 hours.

Pharmacokinetics in a special population

Metabolites of desmethyldapoxetine have pharmacological effects of Andopoxetine, especially if its effects are increased. The elevation of active fraction parameters for some populations is shown below. This is the sum of exposure to unconjugated dapoxetine and desmethyldapoxetine. Dismethyldapoxetine is comparable in activity to dapoxetine. Dismethyldapoxetine is estimated to be evenly distributed throughout the CNS, but it is not known whether this is the case.

Races

A single dose of 60 mg of dapoxetine in Caucasians, Europeans, representatives of the Negroid race, Latin Americans and people of Asian race did not reveal a precise  statistical indicator. Dapoksetinin farmakokinetikasının avropalılar və  yaponlar arasındakı müqayisəsi, ikincidə  bədən  çəkisinin  az_cc781905-5cde-3194-bb3b -136bad5cf58d_ olması  ilə  əlaqədar (10-20%) Cmax və AUC  daha  yüksək_cc781905-5cde -3194-bb3b-136bad5cf58d_ reported difference .

A higher level of systemic exposure is unlikely to yield a significant clinical effect difference .

Seniors (age group 65 years and above):

During the analysis of clinical pharmacology studies of a single dose of 60 mg of dapoxetine, it was shown that there were no significant differences in pharmacokinetic parameters (Cmax), (AUCinf ), (Tmax) between healthy elderly men and healthy young men. The effectiveness or safety of the use of the drug in this age group has not been studied

Kidney failure

An increase in the AUC of Dapoxetine was not observed with a decrease in renal function. Although there are limited data on acute kidney injury, AUC was approximately 2-fold higher in patients with acute kidney injury compared to patients with normal renal function.

The pharmacokinetics of dapoxetine have not been evaluated in patients requiring renal dialysis

Liver failure

In patients with mild hepatic impairment, the unconjugated Cmax of dapoxetine was reduced by 28% and the unconjugated AUC was unchanged. The unbound Cmax and AUC of the active fraction (the sum of unbound dapoxetine and desmethyldapoxetine) decreased by 30% and 5%, respectively. In patients with moderate hepatic insufficiency, the unbound Cmax of dapoxetine was not significantly changed (3% decrease) and the unbound AUC was increased by 66%. The unbound Cmax of the active fraction did not change to a clinically significant extent, and the AUC doubled. In patients with severe hepatic impairment, the unbound Cmax-I of dapoxetine decreased by 42% and the unbound AUC increased by approximately 223%. Similar changes in Cmax and AUC of the active fraction were noted

CYP2D6 Polymorphism

In clinical pharmacology studies of a single dose of 60 mg dapoxetine, plasma concentrations were higher in poor CYP2D6 metabolizers than in active CYP2D6 metabolizers (approximately 31% higher for dapoxetine Cmax and 36% higher for AUCinf and 98% higher for desmethyldapoxetine Cmax and 161% higher for AUCinf). The active fraction of dapoxetine can increase Cmax by about 46% and AUC by about 90%. These increases may result in increased frequency and severity of dose-related side effects. The safety of dapoxetine may be questionable in patients with poor CYP2D6 metabolisers when co-administered with other drugs, such as moderate and potent CYP3A4 inhibitors, which may inhibit the metabolism of dapoxetine.

 

Instructions for use

Andopoxetine is indicated for the treatment of premature ejaculation (PE) (premature ejaculation) in adult men aged 18 to 64 years.

Andopoxetine should only be prescribed to patients who meet all of the following criteria:

  • If the intravaginal ejaculatory latency period (IELM) is less than two minutes;

  • Ejaculation that continues or returns during minimal sexual stimulation before, during, and shortly after penetration, and before the patient's desire.

  • Personal distress or interpersonal difficulties identified as a result of premature ejaculation.

  • Poor control over ejaculation

  • Premature ejaculation often starts 6 months before sexual intercourse.

Andopoxetine should not be prescribed to delay ejaculation in men who have not been diagnosed with premature ejaculation.

 

Contraindications

The use of the drug is contraindicated in cases of hypersensitivity to any of its ingredients.

