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Vega Extra Cobra (sildenafil citrate)

Vega Extra Cobra (sildenafil citrate)

$ 1.02 per pill

Quick Overview

Selective Vegah Extra 120 Indication 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 Extra 120 Indication 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.

Vega Extra Cobra® (Signature)

Vega Extra Cobra (Sildenafil citrate) 120 mg

Vega Extra Cobra
Sildenafil citrate
120 mg × 180 pills
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Vega Extra Cobra
Sildenafil citrate
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Sildenafil citrate
120 mg × 90 pills
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Vega Extra Cobra
Sildenafil citrate
120 mg × 60 pills
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Vega Extra Cobra
Sildenafil citrate
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Sildenafil citrate
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Vega Extra Cobra
Sildenafil citrate
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Information

The pharmacokinetics of Vegah Extra 120 Indication in the recommended dose range is linear.

Suction. After intake of Vega Extra Strong 120 is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Vega 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 Signature Cobra Vega 100 mg average Cmax free Signature Cobra Vega in plasma men is about 18 ng/ml (38 nm). Cmax when taking Cobra Vega 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 Sildenafil Tablets Vegah Extra Cobra is 105 l. the Association of Vegah Extra 120 Indication 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 Extra 120 Indication (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 Cobra Vega 120 Mg, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Vegah Extra 120 Indication, and its activity against PDE-5 in vitro is about 50% of the activity of Sildenafil Vega Extra 120. 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 Vegah Extra 120 Indication is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Vegah Extra 120 Indication is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).

Cardiovascular complications

During the post-marketing use of Vegah Extra 120 Indication 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 Vega Extra Cobra 130 Mg. 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 Vegah Extra 120 Indication without subsequent sexual activity. It is not possible to establish a direct link between the reported adverse events and those or other factors.

Visual impairment

In rare cases, during post-approval use of all of the inhibitors of PDE5, including Cobra 120 Vega Extra, 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 of developing 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 Vegah Extra 120 Indication 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 Sildenafil Vega Extra 120, in such patients should be used with caution and only in situations where the expected benefit outweighs the risk.

When using the drug Vegah Extra 130 in doses exceeding the recommended, adverse events were similar to those noted above, but usually more common.

*Side effects identified during post-marketing studies.

Interaction

Effect of other drugs on the pharmacokinetics of Vegah Extra 120 Indication

The metabolism of Vegah Extra 120 Indication occurs mainly under the action of CYP3A4 isoenzyme (main pathway), so inhibitors of this isoenzyme can reduce the clearance of Vegah Extra 120 Indication, and inducers, respectively, increase the clearance of Vegah Extra 120 Indication. A decrease in the clearance of Vegah Cobra with simultaneous use of inhibitors of CYP3A4 isoenzyme (ketoconazole, erythromycin, cimetidine).

Cimetidine (800 mg), a nonspecific inhibitor of CYP3A4 isoenzyme, when taken together with Vegah Extra 120 Indication (50 mg) causes an increase in the concentration of Sildenafil Vega Extra 130 Mg in plasma by 56%.

A single dose of 100 mg of Vega Cobra together with erythromycin (500 mg/day 2 times a day for 5 days), a moderate inhibitor of CYP3A4 isoenzyme, while achieving a constant concentration of erythromycin in the blood, leads to an increase in the AUC of Vegah Extra 120 Indication by 182%.

When co-administered Vega Extra (once 100 mg) and saquinavir (1200 mg/day 3 times daily), an inhibitor of HIV protease and of CYP3A4, on the background to achieve a constant concentration of saquinavir in the blood, Cmax of Vegah Extra 120 Indication was increased by 140% and the AUC increased by 210%.

Stronger inhibitors of CYP3A4 isoenzyme, such as ketoconazole and Itraconazole, can cause more pronounced changes in the pharmacokinetics of Vegah Extra 120 Indication.

The simultaneous use of Vegah Extra 120 Indication (100 mg once) and ritonavir (500 mg 2 times a day), an inhibitor of HIV protease and a strong inhibitor of cytochrome P450, on the background to achieve a constant concentration of ritonavir in the blood leads to an increase in Cmax of Vega 120 Mg by 300% (4 times), a AUC by 1000% (11-fold). After 24 h, the concentration of Vegah Extra 120 Indication in blood plasma is about 200 ng/ml (after a single application of one Cobra 120 Vega Extra — 5 ng/ml). This is consistent with the ritonavir effect on a wide range of cytochrome P450 substrates. Vegah Extra 120 Indication does not affect the pharmacokinetics of ritonavir. Given these data, the simultaneous reception of ritonavir and Vegah Extra 120 Indication is not recommended. In any case, the maximum dose of Vegah Extra 120 Indication under any circumstances should not exceed 25 mg for 48 hours. If Vegah Extra 120 Indication is taken in the recommended doses, patients receiving strong inhibitors of CYP3A4 isoenzyme at the same time, then Cmax free Vegah Extra 120 Indication does not exceed 200 nm, and the drug is well tolerated.

