1, African Church close, off Coker Road, Ilupeju, Lagos, Nigeria
Tel: 01-773-1473, 01-8179648, 08033160649
Rajat Pharmachem Limted, Plot 307-311, G.I.D.C, Ankleshwar – 393002, Gujarat, India.
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN:04-5909): Ketoconazole USP 200 mg.
Pack size: 1 blister of 10 tablets in a box.
The absorption of Ketoconazole from the gastrointestinal tract is variable and increases with decreasing stomach pH. Mean peak plasma concentrations of about 3.5 micrograms/mL have been obtained 2 hours after administration of 200 mg by mouth. Systemic absorption following topical or vaginal application in healthy subjects is minimal.
Ketoconazole is more than 90% bound to plasma proteins, mainly albumin. It is widely distributed and appears in breast milk. Penetration into the CSF is poor.
The elimination of Ketoconazole is reported to be biphasic, with an initial half-life of 2 hours and a terminal half-life of about hours.
Ketoconazole is contraindicated in patients who have shown hypersensitivity to the drug. Co-administration of Ketoconazole with Terfenadine is contraindicated. Rare cases of serious cardiovascular adverse effects including death, ventricular tachycardia and torsades de pointes have been observed with patients taking Ketoconazole concomitantly with Terfenadine. This is due to increased Terfenadine concentrations induced by Ketoconazole.
Co-administration of Ketoconazole with Astemizole is contraindicated. Oral Ketoconazole inhibits the metabolism of Astemizole resulting in elevated plasma concentration of Astemizole and its active metabolite desmethylastemizole which may prolong QT intervals.
Co-administration of Ketoconazole and Cisapride is contraindicated. Serious cardiovascular adverse effects including ventricular tachycardia, ventricular fibrillation and torsades de pointes have occurred in patients taking both drugs concomitantly.
Kentoconazole tablets have been demonstrated to lower the serum testosterone. Testosterone levels are impaired with doses of 600 mg per day and aborted by 1000 mg per day.
Patients should be instructed to report any sign and symptoms which may suggest liver dysfunction so that appropriate biochemical testing can be done. Such signs and symptoms may include unusual fatigue, anorexia, nausea and vomiting, jaundice, dark urine and pale stools.
Gastrointestinal disturbances are the most frequently reported adverse effect following the oral administration of Ketoconazole. Nausea, vomiting, diarrhea, constipation, abdominal pain and pruritus. These adverse effects are dose-related and may be reduced by giving Ketoconazole with food.
Rarely headache, dizziness, impotence, somnolence, fever, chills, photophobia, gynecomastia, thrombocytopenia, leucopenia and hemolytic anemia.
Asymptomatic transient elevations in serum concentrations of liver enzymes may occur. Hepatitis may occur and the risk appears to increase, if treatment with Ketoconazole is prolonged; it is usually reversible on discontinuation of Ketoconazole but fatalities have occurred.
Endocrine effects include gynaecomastia and adrenal cotex suppression.
Dosage & Administration
The recommended starting dose is single daily administration of 200 mg (1 tablet). In very serious infections or where its clinical responsiveness is insufficient, the dose may be increased to 400 mg (2 tablets) once daily.
In children over 2 years of age, a single daily dose of 3.3 mg/kg is recommended. The tablets have not been studied in children under 2 years of age.
Treatment should be continued until indication the active fungal infection has subsided. Minimum treatment period for Candidiasis one or two weeks. Patients with chronic mucocutaneous candidiasis usually require maintenance therapy.
Minimum treatment for recalcitrant dermatophyte infection four weeks.
In the event of accidental overdosage, supportive measures including gastric lavage with Sodium bicarbonate should be employed.
Store in a cool and dry place, protect from light.