Azole derivatives Flashcards
Azole derivatives (2 groups)
Diazole compounds
Triazole compounds
Diazole compounds (3 drugs)
Clotrimazole
Econazole
Ketoconazole
Triazole compounds (4 drugs)
Fluconazole
Itraconazole
Posaconazole
Voriconazole
Azole derivatives that can be adm IV (2 drugs)
Fluconazole
Voriconazole
Azole drugs that cannot be used with drugs that decrease gastric acid (3 drugs)
Ketoconazole
Itraconazole
Posaconazole
Only azole drug used for fungal meningitis
Fluconazole (both prophylaxis and treatment)
Azole drugs - adverse effects
Birth defects
Systemic adm: Hepatic injury, hematopoietic toxicity
Azole drugs - interactions
Inhibits metabolism of: HMG-CoA reductase inhibitors Some benzodiazepines Quinidine Warfarin
Azole drugs - contraindications
Pregnancy (Cat D for longterm, high doses. Cat C for short term, vaginal)
Itraconazole - indications
Systemic mycoses: Blastomycosis, histoplasmosis.
Superficial mycoses: onychomycosis (nails)
Itraconazole - amdinistration
Orally in pulse dosing
Fluconazole - indications
Cryptococcal meningitis in AIDS
Mucocutaneous and disseminated candidiasis
UTI by candida
Azole drug for single dose adm for acute vaginal candidiasis (1 drug)
Fluconazole
Second generation triazoles (2 drugs)
Voriconazole
Posaconazole
Voriconazole - indications
Invasive aspergillosis
Esophageal candidiasis
Invasive candidiasis
Voriconazole - interactions
Additive activity with caspofungin (used for treatment of invasive aspergillosis)
Voriconazole - adverse effects
Visual disturbances (altered light perception, chromatopsia, photophobia). Increased liver enzymes, liver failure (with death sometimes)
Posaconazole - indications
Systemic infections not responding to other agents (aspergillus, fusarium, rhizopus, mucormycosis)
Which azole drug has higher incidence of drug interactions
Ketoconazole
Ketoconazole - indications and adm
Adm topical for seborrheic dermatitis
Clotrimazole and econazole - indications
Candida (mouth, throat, vagina, vulva)
Tinea versicolor
Tinea pedis, tinea cruris
Clotrimazole and econazole (+other topicals) are not effective for…
Tinea capitis
Tinea unguium/onychomycosis
Azole drugs - MOA
Inhibits 14α-demethylase, and conversion of lanosterol to ergosterol