Priligy (Dapoxetine) was invented by the most respected and old pharmaceutical US company – «EliLilly», which already by 1898 had unprecedented at that time annual turnover of $ 300 000. The drug was created as a cure for premature ejaculation, although some analogues are used as antidepressants. In 2003, patent for Priligy (Dapoxetine) production, doctors reviews on which were positive, was sold to «Johnson&Johnson» company. Today, this drug is produced mainly in India and Asian countries.
Canadian Pharmacy Priligy (Dapoxetine) is a drug that is used in case of problems with sexual function in male body. It helps to cope with premature ejaculation, can be used simultaneously with other similar erectile dysfunction pills (Viagra, Cialis, Levitra). Before taking the drug, read the instruction about how to use Dapoxetine (Priligy), as there are contraindications for its use.
Structure and Composition
This medicament is produced in the form of coated pills. Drugstore chains sell the following types:
- dapoxetine 60 mg;
- dapoxetine 90 mg;
- dapoxetine 30 mg.
This marking corresponds to the content of the main active ingredient – dapoxetine hydrochloride. Effectiveness of this drug does not depend on what type the patient is taking – it is important to observe regularity of treatment and carry out therapeutic measures under doctor’s supervision.
Canadian Priligy (Dapoxetine) has distinctive appearance – double radius blue-green pills.
Generic Priligy is used by men with existing problems in sexual sphere. This drug helps to cope with premature ejaculation. Despite the fact that diagnosis can be made by every man by himself, in case of presence of correspondent signs, experts insist on referring to doctors. Only with full examination of male body it is possible to reveal causes of premature ejaculation – perhaps the case is in psychological disorders.
Tests have proven that Priligy (Dapoxetine) is highly effective in premature ejaculation treatment in men older than 18 years. Canadian Priligy (Dapoxetine) helps to delay ejaculation by 3 – 4 times. This happens due to blocking receptors in cerebral cortex. As a result, serotonin is absorbed and ejaculation occurs several times later.
In comparison with other drugs of similar action Priligy (Dapoxetine) starts to act immediately after taking the first pill. In this case, duration of drug effect on the body is 5 to 8 hours. Thus, to achieve maximal effect you will need only 1 hour.
Priligy (Dapoxetine) Drug Interactions
Interactions with MAO inhibitors
Patients receiving both SSRI and MAO inhibitors observed serious, sometimes fatal reactions, including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of system of vital functions indicators and mental state changes including strong agitation, progressing into delirium and coma. These reactions have also been observed in patients who have recently withdrawn SSRIs and started treatment with MAO inhibitors. In some cases symptoms resembled neuroleptic malignant syndrome.
Data on combined use of SSRIs and MAO inhibitors in animals suggest that these drugs may synergistically increase arterial blood pressure and cause behavioral excitement. Therefore, Canadian Pharmacy Priligy drug should not be taken with MAO inhibitors simultaneously and 14 days after their admission cessation. Likewise, MAO inhibitors should not be taken within 7 days after Priligy drug withdrawal.
Interaction with Thioridazine
Thioridazine prolongs QTc interval, which is accompanied by ventricular fibrillation. Drugs such as Canadian Priligy (Dapoxetine) that inhibit CYP2D6 enzyme, appears to inhibit thioridazine metabolism. It is expected that caused by this increase in thioridazine level will prolong QTc interval. Priligy (Dapoxetine) drug should not be taken with thioridazine simultaneously and 14 days after its admission cessation. Likewise, thioridazine should not be taken within 7 days after Priligy (Dapoxetine) withdrawal.
Medications with Serotonergic Effect
As with SSRIs, Canadian Pharmacy Priligy drug administration simultaneously with serotonergic medications (including MAO inhibitors, L-tryptophan, triptans, tramadol, linezolid, SSRIs, inhibitors of serotonin and norepinephrine, lithium, and St John’s wort drugs (Hypericum perforatum)) may increase serotoninergic side effects. Generic Priligy (Dapoxetine) should not be taken with other SSRIs, MAOIs or other serotonergic agents simultaneously and 14 days after these drugs withdrawal. Likewise, these drugs should not be taken within 7 days after Canadian Priligy (Dapoxetine) withdrawal.
Drugs with Effect on CNS
Canadian Pharmacy Priligy (Dapoxetine) administration simultaneously with drugs acting on central nervous system in patients with premature ejaculation has not been studied. Caution advised to be taken if it is necessary to take these drugs together.
Influence of Other Drugs on Dapoxetine Hydrochloride
Studies with human liver microsomes, kidney and intestines in vitro showed that dapoxetine is metabolized mainly by CYP2D6, CYP3A4 and flavin-containing monooxygenase 1 (PMO1). Therefore, inhibitors of these enzymes may reduce dapoxetine clearance.
Active CYP3A4 Inhibitors
Ketoconazole in dosage of 200 mg 2 times a day during 7 days increased Cmax and AUC0-∞ of dapoxetine (60 mg single dose), by 35% and 99% respectively. Taking into account proportion of unbound dapoxetine and desmethyldapoxetine, Cmax of active fraction (amount of unbound dapoxetine and desmethyldapoxetine) in presence of active CYP3A4 inhibitors may increase by about 25%, AUC can be doubled. This increase in Cmax and AUC of active fraction can be much more pronounced in subpopulation of patients who have no functionally active enzyme, and also while receiving active CYP2D6 inhibitors.
