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Vizarsin pills 100 mg 4 pcs

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Active ingredients

Sildenafil

Release form

Pills

Composition

Sildenafil citrate 140.48 mg,; which corresponds to the content of Sildenafil 100 mg; Excipients: microcrystalline cellulose (Aftsel PH101) - 147.52 mg, calcium dihydrogenphosphate - 204 mg, croscarmellose sodium - 24 mg, hypromellose - 18 mg, microcrystalline cellulose - Avcel squirt - 24 mg, hypromellose - 18 mg, microcrystalline cellulose - Avcel squirt - 24 mg; 60 mg, magnesium stearate - 6 mg; Coating composition: opadry II 31K58875 white - 20 mg (hypromellose - 28%, lactose monohydrate - 40%, titanium dioxide - 24%, triacetin - 8%).

Pharmacological effect

Pharmacological action - vasodilating, restoring erectile function.

Pharmacokinetics

The pharmacokinetics of sildenafil in the recommended dose range is linear .; Suction. After oral administration, sildenafil is rapidly absorbed. Absolute bioavailability averages about 40% (from 25 to 63%). In vitro, sildenafil at a concentration of about 1.7 ng / ml (3.5 nM) inhibits human PDE-5 activity by 50%. After a single dose of sildenafil in a dose of 100 mg, the average Cmax of free sildenafil in the blood plasma of men is about 18 ng / ml (38 nM). Cmax when taking sildenafil inside on an empty stomach is achieved on average within 60 minutes (from 30 to 120 minutes). When taken simultaneously with fatty foods, the absorption rate decreases: Cmax decreases on average by 29%, and Tmax increases by 60 minutes, however, the degree of absorption does not significantly change (AUC decreases by 11%) .; Distribution. Vss of sildenafil averages 105 liters; The relationship of sildenafil and its main circulating N-demethyl metabolite with plasma proteins is about 96% and does not depend on the total concentration of sildenafil. Less than 0.0002% of a dose of sildenafil (average 188 ng) was detected in semen 90 minutes after taking the drug .; Metabolism. Sildenafil is metabolized mainly in the liver by the action of the isoenzyme CYP3A4 (main route) and the isoenzyme CYP2C9 (additional route). The main circulating active metabolite resulting from N-demethylation of sildenafil is further metabolized. The selectivity of this metabolite with respect to PDE is comparable to that of sildenafil, and its activity against PDE-5 in vitro is about 50% of the activity of sildenafil. The metabolite concentration in the blood plasma of healthy volunteers was about 40% of the concentration of sildenafil. The N-demethyl metabolite undergoes further metabolism, its T1 / 2 is about 4 hours; Inference. The total clearance of sildenafil is 41 l / h, and the final T1 / 2 is 3-5 hours.After ingestion, as well as after iv administration, sildenafil is excreted as metabolites, mainly by the intestine (about 80% of the dose ingested) and to a lesser extent by the kidneys (about 13% of the dose taken by mouth) .; Special patient groups; Elderly patients. In healthy elderly patients (over 65 years), the clearance of sildenafil is reduced, and the concentration of free sildenafil in the blood plasma is about 40% higher than in young patients (18–45 years). Age does not have a clinically significant effect on the incidence of side effects .; Impaired renal function. With mild (Cl creatinine - 50–80 ml / min) and moderate (Cl creatinine - 30–49 ml / min) renal insufficiency, the pharmacokinetics of sildenafil after a single dose of 50 mg are not changed. With severe renal failure (Cl creatinine ≤30 ml / min), the clearance of sildenafil is reduced, which leads to an approximately twofold increase in AUC (100%) and Cmax (88%) compared with those in patients of the same age group with normal renal function ; Liver dysfunction. In patients with cirrhosis of the liver (class A and B according to Child-Pugh classification), the clearance of sildenafil is reduced, which leads to an increase in AUC (84%) and Cmax (47%) compared with those in patients of the same age group with normal function liver; The pharmacokinetics of sildenafil in patients with severely impaired liver function (Child-Pugh class C) has not been studied.

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.

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, Vizarsin is not intended for use in women. With caution it is necessary to prescribe the drug 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 of the drug Vizarsin is not intended for use in women.

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 it is applied on an empty stomach. The recommended dose is 50 mg / day, taken about 1 hour before the intended sexual activity. Depending on the efficacy and tolerance, the dose of 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 the drug is 1 time / day; dose adjustment of the drug Vizarsin in elderly patients is not required.; In case of mild to moderate severity (CK 30-80 ml / min), dose adjustment is not required, in case of severe renal failure degree (QC less than 30 ml / min) the dose of Vizarsin should be reduced to 25 mg / day. In patients with impaired liver function (eg, cirrhosis of the liver), the dose is 25 mg / day.

