V-car tablets p/o 50mg №4×1

NameV-car. Release form film-coated tablets Dosage 50 mg. Pack quantity: 2 pcs. ProducerFarmakea MNNSildenafil FTGERectile dysfunction treatment, PDE-5 inhibitor IngredientsV-car 50 mg Each tablet contains: active ingredient – sildenafil 50 mg (as sildenafil citrate); excipients: microcrystalline cellulose pH 101, magnesium stearate, sodium croscarmellose, anhydrous colloidal silica, opadry II blue: lactose monohydrate, hypromellose, titanium dioxide, polyethylene glycol / macrogol, FD&C blue No. 2 / aluminum varnish based on indigo carmine E132, FD&C blue No. 2 / aluminum lacquer based on brilliant blue E133, iron oxide black E125. V-car 100 mg Each tablet contains: active substance – sildenafil 100 mg (as sildenafil citrate); excipients: microcrystalline cellulose pH 101, magnesium stearate, sodium croscarmellose, anhydrous colloidal silica, opadry II blue: lactose monohydrate, hypromellose, titanium dioxide, polyethylene glycol / macrogol, FD&C blue No. 2 / aluminum varnish based on indigo carmine E132, FD&C blue No. 2 / aluminum lacquer based on brilliant blue E133, iron oxide black E125. Brief characteristicsV-car 50 mg Film-coated tablets, triangular, blue V-car 100 mg Film-coated tablets, rhombus-shaped, blue Pharmacotherapeutic group Drugs used for erectile dysfunction. ATX code: G04BE03. Pharmacological properties During sexual arousal, phosphodiesterase type 5 is inhibited by sildenafil, cGMP levels increase, which leads to relaxation of smooth muscles and increased blood flow in the penis. The use of sildenafil is ineffective in the absence of sexual activity. Pharmacodynamic properties The active ingredient B-car Sildenafil citrate is a selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE-5). The physiological mechanism of erection involves the release of nitric oxide (NO) in the cavernous body during sexual activity. Nitric oxide activates the enzyme guanylate cyclase, which leads to an increase in the level of cyclic guanosine monophosphate (cGMP), relaxation of the smooth muscles of the cavernous body and increased blood flow in the penis. Sildenafil enhances the effect of nitric oxide on this tissue, as it inhibits phosphodiesterase type 5 (PDE-5), which ensures the breakdown of cGMP in the cavernous body. Pharmacokinetic propertiesB-car is rapidly absorbed when taken orally, the absolute bioavailability is 40%. Its pharmacokinetics is dose-dependent within the recommended dose range. It is eliminated mainly by hepatic metabolism (cytochrome P4503A4 system), turning into an active metabolite; the active substance and the metabolite have the same half-life (T1 / 2) of 4 hours. Peak plasma concentrations are reached in 30-120 minutes when taken orally on an empty stomach. The mean volume of distribution at steady state (Vd) is 105 L, indicating distribution to all body tissues. Sildenafil and its active N-dismethyl metabolite bind to plasma proteins by 96%, regardless of the oral dose taken. The N-dismethyl metabolite undergoes further metabolism. The N-dismethyl metabolite is selective for PDE-5, in vitro it demonstrates activity for PDE-5, which is 50% of the activity of sildenafil, in vivo the activity of the metabolite is 20% of the activity of sildenafil. Sildenafil is excreted mainly as metabolites in the feces (80% of the oral dose), and slightly in the urine (13% of the oral dose). Similar pharmacokinetics are observed in volunteers and in patients. Geriatrics: in healthy elderly volunteers (65 years and older), there is a reduced clearance of sildenafil: free plasma concentration is 40% higher than plasma concentration in young volunteers (18-45 years). Renal failure: with mild (creatinine clearance = 50-80 ml / min.) And moderate (creatinine clearance = 30-49 ml / min.) renal failure, the pharmacokinetics of a single oral dose does not change. In severe renal insufficiency (creatinine clearance = <30 ml / min.), The clearance of sildenafil is reduced compared to the clearance in elderly people without renal insufficiency (AUC and Cmax values double). Hepatic insufficiency: in patients with cirrhosis of the liver, the clearance of sildenafil is reduced, this is expressed in an increase in the values of AUC (84%) and Cmax (47%) compared with those in elderly volunteers without liver damage. The recommended starting dose for these patients is 25 mg. The pharmacokinetics of sildenafil in patients with severe hepatic impairment has not been studied. Indications for use Erectile dysfunction, characterized by the inability to achieve or maintain an erection of the penis sufficient for satisfactory intercourse. The drug is effective only in the presence of sexual stimulation. Dosing and Administration Tablets of V-car are taken orally. Use in adults The recommended dose of 50 mg is taken, if necessary, approximately one hour before the planned sexual activity. But in some cases, it is possible to use B-car from 4 hours to 0.5 hours before sexual activity. Based on 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 application is once a day. Use in