Known pathological heart diseases mentioned below:

  • Heart failure (NYHA class II-IV heart failure)

  • Cardiac conduction disorders such as atrioventricular block or sinus node weakness syndrome

  • Ischemic heart disease

  • Valvular heart disease (diseases of the heart valves)

  • Those with a history of fainting.

  • Cases of mania or severe depression.

Use of the drug together with monoamine oxidase inhibitors (MAOIs) or within 14 days after stopping treatment with monoamine oxidase inhibitors (MAOIs) is contraindicated. At the same time, monoamine oxidase inhibitors (MAOIs) should not be used for 7 days after stopping Andopoxetine.

Use of the drug together with thioridazine, or within 14 days after stopping treatment with thioridazine, is contraindicated. At the same time, thioridazine should not be used for 7 days after stopping Andopoxetine.

Serotonin reuptake inhibitors [selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SSRIs), tricyclic antidepressants (TSA)] or other drugs/herbals with serotonergic effects [eg, L-tryptophan, triptans, Concomitant treatment with tramadol, linezolid, lithium, preparations containing St. John's wort (Hypericum perforatum)] or within 14 days of stopping treatment with these drugs/herbal preparations is contraindicated. Also, these drugs/herbals should not be used for 7 days after stopping Andopoxetine.

Ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazadone, nelfinavir, atazanavir, etc. simultaneous treatment with potent CYP3A4 inhibitors.

Moderate or severe hepatic insufficiency.

 

Special instructions and precautions

General recommendations

Andopoxetine is only indicated for use in patients with premature ejaculation.

Andopoxetine should not be prescribed to patients who have not been diagnosed with premature ejaculation. The safety of the use of the drug in patients with undetermined premature ejaculation has not been studied, and there is no data on the effects of delaying ejaculation.

Other forms of sexual dysfunctions:

Before starting treatment, people with other sexual dysfunctions, including erectile dysfunction, should be carefully examined by their doctors.

Andopoxetine should not be used in men with erectile dysfunction (ED) who are using PDE5 inhibitors

Orthostatic hypotension

Before starting the treatment, the doctor should carry out an accurate medical examination of the patient, including orthostatic conditions. Orthostatic test should be performed before starting treatment with the drug (blood pressure and pulse rate, lying or standing). The use of andopoxetine should be avoided in patients with a history of orthostatic reactions or who are subject to orthostatic reactions.

The prescriber should advise the patient in advance to lie down and keep the head lower than the rest of the body or sit with the head between the knees until the symptoms resolve if they experience possible prodromal conditions such as lightheadedness after standing up. The prescriber should advise the patient not to get up quickly after prolonged lying or sitting.

Suicide/suicidal thoughts

Antidepressants, including selective serotonin reuptake inhibitors, have been shown to increase the risk of suicidal ideation and suicidality in children and adolescents with major depressive disorder and other psychiatric disorders compared to a placebo group in short-term studies. In short-term studies, there was no increased risk of suicide with antidepressants compared with placebo in adults over 24 years of age.

syncope (fainting)

Because of the possibility of syncope or its prodromal symptoms, such as dizziness or headache, patients should be cautioned to avoid situations where injury may occur, including driving or operating hazardous vehicles.

Possible prodromal symptoms such as nausea, dizziness/lightheadedness, and diaphoresis were reported more frequently in dapoxetine-treated patients compared to placebo.

Patients should be advised that syncope may occur at any time during Andopoxetine treatment, regardless of the presence or absence of prodromal symptoms. Prescribers should educate patients about the importance of maintaining adequate hydration and how to recognize prodromal signs and symptoms of loss of consciousness to reduce serious injury. If the patient experiences possible prodromal symptoms, they should be advised to lie down immediately and keep the head lower than other parts of the body or to sit with the head between the knees until the symptoms resolve, and also if the patient is experiencing syncope or other central nervous system symptoms. they should be warned to avoid activities that could result in injury, including driving or operating dangerous machinery because of the possibility of adverse effects.

