ZEAGRA Tablet

ZEAGRA is indicated for the treatment of Erectile Dysfunction(ED).

Dosage& Administration

For most patients, the recommended dose is 50mg taken, as needed, approximately 1 hour before sexual activity. However, ZEAGRA may be taken anywhere from 4 hours to 30 minutes before sexual activity. Based on effectiveness and toleration, the dose may be increased to a maximum recommended dose of 100mg or decreased to 25mg. The maximum recommended dosing frequently is once per day.

Consistent with its known effects on the nitric oxide/cGMP pathway, ZEAGRA was shown to potentiate the hypotensive effects on nitrates and its administration to patients who are using organics nitrates, either regularly and/or intermittently, in any form is therefore contraindicated, ZEAGRA is contraindicated in patients with a known hypersensitivity to any component of the tablet.

There is a potential for cardiac risk of sexual activity in patients with pre-existing cardiovascular disease. Therefore, treatments for erectile dysfunction, including ZEAGRA should not generally used in men for whom sexual activity is inadvisable because of their underlying cardiovascular status.

There is no controlled clinical data on the safety or efficacy of ZEAGRA in the following groups, if prescribed, this should be done with caution:

- Patients who have suffered a myocardial infarction, stroke of life-threatening arrhythmia within the last 6 months.

- Patients with resting hypotension (BP<90/50) or hypertension (BP>170/110).

- Patients with cardiac failure or coronary artery disease causing unstable angina.

- Patients with retinitis pigmented.

A reduction in sildenafil clearance occurs when it was co-administered with CYP3A4 inhibitors, such as ketoconazole, itraconazole, erythromycin or cimetidine. It can be expected that concomitant administration of CYP3A4 inducers, such as rifampin will decrease the plasma levels of sildenafil.

Co-administration with HIV protease inhibitors ritonavir/saquinavir results in increase in sildenafil Cmax&Plasma AUC.

ZEAGRA is not indicated for use in new borns, children or women.

Commonly reported adverse events of patients treated with sildenafil include the following:

headache(16%), flushing(10%), dyspepsia(7%), nasal congestion(4%), abnormal vision(3%), diarrhea(3%), dizziness(2%), resh(2%).

In studies with healthy volunteers of single doses up to 800mg adverse events were similar to those seen at lower doses but incidence rates were increased.

An oral therapy for erectile dysfunction (ED), is the citrate salt of sildenafil, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specified Phosphodiesterase type 5 (PDE5).

Sildenafil citrate is designed chemically as 1-{(3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1 H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl) sulfonyl}-4-methylpiperazine citrate and has a molecular weight of 666.7.

The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. Nitric Oxide (NO) then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation in the courpus cavernosum and allowing inflow of blood. Sildenafil has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of nitric oxida (NO) by inhibiting phos-phodiesterase type 5 (PDE5), which is responsible for degeneration of cGMP in the corpus cavernosum.

When sexual stimulation cause local release of nitric oxide (NO),inhibition of PDE5 by sildenafil causes increased levels of cGMP in the corpus cavernosum, Sildenafil at recommended doses has no effect in the absence of sexual stimulation.