the elderly and patients with mild to moderate renal impairment (CC 30-80 ml / min) The recommended regimen is the same as in adults. Use in patients with severe renal impairment (CC <30 ml / min) and impaired liver function. The dose of the drug should be reduced to 25 mg / day. Use in patients taking drugs that affect the safety of sildenafil The expediency of prescribing the drug at a dose of 25 mg / day in each individual case is considered. The drug is not intended for use in patients under the age of 18 years. Side effects The frequency of side effects is defined as: very often (≥ 1/10), often (≥ 1/100 to < 1/10), infrequently (≥ 1/1000 to < 1/100), rarely (≥ 1/10 000 to < 1/1,000), very rare (> 1/10,000) and not known (cannot be estimated from existing data). From the immune system: rarely – hypersensitivity reactions. From the nervous system: very often – headache; often – dizziness; infrequently – drowsiness, hypesthesia; rarely – cerebrovascular accident, fainting; unknown – transient ischemic attack, convulsions, provoking a convulsive seizure. On the part of the organ of vision: often – impaired vision, impaired color perception; infrequently – damage to the conjunctiva, eye diseases, impaired function of the lacrimal glands, other eye disorders; unknown – anterior ischemic optic neuropathy not associated with arteritis, retinal vascular occlusion, visual field defects. On the part of the organ of hearing and the vestibular apparatus: infrequently – dizziness, tinnitus; rarely – hearing loss. From the side of the heart: infrequently – palpitations, tachycardia; rarely – myocardial infarction, atrial fibrillation; unknown – ventricular arrhythmias, unstable angina pectoris, sudden cardiac death. From the side of the vessels: often – a feeling of “tides”; rarely – hypertension, hypotension. From the respiratory system and chest organs: often – nasal congestion; rarely – nosebleeds. From the digestive system: often – dyspepsia; infrequently – nausea, vomiting, dry mouth. From the side of the skin and soft tissues: infrequently – rash; unknown – Stevens-Johnson syndrome, toxic epidermal necrolysis. From the side of the muscular system and connective tissue: infrequently – myalgia. From the side of the kidneys and urinary system: infrequently – hematuria. From the reproductive system: infrequently – hematospermia, hemorrhages in the penis; unknown – priapism, prolonged erection. Other adverse reactions: infrequently – chest pain, fatigue. From the side of research: infrequently – an increase in heart rate. Contraindications Hypersensitivity to any component of the drug. the drug is contraindicated for use in patients receiving constantly or intermittently nitric oxide donators, organic nitrates or nitrates in any form, tk. sildenafil enhances the hypotensive effect of nitrates. Erectile dysfunction medications, including sildenafil, should not be used in men who are not recommended for sexual activity (for example, patients with severe cardiovascular disease such as unstable angina or severe heart failure). Sildenafil is contraindicated in patients with loss of vision in one eye associated with anterior ischemic optic neuropathy not associated with arteritis, regardless of whether this episode was associated with previous use of a PDE-5 inhibitor (see section “Precautions”). The safety of sildenafil has not been studied in the following subgroups of patients and therefore its use is contraindicated: severe hepatic insufficiency, arterial hypotension (blood pressure <90/50 mmHg), recent stroke or myocardial infarction, established diagnosis of hereditary degenerative retinal disease, such as pigmentary retinitis (some of these patients have genetic disorders of retinal phosphodiesterase). With caution The drug should be used for: anatomical deformity of the penis (including angulation, cavernous fibrosis or Peyronie's disease); diseases predisposing to the development of priapism (such as sickle cell anemia, multiple myeloma, leukemia, thrombocythemia); diseases accompanied by bleeding, exacerbation of peptic ulcer, heart failure; transferred in the last 6 months of life-threatening arrhythmia, arterial hypertension (blood pressure (BP)> 170/100 mm Hg. Art.). PrecautionsTo diagnose erectile dysfunction, determine their possible causes and select adequate treatment, it is necessary to take a complete medical history and conduct a thorough physical examination. Sexual activity poses a certain risk in heart disease; in this regard, before starting any therapy for erectile dysfunction, the doctor may consider it necessary to examine the cardiovascular system. Sexual activity is undesirable in patients with heart failure, unstable angina, myocardial infarction or stroke in the last 6 months, life-threatening arrhythmias, hypertension (BP > 170/100 mmHg) or hypotension (BP < 90/50 mmHg) st.). Sildenafil has a systemic vasodilatory effect, which leads to a transient decrease in blood pressure. This effect is of little or no consequence in most patients. However, before prescribing sildenafil, the