Side effects

Classification of the incidence of side effects (WHO): very often (> 1/10), often (from> 1/100 to less than 1/10), infrequently (from> 1/1000 to less than 1/100), rarely (from> 1/10 000 to less than 1/1000), very rarely (from less than 1/10 000, including individual messages); Allergic reactions: hypersensitivity reactions (including skin rash); From the nervous system: very much often - headache; often - dizziness; infrequently - drowsiness,hypesthesia; rarely cerebrovascular disorders, syncope; unknown - transient ischemic attacks, convulsions. On the part of the organ of vision: often - visual impairment, 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. On the part of the organ of hearing and the vestibular apparatus: infrequently - dizziness, tinnitus; rarely - deafness; From the side of the cardiovascular system: often - flushing of the skin of the face; infrequently - palpitations, tachycardia; rarely, arterial hypertension, arterial hypotension, myocardial infarction, atrial fibrillation; unknown - ventricular arrhythmia, unstable stenocardia, sudden cardiac arrest.; On the part of the respiratory system: often - nasal congestion; rarely - nosebleeds. From the digestive system: often - dyspepsia; infrequently - vomiting, nausea, dry mouth. From the musculoskeletal system: infrequently - myalgia. From the reproductive system: unknown - priapism, prolonged erection.; From the whole body: rare - chest pain, general weakness .; * Sudden hearing loss or loss was observed in a small number of cases during postmarketing use or during clinical studies of all PDE5 inhibitors, including sildenafil.

Overdose

Symptoms: with a single dose of sildenafil in doses up to 800 mg, undesirable reactions were similar to those when taking the drug in lower doses, while the severity and frequency increased. Reception of sildenafil in a dose of 200 mg did not lead to an increase in efficiency, however, the frequency of undesirable reactions (headache, sensation of hot flashes, dizziness, dyspepsia, nasal congestion, visual impairment) increased .; Treatment: symptomatic. Hemodialysis is ineffective because Sildenafil binds strongly to plasma proteins and is not excreted by the kidneys.

