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- Oct 23, 2007 9:55pm
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Viagra, the drug to increase potency.
International title
Sildenafil
* Synonyms: Via ́ Gras-commercially known drug developed by the American company Pfizer, Xia ́ Gras, Jena ́ Gras, etc. Potential-drug commercial names, a large percentage of drugs produced in India.
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The history of
In early 1990 the company Pfizer researchers develop medicines from chest pains while in stenocardia. In clinical trials of biologically active substance sildenafil did not have the expected action on the heart. But the test were enthusiastic because of the strong-side effect with respect to potency. When some of them refused to pay the remaining pills [source?] (And one even burst into the laboratory, where sildenafil placed to stock lots drug source) [?] , Company managers realized that met with a gold lived. Thus was born Viagra.
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Drug Form
Thickly-coated pills
Pharmacological Effects
Selective inhibitors tsGMF-spetsificheskoy FDE5, which is responsible for the break-in tsGMF pescheristom sexual body member. Actively increases relaxing effect on the nitrogen oxide smooth muscle kavernoznogo body and increases blood flow to the members of the sexes. When the chain NO- tsGMF, observed with sexual initiation, oppression FDE5 leads to an increase in tsGMF kavernoznom body. Pharmacological effects achieved only if there is sexual stimulation. Activity against FDE5 in 10-10000 exceeds activity against others izofermentov FDE
Pharmacokinetics
TCmax reception inside, IFG - 0.5-2 h, bioavailability - 25-60%. With admission to the Cmax fat diet reduced by 20-40% and achieved through 1.5-3 h. The volume of distribution of equilibrium state, 105 liters. Communication with plasma protein-96%. Metabolized mainly by the action of CYP3A4, CYP3A5, CYP3A7 (main path), and CYP2C9 (additional path) mikrosomalnyh izofermentov liver metabolites education. The main circulating an active metabolite N-dezmetilmetabolit, activity which is 50% sildenafila activity. Overall keel clearance-41 l / h. T1 / 2 and N-sildenafila dezmetilmetabolita for 3-5 hours Report the inactive metabolites in the form of colon masses (80%) and kidneys (15%). Do patients with renal insufficiency (QC less than 30 ml / min), liver cirrhosis and in the elderly keel clearance sildenafila lowered.
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Testimony
Violations Mature different etiology (organic, psychogenic, mixed). Impotence
Contraindications
Hypersensitivity; Simultaneous reception Scharenberg nitrogen oxide or nitrates in any form. C caution. Heart Disease, anatomical deformation of sexual member, Sickle-cell anemia, multiorgan myeloma, leukemia, children's age.
Metering Mode
Inside, about 1 hour before the sexual activity. Disposable dose for adults is 50 mg once a day. Given the efficiency and Portability dose may be increased to 100 mg or 25 mg reduced to. Disposable maximum dose is 100 mg. Do patients with impaired liver or kidney function in older patients and correction dose is not required.
Side effects
Headache pain, "tides" of blood-to-face, dizziness, dyspepsia, zalozhennost nose, visual impairment (changing color objects (blue / green), reinforced the perception of light, clarity violation of view).
Interaction
Tsimetidin, fatigue, erythromycin reduce keel clearance and increased concentration in the blood sildenafila. Antiagregantny enhances the effect of sodium nitroprussida. Increases hypotensive effect of nitrates (sildenafila combination with nitrates can cause fatal), a potentially dangerous to the life of a joint appointment with
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