Patients with cardiovascular risk factors

Patients with structural cardiovascular disease (eg, patients with established outflow obstruction, valvular heart disease, carotid artery stenosis, and coronary artery disease) are at increased risk of cardiovascular adverse effects as a result of syncope (cardiac syncope and syncope from other causes). . There are insufficient data to determine whether these increased risks extend to vasovagal syncope in patients with cardiovascular disease.

Use together with drugs that have serotoninergic effects

Patients should be advised not to use Andopoxetine in combination with drugs that have serotonergic effects.

The combined use of Andopoxetine with drugs that have serotoninergic activity, such as ketamine, methylenedioxymethamphetamine (MDMA), and lysergic acid diethylamide (LSD), can lead to potentially serious reactions. These reactions include, but are not limited to, arrhythmia, hyperthermia, and serotonin syndrome. Concomitant use of Andopoxetine with drugs that have sedative properties, such as narcotics and benzodiazepines, may further increase drowsiness and dizziness.

Ethanol

Patients should be advised not to use Andopoxetine at the same time as alcohol.

The combination of alcohol with dapoxetine may increase alcohol-related neurocognitive effects and also potentiate neurocardiogenic side effects such as syncope, which in turn increases the risk of accidental injury; therefore, patients should be advised not to consume alcohol while using andopoxetine

Medicinal preparations with vasodilation properties

Andopoxetine should be prescribed with caution to patients treated with drugs with vasodilator properties (alpha-adrenergic receptor antagonists and nitrates) due to possible reduction of orthostatic tolerance.

CYP3A4 inhibitors with moderate activity

Patients receiving moderate CYP3A4 inhibitors are advised to use the drug with caution and limit the dose to 30 mg.

CYP2D6 inhibitors with strong activity

Caution is recommended when increasing the dose up to 60 mg in patients receiving potent (strong) active CYP2D6 inhibitors or up to 60 mg in patients known to have a CYP2D6 genotype with weak activity, as in this case, as a result of increased effects of the drugs at higher levels, the frequency and severity of dose-dependent adverse effects are likely to increase

Mania

Andopoxetine should not be used in patients with established mania/hypomania or bipolar disorders, and the drug should be discontinued in any patient who develops symptoms of these disorders.

Seizures

Because of the potential of selective serotonin reuptake inhibitors to reduce seizures, andopoxetine should be discontinued in all patients who develop seizures and its use should be avoided in patients with unstable epilepsy. Careful observation is required in treated epilepsy patients.

Depression and/or psychiatric disorders

In order to prevent undiagnosed depressive disorders, individuals with signs and symptoms of depression should be screened before starting treatment with Andopoxetine. Concomitant use of andopoxetine with antidepressants, including selective serotonin reuptake inhibitors and serotonin norepinephrine reuptake inhibitors, is contraindicated. It is not recommended to discontinue treatment of ongoing depression or anxiety in order to initiate the use of andopoxetine for the treatment of premature ejaculation (premature ejaculation). Andopoxetine is not indicated for psychiatric disorders and should not be used in individuals with psychiatric disorders such as schizophrenia or existing depression due to worsening of depression-related symptoms. This may be the result of an underlying psychiatric disorder or drug therapy. Physicians should instruct patients to report any thoughts or feelings of stress (anxiety) that may arise at any time, and that Andopoxetine should be discontinued if signs and symptoms of depression develop during treatment.

Hemorrhage

Bleeding pathologies have been noted during the use of selective serotonin reuptake inhibitors. [NSAID], antiplatelet drugs) or concomitant use with anticoagulants (e.g. warfarin), as well as caution is advised when used in patients with a history of bleeding or coagulation disorders

Kidney failure

The use of Andopoxetine is not recommended in patients with severe renal impairment, and caution is required when using the drug in patients with mild or moderate renal impairment.

Side effects that may occur during sudden withdrawal from the drug

Abrupt discontinuation of selective serotonin reuptake inhibitors (SSRIs) used long-term in the treatment of chronic depressive disorders has seen the following symptoms: dysphoric states (mood changes), irritability, anxiety, dizziness, sensory disturbances (e.g., paresthesias), agitation, confusion, headache, lethargy, emotional lability, insomnia and hypomania.

