Potentsagra

General characteristics. Structure:

Active ingredient: 50 mg of a sildenafil of citrate in 1 capsule.

Pharmacological properties:

Pharmacodynamics. Drug selectively inhibits the tsGMF-dependent phosphodiesterase of type 5 which is contained preferential in unstriated muscles of a cavernous body and interferes with destruction of tsGMF. Increase in level of the last leads to decrease in intracellular concentration of calcium and relaxation of smooth muscle cells of a cavernous body with the subsequent increased filling of sine with blood (against the background of increase in an arterial blood-groove in a penis) and a prelum of the taking-out veins.

Drug strengthens and increases duration of the erection which resulted from sexual stimulation. Efficiency of drug remains at prolonged treatment (1 year).

Inhibits phosphodiesterase of type 6 of a retina (though is weaker, than phosphodiesterase of type 5, selectivity of action 10:1) and can cause disturbances of color sight. Increases antiagregantny and dezagregatsionny effects of nitrogen oxide (II) and its donors, blocks formation of blood clots of ex vivo. At introduction in high doses considerably increases a bleeding time (does not exert impact on a blood clotting time). The single dose inside in doses higher than 30 mg is followed by increase in the tsGMF level in plasma. Expands both arterial, and venous vessels, causes decrease in systolic and diastolic arterial pressure and increase in heart rate. Has antidiuretic effect.

Does not influence reproductive function. Does not exert impact on morphology, mobility and viability of spermatozoa, volume and viscosity of an ejaculate. Has no teratogenic, mutagen, clastogene and cancerogenic properties.

Pharmacokinetics. At intake on an empty stomach it is quickly and almost completely soaked up. The maximum concentration in plasma is reached in 0,5 — 2 hours. Absolute bioavailability makes 41% (is exposed to presistemny metabolism). Reception of greasy food reduces extent of absorption and the maximum concentration in blood, increases the period of achievement of the maximum concentration in blood for 1 hour. For 96% contacts proteins of a blood plasma. The elimination half-life makes 4 hours (can vary from 2 to 8 hours). Collects in an organism: at use 3 times a day within 9 days cumulation makes 36%.

At patients of advanced age the clearance decreases, concentration of a sildenafil in a blood plasma increases. At a renal failure value of the maximum concentration in a blood plasma is twice higher, than at healthy. At patients with stable cirrhosis the clearance of a sildenafil is reduced by 46%, the maximum concentration in a blood plasma is 47% higher.

Drug is exposed to intensive biotransformation. The metabolite has similar with sildenafily effect, but concedes to it on activity approximately for 50%. To 80% of metabolites of a sildenafil also 14% — with urine are removed with excrements.

Indications to use:

Disturbances of an erection (organic, psychogenic, mixed), including at patients with a diabetes mellitus, obesity, after a radical prostatectomy or an injury of a spinal cord.

Route of administration and doses:

Accept inside, in 1 hour prior to sexual intercourse. For most of patients the recommended dose makes 0,05 g. At insufficient efficiency against the background of good tolerance the dose can be increased to 0,1 g.

The maximum recommended frequency rate of use of drug — 1 time a day.

At use of drug for patients 65 years are aged more senior, than patients with abnormal liver functions, with a heavy renal failure, and also in case of simultaneous use of drugs — CYP3A4 inhibitors (a P450 cytochrome isoenzyme) increase in concentration of a sildenafil in a blood plasma is noted. In this regard increase in efficiency of drug and strengthening of side effects is possible (it is necessary to consider expediency of purpose of drug in a dose of 0,025 g).

Features of use:

Drug is not intended for use for patients aged 18 years are younger.

Precautionary measures. Before administration of drug for diagnosis of disturbances of an erection, definition of its possible reasons and the choice of adequate methods of treatment it is necessary to collect the full medical anamnesis and to conduct careful urological and all-clinical examination, especially at patients with the accompanying cardiovascular diseases at which the increased sexual activity is undesirable (for example, severe forms of coronary heart disease and an idiopathic hypertensia).

Purpose of high doses is not recommended to elderly patients. Frequent (more than 1 time a day) use in high doses increases risk of emergence of by-effects. Patients with the accompanying coronary heart disease belong to the category of the increased risk. Ratio assessment advantage/risk is necessary at patients with heart failure, low volume of the circulating blood. With care appoint to patients with arterial hypertension (the ABP of 170/110 mm of mercury.) and arterial hypotension (ABP of 90/50 mm of mercury.). With extra care appoint to the patients with the accompanying arterial hypertension receiving multicomponent hypotensive pharmacotherapy.

With care appoint to patients at the diseases contributing to development of a priapism (a sickemia, a multiple myeloma, leukemia).

It is not recommended to combine with other drugs for treatment of erectile dysfunction.

Side effects:

At administration of drug the headache, dizziness, a vazodilatation (inflows), hypotension, an adynamy, a nose congestion, dacryagogue, disturbance sacred and color perception, sight clearnesses, dyspepsia, diarrhea, nausea, an abdominalgiya, a lyumbalgiya, an arthralgia, a mialgiya, a hyper tone of muscles, sleeplessness, short wind, skin rashes, predisposition to an infection of respiratory and urinary tract, a long painful erection are possible.

Interaction with other medicines:

Strengthens the orthostatic hypotension caused by nitroglycerine, antiagregantny effects of Sodium nitroprussidum.

Cimetidinum, кетоконазол, итраконазол, erythromycin, саквинавир, ритонавир and some other drugs (CYP3A4 inhibitors) increase concentration of a sildenafil in a blood plasma, rifampicin, etc. the inductors CYP3A4 reduce concentration in a blood plasma.

Contraindications:

Hypersensitivity, therapy by nitrates. Heavy abnormal liver functions and kidneys, anatomic deformations of a penis, a multiple myeloma, acute leukoses, a sickemia, the increased tendency to bleedings, a hereditary pigmental retinitis, an aggravation of a peptic ulcer of a stomach and duodenum, severe forms of an arterial hypertension and hypotonia, anamnestic instructions on the heart attack which is had in the previous 6 months and a stroke, life-threatening arrhythmias, heart failure, unstable stenocardia, age up to 18 years.

Overdose:

Symptoms: feeling of heat, dizziness, face reddening, headache, disturbance of clearness of sight, dispeptic phenomena, lowering of arterial pressure. Symptomatic therapy; dialysis is inefficient.

Heavy abnormal liver functions and kidneys, anatomic deformations of a penis, a multiple myeloma, acute leukoses, a sickemia, the increased tendency to bleedings, a hereditary pigmental retinitis, an aggravation of a peptic ulcer of a stomach and duodenum, severe forms of an arterial hypertension and hypotonia, anamnestic instructions on the heart attack which is had in the previous 6 months and a stroke, life-threatening arrhythmias, heart failure, unstable stenocardia, age up to 18 years.

Issue conditions:

According to the recipe

Packaging:

Capsules on 50 mg in a blister strip packaging No. 2.