The pharmacokinetics of Vega Visa in the recommended dose range is linear.
Suction. After intake of Vegal Extra is rapidly absorbed. Absolute bioavailability averages about 40% (25 to 63%). In vitro Cobra Vega 120 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 130 100 mg average Cmax free Cobra Vega 120 in plasma men is about 18 ng/ml (38 nm). Cmax when taking Vega Visa 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 120 is 105 l. the Association of Cobra Vega 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 Cobra Vega 120 (an average of 188 ng) was found in sperm 90 minutes after taking the drug.
Metabolism. Vegah 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 Cobra Vega 120, undergoes further metabolism. The selectivity of this metabolite against PDE is comparable to that of Sildenafil Vega Extra 130 Mg Cobra, and its activity against PDE-5 in vitro is about 50% of the activity of Cobra Vega 120. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of Sildenafil Tablets Vegah Extra Cobra. N-demethyl metabolite undergoes further metabolism; its T1/2 is about 4 no.
Breeding. The total clearance of Vega Extra Cobra 120 is 41 l/h, and the final T1/2 — 3-5 h. After oral administration, as well as after I/V, Sildenafil Tablets Vegah Extra Cobra is excreted as metabolites, mainly by the intestine (about 80% oral dose) and to a lesser extent by the kidneys (about 13% oral dose).
Side effect
The most common side effects were headache and tides.
Usually the side effects of Vega 120 Mg 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.
Contraindications
hypersensitivity to Cobra Vega 120 or any other component of the drug;
application in patients receiving constantly or intermittently nitric oxide donators, organic nitrates or nitrites in any form, as Cobra 120 Vega Extra enhances the hypotensive effect of nitrates (see "Interaction»);
the combined use of inhibitors of PDE5, including Sildenafil Vega Extra 130, called guanylate cyclase stimulants such as riociguat, because it can lead to symptomatic hypotension;
concomitant use with other agents for the treatment of erectile dysfunction (safety and efficacy of Cobra Vega 120 when used together has not been studied (see. "Special instructions»);
lactose intolerance, lactase deficiency, glucose-papacosma malabsorption;
severe liver failure (class C classification for child-Pugh);
simultaneous administration of ritonavir;
severe cardiovascular diseases (severe heart failure, unstable angina, stroke or myocardial infarction during the last 6 months, life-threatening arrhythmias, hypertension (BP >170/100 mm Hg). art.) or hypotension (blood PRESSURE <90/50 mm Hg.art.) (see "Special instructions»);
patients with episodes of development partizanai anterior ischemic optic neuropathies (NESN) with loss of vision in one eye;
hereditary retinitis pigmentosa (see special instructions»);
according to the registered indication is not intended for use in women;
according to the registered indication is not intended for use in children under 18 years.
With caution: anatomic deformity of the penis (angulation, cavernous fibrosis or Peyronie's disease) (see "Special instructions"); diseases of, predisposing to the development of priapism (sickle-cell anemia, multiple myeloma, leukemia, thrombocythemia) (see "Special instructions"); diseases accompanied by haemorrhage; ulcer disease of stomach and duodenum in the acute phase; liver dysfunction; severe renal insufficiency (Cl creatinine <30 ml/min); patients with an episode of partizanai development of the anterior ischemic optic neuropathies in history (see "Special instructions); simultaneous reception of blockers α-adrenergic receptors.
Use during pregnancy and breast-feeding
According to the registered indication, the drug is not intended for use in women.
Vegal Extra 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 Coin 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 Cobra Vega 120 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. Cobra Vega 120 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 Cobra Vega 120 is sexual stimulation.
Cobra Vega 120 restores impaired erectile function in conditions of sexual stimulation by increasing blood flow to the cavernous bodies of the penis.
Vegal Extra