Canadian Pharmacy Priligy (Dapoxetine) drug should not be taken simultaneously with active CYP3A4 inhibitors, such as ketoconazole, itraconazole, ritonavir, saquinavir, telithromycin, nefazodone, nelfinavir and atazanavir.
Moderately Active CYP3A4 Inhibitors
Concomitant use of moderately active CYP3A4 inhibitors, such as erythromycin, clarithromycin, fluconazole, amprenavir, fosamprenavir, aprepitant, diltiazem or verapamil, can significantly increase level of dapoxetine and desmethyldapoxetine systemic exposure, especially in patients with low CYP2D6 activity. Maximal dosage of generic Priligy received simultaneously with these drugs should be limited to 30 mg and taken with caution.
Active CYP2D6 Inhibitors
Taking fluoxetine in dosage of 60 mg/day for 7 days increased Cmax and AUC0-∞ of dapoxetine (60 mg single dose), 50% and 88% respectively. Taking into account proportion of unbound dapoxetine and desmethyldapoxetine, Cmax of active fraction (amount of unbound dapoxetine and desmethyldapoxetine) in presence of active CYP2D6 inhibitors may increase by about 50%, AUC can be doubled. This increase in Cmax and AUC of active fraction is close to that expected in patients with low CYP2D6 activity and may increase frequency and severity of dose-dependent adverse reactions.
Therefore, caution is advised to be taking when increasing Priligy (Dapoxetine) dosage to 60 mg in patients receiving active CYP2D6 inhibitors and in patients with low CYP2D6 activity.
Interaction with Drugs Metabolized by CYP1A and CYP2B6 isoenzymes
Based on comparative data dapoxetine Cmax when taking 60 mg of the drug and dapoxetine concentration at 50% inhibition (IC50) of CYP1A2 isoenzyme in vitro, it was concluded that dapoxetine influence on concentration of simultaneously prescribed drugs, metabolized by this isoenzyme, is not expected. Influence of dapoxetine on CYP2B6 isoenzyme has not been studied.
There were studies on dapoxetine pharmacokinetics received at dosage of 60 mg together with tadalafil (20 mg) and sildenafil (100 mg). Tadalafil did not affect dapoxetine pharmacokinetics. Sildenafil significantly increased AUC0-∞ and Cmax of dapoxetine (22% and 4% respectively), which is considered not clinically significant. Canadian Priligy (Dapoxetine) should be used with caution by patients taking PDE-5 inhibitors due to possible reduced tolerance of these patients to orthostatic hypotension.
Influence of Dapoxetine Hydrochloride on Drugs, Taken Simultaneously
Single and multiple reception of the drug in doses of 30 mg and 60 mg by patients taking tamsulosin daily did not change pharmacokinetics of the latter. It also did not change orthostatic hypotension rate, which was the same when receiving tamsulosin alone or in combination with Canadian Priligy 30 mg or 60 mg. Priligy (Dapoxetine) drug should be used with caution by patients taking alpha-blockers, because of possibility of tolerance reduction of these patients to orthostatic hypotension.
Drugs, Metabolized by CYP2D6
Multiple reception of Canadian Pharmacy Priligy (Dapoxetine) drug (60 mg/day during 6 days) increased Cmax and AUC 0-∞ of desipramine (50 mg single dose) by 11% and 19% respectively, compared to desipramine reception alone. Dapoxetine can likewise increase concentration of other drugs, metabolized by CYP2D6, in blood plasma. Clinical relevance of this phenomenon is likely to be small.
Drugs, Metabolized by CYP3A
Multiple reception of Canadian Priligy drug (60 mg/day for 6 days) reduced AUC0-∞ of midazolam (8 mg single dose) approximately by 20% (range from -60% to +18%). Clinical relevance of this phenomenon in majority of patients is likely to be small. However, increase in CYP3A activity may be of clinical relevance in some patients simultaneously taking medications metabolized mainly by CYP3A and having narrow therapeutic window.
Drugs, Metabolized by CYP2C19
Multiple reception of generic Priligy (Dapoxetine) drug (60 mg/day for 6 days) did not affect pharmacokinetics of omeprazole (40 mg single dose). Dapoxetine is unlikely to affect pharmacokinetics of other CYP2C19 substrates.
Drugs, Metabolized by CYP2C9
Multiple reception of Priligy (Dapoxetine) drug (60 mg/day for 6 days) did not affect pharmacokinetics and pharmacodynamics of glyburide (5 mg single dose). Dapoxetine is unlikely to affect pharmacokinetics of other CYP2C9 substrates.
Study results showed that dapoxetine (60 mg) did not affect pharmacokinetics of tadalafil (20 mg) and sildenafil (100 mg).
There are no data on effects of long-term use of warfarin in combination with Canadian Pharmacy Priligy (Dapoxetine) drug. Caution is advised to be taken when taking Priligy drug by patients, long taking warfarin. In study of pharmacokinetics, multiple dose of dapoxetine (60 mg/day for 6 days) did not affect pharmacokinetics and pharmacodynamics (PT and MHO) of warfarin (25 mg single dose).