Dwagra 25
- Sildenafil a novel effective oral therapy for male erectile
dysfunction, is the citrate salt of Sildenafil, a selective
inhibitor of phosphodiestrase type 5 (PDE5), that enhances
the effect of nitric oxide during sexual stimulation which
results in increased levels of cyclic guanosine
monophosphate producing smooth muscle relaxation in the
corpus cavernosum, allowing inflow of blood and hence
increasing the pressure in the penis and leading to
tumescence. The erectile response generally increased with
increasing sildenafil dose and plasma concentration. The time
course of effect for up to 4 hours but the response may be
diminished compared to 2 hours.
- Sildenafil at recommended doses has no effect in the absence
of sexual stimulation.
- The decrease in blood pressure was most notable
approximately 1- 2 hours after single oral dose of sildenafil,
this effect is not releated to dose or plasma levels.
- Sildenafil is rapidly absorbed following administration by
mouth, with a bioavailability of approximately 40%. Peak
plasma concentrations are attained within 30 to 120 minutes;
the rate of absorption is reduced when administered with
food. It is widely distributed into tissues and is approximately
96% bound to plasma proteins.
-Sildenafil is metabolized in the liver primarily by cytochrome
P450 3A4 and P450 2C9 isoforms. The major metabolite
N-desmethylsildenafil has the same activity of Sildenafil ,
The major metabolite has a potency for PDE5 approximately
50% of the parent drug.
- Excretion is predominantly as metabolites in the faeces and
to a lesser extent in the urine.