Disturbances in the eyes

The use of andopoxetine causes ocular effects such as mydriasis and eye pain. Andopoxetine should be used with caution in patients with elevated intraocular pressure or in patients with established angle-closure glaucoma.

Lactose intolerance

This drug should not be used in patients with rare hereditary problems such as galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.

 

Interaction with other drugs

Pharmacodynamic interactions

Interactions with monoamine oxidase inhibitors:

In patients receiving monoamine oxidase inhibitors (MAOIs) in combination with selective serotonin reuptake inhibitors, hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid changes in vital signs, and hyperexcitability (agitation) progressing to states of wakefulness and coma.   serious and sometimes fatal reactions, including mental status changes, have been reported. These reactions have also been reported in patients who have recently stopped using selective serotonin reuptake inhibitors and started using monamine oxidase inhibitors.

In some cases, symptoms reflecting neuroleptic malignant syndrome have been noted. For this reason, Andopoxetine should not be used in combination with monamine oxidase inhibitors or within 14 days after stopping treatment with monamine oxidase inhibitors. At the same time, monamine oxidase inhibitors (MAOIs) should not be prescribed for 7 days after stopping Andopoxetine

Interactions with thioridazine:

Single administration of thioridazine causes prolongation of the QTc interval, which is accompanied by serious ventricular arrhythmias. Medicines such as Andopoxetine, which inhibit CYP2D6 isoenzymes, inhibit the metabolism of thioridazine  and as a result of the increase in the amount of thioridazine  QTc interval is expected to increase.  

Andopoxetine should not be used concurrently with thioridazine or within 14 days of discontinuation of thioridazine. At the same time, thioridazine should not be prescribed for 7 days after stopping the use of Andopoxetine

Medicinal/herbal preparations with serotoninergic effects

As with other selective serotonin reuptake inhibitors, the drug may interact with serotonergic drugs/herbals (monoamine oxidase inhibitors, L-tryptophan, triptans, tramadol, linezolid, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, lithium, and St. John's wort). (including Hypericum perforatum) preparations) may lead to serotonin-related side effects. Andopoxetine should not be used in combination with other selective serotonin reuptake inhibitors, monoamine oxidase inhibitors, or other serotonergic drugs/herbals, or within 14 days after stopping treatment with these drugs/herbals. At the same time, these drugs/herbal preparations should not be prescribed for 7 days after stopping the use of Andopoxetine.

Medicines affecting the central nervous system

The use of Andopoxetine in combination with drugs affecting the central nervous system (eg, antiepileptics, antidepressants, antipsychotics, anxiolytics, sedative hypnotics) in patients with established premature ejaculation has not been systematically evaluated. For this reason, caution is advised when concomitant use of Andopoxetine and such drugs is required.

Pharmacokinetic interactions

Effect of co-administered drugs on the pharmacokinetics of dapoxetine:

In vitro studies in human liver, kidney, and intestinal microsomes indicate that dapoxetine is metabolized primarily by CYP2D6, CYP3A4, and flavin monooxygenase 1 (FMO1). Therefore, inhibitors of these enzymes can reduce the clearance of dapoxetine.

CYP3A4 inhibitors

CYP3A4 inhibitors with potent activity. Administration of ketoconazole (200 mg twice daily for 7 days) increased dapoxetine Cmax by 35% and AUCinf by 99%. Taking into account the ratio of unconjugated dapoxetine and desmethyldapoxetine, the Cmax of the active fraction can be increased by about 25% and the AUC of the active fraction can be doubled when co-administered with potent CYP3A4 inhibitors.

Cmax and AUC of the active fraction increased in a certain group of population without functional CYP2D6 enzymes, that is, CYP2D6 metabolizers with poor activity or using active CYP2D6 inhibitors in combination.

Therefore, the combined use of dapoxetine and potent CYP3A4 inhibitors such as ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nelfinavir, and atazanavir is contraindicated.

Grapefruit juice is also a strong inhibitor of the CYP3A4 isoenzyme. For this reason, grapefruit juice should not be drunk 24 hours before the use of the drug.

