Week 10 - Systemic Azoles (antifungals) Flashcards
Fluconazole: indications
Candidiasis - vaginal, oropharyngeal, esophageal
Fluconazole: MOA
Interferes w/ fungal cytP450 activity, decreasing ergosterol synthesis (principle sterol in fungal cell membrane) and inhibiting cell membrane formation
Fluconazole: caution and contraindications
- Risk of QT prolongation
- Caution in patients with arrhythmias
- Caution in renal and hepatic impairment
- Avoid in pregnancy and lactation
- Approved in pediatrics
Fluconazole: ADR
HA, dizziness, N/V/D
Rare: hepatoxicity, anaphylaxis, skin reactions
Itraconazole: indications
Onychomycosis (infection of nail bed)
Itraconazole: MOA
Interferes with fungal cytP450 activity, decreasing ergosterol synthesis (principle sterol in fungal cell membrane), and inhibiting cell membrane formation
Itraconazole: caution and contraindications
- BLACK BOX: avoid in patients with HF
- Risk for QT prolongation
- Caution in patients with arrhythmias
- Caution in renal and hepatic impairment
- Avoid in pregnancy and lactation
Itraconazole: ADR
HA, skin rash, edema, V/D
Rare: hepatotoxicity, skin reactions
Terbinafine: indications
Onychomycosis
1st line treatment option
Terbinafine: MOA
Synthetic allylamine derivative that inhibits squalene epoxidase (key enzyme in sterol biosynthesis in fungi) –> fungal cell death
Terbinafine: caution and contraindications
- Caution in patients with arrhythmias
- Caution in renal and hepatic impairment
- Avoid in pregnancy and lactation
Terbinafine: ADR
HA, depression, taste disturbance, N/V/D
Rare: hepatotoxicity, hepatic failure, skin reactions, ocular effects
Which systemic azoles inhibit CYP3A4?
Fluconazole, itraconazole, ketoconazole
Which systemic azoles have interactions w/ ingested materials that can effect absorption?
Itraconazole = enhanced by food
Griseofulvin = enhanced by fat
Systemic azoles: ADR
Hepatotoxicity