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There are three drugs on the market that are first line for treating erectile dysfunction. Those are Tadacip (Tadalafil), Sildenafil and Vardenafil. Those three have similar mechanism of action – they inhibit enzyme phosphodiesterase 5, but Tadacip (Tadalafil) stands apart from the rest by the duration of action, structure of molecule, administration etc.
Phosphodiesterase inhibitors are first-line drugs for the treatment of ED. The mechanism of action of all three drugs in this group is the same: they produce a peripheral effect by selectively inhibiting cGMP-specific PDE5, which is responsible for the breakdown of cGMP in cavernous bodies. Due to the blockade of PDE5 and stabilization of cGMP, drugs of this group enhance the effect of nitric oxide, which activates guanylate cyclase, which leads to an increase in cGMP, relaxation of the smooth muscles of the corpora cavernosa and blood flow to them. There is no direct relaxing effect on the smooth muscles of the corpora cavernosa in these preparations.
Numerous clinical studies have proven the efficacy and safety of PDE5 inhibitors for the treatment of ED. These drugs differ in duration of action: sildenafil citrate and vardenafil act up to 5 hours, Tadacip (Tadalafil) - up to 36 hours. The effect is manifested only with sexual arousal. The long-term effectiveness of Tadacip (Tadalafil) allows you to restore the spontaneity and naturalness of sexual relations.
Sildenafil citrate and vardenafil have a similar chemical structure, while Tadacip (Tadalafil) is significantly different from them in structure and pharmacokinetic properties.
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 in these tissues can lead to an increase in the anti-aggregation activity of platelet nitric oxide in vitro, inhibition of platelet aggregation and in vivo peripheral arteriovenous dilatation. There are clear differences between the drugs in terms of activity with respect to PDE6, which plays an important role in the conversion of light impulses to nerve in the retina. In addition, these three drugs differ in their activity against PDE11. Tadacip (Tadalafil) is 14 times more selective for PDE5 than PDE11, but does not inhibit this enzyme in therapeutic doses.
In all PDE5 inhibitors, the onset of action is approximately the same (after 30-60 minutes), but the duration varies significantly. The Tadacip (Tadalafil) effect is manifested longer than others (up to 36 hours).
This medicine is taken inside, per os, about 1 hour before intercourse. All three drugs (sildenafil citrate, vardenafil and Tadacip (Tadalafil)) are rapidly absorbed in the gastrointestinal tract. The absolute bioavailability is different: sildenafil citrate - 40%, vardenafil 15%. The concentration of sildenafil citrate and vardenafil peaks after 1 h, and Tadacip (Tadalafil) after 2 hours. Absorption occurs mainly in the small intestine; ingestion of fatty foods does not delay or impair the absorption of Tadacip (Tadalafil), but reduces and slows down the absorption of sildenafil citrate and vardenafil.
The half-life of sildenafil citrate and vardenafil from blood plasma is 3-5 hours, and Tadacip (Tadalafil) is 17-21 hours. Despite the long half-life, Tadacip (Tadalafil) does not have the ability to cumulate, equilibrium concentrations are reached on the fifth day with daily use.
For patients with frequent sexual activity (more than 2 times a week) the recommended frequency of Tadacip (Tadalafil) administration is daily, 5 mg 1 time per day, at the same time, regardless of food intake. The daily dose can be reduced to 2.5 mg, depending on individual sensitivity.
For patients with infrequent sexual activity (less than 2 times a week): it is recommended to prescribe Tadacip (Tadalafil) in a dose of 20 mg immediately before sexual activity, according to the instruction. The maximum daily dose of Tadacip (Tadalafil) is 20 mg.
The recommended dose of Tadacip (Tadalafil) when used once a day is 5 mg; the drug should be taken at approximately the same time of the day, regardless of the time of sexual activity. The duration of treatment is set by the doctor individually.
Special patient groups
In patients with renal failure, mild (Cl creatinine from 51 to 80 ml / min) and moderate severity (Cl creatinine from 31 to 50 ml / min) dose adjustment is not required.
In patients with severe renal failure (Cl creatinine <30 ml / min and on hemodialysis), the use of Tadacip (Tadalafil) is contraindicated.
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