Pharmacological group antifungal agents
Pharmacodynamics
Fluconazole, a triazole antifungal agent, is a potent selective inhibitor of sterol synthesis in the fungal cell.
Fluconazole has demonstrated in vitro activity in clinical studies against most of the following microorganisms: Candida albicans, Candida glabrata (many strains are moderately sensitive), Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans.
Fluconazole has been shown to be active in vitro against the following microorganisms, but its clinical significance is unknown: Candida dubliniensis, Candida guilliermondii, Candida kefyr, Candida lusitaniae.
When administered orally, fluconazole is active in various models of fungal infections in animals. The activity of the drug in opportunistic mycoses, incl. caused by Candida spp. (including generalized candidiasis in immunosuppressed animals), Cryptococcus neoformans (including intracranial infections), Microsporum spp. and Trychophyton spp. The activity of fluconazole has also been established in models of endemic mycoses in animals, including infections caused by Blastomyces dermatitides, Coccidioides immitis (including intracranial infections) and Histoplasma capsulatum in animals with normal and suppressed immunity.
Fluconazole has a high specificity for fungal enzymes dependent on cytochrome P450. Therapy with fluconazole at a dose of 50 mg / day for up to 28 days does not affect the concentration of testosterone in the blood plasma in men or the concentration of steroids in women of childbearing age. Fluconazole at a dose of 200-400 mg / day has no clinically significant effect on the levels of endogenous steroids and their response to ACTH stimulation in healthy male volunteers.
Mechanisms of development of resistance to fluconazole
Fluconazole resistance can develop in the following cases: a qualitative or quantitative change in the enzyme that is the target of fluconazole (lanosteril 14-α-demethylase), a decrease in access to the target of fluconazole, or a combination of these mechanisms.
Point mutations in the ERG11 gene encoding the target enzyme lead to a modification of the target and a decrease in affinity for azoles. An increase in the expression of the ERG11 gene leads to the production of high concentrations of the target enzyme, which creates a need to increase the concentration of fluconazole in the intracellular fluid to suppress all enzyme molecules in the cell.
The second significant mechanism of resistance is the active removal of fluconazole from the intracellular space through the activation of two types of transporters involved in the active removal (efflux) of drugs from the fungal cell. These transporters include the master messenger encoded by the MDR genes (multiple drug resistance) and the ATP-binding cassette transporter superfamily encoded by the CDR genes (candida resistance genes to azole antimycotics).
Overexpression of the MDR gene leads to resistance to fluconazole, while overexpression of the CDR genes can lead to resistance to various azoles.
Resistance to Candida glabrata is usually mediated by overexpression of the CDR gene, resulting in resistance to many azoles. For those strains in which the MIC is defined as intermediate (16–32 μg / ml), it is recommended to use the maximum dose of fluconazole.
Candida krusei should be considered resistant to fluconazole. The mechanism of resistance is associated with reduced sensitivity of the target enzyme to the inhibitory effect of fluconazole.
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