COMPOUND:
OTHER INGREDIENTS:
Gelatin, magnesium stearate
RELEASE FORM:
Capsules in a plastic bottle with control of the first opening (30 pcs).
INDICATIONS:
Erectile dysfunction of various etiologies.
Increases blood supply to the penis, reproduces an adequate physiological response to sexual arousal. The medicine begins to act in the presence of sexual stimulation.
The occurrence of an erection is associated with the release of NO (nitric oxide) in the cavernous (cavernous) body of the male penis shaft. NO (nitric oxide) activates the enzyme - sGC (soluble guanylate cyclase). As a result of the interaction of the sGC enzyme and the nucleotide GTP (guanosine triphosphate), cGMP (cycloguanosine monophosphate) is formed. An increase in the level of the cyclic form of the nucleotide - cGMP, initiates relaxation of the smooth muscles of the tissues of the cavernous body of the penis and an increase in blood flow.
Sildenafil has no direct effect on smooth muscle. It is an inhibitor of PDE5 (phosphodiesterase type 5), the enzyme responsible for the breakdown of cGMP.
Absorbed quickly. Bioavailability 40%. With a one-time intake of D (dose) - 100 mg of sildenafil Cmax (maximum concentration) - 18ng / ml, an average TCmax (time to reach maximum concentration) is achieved - 75 minutes (30 -120 minutes) provided that the medicine is taken on an empty stomach. (in vitro, sildenafil inhibits the activity of the PDE5 enzyme by 50% at a concentration of already 1.7 ng / ml). Sildenafil is poorly compatible with fatty foods: the maximum concentration of the medicine (Cmax) in plasma decreases by 29%, the time to reach the maximum concentration (TCmax) increases by 60 minutes, the time under the pharmaceutical curve (AUC) decreases by 11%.
Vd (volume of distribution) - 105 l. Sildenafil and N-desmethylmetabolite (the main metabolite of sildenafil) bind to plasma proteins by 96%. The percentage does not depend on the concentration of the medicine. 0.0002% of the dose received is detected in semen after 90 minutes from the moment of administration.
It is metabolized in the liver. There are two pathways of sildenafil metabolism: major and minor (additional). Under the influence of liver isoenzymes CYP3A4, CYP3A5, CYP3A7, metabolism is carried out along the main pathway. The CYP2C9 isoenzyme is responsible for the minor pathway. N-desmethylmetabolite, the main circulating metabolite of sildenafil, exhibits the same selectivity of action with respect to PDE5 as sildenafil and half as much activity compared to sildenafil. Subsequently, the N-desmethyl metabolite undergoes a process of further metabolism.
T1 / 2 (half-life) of sildenafil - 180-300 minutes. The total clearance is 41 l / h. 80% of sildenafil in the form of inactive metabolites is excreted in the feces by the intestines. 13% is excreted in the urine by the kidneys.
APPLICATION:
1 capsule 40-60 minutes before sexual activity. Do not take more than 1 capsule per day.
SIDE EFFECTS:
Occurring adverse reactions increase with increasing dosage. May be corrected by dosage reduction. Seeking medical help with the development of such reactions is indicated only in severe cases.
RARE ADVERSE REACTIONS (FROM 0.01% TO 0.1%):
CONTRAINDICATIONS:
The use by persons with impaired functioning of the liver and kidneys requires special care. It is recommended not to exceed the dose of 25 mg.
STORAGE:
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