brief introduction
Levitra Chinese trademark: ALIDA. This is an orange pill, nicknamed "Flame". It is a new generation of Viagra produced in Germany. It is a very powerful PDE-5 inhibitor, and it is "quick to take effect, high in erectile hardness, safe and independent", which allows both parties to "seize the passionate moment together"!
Two characteristics
This product is a light orange to dark orange film-coated tablet, which is white after removing the film-coated tablet.
3 pharmacological mechanism
pharmacological action
Penile erection is a hemodynamic process involving the relaxation of cavernous smooth muscle and its related arterioles. During sexual stimulation, the nerve endings in the corpus cavernosum release nitric oxide (NO), which activates guanylate cyclase in smooth muscle cells and increases the level of cyclic guanylate (cGMP) in cells, which eventually leads to the relaxation of smooth muscle and increases the blood flow of penis.
Vardenafil can increase the release of endogenous nitric oxide from corpus cavernosum by inhibiting phosphodiesterase 5 (PDE5) which degrades cGMP in human corpus cavernosum, thus enhancing the natural response to sexual stimulation.
indicate
Treat erectile dysfunction of male penis.
Contraindications
1. It is forbidden for patients with allergic symptoms of any component (active or inactive) of the drug.
2.PDE5 inhibitor may enhance the antihypertensive effect of nitrate drugs, which is similar to the mechanism of PDE inhibitor in NO/cGMP pathway. Therefore, patients receiving nitrate or nitric oxide donor therapy should avoid concurrent use of vardenafil.
3. Avoid using HIV protein kinase inhibitor indinavir or ritonavir and vardenafil at the same time, because they are powerful CYP3A4 inhibitors.
Toxicological study
Acute toxicity: LD50 of rats was 190mg/kg, and no drug visual effect was observed by light microscope, electron microscope and visual inspection. Long-term toxicity: The maximum non-toxic dose (NOEL) of rats and dogs is 3mg/kg. In addition, all animals showed cardiovascular toxicity related to PDE5, and rats also showed pancreatic, exocrine and thyroid toxicity related to PDE.
Genotoxicity: Vardenafil was not found to be genotoxic and mutagenic in vitro Salmonella typhimurium reversion mutation test, mammalian cell HPRT mutation test, in vivo mouse chromosome aberration test and micronucleus test. Reproductive toxicity: rats and rabbits take vardenafil orally, and vardenafil has no effect on animal fertility and embryo development. Carcinogenicity: rats and mice were given vardenafil for 24 consecutive menstrual periods, and the dosage was 225 times and 450 times of the clinical maximum recommended dosage of 20mg calculated by body surface area, and 360 times and 25 times of the clinical maximum recommended dosage of 20mg calculated by AUC. At this time, vardenafil is not carcinogenic.