Sildenafil offers an opportunity to treat male erectile dysfunction with an effective, licensed oral
preparation.
• It is taken on a “when required” basis and only works in the presence of sexual stimulation.
• 70-80% of men in trials show a statistically significant improvement in erectile or sexual function
compared with about 25% of men who receive placebo. In the dose-escalation study in 329 men,
around 2 men would need to be treated with sildenafil for 12 weeks for one man to report improved
erections (NNT). There is no clear figure of how this relates to successful sexual intercourse, although
69% of all attempts were successful compared to 22% with placebo.
• Open label follow up studies indicate that most men who initially respond to the drug continue to take
it. A fully-published randomised controlled trial has also demonstrated the efficacy of sildenafil in men
with diabetes mellitus and erectile dysfunction.
• Sildenafil appears to be well tolerated. 2.5% of patients withdrew from studies because of adverse
effects, compared to 2.3% with placebo. The US Food and Drug Administration has reported 69
deaths in people taking sildenafil which led to an update of the US label. Forty-six deaths were known
to be due to cardiovascular events. Since sexual activity is itself a risk factor in cardiovascular death
the role of sildenafil is difficult to determine.
• As yet there are no direct comparisons of sildenafil with alternative treatments.
• The long-term safety profile of sildenafil is yet to be established.
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Sildenafil is rapidly absorbed after oral administration
reaching maximum plasma concentration within 30-120
minutes of dosing in fasted subjects. It has a bioavailability
of about 40% and fatty food has been shown to reduce the
rate of absorption and the peak concentrations achieved,
without affecting the extent of absorption. It is therefore
advised that sildenafil is taken 30-60 minutes before planned
sexual activity. One small study, which is only available as
an abstract, has shown that sildenafil still has an effect on
erectile function for 4-5 hours after dosing [4].
Sildenafil is mainly eliminated by hepatic metabolism
(principally cytochrome P450 3A4) and converted to the
active N-desmethyl metabolite, which accounts for about
20% of its overall pharmacological effect. Both sildenafil
and the metabolite have terminal half-lives of about 4 hours
and are excreted predominately in the faeces. No significant
accumulation is expected to occur on single daily dosing.
Studies have shown that renal insufficiency (creatinine
clearance (CLcr) <30ml/min), hepatic insufficiency and age
(over 65 years) are all associated with increased plasma
concentrations when compared with matched controls.
Sildenafil and its major metabolite are highly bound to plasma
proteins
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Posted by Mr Procces at 7:42 AM
Labels: sildenafil, viagra
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1 comments:
One factor that has tremendously hiked up the number of researches going into the male sexual dysfunction disease, erectile dysfunction, is definitely the ED drugs like cialis.Definitely every man dreads the prospect of falling back on medicines, no matter how much good they have done or how effective they are. One way of possibly staying away from ED is to have sex atleast thrice a week. This exercise can be phenomenal in cutting down the risks of ED to half.
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