Generic Viagra Medical Drug Information | . |
Sildenafil citrate was shown to potentiate the hypotensive effects of nitrates and its administration in patients who use nitric oxide donors or nitrates in any form is therefore contraindicated. Recommended Storage: Store at controlled room temperature, 15-30°C (59-86°F). Mechanism of Action Studies 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 citrate 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. Medicine Contraindications References: Consistent with its known effects on the nitric oxide/cGMP pathway, sildenafil citrate 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, 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. Sildenafil is contraindicated in patients with a known hypersensitivity to any component o the tablet. |
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