physician must carefully weigh the risk of adverse vasodilatory effects in patients with certain comorbidities, especially during sexual activity. Increased susceptibility to vasodilators has been observed in patients with left ventricular outflow tract obstruction (eg, aortic stenosis, hypertrophic cardiomyopathy), as well as the rare multiple system atrophy syndrome, manifested by severe dysregulation of blood pressure from the autonomic nervous system. Since the combined use of sildenafil and alpha-blockers can lead to symptomatic hypotension in some susceptible patients, sildenafil should be administered with caution to patients taking alpha-blockers. The physician should inform patients about what actions to take if symptoms of postural hypotension appear. Sildenafil enhances the antiplatelet effect of sodium nitroprusside (nitric oxide donor) on human platelets in vitro. Serious cardiovascular events have been reported in post-marketing reports, including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmias, cerebrovascular bleeding, transient ischemic attacks, hypertension and hypotension, with a temporal association with sildenafil. Most, but not all, of these patients had cardiovascular risk factors. Many events occurred during or immediately after sexual intercourse; in several reports, cardiovascular events have occurred shortly after the use of sildenafil without sexual activity. It is impossible to determine whether these events are directly related to the intake of sildenafil or other factors. There are reports of prolonged erections over 4 hours and priapism (painful erections lasting over 6 hours); In the case when the erection lasts more than 4 hours, the patient should seek medical help. If emergency care is not provided, damage to the tissue of the penis can occur, resulting in a permanent loss of potency. The safety and efficacy of sildenafil in combination with other drugs intended for the treatment of erectile dysfunction have not been studied. In this regard, the use of such combinations is not recommended. Caution should be exercised when prescribing sildenafil to patients taking the protease inhibitor ritonavir, an 11-fold increase in the AUC value of sildenafil may occur. Data on patients with high serum levels of sildenafil are limited. This is expressed in a decrease in blood pressure, fainting, prolonged erection - cases are described in healthy volunteers who received 200-800 mg of sildenafil. Patients taking ritonavir are advised to reduce the dose of sildenafil to avoid side effects. Impact on vision. Cases of visual defects and cases of anterior ischemic optic neuropathy not associated with arteritis associated with the use of sildenafil and other PDE-5 inhibitors have been reported. If sudden visual defects occur, the patient should stop taking sildenafil and consult a doctor immediately (see section "Contraindications"). The film-coated tablet contains lactose. Sildenafil should not be administered to men with rare hereditary problems of galactose intolerance, the lactase deficiency or glucose-galactose malabsorption syndrome. Use during pregnancy and lactationV-car is not intended for use in women. Fertility A single oral dose of B-car at a dose of 100 mg in healthy volunteers was not accompanied by changes in sperm motility or morphology. Overdose In studies in healthy volunteers, a single dose of 800 mg of sildenafil caused the same side effects as lower doses, although the incidence rate increased. In case of overdose, supportive therapy is recommended. Renal dialysis does not increase the clearance of sildenafil due to its strong association with plasma proteins, sildenafil is not excreted by the kidneys. Interaction with other drugs and food With the simultaneous use of CYP3A4 inhibitors (such as ketoconazole, erythromycin, cimetidine), a decrease in the clearance of sildenafil was noted. Cimetidine (800 mg), which is a non-specific inhibitor of CYP3A4, when taken simultaneously with sildenafil (50 mg), causes an increase in plasma concentrations of sildenafil by 56%. A single dose of sildenafil at a dose of 100 mg simultaneously with erythromycin, a specific inhibitor of CYP3A4 (when taking erythromycin 2 times / day, 500 mg for 5 days), against the background of achieving a constant level of erythromycin in the blood, leads to an increase in the AUC of sildenafil by 182%. With the simultaneous use of sildenafil (once at a dose of 100 mg) and saquinavir, which is both an inhibitor of HIV protease and an inhibitor of CYP3A4 (when taking saquinavir 3 times / day at a dose of 1200 mg), against the background of achieving a constant level of saquinavir in the blood, the maximum concentration sildenafil in the blood increased by 140%, and AUC increased by 210%. Sildenafil did not affect the pharmacokinetic parameters of saquinavir. Stronger inhibitors of the CYP3A4 isoenzyme, such as ketoconazole or itraconazole, can cause more pronounced changes in the pharmacokinetics of sildenafil. Simultaneous use of sildenafil (once at a dose of 100 mg) and ritonavir, which