Generic Levitra

Active substance: vardenafil hydrochloride trihydrate - 23.705 mg, which is equivalent to 20 mg of vardenafil, respectively;

Auxiliary substances: crospovidone - 8,850 mg, magnesium stearate - 1,770 mg, microcrystalline cellulose - 141.797 mg, colloidal silicon dioxide - 0.885 mg;
Shell: macrogol 400 - 1,128 mg, hypromellose - 3,385 mg, titanium dioxide - 0.925 mg, iron oxide yellow dye - 0.188 mg iron oxide red dye - 0.015 mg.
1 or 4 tablets in an Al/PP blister.

1 blister in a cardboard pack (after the first opening, together with the instructions for use. Additionally, for a dosage of 5 mg: 5 blisters of 4 tablets in a cardboard pack with the control of the first opening, together with the instructions for use.

Description of the dosage form

Round, biconvex tablets covered with a film coating from light orange to grayish-orange color, with an engraving applied by embossing: on one side - the branded Bayer cross, on the other - the dosage designation "20".

Pharmacokinetics

  • After oral administration, vardenafil is rapidly absorbed. When taken on an empty stomach, the early peak of the maximum concentration (Cmax) can be reached after 15 minutes, but in 90% of cases, on average, the maximum concentration is reached after 60 minutes (from 30 to 120 minutes).
  • Due to the significant effect of the first pass, the absolute bioavailability is about 15%. In the recommended dose range (5-20 mg), the value of the indicator "area under the curve of the concentration-time ratio" (ACC) and Cmax increase in proportion to the dose.
  • When taking vardenafil simultaneously with food containing a large amount of fat (57%), the absorption rate decreases with an increase in the time to reach the maximum concentration (Tmax) up to 60 minutes, and the Cmax decreases on average by 20% without a significant change in the PPK index. When taken with normal food containing no more than 30% fat, the pharmacokinetic parameters of vardenafil (Cmax, Tmax, PPK) do not change. Based on these data, vardenafil can be used regardless of food intake.

Distribution

The average volume of distribution of vardenafil in a stable state of pharmacokinetic parameters is 208 liters, which demonstrates its good distribution in tissues. Vardenafil and its main metabolite (Ml) bind well to plasma proteins (up to 95%), and this property is reversible and does not depend on the total concentration of the drug.

90 minutes after taking vardenafil, no more than 0.00012% of the dose received can be determined in the sperm of healthy patients.

Metabolism

Vardenafil is metabolized mainly by hepatic enzymes involving the cytochrome CYP3A4 system, as well as CYP3A5 and CYP2C9 isoforms. The average half-life (T1/2) of vardenafil is 4-5 hours, and the main metabolite M1 (formed by deethylation of the piperazine part of the molecule) is about 4 hours. The blood contains glucuronide in the form of a conjugate (glucuronic acid), which is part of the M1 metabolite. The concentration of the rest of the M1 metabolite (non-glucuronic) is 26% of the concentration of the active substance. The selectivity profile for phosphodiesterase in M1 is similar to that of vardenafil; its ability to inhibit PDE-5 in vitro is 28%, compared with vardenafil, which corresponds to 7% of the effectiveness of the drug.