The Mechanism of Action of Azole Antifungal Drugs: Targeting Ergosterol Synthesis in Fungi for Effective Treatment

Which drug class has the following MOA: inhibition of fungal CYP450 dependent ergosterol synthesis resulting in loss of ergosterol in the fungal cell wall?

The drug class that has the described mechanism of action is the group of antifungal drugs called Azoles

The drug class that has the described mechanism of action is the group of antifungal drugs called Azoles.

Azoles inhibit the activity of the enzyme cytochrome P450-dependent lanosterol 14-alpha-demethylase, which is responsible for converting lanosterol into ergosterol in the fungal cell membrane. By inhibiting this enzyme, azoles prevent the synthesis of ergosterol, which is an essential component of the fungal cell wall.

Without ergosterol, the fungal cell wall becomes weakened and more permeable, leading to the loss of cellular integrity and eventually cell death. Ergosterol is crucial for maintaining the structural integrity and function of the fungal cell membrane, similar to how cholesterol functions in mammalian cells.

By selectively targeting the synthesis of ergosterol in fungi, azoles effectively kill or inhibit the growth of various fungal pathogens. Common examples of azole antifungal drugs include fluconazole, itraconazole, voriconazole, and posaconazole.

It is important to note that azoles can also inhibit certain human cytochrome P450 enzymes, which can lead to drug-drug interactions and affect the metabolism of other medications. Therefore, caution should be exercised when using azoles in patients taking other medications.

More Answers:

Optimizing Therapeutic Drug Monitoring for Voriconazole and Fluconazole: Ensuring Safe and Effective Antifungal Treatment
Understanding Hepatic Elimination of Fluconazole and Itraconazole: A Crucial Aspect in Azole Drug Pharmacokinetics
Fluconazole: The Renally Eliminated Azole Drug for Fungal Infections

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