Vizarsin pills 50mg №1

Indications

- 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 in the presence of sexual stimulation.

Dosage and administration

The drug is taken orally. When using the drug Vizarsin ^® with food, the effect of the drug may develop later than when applied on an empty stomach.

The recommended dose is 50 mg / day, taken approximately 1 hour before the intended sexual activity. Depending on the efficacy and tolerability of the dose of the drug Vizarsin^® can be increased to 100 mg / day or reduced to 25 mg / day.

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

Correction of the dose of the drug Vizarsin^® at elderly patients not required.

At renal failure mild and moderate severity (CC 30-80 ml / min) dose adjustment is not required when severe renal failure (CC less than 30 ml / min) dose of the drug Vizarsin^® should be reduced to 25 mg / day.

Have patients with impaired liver function (for example, liver cirrhosis) the dose is 25 mg / day.

Adverse effects

Classification of the incidence of side effects (WHO): very often (> 1/10), often (from> 1/100 to <1/10), infrequently (from> 1/1000 to <1/100), rarely (from> 1/10 000 to <1/1000), very rarely (from <1/10 000, including individual messages).

Allergic reactions: hypersensitivity reactions (including skin rash).

Nervous system: very often - a headache; often - dizziness; infrequently - drowsiness, hypesthesia; rarely cerebrovascular disorders, syncope; unknown - transient ischemic attacks, convulsions.

Special senses: often - visual disturbances, transient disturbances of color perception (chromatopsia); infrequently - the defeat of the conjunctiva, a violation of tears; unknown - anterior ischemic neuropathy of non-arterial origin (NAION), retinal vascular occlusion, narrowing of the visual fields.

From the organ of hearing and vestibular apparatus: infrequently - dizziness, tinnitus; rarely - deafness *.

Cardiovascular: often - flushing of the skin of the face; infrequently - palpitations, tachycardia; rarely, arterial hypertension, arterial hypotension, myocardial infarction, atrial fibrillation; unknown - ventricular arrhythmia, unstable angina, sudden cardiac arrest.

Respiratory: often - nasal congestion; rarely - nosebleeds.

Gastrointestinal: often - dyspepsia; infrequently - vomiting, nausea, dry mouth.

Musculoskeletal system: infrequently - myalgia.

From the reproductive system: unknown - priapism, prolonged erection.

On the part of the body as a whole: infrequently - chest pain, general weakness.

* A sudden decrease or loss of hearing was observed in a small number of cases during post-marketing use or during clinical studies of all PDE5 inhibitors, including Sildenafil.

Contraindications

- simultaneous use with nitric oxide donors (such as amyl nitrite) or nitrates in any dosage form, since Sildenafil may enhance the hypotensive effect of nitrates (given the known effect of sildenafil on NO / cGMP);

- use in men who do not recommend sexual activity (for example, patients with severe cardiovascular diseases, such as unstable angina or severe heart failure);

- reduction of vision due to anterior ischemic optic neuropathy of non-arterial origin (NAION), whether or not it is associated with the use of PDE5 inhibitors;

- established congenital dystrophy of the retina, incl. retinitis pigmentosa (retinitis pigmentosa);

- severe liver dysfunction;

- arterial hypotension (BP less than 90/50 mm Hg);

- a recent stroke or myocardial infarction;

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

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

According to the registered indication drug Vizarsin^® not intended for use in women.

Carefully the drug should be prescribed for lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; diseases of the cardiovascular system; multiple systemic atrophy syndrome; anatomical deformation of the penis; priapism; sickle cell anemia; multiple myeloma; leukemia; simultaneous use of alpha-blockers.

Use during pregnancy and lactation

According to the registered indication drug Vizarsin^® not intended for use in women.

Application for violations of the liver

Have patients with impaired liver function (for example, liver cirrhosis) the dose is 25 mg / day.

In case of marked impaired liver function, the use of the drug is contraindicated.

Application for violations of kidney function

At renal failure mild and moderate severity (CC 30-80 ml / min) dose adjustment is not required when severe renal failure (CC less than 30 ml / min) dose of the drug Vizarsin^® should be reduced to 25 mg / day.

Use in children

The use of the drug is contraindicated in children and adolescents up to 18 years.

Use in elderly patients

Correction of the dose of the drug Vizarsin^® at elderly patients not required.

Special notes

Before prescribing medication, it is necessary to carefully evaluate the history and conduct a clinical examination to diagnose erectile dysfunction and identify its possible causes.

Sexual activity poses a certain risk in the presence of diseases of the cardiovascular system, so before starting any therapy for erectile dysfunction, the patient’s condition should be evaluated. Sildenafil has a systemic vasodilating effect, leading to a small and transient decrease in blood pressure. Before using sildenafil, you should carefully evaluate the risk of possible undesirable vasodilating effects in patients with appropriate diseases, especially against the background of sexual activity.Increased susceptibility to vasodilators is observed in patients with obstruction of the outflow tract of the left ventricle (for example, aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as with rarely encountered multiple systemic atrophy syndrome, which manifests itself as a severe violation of autonomous regulation of blood pressure.

