Questions and Answers
What is the mechanism of action of Polyenes?
Which antifungal agent inhibits squalene epoxidase?
What is the mechanism of action of Echinocandins?
Which of the following is a broad-spectrum antifungal?
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What is a common adverse effect of antifungal agents?
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Which enzyme is inhibited by Azoles?
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What is the mechanism of action of Fluoropyrimidines?
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Which of the following is an example of an Allylamine?
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What is a severe adverse effect of antifungal agents?
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Which of the following may interact with antifungal agents?
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Study Notes
Classification of Antifungal Agents
-
Polyenes:
- Bind to ergosterol in fungal cell membranes, creating pores and disrupting membrane function
- Examples: Amphotericin B, Nystatin
-
Azoles:
- Inhibit lanosterol 14α-demethylase, blocking ergosterol synthesis
- Examples: Fluconazole, Itraconazole, Voriconazole
-
Allylamines:
- Inhibit squalene epoxidase, blocking ergosterol synthesis
- Examples: Terbinafine
-
Echinocandins:
- Inhibit β-(1,3)-glucan synthase, blocking fungal cell wall synthesis
- Examples: Caspofungin, Micafungin, Anidulafungin
-
Fluoropyrimidines:
- Inhibit thymidylate synthase, blocking DNA synthesis
- Examples: Flucytosine
Mechanisms of Action
-
Fungal cell membrane disruption:
- Polyenes and Azoles disrupt fungal cell membranes, leading to cell death
-
Inhibition of ergosterol synthesis:
- Azoles, Allylamines, and Fluoropyrimidines inhibit ergosterol synthesis, disrupting fungal cell membrane function
-
Inhibition of fungal cell wall synthesis:
- Echinocandins inhibit β-(1,3)-glucan synthase, blocking fungal cell wall synthesis
Spectrum of Activity
-
Broad-spectrum antifungals:
- Effective against a wide range of fungi, including Candida, Aspergillus, and Histoplasma
- Examples: Amphotericin B, Voriconazole
-
Narrow-spectrum antifungals:
- Effective against specific types of fungi, such as dermatophytes
- Examples: Terbinafine
Adverse Effects and Interactions
-
Common adverse effects:
- Nausea, vomiting, diarrhea, headache
-
Severe adverse effects:
- Hepatotoxicity, nephrotoxicity, allergic reactions
-
Interactions:
- CYP450 inhibitors or inducers may affect antifungal pharmacokinetics
- Antifungals may interact with other medications, such as warfarin and statins
Classification of Antifungal Agents
- Polyenes bind to ergosterol in fungal cell membranes, creating pores and disrupting membrane function, with examples including Amphotericin B and Nystatin.
- Azoles inhibit lanosterol 14α-demethylase, blocking ergosterol synthesis, and include Fluconazole, Itraconazole, and Voriconazole.
- Allylamines inhibit squalene epoxidase, blocking ergosterol synthesis, with Terbinafine as an example.
- Echinocandins inhibit β-(1,3)-glucan synthase, blocking fungal cell wall synthesis, including Caspofungin, Micafungin, and Anidulafungin.
- Fluoropyrimidines inhibit thymidylate synthase, blocking DNA synthesis, with Flucytosine as an example.
Mechanisms of Action
- Polyenes and Azoles disrupt fungal cell membranes, leading to cell death through fungal cell membrane disruption.
- Azoles, Allylamines, and Fluoropyrimidines inhibit ergosterol synthesis, disrupting fungal cell membrane function.
- Echinocandins inhibit β-(1,3)-glucan synthase, blocking fungal cell wall synthesis.
Spectrum of Activity
- Broad-spectrum antifungals, including Amphotericin B and Voriconazole, are effective against a wide range of fungi, such as Candida, Aspergillus, and Histoplasma.
- Narrow-spectrum antifungals, such as Terbinafine, are effective against specific types of fungi, like dermatophytes.
Adverse Effects and Interactions
- Common adverse effects of antifungal agents include nausea, vomiting, diarrhea, and headache.
- Severe adverse effects include hepatotoxicity, nephrotoxicity, and allergic reactions.
- Interactions with antifungal agents can occur with CYP450 inhibitors or inducers, affecting pharmacokinetics, and with other medications, such as warfarin and statins.
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Description
Learn about the different types of antifungal agents, including polyenes, azoles, allylamines, and echinocandins, and how they work to combat fungal infections.