Viasil

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of a sildenafil (in the form of citrate).

Excipients: cellulose microcrystallic, potato starch, magnesium stearate, lactoses monohydrate, опадрай blue (talc, polyethyleneglycol, titanium dioxide, alcohol polyvinyl, diamond blue (E133), indigo carmine (E132), orange yellow (E110), aluminum hydroxide.

The drug used at erectile dysfunction.

Pharmacological properties:

Pharmacodynamics. Selectively inhibits the phosphodiesterase of type 5 (FDE5) which is contained preferential in unstriated muscles of a cavernous body and interferes with destruction of tsGMF. Increase in the tsGMF level leads to decrease in intracellular concentration of calcium 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 degree and increases a prodozhitelnost of the erection which resulted from sexual stimulation. Efficiency of drug remains at prolonged treatment (during 1 year).

Sildenafil inhibits eye retina FDE6 (though is weaker, than FDE6, selectivity of action 10:1) and can cause disturbances of color sight.

Sildenafil increases antiagregantny and dezagregatsionny effect of nitrogen oxide (II) and its donors, blocks formation of blood clots of ex vivo. At use of drug in high doses the bleeding time considerably increases (does not exert impact on a blood clotting time).

The single dose in a dose higher than 30 mg is followed by increase in the tsGMF level in plasma. Both arterial, and venous vessels extend, causing decrease in the systolic and diastolic ABP, increase in ChSS.

Has antidiuretic effect.

Does not influence reproductive function: on morphology, mobility and viability of spermatozoa, volume and viscosity of an ejaculate.

Teratogenic, mutagen, clastogene and cancerogenic properties are noted.

Indications to use:

The erectile dysfunction which is characterized by inability to reach or keep the penis erection sufficient for satisfactory sexual intercourse.

Sexual stimulation is necessary for effective action of a sildenafil.

Route of administration and doses:

Viasil's pill is taken inside. Use for adult patients. For most of patients the recommended dose makes 50 mg, applied in 1 hour prior to sexual intercourse. Depending on efficiency and portability of drug, the dose can be increased to the maximum recommended dose of 100 mg or is reduced to 25 mg. Frequency of reception of the maximum recommended dose makes once a day.

Use for elderly patients. At patients 65 years with a liver and heavy renal failure are more senior, and also at simultaneous use of strong inhibitors of P450 ZA4 cytochrome (кетоконазол, итраконазол, erythromycin, саквинавир), use of drug in an initial dose of 25 mg as higher concentration in plasma can increase both efficiency, and frequency of side reactions is recommended.

Use for patients with a renal failure. With a renal failure of easy and moderate severity (clearance of creatinine within 30-80 ml/min.) dose adjustment is not required from patients.

Use for patients with an abnormal liver function. As at patients with an abnormal liver function (for example, at cirrhosis) the clearance of a sildenafil is reduced, it is recommended to use a dose of 25 mg.

Use for the patients accepting other drugs. Considering data on interaction of a sildenafil at its concomitant use with ritonaviry, it is recommended not to exceed the maximum single dose of 25 mg of a sildenafil within 48 hours.

Use of a sildenafil in an initial dose of 25 mg is recommended for the patients receiving at the same time isoenzyme inhibitors: CYP3A4 (for example, erythromycin, саквинавир, кетоконазол, итраконазол).

 For the purpose of decrease to a minimum of probability of development of postural hypotension, patients have to be in a stable state when performing treatment, alpha adrenoblockers prior to use of a sildenafil. Besides, in such cases it is recommended to begin use of a sildenafil with lower doses.

Features of use:

Drug is not appointed for use for patients aged up to 18 years.

Before use of drug for diagnosis of disturbance 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 hg) and arterial hypotension (the ABP of 90/50 mm hg). 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.

Sildenafil is not intended for use for women. In researches of influence of the sildenafil accepted inside on reproductive function at rats and rabbits teratogenic action, disturbances of fertility or side effect on peri-both post-natal fetation and the newborn is not revealed.

The corresponding controlled tests at women at pregnancy and a lactation it was not carried out.

Influence of a sildenafil on ability to driving of motor transport and to control of mechanisms was not studied. In clinical tests of a sildenafil cases of dizziness and decrease in sight were registered, patients have to be informed on individual effect of drug on an organism before driving of the car or control of mechanisms.

With care to appoint drug at anatomic deformation of a penis, a multiple myeloma, acute leukoses, a sickemia, the increased tendency to bleedings, a hereditary pigmental retinitis, a peptic ulcer of a stomach and a 12-perstny gut in an aggravation stage, severe forms of an arterial hypertension, anamnestic instructions to the previous 6 months postponed in a heart attack or a stroke, life-threatening arrhythmias, heart failure, unstable stenocardia.