Vizarsin^® enhances the hypotensive effect of nitrates.

With the post-marketing use of sildenafil, serious cardiovascular events have been reported, including myocardial infarction, unstable angina, sudden coronary death, ventricular arrhythmias, hemorrhagic stroke, transient ischemic attacks, arterial hypertension or hypotension. Most of these patients, but not all, had predisposing cardiovascular risk factors. Many of the observed phenomena developed in a short period of time after taking sildenafil, even in the absence of sexual activity. It is impossible to determine whether these phenomena are directly related to the described or other factors.

Preparations for the treatment of sexual dysfunction, including sildenafil, should be used with caution in patients with anatomical deformities of the penis (such as angulation, cavernous fibrosis or Peyronie's disease), as well as in patients with conditions predisposing to priapism (such as sickle cell anemia, multiple myeloma or leukemia).

The safety and efficacy of sildenafil in combination with other drugs intended for the treatment of erectile dysfunction have not been studied, so the use of such combinations is not recommended.

Cases of visual impairment and the development of anterior ischemic optic neuropathy of non-arterial genesis have been observed against the background of the use of sildenafil and other PDE5 inhibitors. Patients should be informed that in case of loss of sight or a sudden deterioration of it, discontinue use of the drug Vizarsin^® and immediately consult a doctor.

Sildenafil should be used with caution in patients taking alpha-blockers, as the simultaneous use of sildenafil and alpha-blockers can lead to symptomatic arterial hypotension in certain susceptible patients. Hypotension most often develops 4 hours after sildenafil. To minimize the risk of postural hypotension in these patients, sildenafil should be taken only after stabilization of hemodynamics has been achieved while taking alpha blockers. The use of sildenafil should begin with a dose of 25 mg. In addition, the patient should be explained what can be done in case of development of arterial hypotension.

Studies with human platelets have shown that sildenafil potentiates the anticoagulant effect of sodium nitroprusside in vitro.There is no information on the safety of sildenafil in patients with bleeding or active peptic ulcers. Therefore, sildenafil can be used in these patients only after a thorough evaluation of the benefit / risk ratio.

Drug Vizarsin^® contains lactose, and therefore caution should be exercised when using the drug with lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.

Drug Vizarsin^® not intended for use in women.

Influence on ability to drive motor transport and control mechanisms

Studies have not been conducted to study the effect on the ability to drive vehicles and work with mechanisms, but because of the possibility of visual impairment, dizziness, one should be attentive to the individual action of the drug, especially at the beginning of treatment and when changing the dosage regimen.

Overdose

Symptoms: headache, flushing to the skin of the face, dizziness, dyspepsia, nasal congestion, blurred vision.

Treatment: conducting symptomatic therapy. Hemodialysis is ineffective.

Drug interaction

Effect of Other Drugs on Sildenafil Pharmacokinetics

Sildenafil metabolism occurs mainly under the action of cytochrome P450 - CYP3A4 (main route) and CYP2С9 (secondary route) isoenzymes, therefore inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inductors, respectively, increase the clearance of sildenafil.

The simultaneous use of CYP3A4 isoenzyme inhibitors (such as Ketoconazole, Erythromycin, pymetidine) and sildenafil reduces its clearance.

Ritonavir increases AUC of sildenafil 11 times; simultaneous use of these drugs is not recommended. If necessary, simultaneous use with ritonavir maximum single dose of the drug Vizarsin^® should not exceed 25 mg, and the multiplicity of use - 1 time in 48 hours

With simultaneous use of sildenafil (100 mg 1 time / day) and HIV protease inhibitor and CYP3A4 isoenzyme inhibitor saquinavir, while achieving a constant concentration of saquinavir in the blood (1200 mg 3 times / day), C_max Sildenafil is increased by 140%, and AUC - by 210%. Sildenafil has no effect on the pharmacokinetics of saquinavir. More potent inhibitors of the isoenzyme CYP3A4, such as ketoconazole and itraconazole, presumably, can cause more pronounced changes in the pharmacokinetics of sildenafil.

The use of sildenafil in a dose of 100 mg 1 time / day simultaneously with erythromycin, a specific inhibitor of CYP3A4, while achieving a constant concentration of erythromycin in the blood (500 mg 2 times / day for 5 days), leads to an increase in AUC of sildenafil by 182%. In healthy male volunteers, Azithromycin (500 mg / day for 3 days) did not affect AUC, C_max, T_max, removal rate constant and T_1/2 sildenafil or its major circulating metabolite. Cimetidine (at a dose of 800 mg), a nonspecific inhibitor of CYP3A4, when taken together with sildenafil (at a dose of 50 mg) by healthy volunteers, caused an increase in plasma concentration of sildenafil by 56%.

