Product Name: Sildenaver
Active substance: Sildenafil
Selective inhibitor of cGMP-specific PDE5, which is responsible for the breakdown of cGMP in the cavernous body of the penis. Actively enhances the relaxing effect of nitric oxide in the corpus cavernous smooth muscle and increases blood flow to the penis. When activated, the chain NO-cGMP which is observed during sexual arousal, inhibition of PDE5 increases cGMP in the cavernous body. The pharmacological effect is achieved only if there is sexual stimulation. Activity against PDE5 10-10,000 times greater activity against other PDE isoenzymes (1, 2, 3, 4, 6).
Treatment of erectile dysfunction characterized by the inability to achieve or maintain an erection of the penis sufficient for satisfactory sexual intercourse. Effective only in sexual stimulation.
Contraindications and Cautions:
- concomitant use of nitric oxide donators or organic nitrates or nitrites in any LF;
- concomitant use of other drugs that stimulate the erection of ritonavir;
- contraindications to have sex, including unstable angina, severe heart failure;
Loss of vision due to ischemic optic neuropathy, severe liver failure, hypotension, myocardial infarction, stroke, or a history of hereditary retinal degenerative diseases, female age up to 18 years.
Diseases of the cardiovascular system, syndrome of multiple system atrophy, anatomical deformation of the penis, priapism, sickle cell anemia, multiple myeloma, leukemia, concomitant use of alpha-blockers.
For LF containing lactose (optional): lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Very often - more than 1/10 - often more than 1/ 100 or less than 1 /10, infrequently - more than 1/ 1000 and less than 1/100, rare - more than 1/ 10000 and less than 1/1000.
On the part of the immune system: rarely - hypersensitivity.
The nervous system: very often - headache, often - dizziness, rarely - drowsiness, hypoesthesia, rarely - stroke, fainting, frequency unknown - transient ischemic attack, seizures, including recurrent.
Part of the vision: often - blurred vision, impaired color vision, rarely - the defeat of the vision including the defeat of the conjunctiva. On the part of the organ of hearing: Infrequent - vertigo, tinnitus, rarely - deafness.
From the CCC : often - "tides" , rarely - palpitations, tachycardia, increased heart rate , rarely - increased or decreased blood pressure , myocardial infarction , atrial fibrillation, the frequency is unknown - ventricular arrhythmias , unstable angina , sudden cardiac death .
The respiratory system: often - nasal congestion, rarely - nosebleeds.
From the digestive system: often - indigestion, rarely - nausea, and vomiting, dry mucous membranes of the mouth.
For the skin: rarely - a skin rash.
On the part of the musculoskeletal system: Infrequent - myalgia.
Reproductive system: the frequency is unknown - priapism, a prolonged erection.
Other: rarely - pain in the chest, fatigue.
Inside, approximately 1 hour before planned sexual activity. An adult dose - 50 mg 1 time per day. Given the efficacy and tolerability of the dose may be increased to 100 mg or decreased to 20 mg. The maximum daily dose - 100 mg.
In mild and moderately severe chronic renal failure (creatinine clearance 30-80 ml ??/ min), dose adjustment is not required. In severe renal failure (creatinine clearance less than 30 ml / min) or hepatic failure start with 20 mg.
Before taking Sildenaver should be succeeded again to a stable state patient taking alpha-blockers, Sildenaver start with 20 mg.
Inhibitors of CYP3A4 and CYP2C9 isoenzymes decrease metabolism and increase the concentration of Sildenaver in the blood, treatment should be started with a dose of 25 mg. Ritonavir increases the AUC of Sildenaver at 11 times the combined use of these drugs is not recommended. Saquinavir, ketoconazole, itraconazole, erythromycin increase AUC Sildenaver more than 3 times. Grapefruit juice may moderately increase the concentration of Sildenaver in the blood. Inductors isozymes CYP3A4 and CYP2C9 increase metabolism and reduce the concentration of Sildenaver in the blood.
Nicorandil (due nitrate component) can potentiate the side effects of Sildenaver. Enhances the effects of organic nitrates and other nitrogen oxide donators II, co-administration of these drugs and Sildenaver is contraindicated. Simultaneous treatment with alpha-blockers may result in orthostatic hypotension, especially in the first 4 hours after administration of Sildenaver. May enhance the effect of antihypertensive drugs. Enhances the antiplatelet effect of sodium nitroprusside in vitro.
The drug should be stored out of reach of children, dry place at a temperature not exceeding 30 ° C. Shelf life - 5 years.