The pharmacokinetics of Sildenafil Vega Extra 120 in the recommended dose range is linear.

Suction. After intake of Vega Pills is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Extra 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 Sildenafil Vega Extra 120 100 mg average Cmax free Vega Extra 120 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 Sildenafil Vega Extra 120 is 105 l. the Association of Sildenafil Vega Extra 120 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 Sildenafil Vega Extra 120 (an average of 188 ng) was found in sperm 90 minutes after taking the drug.

Metabolism. Sildenafil Vega Extra 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 Sildenafil Vega Extra 120, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Sildenafil Vega Extra 120, and its activity against PDE-5 in vitro is about 50% of the activity of Vega Extra 120 Mg. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Sildenafil Vega Extra 120. 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, Signature Cobra Vega is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).

Influence of Vega Extra on other drugs

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

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

Sildenafil Vega Extra 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 Vega Extra Cobra 120 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.

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

Sildenafil Vega Extra 120 (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 Vega 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 120 Mg in combination with antihypertensive agents does not lead to additional side effects.

Clinical data

Cardiac studies. The use of Sildenafil Vega Extra 120 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 Mg 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 Sildenafil Vega Extra 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%. Vega Extra Cobra 130 Mg 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 Sildenafil Vega Extra 130 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 Vegal Extra (up to 100 mg) in men (n=568) with erectile dysfunction and hypertension, taking more than two antihypertensive drugs, was studied. Sildenafil Vega Extra 120 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 Vega Visa 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. Sildenafil Vega Extra 120 had no effect on visual acuity, contrast perception, electroretinogram, IOP or pupil diameter.

Side effect

The most common side effects were headache and tides.

Usually the side effects of Sildenafil Vega Extra 120 are mild or moderate and are transient.

Studies using a fixed dose have shown that the frequency of some adverse events increases with increasing dose.

The frequency of adverse reactions is presented in the following classification: very often — ≥10%; often — ≥1% and <10%; infrequently — ≥0.1% and <1%; rarely — ≥0.01% and <0.1%; very rarely — <0.01%; frequency unknown — cannot be determined based on available data.

Co side of the immune system: infrequently — hypersensitivity reactions (including skin rash), allergic reactions.

On the part of the organ of vision: often — blurred vision, blurred vision, cyanopsia; rarely, eye pain, photophobia, photopsia, chromatopsia, eye redness/injection of the sclera, changing the brightness of cvetovete, mydriasis, conjunctivitis, hemorrhage in the tissue of the eye, cataract, a disorder of the lacrimal apparatus; rarely — swelling of the eyelids and adjacent tissues, a feeling of dryness in the eyes, the presence of iridescent circles in the field of view around the light source, increased fatigue of the eyes, vision of objects in yellow (xanthopsia), vision of objects in red (erythropsia), conjunctival hyperemia, irritation of the mucous membrane of the eyes, unpleasant sensations in the eyes; the frequency is unknown — NPINZN, occlusion of retinal veins, visual field defect, diplopia*, temporary vision loss or decreased visual acuity, increased IHD, edema retina, retinal vascular disease, vitreous detachment/vitreal traction.

On the part of the organ of hearing: infrequent — a sudden decrease or loss of hearing, tinnitus, pain in the ears.

From the CCC: often — tides; infrequently — tachycardia, palpitations, decreased blood PRESSURE, increased heart rate, unstable angina, AV-blockade, myocardial infarction, cerebral thrombosis, cardiac arrest, heart failure, deviations in ECG readings, cardiomyopathy; rarely — atrial fibrillation, sudden cardiac death*, ventricular arrhythmia*.

The blood and lymphatic system: rarely — anemia, leukopenia.

On the part of metabolism and nutrition: infrequently — a feeling of thirst, swelling, gout, uncompensated diabetes, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemia, hypernatremia.

From the respiratory system: often — nasal congestion; infrequent — nosebleeds, rhinitis, asthma, dyspnea, laryngitis, pharyngitis, sinusitis, bronchitis, increased volume of sputum, increased cough; rarely — a feeling of tightness in the throat, dryness of the nasal mucosa, swelling of the nasal mucosa.

From the digestive tract: often — nausea, dyspepsia; uncommon — GERD, vomiting, pain in the abdomen, dryness of the mucous membrane of the mouth, glossitis, gingivitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, rejection of liver function tests from normal, rectal bleeding; rarely, hypesthesia of the mucous membrane of the oral cavity.

On the part of the musculoskeletal system: often — back pain; infrequently — myalgia, pain in the limbs, arthritis, arthrosis, tendon rupture, tenosynovitis, bone pain, myasthenia gravis, synovitis.

From the genitourinary system: infrequently — cystitis, nicturia, breast enlargement, urinary incontinence, hematuria, ejaculation disorders, genital edema, anorgasmia, hematospermia, damage to the tissues of the penis; rarely — prolonged erection and/or priapism.

From the Central and peripheral nervous system: very often — headache; often — dizziness; infrequently — drowsiness, migraine, ataxia, hypertension, neuralgia, neuropathy, paresthesia, tremor, vertigo, symptoms of depression, insomnia, unusual dreams, increased reflexes, hypesthesia; rarely — convulsions*, repeated convulsions*, fainting.

On the part of the skin and subcutaneous tissues: infrequently — skin rash, urticaria, herpes simplex, itching, sweating, skin ulceration, contact dermatitis, exfoliative dermatitis; the frequency is unknown — Stevens-Johnson syndrome, toxic epidermal necrolysis.

Other: infrequently — a feeling of heat, swelling of the face, photosensitivity reaction, shock, asthenia, fatigue, pain of various localization, chills, accidental falls, chest pain, accidental injuries; rarely — irritability.

Vega Extra Cobra