According to post-market researches the tranzitorny ischemic attacks synchronized use of a sildenafil.

In case of an erection which remains more than 4 hours and a priapism the patient should ask immediately for medical care in order to avoid damage of tissues of penis and irreversible impotence.

In clinical tests it was shown that sildenafit can cause system vasodilatation that leads to passing pressure decrease of blood. For most of patients it practically does not implicate. However before purpose of a sildenafil the doctor should consider carefully possible effects of such vasodilating effect for this specific patient taking into account his state, especially in combination with sexual activity. Sildenafil is contraindicated to patients with hypersensitivity to vazodilatator, including the patients having the complicated outflow of blood from a left ventricle (for example, at a stenosis of an aorta, a hypertrophic subaortic stenosis), and patients with a rare syndrome of the multiple system atrophy which is shown heavy disturbance of autonomous regulation of arterial pressure.

The front ischemic visual neuropathy which is not connected with arteritis (NAION, non-arteritic anterior ischemic optic neuropathy), leading to decrease in sight or to its loss was in rare instances noted at post-market researches at use of all FDE5 inhibitors, including sildenafit. Doctors should discuss with patients the increased risk of development of this disturbance at those who already transferred NAION earlier. It is necessary to inform patients that in case of sudden loss of sight it is necessary to stop reception of a sildenafil and to consult with the doctor.

It is necessary to appoint with care sildenafit to the patients accepting alpha adrenoblockers since at the few more sensitive of them it can lead to symptomatic hypotension. For decrease to a minimum of probability of development of postural hypotension, patients have to have a steady condition of a hemodynamics when performing treatment by alpha blockers prior to use of a sildenafil. It is recommended to begin use of a sildenafil with lower doses. Besides, doctors need to instruct patients about what they should do in case of symptoms of postural hypotension. To the patients who were already receiving FDE5 inhibitors in an optimum dose, it is necessary to begin use of alpha blockers with the lowest dose. At patients with an unstable state the risk of symptomatic hypotension at the accompanying use of FDE5 inhibitors is increased.

Safety of the combined use of FDE5 inhibitors and alpha adrenoblockers can be reflected in other indicators, including reduction of intravascular volume and use of other anti-hypertensive drugs. As sildenafit has system vazodilyatatorny effect, it can strengthen hypotensive effect and other anti-hypertensive medicines.

Small part of patients with an inborn pigmental retinitis has genetic disorders of phosphodiesterase of a retina. Since there are no data on safety of use of a sildenafil for patients with a pigmental retinitis, to appoint sildenafit to such patients follows with care.

In researches on thrombocytes of the person of in vitro it was shown that sildenafit potetsirut antiagregantny action of Sodium nitroprussidum (the donor of nitrogen oxide). There are no data on safety of use of a sildenafil for patients with bleedings or active round ulcers therefore such patients should appoint sildenafit with care. Drugs for treatment of erectile dysfunction have to be used with care at patients with anatomic deformations of a penis (an angulation, cavernous fibrosis, Peyroni's disease) and at patients with the diseases contributing to development of a priapism (such as sickemia, multiple myeloma or leukemia).

Safety and efficiency of a combination of a sildenafil with other means for treatment of erectile dysfunction are not studied therefore use of such combinations is not recommended.

In post-market and clinical trials it was reported about insignificant quantity of cases of sudden decrease or a hearing loss at use of FDE5 inhibitors, including sildenafit. Most of these patients had risk factors of sudden decrease or a hearing loss. No relationship of cause and effect between reception of FDE5 inhibitors both sudden decrease and a hearing loss was revealed. It is necessary to inform patients that in case of sudden decrease or a hearing loss it is necessary to stop reception of a sildenafil and to consult with the doctor.

Since Viasil contains lactose, men should not appoint him with rare hereditary diseases: inborn galactosemia, deficit of lactase, glucose/galactose sprue.

Side effects:

Undesirable manifestations usually were passing and easy or moderate on the expressiveness.

With the fixed doses the frequency of undesirable manifestations increased in researches at increase in a dose.

The main undesirable manifestations in researches with selection of a dose which reflect the mode of use of the recommended doses better were similar to the undesirable manifestations revealed in researches with the fixed doses.

