Index of drugs

The drug is indicated for use in adult men with erectile dysfunction, 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 50 mg or 100 mg sildenafil; Table. powl. contain lactose. 1 tabl orally disintegrating contains 50 mg or 100 mg sildenafil; Table. submissive. start in the mouth contain aspartame and sorbitol.

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. 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 due to non-arteritic anterior ischemic optic neuropathy regardless of whether or not it has been associated with previous PDE5 inhibitor exposure. It is contraindicated in patients with severe hepatic impairment, hypotension (blood pressure <90/50 mmHg), recent stroke or myocardial infarction, and in patients with hereditary degenerative changes of the retina, such asretinitis pigmentosa (a small proportion of these patients have genetically determined disorders of retinal phosphodiesterase) - the safety of sildenafil patients.

Before pharmacological treatment, the patient should undergo a physical and physical examination to identify and determine the causes of erectile dysfunction. Before starting treatment, the cardiovascular status should be assessed and whether the patient may be susceptible to vasodilation, especially during sexual activity. Increased sensitivity to vasodilators is demonstrated by patients with impaired left-ventricular blood outflow (eg aortic stenosis or hypertrophic cardiomyopathy with narrowing of the outflow tract) or with a rare multiple organ system atrophy, characterized by a strong disturbance of blood pressure control by the autonomic nervous 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).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. To date, the safety and efficacy of concomitant use of sildenafil with other PDE5 inhibitors, pulmonary arterial hypertension (PAH) therapies with sildenafil or other treatments for erectile dysfunction have not been studied - the use of such combinations is not recommended. The concomitant use of sildenafil and ritonavir is not recommended. Sildenafil is not indicated for use in women and patients <18 years. Table. powl. contain lactose - do not use in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. Table. those that disintegrate in the mouth contain aspartame - they can be harmful to patients with phenylketonuria; they also contain sorbitol - do not use in patients with hereditary fructose intolerance.

The drug is not indicated for use in women.

Very common: headache. Common: dizziness, blurred vision, blurred color vision (green vision, chromatopsia, blue vision, red vision, yellow vision), blurred vision, sudden redness, hot flush, nasal congestion, nausea, indigestion. Uncommon: rhinitis, hypersensitivity reactions, drowsiness, hypoaesthesia, lacrimation disorders (including dry eye syndrome, lacrimation, increased tearing), eye pain, photophobia, photopsy, ocular hyperaemia, glaring eyes, conjunctivitis, dizziness, tinnitus, palpitations, tachycardia, hypertension, hypotension, nosebleeds, sinus congestion, gastroesophageal reflux disease, vomiting, upper abdominal pain, dry mouth, rash, muscle pain, limb pain, hematuria, pain in the chest, fatigue, feeling hot, accelerated heart rate. Rare: cerebrovascular accident, transient ischemic attack, convulsions, recurrent convulsions, syncope, anterior ischemic optic neuropathy not associated with atheritis (NAION), retinal vascular occlusion, retinal hemorrhage, atherosclerotic retinopathy, retinal disorders, glaucoma, visual field defects, vision double, reduced visual acuity, myopia, visual impairment, vitreous vitreousness, iris disorder, mydriasis, peripheral vision around the light sources, eye edema, swollen eye, eye disorder, conjunctival hyperaemia, eye irritation, abnormal sensations in the eye, eyelid edema scleral discoloration, hearing loss, sudden cardiac death, myocardial infarction, ventricular arrhythmia, atrial fibrillation, unstable angina, throat tightness, nasal mucosa edema, dry nose, hypoaesthesia, Stevens-Johnson syndrome, toxic epidermal necrolysis, bleeding from the penis, priapism, bloody sperm, increased erection, irritability.

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. In the elderly and in patients with mild or moderate renal impairment (creatinine clearance 30-80 ml / min), no dose adjustment is necessary. In patients with severe renal impairment (creatinine clearance <30 ml / min), in patients with impaired liver function (e.g.with cirrhosis), due to the decreased 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 (except ritonavir not recommended) or alpha-blocker therapy, consideration should be given to initiating sildenafil 25 mg.Way of giving. Tablet it should be swallowed whole. The disintegrating tablet should be placed in the mouth, on the tongue, where it rapidly disintegrates under the influence of saliva and can easily be swallowed. The tablet can be swallowed with or without liquid. It is difficult to remove the orodispersible tablet from the oral cavity intact. The orodispersible tablet is fragile, therefore it should be taken immediately after removal from the blister. Orally disintegrating tablets may be used as an alternative to coated tablets in patients who have difficulty swallowing. If the medicine is taken with food, the onset of action may be delayed compared to taking an empty stomach.