Interaction with other drugs

The effect of other drugs on the pharmacokinetics of sildenafil; 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 marked decrease in the clearance of sildenafil with simultaneous use of CYP3A4 isoenzyme inhibitors (ketoconazole, erythromycin, cimetidine). Cimetidine (800 mg), a non-specific inhibitor of the isoenzyme CYP3A4, when taken concurrently with sildenafil (50 mg) causes an increase in plasma concentration of sildenafil by 56%. A single dose of 100 mg of sildenafil simultaneously with erythromycin (500 mg / day, 2 times a day for 5 days), a moderate inhibitor of the isoenzyme CYP3A4, while achieving a constant concentration of erythromycin in the blood leads to an increase in AUC of sildenafil by 182%. With simultaneous administration of sildenafil (once 100 mg) and saquinavir (1200 mg / day 3 times a day), HIV protease inhibitor and CYP3A4 isoenzyme, while reaching a constant concentration of saquinavir in the blood, Cmax of sildenafil increased by 140%, and AUC increased by 210 % Sildenafil has no effect on the pharmacokinetics of saquinavir. More potent inhibitors of the isoenzyme CYP3A4, such as ketoconazole and itraconazole, can cause stronger changes in the pharmacokinetics of sildenafil. The simultaneous use of sildenafil (once 100 mg) and ritonavir (500 mg 2 times a day), HIV protease inhibitor and a strong inhibitor of cytochrome P450, while achieving a constant concentration of ritonavir in the blood leads to an increase in Cmax of 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 alone - 5 ng / ml) .; If sildenafil is taken in recommended doses, patients receiving simultaneously strong inhibitors of CYP3A4 isoenzyme, then Cmax of 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 .; In studies involving healthy volunteers with simultaneous use of bosentan, an antagonist of endothelin receptors (moderate inducer of the isoenzyme CYP3A4, CYP2C9, and possibly CYP2C19) when Css is reached (125 mg 2 times a day) and sildenafil when Css is reached (80 mg 3 times a day ) there was a decrease in AUC and Cmax of sildenafil by 62.6% and 52.4%, respectively. The use of sildenafil increased the AUC and Cmax of bosentan by 49.8 and 42%, respectively. It is assumed that the simultaneous use of sildenafil with powerful inducers of CYP3A4 isoenzyme, such as rifampicin, can lead to a greater decrease in the concentration of sildenafil in the blood plasma .; CYP2C9 isoenzyme inhibitors (tolbutamide, warfarin), CYP2D6 isoenzyme (SSRIs,tricyclic antidepressants), thiazide and thiazide-like diuretics, ACE inhibitors and calcium antagonists, do not affect the pharmacokinetics of sildenafil .; Azithromycin (500 mg / day for 3 days) has no effect on AUC, Cmax, Tmax, the rate of elimination rate and T1 / 2 of sildenafil or its main circulating metabolite .; The effect of sildenafil on other drugs; Sildenafil is a weak inhibitor of isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 (IC50> 150 µmol). When taking sildenafil at recommended doses, its Cmax is about 1 micromol, so it is unlikely that sildenafil can affect the clearance of substrates of these isoenzymes .; Sildenafil enhances the hypotensive effect of nitrates, both with prolonged use of the latter, and with their use for acute indications. In this regard, the use of sildenafil simultaneously with nitrates or NO donators is contraindicated .; With simultaneous intake of α-adrenergic blocker of doxazosin (4 and 8 mg) and sildenafil (25, 50 and 100 mg) in patients with benign prostatic hyperplasia with stable hemodynamics, the mean additional decrease in SBP / DAD in the supine position was 7/7, 9/5 and 8/4 mm Hg st. respectively, and in the standing position - 6/6, 11/4 and 4/5 mm Hg. st. respectively. Rare cases of the development of symptomatic orthostatic hypotension, manifested in the form of dizziness (without fainting), are reported in these patients. In individual sensitive patients receiving β-blockers, the simultaneous use of sildenafil can lead to symptomatic arterial hypotension .; Signs of significant interaction with tolbutamide (250 mg) or warfarin (40 mg), which are metabolized by the CYP2C9 isoenzyme, have not been identified .; Sildenafil (100 mg) has no effect on the pharmacokinetics of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of CYP3A4 isoenzyme, at their constant level in the blood .; The simultaneous use of sildenafil in the equilibrium state (80 mg 3 times a day) leads to an increase in the AUC and Cmax of bosentan (125 mg 2 times a day) by 49.8 and 42%, respectively; Sildenafil (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg) .; Sildenafil (50 mg) does not enhance the hypotensive effect of alcohol in healthy volunteers with an average blood alcohol Cmax of 0.08% (80 mg / dL) .; In patients with arterial hypertension, signs of the interaction of sildenafil (100 mg) with amlodipine were not identified .; The average additional decrease in blood pressure in the supine positionmakes 8 mm of mercury. st. (SBP) and 7 mm Hg. st. (dad) .; The use of sildenafil simultaneously with antihypertensive drugs does not lead to additional side effects.

special instructions

For the diagnosis of erectile dysfunction, the determination of their possible causes and the choice of adequate treatment, it is necessary to gather a full medical history and conduct a thorough physical examination. Erectile dysfunction medications should be used with caution in patients with anatomical deformation of the penis (angulation, cavernous fibrosis, Peyronie's disease) or in patients with risk factors for priapism (sickle-cell anemia, multiple myeloma, leukemia) (see With caution) .; During postmarketing studies, cases of prolonged erection and priapism have been reported. If an erection persists for more than 4 hours, you should immediately seek medical help. If priapism therapy was not carried out immediately, it can cause damage to the tissues of the penis and irreversible loss of potency. Drugs intended for the treatment of erectile dysfunction should not be used for men for whom sexual activity is undesirable .; Sexual activity poses a certain risk in the presence of heart disease, therefore, before starting any therapy for erectile dysfunction, the doctor should refer the patient to an STS examination. Sexual activity is undesirable in patients with heart failure, unstable angina, suffered myocardial infarction or stroke in the last 6 months, life-threatening arrhythmias, arterial hypertension (BP> 170/100 mm Hg) or hypotension (BP less than 90/50 mm RT Art.) (see. With care). Clinical studies have shown no differences in the incidence of myocardial infarction (1.1 per 100 people per year) or the mortality rate from cardiovascular diseases (0.3 per 100 people per year) in patients who received sildenafil, compared with patients receiving placebo .; Cardiovascular complications. During the post-marketing use of sildenafil for the treatment of erectile dysfunction, adverse effects such as severe cardiovascular complications (includingmyocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, hypertension and hypotension), which had a temporary connection with the use of sildenafil. Most of these patients, but not all of them, had risk factors for cardiovascular complications. Many of these adverse events were observed shortly after sexual activity, and some of them were observed after taking sildenafil without subsequent sexual activity. It is not possible to establish the existence of a direct link between the observed adverse events and the indicated or other factors .; Hypotension. Sildenafil has a systemic vasodilating effect, leading to a transient decrease in blood pressure, which is not a clinically significant event and does not lead to any consequences in most patients. However, before prescribing Vizarsin, a doctor should carefully evaluate the risk of possible undesirable manifestations of the vasodilating action in patients with appropriate diseases, especially against the background of sexual activity .; Increased susceptibility to vasodilators is observed in patients with obstruction of the left ventricular output tract (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as the rarely encountered multiple systemic atrophy syndrome, manifested by a severe dysregulation of blood pressure in the autonomic nervous system .; Since the simultaneous use of sildenafil and β-blockers can lead to symptomatic arterial hypotension in certain sensitive patients, Vizarsin should be used with caution in patients taking β-blockers (see "Interaction") .; In order to minimize the risk of orthostatic hypotension in patients taking β-adrenoblockers, Vizarsin should be started only after stabilization of hemodynamic parameters in these patients is achieved. It should also consider the feasibility of reducing the initial dose of the drug Vizarsin (see. "

