Ketoral 200 Ketoconazole Tablets

KETORAL-200

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.

 

NET CONTENT

Each uncoated tablet contains:

Ketoconazole USP 200 mg

Excipients q.s.

 

CLINICAL PHARMACOLOGY

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.

 

PHARMACOKINETICS

Absorption

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.

Distribution

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.

Metabolism

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.

Excretion

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.

 

CONTRAINDICATION

In patients with a known hypersensitivity to ketoconazole, to any of the other excipients, or to any other imidazole antifugal.

 

INTERACTIONS

Oral anticoagulant, busulphan, docetaxel, erlotinib, ciclosporin, tacrolimus, budesonide, fluticasone, dexamethasone.

 

WARNINGS

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

Pregnancy

Not recommended.

Lactation

Ketoconazole is excreted in the milk, mothers who are under treatment should not breast-feed whilst being treated with Ketoral 200 mg tablets.

 

PRECAUTIONS

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.

 

ADVERSE REACTION

Headache, dizziness, somnolence, nausea, vomiting, abdominal pain, diarrhea, pruritus, rash.

 

DRUG ABUSE AND DEPENDENCE

Not applicable.

 

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

Not applicable.

 

PRESENTATION

1 x 10 tablets packed in a carton along with Patient information leaflet.

 

STORAGE CONDITION

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

 

Manufactured by

Saga Laboratories

Survey No. 198/2 & 198/3

Chachrawadi Vasna, Taluka Sanand

District Ahmedabad-382 210, Gujarat, India.

 

Sole Agent

Embassy Pharmaceutical & Chemicals Ltd.

41 Ademola Street South West Ikoyi,

Lagos Nigeria