Sildenafil pills 50mg №20

Sildenafil-SZ

International non-proprietary name: Sildenafil

Dosage Form: film-coated tablets

Composition

1 tablet, film coated, contains:

dosage 25 mg: active ingredient: sildenafil citrate in terms of sildenafil - 25 mg of excipients (core): microcrystalline cellulose - 50.0 mg; lactose monohydrate (milk sugar) - 61.5 mg; croscarmellose sodium (primelloza) - 7.5 mg; Povidone (middle molecular weight polyvinylpyrrolidone) - 4.5 mg; Magnesium stearate - 1.5 mg; excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 2.0 mg; titanium dioxide E 171 - 1.145 mg; macrogol (polyethylene glycol 3350) - 1.01 mg; talc - 0.74 mg; aluminum varnish based brilliant blue - 0.096 mg; iron oxide (II) yellow E 172 - 0.0085 mg; iron oxide (II) black E 172 - 0.0005 mg).

dosage 50 mg: active ingredient: sildenafil citrate in terms of sildenafil - 50 mg of excipients (core): microcrystalline cellulose - 54.0 mg; lactose monohydrate (milk sugar) - 74.0 mg; Croscarmellose sodium (primelloza) - 10.0 mg; Povidone (polyvinylpyrrolidone middle molar) - 10.0 mg; magnesium stearate - 2.0 mg; excipients (shell): Opadry II (polyvinyl alcohol,partially hydrolyzed - 2.4 mg; titanium dioxide E 171-1.374 mg; macrogol (polyethylene glycol 3350) - 1.212 mg; talc - 0.888 mg; aluminum blue varnish based on brilliant blue - 0.1152 mg; iron oxide (II) yellow E 172 - 0,0102 mg; ferric oxide (II) black E 172 - 0.0006 mg).

dosage of 100 mg: active ingredient: sildenafil citrate in terms of sildenafil - 100 mg of excipients (core): microcrystalline cellulose - 83.5 mg; lactose monohydrate (milk sugar) - 83.5 mg; croscarmellose sodium (primelloza) - 15.0 mg; Povidone (polyvinylpyrrolidone middle molar) - 15.0 mg; magnesium stearate - 3.0 mg; excipients (shell): Opadry II (polyvinyl alcohol, partially hydrolyzed - 3.6 mg; titanium dioxide E 171-2.061 mg; macrogol (polyethylene glycol 3350) - 1.818 mg; talc - 1.332 mg; aluminum varnish based on brilliant blue - 0.1728 mg; iron oxide (II) yellow E 172 - 0.0153 mg; iron oxide (II) black E 172 - 0.0009 mg).

Pharmacotherapeutic group of the drug:

The treatment for erectile dysfunction is a PDE5 inhibitor.

Pharmacology

Pharmacodynamics

Sildenafil is a powerful selective inhibitor of cycloguanosine monophosphate (cGMP) - specific phosphodiesterase type 5 (PDE5).

Mechanism of action

The implementation of the physiological mechanism of erection is associated with the release of nitric oxide (NO) in the cavernous body during sexual stimulation. This, in turn, leads to an increase in the level of cGMP, subsequent relaxation of the smooth muscle tissue of the cavernous body and an increase in blood flow.Sildenafil does not have a direct relaxing effect on the isolated cavernous body of a person, but enhances the effect of nitric oxide (NO) by inhibiting PDE5, which is responsible for the breakdown of cGMP. Sildenafil is selective for PDE5 invitro, its activity against PDE5 is superior to that for other known phosphodiesterase isoenzymes: PDE6 - 10 times; PDE1 - more than 80 times; PDE2, PDE4, PDE7-PDE11 - more than 700 times. Sildenafil is 4,000 times more selective with respect to PDE5 compared with PDE3, which is of paramount importance, since PDE3 is one of the key enzymes in the regulation of myocardial contractility.

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 people (18-45 years). Age does not have a clinically significant effect on the incidence of side effects.

