Index of drugs

Treatment of erectile dysfunction in men, i.e. inability to obtain or maintain penile erection sufficient to undergo sexual intercourse. Sexual stimulation is required for effective action of the drug.

1 tabl powl. contains 100 mg of Sildenafil as citrate; Table. contain lactose.

Sildenafil is a potent selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5), which is responsible for the distribution of cGMP in the corpus cavernosum. It triggers an erection through its peripheral action. It does not exhibit a direct relaxant effect on isolated human corpora cavernosa, but significantly increases the diastolic effect of nitric oxide on this tissue. During sexual arousal, when the metabolic reactions in which nitric oxide and cGMP are involved, inhibition of PDE5 activity by sildenafil causes an increase in cGMP concentration in the corpus cavernosum. Sexual arousal is essential for sildenafil to have its intended pharmacological action. Sildenafil causes a slight and transient decrease in blood pressure, in most cases without significant clinical significance. Sildenafil is rapidly absorbed after oral administration, reaching C_max during 30-120 minutes after administration on an empty stomach. Using sildenafil with a meal reduces its absorption rate; T delay_max is 60 minutes and the average reduction is C_max - 29%. Sildenafil and its main circulating N-desmethyl metabolite bind to plasma proteins in approximately 96%. Sildenafil is primarily metabolised by the cytochrome P450 enzyme system, including CYP3A4 and, to a lesser extent, CYP2C9. The main metabolite of sildenafil arises as a result of its N-demethylation. It exhibits sildenafil-like selectivity for phosphodiesterases. The metabolite's action on PDE5 was determinedinvitro at 50% of the potency of the parent drug, whereas its concentration in the blood corresponds to 40% of the concentration of sildenafil. The N-desmethyl metabolite of sildenafil undergoes further changes; his T_0,5 is about 4 hours. T_0,5 Sildenafil is 3-5 hours. After oral administration, sildenafil is excreted as metabolites, mainly in the faeces (80%) and to a lesser extent in the urine (13%).

Hypersensitivity to the active substance or to any of the excipients. Use with nitric oxide eluting drugs (eg, amyl nitrite) or nitrates in any form. Do not use in men for whom sexual activity is not indicated (eg in patients with severe diseases of the cardiovascular system, such as unstable angina or severe heart failure). Patients who lost vision in one eye due to non-arteritic anterior ischemic optic neuropathy (NAION) regardless of whether or not it was associated with previous PDE5 inhibitor exposure. Due to the lack of safety data, sildenafil is contraindicated in patients with: severe hepatic insufficiency, hypotension (blood pressure <90/50 mmHg), recent stroke or myocardial infarction and in patients with hereditary degenerative changes of the retina, such as howretinitis pigmentosa (a small proportion of these patients have genetically determined disorders of retinal phosphodiesterase).

Before pharmacological treatment, the patient should undergo a physical and physical examination to identify and determine the causes of erectile dysfunction. Before commencing treatment, the condition of the cardiovascular system should be assessed and whether the patient may be susceptible to vasodilating, especially during sexual activity. Increased sensitivity to vasodilators is demonstrated by patients with narrowing of the left ventricle outflow pathway (eg aortic stenosis or hypertrophic cardiomyopathy with narrowing of the outflow tract) or patients with a rare multiple organ system atrophy, characterized by significant impairment of blood pressure control by an autonomic system nervous.The drug should be used with caution in patients with anatomical penile deformities (such as bending, corpora cavernosa fibrosis or Peyronie's disease) and with conditions predisposing to priapism (eg sickle cell disease, multiple myeloma or leukemia). To date, the safety and efficacy of concomitant use of sildenafil with other treatments for erectile dysfunction have not been studied - the use of such combinations is not recommended. Patients should be advised that in the event of a sudden visual disorder, they must stop taking sildenafil and consult a physician immediately. Sildenafil enhances the antiaggregating effect of sodium nitroprusside. There is no information on the safety of sildenafil in patients with bleeding disorders or active peptic ulcer disease - in these patients, sildenafil should only be used after careful consideration of the potential benefits and risks. Caution should be exercised when administering sildenafil to patients using alpha-blocker medications due to the risk of hypotension, which usually occurs within 4 hours of sildenafil administration. In order to reduce the risk of orthostatic hypotension, the patient's condition of alpha-blocker therapy should be haemodynamically stable before starting treatment with sildenafil. The concomitant use of sildenafil and ritonavir is not recommended. Sildenafil is not indicated for use in women and patients <18 years. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The drug is not indicated for use in women.

Very common: headache. Common: dizziness, blurred vision, blurred color vision, hot flush, nasal congestion, indigestion. Uncommon: drowsiness, hypoaesthesia, conjunctivitis, eye disorder, lacrimation, other eye disorders, labyrinthine dizziness, tinnitus, palpitations, tachycardia, vomiting, nausea, dry mouth, skin rash, muscle pain, pain in the eyes chest, fatigue, accelerated heart rate. Rarely: hypersensitivity reactions, cerebrovascular accident, syncope, hearing loss, hypertension, hypotension, myocardial infarction, atrial fibrillation, nasal bleeding. Not known: transient ischemic attack, convulsions, recurrent seizures, non-arteritic anterior ischemic optic neuropathy (NAION), retinal vascular occlusion, visual field defects, ventricular arrhythmias, unstable angina, sudden cardiac death, priapism, prolonged erection, syndrome Stevens-Johnson, toxic epidermal necrolysis, priapism, accelerated erection.

Orally. Adults: the recommended dose is 50 mg; it should be taken depending on the needs about 1 hour before planned sexual activity. Depending on the effectiveness and tolerability of the drug, the dose can be increased to 100 mg or reduced to 25 mg. The maximum recommended dose is 100 mg. Sildenafil is not recommended more frequently than once a day.Special groups of patients. Elderly patients and patients with mild or moderate renal impairment (creatinine clearance 30-80 ml / min) do not need to modify the dose. In patients with severe renal impairment (creatinine clearance <30 ml / min) and in patients with hepatic impairment (eg cirrhosis), a 25 mg dose should be considered due to decreased sildenafil clearance; depending on the efficacy and tolerability of the drug, the dose may be increased to 50 mg or 100 mg. In patients co-administering CYP3A4 inhibitors (except ritonavir not recommended) or alpha-blocker therapy, consideration should be given to initiating sildenafil 25 mg.Way of giving. The tablet can be divided into two equal doses along the dividing line. If the medicine is taken with food, the onset of action may be delayed compared to taking an empty stomach.