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An agent for the treatment of erectile dysfunction, is a reversible selective inhibitor of specific PDE5 cGMP. When sexual arousal induces local release of nitric oxide, inhibition of PDE5 by tadalafil results in an increase in cGMP levels in the corpus cavernosum of the penis. The consequence is relaxation of the smooth muscles of the arteries and blood flow to the tissues of the penis, which causes an erection. Tadalafil is ineffective in the absence of sexual stimulation.

In vitro studies have shown that tadalafil is a selective PDE5 inhibitor. PDE5 is an enzyme found in the smooth muscle of the corpora cavernosa, in the smooth muscle of the vessels of the internal organs, in skeletal muscle, platelets, kidneys, lungs, and cerebellum.

The effect of tadalafil on PDE5 is more active than on other phosphodiesterases. Tadalafil is 10,000 times more active against PDE5 than against PDE1, PDE2, PDE4, which are localized in the heart, brain, blood vessels, liver and other organs. Tadalafil is 10,000 times more active at blocking PDE5 than PDE3, an enzyme found in the heart and blood vessels. This selectivity for PDE5 over PDE3 is important because PDE3 is an enzyme involved in cardiac muscle contraction. In addition, tadalafil is about 700 times more active against PDE5 than against PDE6, which is found in the retina and is responsible for phototransmission. Tadalafil is also 10,000 times more active against PDE5 than it is against PDE7-PDE10.

Valid for 36 hours. The effect is manifested within 16 minutes after ingestion in the presence of sexual arousal.

Tadalafil in healthy individuals does not cause significant changes in systolic and diastolic pressure compared to placebo in the supine position (the average maximum decrease is 1.6 / 0.8 mm Hg, respectively) and standing (the average maximum decrease is 0.2 / 4 , 6 mm Hg, respectively). respectively). Tadalafil does not cause significant changes in heart rate.

Tadalafil does not cause changes in color recognition (blue / green) due to its low affinity for PDE6. In addition, no effect of tadalafil on visual acuity, electroretinogram, intraocular pressure and pupil size was noted.

There was no clinically significant effect on sperm characteristics in men who took tadalafil in daily doses for 6 months.

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