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The rising fungal resistance to fluconazole and related azole drugs spurs the need to find effective combative solutions swiftly. Rising resistance raises concerns since fluconazole is commonly used due to its inexpensiveness and ease of administration, according to the World Health Organization.
Later, triazoles fluconazole and itraconazole, with a broader spectrum of antifungal activity and improved safety profile were developed. In order to overcome limitations such as sub-optimal spectra of activity, drug-drug interactions, toxicity, development of resistance and unfavorable pharmacokinetics, analogues were
Topical antifungal drugs are used to treat fungal infections on the skin, scalp, nails, vagina or inside the mouth. These medications come as creams, gels, lotions, ointments, powders, shampoos, tinctures and sprays. Most antifungal drugs induce fungal cell death by destroying the cell wall of the fungus.
[23] [13] First made in 1977, [20] ketoconazole was the first orally-active azole antifungal medication. [23] However, ketoconazole has largely been replaced as a first-line systemic antifungal medication by other azole antifungal agents, such as fluconazole and/or itraconazole , because of ketoconazole's greater toxicity, poorer absorption ...
Itraconazole is a relatively well-tolerated drug (although not as well tolerated as fluconazole or voriconazole) and the range of adverse effects it produces is similar to the other azole antifungals: [22] elevated alanine aminotransferase levels are found in 4% of people taking itraconazole
For example, the azole antifungals such as ketoconazole or itraconazole can be both substrates and inhibitors of the P-glycoprotein, which (among other functions) excretes toxins and drugs into the intestines. [34] Azole antifungals are also both substrates and inhibitors of the cytochrome P450 family CYP3A4, [34] causing increased ...
Itraconazole has a broader spectrum of activity than fluconazole (but not as broad as voriconazole or posaconazole). In particular, it is active against Aspergillus, which fluconazole is not. The mechanism of action of itraconazole is the same as the other azole antifungals: it inhibits the fungal-mediated synthesis of ergosterol.
Isoconazole is an azole antifungal drug and could inhibit gram positive bacteria. [1] [2] For foot and vaginal infections, isoconazole has a similar effectiveness to clotrimazole. [3] [4] Isoconazole nitrate may be used in combination with corticosteroid diflucortolone to increase its bioavailability. [1]
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