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Ladygra (Sildenafil) belongs to the pharmacological group – Inhibitors of phosphodiesterase 5. PDE-5 inhibitors are drugs that are selective blockers of the type 5 phosphodiesterase enzyme and are used to treat erectile dysfunction in men.
The overall effect of this group of drugs is to increase an erection in the presence of sexual arousal and increase its duration.
Also specific for this group of drugs is the fact that after taking Ladygra (Sildenafil) an erection occurs only with adequate sexual arousal.
In other words, PDE-5 inhibitors including Ladygra (Sildenafil) per se do not increase libido and do not cause sexual desire. Therapy with these drugs is symptomatic, that is, it does not eliminate the causes of erectile dysfunction.
The mechanism of action of Ladygra (Sildenafil) is due to blocking the action of the corresponding enzyme, which, in turn, leads to an increase in the number of cyclic guanosine monophosphate and relaxation of smooth muscles in the arteries of the penis.
The latter contributes to the filling of the cavernous bodies of the penis with blood and the appearance of an erection. After sexual intercourse, the blood supply to the penis is reduced to the original values.
Pharmacology of Ladygra (Sildenafil)
Pharmacological action - Ladygra (Sildenafil) improves erectile function.
Ladygra (Sildenafil) exerts a peripheral effect by selectively inhibiting cGMP-specific type 5 phosphodiesterase (PDE5), which is responsible for the breakdown of cGMP in cavernous bodies. The physiological mechanism of erection involves the release of nitric oxide in the cavernous bodies of the penis during sexual stimulation. Nitric oxide activates guanylate cyclase, which leads to an increase in cGMP, relaxation of the smooth muscles of the corpora cavernosa and blood flow to them. Ladygra (Sildenafil) does not have a direct relaxing effect on the smooth muscles of the corpora cavernosa, but due to the blockade of PDE5 and stabilization of cGMP enhances the relaxing effect of nitric oxide.
In vitro studies have shown that the activity of Ladygra (Sildenafil) in relation to PDE5 is superior to that in relation to other isoforms of phosphodiesterase. So, the effect of sildenafil on PDE5 is more than 80 times stronger than PDE1, more than 1000 times stronger than PDE2, PDE3 and PDE4; in particular, activity in relation to PDE5 is 4,000 times higher than that in relation to PDE3 (PDE3 is involved in heart contraction). The activity of sildenafil in relation to PDE5 is only 10 times higher than that in relation to PDE6 (PDE6 is involved in color perception).
In addition to the smooth muscles of cavernous bodies, PDE5 is also found in small quantities in platelets, smooth muscle tissue of blood vessels and internal organs, and in skeletal muscle. Inhibition of PDE5 by sildenafil in these tissues can lead to an increase in the anti-aggregation activity of platelet nitric oxide in vitro, inhibition of platelet aggregation and peripheral arteriovenous dilatation in vivo.
In 21 randomized, double-blind, placebo-controlled studies lasting up to 6 months, the efficacy and safety of Ladygra (Sildenafil) was studied in more than 3,000 patients aged 19–87 years with erectile dysfunction of organic, psychogenic and mixed etiology. Most studies have shown that the effect of Ladygra (Sildenafil) develops approximately 60 minutes after ingestion.
Erectile response, incl. evaluated according to phalloplethysmography, increased with increasing dose of sildenafil and its plasma concentration. The duration of action of Ladygra (Sildenafil) was evaluated in one study, which showed its effectiveness for 4 hours with a decrease in erectile response after 2 hours from the time of administration. When using fixed doses of 25 mg, 50 mg and 100 mg, an improvement in erectile function was observed in 63%, 74% and 82% of patients, respectively (when taking placebo, in 24%).
Hypersensitivity, nitrate therapy.
Anatomical deformation of the penis (angulation, cavernous fibrosis, Peyronie's disease), diseases predisposing to the development of priapism (myeloma, sickle cell anemia, leukemia), increased tendency to bleeding, exacerbation of gastric ulcer and duodenal ulcer, hereditary liver function, including with cirrhosis, severe renal insufficiency.
Side effects of Ladygra (Sildenafil)
Side effects of dose-adjusted sildenafil observed in placebo-controlled trials and observed in ≥2% of patients taking sildenafil, with a frequency greater than placebo (in parentheses % indicates occurrence in the placebo group).
From the nervous system and sensory organs: headache 16% (4%), dizziness 2% (1%), flushing 10% (1%), visual impairment (color perception, increased sensitivity to light, blurred vision) thirty%).
From the respiratory system: nasal congestion 4% (2%).
From the digestive tract: dyspepsia 7% (2%), diarrhea 3% (1%).
From the genitourinary system: urinary tract infections 3% (2%).
From the skin: rash 2% (1%).
As you can see, the side effects of Ladygra (Sildenafil) are really small and close to the placebo group.
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