Grapefruit juice, a weak CYP3A4 inhibitor, can moderately increase plasma concentrations of sildenafil.

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

Although special pharmacokinetic studies were not conducted with all drugs, population pharmacokinetic analysis did not reveal any changes in the pharmacokinetics of each of the Cephalic acidophilia when combined with such inhibitors of the CYP2C9 isoenzyme, as tolbutamide, Warfarin, phenytoin, with inhibitors of the CYP2D6 isoenzyme (selective inaccuracy of the current mode, in the case of imitative CYP2D6 isoenzyme (selective inaccuracy), with the CYP2D6 isoenzyme (selective inhibitions for the use of the isoenzyme), I did not use the CYP2D6 isoenzyme (selective inhibitors of cell imitations), which did not use the CYP2D6 isoenzyme (selective inhibitors of cell imitation), which did not apply for the CYP2D6 isoenzyme (selective inhibitors of cell-pendulum therapy). and similar diuretics, loop and potassium-sparing diuretics, ACE inhibitors, Calcium channel blockers, b ta-blockers or isoenzyme inducers CYP450 (such as rifampicin, barbiturates).

Nicorandil is a hybrid of nitrate and an activator of potassium channels. Due to the presence of the nitrate component, it may enter into an undesirable interaction with sildenafil.

The 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 using sildenafil at the recommended doses of C_max blood plasma is about 1 μmol, so it is unlikely that Vizarsin^® may affect the substrate clearance of these isoenzymes.

There are no data on the interaction of sildenafil with non-specific phosphodiesterase inhibitors, such as theophylline or Dipyridamole.

Given the well-known effect of sildenafil on NO / cGMP, it can enhance the hypotensive effect of nitrates, therefore its simultaneous use with nitric oxide donators or nitrates in any dosage form is contraindicated.

The simultaneous use of sildenafil and alpha-blockers can lead to symptomatic arterial hypotension in certain susceptible patients. Hypotension most often develops 4 h after administration of sildenafil. In three special studies on drug interactions in patients with benign prostatic hyperplasia (BPH) with stable hemodynamics while receiving Doxazosin (in doses of 4 mg and 8 mg), sildenafil (in doses of 25 mg, 50 mg, or 100 mg) were simultaneously administered. In all three studies, there was an average additional decrease in blood pressure in the prone position at 7/7 mm Hg, 9/5 mm Hg, and 8/4 mm Hg. and an additional decrease in blood pressure in the standing position at 6/6 mm Hg, 11/4 mm Hg, and 4/5 mm Hg, respectively. With simultaneous use of sildenafil and doxazosin in patients with stable hemodynamics while receiving doxazosin, rare cases of symptomatic postural hypotension have been observed. In these described cases, dizziness or a feeling of lightness developed, but without the development of fainting states. To reduce the likelihood of developing orthostatic hypotension, it is necessary to achieve a stable state during therapy with alpha-blockers before starting sildenafil.

There was no significant interaction with the simultaneous use of sildenafil (50 mg dose) and tolbutamide (250 mg dose) or warfarin (40 mg dose), which are metabolized with the participation of CYP2C9.

Sildenafil (at a dose of 50 mg) does not potentiate the increase in bleeding time caused by Acetylsalicylic acid (at a dose of 150 mg).

Sildenafil (at a dose of 50 mg) does not potentiate the hypotensive effect of ethanol in healthy volunteers with a maximum blood ethanol content of 80 mg / dl.

Summarizing the available data on the following drugs: diuretics, beta-blockers, ACE inhibitors, angiotensin II receptor blockers, vasodilators and central-acting antihypertensive agents, adrenergic neuron blockers, calcium channel blockers and alpha adrenoreceptor blockers, did not reveal differences in the profile of calcium channel blockers and alpha adrenoreceptor blockers, did not reveal differences in the profile of the calcium channel blockers and alpha adrenoreceptor blockers, did not reveal differences in the profile of the calcium channel blockers and alpha adrenoreceptor blockers, did not reveal differences in the profile of the calcium channel blockers and alpha adrenoreceptor blockers, did not reveal differences in profiles of patients taking sildenafil or placebo at the same time. In a specially conducted study, sildenafil (at a dose of 100 mg) was used simultaneously with Amlodipine in patients with arterial hypertension, and additionally decreased systolic blood pressure in the supine position, on average, by 8 mm Hg, and diastolic blood pressure - by 7 mm Hg. st. This additional decrease in blood pressure was the same as when using only sildenafil in healthy volunteers.

Terms and conditions of storage

The drug should be stored out of the reach of children at a temperature not higher than 30 ° C.