Axoral Ketoconazole Tablets USP

AXORAL
Ketoconazole Tablets USP 200mg

 

COMPOSITION

Each uncoated tablet contains:

Ketoconazole USP 200 mg

Excipients q.s.

 

PHARMACOLOGICAL ACTION

Ketoconazole is a synthetic imidazole dioxolaine derivative, active in vitro against dermatophytes, yeasts and other pathogenic fungi. In vitro Ketoconazole is fungicidal and, therefore, suppresses the formation of mycelia. In vivo, at therapeutic levels however, it is primarily fungistatic. Ketoconazole acts in the case of C. albicans by inhibiting lanosterol demethylation in the biosynthesis of ergosterol, resulting in cell membrane defects.

 

PHARMACOKINETICS

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.

 

INDICATIONS

AXORAL TABLETS is indicated for:

Treatment of superficial and deep mycoses:

-Systemic mycotic infections such as systemic candidiasis;

-Chronic and recurrent vaginal candidiasis not responding to topical treatment;

-Serious chronic infections of the skin, hair and nails caused by sensitive dermatophytes, e.g. Trichophyton rubrum, T. mentagrophytes, and/or yeasts (dermatomycoses, paronychia, serious chronic mucocutaneous candidiasis, etc.);

-When topical treatment is ineffective owing to the involvement of large areas of the skin, or lesions penetrating the deeper dermal layers, nails and hair.

 

CONTRAINDICATIONS

AXORAL TABLETS are contraindicated in persons with a history of hypersensitivity to Ketoconazole.

 

DOSAGE

Adult: The recommended starting dose is a single daily administration of 200mg (1 tablet). In very serious infections or where its clinical responsiveness is insufficient, the dose may be increased to 400mg (2 tablets) once daily.

Children: 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 is one or two weeks.

 

OVERDOSAGE

In the event of accidental overdosage, supportive measures including gastric lavage with Sodium bicarbonate should be employed.

 

ADVERSE EFFECTS

Gastrointestinal disturbances are the most frequently reported adverse effect following the oral administration of Ketoconazole. Nausea, vomiting, diarrhoea, constipation, abdominal pain and pruritis. Rarely headache, dizziness, impotence, somnolence, fever, chills, photophobia, gynecomastia, thrombocytopenia, leucopenia and hemolytic anemia.

 

PRECAUTIONS

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.

 

DRUG INTERACTIONS

Drugs like Terfenadine, astemizole, mizolastine, cisapride, triazolam, oral midazolam, dofetllide, quinidine, pimozide, CYP3A4 metabolised HMG-Co A reductase inhibitors such as simvastatin and lovastatin should not be used during treatment with Ketoconazole.

 

USE IN PREGNANCY AND LACTATION

Pregnancy: Ketoconazole is teratopenic in small, laboratory animals.
No studies are available on its use in pregnant women. Therefore it must not be administered during pregnancy.

Lactation: Since Ketoconazole is excreted in the milk, mothers who are under treatment should not breast feed.

 

SHELF LIFE

36 months from the date of manufacturing.

 

STORAGE

Store in a cool, dry and dark place.

Keep all medicines out of reach of children.

 

PRESENTATION

Alu-Alu blister pack of 10 tablets in a carton with pack insert.

 

NAFDAC Reg. No: B4-5194

 

Manufactured in India by

DUPEN LABORATORY PVT., LTD.

C/1-49 & 36, Degam Road,

Industrial Township – Vapi 396 195

 

Sole Agent

AXIOM DRUGS LTD.

13 Olowu Street, Ikeja,

Lagos, Nigeria.

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