Composition : Itraconazole Capsules
Itraconazole Capsule is one of the triazole antifungal agents that inhibits cytochrome P-450-dependent enzymes resulting in impairment of ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis & aspergillosis.
Itraconazole is indicated for the treatment of the following fungal infections when thought likely to be susceptible:
- Vulvovaginal candidiasis.
- Pityriasis versicolor.
- Dermatophytoses caused by organisms susceptible to itraconazole .e.g. tinea pedis, tinea cruris, tinea corporis, tinea manuum.
- Oral candidiasis.
- Onychomycosis caused by dermatophytes and/or yeasts.
Itraconazole is contraindicated in patients with known hypersensitivity to the active substance or to any of the followingexcipients :Sugar spheres,Poloxamer 188, Hypromellose, Capsule shell.
Side effects :
Vomiting, diarrhoea, headache, stomach upset, or dizziness may occur.
Itraconazole is an imidazole/triazole type antifungal agent. Itraconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethylation via the inhibition of the enzyme cytochrome P450 14α-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 α-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Itraconazole exhibits in vitro activity against Cryptococcus neoformans and Candida spp. Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to Cryptococcus neoformans and for systemic infections due to Candida albicans.
Mechanism of action :
Itraconazole interacts with 14-α demethylase, a cytochrome P-450 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. Itraconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
- Do not store above 25°C.
- Store in the original package in order to protect from moisture.