Sildenafil pharmacokinetics

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    Sildenafil pharmacokinetics


    This study will evaluate the pharmacokinetics and safety of sildenafil in premature infants. Up to 8 will receive a single intravenous dose of sildenafil, and up to 16 additional participants will be enrolled if they receive sildenafil as part of standard care. The study will be open to children of both sexes and all racial and ethnic groups. The study is expected to last approximately 24 months; each subject in the single-dose study will participate for up to 8 days. The most common health problem associated with premature birth is bronchopulmonary dysplasia. Up to 20% of infants with bronchopulmonary dysplasia develop pulmonary arterial hypertension, and up to 40% of these infants die. Food and Drug Administration for the treatment of pulmonary arterial hypertension in adults. Currently, few drugs are available to prevent bronchopulmonary dysplasia, and none can reduce mortality in infants with bronchopulmonary dysplasia and pulmonary arterial hypertension. The effectiveness of sildenafil in pediatric pulmonary hypertension patients has not been established. Although sildenafil studies in premature infants at risk for or diagnosed with pulmonary arterial hypertension are limited, the drug is increasingly being used off-label in this fragile population. Erectile dysfunction (ED) is highly prevalent in men with renal disease. The clearance of sildenafil citrate, a highly effective oral treatment for ED, is decreased in men with severe renal insufficiency, but the pharmacokinetic and hemodynamic profiles during maintenance hemodialysis in men with end-stage renal disease have not been studied. Fifteen men undergoing chronic outpatient maintenance hemodialysis received a single 50-mg oral dose of sildenafil on 2 occasions, once 2 hours before, and once 2 hours after hemodialysis, with randomized assignment to sequence. Blood and dialysate samples were collected, and hemodynamic measurements were made. Hemodialysis did not significantly clear either sildenafil or its primary metabolite, UK-103,320. Administration after hemodialysis was associated with a 17% higher peak plasma concentration and earlier time to peak, which were not clinically meaningful, whereas the overall extent of absorption and the elimination half-life were not affected. The average extent of drug bound to plasma protein was approximately 96% in hemodialysis patients.

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    Sep 21, 2006. sildenafil, vardenafil and tadalafil are largely determined by their. pharmacokinetics and pharmacokinetic pharmacodynamic PK/PD. Results. Hemodialysis did not significantly clear either sildenafil or its primary metabolite, UK-103,320. Administration after hemodialysis was associated with a 17%. Clinical Therapeutics/Volume 36, Number 2, 2014. Pharmacokinetics of a Novel Orodispersible Tablet of. Sildenafil in Healthy Subjects. Bharat Damle, PhD. 1.

    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.

    Sildenafil pharmacokinetics

    Pharmacokinetics and Pharmacodynamics of Sildenafil in a Pat., The pharmacokinetics and hemodynamics of sildenafil. -.

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  5. Oct 10, 2018. To determine the absolute bioavailability, dose proportionality and the effects of food on the pharmacokinetics of single oral doses of sildenafil.

    • Pharmacokinetics of sildenafil after single oral doses in healthy male..
    • Pharmacokinetics of a Novel Orodispersible Tablet of Sildenafil in..
    • Pharmacokinetics of Sildenafil in Premature Infants - Full Text..

    The pharmacokinetics and hemodynamics of sildenafil citrate in male hemodialysis patients. Aug 29, 2018. Several papers reported that Sildenafil pharmacokinetics are altered in response to food-drug or drug-druginteractions.5,15-17 It has been. Sep 24, 2018. Sildenafil citrate, a highly selective phosphodiesterase type 5 inhibitor, is used to treat pulmonary hypertension PH in veterinary medicine.

     
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