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The molecular structure of sildenafil is similar to that of cGMP and acts as a competitive binder of PDE5. Therefore, in corpus cabernosum, resulting in more cGMP and increased penile response to sexual activity. Stimulation. In the absence of sexual stimulation, the lack of activation of the NO/cGMP. So, the system means that sildenafil should not cause an erection.
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Other drugs that work by the same mechanism include tadalafil (Cialis) and vardenafil (Levitra). Sildenafil in the liver by cytochrome p450 enzyme, mainly by liver metabolism using CYP450 3A4 (main pathway). As well as by CYP2C9 (minor pathway) liver isoenzyme. The main product of metabolism by this enzyme is N-demethylat sildenafil, which is further metabolizes . Such metabolites also have an affinity for the PDE receptor, which is about 40% of sildenafil. Thus, the metabolite is responsible for about 20% of the action of sildenafil.
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