is an inhibitor of HIV protease and a strong inhibitor of cytochrome P450 (when taking ritonavir 500 mg 2 times / day), against the background of achieving a constant level of ritonavir in the blood, the Cmax of sildenafil increased by 300 % (4 times), and AUC by 1000% (11 times). After 24 hours, the plasma level of sildenafil was approximately 200 ng / ml (comparative concentration with a single application of one sildenafil after 24 hours was 5 ng / ml). This is consistent with the effect of ritonavir on a number of drugs that are substrates of cytochrome P450. A single dose of an antacid (magnesium hydroxide / aluminum hydroxide) does not affect the bioavailability of sildenafil. Inhibitors of CYP2C9 (such as tolbutamide, warfarin), CYP2D6 (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazides and thiazide-like diuretics, ACE inhibitors and calcium antagonists do not affect the pharmacokinetic parameters of sildenafil. Simultaneous administration of azithromycin (500 mg / day for 3 days) does not affect the AUC, Cmax, Tmax, excretion rate constant and T1 / 2 of sildenafil or its main circulating metabolite. Sildenafil is a weak inhibitor of cytochrome P450 isoenzymes - 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IC50 150 µmol). It is unlikely that sildenafil can affect the clearance of substrates of these isoenzymes. Sildenafil enhances the hypotensive effect of nitrates both with long-term use and with acute indications. In this regard, the use of sildenafil in combination with nitrates or nitric oxide donators is contraindicated. Nicorandil is a hybrid of potassium channel activators and nitrates. Due to the presence of the nitrate component, a serious interaction with sildenafil is possible. With the simultaneous administration of the alpha-blocker doxazosin (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) in patients with benign prostatic hyperplasia with stable hemodynamics, the average additional reduction in systolic / diastolic blood pressure in the supine position was 7 /7 mmHg Art., 9/5 mm Hg. Art. and 8/4 mm Hg. Art., respectively, and in a standing position - 6/6 mm Hg. Art., 11/4 mm Hg. Art. and 4/5 mm Hg. Art., respectively. Rare cases have been reported in these patients of symptomatic postural hypotension, manifested in the form of dizziness (without syncope). In selected sensitive patients receiving alpha-blockers, the simultaneous use of sildenafil may lead to symptomatic hypotension. Signs of a significant interaction of sildenafil with tolbutamide (250 mg) or warfarin (40 mg), which are metabolized by CYP2C9, have not been identified. Sildenafil at a dose of 100 mg did not affect the pharmacokinetic parameters of HIV protease inhibitors at a constant level in the blood, such as saquinavir and ritonavir, which are both CYP3A4 substrates. Sildenafil (50 mg) did not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg). Sildenafil (50 mg) did not enhance the hypotensive effect of ethanol in healthy volunteers at a maximum blood ethanol level of 80 mg/ml on average. In patients with arterial hypertension, there were no signs of the interaction of sildenafil (100 mg) with amlodipine. The average additional decrease in blood pressure in the supine position is: systolic - by 8 mm Hg. Art., diastolic - 7 mm Hg. Art. There is no difference in the nature of side effects in patients treated with sildenafil in combination with antihypertensive agents and without them. There are no data on the interaction of sildenafil and non-specific phosphodiesterase inhibitors such as theophylline or dipyridamole. Grapefruit juice, which is a weak inhibitor of CYP3A4 metabolism in the intestinal wall, can lead to a moderate increase in plasma sildenafil. Influence on the ability to drive vehicles and work with dangerous devices and mechanismsV-car does not affect the ability to drive vehicles and work with dangerous devices and mechanisms. But since when taking the drug, a decrease in blood pressure is possible, the development of chromatopsia, blurred vision, one should carefully consider the individual effect of the drug in these situations, especially at the beginning of treatment and when changing the dosing regimen. Storage conditions Store in a place protected from moisture and light at a temperature not exceeding +25°C. Keep out of the reach of children. Shelf life 3 years. Do not use after the expiry date stated on the packaging. Release conditions Released from pharmacies by prescription. Packaging Tablets 50 mg: 2 tablets in a blister pack made of aluminum foil and PVC, together with instructions for medical use, are packed in a cardboard box. 4 tablets in a blister pack made of aluminum foil and PVC, together with instructions for medical use, are packed in a cardboard box. Tablets 100 mg: 2 tablets in a blisters made of aluminum foil and PVC, together with instructions for medical use, are packed in 1 or 2 blisters in a carton box. 20 tablets in a HDPE jar, packed with instructions for medical use in a cardboard box. Buy V-car tablets p/o 50mg No. 4x1 about 50mg №4x1