Itraconazole Aspergillus

The spectrum of action of azole medications is broad, including many Candida species, C neofbrmans, the endemic mycoses (blastomycosis, coccidioidomycosis, histoplasmosis), the dermatophytes, and, in the case of itraconazole and voriconazole, even aspergillus infections. They are also useful in the treatment of intrinsically amphotericin-resistant organisms such as P boydii. 

Aspergillus species Voriconazole Amphotericin B, itraconazole, caspofungin... 

Three patients with culture proven Aspergillus flavus corneal ulcers and hypopyon who did not respond to 5% topical natamycin, 0.15% amphotericin B solution, or oral itraconazole, received intracameral amphotericin B injections and had complete resolution of the ulcer and hypopyon (Kaushik et al.). 

A small prospective study reported that 13 of 14 patients with severe fungal keratitis (Aspergillus, Pusarium, and Candida ) had resolution with subconjunctival fluconazole after failing to respond to topical and systemic fluconazole and itraconazole therapy. No local or systemic toxic side effects were reported (Yihnaz and Maden). 

The combination of amphotericin with ketoconazole appears to lead to antagonism (148). A study of the effects of combinations of amphotericin with fluconazole, itraconazole, or ketoconazole against strains of Aspergillus fumigatus in vitro showed antagonistic effects in some strains, but different effects in other strains (152). In one group of mice infected with Candida, combinations of amphotericin with fluconazole were more effective... 

Pleural and subsequent pericardial effusion developed in a woman treated with itraconazole 200 mg bd for a localized pulmonary infection with Aspergillus fumiga-tus (SEDA-18, 282). After more than 9 weeks of treatment she developed a pericardial effusion, which necessitated drainage. Itraconazole was withdrawn. Six weeks later, and 2 weeks after the resumption of itraconazole, she developed signs of pulmonary edema and cardiac enlargement. These signs disappeared rapidly on discontinuation of itraconazole. 

Saperconazole is an experimental, water-insoluble, lipophilic, fluorinated triazole. Its structure resembles that of itraconazole and it has a long half-life. It has a broad antifungal spectrum, including Cryptococcus Species and Aspergillus species. In early studies in cases of compassionate use, only a few adverse effects were described, including hepatotoxicity (1,2), and its adverse effects were expected to resemble those of itraconazole (3). However, the manufacturers stopped developing it because of concerns about toxicity. 

Itraconazole is a triazole with a broad spectrum of activity against filamentous fungi it is particularly effective against Aspergillus spp. Lack of availability of a formulation suitable for topical ophthalmic use may be a problem. A noncommercial, 1% itraconazole-30% dimethyl sulfoxide ointment preparation used topically in trials in the northeastern USA was found to be effective in 8 out of 10 horses with keratomycosis (Ball et al 1997). It may be given orally, at 3 mg/kg twice daily, in conjunction with topical administration, but it is expensive. 

Aspergillus spp. in vitro K Anidulafungin and itraconazole or voriconazole show a synergistic antifungal activity, while anidulafungin and amphotericin B show low in vitro activity against Aspergillus spp. and... 

Mann, P.A., and Perlin, D.S. (2003) Multiple resistance mechanisms among Aspergillus fumigatus mutants with high-level resistance to itraconazole. Antimicrobial Agents and Chemotherapy, 47, 1719-1726. 

Aspergillus spp. Skin, pulmonary, central nervous system Amphotericin B 1 mg/kg/day 5-flucytosine itraconazole 200-400 mg daily lipid-associated amphotericin B 4-5 mg/kg daily caspofungin 50 mg daily voriconizole 4 mg/kg every 12... 

Antifungal prophylaxis does not decrease the incidence of invasive mold infections. In addition to environmental precautions, strategies being investigated for Aspergillus prophylaxis in neutropenic patients include oral itraconazole, low (0.1-0.25 mg/kg per day) to moderate (0.5 mg/kg per day) doses of amphotericin B, intranasal and aerosolized amphotericin B, and hpid-associated amphotericin B products. None of these interventions can be recommended routinely in clinical practice at this time. 

Posaconazole - a derivative of itraconazole which provides cover against Aspergillus, Candida species and Cryptococcus but is only available in an oral formulation. 

Itraconazole. Itraconazole (18) is a highly lipophilic compound with a triazole structure. Compared to ketoconazole, itraconazole has a broader spectrum (including Aspergillus spp.) (29,30) and an in vitro activity that is 10 times higher than ketoconazole for most species. 

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