Contraindications

hypersensitivity to Cobra Vega 120 Mg 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 Vega 120 Mg enhances the hypotensive effect of nitrates (see "Interaction»);

the combined use of inhibitors of PDE5, including Sildenafil Tablets Vega Extra Cobra, 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 Sildenafil Vega Extra 130 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.

The pharmacokinetics of Sildenafil Vega Extra 130 in the recommended dose range is linear.

Suction. After intake of Vegab Extra is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Sildenafil Vega Extra 130 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 Vega Extra 120 100 mg average Cmax free Sildenafil Vega Extra 130 in plasma men is about 18 ng/ml (38 nm). Cmax when taking Sildenafil Vega Extra 130 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 Cobra Vega Extra is 105 l. the Association of Sildenafil Vega Extra 130 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 Vega Extra 130 (an average of 188 ng) was found in sperm 90 minutes after taking the drug.

Metabolism. Vegah Extra 120 Indication 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 Sildenafil Vega Extra 130 Mg Cobra, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Cobra Vega Extra Strong 120 Mg, and its activity against PDE-5 in vitro is about 50% of the activity of Vegah Cobra. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Sildenafil Vega Extra 130. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.

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

Sildenafil Vega Extra 130 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.

Vega Extra 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 Cobra Vega Extra Strong 120 Mg 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. Vega Extra 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 Vega Extra 130 is sexual stimulation.

Sildenafil Vega Extra 130 restores impaired erectile function in conditions of sexual stimulation by increasing blood flow to the cavernous bodies of the penis.

Clinical data

In a placebo-controlled cross-examination of patients with proven early age macular degeneration (n=9), Sildenafil Vega Extra 130 was well tolerated at a single dose of 100 mg. There were no clinically significant changes in vision evaluated by special visual tests (visual acuity, Amsler lattice, color perception, color simulation, Humphrey perimeter and photostress).

Efficiency. The efficacy and safety of Vega Extra Strong 120 were evaluated in 21 randomized double-blind placebo-controlled studies lasting up to 6 months in 3000 patients from 19 to 87 years with erectile dysfunction of different etiology (organic, psychogenic or mixed). The efficacy of the drug was evaluated globally using an erection diary, an international erectile function index (validated questionnaire on the state of sexual function) and a partner survey.

The effectiveness of Sildenafil Vega Extra 130, defined as the ability to achieve and maintain an erection sufficient for satisfactory sexual intercourse, has been demonstrated in all studies and confirmed in long-term studies lasting 1 year. In studies with the use of fixed-dose proportion of patients reporting that treatment improved their erections were 62% (dose of Vega Cobra 120 25 mg), 74% (dose Vega Cobra 120 50 mg) and 82% (dose Vega Extra 120 Mg 100 mg) compared to 25% in the placebo group. Analysis of the international index of erectile function showed that in addition to improving erection treatment Sildenafil Vega Extra 130 also increased the quality of orgasm, allowing to achieve satisfaction from sexual intercourse and overall satisfaction.

According to the generalized data, 59% of patients with diabetes, 43% of patients who underwent radical prostatectomy and 83% of patients with spinal cord injuries (against 16, 15 and 12% in the placebo group, respectively) were reported to have improved erection in the treatment of Cobra Vega Extra Strong 120 Mg.

Pharmacokinetics

Vega Cobra 120 Mg