EREXESIL PILLS 100MG

- treatment of erectile dysfunction, characterized by the inability to achieve or maintain an erection of the penis, sufficient for satisfactory sexual intercourse.

Sildenafil is effective only with sexual stimulation.

Dosage and administration

The drug Erexezil is taken orally.

The recommended dose for most adult patients is 50 mg approximately 1 hour before sexual activity. Given the efficacy and tolerability, the dose may be increased to 100 mg or reduced to 25 mg.

The maximum recommended dose is 100 mg. The maximum recommended frequency of use is 1 time / day.

Have elderly patients dose adjustment of the drug Erexesil® not required.

At renal failure mild and moderate degree (CC 30-80 ml / min) dose adjustment is not required when severe renal failure (CC <30 ml / min) the dose of Sildenafil should be reduced to 25 mg.

Since the elimination of sildenafil is violated patients with liver damage (including in case of cirrhosis), the dose of sildenafil should be reduced to 25 mg.

Combined use with other drugs

With simultaneous use with ritonavir, the maximum single dose of sildenafil should not exceed 25 mg, and the frequency of use - 1 time in 48 hours.

With simultaneous use of cytochrome CYP3A4 isoenzyme inhibitors (erythromycin, saquinavir, Ketoconazole, itraconazole), the recommended initial dose of the drug is 25 mg.

To minimize the risk of postural hypotension in patients taking alpha blockers, use of the drug Erexezil® should begin only after achieving stabilization of hemodynamics in these patients. It should also consider the feasibility of reducing the initial dose of sildenafil.

Side Effects of Erexecil

Usually, the side effects of sildenafil are mild or moderate and are transient.

In studies using a fixed dose, it has been shown that the incidence of some adverse events increases with increasing dose.

When sildenafil was used in doses higher than recommended, adverse events were similar to those noted above, but were usually more frequent.

Allergic reactions: hypersensitivity reactions (including skin rash).

Nervous system: convulsions.

Special senses: eye pain, eye redness / sclera vascular injection.

Cardiovascular: tachycardia, lowering blood pressure, syncope, epistaxis.

Gastrointestinal: vomiting.

From the reproductive system: prolonged erection and / or priapism.

Contraindications to the use of Erexesil

- use in patients who are constantly receiving or intermittently donators of nitric oxide, organic nitrates or nitrites in any form, since sildenafil enhances the hypotensive effect of nitrates;

- simultaneous use of Erexesil with other drugs for the treatment of erectile dysfunction (the safety and efficacy of sildenafil in such combinations has not been studied);

- simultaneous use of sildenafil with ritonavir;

- children's and teenage age up to 18 years;

- women;

- Hypersensitivity to sildenafil or any other component of the drug.

Carefully Erexesil should be used for anatomical deformation of the penis (angulation, cavernous fibrosis, Peyronie's disease); diseases predisposing to the development of priapism (myeloma, sickle cell anemia, leukemia, thrombocytopenia); increased tendency to bleed; exacerbation of gastric ulcer and duodenal ulcer; hereditary pigment retinitis; heart failure; unstable angina; suffered myocardial infarction in the last 6 months,stroke or life-threatening arrhythmias; hypertension (BP> 170/110 mm Hg) and hypotension (BP <90/50 mm Hg); developmental episodes in patients with anterior non-arteritis ischemic neuropathy of the optic nerve (in history).

The use of Erexecil during pregnancy and breastfeeding

According to the registered indication Erexezil is not intended for use in women.

Application for violations of the liver

Since the elimination of sildenafil is violated patients with liver damage (including in case of cirrhosis), the dose of sildenafil should be reduced to 25 mg.

Application for violations of kidney function

At renal failure mild and moderate degree (CC 30-80 ml / min) dose adjustment is not required when severe renal failure (CC <30 ml / min) the dose of sildenafil should be reduced to 25 mg.

Use in children

According to the registered indication Erexesil is not intended for use in children and adolescents under 18 years of age.

Use in elderly patients

Have elderly patients dose adjustment of the drug Erexesil® not required.

Special notes

For the diagnosis of erectile dysfunction, the determination of possible causes and the choice of adequate treatment, it is necessary to collect a complete medical history and conduct a thorough physical examination.

Sexual activity poses a certain risk in the presence of heart disease, so before starting any therapy for erectile dysfunction, the doctor should refer the patient to an examination of the cardiovascular system.Sexual activity is undesirable in patients with HF, unstable angina, suffered myocardial infarction or stroke, life-threatening arrhythmias, arterial hypertension (BP> 170/100 mm Hg) or hypotension (BP <90/50 mm Hg) in the last 6 months. Art.). Clinical studies have shown no differences in the incidence of myocardial infarction (1.1 per 100 people per year) or the mortality rate from diseases of the cardiovascular system (0.3 per 100 people per year) in patients who received sildenafil compared with patients who received placebo. Drugs intended for the treatment of erectile dysfunction should not be given to men for whom sexual activity is undesirable.

