Azole - Antifungal Class Flashcards
(T/F) - Azoles have become mainstay of antifungal therapy
TRUE
What is the MOA of azoles?
Inhibits fungal cytochrome P450, decreasing ergosterol production
Itraconazole has a good spectrum in which fungi organisms?
- C. albicans
- C. lusitaniae
- C. tropicalis
- C. parapsilosis
- Cryptococcus neoformans
- Aspergillus spp
- Many dimorphic fungi
What AEs can occur in itraconazole?
- Hepatotoxicity
- QTc prolongation
- Negative inotrope
Itraconazole is contraindicated in what?
Heart failure patients
Itraconazole strongly inhibits what?
CYP3A4
What are the popular itraconazole formulations?
- Capsules
- Solution
Which itraconazole formulation has a lower bioavailability?
Capsules
Which itraconazole formulation is less preferred for systemic fungal infections?
Capsules
Which itraconazole formulation should be taken with a full meal?
Capsules
Which itraconazole formulation should be taken on an empty stomach?
Solution
If someone wants to lower the absorption levels of itraconazole, how can it be lowered?
With PPIs; or take itraconazole with a soda
What is the drug of choice for itraconazole?
Histoplasmosis; a dimorphic infection
Fluconazole has a good spectrum in which fungi organisms?
- C. albicans
- C. tropicalis
- C. parapsilosis
- C. lusitaniae
- Cryptococcal neoformans
- Coccidioides immitis
What AEs can occur with fluconazole?
- Rash
- Hepatotoxicity
- QTc prolongation
Fluconazole strongly inhibits what?
- CYP2C19
- CYP2C9
Fluconazole moderately inhibits what?
CYP3A4
(T/F) - Fluconazole has a high bioavailability, regardless of formulation
TRUE
(T/F) - Fluconazole needs to adjust doses in renal insufficient patients
TRUE
(T/F) - Fluconazole has a strong activity against C. krusei and C. glabrata
FALSE - poor activity against those fungi organisms
If fluconazole will be used for C. krusei or C. glabrata, what should be done before giving fluconazole and at what dose should fluconazole be given?
Check susceptibilities; 800 mg/day
What is the drug of choice for fluconazole?
Susceptible fungal infections
Voriconazole has a good spectrum in which fungi organisms?
- C. albicans
- C. tropicalis
- C. parapsilosis
- C. lusitaniae
- C. krusei
- Aspergillus spp
- Many other moulds
What AEs can occur with voriconazole?
- Hepatotoxicity
- Rash
- QTc prolongation
- Visual and auditory hallucinations
- Visual effects
- Photosensitivity
What kind of visual effects can occur with voriconazole?
- Wavy lines
- Flashing
Voriconazole moderately inhibits what?
- CYP2C9
- CYP3A4
(T/F) - The IV formulation of voriconazole can be nephrotoxic
TRUE - it contains a cyclodextrin vehicle which can accumulate in renal dysfunction patients
Voriconazole IV is contraindicated in what?
CrCl < 50 mL/min
Can another formulation of voriconazole be used for renal dysfunction patients?
Oral formulations
Voriconazole is not useful for what treatment?
Candiduria
Voriconazole is eliminated where?
Hepatically
What is the drug of choice for voriconazole?
Invasive aspergillus
Posaconazole has a good spectrum in which fungi organisms?
- C. albicans
- C. parapsilosis
- C. tropicalis
- C. lusitaniae
- C. krusei
- Aspergillus spp
- Many moulds
- Dimorphic fungi
- Mucorales (Zygomycetes spp)
What AEs can occur with Posaconazole?
- Hepatotoxicity
- Rash
- Possible QTc prolongation
- GI disturbances
Posaconazole is a strong inhibitor of what?
CYP3A4
What are the formulation of Posaconazole in the market?
- Oral delayed release tablets
- Oral suspension
- IV injection
Which formulations are not interchangeable with posaconazole?
Oral delayed release tablets and oral suspension
Which formulations need to be taken with a meal with posaconazole?
Oral formulations
What is the indicated choice for PO tabs, suspension and IV posaconazole formulations?
- Prophylaxis of candida
- Aspergillus in high-risk patients
What is the indicated choice for PO suspension of posaconazole formulation?
- Oropharyngeal candidiasis
- Resistance of fluconazole and/or itraconazole
Isavuconazole has a good spectrum in which fungal organisms?
- Candida spp
- Aspergillus spp
- Mucorales (zygomycetes spp)
- Other moulds
- Dimorphic fungi
What AEs can occur with isavuconazole?
- Hepatotoxicity
Isavuconazole is a substrate from what?
CYP3A4
Isavuconazole is an inhibitor of what?
- CYP4A4
- P-gp
- Organic cation transporter 2
What are the formulations available with isavuconazole?
- Capsules
- IV
(T/F) - Isavuconazole capsules need to be taken with food
FALSE - can be taken with or without food
(T/F) - Isavuconazole is supplied as a prodrug
TRUE
(T/F) - Isavuconazole is a narrow spectrum drug
FALSE - broad spectrum
(T/F) - Isavuconazole has a very long t 1/2
TRUE
Does the loading dose of isavuconazole need extensive dosing?
Yes; q8h for 48h then 24h
What is the drug of choice for isavuconazole?
Invasive mold infections
