DD Antifungals Flashcards
Polyenes
Amphotericin B (Fungizone)
Nystatin (Mycostatin)
MOA of:
Amphotericin B (Fungizone)
Nystatin (Mycostatin)
do they display selective toxicity?
Binds to ergesterol in fungal cell membrane pores = leakage of cellular material and eventual death.
Not super selective toxicity because it binds to cholesterol in mammal cells
ROA of
Amphotericin B (Fungizone)
Nystatin (Mycostatin)
Amphotericin B (Fungizone) - IV, Topical Nystatin (Mycostatin) - Topical
Route of excretion of Polyenes
Amphotericin B (Fungizone) Nystatin (Mycostatin)
- Mainly through biliary tract (slow renal)
Spectrum of use: Amphotericin B (Fungizone)
Broad spectrum,
opportunistic
and systemic
Spectrum of use: Nystatin (Mycostatin)
Candidal infections of:
skin,
mucous membranes,
GI/Vaginal tract
Pharmacokinetic properties of Amphotericin B (Fungizone)
Rapidly sequestered in tissues,
little released to CNS,
λ = 15 days (terminal)
Adverse rxn of Amphotericin B (Fungizone)
VERY TOXIC DRUG!!!
1) Nephrotoxicity - main issue, nearly all patients get this
2) Infusion-related toxicity - chills, fever, vomiting with IV use
3) Anemia - 75% due to BM depression
Pharmacotherapeutic Advantages of polyenes
Drug of choice for life-threatening systemic fungal infections.
-Used as initial therapy, then replaced with azoles
(gotta watch out for nephrotoxicity)
Adverse rxn of Nystatin (Mycostatin)
Mild and transient GI upset
Echinocandins (3)
Anidulafungin (Eraxis)
Capsofungin (Cancidas)
Micafungin (Mycamine)
MOA of Echinocandins
Inhibit synthesis of β (1,3) D-glucan, disrupt cell wall synthesis.
High selective toxicity
ROA of Echinocandins
IV
Route of Excretion of Echinocandins
Renal & Hepatic
Spectrum of Echinocandins
Broad spectrum.
Invasive candida
Invasive aspergillosis
For Echinocandins: what do we do to dose if:
- Pt has hepatic insufficiency?
- Pt has renal dysfunction?
- Pt is taking CYP450 inducer?
- reduce dose (liver can’t break it down fast enough)
- no dose change needed
- Increase (bc it gets processed too fast)
Adverse rxns of echinocandins?
Histamine-mediated symptoms (rash, facial swelling)
and nausea, vomiting, headache , fever, phlebitis
Which antifungal is best used in patients with aspergillosis that are refractory or intolerant to other therapies (amphotericin B, itraconazole)?
Echinocandins
Triazoles
Fluconazole (Diflucan)
Itraconazole (Sporanox)
Voriconazole (Vfend)
Terconazole (Terazole)
MOA of triazoles
-Fungistatic or cidal?
Fungistatic - highly specific
inhibition of fungal cytochrome P450 = ↓ Ergosterol synthesis.
Which triazole is administered topically?
Terconazole (Terazole)
rest are oral
Which triazole is excreted via hepatic?
Itraconazole (Sporanox)
Voriconazole (Vfend)
Terconazole (Terazole)
*Fluconazole (Diflucan) is the only renal one
Spectrum of Use: Fluconazole (Diflucan)
Candidiases (vaginal, esophageal, oropharyngeal)