Dosage and administration

"). The physician should inform the patient about what action should be taken in case of symptoms of orthostatic hypotension .; Visual disturbances.In rare cases, during post-registration use of all PDE-5 inhibitors, incl. Sildenafil, reported NPINZN - a rare disease and the reason for the reduction or loss of vision. Most of these patients had risk factors, in particular a decrease in the ratio of excavation diameters and optic nerve head ("stagnant disc"), age over 50 years, diabetes mellitus, arterial hypertension, IHD, hyperlipidemia and smoking. In an observational study, it was evaluated whether the recent use of drugs of the class of PDE-5 inhibitors is related to the acute onset of NPINSN. The results indicate an approximately twofold increase in the risk of NPINZN within 5 T1 / 2 after the use of the PDE-5 inhibitor. According to published literature data, the annual incidence of NPINZN is 2.5–11.8 cases per 100,000 men aged ≥50 years in the general population. Patients should be advised to discontinue sildenafil therapy in the event of a sudden loss of vision and immediately consult a physician. Persons who have already had a case of an NPINZN have an increased risk of a recurrence of NPINZN. Therefore, the physician should discuss this risk with such patients, as well as the potential chance of adverse effects of PDE-5 inhibitors. PDE-5 inhibitors, incl. sildenafil, in such patients should be used with caution and only in situations where the expected benefit exceeds the risk .; A small number of patients with hereditary retinitis pigmentosa have genetically determined impaired PDE of the retina. There is no information about the safety of using sildenafil in patients with retinitis pigmentosa, therefore Vizarsin should be used with caution (see With caution) .; Hearing impairment. Some post-marketing studies have reported cases of sudden deterioration or hearing loss associated with the use of all PDE-5 inhibitors, including sildenafil; Most of these patients had risk factors for sudden deterioration or loss of hearing. A causal relationship between the use of PDE-5 inhibitors and a sudden deterioration in hearing or hearing loss has not been established. In the event of a sudden deterioration in hearing or hearing loss during the administration of Vizarsin, consult a doctor immediately .; Bleeding.Sildenafil enhances the antiplatelet effect of sodium nitroprusside, NO donator, on human platelets in vitro. There are no data on the safety of using sildenafil in patients with a tendency to bleeding or exacerbation of gastric ulcer and duodenal ulcer, therefore Vizarsin should be used with caution in such patients (see. With caution). The incidence of nasal bleeding in patients with pulmonary hypertension associated with diffuse connective tissue diseases was higher (Sildenafil 12.9, placebo 0%) than in patients with primary pulmonary hypertension (Sildenafil 3, 2.4% placebo). In patients receiving sildenafil in combination with a vitamin K antagonist, the frequency of nosebleeds was higher (8.8%) than in patients not taking a vitamin K antagonist (1.7%) .; Simultaneous use with other drugs for the treatment of erectile dysfunction. The safety and efficacy of Vizarsin at the same time as other PDE-5 inhibitors or other drugs for the treatment of pulmonary hypertension containing sildenafil or other means of treating erectile dysfunction have not been studied, therefore the use of such combinations is not recommended (see "Contraindications") .; Influence on the ability to perform potentially hazardous activities that require special attention and quick reactions (for example, driving vehicles, working with moving machinery). Since when taking sildenafil may develop dizziness, lower blood pressure, the development of chromatopsia, blurred vision, etc. side effects, caution should be exercised when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions. You should also be attentive to the individual action of the drug Vizarsin in these situations, especially at the beginning of treatment and when changing the dosage regimen.

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