CYP3A4 inhibitors with moderate activity

Concomitant treatment with moderately active CYP3A4 inhibitors (eg, erythromycin, clarithromycin, fluconazole, amprenavir, fosamprenavir, aprepitant, verapamil, diltiazem) may lead to clinically significant increases in the amount of dapoxetine and desmethyldapoxetine, especially in poor CYP2D6 metabolizers._cc781905- 5cde-3194-bb3b-136bad5cf58d_ When co-administered with these drugs, the maximum dose of Dapoxetine to be used should be 30 mg. These two indications apply to all patients unless the patient is genotyped or phenotypically confirmed to have active CYP2D6 metabolizers. In patients who are active CYP2D6 metabolizers, the maximum recommended dose of dapoxetine when used in combination with an active CYP3A4 inhibitor is 30 mg, and caution is advised when using dapoxetine at a dose of 60 mg with a moderate CYP3A4 inhibitor._cc781905-5cde-3194-bb3b- 136bad5cf58d_

Active CYP2D6 inhibitors

Cmax and AUC of dapoxetine (60 mg single dose) increased by 50% and 88%, respectively, when co-administered with fluoxetine (60 mg/day for 7 days). Taking into account the ratio of unconjugated dapoxetine and desmethyldapoxetine, when co-administered with potent CYP2D6 inhibitors, the Cmax of the active fraction may increase by approximately 50% and the AUC of the active fraction may increase twice. Increases in Cmax and AUC of the active fraction are similar to those expected for poor CYP2D6 metabolizers and may result in an increase in the frequency and severity of dose-dependent side effects.

PDE5 inhibitors

Dapoxetine  should not be used in patients using PDE5 inhibitors due to the possibility of decreased orthostatic tolerance. The pharmacokinetics of dapoxetine  (60 mg) administered simultaneously with tadalafil (20 mg) and sildenafil (100 mg) were studied. Tadalafil does not affect the pharmacokinetics of dapoxetine. Sildenafil caused mild changes in the pharmacokinetics of dapoxetine (22% increase in AUC f and 4% increase in Cmax) of no clinical significance.

Concomitant use of dapoxetine with PDE5 inhibitors may result in orthostatic hypotension. Efficacy and safety of dapoxetine in patients with premature ejaculation and erectile dysfunction treated with dapoxetine and PDE5 inhibitors have not been studied.

Effect of Dapoxetine on the Pharmacokinetics of Concomitantly Used Drugs

Tamsulosin

Administration of single or multiple doses of dapoxetine 30 mg or 60 mg in addition to patients receiving a daily dose of tamsulosin did not cause any changes in the pharmacokinetics of tamsulosin. The addition of dapoxetine to tamsulosin did not cause changes in the orthostatic profile, and no differences in the orthostatic effects of tamsulosin used alone versus tamsulosin used in combination with dapoxetine 30 or 60 mg were identified; however, Andopoxetine should be prescribed with caution in patients using alpha-adrenergic receptor antagonists  due to possible decreased orthostatic tolerance

Drugs metabolized by CYP3A4:

Multiple doses of dapoxetine (60 mg/day for 6 days) decreased the AUCinf of midazolam (8 mg single dose) by approximately 20% (range -60 to +18%). The clinical significance of the effect on midazolam may be small in most patients. An increase in CYP3A activity may be of clinical significance in some patients treated concomitantly with drugs that are predominantly metabolized by CYP3A and have a narrow therapeutic window.

Drugs metabolized by CYP2C19

Multiple doses of dapoxetine (60 mg/day for 6 days) did not inhibit the metabolism of omeprazole at a single dose of 40 mg. Dapoxetine is unlikely to affect the pharmacokinetics of other CYP2C19 substrates .

Drugs metabolized by CYP2C9

Multiple doses of dapoxetine (60 mg/day for 6 days) did not affect the pharmacokinetics or pharmacodynamics of a single 5 mg dose of glyburide. Dapoxetine is unlikely to affect the pharmacokinetics of other CYP2C9 substrates.

