I-Zol Capsule

Itraconazole inhibits Cytochrome P-450 dependent enzymes resulting in impairment of the biosynthesis of ergosterol, a major component of the cell membrane of yeast and fungal cells. Being integral to the proper functioning of the cell membrane, inhibition of the synthesis of ergosterol leads to a cascade of abnormalities in permeability, membrane bound enzyme activity, and co-ordination of chitin synthesis leading to inhibition of growth, abnormal cell wall formation and accumulation of intracellular lipids and membranous vesicles.

SUBA (Super Bio-available) technology is a novel technology for enhancing the bioavailability of poorly soluble drugs. This technology utilizes a solid dispersion of drug in a polymer that improves the dissolution of poorly soluble drugs compared to their normal crystalline form. SUBA technology Itraconazole is an orally active triazole antifungal drug that has demonstrated a broad spectrum of activity and favorable pharmacokinetic profile.

100 & 200 mg preparation:
For non-systemic fungal disease-

• Vulvovaginal candidiasis: 200 mg twice daily for 01 day
• Pityriasis versicolor: 200 mg once daily for 07 days
• Tinea corporis, tinea cruris: 100 mg once daily for 15 days or 200 mg once daily for 7 days
• Tinea pedis, tinea manuum: 100 mg once daily for 30 days
• Oropharyngeal candidiasis: 100 mg once daily for 15 days, Increase dose to 200 mg once daily for 15 days in AIDS or neutropenic patients because of impaired absorption in these groups.
• Onychomycosis (toenails with or without fingernail involvement): Either 200 mg daily for 3 months or course (pulse) of 200 mg twice daily for 7 days, subsequent courses repeated after 21 days' interval. Fingernails two courses, toenails three courses.

For systemic fungal disease-

• Aspergillosis: 200 mg once daily for 2-5 months Increase dose to 200 mg twice daily in case of invasive or disseminated disease
• Candidiasis: 100-200 mg once daily for 3 weeks-7 months. Increase dose to 200 mg twice daily in case of invasive or disseminated disease
• Non-meningeal Cryptococcosis: 200 mg once daily for 10 weeks
• Cryptococcal meningitis: 200 mg twice daily for 2-6 months
• Histoplasmosis: 200 mg once daily twice daily for 8 months
• Maintenance in AIDS: 200 mg once daily until immune recovery
• Prophylaxis in neutropenia: 200 mg once daily until immune recovery

The dose and duration of treatment for systemic antifungal disease should be adjusted depending on the clinical response.

65 mg & 130 mg preparation:
For non-systemic fungal disease-

• Vulvovaginal candidiasis: 130 mg twice daily for 1 day
• Pityriasis versicolor: 65 mg twice daily for 7 days
• Tinea corporis and tinea cruris: 65 mg daily for 15 days OR 65 mg twice daily for 7 days
• Tinea pedis and tinea manuum: 65 mg once daily for 30 days
• Oropharyngeal Candidiasis: 65 mg once daily for 15 days, increase dose to 65 mg twice daily for 15 days in AIDS or neutropenic patients because of impaired absorption in these groups.
• Onychomycosis (toenails with or without fingernail involvement): Either 65 mg twice daily for 3 months or course (pulse) of 130 mg twice daily for 7 days, subsequent courses repeated after 21 days interval. Fingernails two courses, toenails three courses.

For systemic fungal disease-

• Aspergillosis: 65 mg twice daily for 2-5 months.Increase dose to 130 mg twice daily in case of invasive or disseminated disease
• Candidiasis: 65-130 mg once daily for 3 weeks-7 months. Increase dose to 65 mg twice daily in case of invasive or disseminated disease
• Non-meningeal Cryptococcosis: 65 mg twice daily for 10 weeks
• Cryptococcal meningitis: 130 mg twice daily for 2-6 months
• Histoplasmosis: 130 mg once daily-twice daily for 8 months
• Maintenance in AIDS: 65 mg twice daily until immune recovery
• Prophylaxis in neutropenia: 65 mg twice daily until immune recovery

The dose and duration of treatment for systemic anti-fungal disease should be adjusted depending on the clinical response.

pediatric use: The efficacy and safety of the Itraconazole capsule have not been established in pediatric patients.

The drugs like terfenadine, astemizole, cisapride, HMG-CoA reductase inhibitors such as simvastatin, oral midazolam or triazolam should not be given concurrently with I-Zol. Significant interactions also observed during co-administration of rifampin, phenytoin, phenobarbital, digoxin, and calcium channel blockers. There is no experience of overdosage with I-Zol.

Itraconazole is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation. Patients who have severe hepatic disease are not advised to take Itraconazole. It is not advisable to use the drug in patients taking rifampin, which appears to initially inhibit and then enhance the metabolism of Itraconazole.

Nausea, abdominal pain, dyspepsia, constipation, headache, dizziness, raised liver enzymes, menstrual disorders, allergic reactions (including pruritus, rash, urticaria and angioedema), hepatitis and cholestatic jaundice, peripheral neuropathy and Stevens-Johnson syndrome reported. On prolonged use hypokalaemia, oedema and hair loss reported.

Itraconazole is contraindicated in pregnancy. Breast feeding while receiving Itraconazole is not recommended.

Absorption is impaired when gastric acidity is reduced. In patients receiving acid neutralizing medicines (e.g. aluminium hydroxide), these should be administered at least 2 hours after the intake of I-Zol. The drug should be administered after a full meal. Rarely, cases of hepatitis and jaundice have been reported mainly in patients treated for longer than one month. It is therefore, advised to monitor liver function in patients receiving continuous treatment of more than one month.

Drugs for subcutaneous and mycoses

Store below 25°C, in a cool & dry place. Keep away from light. Keep all the medicine out of the reach of children.