With mild (creatinine clearance (CK) 50-80 ml / min) and moderate (CK 30-49 ml / min) degree of renal failure, the pharmacokinetics of sildenafil after a single dose of 50 mg are not changed. With severe renal failure (CK ≤ 30 ml / min), the clearance of sildenafil decreases, which leads to an approximately twofold increase in AUC (100%) and Cmax (88%) compared with those in normal renal function in patients of the same age group.

Liver function disorders

In patients with cirrhosis of the liver (stages A and B according to Child-Pugh classification), the clearance of sildenafil is reduced, which leads to an increase in the AUC value (84%) and Cmax (47%) compared with those in normal liver function in patients of the same age groups. The pharmacokinetics of sildenafil in patients with severe hepatic impairment (Child-Pugh stage C) has not been studied.

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 with sexual stimulation.

Contraindications

Hypersensitivity to sildenafil or to any other component of the drug. Use in patients who constantly or intermittently donate nitric oxide, organic nitrates or nitrites in any form, as sildenafil enhances the hypotensive effect of nitrates (see the section "Interaction with other drugs"). Safety and the effectiveness of Sildenafil when combined with other means of treating erectile dysfunction has not been studied, therefore, the use of such combinations is not recommended uetsya (see. "Special Instructions" section) at the registered indication the drug Sildenafil is not intended for use in children under 18 years under the registered indication the drug Sildenafil is not intended for use in women lactase deficiency,lactose intolerance, glucose-galactose malabsorption. The simultaneous use of sildenafil with ritonavir is not recommended.

Anatomical deformity of the penis (angulation, cavernous fibrosis or Peyronie's disease) (see the section "Special Instructions"). Diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia) (see section "Special instructions"). Diseases accompanied by bleeding. Exacerbation of gastric ulcer and 12 duodenal ulcer. Hereditary retinitis pigmentosa (see section "Special instructions"). heart failure, unstable angina, suffered a myocardial infarction, stroke or life-threatening arrhythmias in the last 6 months, arterial hypertension (BP> 170/100 mm Hg) or hypotension (BP <90/50 mm Hg) (see section "Special instructions"). In patients with episodes of development of anterior non-arteritis ischemic neuropathy of the optic nerve (in history).

Pregnancy and Breastfeeding

According to the registered indication of the drug is not intended for use in women.

Inside The recommended dose for most adult patients is 50 mg approximately 1 hour before sexual activity. Given the 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 use is once a day.

With mild and moderately severe renal failure (CK 30-80 ml / min), dose adjustment is not required, with severe renal failure (CK <30 ml / min) - the dose of sildenafil should be reduced to 25 mg.

Liver function disorders

Since the elimination of sildenafil is impaired in patients with liver damage (in particular, in case of cirrhosis), the dose of Sildenafil should be reduced to 25 mg.

Combined use with other medicines

When combined with ritonavir, the maximum single dose of Sildenafil should not exceed 25 mg, and the frequency of use - 1 time in 48 hours (see the section "Interaction with other drugs"). When used together with cytochrome CYPZA4 isoenzyme inhibitors (erythromycin, saquinavir, Ketoconazole, itraconazole), the initial dose of Sildenafil should be 25 mg (see section "Interaction with other drugs"). To minimize the risk of postural hypotension in patients taking α-blockers, taking Sildenafil should be started only after stabilization of hemodynamics is achieved in these patients. It should also consider the feasibility of reducing the initial dose of sildenafil (see sections "Special instructions" and "Interaction with other drugs").

Dosage adjustment of Sildenafil is not required.

With a single dose of sildenafil at a dose of up to 800 mg, adverse events were comparable to those with a lower dose, but were more common. Symptomatic treatment. Hemodialysis does not accelerate the clearance of sildenafil, since the latter is actively associated with plasma proteins and is not excreted by the kidneys.

Do not use beyond the expiration date printed on the package.

In a dry, dark place, at a temperature not higher than 25 ° C. Keep out of the reach of children.