Azole antifungals

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Azole Antifungals[edit | edit source]

Azole antifungals are a class of antifungal drugs that are used to treat a variety of fungal infections. They are characterized by the presence of an azole ring, which is a five-membered ring containing at least one nitrogen atom. Azole antifungals are widely used due to their broad spectrum of activity and relatively low toxicity compared to other antifungal agents.

Classification[edit | edit source]

Azole antifungals are divided into two main groups based on their chemical structure:

  • Imidazoles: These contain two nitrogen atoms in the azole ring. Examples include:
 * Clotrimazole
 * Ketoconazole
 * Miconazole
  • Triazoles: These contain three nitrogen atoms in the azole ring. Examples include:
 * Fluconazole
 * Itraconazole
 * Voriconazole
 * Posaconazole

Mechanism of Action[edit | edit source]

Azole antifungals work by inhibiting the enzyme lanosterol 14α-demethylase, which is involved in the biosynthesis of ergosterol, a critical component of fungal cell membranes. By disrupting ergosterol synthesis, azoles compromise the integrity of the fungal cell membrane, leading to cell death.

Clinical Uses[edit | edit source]

Azole antifungals are used to treat a variety of fungal infections, including:

Pharmacokinetics[edit | edit source]

Azole antifungals vary in their absorption, distribution, metabolism, and excretion:

  • Fluconazole is well absorbed orally and has good penetration into the cerebrospinal fluid, making it effective for treating cryptococcal meningitis.
  • Itraconazole requires an acidic environment for absorption and is often taken with food or an acidic beverage.
  • Voriconazole is metabolized by the liver and has a non-linear pharmacokinetic profile, requiring careful monitoring of drug levels.

Side Effects[edit | edit source]

Common side effects of azole antifungals include:

  • Gastrointestinal disturbances (nausea, vomiting, diarrhea)
  • Hepatotoxicity (liver damage)
  • QT prolongation, which can lead to arrhythmias
  • Drug interactions due to inhibition of cytochrome P450 enzymes

Resistance[edit | edit source]

Resistance to azole antifungals can occur through several mechanisms, including:

  • Mutations in the target enzyme, lanosterol 14α-demethylase
  • Overexpression of efflux pumps that remove the drug from the fungal cell
  • Alterations in the ergosterol biosynthesis pathway

Conclusion[edit | edit source]

Azole antifungals are a vital component of the antifungal armamentarium, offering effective treatment for a wide range of fungal infections. However, their use must be carefully managed to minimize side effects and the development of resistance.

References[edit | edit source]

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Contributors: Prab R. Tumpati, MD