Sildenafil (as citrate) 100 mg
Each film coated tablet contains: Sildenafil Citrate equivalent to Sildenafil 100 mg
Sildenafil is indicated for the treatment of erectile dysfunction.
For most patients, the recommended dose is 50 mg taken, as needed approximately 1 hour before sexual activity. However, Sildenafil 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.
The following factors are associated with increased plasma levels of sildenafil: age> 65 (40% increase in AUC), hepatic impairment (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%). 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 patients.
Sildenafil was administered to over 3700 patients (aged 19-87 years) during clinical trials worldwide. Over 550 patients were treated for longer than one year. In placebo-controlled clinical studies, the discontinuation rate due to adverse events for Sildenafil (2.5%) was not significantly different from placebo (2.3%). The adverse events reported with Sildenafil were generally transient and mild to moderate in nature.
In trials of all designs. adverse events reported by patients receiving Sildenafil were generally similar. When Sildenafil was taken as recommended (on an as-needed basis) in flexible dose, placebo-controlled clinical trials, adverse events reported by 2% of patients (more frequently with Sildenafil than placebo) were headache, flushing, dyspepsia, nasal congestion, urinary tract infection, diarrhea, dizziness, rash, and abnormal vision (mild and transient, predominantly color tinge to vision, but also increased sensitivity to light or blurred vision).
Other adverse reactions occurred at a rate of > 2%, but equally common on placebo: respiratory tract infection, back pain, flu syndrome. and arthralgia. In fixed-dose studies, dyspepsia (17%) and abnormal vision (11%) were more Common at 100 mg than at lower doses. At doses above the recommended dose range, adverse events were similar to those detailed above but generally were reported more frequently.
Use of Sildenafil is contraindicated in patients with a known hypersensitivity to any component of the tablet Consistent with its known effects on the nitric oxide/cGMP pathway. Sildenafil was shown to potentiate the hypotensive effects of nitrates, and its administration to patients who are concurrently using organic nitrates in any term is therefore contraindicated.
Effects of Other Drugs on Sildenafil:
in vitro studies: Sildenafil metabolism is principally mediated by the cytochrome P4SO (CYP) isoforms 3A4 (major route) and 209 (minor route). Therefore, inhibitors of these isoenzymes may reduce Sildenafil clearance.
In vivo studies: Cimetidne (800 mg), a non-specific CYP inhibitor, caused a 56% increase in plasma Sildenafil concentrations when co-administered with Sildenafil (50 mg) to healthy volunteers.
Stronger CYP3A4 inhibitors such as ketoconazole, itraconazale or mibefraCil would be expected to have still greater effects, and population data trom patients in clinical trials did indicate a reduction in Sildenafil clearance when it was co-administered with CYP3A4 inhibitors (such as ketoconazole, erythromycin, or cimetidine). It can be expected that concomitant administration of CYP3A4 inducers. such as rifarnpin, will decrease plasma levels of sildenafil.
Single doses 0t antacid (magnesium hydroxide/ aluminum hydroxide) did not affect the bioavailability 0t sildenafil
Pharmacokinetic data from patients in clinical trials showed no effect on Sildenafil pharmacokinetics of CYP2C9 inhibitors (such as tolbutamide, warfarin),
peak plasma concentrations or approximately 1 11M after recommended doses, it is unlikely that Sildenafil will alter the clearance 01 substratos of these isoenzymes.
In vivo studies: NO significant interactions were shown with tolbutamide (250 mg) or wartarin (40 mg), both of which are metabolized by CYP2C9.
Sildenafil (50mg) did not potentiate the increase in bleeding time caused by aspirin (150 mg),
Sildenafil (50 mg) did not potentiate the hypotonsivo effect of alcohol in healthy volunteers with mean maximum blood alcohol levels of 0.08%.
NO interaction was seen when Sildenafil (100 mg) was co-administered with amlodipine in hypertensive patients. The mean additional reduction on supino blood pressure (systolic, 8 mm Hg; diastolic, 7 mm Hg) was of a similar magnitude to that seen when Sildenafil was administered alone to healthy volunteers.
Analysis of the safety database showed no difference in the side effect profile in patients taking Sildenafil with and without anti-hypertensive medication.
Carcinogenesis, Mutagenesis, Impairment of Fertility Sildenafil was not carcinogenic when administered to rats and mice. Sildenafil was negative in in vitro bacterial and Chinese hamster ovary cell assays to detect mutagenicity, and in vitro human lymphocytes and in vivo mouse micronucleus assays to detect clastogenicity. No evidence 0t teratogenecity, embryotoxicity or fetotoxicity was observed in animal studies.
There was no impairment of fertility in rats given Sildenafil up to 60 mgÀg/day for 36 days to females and 102 days to males, a dose producing an AUC value of more than 25 times the human male AUC.
There was no effect on sperm mortality or morphology after single 100 mg oral doses of Sildenafil in healthy volunteers.
Sildenafil is not indicated for use in women
here are no adequate and well-controlled studies of Sildenafil in pregnant women. Sildenafil is not indicated in pregnant women.
Lactation Sildenafil is not indicated in nursing mothers.
In Studies with healthy volunteers of single doses up to 800 mg, adverse events were similar to those seen at lower doses but incidence rates were increased.
In cases of overdose, standard supportive measures should be adopted as required. Renal dialysis is not expected to accelerate clearance as Sildenafil is highly bound to plasma proteins and it is not eliminated in the urine.
Store below 30°C and protect from light and moisture.
Erecto-100 Blister of 4 Tablets
Farnoush Darou Teb Co.