Azole Antifungals Drug Class

Azole drugs are used in the treatment of many types of fungal infection. These drugs can be administered through a variety of means – including orally, topically, intravenously, and as a shampoo. Thus, azole drugs are used in the treatment of both topical and systemic fungal infections. Azoles, such as ketoconazole and fluconazole, work by interfering with a substance called ergosterol – a component specific to fungal cell membranes. By interfering with the synthesis of ergosterol, azole drugs critically affect the integrity of fungal cells, ultimately causing their death. Azole drugs are also associated with many clinically significant drug interactions.

Azole Antifungals Drugs

The drugs that are part of this drug class are distinguished by imidazole azoles or triazoles azoles.

Imidazole Azoles

Triazole Azoles

Azole Antifungals Uses

Even though they are widely known as primarily antifungal drugs, the azole class is a diverse one and, consequently, many individual drugs of this class can be employed for multiple conditions. Ketoconazole, for example, is not only used as a topical and systemic antifungal drug, but has also demonstrated efficacy in androgenic alopecia. As a result, ketoconazole is available in shampoo form to cater for this effect. However, the mainstay of indications resides with fungal infections. Clotrimazole is, for example, typically prescribed for those suffering from yeast infections, oral thrush, and jock itch. Other infections such as athlete’s foot, ringworm, and seborrheic dermatitis are commonly treated with the azole class of drugs.

Azole Antifungals Side Effects

Side effects of azoles will depend on whether they are of the imidazole or triazole variety.

Imidazole Azoles Side Effects

  • Abdominal pain
  • Cramping
  • Bloating
  • Nausea
  • Vomiting
  • Rash
  • Itching

Triazole Azoles Side Effects

  • Nausea
  • Abdominal Pain
  • Diarrhea
  • Headache
  • Rash
  • Taste disturbances
  • Increase risk of heart failure

Azole Antifungals Interactions

Ketoconazole is best absorbed in highly acidic environments such as the stomach. Therefore, it may be advised to take the oral version of the drug with drinks such as cola. Certain medications, such as antacids, will decrease the acidity present in the stomach and they should therefore be avoided on administration. Ketoconazole also affects the absorption of other drugs.

Taking imidazole azoles – such as ketoconazole, clotrimazole, or miconazole – with drugs such as cyclosporine, tacrolimus, and warfarin, will increase the effects of these drugs. Though, it’s worth noting these interactions only occur with the oral version of the drug. This is because imidazoles inhibits a liver enzyme known as CYP3A4 – and it’s this enzyme that metabolises drugs such as warfarin. Thus, if you take ketoconazole and inhibit this enzyme, levels of warfarin will rise – and this can have clinically significant consequences.