The most often noted undesirable phenomena included a headache and inflows (increase in inflow of blood to face skin). The main side effects of the sildenafil accepted with selection of a dose, observed in placebo - controlled tests and noted> sildenafit =2% of the patients accepting with a frequency of more placebo (in brackets the occurrence % in group of placebo is specified):

From a nervous system and sense bodys: a headache of 16% (4%), dizziness of 2% (1%), rushes of blood to the person of 10% (1%), a vision disorder (change of color perception, increase in light sensitivity, sight misting) of 3% (0%).

From respiratory system: congestion of a nose of 4% (2%).

From a GIT: dyspepsia of 7% (2%), diarrhea of 3% (1%).

From urinogenital system: infections of urinary tract of 3% (2%).

From integuments: pour 2% (1%).

At use of the doses exceeding the recommended, undesirable manifestations were similar with stated above, but were noted, as a rule, more often.

In the analysis of these clinical trials with double blind placebo control, vklyuchashchy more than 700 of observations with reception of placebo and more than 1300 – with reception of a sildenafil, various frequency of occurrence of the myocardial infarction (MI) and mortality because of cardiovascular disturbances at the patients receiving was not revealed sildenafit, in comparison with the receiving placebos. Frequency to THEM made 1,1 for 100 patients/years as at the men accepting sildenafit, and at the receiving placebos. Mortality because of cardiovascular disturbances made 0,3 on patients/years as well as at the men accepting sildenafit, and at the receiving placebos.

The side effects of a sildenafil observed in placebo - controlled tests and meeting with frequency less than 2% (communication with reception of a sildenafil is not clear).

From a nervous system and sense bodys: uneasiness and tranzitorny full amnesia, disturbances of cerebral circulation, the tranzitorny ischemic attacks, an adynamy, dizziness, migraine, an ataxy, a tremor, neuralgia, weakening of reflexes, paresthesia, a hyperesthesia, a faint, a depression, a sleep disorder (sleeplessness/drowsiness), conjunctivitis, a photophobia, hemorrhages in an eyeglobe, a mydriasis, a cataract, a xerophthalmia, pain in eyeglobes and ears, a ring in ears, deafness.

From CCC and blood: arterial hypotension, orthostatic hypotension, tachycardia, heartbeat, myocardium ischemia, stenocardia, a cardiomyopathy, heart failure, changes on an ECG, including AV blockade, a cardiac standstill, thrombosis of vessels of a brain, anemia, a leukopenia, arrhythmia of ventricles, arterial hypertension, a myocardial infarction and fibrillation of auricles.

From respiratory system: pharyngitis, sinusitis, laryngitis, bronchitis, диспноэ, increase in quantity of a phlegm, strengthening of cough, bronchial asthma.

From a GIT: a glossitis, an ulitis, stomatitis, dryness in a mouth, a dysphagy, an esophagitis, nausea, gastritis, a gastroenteritis, colitis, rectal bleeding, change of biochemical hepatic indicators, vomiting.

From a metabolism: thirst, a hypernatremia, gout, a hyperuricemia, labile diabetes, hyper - and a hypoglycemia.

From urinogenital system: nocturia, frequent urination, cystitis, urine incontience, disturbance of an ejaculation, anorgazmiya, hypostasis of generative organs, gynecomastia.

From a musculoskeletal system: arthritis, arthrosis, an ossalgiya, a mialgiya, a myasthenia, a rupture of sinews, tendosinovit, a synovitis, ostealgias.

From integuments: urticaria, herpes simplex, itch, skin ulcerations, contact dermatitis, exfoliative dermatitis.

Others: peripheral hypostases, including face edema, pain syndromes, including breast t abdominal pain, accidental falling, wounds and bruises, perspiration, fever, photosensitization, shock, allergic reactions.

When carrying out post-marketing observations the following undesirable manifestations were noted.

Disturbances of immune system: hypersensitivity reactions (including skin rash).

Disturbances of a nervous system: convulsive attacks, series of convulsive attacks.

Disturbances of urinogenital system: long erection, priapism and hamaturia.

Disturbances of sense bodys: hyperemia of eyes, diplopia, temporary loss of sight, increase in VGD.

Vascular disorders: hypotension, faints, nasal bleedings.

Hearing disorder: it was reported about insignificant quantity of cases of sudden decrease or a hearing loss at use of FDE5 inhibitors, including sildenafit.

At emergence above the listed side reactions, and also any side reaction which is not mentioned in the instruction needs to see a doctor.

Interaction with other medicines:

Sildenafil is metabolized, mainly, under the influence of isoenzymes of P450 CYP3A4 cytochrome (the main way) and 2C9 (an additional way). Therefore the inhibition of these isoenzymes of a liver can reduce clearance of a sildenafil, and stimulation of these ikhoferment can increase clearance of a sildenafil.