Warfarin and drugs affecting coagulation and/or platelet function

There are no data evaluating the effects of chronic warfarin use on dapoxetine, therefore, caution is advised when using dapoxetine in patients on chronic warfarin use. Multiple doses of dapoxetine (60 mg/day for 6 days) did not affect the pharmacokinetics or pharmacodynamics (PT or INR) of a single 25 mg dose of warfarin.

Bleeding pathologies associated with the use of selective serotonin reuptake inhibitors have been noted 

Ethanol

Concomitant use of ethanol at a single dose of 0.5 g/kg (about 2 drinks) did not affect the pharmacokinetics of dapoxetine (60 mg single dose); however, coadministration of dapoxetine with ethanol increased drowsiness and significantly decreased wakefulness. Pharmacodynamic measures of cognitive impairment have also shown that co-administration of dapoxetine with ethanol causes additive effects. Concomitant use of alcohol and dapoxetine increases the frequency or severity of side effects such as dizziness, drowsiness, impaired reflexes, or altered thoughts. The combined use of dapoxetine with alcohol may increase the alcohol-dependent effects and also potentiate neurocardiogenic side effects such as syncope, and as a result, the risks of accidental injury may increase; therefore, patients should be advised to avoid alcohol while taking andopoxetine

 

Use during pregnancy and lactation

Andopoxetine is not indicated for use in women.

It is not known whether dapoxetine or its metabolites pass into breast milk.

 

Use in pediatrics

Andopoxetine should not be used in people under 18 years of age.

 

Effects on the ability to drive vehicles and other potentially dangerous mechanisms

Andopoxetine has a slight or moderate effect on the ability to drive vehicles and other potentially dangerous mechanisms. Dizziness, impaired concentration, syncope (fainting), blurred vision, and drowsiness have been reported in clinical studies in individuals using dapoxetine. Therefore, patients should be cautioned to avoid activities that may cause injury, including driving or operating dangerous machinery.

Concomitant use of dapoxetine with alcohol may increase alcohol-dependent neurocognitive effects and may also potentiate neurocardiogenic side effects such as syncope, resulting in an increased risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking andopoxetine.

 

Method of use and dosage

Adult men (18 to 64 years old)

The recommended starting dose of the drug for all patients is 30 mg approximately 1-3 hours before sexual activity.

Treatment with andopoxetine should not be initiated at a dose of 60 mg.

Andopoxetine is not intended for daily use. Andopoxetine should only be taken when sexual activity is expected. Andopoxetine should not be used more than once every 24 hours.

If the individual response to a dose of 30 mg of the drug is insufficient and the patient does not experience moderate or severe side effects or prodromal symptoms leading to syncope, the dose can be increased to the maximum recommended 60 mg 1-3 hours before sexual activity. The effects and severity of adverse reactions are higher when using a dose of 60 mg.

In cases of orthostatic reactions during the use of the initial dose, the dose should not be increased to 60 mg.

After the first four weeks of andopoxetine treatment (or after at least 6 doses of treatment), a careful assessment of the individual benefits and risks of andopoxetine should be carried out by the physician to determine whether continued treatment is appropriate.

Data on the efficacy and safety of andopoxetine beyond 24 weeks are limited.

The clinical need and benefit-risk balance of continuing treatment with andopoxetine should be reassessed at least every six months.

Seniors (65 years and older)

The efficacy and safety of Andopoxetine use in patients 65 years of age and older have not been established

Pediatric group

Andopoxetine is not considered suitable for use in this age group in indications for premature ejaculation.

Patients with kidney failure

Caution is recommended when using the drug in patients with mild or moderate renal insufficiency. Andopoxetine is not recommended for patients with severe renal failure

Patients with liver failure

The use of Andopoxetine is contraindicated in patients with moderate and severe hepatic insufficiency (classes B and C according to the Child-Pugh classification).

Patients treated with known CYP2D6 poor metabolizers or potent CYP2D6 inhibitors

Special caution is recommended when increasing the dose to 60 mg in patients with a known CYP2D6 poor metabolizer genotype or concomitantly treated with potent CYP2D6 inhibitors.

