Ketoconazole Tablets USP 200 mg
DOSAGE FORM AND STRENGTH
Oral Solid Dosage Form: Tablets
Strength: 200 mg
HISTORY OF ACTIVE INGREDIENTS
Ketoconazole is a synthetic, imidazole-derived medication used primarily to treat fungal infections.
Each uncoated tablet contains:
Ketoconazole USP 200 mg
Ketoconazole is an imidazole-dioxolane anti-mycotic, which is effective after oral administration and has a broad spectrum of activity against dematophytes, yeast and other pathogen fungi.
In vitro studies have demonstrated that ketoconazole impairs the synthesis of ergosterol in fungai cells. Ergosterol is a vital cell membrane component in fungi. Impairment of its synthesis ultimately results in an antifungal effect.
Ketoconazole is a weak dibasic agent and thus requires acidity for dissolution and absorption. Mean peak plasma concentrations 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.
In vitro, the plasma protein binding is about 99%, mainly to the albumin fraction. Ketoconazole is widely distributed into tissues; however, only a negligible proportion of ketoconazole reaches the cerebral-spinal fluid.
Following absorption from the gastro-intestinal 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.
Plasma elimination is biphasic with a half-life of 2 hours during the first 10 hours and 8 hours thereafter. 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.
INDICATION AND USAGE
Treatment of dermatophylosis and Malassezia (previously called Pityrosporum) folliculitis that cannot be treated topically because of the site, extent of the lesion or deep infection for the skin, in patients resistant to or intolerant of both fluconazole and itraconazole.
In patients with a known hypersensitivity to ketoconazole, to any of the other excipients, or to any other imidazole antifugal.
Oral anticoagulant, busulphan, docetaxel, erlotinib, ciclosporin, tacrolimus, budesonide, fluticasone, dexamethasone.
Because of the risk for serious hepatic toxicity, Ketoral 200 mg tablets should be used only when the potential benefits are considered to outweigh the potential risks, taking into consideration the availability of other effective antifungal therapy.
PREGNANCY AND LACTATION
Ketoconazole is excreted in the milk, mothers who are under treatment should not breast-feed whilst being treated with Ketoral 200 mg tablets.
Liver function must be monitored in all patients receiving treatment with Ketoral 200 mg tablets.
Monitor liver function prior to treatment to rule out acute or chronic liver disease.
Headache, dizziness, somnolence, nausea, vomiting, abdominal pain, diarrhea, pruritus, rash.
DRUG ABUSE AND DEPENDENCE
SYMPTOMS OF OVERDOSE AND ANTIDOTE
No specific data are available.
DOSAGE AND ADMINISTRATION
There is no known antidote to ketoconazole.
In the event of accidental overdose, treatment consists of supportive measures. Within the first hour after ingestion gastric lavage may be performed. Activated charcoal may be given if considered appropriate.
THE PREPARATION FOR USE
1 x 10 tablets packed in a carton along with Patient information leaflet.
Keep in a cool, dry and dark place at a temperature not exceeding 30oC.
Keep medicines out of reach of children
NAFDAC REG. NO.: 04-9538
Survey No. 198/2 & 198/3
Chachrawadi Vasna, Taluka Sanand
District Ahmedabad-382 210, Gujarat, India.
Embassy Pharmaceutical & Chemicals Ltd.
41 Ademola Street South West Ikoyi,