Single administration of antacid (magnesium hydroxide/aluminum hydroxide) does not affect the bioavailability of Vega Extra Cobra 130 Mg.

Studies involving healthy volunteers with simultaneous use of endothelin receptor antagonist, bosentan (CYP3A4 isoenzyme inducer (moderate), CYP2C9, and possibly CYP2C19) in Css (125 mg 2 times a day) and Vegah Extra 120 Indication in Css (80 mg 3 times a day) showed a decrease in AUC and Cmax Cobra Vega Extra Strong 120 Mg by 62.6 and 52.4%, respectively. Extra Vega increased the AUC and Cmax of bosentan by 49.8 and 42%, respectively.

It is assumed that the simultaneous use of Sildenafil Vega Extra 130 Mg Cobra with powerful inducers of CYP3A4 isoenzyme, such as rifampicin, can lead to a greater decrease in the concentration of Vega Extra Cobra 120 in blood plasma.

CYP2D6 isoenzyme inhibitors (SSRIs, tricyclic antidepressants), thiazide and thiazide-like diuretics, ACE inhibitors and calcium antagonists have no effect on the pharmacokinetics of Vega Coin.

Azithromycin (500 mg/day for 3 days) has no effect on AUC, Cmax, Tmax, excretion rate constant and T1/2 Vegah Extra 120 Indication or its main circulating metabolite.

Clinical data

Cardiac studies. The use of Vegah Extra 120 Indication in doses up to 100 mg did not lead to clinically significant ECG changes in healthy volunteers. The maximum decrease in systolic pressure in the supine position after taking Vegah Extra 120 Indication at a dose of 100 mg was 8.3 mm Hg.art., and diastolic pressure — 5.3 mm Hg.a More pronounced, but also transient effect on blood PRESSURE was observed in patients taking nitrates (see "Contraindications" and "Interaction").

In a study of the hemodynamic effect of Vega Extra Strong 120 in a single dose of 100 mg in 14 patients with severe coronary artery disease (more than 70% of patients had stenosis of at least one coronary artery), systolic and diastolic resting pressure decreased by 7 and 6%, respectively, and pulmonary systolic pressure decreased by 9%. Vegah Extra 120 Indication did not affect cardiac output and did not interfere with blood flow in stenotic coronary arteries, and also led to an increase (by about 13%) of adenosine-induced coronary flow in both stenotic and intact coronary arteries. In a double-blind placebo-controlled study of 144 patients with erectile dysfunction and stable angina, taking antianginal drugs (except nitrates), exercise was performed until the severity of symptoms of angina increased. The duration of the exercise was significantly longer (19.9 seconds; 0.9–38.9 seconds) in patients taking Vega 120 Mg in a single dose of 100 mg, compared with patients receiving placebo.

In a randomized double-blind placebo-controlled study, the effect of changing the dose of Vegah Extra 120 Mg (up to 100 mg) in men (n=568) with erectile dysfunction and hypertension, taking more than two antihypertensive drugs, was studied. Vega Extra 120 Mg improved erection in 71% of men compared to 18% in the placebo group. The frequency of adverse effects was comparable to that in other groups of patients, as well as in those taking more than three antihypertensive drugs.

Studies of visual impairment. In some patients, 1 h after taking Vegah Extra 120 Indication at a dose of 100 mg with the Farnsworth-Mansell test 100 revealed a slight and transient violation of the ability to distinguish shades of color (blue/green). After 2 hours after taking the drug, these changes were absent. It is believed that color vision impairment is caused by inhibition of PDE-6, which is involved in the process of color transmission in the retina. Vega Visa had no effect on visual acuity, contrast perception, electroretinogram, IOP or pupil diameter.

Influence of Vega Visa on other drugs

Vega Extra Strong 120 is a weak inhibitor of cytochrome P450 — 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 ISOENZYMES (IC50 >150 µmol). When taking Vegah Extra 120 Indication in recommended doses, its Cmax is about 1 µmol, so it is unlikely that Vega Extra Cobra 120 can affect the clearance of the substrates of these isoenzymes.

Vega 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 Vegah Extra 120 Indication in combination with nitrates or nitric oxide donators is contraindicated. While taking α-adrenoblocker doxazosin (4 and 8 mg) and Vegah Extra 120 Indication (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 Cobra Vega Extra Strong 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.

Vegah Extra 120 Indication (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 Indication 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 Indication (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg).

Vegah Extra 120 Indication (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 Indication (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 Coin in combination with antihypertensive agents does not lead to additional side effects.



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