Commercial name: Esculap
DCI of the active substance: Tadalafilum
Composition and presentation: 1 tablet contains:
active substance: tadalafil - 20 mg
»Auxiliary substances: magnesium stearate, Kollidon CL (crospovidone), colorant FD & C Yellow no. 6, Ludi-press (lactose, povidone, crospovidone).
Description: Round-shaped, orange-colored tablets on one side with a dividing line and "BP" print, with sharp edges, rounded-edge side. Marble is allowed on the surface of the tablets.
Pharmaceutical form: Tablets.
Pharmacotherapeutic group and ATC code: Drug for the treatment of erectile dysfunction, G04BE08.
Tadalafil is a selective, reversible selective phosphodiesterase type 5 (PDE5) specific for cyclic guanosine monophosphate (GMPc). When sexual stimulation causes local release of nitric oxide, inhibition of PDE5 by tadalafil produces increases in GMPc values in the corpus cavernosa of the penis. As a result, relaxation of the smooth muscles of the arteries and infiltration of the blood into the tissues of the penis results in erection. Tadalafil has no effect in the absence of sexual stimulation. In vitro studies have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in the smooth muscles of cavernous bodies in vascular and visceral smooth muscles in skeletal muscles, platelets, kidneys, lungs and cerebellum. The effect of tadalafil on PDE5 is stronger than the effect on other phosphodiesterases. Tadalafil is over 10,000 times more selective for PDE5 than for PDE1, PDE2 and PDE4, enzymes found in the cord, brain, blood vessels, liver and other organs. Tadalafil is over 10,000 times more selective for PDE5 than for PDE3, the enzyme found in the cord and in the blood vessels. Selectivity for PDE5 compared to PDE3 is important because PDE3 is an enzyme involved in cardiac contractility. In addition, tadalafil is approximately 700 times more selective for PDE5 than for PDE6, the enzyme found in the retina and is responsible for fo-transduction. Tadalafil is also more than 10,000 times more selective for PDE5 than for PDE7 to PDE10.
Tadalafil improves erectile function and ability to have a successful sexual act. The preparation works for 36 hours. The effect is already over 15 minutes after the preparation of this sexual stimulation.
Tadalafil in healthy subjects does not produce significant differences compared to placebo of systolic and diastolic blood pressure in the lying position (mean decrease of 1.6 mm Hg and 0.8 mm Hg, respectively) and in orthostatism (mean decrease of 0.2 mm Hg and 4.6 mm Hg, respectively). Tadalafil does not produce any significant change in the frequency of cardiac contractions. Tadalafil does not produce changes in color perception (blue / green), which is reflected by the low affinity of tadalafil for PDE6. Similarly, no influence of tadalafil on visual acuity, electroretinogram, intraocular pressure, and pupil size was determined. No clinically significant changes in sperm count, sperm concentration, motility and morphology have been determined in male tadalafil studies in the 10 mg daily dose.