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 Vega Extra 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 Vegah Cobra 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 Vegah Cobra 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) Vegah Cobra dose should be reduced to 25 mg.

Hepatic impairment. Since the excretion of Vegah Cobra is disturbed in patients with liver damage (in particular, cirrhosis), the dose of Vega Extra Cobra 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 Vega Extra Cobra 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 Signature Cobra Vega should be 25 mg (see "Interaction").

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

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

Vegah Cobra 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.

Vegah Cobra 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 Vega Extra Strong 120 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. Vegah Cobra 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 Vegah Cobra is sexual stimulation.

Vega Extra 120 Mg restores impaired erectile function in conditions of sexual stimulation by increasing blood flow to the cavernous bodies of the penis.

Influence of Vegah Cobra on other drugs

Vegah Cobra is a weak inhibitor of cytochrome P450 — 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 ISOENZYMES (IC50 >150 µmol). When taking Vega Coin in recommended doses, its Cmax is about 1 µmol, so it is unlikely that Vega Extra can affect the clearance of the substrates of these isoenzymes.

Sildenafil Tablets Vega Extra Cobra increases the hypotensive effect of nitrates both with long-term use of the latter, and with their appointment for urgent indications. In this regard, the use of Sildenafil Vega Extra 120 in combination with nitrates or nitric oxide donators is contraindicated. While taking α-adrenoblocker doxazosin (4 and 8 mg) and Vegah Cobra (25, 50 and 100 mg) in patients with benign prostate hyperplasia with stable hemodynamics, the average additional decrease in sad/dad in the supine position was 7/7, 9/5 and 8/4 mm Hg.article, respectively, while in the standing position — 6/6, 11/4 mmHg, and 4/5.art. respectively. Reported rare cases of symptomatic postural hypotension in such patients, manifested in the form of dizziness (without fainting). In some sensitive patients receiving α-blockers, simultaneous use of Vegah Cobra can lead to symptomatic hypotension.

There were no signs of significant interaction with tolbutamide (250 mg) or warfarin (40 mg), which are metabolized by CYP2C9 isoenzyme.

Vegah Cobra (100 mg) has no effect on the pharmacokinetics of the HIV protease inhibitor, saquinavir, which is a substrate of CYP3A4 isoenzyme, at its constant level in the blood.

The simultaneous use of Vegah Cobra at equilibrium (80 mg 3 times a day) leads to an increase in the AUC and Cmax of bosentan (125 mg 2 times a day) by 49.8 and 42%, respectively.

Vegah Cobra (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg).

Sildenafil Tablets Vegah Extra Cobra (50 mg) does not increase the hypotensive effect of alcohol in healthy volunteers with Cmax of alcohol in the blood on average 0.08‰ (80 mg/DL).

In patients with hypertension, no signs of interaction of Sildenafil Vega Extra 120 (100 mg) with amlodipine were found. The average additional reduction in blood PRESSURE in the supine position is 8 mm Hg.V. (systolic) and 7 mm Hg.V. (diastolic).

The use of Vegah Cobra in combination with antihypertensive agents does not lead to additional side effects.

The pharmacokinetics of Vegah Cobra in the recommended dose range is linear.

Suction. After intake of Vega Visa is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Signature Cobra Vega at a concentration of about 1.7 ng/ml (3.5 nm) inhibits the activity of PDE-5 50%. After a single dose of Extra Vega 100 mg average Cmax free Vegah Cobra in plasma men is about 18 ng/ml (38 nm). Cmax when taking Vegah Cobra 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 Vegah Cobra is 105 l. the Association of Cobra Vega Extra Strong 120 Mg 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 Vegah Cobra (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 Vegah Cobra, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Vega Extra Cobra 120, and its activity against PDE-5 in vitro is about 50% of the activity of Sildenafil Vega Extra 130. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Vega 120 Mg. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.

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

Vega Cobra