Синегра®

General characteristics. Structure:

Active ingredient: 35,12 mg, 70,24 mg or 140,48 mg of a sildenafil of citrate that is equivalent to 25 mg, sildenafit 50 mg or 100 mg respectively.

Excipients: calcium hydrophosphate anhydrous, cellulose.

Microcrystallic PH 102, sodium of a kroskarmelloz, silicon dioxide colloid (aerosil 200), magnesium stearate.

Structure of a cover: polyethyleneglycol 3350 (macrogoal 4000), titanium E 171 dioxide, talc, FD & C Blue #2/индигокармин E 132 aluminum, iron oxide yellow E 172 and polyvinyl alcohol.

Pharmacological properties:

Pharmacodynamics. The effect of a sildenafil develops approximately in 30 - 60 minutes after reception. Expressiveness of an erection, in general, increases with increase in a dose of a sildenafil and increase in its concentration in plasma. Sildenafil causes decrease in systolic/diastolic arterial pressure, on average, on 8,4/5,5 mm of mercury which is most often noted within one-two hours after administration of drug. At reception Синегра® 25, Синегра® 50 and Синегра® 100 the identical effect on arterial pressure is observed and, therefore, this action of a sildenafil does not depend on a dose or the level of drug in plasma within dosages from 25 mg to 100 mg.

Sildenafil has no the direct weakening effect separately on a cavernous body, but strengthens action of an oxide of nitrogen by inhibition of phosphodiesterase of the type 5 (FDE 5) which is responsible for disintegration cyclic monophosphate guanine riboside (ts-GMF) in a cavernous body. When at sexual excitement there is a local release of an oxide of nitrogen, the inhibition of FDE 5 leads to increase in level ts-GMF in a cavernous body therefore there is a relaxation of unstriated muscles and inflow of blood to a cavernous body.

Pharmacokinetics. Синегра® it is quickly soaked up after intake and the maximum concentration in plasma is reached within from 30 to 120 minutes (on average 60 minutes). Absolute bioavailability of drug makes about 40%. At reception of a sildenafil along with greasy food the speed of absorption decreases in this connection time of achievement of the maximum concentration (Tmax) is slowed down, on average, up to 60 minutes and the maximum concentration (Cmax) in blood decreases to 29%. Sildenafil and his main N-desmetilny a metabolite contact proteins of plasma approximately for 96%. Linkng with proteins does not depend on the general concentration of drug.

Sildenafil is metabolized by preferential microsomal isoenzymes of a liver - CYP3A4 (the main way) and CYP2C9 (a minor way). The main metabolite which is formed as a result of N-desmetilirovaniya of a sildenafil is exposed to further metabolism. Concentration of a metabolite in plasma makes about 40% of concentration of a sildenafil and pharmacological action of a metabolite makes about 20% of pharmacological action of a sildenafil. After intake about 80% of a dose of drug also about 13% - with urine are allocated in the form of metabolites preferential with a stake.

Indications to use:

- disturbance of an erection.

Route of administration and doses:

The recommended dose of 50 mg in 1 hour prior to alleged sexual intercourse. Depending on effect the dose can be reduced to 25 mg or is increased to 100 mg. The maximum recommended dose of 100 mg of 1 times a day.

Features of use:

Sildenafil has system vazodilatiruyushchy property that can lead to passing lowering of blood pressure in this connection before purpose of the drug Sinegra®neobkhodimo carefully to weigh risk of undesirable manifestations at patients with cardiovascular diseases, especially against the background of sexual activity.

The raised susceptibility to vazodilatator is observed at patients with obstruction of an output path of a left ventricle (for example, an aortal stenosis, an idiopathic subaortal stenosis) and at patients with heavy disturbance of vegetative regulation of blood pressure.

At purpose of drug patients should be careful:

- with disturbance of cerebral circulation or life-threatening arrhythmia within the last 6 months;

- with hypotension (the ABP <90/50) or hypertensia (the ABP> 170/110);

- with the heart failure or coronary heart disease caused by unstable stenocardia;

- with a pigmental retinitis (minority of these patients inherited disorders of phosphodiesterase of a retina have).

In case of a condition of the erection proceeding more than 4 hours, patients have to ask for medical care immediately. If the priapism is not cured immediately, development of irreversible impotence is possible.

