ITRAFIX 100

Each hard gelatin capsule contains:

Itraconazole Pellets equivalent to Itraconazole BP 100mg

Capsule for Oral Use

Itraconazole is an imidazole/triazole type antifungal agent. It is a highly selective inhibitor of fungal cytochrome P-450. It interacts with 14 α-demethylase, a cytochrome P450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents.

Bioavailability: 55%, rapidly and well absorbed after oral administration. Oral bioavailability is maximal when the capsules are taken immediately after meal.

Half- life: 17 hrs after single dose and increases to 34 to 42 hrs after repeated dosing.

Protein Binding: 99.9%

Distribution: Itraconazole is extensively distributed into most tissues that are prone to fungal invasion but only minimally to CSF and ocular fluid. Concentrations in lungs, kidney, liver, bone, stomach, spleen and muscle are found to be 2 to 3 times higher than the corresponding plasma concentration.

Metabolism: Hepatic metabolism. Hydro-oxy Itraconazole is one of its metabolite which has in vitro antifungal activity comparable to Itraconazole.

Excretion: 35% via urine, 54% via faeces

• Superficial Dermatocycoses not responding to topical treatment.
• Fungal Keratitis which has failed to respond to topical treatment or where the disease is progressing rapidly.
• Pityriasis not responding to any other treatment.
• Vulvovaginal candidiasis not responding to topical treatment.
• Oral Candidiasis in immunocompromised patients.
• Onchomycosis caused by Dermatophytes.
• Systemic Mycoses
• Fluconazole resistant fungal meningitis

ADVERSE REACTION:

Common: Dizziness, Headache, Nausea, Vomitting, Diarrhoea, Abdominal Pain, Constipation, Dyspepsia.

Rare: Allergic reactions such as pruritus, rash, urticaria

Very Rare: Liver Hepatitis

DOSAGE AND ADMINISTRATION:

Superficial Dermatocycoses:

• Tinea Corporis, Tinea Curis: 100 mg daily for 2 weeks.
• Tinea Pedis, Tinea Manus: 100 mg daily for 4 weeks.

Fungal Keratitis:

• 2 capsules (200mg) once daily for 3 weeks.

Pityriasis versicolor:

• 2 capsules (200mg) once daily for 1 week.

Vulvovaginal Candidiasis

• 2 capsules (200mg) morning and evening for 1 day or 2 capsules (200mg) once daily for 3 days and also on the 1^st day of menses for 6 cycle.

Oral Candidiasis in immunocompromised patients:

• 1 Capsule (100mg) or 2 Capsules (200 mg) daily for 4 weeks.

Onychomycosis:

• 2 capsules (200 mg) once daily for 3 months   OR
• Pulse Therapy

Fingernail involvement only: 200 mg twice daily for 1 week; repeat 1-week course after 3-week off-time

Toenails with or without fingernail involvement): 200 mg twice daily for 1 week; repeat 1-week course twice with 3-week off-time between each course

Systemic Mycoses:

Aspergilosis: 200mg OD for 2-5 months. Increase dose to 200mg BID in cases of invasive or disseminated disease.

Histoplasmosis: 200 mg OD- BID for 8 month. Continue as necessary in AIDS Patients.

Sporotrichosis: 100 mg OD for 3 months.

Candidiasis: 100-200 mg OD for 3weeks – 7 months

CONTRAINDICATIONS:

• Hypersensitivity to Itraconazole
• Congestive heart failure, patient with ventricular dysfunction
• Must not be used during pregnancy

WARNINGS AND PRECAUTIONS:

• Caution should be used when co-administrating Itraconazole and calcium channel blockers.
• Discontinue if liver disease develops and perform liver function test.
• Itraconazole should not be used within 2 weeks after discontinuation of treatment with CYP3A4 inducing agents (Rifampicin, Rifabutin, Phenobarbital, Phenytoin, Carbamazepine).The use of Itraconazole with these drugs may lead to subtherapeutic plasma levels of Itraconazole and leads to treatment failure.