Index of drugs

Treatment of men with erectile dysfunction (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 50 mg or 100 mg of Sildenafil in the form of citrate.

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_max29%. 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 determinedin vitro 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. 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. Simultaneous use of sildenafil with nitric oxide eluting drugs (eg, amyl nitrite) or nitrates in any form. Sildenafil should not be used 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). Sildenafil is contraindicated in patients who have lost their sight in one eye as a result of non-arteritic anterior ischemic optic neuropathy, regardless of whether it was related to previous PDE5 inhibitor exposure. The use of the drug is contraindicated in patients with severe hepatic impairment, hypotension (blood pressure <90/50 mmHg), recent stroke or myocardial infarction, and in patients with inherited retinal degenerative changes such as retinal pigment degeneration.retinitis pigmentosa (a small proportion of these patients have genetically determined abnormalities of retinal phosphodiesterase) - the safety of sildenafil in these patients has not been studied.

Before pharmacological treatment, the patient should undergo a physical and physical examination to identify and determine the causes of erectile dysfunction. Before starting any treatment for erectile dysfunction, it is recommended to assess the patient's cardiovascular status. Before prescribing Sildenafil, it should be assessed whether the patient may be susceptible to vasodilating, particularly during sexual activity. Increased sensitivity to vasodilators is demonstrated by patients with left ventricular blood flow disorder (eg aortic stenosis or hypertrophic cardiomyopathy with narrowing of the outflow pathway) and a rare multiple organ system atrophy, characterized by a strong impairment of blood pressure control by the autonomic system.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. If you have sudden vision problems, stop taking sildenafil and consult a doctor immediately. Cases associated with the use of the product in cardiovascular dysfunctions, such as myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmias, cerebral haemorrhage, transient ischemic attack, hypertension or hypotension have been reported. Most, but not all of these patients belonged to the group with pre-existing risk factors for cardiovascular disease. Many disorders occurred during sexual intercourse or shortly after its completion, and in individual cases these disorders occurred shortly after application before sexual activity. 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. Sildenafil is not indicated for use in women and patients <18 years.

The drug is not indicated for use in women.

Very common: headache. Common: dizziness, blurred vision, blurred color vision, hot flushes, nasal obstruction, indigestion. Uncommon: drowsiness, hypoesthesia, conjunctivitis, eye diseases, lacrimation, other eye diseases, dizziness, tinnitus, palpitations, tachycardia, vomiting, nausea, dry mouth, skin rash, muscle pain, haematuria, bleeding with penis, hematospermia, chest pain, fatigue, fast 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 ischemic optic neuropathy, retinal vascular occlusion, visual field defects, ventricular arrhythmia, unstable angina, sudden cardiac death, priapism, prolonged erection, Stevens-Johnson syndrome and toxic Necrotic separation of the epidermis.

Orally. Adults: the recommended dose is 50 mg; it should be taken depending on the needs about 1 hour before 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. The maximum recommended frequency of use is once a day. 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), due to the reduced clearance of sildenafil, a 25 mg dose should be considered; 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 (with the exception of ritonavir not recommended concomitantly with sildenafil) or alpha blockers, consideration should be given to initiating sildenafil 25 mg. In order to minimize the risk of orthostatic hypotension, the patient's condition should be stable prior to initiation of treatment. If the medicine is taken with food, the onset of action may be delayed compared to taking an empty stomach.