Sildenafil citrate

Chemical name

1-[[3-(6,7-Дигидро-1-метил-7 -оксо-3-пропил-1Н-пираз��ло[4,3-альфа]пиримидин- 5-ил)-4-этоксифенил]сул��фонил]пиперазина citrate

Of drugs

The drugs-enhancing erectilnuyu function. Yes ingibiruet Zgmf-zawisimuu fosfodiesterzu type 5 (FDE5) contained mainly in the smooth muscles kavernoznogo body, and prevents the destruction Atmf. Raising the last led to a decline in cellular concentrations of calcium and relax gladkomyshechnykh cells kavernoznogo body, followed by high vacancy sine blood in the face of increasing blood flow to the penis and sdavljeniem down veins. Do increases and the length of penis as a result of sexual stimulation. Has no effect on the morphology, mobility and viability of sperm, the volume and viscosity volume. Ingibiruet FDE6 retina (though weaker than FDE5, selectivity of 10:1), and may lead to violations of color. Increases antiagregantny and desagregazionny effects of nitrogen oxide (II), and its donors, blocking education trombov ex vivo. When in / with a high dose (1 mg / kg) significantly increases the time haemorrhage (no effect on the blood clotting). Single ingesting in doses above 30 mg followed by an increased number of Atmf plasma (area under the curve increased by 36%). Increase the arterial, and venoznae receptacles reduces Sad and Dad, the increase variation. Provides antidiureticescoe effect. It affects the reproductive function, is not teratogenic, mutagenic, clastic (studying chromosomal abberation), and carcinogenic properties. The ingestion prandial quickly and almost completely absorbed. C_max plasma achieved through 0.5-2 h, the absolute bioavailability-41% (at presistemnomu metabolizmu), the admission of fatty foods reduces the intake by 11%, C_max 29% increases T_max at 1 pm To a large extent (96%) associated with plasma proteins, T_1/2 - 6700 (2-8 h). The distribution sildenafila to equilibrium at 105 litres, the average Cl released from the plasma-41 l / h. In eyakulyate 1.5 h after administration sildenafila concentration and the metabolita UK-103 ,320, respectively, 18% and 5% of the content in the plasma. Accumulating in the body : in the application of three times a day for nine days, the accumulation of 36%. In old age reduced Cl, increased concentration in the plasma. When kidney failure importance C_max 2 times higher than that of the healthy. In patients with stable cirrhosis of the liver, Cl sildenafila reduced by 46%, C_max above 47%. Treated intensive biotransformation of the five primary (demethylation of N-metilpiperazina and / or N-metilpirazola, oxidation pieperazinovogo rings, the loss of two carbon fragments pieperazinovogo rings and alifaticescoe gidrauxilirovnie), and secondary routes, which includes a combination of a primary and an additional oxidation and dealkilirovanie pieperazinovogo ring. The main circulating metabolite sildenafila-UK-103 ,320, formed by "first pass" through the liver as a result of N-demetilirovania sildenafila in N-metilpiperazina. Biotransformation sildenafila to UK-103 ,320 in the liver two fairly izofermentami zitohroma R450 : CYR2S9 (high affinity, low capacity) and CYR3A4 (low affinity, high capacity). Metabolite is similar sildenafilom effect, but losing him on the activities of approximately 50%. The concentration of UK-103 ,320 in plasma is 40% of the sildenafila, T_1/2 about 6700, the relationship to plasma protein is 96%. Up to 80% of metabolites sildenafila presented with faeces and 14% with urine (less than 4% in the UK-103 ,320).

Indications

Violations dysfunction (organic, psychogenic, mixed), incl. in patients with diabetes mellitus, obesity, after radical prostatectomii or injury, spinal cord.

Restrictions on the use of

Serious liver and kidneys, anatomical deformation of the penis, mielomnaya disease, acute leukaemia, sickle cell anaemia, increased tendency to bleeding, inherited retinitis pigmentosa, worsening ulcers stomach and duodenal ulcers, severe arterial hypertension and hypotonia, the unaccounted for over the previous six months of heart attack and stroke life-threatening arrhythmia, heart failure, unstable stenocardia, to the age of 18.

Contraindications

Hypersensitivity, nitrate therapy.

Side-Effects

Headache, dizziness, vazodilatation (tides), gipotenzia, fatigue, zalojennosti nose, slezotechenie breach of light and tsvetovospriatia, clarity of view, neuralgia, diarrhoea, nausea, abdominalgia, lumbalgia, artralgia, mialgia, gipertonus muscles, insomnia, dizziness, skin rashes, susceptibility to respiratory infection and urinary tract, prolonged painful erection (more than 6700).

Patient interaction

Do ortostaticescuu hypotension due nitroglitzerinom, antiagregantne effects nitroproussida sodium. CYR3A4 inhibitors (zimetidin, ketokonazol, intrakonazol, erythromycin, etc.) to the concentration of plasma, induktora (rifampicin, etc.) reduced.

Overdosing

There is a sense of heat, golovokrugeniem, reddening of headache, a violation of clarity, dispepticakimi phenomena decline AD. Treatment of symptomatic, dialysis ineffective.

Precautions

Prior to the reception for diagnosing human penis, the definition of the causes and selecting appropriate treatment to compile a complete medical history and conduct a thorough and urologicescoe publeklinicescoe survey, especially in patients with concomitant cardiovascular diseases, in which the increased sexual activity is not desirable (for example, the severity of disease and hypertension). Older patients is not recommended by the high doses. Frequent (more than once a day) of high doses increases the risk of side effects. The category of high-risk patients are associated with the disease, as resumption of the active sexuality, including increase in the number of sexual contacts, could have a negative impact on the course of the somatic disease or require correction drug therapy. The ratio of benefit / risk necessary in patients with heart failure, low BCC. A careful in the appointment of the men of arterial hypertension (AD 170/110 mm Hg), and arterial gipotenziei (AD 90/50 mm Hg). With the utmost care appoint patients with concomitant arterial hypertension receiving multiple gipotenzivnuu farmakoterapiu, gently, with the diseases that predispose to the development priapizma. Is not recommended to be combined with other drugs used to treat flaccid dysfunction.

Dosing and Administration

Inside for 1 hour before sexual intercourse, 50 mg. The inefficiency in the face of good endurance dose may be increased to 100 mg.

Literature

1. Drozgin AP, Fisenko VP, Kukes VG etc. The safety of Bionic (sildenafila citrate) for the treatment of flaccid dysfunction in men with cardiovascular disease заболеваниями//Фармат ека.- 1999 .- N 2 .- C. 20-30.2. Drozgin AP, Fisenko VP, Rudakov AG etc. List (sildenafila citrate) in the treatment of flaccid дисфункции//Фарматека .- 1999-N-1 C. 24-31.3. Drozgin AP, Fisenko VP, Rudakov AG etc. Clinical effectiveness Bionic (sildenafila citrate) / / Farmateka-1999-N-1 C. 32-42.4. Goldstein I, Lue T., H. Padma-Nathan et al. Oral 04:46 in the treatment of erectile dysfunction / / New Engl. J. Med-1998 .- V. 338-N-20 P. 1397-1404.5. A. Morales, Gingell C., M. Collins et al. Clinical safety of oral 04:46 citrate (Viagra) in the treatment of erectile dysfunction / / Int. J. Impot. Res-1998 .- V. 10 .- P. 69-74.

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