Itrapex

Generic Name: Itraconazole

Therapeutic Class: Antifungal

View Prescribing Detail

Composition
Itrapex 100 Capsule: Each capsule contains Itraconazole pellets equivalent to Itraconazole USP 100 mg.
Pharmacology
Itraconazole is an orally active triazole antifungal drug that has demonstrated a broad spectrum of activity and favorable
pharmacokinetic profile. 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.
Indication
Itrapex (Itraconazole) is used for the treatment of oropharyngeal candidiasis, vulvovaginal candidiasis, pityriasis versicolor, tinea
pedis, tinea cruris, tinea corporis, tinea manuum, onychomycosis, histoplasmosis. It is indicated in the treatment of systemic
candidiasis, aspergillosis, and cryptococcosis (including cryptococcal meningitis). It is also used for maintenance therapy in AIDS
patients to prevent relapse of underlying fungal infections and in the prevention of fungal infection during prolonged neutropenia.
Dosage & Administration
Oropharyngeal candidiasis: 100 mg daily (200 mg daily in AIDS or neutropenia) for 15 days. Vulvovaginal candidiasis: 200 mg
twice daily for 1 day. Pityriasis versicolor: 200 mg daily for 7 days. Tinea corporis and tinea cruris: either 100 mg daily for 15 days
or 200 mg daily for 7 days. Tinea pedis and tinea manuum: either 100 mg daily for 30 days or 200 mg twice daily for 7 days.
Onchomyoycosis: 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. EIC infections (aspergillosis, candidiasis and
cryptococcosis including Cryptococcal meningitis) where other antifungal drugs inappropriate or ineffective: 200 mg once daily,
increased in invasive or disseminated disease and in cryptococcal meningitis to 200 mg twice daily. Histoplasmosis: 200 mg 1-2
times daily. Maintenance in AIDS patient to prevent relapse of underlying fungal infection and prophylaxis in neutropenia when
standard therapy is inappropriate: 200 mg once daily increased to 200 mg twice daily if low plasma ltraconazole concentration is
detected. Child dose: The recommended dose is 3 to 5 mg/kg/day.
Contraindication
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.
Precaution
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 Itraconazole. The drug should be administered after
a full meal. Rarely, cases of hepatitis and jaundice have been reported mainly in patients treated tor longer than one month. It is
therefore, advised to monitor liver function in patients receiving continuous treatment of more than one month.
Side Effect
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.
Use in Pregnancy & Lactation
Itraconazole is contraindicated in pregnancy. Breastfeeding while receiving itraconazole is not recommended.
Drug Interaction
The drugs like terfenadine, astemizole, cisapride, HMG-CoA reductase inhibitors such as simvastatin, oral midazolam or
triazolam should not be given concurrently with Itraconazole. Significant interactions also observed during co-administration of
rifampin, phenytoin, phenobarbital, digoxin, and calcium channel blockers.
Overdose
Itraconazole is not removed by dialysis. In the event of accidental overdosage, supportive measures should be employed.