Antifungal azoles miconazole

Azole antifungals -azole Fluconazole, miconazole Fungal infections [35]... 

Other inhibitors of HZ formation are thought to act similarly to the quinohne family. Binding of the antifungal azole-based drugs (clotrimazole, ketoconazole, and miconazole) to heme is thought to damage parasite cell membranes and cause... 

For details of interactions with individual antifungal azoles, see individual monographs (fluconazole, itraconazole, ketoconazole, miconazole, and voriconazole). 

The indications for miconazole have diminished with the advent of newer antifungal azoles (3) and it has largely been superseded by other azoles infection with Pseudallescheria boydii remains one of the few indications (4). 

The azole antifungal drug ketoconazole was found to inhibit Fe(III)-ascorbate dependent lipid peroxidation using either rat hver microsomes or ox-brain phospholipid hposomes as the substrates (Wiseman et al. 1991). It also inhibited microsomal peroxidation induced by the Fe(III)-ADP/NADPH system. The related azoles, miconazole and clotrimazole, were much weaker inhibitors than ketoconazole. Ketoconazole was approximately equipotent... 

Raab [123] presented a discussion on the topical clinical pharmacology of miconazole and two other azole antifungal agents. 

Azole antifungals (fluconazole, itraconazole, ketoconazole, miconazole)... 

The azole derivatives for systemic administration include the imidazoles ketoconazole and miconazole and the triazoles fluconazole, itraconazole, posaconazole and voriconazole. They are broad spectrum antifungals and have activity against several dermatophytes, Candida, Cryptococcus and other fungi that cause deep-seated infections. 

CILOSTAZOL ANTIFUNGALS Fluconazole, itraconazole, ketoconazole and miconazole t cilostazol levels These azoles inhibit CYP3A4-mediated metabolism of cilostazol Avoid co-administration... 

CARBAMAZEPINE ANTIFUNGALS - ITRACONAZOLE, KETOCONAZOLE, MICONAZOLE, POSACONAZOLE, VORICONAZOLE 1 plasma concentrations of itraconazole and of its active metabolite, ketoconazole, posaconazole and voriconazole, with risk of therapeutic failure, t carbamazepine plasma concentrations These azoles are highly lipophilic, and clearance is heavily dependent upon metabolism by CYP isoenzymes. Carbamazepine is a powerful inducer of CYP3A4 and other CYP isoenzymes (CYP2C18/19, CYP1A2), and the result is very low or undetectable plasma levels. Inhibition of P-gp t bioavailability of carbamazepine Avoid co-administration of posaconazole or voriconazole with carbamazepine. Watch for inadequate therapeutic effects, and t dose of itraconazole. Higher doses of itraconazole may not overcome this interaction. Consider use of the less lipophilic fluconazole, which is less dependent on CYP metabolism. Necessary to monitor carbamazepine levels... 

B. Azole antifungals include systemic agents such as keto-conazole, fluconazole, itraconazole, and voriconazole. Topical agents used for the treatment of vaginal candidiasis and thrush include miconazole and clotrimazole. The pharmacologic properties of the systemic azoles differ considerably. Ketoconazole, the first oral azole developed, has poor bioavailability and requires an acidic environment for enhanced absorption. Thus, initial studies required ketoconazole to be administered with a cola to increase bioavailability. Fluconazole, unlike itraconazole and ketoconazole, is hydrophillic and has increased penetration across the blood-brain barrier. Fluconazole is also the only azole that is renally eliminated. 

Fig. 4.3 Structures of polyene (amphotericin B) and azole (itraconazole, fluconazole, miconazole and ketoconazole) antifungal agents.

Ketoconazole (KC) as the first systemlcally-active azole antifungal has been the subject of a number of reviews including the general management of fungal disease,and its efficacy in superficial and systemic infections 0 it was the subject of a number of papers at a recent symposium, The use of KC in the treatment of coccidioidomycosis has been recently reviewed in detail, 2 gjid parallel reviews of the indications for coccidioidomycosis treatment in general, 5 and the use of AMB and miconazole (MC) 5 in particular have been presented. 

The evidence suggests that all the azole antifungals can raise ciclosporin levels to a greater or lesser degree. Ketoconazole may cause five- to tenfold rises, while itraconazole, fluconazole and voriconazole may cause two- to threefold rises. A case report suggests that intravenous miconazole interacts similarly and in theory, miconazole oral gel may also interact. Posaconazole may also modestly raise ciclosporin levels. Rhabdomyolysis has been reported with the combination of ciclosporin and itraconazole, but four of these cases were complicated by the presence of statins. 

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