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Revatio

Pfizer Inc.

Drug Names(s): sildenafil citrate

Description: BioMedTracker has separate profiles for Viagra and Revatio (pulmonary arterial hypertension). Please also see Viagra.

Revatio is the citrate salt of sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5).

Sildenafil citrate is designated chemically as 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate.

The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate cyclase,which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smoothmuscle relaxation in the corpus cavernosum and allowing inflow of blood. Sildenafil has nodirect relaxant effect on isolated human corpus cavernosum, but enhances the effect of nitricoxide (NO) by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradationof cGMP in the corpus cavernosum. When sexual stimulation causes local release of NO,inhibition of PDE5 by sildenafil causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil at recommended doses has no effect in the absence of sexual stimulation.


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