Sildenafil has a systemic vasodilating effect, leading to a transient decrease in blood pressure. This effect is not clinically significant and does not lead to any consequences in most patients. However, before prescribing, the doctor should carefully evaluate the risk of possible undesirable manifestations of the vasodilator effect in patients with relevant diseases, especially against the background of sexual activity. Hypersensitivity to vasodilators is observed in patients with obstruction of the left ventricular outflow tract (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as with rarely encountered multiple systemic atrophy syndrome, manifested by severe dysregulation of blood pressure by the autonomic nervous system.

Rare cases of the development of anterior ischemic optic nerve neuropathy of non-arterial origin were noted as a cause of deterioration or loss of vision against the background of the use of all PDE5 inhibitors, including sildenafil. Most of these patients had risk factors such as excavation (deepening) of the optic nerve head, over 50 years of age, diabetes mellitus, arterial hypertension, IHD, hyperlipidemia, and smoking. There is no causal relationship between taking PDE5 inhibitors and the development of anterior ischemic optic nerve neuropathy. The doctor should inform the patient about the increased risk of developing anterior ischemic optic neuropathy of non-arterial origin, if this condition has already been noted before.

Since the combined use of sildenafil and alpha-blockers can lead to symptomatic hypotension in individual sensitive patients, sildenafil should be used with caution in patients taking alpha-blockers. To minimize the risk of postural hypotension in patients taking alpha blockers, the use of sildenafil should be started only after stabilization of hemodynamics in such patients is achieved. It should also consider the feasibility of reducing the initial dose of the drug Erexesil. It is necessary to inform patients about what actions should be taken in case of symptoms of postural hypotension.

A small number of patients with hereditary retinitis pigmentosa have genetically determined abnormalities of retinal phosphodiesterase functions. Information about the safety of sildenafil in patients with retinitis pigmentosa is absent, therefore, sildenafil should be used with caution.

Sildenafil enhances the anti-aggregation effect of sodium nitroprusside (donor NO) on human platelets in vitro. There is no information about the safety of using sildenafil in patients with internal bleeding or active peptic gastric ulcer, so it should be used with caution.

Erectile dysfunction treatment should be prescribed with caution to patients with anatomical deformation of the penis (angulation, cavernous fibrosis, Peyronie's disease) or patients with risk factors for priapism (sickle cell anemia, multiple myeloma, leukemia).

The safety and effectiveness of sildenafil with other drugs for the treatment of erectile dysfunction has not been studied, so the use of such combinations is not recommended.

Some post-marketing and clinical studies using all PDE5 inhibitors, including sildenafil, have reported a sudden decrease or loss of hearing in patients. However, the majority of these patients had risk factors for the development of this pathology, and no correlation was found between the use of PDE5 inhibitors and a sudden decrease or hearing loss.In the event of a sudden decline or loss of hearing, the patient should discontinue sildenafil therapy and consult a physician immediately.

Influence on ability to drive motor transport and control mechanisms

Against the background of the use of sildenafil, no negative effect on the ability to drive a car or other technical means was observed. However, since the admission of sildenafil may decrease blood pressure, the development of chromatopsia, blurred vision and other side effects, you should carefully consider the individual action of the drug in these situations, especially at the beginning of treatment and when changing the dosage regimen.

Overdose

With a single dose of sildenafil at a dose of 800 mg, adverse events were comparable to those with a lower dose, but were more common.

Symptoms: increased severity of side effects.

Treatment: conducting symptomatic therapy. Hemodialysis does not accelerate the clearance of sildenafil, since the latter is actively associated with plasma proteins and is not excreted by the kidneys.

Drug interaction

Effect of Other Drugs on Sildenafil Pharmacokinetics

Sildenafil metabolism occurs mainly under the action of CYP3A4 isoenzymes (main route) and CYP2C9, therefore inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inductors, respectively, increase the clearance of sildenafil.A decrease in the clearance of sildenafil with simultaneous use of cytochrome CYP3A4 isoenzyme inhibitors (ketoconazole, Erythromycin, cimetidine) was noted.

Cimetidine (at a dose of 800 mg), a non-specific inhibitor of the cytochrome CYP3A4 isoenzyme, when used together with sildenafil (at a dose of 50 mg) causes an increase in plasma concentration of sildenafil by 56%.

