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Sildenafil citrate medical information!
Remember that no medicine is for everyone. If you use nitrate drugs, often used to control chest pain (also known as angina), don't take Sildenafil citrate. This combination could cause your blood pressure to drop to an unsafe or life-threatening level. Be sure to ask your doctor if your heart is healthy enough for sexual activity.
For most patients, the recommended dose is 50 mg taken, as needed, approximately 1 hour before sexual activity. However, sildenafil citrate may be taken anywhere from 4 hours to 0.5 hour before sexual activity. Based on effectiveness and toleration, the dose may be increased to a maximum recommended dose of 100 mg or decreased to 25 mg. The maximum recommended dosing frequency is once per day.
Following Factors are Associated with Increased Plasma Levels of Sildenafil:
Age >65 (40% increase in AUC), hepatic
(e.g., cirrhosis, 80%), severe renal impairment (creatinine clearance
<30 ml/min, 100%), and concomitant use of potent cytochrome P450 3A4
inhibitors (erythromycin, ketoconazole, itraconazole, 200%, saquinavir
210%). Since higher plasma levels may increase both the efficacy and incidence
of adverse events, a starting dose of 25 mg should be considered in these
Recommended Storage: Store at controlled room temperature, 15-30°C (59-86°F).
in vitro have shown that sildenafil is selective for PDE5. Its effect
is more potent on PDE5 than on other known phosphodiesterases (>80-fold
for PDE1, >1000-fold for PDE2, PDE3, and PDE4). The approximately 4000-fold
selectivity for PDE5 versus PDE3 is important because that PDE is involved
in control of cardiac contractility. Sildenafil is only about 10-fold
as potent for PDE5 compared to PDE6, an enzyme found in the retina; this
lower selectivity is thought to be the basis for abnormalities related
to color vision observed with higher doses or plasma levels (see Pharmacodynamics).
Consistent with its known effects on the nitric oxide/cGMP pathway, it was shown to potentiate the hypotenive effects of nitrates and its administration to patients who are using organic nitrates, either regularly and/or intermittently, in any form is therefore contraindicated.
After patients have taken sildenafil citrate, it is unknown when nitrates, if necessary, can be safely administered. Based on the parmacokinetic profile o a single 100 mg oral dose given to healthy normal volunteers, the plasma levels of sildenafil at 24 hours post dose are approximately 2ng/ml (compared to peak plasma levels of approximately 440ng/ml, in the following patients: age >65, hepatic impairment (e.g, creatinine clearance <30mL/min), and concomitant use of potent cytochrome P450 3A4 inhibitors (erythromycin), plasma levels of sildenafil at 24 hours post dose have been found to be 3 to 8 times higher than those seen in healthy volunteers. Although plasma levels of sildenafil at 24 hours post dose are much lower than at peak concentration, it is unknown whether nitrates can be safely coadministered at this time point. It is contraindicated in patients with a known hypersensitivity to any component to the tablet.
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