Ketoconazole Tablets USP 200 mg.
Each uncoated tablets contains:
Ketoconazole USP 200mg
Ketoconazole is a synthetic imidazole dioxolane 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 level, however it is primarily fungi static. Ketoconazole acts in the case of C. albicans by inhibiting lanosterol demethylation in the biosynthesis of ergo sterol, resulting in cell membrane defects.
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, Tmentagropytes and/or yeasts (dermatomycoses, paronychia, serious mucocutaneous candidiasis etc);
• When topical treatment is ineffective owing to the involvement of large areas of the skin, or lesion penetrating the deeper dermal layer nails and hair;
• Serious mycoses of the gastro-intestinal tract not responsive to other therapy or when the organism is resistant to other therapy;
• Serious chronic mucocutaneous candidiasis not responsive to other therapy or when the organism is resistant to other therapy;
• Pulmonary, oral and/or disseminated histoplasmosis; and
Ketoconazole is contra- indicated in patients who have shown hypersensitivity to it or any of its ingredients. Ketoconazole should not be given to patients with pre-existing liver disease. Ketoconazole is not recommended during pregnancy, as Ketoconazole has been shown to be teratogenic in animals. Ketoconazole should not be used by breastfeeding mothers. Ketoconazole is not intended for use in children, as safety has not been proven. The concomitant administration of terfenadine and astemizole with Ketoconazole is contra-indicated.
Patients taking Ketoconazole should avoid alcohol. Cases have been reported of a disulfiram – like reaction to alcohol, characterised by flushing peripheral oedema, nausea and headache. Hepatitis has been reported during treatment with Ketoconazole. If symptoms or signs suggestive of hepatic dysfunction are detected medication should be stopped at once. Patients on Ketoconazole should be instructed to report any of the prodromal symptoms of hepatitis such as fatigue associated with nausea or vomiting, jaundice, dark urine or pale stools, immediately and stop treatment.
DOSAGE AND DIRECTIONS FOR USE
As directed by the physician.
Note: Ketoconazole should be taken with meats for maximal absorption. Effective absorption depends upon intact gastric activity; hence concomitant administration with drugs that reduce gastric secretion (ant cholinergic drugs antacids and H2 blockers) should be avoided. When indicated, these drugs should not be taken within two hours after Ketoconazole.
SIDE – EFFECT AND SPECIAL PRECAUTIONS
Side-effects: Nausea, vomiting, gastro- intestinal complaints, constipation, headache, dizziness, somnolence or drowsiness, photophobia, paraesthesia, thrombocytopenia, exanthema or itching have been reported. Increases in serum liver enzymes may occur. Anaphylactoid reactions, alopecia, urticaria, rash, transient decreased libido, reversible gynaecomastia and oligospermia may occur.
Serum cortisol levels may decrease and response of cortisol on ACTH may be blunted. The adrenal function should therefore be monitored in patients with adrenal insufficiency or with borderline adrenal function and in patients under prolonged periods of stress (major surgery intensive care etc)
Interactions: The concomitant administration of rifampicin or isoniazid with Ketoconazole reduces the blood level of the latter. Both drugs should not be administered concomitantly.
Since Ketoconazole inhibits certain hepatic oxidase enzymes, it may decrease the elimination of co-administered drugs whose metabolism depends on such enzymes. Increased levels of such drugs, when used together with Ketoconazole have been associated with an increase in side – effects.
Known examples of serious interactions include those with cyclosporine, terfenadine astemizole, cisapride oral midazolam, triazole anticoagulants (e.g. warfarin) methylprednisolone, phenytoin and possibly busulphane and tacrolimus. Terfenadine astemizole cisapride, oral midazolam and triazotam, should not be used by patients using Ketoconazole. Ketoconazole interacts with certain anti – retroviral agents, namely didanosine saquinavir, ritonavir and indinavir.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
See Side – effects and Special Precautions. In the event of accidental over dosage, supportive and symptomatic measures including gastric lavage with sodium bicarbonate should be employed.
Store below 30°C. Protect from light and moisture.
Keep all medicines away from children.
Pack of 10’ Tablets
NAFDAC Reg. No.: A4-6804
Maydon Pharmaceutical Ltd
15, Wilmer Street, Off Town Planning way,
Manufactured in India by
Maxheal Laboratories Pvt. Ltd.
H.O.: 401, Maxheal House, Bangur Nagar, Goregaon-W,
Factory: 2-7/80-85, SURSEZ, Sachin, Dist.
Dist. Surat, Gujarat-394230.