Summary of Antifungal: Imidazoles
Fluconazole is an ergosterol inhibitors antifungal medication that is administered orally or intravenously. It is used to treat a variety of fungal infections, especially Candida infections of the vagina ("yeast infections'), mouth, throat, and bloodstream. It is also used to prevent infections in people with weak immune systems, including those with neutropenia due to cancer chemotherapy, transplant patients, and premature babies. Its mechanism of action involves interfering with synthesis of the fungal cell membrane.
Ketoconazole is a synthetic imidazole ergosterol inhibitor that is used primarily to treat fungal infections. Ketoconazole is sold commercially as a tablet for oral administration (although this use has been discontinued in a number of countries), and in a variety of formulations for topical administration, such as creams (used to treat tinea; cutaneous candidiasis, including candidal paronychia; and pityriasis versicolor) and shampoos (used primarily to treat dandruff—seborrhoeic dermatitis of the scalp).
Itraconazole is an ergosterol inhibitor that has a broader spectrum of activity than fluconazole (but not as broad as voriconazole or posaconazole). In particular, it is active against Aspergillus, which fluconazole is not. It is also licensed for use in blastomycosis, sporotrichosis, histoplasmosis, and onychomycosis. Itraconazole is over 99% protein-bound and has virtually no penetration into cerebrospinal fluid. Therefore, it should never be used to treat meningitis or other central nervous system infections.
Miconazole is an ergosterol inhibitor commonly applied topically to the skin or to mucous membranes to cure fungal infections. It can also be used against certain species of Leishmania protozoa which are a type of unicellular parasites that also contain ergosterol in their cell membranes. In addition to its antifungal and antiparasitic actions, it also has some antibacterial properties.
Clotrimazole (brand name Canesten or Lotrimin) is an ergosterol inhibitor commonly used in the treatment of fungal infections (of both humans and other animals) such as vaginal yeast infections, oral thrush, and ringworm. It is also used to treat athlete's foot and jock itch. It is on the World Health Organization's List of Essential Medicines, the most important medication needed in a basic health system.
Voriconazole (brand name Vfend) is a triazole ergosterol inhibitor that is generally used to treat serious, invasive fungal infections. These are generally seen in patients who are immunocompromised, and include invasive candidiasis, invasive aspergillosis, and certain emerging fungal infections.
Flashcards on Antifungal: Imidazoles
The mechanism of action of ketoconazole in the prevention of hirsutism in polycystic ovarian syndrome is the inhibition of , an enzyme involved in steroid synthesis.