Product INN: Itraconazolum
Deva: 100 mg hard capsules
Product ATC Code: J02AC02
ITRANOLS® 100 mg hard capsules are indicated for the treatment of the following diseases:
- Vulvovaginal candidiasis.
- Pityriasis versicolor
- Oropharyngeal candidiasis.
- Fungal keratitis
- Onychomycosis caused by dermatophytes and/or yeasts.
- Systemic mycoses: aspergillosis, candidosis, cryptococcosis (including cryptococcal meningitis), histoplasmosis, sporotrichosis, paracoccidioidomycosis, chromomycosis, blastomycosis.
Product Mechanism of Action
Itraconazole impairs the synthesis of ergosterol in fungal cells. Ergosterol is a vital cell membrane component in fungi and impairment of its synthesis ultimately results in an antifungal effect. Fungal resistance to azole derivatives develops slowly and often is a result of multiple genetic mutations. Prevalence of acquired resistance in different geographical areas may vary in different species. Cross-resistance to azole derivatives was observed in Candida sp. According to the CLSI (Clinical and Laboratory Standard Institute) data itraconazole minimum inhibitory concentration (MIC) in case of Candida sp. infection is ≤ 0.125 mg / L, resistant in fungus, the MIC of which is ≥ 1 mg / L. Itraconazole MIC can vary greatly. Itraconazole MIC90 is <1 mg / L.
Commonly susceptible species: Aspergillus spp.2, Blastomyces dermatitidis1, Candida albicans, Candida parapsilosis, Cladosporium spp. Coccidioides immitis1, Crytococcus neoformans, Crytococcus neoformans, Epidermophyton floccosum, Fonsecaea spp.1, Geotrichum spp., Histoplasma spp., Malassezia (formerly Pityrosporum) spp., Microsporum spp. Paracoccidioides brasiliensis1, Penicillium marneffei1, Pseudallescheria boydii, Sporothrix schenckii, Trichophyton spp., Trichosporon spp.
Species for which acquired resistance may be a problem: Candida glabrata3, Candida krusei, Candida tropicalis3.
Resistant species : Absidia spp., Fusarium spp., Mucor spp. Rhizomucor spp., Rhizopus spp.
Scedosporium proliferans, Scopulariopsis spp.
1 This fungal infection can occur in patients who have returned from a trip outside Europe.
2 There have been reports of itraconazole resistance to Aspergillus fumigatus.
3 Characteristic average sensitivity.
Product Therapeutic Indications
Cryptococcosis (including cryptococal meningitis): Patients with suppressed immune system and patients with cryptococcosis, and cryptococcosis of central nervous system are indicated itraconazole only if the usual recommended initial therapy is inadequate or ineffective.
Aspergillosis: Itraconazole can be used for the treatment of invasive aspergillosis in patients who are resistant or intolerant to treatment with amphotericin B.
Due to pharmacokinetic properties of itraconazole for oral use (capsules) it should not be used to initiate treatment in patients with severe life-threatening systemic mycosis . After starting treatment with i.v. administered itraconazole (see section 4.4) oral dosage forms of the drug can be used to continue therapy.
The official national guidelines for using of antifungal products should be taken into account.
Itraconazole maximal absorption is achieved when ITRANOL® capsules are used immediately after a meal. The capsule should be swallowed whole with water.
- Vulvovaginal candidiasis: 200 mg twice daily during one day or 200 mg once daily for 3 days.
Skin and eye disorders:
- Dermatomycose: 200 mg once daily for 7 days or 100 mg once daily for 15 days(1).
- Pituriasis versicolor: 200 mg once daily for 7 days.
- Oropharyngeal candidiasis: 100 mg once daily for 15 days(2).
- Fungal keratitis: 200 mg once daily for 21 days. Treatment duration can change according to clinical response reaction.
1) In case of Tinea pedis and Tinea manus the drug should be used at a dose of 200 mg twice daily for 7 days or 100 mg once daily for 30 days.
2) Bioavailability of ITRANOL® may be reduced in some patients with immunosupression such as AIDS and neutropenic patients, patients after organ transplantation, therefore the dose of the medicine may be doubled.
- Pulse therapy and continuous therapy can be used for the treatment of onychomycosis.
Pulse therapy: Take 2 capsules twice daily (200 mg twice daily) for 1 week (one pulse). For fingernail infections 2 pulses are recommended, for toenails infections 3 pulses are recommended. The pulse treatments are separated by a 3-week period without ITRANOL®
Continuous therapy: In case of toenails with or without fingernail infections the medicine should be taken at a dose of 200 mg once daily during 3 months.
Elimination of itraconazole from skin and nails is slower than from plasma.
Optimal clinical and mycological responses reaction is achieved within 2-4 weeks after cessation of skin infections treatment and 6-9 months after the cessation of nail infections treatment when the nails are grown.
Duration of systemic fungal infections treatment depends on clinical and mycological responses reaction for therapy.
Reduced gastric juice acidity:
If gastric juice acidity is lower, itraconazole absorption impairs. Due to the impaired itraconazole absorption in AIDS patients and patients with neutropenia itraconazole plasma concentration is decreased. Itraconazole blood concentration should be monitored in these patients, and if necessary, the dose should be increased.
Clinical data on the use of itraconazole in paediatric patients are limited. Itraconazole should be used in paediatric patients only in exceptional cases, when the potential benefit outweighs the potential risk.
The medicine is not recommended for use in the elderly.
Impaired hepatic function:
The restricted data are available of itraconazole oral use in patients with liver function disturbances. A careful dose adjustment should be considered for this group of patients.
Impaired renal function:
The restricted data are available of itraconazole oral use in patients with renal function disturbances. A careful dose adjustment should be considered for this group of patients.
Medicines unreasonable use is harmful to health.