Sildenafil metabolism

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    Sildenafil metabolism


    However, patient may take drug 30 minutes to 4 hours before sexual activity. as a single dose, p.r.n., 1 hour before sexual activity. Based on effectiveness and tolerance by patient, may increase dose to maximum single dose of 100 mg or decrease dose to 25 mg. A maximum recommended dosing frequency is once daily. Erectile action: Sildenafil has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of nitric oxide (NO) by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cyclic guanosine monophosphate (c GMP) in the corpus cavernosum. When sexual stimulation causes local release of NO, inhibition of PDE5 by sildenafil causes increased levels of c GMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. Absorption: Rapidly absorbed after oral administration. A high-fat meal delays the rate of absorption by about 1 hour and reduces peak levels by one-third. The primary indication of sildenafil is treatment of erectile dysfunction (inability to sustain a satisfactory erection to complete intercourse). Its use is now one of the standard treatments for erectile dysfunction, including for men with diabetes mellitus. Rare but serious adverse effects found through postmarketing surveillance include prolonged erections, severe low blood pressure, myocardial infarction (heart attack), ventricular arrhythmias, stroke, increased intraocular pressure, and sudden hearing loss. Care should be exercised by people who are also taking protease inhibitors for the treatment of HIV infection. Protease inhibitors inhibit the metabolism of sildenafil, effectively multiplying the plasma levels of sildenafil, increasing the incidence and severity of side effects. Those using protease inhibitors are recommended to limit their use of sildenafil to no more than one 25 mg dose every 48 hours. blocker (typically prescribed for hypertension or for urologic conditions, such as benign prostatic hypertrophy) at the same time may lead to low blood pressure, but this effect does not occur if they are taken at least 4 hours apart.

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    Feb 5, 2018. Sildenafil is a common medication used to stimulate erections in. Depending on your metabolism, Viagra can take five to six hours to fully. Sildenafil, sold as the brand name Viagra among others, is a medication used to treat erectile. Other drugs that interfere with the metabolism of sildenafil include erythromycin and cimetidine, both of which can also lead to prolonged plasma. Sildenafil, a novel orally active drug for the treatment of penile erectile. sildenafil is via 5 principal pathways of oxidative metabolism, the majority of the dose.

    Sildenafil is a common medication used to stimulate erections in men with erectile dysfunction (ED) and treat certain heart conditions. Many factors can influence how long Viagra takes to start working. In general, Viagra takes about 30 minutes to produce noticeable effects. But your diet, your overall health, the medications you’re taking, underlying conditions, and much more can all affect the amount of time Viagra takes to work in your body and how long it lasts. An erection happens when nerves in your penis are stimulated. Then, muscles around two cylinder-shaped chambers of spongy material along your penis, known as the corpus cavernosa, relax and allow blood to flow in, causing an erection. With ED, your nerves don’t communicate properly with your brain and blood doesn’t flow properly into the corpus cavernosa. Taking Viagra relaxes the walls of your blood vessels and lets blood flow more easily into the parts of your penis that cause an erection. You’ll still need to feel sexually aroused to get an erection. Sildenafil is a vasoactive agent used to treat erectile dysfunction and reduce symptoms in patients with pulmonary arterial hypertension (PAH). Sildenafil elevates levels of the second messenger, c GMP, by inhibiting its breakdown via phosphodiesterase type 5 (PDE5). PDE5 is found in particularly high concentrations in the corpus cavernosum, erectile tissue of the penis. It is also found in the retina and vascular endothelium. Increased c GMP results in vasodilation which facilitates generation and maintenance of an erection. The vasodilatory effects of sildenafil also help reduce symptoms of PAH.

    Sildenafil metabolism

    Integrating In Vitro Sildenafil Metabolism into a Physiologically-Based., Sildenafil - Wikipedia

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  3. Jan 1, 2018. Here, we revisited sildenafil metabolism in human liver microsomes using a metabolomics approach to achieve a global picture of sildenafil.

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    Metabolism. Sildenafil is cleared predominantly by the CYP3A4 major route and CYP2C9 minor route hepatic microsomal isoenzymes. The major circulating. The Biological Action of Sildenafil CitrateViagra™. Sildenafil is broken down in the liver by hepatic metabolism using cytochrome p450 enzymes, mainly. Xenobiotica. 1999 Mar;293297-310. Pharmacokinetics and metabolism of sildenafil in mouse, rat, rabbit, dog and man. Walker DK1, Ackland MJ, James GC.

     
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