A single dose of sildenafil in a dose of 100 mg together with erythromycin (500 mg / day 2 times / day for 5 days), a specific inhibitor of the cytochrome CYP3A4 isoenzyme, against the background of achievement Css erythromycin in the blood leads to an increase in AUC of sildenafil by 182%.

When co-administration of sildenafil (once in a dose of 100 mg) and saquinavir (1200 mg / day in 3 doses), HIV protease inhibitor and cytochrome CYP3A4 isoenzyme, against the background of achievement Css saquinavir in the bloodmax Sildenafil increased by 140%, and AUC increased by 210%. Sildenafil has no effect on the pharmacokinetics of saquinavir.

More potent inhibitors of cytochrome CYP3A4 isoenzyme, such as ketoconazole and itraconazole, can also cause stronger changes in the pharmacokinetics of sildenafil.

The simultaneous use of sildenafil (once in a dose of 100 mg) and ritonavir (500 mg 2 times / day), an HIV protease inhibitor and a strong inhibitor of cytochrome P450, against the background of achievement Css ritonavir in the blood leads to an increase in Cmax Sildenafil by 300% (4 times), and AUC - by 1000% (11 times). After 24 h, the concentration of sildenafil in the blood plasma is about 200 ng / ml (after a single application of sildenafil only 5 ng / ml).

If sildenafil is taken in recommended doses, patients receiving simultaneously strong inhibitors of the cytochrome CYP3A4 isoenzyme, then Cmax free sildenafil does not exceed 200 nM, and the drug is well tolerated.

A single antacid (magnesium hydroxide / aluminum hydroxide) does not affect the bioavailability of sildenafil.

Cytochrome CYP2C9 isoenzyme inhibitors (tolbutamide, warfarin), CYP2D6 cytochrome isoenzyme (selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazide and thiazide-like diuretics, ACE inhibitors and Calcium antagonists, have no effect on the effect of calcium, calcium antagonists, tiazide and thiazide-like diuretics, ACE inhibitors and calcium antagonists, tacyclic antidepressants, tiazidnymi and thiazide-like diuretics, ACE inhibitors and calcium antagonists, calcium antagonists, tiazidnymi

Azithromycin (500 mg / day for 3 days) has no effect on AUC, CmaxTmax, removal rate constant and T1/2 sildenafil or its major circulating metabolite.

Effect of sildenafil on other drugs

Sildenafil is a weak inhibitor of cytochrome P450 isoenzymes - 1A2, 2C9, 2C19, 2D6, 2E1, and 3A4 (IR50 > 150 μmol). When taking sildenafil in recommended doses, its Cmax is about 1 μmol, so it is unlikely that sildenafil can affect the substrate clearance of these isoenzymes.

Sildenafil enhances the hypotensive effect of nitrates both with long-term use of the latter, and with their appointment for acute indications. In this regard, the use of sildenafil in combination with nitrates or nitric oxide donors is contraindicated. While taking alpha-adrenergic blocker Doxazosin (in doses of 4 or 8 mg) and sildenafil (in doses of 25, 50 or 100 mg) in patients with benign prostatic hyperplasia with stable hemodynamics, the average additional decrease in systolic and diastolic blood pressure in the supine position was 7 / 7, 9/5 and 8/4 mm Hg, respectively, and in the standing position - 6/6, 11/4 and 4/5 mm Hg, respectively.Rare cases of the development of symptomatic postural hypotension, manifested in the form of dizziness (without fainting), have been reported in these patients. In some sensitive patients receiving alpha-blockers, the simultaneous use of sildenafil can lead to symptomatic hypotension.

There were no signs of significant interaction with tolbutamide (at a dose of 250 mg) or Warfarin (at a dose of 40 mg), which are metabolized by the CYP2C9 isoenzyme.

Sildenafil (at a dose of 100 mg) has no effect on the pharmacokinetics of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of the cytochrome CYP3A4 isoenzyme, at their constant level in the blood.

Sildenafil (at a dose of 50 mg) does not cause an additional increase in bleeding time with the use of Acetylsalicylic acid (at a dose of 150 mg).

Sildenafil (in a dose of 50 mg) does not enhance the hypotensive effect of ethanol in healthy volunteers at Cmax ethanol in blood averages 0.08% (80 mg / dL).

In patients with AH, there was no evidence of sildenafil (at a dose of 100 mg) with Amlodipine . The average additional decrease in blood pressure in the supine position is 8 mm Hg. (systolic blood pressure) and 7 mmHg (diastolic blood pressure).

The use of sildenafil in combination with antihypertensive drugs does not lead to additional side effects.

Pharmacy sales terms

The drug is available on prescription.

Terms and conditions of storage

The drug Erexezil should be kept out of the reach of children at a temperature not exceeding 25 ° C.