The pharmacokinetics of Vega Cobra in the recommended dose range is linear.
Suction. After intake of Cobra 120 Vega Extra is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Cobra Vega Extra Strong 120mg at a concentration of about 1.7 ng/ml (3.5 nm) inhibits the activity of PDE-5 50%. After a single dose of Vega Cobra 100 mg average Cmax free Vega Cobra in plasma men is about 18 ng/ml (38 nm). Cmax when taking Vega 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 Cobra Vega Extra Strong 120mg is 105 l. the Association of Vega 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 Vega Cobra (an average of 188 ng) was found in sperm 90 minutes after taking the drug.
Metabolism. Vega Cobra 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 Vega Cobra, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Vega Cobra, and its activity against PDE-5 in vitro is about 50% of the activity of Sildenafil Vega Extra 130 Mg Cobra. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Cobra Vega 120 Mg. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.
Breeding. The total clearance of Sildenafil Vega Extra 130 Mg Cobra is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Vega Extra Cobra 130 Mg is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).
Clinical data
In a placebo-controlled cross-examination of patients with proven early age macular degeneration (n=9), Vegah Extra 120 Mg 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 Sildenafil Vega Extra 130 Mg 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 Vega Cobra, 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 Sildenafil Vega Extra 130 25 mg), 74% (dose Vegab Extra 50 mg) and 82% (dose Vegab Extra 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 Mg Cobra 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 Vega Cobra.
Pharmacokinetics
Hearing impairment
Some post-marketing and clinical studies have reported cases of sudden hearing loss or impairment associated with the use of all PDE-5 inhibitors, including Vega Extra Cobra 130 Mg. Most of these patients had risk factors for sudden impairment or hearing loss. There is no causal relationship between the use of PDE-5 inhibitors and sudden hearing impairment or hearing loss. In case of sudden hearing impairment or hearing loss while taking Vegah Extra 130, consult a doctor immediately.
Bleedings
Vegah Cobra enhances the antiplatelet effect of sodium nitroprusside, a nitric oxide donator, on human platelets in vitro. Data on the safety of Vega Visa in patients with a tendency to bleeding or exacerbation of gastric ulcer and duodenal ulcer are not available, so the drug Vegah Cobra in these patients should be used with caution (see With caution).
The incidence of nosebleeds in patients with pulmonary hypertension associated with diffuse connective tissue diseases was higher (Vega Cobra — 12.9%, placebo — 0%) than in patients with primary pulmonary arterial hypertension (Vega Cobra — 3%, placebo — 2.4%). Patients receiving Cobra Vega 120 in combination with an antagonist of vitamin K, the frequency of nasal bleeding was higher (8.8 percent) than patients who were not taking an antagonist of vitamin K (1.7 percent).
Use in conjunction with other means for the treatment of erectile dysfunction
The safety and efficacy of Signature Cobra Vega together with other PDE-5 inhibitors or other drugs for the treatment of pulmonary hypertension containing Vega Extra 120 Mg (eg, Revatsio®), or other means for the treatment of erection disorders have not been studied, so the use of such combinations is not recommended (see "Contraindications").
Influence on the ability to drive and mechanisms. In patients receiving Vega Cobra any negative effect on the ability to drive a car or other means was not observed. However, since when taking Vegah Extra 120 Mg may develop dizziness, lowering blood PRESSURE, the development of chromatopsia, blurred vision, etc. side effects, care should be taken when driving and doing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions. Also, you should be careful about the individual action of the drug in these situations, especially at the beginning of treatment and when changing the dosage regimen.
Vega 120 Mg 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 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 Cobra 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 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 Vega Visa is sexual stimulation.
Vega Cobra restores impaired erectile function in conditions of sexual stimulation by increasing blood flow to the cavernous bodies of the penis.
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