Patients treated with moderate or strong CYP3A4 inhibitors:

Concomitant use of strong CYP3A4 inhibitors is contraindicated. In patients treated concurrently with moderate CYP3A4 inhibitors, the dose of the drug should be limited to 30 mg, and caution is recommended.

Applied methods

For oral use. In order not to feel the bitterness of the preparation, the tablets should be swallowed whole. It is recommended to take the tablets with at least one full glass of water.  Andopoxetine can be taken with or without food.

Precautionary measures to be taken before using the drug

Before starting treatment with the drug, see the special instructions and precautions for orthostatic hypotension section.

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Digər xüsusi populyasiyalar:

Potent (güclü) CYP2D6 inhibitorları istifadə edən pasiyentlərdə və ya məlum CYP2D6 zəif metabolit genotipinə malik pasiyentlərdə dozanın 60 mq-a qədər artırılması zamanı ehtiyatlı olmaq tövsiyə olunur

Preparatdan qəfil imtina zamanı yarana biləcək əlavə təsirlər

Xroniki depressiv pozğunluqların müalicəsində uzunmüddətli istifadə olunan serotoninin geriyə tutulmasının selektiv inhibitorlarından qəfil imtina nəticəsində aşağıdakı simptomlar müşahidə edilmişdir: disforik vəziyyətlər, əsəbilik, təşviş, başgicəllənmə, sensor pozuntular (məs, paresteziyalar), həyacan, şüurun qarışması, baş ağrısı, letargiya, emosional labillik, yuxusuzluq və hipomaniya.

Əlavə təsirlərin qeydə alınması

Dərman vasitələrinin istifadəsi zamanı yaranan əlavə təsirlər haqqında məlumatlar Azərbaycan Respublikası Səhiyyə Nazirliyi Analitik Ekspertiza Mərkəzinə verilməlidir (Ünvan: AZ1065, Azərbaycan Respublikası; Bakı şəh., Cəfər Cabbarlı küç., 34.;  Faks: (99412) 596-07-16 ; e-mail: adr@pharma.az; Tel.:(99412)596-05-20 Qaynar xətt (99412) 596-07-12).

Doza həddinin aşılması

Klinik tədqiqatlar zamanı doza həddinin aşılması halları qeyd edilməmişdir.

Gündəlik 240 mq dozaya qədər (iki 120 mq doza 3 saat aralığı ilə) Andopoksetinin istifadəsi əlavə təsirlərə səbəb olmamışdır. Ümumiyyətlə, serotoninin geriyə tutulmasının selektiv inhibiorları ilə doza aşımı simptomlarına yuxululuq, ürəkbulanma və qusma kimi mədə-bağırsaq pozuntuları, taxikardiya, titrəmə, təşviş və başgicəllənmə kimi serotoninergik əlavə təsirlər aiddir.

Doza həddinin aşılması hallarında ehtiyac olduqda standart dəstəkləyici terapiya həyata keçirilməlidir. Dapoksetinin plazma zülalları ilə yüksək səviyyədə birləşməsi və böyük həcmdə paylanması ilə əlaqədar olaraq məcburi diurez, dializlər, hemotransfuziya və dəyişilmiş transfuziya faydalı olmaya bilər. Andopoksetin üçün xüsusi antidotlar məlum deyil.

 

Buraxılıç forması

3 tablet, alüminium/şəffaf olmayan(tünd) PVX/PVDX stripdə. 1 strip, içlik vərəqə ilə birlikdə karton qutuya qablaşdırılır.

 

Saxlanma şəraiti

30°C-dən yüksək olmayan temperaturda, quru  və  uşaqların əli çatmayan yerdə saxlamaq lazımdır.

 

Yararlılıq müddəti

2 il.

Yararlılıq muddəti bitdikdən sonra istifadə etmək olmaz.

 

Aptekdən butaxılma şərti

Resept əsasinda buraxılır.

 

İstehsalçı

Al Andalous For Pharmaceutical Industriers, Misir. 

 

Ünvan

Part No, 7/6, 6 th Industrial Area, 6 th of October City-Egypt.

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