Composition:
Sildenafil citrate equivalent to sildenafil base 50mg
Excipients: Lactose, dicalci phosphate, starch, microcrystalline cellulose, polyvinyl pyrrolidone, hydroxypropylmethyl cellulose, polyethylene glycol 6000, silicon dioxide, talc, magnesium stearate, sodium glycolat starch, indigotin q.s 1 tablet
Pharmaceutical form: Film-coated tablet.
Presentation: Box of 1 blister x 4 tablets.
pharmacodynamics: Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. cGMP is degraded by enzyme phosphodiesterase type 5 (PDE5). The inhibition of phosphodiesterase type 5 (PDE5) enhances erectile function by increasing the amount of cGMP. ACTIV-GRA (sildenafil) inhibits PDE5.
Because sexual stimulation is required to initiate the local release of nitric oxide, the inhibition of PDE5 by sildenafil has no effect in the absence of sexual stimulation. Therefore, ACTIV-GRA raises natural response to sexual stimulation.
Indication: ACTIV-GRA is indicated for the treatment of erectile dysfunction (impotence).
Contraindications
- Drug is contraindicated for patients known hypersensitivity to any product components.
- Administration of drug to patients who are using any form of nitrate is contraindicated.
- Women and children under 18 years of age.
- Severe liver impairment.
Precautions
- Sildenafil has vasodilation feature which may result in minor and intermittent hypotensive effect. Patients with left ventricular outflow obstruction, (e.g., aortic stenosis and idiopathic hypertropic subaortic stenosis) can be sensitive to the action of vasodilators, including PDE5 inhibitors.
- Safe use of sildenafil in following groups of patients is inadequately established, therefore, the use of sildenafil is not recommended in these groups until further information is available. Including patients with a myocardial infarction, stroke, or life-threatening arrhythmia within the last 6 months. Patients with cardiac failure or coronary artery disease causing unstable angina, hypotension (<90/50 mmHg), hypertension (>170/100 mmHg), patients with known hereditary degenerative retinal disorders, including retinitis pigmentose.
- This drug should be used with caution in patients with anatomical deformation of the penis (such as angulations, cavernosal fibrosis or Peyronie's disease) or in patients who have conditions which may predispose them to priapism (such as sickle cell anemia, multiple myeloma or leukemia).
Effects on ability to drive and operate machines
Studies of effects on driving and machinery operating person have not been reported adequately. However, if you have any of symptoms such as headache, dizziness or visual changes, do not drive or operate machinery.
Drug interactions
- Sildenafil metabolism is principally mediated by the cytochrome P450 (CYP) isoforms 3A4 (major route) and 2C9 (minor route). Simultaneous administration of CYP3A4 inhibitors such as ketoconazol, itraconazol, erythromycin, clarithromycin and sildenafil may remarkably increase sildenafil level in serum. Otherwise, when administrated concomitantly sildenafil with the drugs that induce CYP3A4, such as rifampicin, phenobarbital, phenytoin and carbamazepin, the level sildenafil can be decreased.
Dosage
- The recommended dose
The recommended starting dose of ACTIV-GRA is a tablet (50mg)/time, taken prior to anticipated sexual activity from 30 minutes to 1 hour. The maximum recommended dosing frequency is once a day in most patients.
Based on individual effectiveness and toleration, the dose may be increased to 100mg (2 tablets) or decreased to 25mg per time. The maximum recommended dose is 100mg per time a day.
- Geriatrics: A starting dose of 25mg should be considered. Based on individual efficacy and tolerability, the dose may be gradually increased.
- Severe renal impairment (creatinine clearance <30 ml/min): A starting dose of 25 mg should be considered. Based on individual efficacy and tolerability, the dose may be gradually increased.
- Severe hepatic impairment: The use of ACTIV-GRA is not recommended.
Administration: ACTIV-GRA is administrated by oral route. In all cases, you should strictly follow physician's instructions.
Side effects: Sildenafil was administered to over 3700 men during clinical trials worldwide. Sildenafil is generally well-tolerated. The reported side effects are normally mild to moderate in nature. Most common side effects: headache, flushing, stomach-ache, mild and temporary visual changes (color perception changes, light perception changes and blurred vision), stuffy nose, indigestion and diarrhea.
Report any side effects to your doctor during period of treatment
Self-life: 36 months from the date of manufacturing.
Storage: Store in a dry and cool place below 28oC, protect from light.
Specification: Manufacturer's.
