Ketozole


Composition:
Each tablet contains:
Ketoconazole              200 mg

Pharmacological Properties:

Ketoconazole is a synthetic broad–spectrum antifungal agent. It inhibits the biosynthesis of ergosterol, a major component of the cell membrane of yeast & fungal cells. Ketozole tablets are active against clinical infections with Blastomyces dermatitidis, Candida spp., Coccidioides immitis, Histoplasma capsulatum, Paracoccidioides brasiliensis & Phialophora SPP. Ketozole tablets are also active against Trichophyton spp, Epidermophyton spp. & Microsporum spp.

Pharmacokinetics:
Ketoconazole is readily but incompletely absorbed after oral dosing.
Mean peak plasma levels (~ 3.5 µg/ml) are reached within 1-2 hours, following oral administration of single 200 mg dose. The major route of excretion is through the bile into the intestinal tract. It is extensively bound to human plasma protein (99%). Ketoconazole undergoes hepatic metabolism.

Indications:
•    Ketozole tablets are indicated for the treatment of the following systemic fungal infections:
     Candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis & paracoccidioidomycosis.
•    Ketozole tablets are also indicated for the treatment of patients with severe, recalcitrant cutaneous dermatophyte infections who have not responded to topical therapy or oral griseofulvin, or who are unable to take griseofulvin.

Contraindications:
•    Preexisting liver disease.
•    Hypersensitivity to imidazole drugs.

Warnings:
•    Hepatotoxicity, primarily of the hepatocellular type, has been associated with the use of ketozole tablets. Liver function tests should be measured before starting treatment & at frequent intervals during treatment.
•    Patients receiving ketozole tablets 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.
•    In rare cases anaphylaxis has been reported after the first dose.

Precautions:
•    Ketozole tablets decrease ACTH-induced corticosteroid serum levels at higher doses.
•    Antacids, anticholinergics & H2–blockers should be given at least two hours after administration of ketozloe tablets.
•    Patients should be instructed to report any signs & symptoms which may suggest liver dysfunction (unusual fatigue, anorexia, nausea &/or vomiting, jaundice, dark urine or pale stools) so that appropriate biochemical testing can be done.

Drug interactions:
•    Ketozole tablets inhibit the metabolism of terfenadine, astemizole & cisapride leading to increased plasma concentration of these drugs resulting in prolonged Q T intervals.
•    Ketozole tablets may alter the metabolism of cyclosporine resulting in elevated plasma concentrations of the latter.
•    Coadministration of ketozole tablets with midazolam or triazolam has resulted in elevated plasma concentrations of the latter two drugs causing potentiation & prolongation of their sedative & hypnotic effects.
•    Concomitant administration of rifampin with ketozole tablets reduces the blood levels of the latter. INH (Isoniazid) is also reported to affect ketozole concentrations adversely.
•    Ketoconazole enhance anticoagulant effect of coumarin like drugs, so their effect should be monitored.
•    Oral hypoglycemic agents effects are enhanced by ketoconazole.

Pregnancy:
In view of its embryotoxic effects in animals, ketoconazole is contraindicated in pregnancy.

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

Side effects:
Most frequent adverse effects are nausea &/or vomiting, abdominal pain & pruritus. Headache, hemolytic anemia, impotence may occur in less than 1% of the patients.

Overdosage:
In the event of accidental overdosage, supportive measures including gastric lavage with sodium bicarbonate, should be done.

Dosage & Administration:
Adults:
One tablet once daily (200 mg/day).
In very serious infections, the dose of ketozole may be increased to two tablets once daily (400 mg/day).
Children:
Children over 2 years of age: 3.3-6.6 mg/kg once daily.
Therapeutic category: Antifungal agent

Legal category: Prescription only medicine.

Storage: Store in a dry place at a temperature below 30º C, protect from light.

Package: Box containing 10 tablets.

THIS IS A MEDICAMENT
Medicament is a product, which affects your health and its consumption contrary to instructions is dangerous for you. Follow strictly the doctor’s prescription, the method of use and the instructions of the pharmacist who sold the medicament.
- The doctor and the pharmacist are the experts in medicines, their benefits and risks.
- Do not by yourself interrupt the period of treatment prescribed.
- Do not repeat the same prescription without consulting your doctor.
- Keep all medicaments out of reach of children.

Council of Arab Health Ministers, Union of Arab Pharmacists.