Each tablet contains Ketoconazole 200 mg.
Pharmacotherapeutic classification: Antimycotics for systemic use, imidazole derivatives.
PHARMACOLOGY: Pharmacodynamics: Ketoconazole is a synthetic imidazole derivative with a fungicidal (normal concentrations) or fungistatic activity (high concentrations) in in-vitro studies.
Ketoconazole is active against clinical infection with Blastomyces dermatitidis, Candida sp., Coccidioides immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis and Phialophora sp. Ketoconazole is also active against Trichophyton sp., Epidermophyton sp., and Microsporum sp. Ketoconazole is also active in vitro against a variety of fungi and yeast.
Ketoconazole inhibits the biosynthesis of ergosterol in fungi and changes the composition of other lipid components in the membrane.
Pharmacokinetics: Absorption: Ketoconazole is a weak dibasic agent and thus requires acidity for dissolution and absorption. Mean peak plasma levels of approximately 3.5 μg/ml are reached within 1 to 2 hours, following oral administration of a single 200 mg dose taken with a meal.
Distribution: In vitro, the plasma protein binding is about 99% mainly to the albumin fraction. Only a negligible proportion of ketoconazole reaches the cerebral-spinal fluid.
Metabolism: Following absorption from the gastrointestinal tract, ketoconazole is converted into several inactive metabolites. The major identified metabolic pathways are oxidation and degradation of the imidazole and piperazine rings, oxidative O-dealkylation and aromatic hydroxylation.
Excretion: About 13% of the dose is excreted in the urine, of which 2 to 4% is unchanged drug. The major route of excretion is through the bile into the intestinal tract. Subsequent plasma elimination is biphasic with a half-life of 2 hours during the first 10 hours and 8 hours thereafter.
Systemic fungal infections such as Blastomycosis caused by Blastomyces dermatitidis, Chromomycosis caused by Phialophora spp., Coccidioidomycosis caused by Coccidioides immitis, Paracoccidioidomycosis caused by Paracoccidioides brasiliensis.
Ketoconazole should not be used for fungal meningitis because it penetrates poorly into the cerebrospinal fluid.
Ketoconazole Tablets are indicated for the treatment of systemic fungal infections in patient who have failed or who are intolerant to other therapies
Children ≥ 2 years: 3.3 - 6.6 mg/kg/day as a single dose for 1 - 2 weeks for candidiasis, for at least 4 weeks in recalcitrant dermatophyte infections, and for up to 6 months for other systemic mycoses.
Adults: The recommended starting dose of ketoconazole is a single daily administration of 200 mg. In very serious infections or if clinical responsiveness is insufficient within the expected time, the dose of ketoconazole may be increased to 400 mg once daily. Minimum treatment for candidiasis is 1 or 2 weeks. Minimum treatment for recalcitrant dermatophyte infections is 4 weeks in cases involving glabrous skin. Minimum treatment for the other indicated systemic mycoses is 6 months.
There is no known antidote to ketoconazole.
In the event of accidental overdosage supportive measures, including gastric lavage with sodium bicarbonate, should be employed.
Hypersensitivity to ketoconazole or any component of the medicine.
Do not use for the treatment of CNS fungal infections due to poor CNS penetration.
Coadministration with terfenadine, astemizole, cisapride, or oral triazolam due to risk of potentially fatal cardiac arrhythmias.
When used orally, ketoconazole has been associated with hepatic toxicity, including some fatalities. Use with caution in patients with impaired hepatic function. Liver function tests (such as alkaline phosphatase, ALT, AST and bilirubin) should be measured before starting treatment and at frequent intervals during treatment. Patients receiving ketoconazole concurrently with other potentially hepatotoxic drugs should be carefully monitored, particularly those patients requiring prolonged therapy or those who have had a history of liver disease.
Ketoconazole requires acidity for dissolution. If concomitant antacids, anticholinergics, and H2-blockers are needed, they should be given at least 2 hours after administration of ketoconazole.
Effects on ability to drive and use machines: No effects have been observed. However, patients should not take ketoconazole with antacids; this may cause dizziness and effect the ability to drive and use machines.
Use in Children: Ketoconazole has not been systematically studied in children of any age, and essentially no information is available on children younger than 2 years. Therefore, it should not be used in pediatric patients unless the potential benefit outweighs the risks.
Pregnancy: There are no adequate and well-controlled studies in pregnant women. FUNGAZOL TABLETS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Since ketoconazole is probably excreted in the milk, mothers who are under treatment should not breastfeed.
The following adverse reactions were found in 1% to 10% of the patients:
Dermatologic: Pruritus (1.5%).
Gastrointestinal: Nausea/vomiting (3% to 10%), abdominal pain (1.2%).
The following adverse reactions were found in less than 1% of the patients: Bulging fontanelles, chills, depression, diarrhea, dizziness, fever, gynecomastia, headache, hemolytic anemia, hepatotoxicity, impotence, leukopenia, photophobia, somnolence, thrombocytopenia.
Concomitant administration of ketoconazole with the following drugs may result in decreased plasma concentrations of ketoconazole.
Antacids: increased gastric pH may inhibit ketoconazole absorption.
Consider giving antacid ≥2 hours after ketoconazole.
Sucralfate: the therapeutic effects of ketoconazole may be reduced; therefore, should be administered ≥2 hours before sucralfate.
Proton pump inhibitor: the bioavailability of ketoconazole may be decreased because of a possible reduction in tablet dissolution in the presence of a high gastric pH.
Histamine H2 antagonists: increased gastric pH may inhibit ketoconazole absorption.
Isoniazid: bioavailability of ketoconazole may be decreased.
Rifampicin: decreased serum levels of either drug may occur. Avoid concurrent use if possible.
Theophyllines: decreased absorption of theophylline may occur, resulting in decreased theophylline serum levels.
Ketoconazole may increase the plasma levels of cyclosporine, tacrolimus, methylprednisolone, midazolam, triazolam, digoxin, hypoglycemic agents, indinavir, ritonavir, saquinavir, tricyclic antidepressants, carbamazepine, quinidine, sulfonylureas, buspirone, HMG-CoA reductase inhibitors, nisoldipine, zolpidem, warfarin, corticosteroids and drugs primarily metabolized by the cytochrome P-450 3A4 enzyme system that could increase or prolong both therapeutic and adverse effects. Therefore, appropriate dosage adjustments may be necessary.
Coadministration of ketoconazole with terfenadine, astemizole and/or cisapride is contraindicated. Ketoconazole inhibits the metabolism of terfenadine, astemizole and cisapride resulting in increased plasma concentrations of these drugs which may prolong QT intervals. Serious cardiovascular adverse events including ventricular tachycardia, ventricular fibrillation and torsades de pointes have been observed in patients taking ketoconazole concomitantly with these drugs.
Store at temperature not exceeding 30°C.
J02AB02 - ketoconazole ; Belongs to the class of imidazole derivatives. Used in the systemic treatment of mycotic infections.
Fungazol tab 200 mg
25 × 10's
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