What are the azole drugs?
Azole antifungal agents have added greatly to the therapeutic options for treatment of systemic fungal infections. The azoles that are available for systemic use can be classified into two groups: the triazoles (fluconazole, itraconazole, voriconazole, posaconazole, and isavuconazole) and the imidazoles (ketoconazole).
What is the mechanism of azole drug?
The main mechanisms of azole resistance include alterations in the C. glabrata ERG11 gene (CgERG11), which encodes the azole target enzyme, and upregulation of the CgCDR1 and CgCDR2 genes, which encode efflux pumps.
Which type of infections are treated by use of azoles?
Azole antifungal agents can be used to treat fungal infections of the body and skin, including athlete’s foot, onychomycosis (fungal nail infections), ringworm, and vaginal candidiasis.
Why are azole drugs effective as an antifungal treatment?
The azole class of antifungal drugs acts by inhibiting the synthesis of ergosterol, which is the major sterol in fungal cell membranes. This drug class can be divided into the imidazoles (e.g., clotrimazole, miconazole, ketoconazole), and the triazoles (e.g., fluconazole, itraconazole, voriconazole, posaconazole).
Is amphotericin B an azole?
In general, the results of studies of amphotericin B-azole combinations obtained in animal models of aspergillosis, can- didiasis, and cryptococcosis have been remarkably consistent, even though the strains of organisms, the animal used, the routes of infection, and the treatment regimens have varied.
What enzyme do azoles target?
Cytochrome P450 of
Cytochrome P450 of fungi: primary target for azole antifungal agents.
Which azole is most hepatotoxic?
The azole fluconazole and voriconazole showed a higher hepatotoxic potential; anidulafungin showed in higher concentrations (5x Cmax, 10x Cmax) a severe impairment of hepatocyte vitality, viability, and function.
What are the side effects of azoles?
The most common adverse effect of topical azoles is local skin and mucous membrane irritation. The most common adverse effects of systemic azoles are gastrointestinal distress, morbilliform rash, and hepatotoxicity.
Is metronidazole an azole?
Metronidazole and ketoconazole belong to different drug classes. Metronidazole is an antibiotic and ketoconazole is an azole antifungal. Brand names of Metronidazole include Flagyl and Flagyl ER.
Is nystatin an azole?
Azoles, fluconazole in particular, have become the mainstay of therapy over the past few years. These include topical and systemic agents. Posaconazole is the most recent addition to this group of antifungals. Polyenes include amphotericin B, liposomal amphotericin B formulations, and topical nystatin.
What is an azole?
Jump to navigation Jump to search. Azoles are a class of five-membered heterocyclic compounds containing a nitrogen atom and at least one other non-carbon atom (i.e. nitrogen, sulfur, or oxygen) as part of the ring.
What are azole antifungals?
Azole antifungals. What are Azole antifungals? Azole antifungals are a group of medicines that contain an azole ring and inhibit the growth of a wide range of fungi.
What is the role of azole in the treatment of mycoses?
For over 20 years, amphotericin B was the mainstay of treatment of serious systemic mycoses. The first oral azole, ketoconazole, was introduced in the United States in 1981 and provided an alternative to amphotericin B for nonmeningeal, non-life-threatening infections and for outpatient treatment of histoplasmosis and blastomycosis (132).
What are the treatment options for relapsing azole toxicity?
Following primary therapy with amphotericin B or an azole, most patients require lifelong maintenance therapy to prevent relapse.