It is not necessary to combine drug with treatment by nitrates (nitroglycerine, etc. drugs of this group), Molsidominum, other donators of an oxide of nitrogen. Sildenafil strengthens the orthostatic hypotension caused by nitroglycerine, antiagregantny effects of a nitroprussil of sodium.

Cimetidinum, кетоконазол, интраконазол, 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.

Influence of other medicines. Pharmacokinetic data of clinical tests showed that CYP2C9 inhibitors (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazide and tiazidopodobny diuretics, APF inhibitors and blockers of calcium channels do not influence pharmacokinetics of a sildenafil.

AUC of an active metabolite of a sildenafil increases by 62% at reception of loopback and kaliysberegayushchy diuretics and for 102% at reception of nonspecific beta adrenoblockers.

Grapefruit juice is weak CYP3A4 inhibitor and can cause slight increase of level of a sildenafil in plasma.

Single doses of antacids (magnesium/aluminium hydroxide) do not influence bioavailability of a sildenafil.

At healthy male volunteers azithromycin influence (500 mg/day within 3 days) on AUC, the maximum concentration of Cmax, Tmax, a constant of speed of elimination and an elimination half-life of a sildenafil and its major circulating metabolites was not revealed.

Influence of a sildenafil on medicines. Sildenafil is weak inhibitor of isoenzymes of P450, 1A2, 2C9, 2C19, 2D6, 2E1 and 3F4 cytochrome (1C50> 150 microns). At achievement of peak concentration of a sildenafil in plasma about 1 micron at use of the recommended doses it is improbable that sildenafit changed clearance of substrates of these mzoferment.

In three special researches of interaction of drugs to patients with a benign hyperplasia of a prostate (BPH, benign prostatic hyperplasia) with a stable state at therapy doksazoziny were at the same time appointed alpha adrenoblocker доксазозин (4 mg and 8 mg) and sildenafit (25, 50 and 100 mg). In population of this research average additional decrease blood pressure in horizontal position and in vertical position was observed. When sildenafit and доксахозин were at the same time appointed to patients with a stable state at therapy doksazoziny, exceptional cases of symptomatic postural hypotension were celebrated. In such cases symptoms of patients included dizziness, but faints were not noted. Sildenafit a simultaneous nznacheniye to the patients accepting alpha blockers, can bring from symptomatic hypotension at a small part of patients with high sensitivity. Interaction with Tolbutamidum (250 mg) or warfarin (40 mg), drugs which are metabolized by isoenzymes of P450 CYP2C9 cytochrome was not revealed.

Sildenafil (100 mg) did not influence pharmacokinetics of a steady condition of inhibitors of HIV protease, a sakvinavir and ritonavir – the drugs which are CYP3A4 substrates. Sildenafil (50 mg) did not exponentiate increase in a bleeding time, вызываемго aspirin (150 mg).

Sildenafil (50 mg) did not exponentiate hypotensive effect of alcohol at healthy volunteers with the average level алкголя 0,08%.

Interaction was not noted at simultaneous apply a sildenafila (100 mg) and an amlodipina to patients with hypertensia. Average additional pressure decrease of blood in horizontal position made 8 mm hg for systolic and 7 mm hg under diastolic pressure.

The analysis of data of safety did not reveal distinctions of a profile of side effects at the patients accepting sildenafit separately and together with angipertenzivny drugs.

Contraindications:

Means for treatment of erectile dysfunction, including, sildenafit, should not be used at men to whom sexual activity is not recommended (for example, patients with a serious cardiovascular illness, such as unstable stenocardia or heavy heart failure). It is contraindicated to patients with loss of sight on one eye owing to front ischemic optical neuropathy.

Safety of a sildenafil was not studied in the following subgroups of patients and therefore its use is contraindicated: a heavy liver failure, arterial hypotension (the ABP <90/50 mm hg), recently had stroke or a myocardial infarction and hereditary degenerative diseases of a retina, such as pigmental retinitis.

Hypersensitivity to any of drug components, therapy by nitrates.

Overdose:

Symptoms: feeling of heat, dizziness, face reddening, headache, disturbance of clearness of sight, dispeptic phenomena, lowering of arterial pressure.

Treatment. symptomatic therapy, dialysis it is not effective.

Storage conditions:

List B. Drug should be stored in packaging of the producer, in the place, unavailable to children, at a temperature from 15 °C to 25 °C. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 2, 4 or 10 tablets in a blister strip packaging. On 1 blister strip packaging in a cardboard pack with the application instruction.