Pharmacological action
A selective inhibitor of cyclo-guanosine monophosphate (cGMP)-specific PDE5. PDE5, responsible for the breakdown of cGMP, is found not only in the penile cavernous body, but also in the vessels of the lungs. Restores damaged erectile function and provides a natural response to sexual arousal. Sildenafil does not have a direct relaxing effect on the cavernous body, but actively enhances the relaxing effect of nitric oxide on this tissue. During sexual arousal, local release of NO under the influence of sildenafil leads to inhibition of PDE5 and an increase in cGMP levels in the cavernous body, resulting in relaxation of smooth muscles and increased blood flow in the cavernous body. As a PDE5 inhibitor, sildenafil increases the content of cGMP in the smooth muscle cells of the pulmonary vessels and causes their relaxation. In patients with pulmonary hypertension, taking sildenafil leads to vasodilation of the lungs and, to a lesser extent, other vessels. Sildenafil is selective for PDE5 in vitro. Its activity against PDE5 is superior to that of other known PDE isoenzymes: PDE 6 involved in light signal transmission in the retina – 10 times; PDE 1-80 times; PDE 2, PDE 4, PDE 7-PDE 11-more than 700 times. Sildenafil’s activity against PDE5 is more than 4,000 times higher than its activity against PDE3, a cAMP-specific PDE involved in heart contraction. Sildenafil may cause mild and transient color discrimination (blue/green). The suspected mechanism of color vision impairment is considered to be inhibition of PDE6, which is involved in the process of light transmission in the retina. In vitro studies have shown that the effect of sildenafil on PDE6 is 10 times less than its activity against PDE5.
Indications
The drug is used to treat disorders of potency, expressed by the inability to achieve or maintain an erection of the sexual organ, in order to ensure a full sexual intercourse. The Active ingredient of the drug (sildenefril) is effective only when exposed to sexual arousal.
Recommendations for use
Treatment of erectile dysfunction: take orally approximately 1 hour before the planned sexual activity. A single dose is 50 mg. Depending on the efficacy and tolerability, the dose can be increased to 100 mg or reduced to 25 mg. The maximum single dose is 100 mg. The maximum frequency of application is 1 time/day. For elderly patients over 65 years of age and with concomitant renal or hepatic impairment, the dose is 25 mg. Pulmonary hypertension: inside 20 mg 3 times / day with an interval of about 6-8 hours, regardless of food intake. The maximum daily dose is 60 mg. In patients with impaired renal function, no dose adjustment is required, but if the dose is poorly tolerated, the dose is reduced to 20 mg 2 times / day.
Contraindications
Before taking this drug, you should consult a doctor, as there are some contraindications:
- individual intolerance was sildenafil or any other component of the drug;
- moved six months ago, heart attack, stroke;
- rehabilitation after abdominal surgery;
- chronic heart disease, and vascular system;
- not suitable for boys under the age of 18;
- hepatic failure, cirrhosis of the liver;
- renal failure in chronic form;
- degenerative changes of the retina;
- not intended for use by women.
Side effects
Like any drug, Vildegra has side effects:
- nervous system: headache, possible dizziness, drowsiness, sometimes fainting, stroke (rare), convulsions;
- cardiovascular system: tachycardia, (rare) high (low) blood pressure, myocardial infarction (rare);
- visual organs: visual impairment, color perception;
- hearing organs: noise in the ears, sometimes with vertigo;
- respiratory: rhinitis symptoms (nasal congestion), epistaxis (rare);
- musculoskeletal system: myalgia (muscle pain);
- gastrointestinal: dyspepsia, rarely vomiting, and sometimes nausea;
- in the region of the genital organs: rarely – hematospermia (blood in semen), bleeding from the penis, rarely, priapism (prolonged and painful erection not associated with sexual arousal), prolonged erection;
- allergic manifestations: very rarely – skin rash;
- other: sudden fatigue, chest pain.
Description
Tablets with a prolonged release, film-coated dark blue color, round, biconvex; on a cross-section, two layers are visible — the core is white or almost white in color and the film shell.
Special instructions
Before taking sildenafil for the treatment of erectile dysfunction, a cardiovascular examination should be performed. Caution should be used in patients with anatomical deformities of the penis (such as angulation, cavernous fibrosis or Peyronie’s disease) and people with diseases that predispose to the development of priapism (such as sickle cell anemia, multiple myeloma or leukemia). It should not be used in patients for whom sexual activity is undesirable. Use with caution in patients with a tendency to bleeding, with peptic ulcer of the stomach and duodenum in the acute phase, with hereditary retinitis pigmentosa. Sildenafil is not used in patients under 18 years of age. Effect on the ability to drive motor vehicles and manage mechanicsmi Sildenafil does not affect the ability to drive motor vehicles and manage mechanisms.
Active ingredient
Sildenafil
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For adults as prescribed by a doctor, For men
Indications
Erectile Dysfunction
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