The pharmacokinetics of Vega Extra 120 Mg in the recommended dose range is linear.
Suction. After intake of Sildenafil Vega Extra 130 is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Sildenafil Vega Extra 130 at a concentration of about 1.7 ng/ml (3.5 nm) inhibits the activity of PDE-5 50%. After a single dose of Cobra 120 Vega Extra 100 mg average Cmax free Sildenafil Vega Extra 130 in plasma men is about 18 ng/ml (38 nm). Cmax when taking Vegab Extra 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 Vega Cobra 120 is 105 l. the Association of Sildenafil Vega Extra 130 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 Vegal Extra (an average of 188 ng) was found in sperm 90 minutes after taking the drug.
Metabolism. Vega 120 Mg 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 130, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Vega 120 Mg, 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 Cobra Vega Extra. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.
Breeding. The total clearance of Signature Cobra Vega is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Sildenafil Vega Extra 130 is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).
Cobra Vega Extra Strong 120 Mg is a weak inhibitor of cytochrome P450 — 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 ISOENZYMES (IC50 >150 µmol). When taking Sildenafil Vega Extra 130 in recommended doses, its Cmax is about 1 µmol, so it is unlikely that Sildenafil Vega Extra 130 can affect the clearance of the substrates of these isoenzymes.
Sildenafil Vega Extra 130 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 130 in combination with nitrates or nitric oxide donators is contraindicated. While taking α-adrenoblocker doxazosin (4 and 8 mg) and Vega Extra Strong 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 130 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 Mg (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 Sildenafil Vega Extra 130 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.
Sildenafil Vega Extra 130 Mg (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg).
Vega Coin (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 Tablets Vega Extra Cobra (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 Visa in combination with antihypertensive agents does not lead to additional side effects.
Cardiovascular complications
During the post-marketing use of Sildenafil Vega Extra 130 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 Pills. 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 Vega Cobra 120 without subsequent sexual activity. It is not possible to establish a direct link between the reported adverse events and those or other factors.
Hypotension
Vegah Extra 120 Mg has a systemic vasodilating effect, leading to a transient decrease in blood PRESSURE, which is not clinically significant and does not lead to any consequences in most patients. However, before prescribing Sildenafil Vega Extra 130, the doctor should carefully assess the risk of possible undesirable manifestations of vasodilating action in patients with relevant diseases, especially against the background of sexual activity. Increased susceptibility to vasodilators is observed in patients with obstruction of the output tract of the left ventricle (aortic stenosis, GOCMP), as well as with the rare syndrome of multiple systemic atrophy, manifested by a severe violation of the regulation of blood PRESSURE from the autonomic nervous system.
Since the combined use of Sildenafil Vega Extra 130 and α-blockers can lead to symptomatic hypotension in some sensitive patients, Sildenafil Vega Extra 130 should be used with caution in patients taking α-blockers (see "Interaction"). To minimize the risk of postural hypotension in patients taking α-blockers, the drug Sildenafil Vega Extra 130 should be started only after achieving stabilization of hemodynamic parameters in these patients. It should also consider reducing the initial dose of Sildenafil Vega Extra 130 (see. "Dosage and administration"). The doctor should inform patients about what actions should be taken in case of symptoms of postural hypotension.
Side effect
The most common side effects were headache and tides.
Usually the side effects of Sildenafil Vega Extra 130 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.
Vegah Cobra
