Sildenafil Vega Extra 120 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 Cobra 130 Mg 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 Vegal Extra 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. Vegal 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 Vegal Extra is sexual stimulation.

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

Cardiovascular complications

During the post-marketing use of Vegal Extra for the treatment of erectile dysfunction, adverse events such as severe cardiovascular complications (including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, hypertension and hypotension) were reported, which had a temporary connection with the use of Cobra Vega Extra. Most of these patients, but not all of them, had risk factors for cardiovascular complications. Many of these adverse events were observed shortly after sexual activity, and some were observed after taking Vega Extra 120 Mg without subsequent sexual activity. It is not possible to establish a direct link between the reported adverse events and those or other factors.

Hypotension

Vegal Extra has a systemic vasodilating effect, leading to a transient decrease in blood PRESSURE, which is not clinically significant and does not lead to any consequences in most patients. However, before prescribing Vega Extra Cobra 130 Mg, the doctor should carefully assess the risk of possible undesirable manifestations of vasodilating action in patients with relevant diseases, especially against the background of sexual activity. Increased susceptibility to vasodilators is observed in patients with obstruction of the output tract of the left ventricle (aortic stenosis, GOCMP), as well as with the rare syndrome of multiple systemic atrophy, manifested by a severe violation of the regulation of blood PRESSURE from the autonomic nervous system.

Since the combined use of Vegal Extra and α-blockers can lead to symptomatic hypotension in some sensitive patients, Vegal Extra should be used with caution in patients taking α-blockers (see "Interaction"). To minimize the risk of postural hypotension in patients taking α-blockers, the drug Vegal Extra should be started only after achieving stabilization of hemodynamic parameters in these patients. It should also consider reducing the initial dose of Vegal Extra (see. "Dosage and administration"). The doctor should inform patients about what actions should be taken in case of symptoms of postural hypotension.

Dosage and administration

Inside, can be taken with or without water. When taking the drug, you should put a tablet, dispersed in the oral cavity, on the tongue, after which it will quickly dissolve, and it can be swallowed. The tablet should be taken immediately after opening the blister. Patients who are recommended a dose of Cobra Vega 120 100 mg, the second tablet of Vegal Extra 50 mg should be taken after complete dissolution of the first tablet.

The recommended dose for most adult patients is 50 mg approximately 1 hour before sexual activity. Taking into account the effectiveness and tolerability of the dose can be increased to 100 mg or reduced to 25 mg (only tablets coated with a film, the appropriate dosage). The maximum recommended dose is 100 mg. Patients who are recommended a dose of Vegal Extra 100 mg, it is necessary to take 2 table., dispersible in the oral cavity, dosage 50 mg consecutively one after another. The maximum recommended frequency of use — 1 time per day. It should be borne in mind that the absorption of Vegal Extra significantly slows down when used in combination with fatty foods.

Special patient groups

Renal impairment. In mild to moderate renal failure dose adjustment is not required, in severe renal failure (Creatinine CL <30 ml/min) Sildenafil Tablets Vega Extra Cobra dose should be reduced to 25 mg.

Hepatic impairment. Since the excretion of Vegal Extra is disturbed in patients with liver damage (in particular, cirrhosis), the dose of Vegah Extra 120 Indication should be reduced to 25 mg.

Joint application with other drugs. Joint use with ritonavir is not recommended. In any case, the maximum dose of Vegal Extra under any circumstances should not exceed 25 mg, and the frequency of application — 1 time in 48 h (see "Interaction").

When combined with inhibitors of CYP3A4 isoenzyme (erythromycin, saquinavir, ketoconazole, Itraconazole), the initial dose of Vegal Extra should be 25 mg (see "Interaction").

To minimize the risk of postural hypotension in patients taking α-blockers, Cobra Vega Extra should be started only after achieving hemodynamic stabilization in these patients. Consideration should also be given to reducing the initial dose of Vega Cobra 120 Mg (see special instructions and Interactions).

Old age. Adjustment of the dose of Vega Cobra 120 Mg is not required.

The pharmacokinetics of Vegal Extra in the recommended dose range is linear.

Suction. After intake of Vegal Extra is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Cobra Vega 120 at a concentration of about 1.7 ng/ml (3.5 nm) inhibits the activity of PDE-5 50%. After a single dose of Vegal Extra 100 mg average Cmax free Vegal Extra in plasma men is about 18 ng/ml (38 nm). Cmax when taking Sildenafil Vega Extra 120 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 Vega Visa is 105 l. the Association of Vegah Cobra 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 Vegal Extra (an average of 188 ng) was found in sperm 90 minutes after taking the drug.

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

Breeding. The total clearance of Vegab Extra is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Vega Extra Cobra 120 is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).

Cobra Vega 120 Mg