
Levitra contains vardenafil – a potent PDE5 inhibitor of the second generation. Vardenfil binds to PDE5 with high selectivity. Vardenafil therefore does not have an effect on the CNS but works on peripheral receptors of the penis. In general PDE5 inhibitors work only upon sexual stimulation. The PDE5 enzyme hydrolyzes cyclic guanosine monophosphate (cGMP) in the cavernosum tissue of the penis. cGMP is needed for the relaxation of the smooth muscles of the cavernosal blood vessels and the arteries supplying the penis with blood which is important for the enlargement of the corpora cavernosa. Thus inhibition of PDE5 results in smooth muscle relaxation and vasodilatation leading to increased arterial blood flow and penile erection.
cGMP, cyclic guanosine monophosphate; eNOS, endothelial nitric oxide synthase; GMP, guanosine monophosphate; GTP, guanosine triphosphate; NO, nitric oxide; PDE-5, phosphodiesterase type 51
Reference:
1. Lue T. N Engl J Med 2000; 342: 1802–13.