14.1 Antifungals Flashcards
What makes Fluconazle so important?
- Good CSF penetration.
- High oral bioavailability.
- Available in oral and IV formulations.
- Moderate inhibitor of CYP3A4.
- Strong inhibitor of CYP2C9: can increase plasma levels of phenytoin, zidovudine and warfarin.
What are the uses for Fluconazole?
- DOC in esophageal, oropharyngeal, vulvovaginal or urinary candidiasis.
- DOC for candidemia.
- DOC for coccidioidomycosis.
- DOC for consolidation and maintenance therapy of cryptococcal meningitis after induction with amphotericin B.
- Alternative to amphotericin B for non-severe criptococcal meningitis.
- DOC for initial and secondary prophylaxis against cryptoccocal meningitis.
Voriconazole is the DOC for what?
invasive aspergillosis
Voriconazole is metabolized and inhibited by what?
CYP2C19,
CYP2C9
and CYP3A4.
Which drug has a spectrum similar to itraconazole, but it has activity against Zygomycetes such as Mucor.
Posaconazole
Posaconazole inhibits which CYP?
3A4
What drugs are large cyclic peptides linked to a long-chain fatty acid
Caspofungin
Caspofungin is active against what? But not what?
Active against candida and aspergillus but not Cryptococcus neoformans.
What is important to know about the PK of Caspofungin?
IV only
What is the MOA of Caspofungin
Inhibit synthesis of β(1-3)-D-glucans in the fungal cell wall.
Griseofulvin is used for treatment of what?
Dermatophytosis
What is the MOA of Griseofulvin?
Disrupts mitotic spindle and inhibits mitosis.
Terbinafine inhibits which enzyme? Which prevents synthesis of what?
Squalene Epoxidase
Ergosterol
Terbinafine causes accumulation of what?
Toxic levels of squalene in the fungal cell
What are the topical drugs for superficial mycoses?
- Nystatin
- Amphotericin B
- Clotrimazole
- Miconazole
- Ketoconazole
- Terbinafine
