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Viagra (sildenafil citrate)

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Information

Sildenafil Used For Erectile Dysfunction is a potent selective inhibitor of cGMP-specific PDE-5.



Mechanism of action

The implementation of the physiological mechanism of erection is associated with the release of nitric oxide (NO) in the cavernous body during sexual stimulation. This, in turn, leads to an increase in the level of cGMP, the subsequent relaxation of smooth muscle tissue of the cavernous body and an increase in blood flow.

Sildenafil Used For Erectile Dysfunction does not have a direct relaxing effect on the isolated cavernous human body, but enhances the effect of nitric oxide by inhibiting PDE-5, which is responsible for the disintegration of cGMP.

Selective Is Viagra Only Used For Erectile Dysfunction against PDE5 in vitro, its activity against PDE5 superior activity against other known PDE isoenzymes: PDE-6 — 10 times; PDE-1 more than 80 times; PDE-2, PDE-4, PDE-7 PDE–11 more than 700 times. Sildenafil Used For Erectile Dysfunction is 4000 times more selective for PDE-5 than PDE-3, which is crucial because PDE-3 is one of the key enzymes in the regulation of myocardial contractility.

A prerequisite for the effectiveness of Sildenafil Used For Erectile Dysfunction is sexual stimulation.

Sildenafil Used For Erectile Dysfunction restores impaired erectile function in conditions of sexual stimulation by increasing blood flow to the cavernous bodies of the penis.

Visual impairment

In rare cases, during post-approval use of all of the inhibitors of PDE5, including Viagra Erectile Dysfunction Treatment, reported NESN is a rare disease and the cause of the decrease or loss of vision. Most of these patients had risk factors, such as decreased ratios of excavation diameter to optic disc (stagnant disc), age over 50, diabetes, hypertension, CHD, hyperlipidemia, and Smoking. In an observational study evaluated whether recent use of drugs class of inhibitors PDE-5 with an acute onset NESN. The results indicate approximately a 2-fold increase in risk NESN within 5T1/2 after application of the PDE-5 inhibitor. According to published literature, the annual incidence of npins IS 2.5–11.8 cases per 100,000 men aged ≥50 years in the General population. Patients should be advised to stop How Effective Is Viagra For Erectile Dysfunction therapy in case of sudden loss of vision and consult a doctor immediately.

Persons who have already had a case NESN have an increased risk of relapse NESN. Therefore, the doctor should discuss this risk with such patients, as well as the potential chance of adverse effects of PDE-5 inhibitors. PDE-5 inhibitors, including Dose Of Viagra For Erectile Dysfunction, in such patients should be used with caution and only in situations where the expected benefit outweighs the risk. In patients with episodes of development PINZN with loss of vision in one eye receiving Sildenafil Used For Erectile Dysfunction is contraindicated (see "Contraindications").

A small number of patients with hereditary retinitis pigmentosa have genetically determined disorders of the PDE of the retina. Information about the safety of the drug Sildenafil Used For Erectile Dysfunction in patients with retinitis pigmentosa absent, so these patients should not be used Viagra Cure Erectile Dysfunction (see "Contraindications").

The pharmacokinetics of Sildenafil Used For Erectile Dysfunction in the recommended dose range is linear.

Suction. After intake of Viagra Erectile Dysfunction Treatment is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Viagra For Diabetes Erectile Dysfunction at a concentration of about 1.7 ng/ml (3.5 nm) inhibits the activity of PDE-5 50%. After a single dose of Sildenafil Used For Erectile Dysfunction 100 mg average Cmax free Does Viagra Work For Erectile Dysfunction in plasma men is about 18 ng/ml (38 nm). Cmax when taking Sildenafil Used For Erectile Dysfunction inside fasting is achieved for an average of 60 minutes (from 30 to 120 minutes). When taken in combination with fatty foods, the rate of absorption decreases: Cmax decreases by an average of 29%, and Tmax increases by 60 minutes, but the degree of absorption does not change significantly (AUC decreases by 11%).

Distribution. The average Vss of Sildenafil Used For Erectile Dysfunction is 105 l. the Association of Sildenafil Used For Erectile Dysfunction and its main circulating N-demethyl metabolite with plasma proteins is about 96% and does not depend on the total concentration of the drug. Less than 0.0002% of the dose of Sildenafil Used For Erectile Dysfunction (an average of 188 ng) was found in sperm 90 minutes after taking the drug.

Metabolism. Can Viagra Be Used For Erectile Dysfunction is metabolized mainly in the liver by the action of CYP3A4 isoenzyme (main pathway) and CYP2C9 isoenzyme (minor pathway). The main circulating active metabolite, formed as a result of N-demethylation of Treatment For Erectile Dysfunction Before Viagra, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Sildenafil Used For Erectile Dysfunction, and its activity against PDE-5 in vitro is about 50% of the activity of Sildenafil Used For Erectile Dysfunction. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Which Is Better For Erectile Dysfunction Viagra Or Cialis. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.

Breeding. The total clearance of Sildenafil Used For Erectile Dysfunction is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Sildenafil Used For Erectile Dysfunction is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).

Contraindications

hypersensitivity to Sildenafil Used For Erectile Dysfunction or any other component of the drug;

application in patients receiving constantly or intermittently nitric oxide donators, organic nitrates or nitrites in any form, as Viagra Temporary Erectile Dysfunction enhances the hypotensive effect of nitrates (see "Interaction»);

the combined use of inhibitors of PDE5, including Sildenafil Used For Erectile Dysfunction, called guanylate cyclase stimulants such as riociguat, because it can lead to symptomatic hypotension;

concomitant use with other agents for the treatment of erectile dysfunction (safety and efficacy of Viagra For Psychological Erectile Dysfunction when used together has not been studied (see. "Special instructions»);

lactose intolerance, lactase deficiency, glucose-papacosma malabsorption;

severe liver failure (class C classification for child-Pugh);

simultaneous administration of ritonavir;

severe cardiovascular diseases (severe heart failure, unstable angina, stroke or myocardial infarction during the last 6 months, life-threatening arrhythmias, hypertension (BP >170/100 mm Hg). art.) or hypotension (blood PRESSURE <90/50 mm Hg.art.) (see "Special instructions»);

patients with episodes of development partizanai anterior ischemic optic neuropathies (NESN) with loss of vision in one eye;

hereditary retinitis pigmentosa (see special instructions»);

according to the registered indication is not intended for use in women;

according to the registered indication is not intended for use in children under 18 years.

With caution: anatomic deformity of the penis (angulation, cavernous fibrosis or Peyronie's disease) (see "Special instructions"); diseases of, predisposing to the development of priapism (sickle-cell anemia, multiple myeloma, leukemia, thrombocythemia) (see "Special instructions"); diseases accompanied by haemorrhage; ulcer disease of stomach and duodenum in the acute phase; liver dysfunction; severe renal insufficiency (Cl creatinine <30 ml/min); patients with an episode of partizanai development of the anterior ischemic optic neuropathies in history (see "Special instructions); simultaneous reception of blockers α-adrenergic receptors.

Use during pregnancy and breast-feeding

According to the registered indication, the drug is not intended for use in women.



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