It is necessary to appoint with care the drug Sinegra® at combined use with ritonaviry as ритонавир considerably increases plasma concentration of a sildenafil by 11 times.

For decrease in risk of side effects at the patients receiving ритонавир it is recommended to reduce a dose of a sildenafil.

Simultaneous use of a sildenafil and alpha adrenoblockers, can lead to arterial hypotension at some patients. Therefore sildenafit doses, the exceeding 25 mg should not be accepted within 4 hours after reception of alpha adrenoblockers. At reception of the raised doses of a sildenafil and a doksazin in a dose of 4 mg development of postural hypotension within 1 - 4 hours after reception is possible.

Safety sildenafit at patients with the diseases which are followed by bleeding and patients with a round ulcer in the period of an aggravation is unknown.

Sildenafil it is necessary to apply with care at patients with anatomic deformation of a penis (including at an angulation, cavernous fibrosis or Peyron's disease) or at patients who have conditions contributing to development of a priapism (such as sickemia, multiple myeloma, leukemia).

Синегра® it is not intended for use for children and teenagers up to 18 years.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms. Against the background of administration of drug of Sinegra® of any negative influence on ability to drive the car or other technical means it was not observed. However as at administration of drug decrease in the ABP, development of a chromatopsia, the obscured sight is possible, it is necessary to inform patients on the danger connected with control of vehicles, service of the mechanical equipment and other potentially dangerous types of activity and shows consideration for individual effect of drug in the specified situations, especially in an initiation of treatment and at change of the mode of dosing.

Side effects:

- headache, dizziness, hyperemia of the person;

- tachycardia, hypotension, faints, nasal bleeding;

- vision disorder (change of color perception, increase in light sensitivity, sight misting), conjunctivitis, photofear;

- congestion of a nose, respiratory infection;

- dryness in a mouth, vomiting, a dysphagy;

- dyspepsia, diarrhea;

- rash, allergic reactions;

- dorsodynia, arthralgias;

- grippopodobny syndrome;

- infections of urinary tract, hypostasis of generative organs, long erection and/or priapism.

Interaction with other medicines:

Combined use of a sildenafil in a dose of 50 mg and nonspecific CYP inhibitor of Cimetidinum leads to increase in concentration of a sildenafil in plasma approximately for 50%.

Single dose of a sildenafil in a dose of 100 mg together with erythromycin, concentration - time" leads to increase in the area under a pharmacokinetic curve "(AUC) approximately for 180%.

The concomitant use was sildenafit once in a dose of 100 mg and by a sakvinavira, increase in Cmax of a sildenafil is promoted in plasma, on average for 140%, and by AUC - for 210%. Sildenafil does not exert impact on a pharmakokinetka of a sakvinavir.

Simultaneous use of a sildenafil and CYP3A4 inhibitors (such as кетоконазол, erythromycin or Cimetidinum) the clearance of a sildenafil can lower.

Sildenafit a concomitant use once in a dose of 100 mg and the ritonavir which is HIV protease inhibitor, and strong inhibitor of P450 cytochrome increase in Cmaxsildenafila is promoted approximately by 4 times, and by AUC - more than by 10 - 11 times.

The concomitant use of a sildenafil and the inductors CYP3A4 (for example, Rifampinum) lower the level of a sildenafil in plasma.

CYP2C9 inhibitors (such as Tolbutamidum, warfarin), CYP2D6 inhibitors (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), tiazida and tiazidopodobny diuretics, inhibitors the angiotensin-the turning enzymes (ATE), blockers of calcium channels do not exert impact on pharmacokinetics of a sildenafil.

At simultaneous use of a sildenafil in a dose of 100 mg with amlodipiny in a dose of 5 mg and 10 mg the arterial pressure (AP) in addition decreases approximately by 7-8 mm of mercury.

Contraindications:

- hypersensitivity to drug components;

- therapy by nitrates;

- children's and teenage age up to 18 years.

Storage conditions:

To store at a temperature not above 25 °C, in dry, protected from light, the place. To store in the place, unavailable to children! Period of storage 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 1 and 4 tablets in a blister strip packaging from a film of polyvinyl chloride and printing aluminum foil.

On 1 planimetric packaging with 1 or 4 tablets, or on 4 planimetric packagings with 1 tablet together with the application instruction in the state and Russian languages place in a pack from a cardboard.