Intagra ІS coated tablets 0.025 g. №4

Description

Intagra 0.025 g. №4 Composition
active substance: sildenafil citrate;

1 tablet contains sildenafil citrate (in terms of sildenafil) 50 mg;

excipients: lactose, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, potato starch, croscarmellose sodium, sodium bicarbonate, gelatin, colloidal silicon dioxide, talc, magnesium stearate, hypromellose (hydroxypropyl methylcellulose), diethylene glycol 17 acesulfame, kandurin, potassium aluminosilicate (E 555), titanium dioxide (E 171).

Intagra 0.025 g. №4 Dosage form
Film-coated tablets.

Basic physical and chemical properties: silver-colored, round tablets with a biconvex surface, film-coated.

Intagra 0.025 g. №4 Pharmacotherapeutic group
Drugs used for erectile dysfunction. Sildenafil ATX code G04B E03.

Pharmacodynamics

Mechanism of action

Sildenafil is an oral drug for the treatment of erectile dysfunction. With sexual arousal, the drug restores reduced erectile function by increasing blood flow to the penis.

The physiological mechanism that leads to an erection, including 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 relaxation of the smooth muscles of the corpora cavernosa, promoting blood flow.

Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase 5 (PDE-5) in the corpora cavernosa, where PDE-5 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 cavernous bodies, but powerfully enhances the relaxing effect of NO on this tissue. When the metabolic pathway NO / cGMP is activated, which occurs during sexual stimulation, inhibition of PDE5 by sildenafil leads to an increase in the level of cGMP in the corpora cavernosa. Thus, in order for sildenafil to cause a pharmacological effect, sexual arousal is necessary.

Impact on pharmacodynamics.

In vitro studies have shown that sildenafil is selective for PDE-5, which is actively involved in the process of erection. The effect of sildenafil on PDE5 is more potent than on other known phosphodiesterases. This effect is 10 times more powerful than the effect on PDE6, which is involved in the processes of phototransformation in the retina. When using the maximum recommended doses, the selectivity of sildenafil in PDE-5 is 80 times higher than its selectivity for PDE1, 700 times higher than in PDE2, PDE-3, PDE4, PDE7, PDE8, PDE9, PDE10 and PDE11. In particular, the selectivity of sildenafil for PDE-5 is 4000 times higher than its selectivity for PDE-3, a cAMP-specific isoform of PDE, which is involved in the regulation of cardiac contractility.

Indications
INTAGRA is recommended for men with erectile dysfunction, which is defined as the inability to achieve or maintain an erection of the penis necessary for successful intercourse.

For the effective action of the INTAGRA drug, sexual arousal is required.

Contraindications
Hypersensitivity to the active substance or to any other component of the drug.
Concomitant use with nitric oxide donors (such as amyl nitrite) or nitrates in any form is contraindicated, since it is known that sildenafil affects the pathways of nitric oxide / cyclic guanosine monophosphate (cGMP) metabolism and potentiates the hypotensive effect of nitrates.
The simultaneous use of PDE-5 inhibitors (including sildenafil) with guanylate cyclase stimulants, such as riociguat, is contraindicated because it can lead to symptomatic hypotension.
Conditions for which sexual activity is not recommended (for example, severe cardiovascular disorders such as unstable angina or severe heart failure).
Loss of vision in one eye due to non-arterial anterior ischemic neuropathy of the optic nerve, regardless of whether this pathology is associated with previous use of phosphodiesterase 5 (PDE-5) inhibitors.
The presence of such diseases as severe liver dysfunction, arterial hypotension (blood pressure below 90/50 mm Hg. Art.), Recent stroke or myocardial infarction and known hereditary degenerative diseases of the retina such as retinitis pigmentosa retinal PDE disorders), since the safety of sildenafil has not been investigated in such patient subgroups.