The pharmacokinetics of Cobra 120 Vega Extra in the recommended dose range is linear.
Suction. After intake of Vegah Extra 130 is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Vegah Extra 120 Mg at a concentration of about 1.7 ng/ml (3.5 nm) inhibits the activity of PDE-5 50%. After a single dose of Vegah Extra 120 Mg 100 mg average Cmax free Vega Cobra in plasma men is about 18 ng/ml (38 nm). Cmax when taking Vegah Extra 120 Mg 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 Extra 120 Mg is 105 l. the Association of Vega Cobra 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 Vega Coin (an average of 188 ng) was found in sperm 90 minutes after taking the drug.
Metabolism. Cobra Vega 120 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 Extra 120 Mg, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Vegah Extra 120 Mg, and its activity against PDE-5 in vitro is about 50% of the activity of Vegah Extra 120 Mg. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Cobra Vega 120. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.
Breeding. The total clearance of Vegah Extra 120 Mg is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Cobra Vega 120 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), Cobra 120 Vega Extra 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 Vegah Extra 120 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 Vegah Extra 120 Mg, 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 Vegah Extra 120 Mg 25 mg), 74% (dose Cobra Vega Extra Strong 120mg 50 mg) and 82% (dose Vega Extra Strong 120 100 mg) compared to 25% in the placebo group. Analysis of the international index of erectile function showed that in addition to improving erection treatment Signature Cobra Vega 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 Sildenafil Vega Extra 130.
Pharmacokinetics
Vega Extra Cobra 120 is a weak inhibitor of cytochrome P450 — 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 ISOENZYMES (IC50 >150 µmol). When taking Vegab Extra in recommended doses, its Cmax is about 1 µmol, so it is unlikely that Vegah Extra 120 Mg can affect the clearance of the substrates of these isoenzymes.
Vega Extra Cobra 120 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 Cobra Vega Extra Strong 120mg in combination with nitrates or nitric oxide donators is contraindicated. While taking α-adrenoblocker doxazosin (4 and 8 mg) and Vegah Extra 120 Mg (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 Extra 120 Mg 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.
Vega Extra Cobra 120 (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 Extra 120 Mg 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 Extra 120 Mg (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg).
Vegah Extra 120 Mg (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 Vegah Extra 120 Mg (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 Vega Extra Cobra 130 Mg in combination with antihypertensive agents does not lead to additional side effects.
Visual impairment
In rare cases, during post-approval use of all of the inhibitors of PDE5, including Vegah Extra 120 Mg, 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 Vega Cobra 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 Vegah Extra 120 Mg, 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 Vegah Extra 120 Mg 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 Vega Extra Cobra 130 Mg in patients with retinitis pigmentosa absent, so these patients should not be used Cobra Vega Extra (see "Contraindications").
Vegah Extra 120 Indication