Infors coated tablets 100 mg. №12

Description

Infors tablets Composition
active substance: sildenafil;

1 film-coated tablet contains sildenafil citrate 70.24 mg, which is equivalent to sildenafil 50 mg;

1 film-coated tablet contains sildenafil citrate 140.48 mg, which is equivalent to sildenafil 100 mg;

Excipients: microcrystalline cellulose, calcium hydrogen phosphate anhydrous, povidone, croscarmellose sodium, magnesium stearate, “Opadry blue 0ZA205003” [hypromellose, microcrystalline cellulose, macrogol stearate, titanium dioxide] (E 171).

Infors tablets Dosage form

Film-coated tablets.

Main physical and chemical properties: blue tablets, oval, biconvex, with a line on both sides. The tablet can be divided into two dose levels.

Infors tablets Pharmacotherapeutic group

Remedies used for erectile dysfunction. Sildenafil. ATX code G04B E03.

Pharmacological properties

Pharmacodynamics.

Mechanism of action.

Sildenafil is an oral drug used to treat erectile dysfunction in men. During sexual arousal, the drug restores reduced erectile function by increasing blood flow to the penis.

The physiological mechanism that causes an erection involves the release of nitric oxide (NO) in the corpora cavernosa during sexual arousal. The released nitric oxide activates the enzyme guanylate cyclase, which stimulates an increase in the level of cyclic guanosine monophosphate (cGMP), which, in turn, causes the smooth muscles of the corpora cavernosa to relax, promoting blood flow.

Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase 5 (PDE5) in corpora cavernosa, where PDE5 is responsible for the breakdown of cGMP. The effects of sildenafil on erection are peripheral. Sildenafil does not have a direct relaxing effect on isolated human corpora cavernosa, but strongly enhances the relaxing effect of NO on this tissue. Upon activation of the NO / cGMP metabolic pathway, which occurs during sexual stimulation, inhibition of PDE5 by sildenafil leads to an increase in cGMP levels in the corpora cavernosa. Thus, sexual arousal is required for sildenafil to produce the desired pharmacological effect.

Pharmacokinetics.

Absorption. Sildenafil is rapidly absorbed. Maximum plasma concentrations of the drug are reached within 30-120 minutes (with a median of 60 minutes) after oral administration on an empty stomach. The average absolute bioavailability after oral administration is 41% (with a range of values ​​from 25 to 63%). In the recommended dose range (25 to 100 mg), the AUC and Cmax of sildenafil after oral administration increase in proportion to the dose.

When sildenafil is taken with food, the degree of absorption decreases with a mean prolongation of Tmax to 60 minutes and a mean decrease in Cmax by 29%.