1-3- (1,4-dihydro-5-methyl-4-oxo-7-propylimidazo5,1-f1,2,4triazin-2-yl) -4-ethoxyphenylsulfonyl-4-ethylpiperazine monohydrochloride
Vardenafil is a selective inhibitor cGMP-specific phosphodiesterase type 5used for treatment erectile dysfunction. By its physical properties - colorless solid, poorly soluble in water. Molecular mass = 488.6 grams per mole. Issued in the form of tablets for oral administration.
Improves erectile function.
Pharmacodynamics and pharmacokinetics
For the normal achievement of an erection, it is necessary that there has been a complete relaxation of the cavernous bodies and associated arterioleserection is a hemodynamic process. In the presence of sexual stimulus, release occurs nitric oxide from the endothelial cells of the vessels of the corpus cavernosum, activated guanylate cyclase and the concentration increases cGMP in the smooth muscles of the cavernous bodies. Cyclic accumulation guanidine monophosphate activates the relaxation of the corpus cavernosum and vascular smooth muscle, blood rushes to the sexual canoe, an erection occurs. The concentration of cGMP can be affected, both by stimulating its synthesis and accelerating degradation. Therefore, when taking vardenafil, an increase in the amount of cGMP and enhanced erectile function. Due to the fact that sexual stimulation is necessary to activate the process described above, an erection does not occur immediately after taking the medicine.
The substance is rapidly absorbed in the digestive tract. The degree of bioavailability is 15%. After a single dose, the maximum concentration of the drug in the blood is reached within an hour. Eating fatty foods reduces the maximum concentration by almost half.
The drug and its active metabolites have a high degree of binding to plasma proteins - almost 95%. The metabolism of the drug occurs in the liver with the participation of isoform CYP3A4, CYP3A5 and CYP2C. As a result, an active metabolite is formed. The half-life of vardenacil and its metabolite is from 4 to 5 hours. A medicine with feces and urine is excreted.
In men over 65, plasma concentration is 35% higher and 52% higher. Auc. In patients with severe hepatic impairment, the plasma concentration rises by 130 or 160%. The medicine does not have carcinogenic, mutagenic properties, does not affect fertility, motility or sperm morphology, and is not toxic.
Indications for use
The substance is prescribed for treatment erectile dysfunction.
The medicine is contraindicated:
- during therapy nitrates, alpha adrenergic blockers or nitric oxide donors;
- under the age of 16;
- at allergies to vardenafil.
The frequency and severity of adverse reactions depends on the dosage taken.
During treatment, the agent may manifest:
- headache, rhinitisflushing of the face, indigestion, sinusitis;
- dizziness, nausea, rising levels creatine kinase;
- laryngeal edema and anaphylactic reactionsswelling of the face, asthenia;
- tinnitus, chest pain, angina pectorisincrease or decrease in blood pressure;
- ischemia myocardium, palpitations, myocardial infarction;
- tachycardia, myalgia, arthralgiapain in the back and neck, insomnia;
- paresthesia, hypersthesia, vertigoblood from the nose;
- photosensitivity sweatingitching and skin rashes;
- blurred vision, conjunctivitiseye pain glaucoma;
- painful or prolonged erection, other disorders of the ejaculation process.
Vardenafil, instructions for use (Method and dosage)
At the initial stages of treatment, it is recommended to take 10 mg of the substance inside, half an hour or an hour before the alleged sexual contact. The medicine is not recommended to be taken more often than once a day.
If the patient tolerates the medicine well, then a single dose can be increased to 20 mg or reduced to 5 mg. The maximum amount of vardenafil that can be taken at a time is 20 mg.
For patients with moderate liver failure, the recommended dosage is 5 mg per day.
When taking more than 0.12 g of a substance at a time, the following are observed: myalgialower back pain, impaired vision.
Supportive therapy is recommended. Dialysis ineffective.
Vardenafil can be combined with cimetidine. It is not recommended to take more than 5 mg of the drug when combined in erythromycin, ketoconazole (200 mg). After taking 400 mg ketoconazole You can take no more than 2.5 mg of vardenafil during the day.
The tool can not be combined with ritonavir. It is not recommended to take more than 2.5 mg of the substance within 3 days.
In conjunction with indinavir It is recommended to take no more than 2.5 mg of the drug.
The drug does not enter into drug interaction with warfarin, glibenclamide, Maalox, digoxin, ranitidine.
The medicine strengthens the farm. the effect of sublingual nitrates when taken after 60 minutes or 4 hours. This combination is contraindicated for use.
Patients who take alpha blockers treatment with vardenafil is contraindicated.
When combined with alcohol, there are no significant fluctuations in the pharmacokinetic parameters of both agents. While taking the medicine and ethyl alcohol, the hypotensive effect of alcohol is potentiated.
Before you assign Vardenafil to a patient, you should evaluate the degree of risk and the state of the cardiovascular system. If a man is not recommended for sexual activity, then treatment for erectile dysfunction is not carried out.
Taking this medication is not recommended for patients with left ventricular obstruction, with aortic stenosis and idiopathic hypertrophic subaortic stenosis.
With extreme caution, the drug is combined with indinavir, ritonavir, ketoconazole, itraconazole and erythromycin. It is necessary to adjust the dosage of drugs.
If after taking the medicine, the patient has an erection lasting more than 4 hours, a phenomenon is observed priapismthen you need to see a doctor. Such adverse reactions can lead to tissue damage and long-term loss of erection.
Due to the fact that the safety and efficacy of vardenafil were not evaluated in the following groups of patients, treatment with the drug is not recommended. With caution, the medicine is used: for unstable angina pectorisuncontrollable arterial hypotensionafter strokewith arrhythmia and myocardial infarctionwith severe heart failure; in patients with severe liver failure; with serious kidney disease; with hereditary degenerative diseases of the retina (retinitis pigmentosa).
Preparations that contain (Analogs)Matches for ATX Level 4 code:TornetisOlmax StrongTaxiereDynamicallyRevazioCoverjectLevitraCialisTentex ForteRailisViagraSildenafilYohimbine HydrochlorideZidenaRange
Tradename: Levitra OTD, Staxyn, Levitra, Vivanza.
Reviews about the pills are mostly good. Men often praise this medication, write that they need small doses (2.5 mg) to provide a lasting and lasting effect. Of the adverse reactions most often complain of dizziness, flushing of the face, slight discomfort in the stomach.
Vardenafil price, where to buy
The price of the drug varies depending on the manufacturer. Buy vardenafil in a pharmacy under the trade name Levitra can be for about 1300 rubles, 2 tablets of 10 mg.