Antifungals Flashcards
Amphotercin
Antifungal Agent
Characteristics:
- A large macrolide
- High affinity for ergosterol (Fungal membrane sterol)
MOA:
- Hydrophillic core forms a transmembrane ion channel
–> Loss of intracellular K+ disrupting cellular permeability and transport systems
AE:
- Renal Toxicity (Potassium leak leading to toxicity)
- Hypotension
- Hypokalemia
- Thrombocytopenia
Reversible when stopping therapy
Nystatin
Antifungal Agent
Characteristics:
- Polyene antibiotic
MOA:
- Hydrophillic core forms a transmembrane ion channel
–> Loss of intracellular K+ disrupting cellular permeability and transport systems
AE:
- Nausea
- Vomiting
- Diarrhea
Griseofulvin
Antifungal Agent
Characteristics:
- Narrow spectrum antifungal isolated from Penicillium griseofulvum
MOA:
- Binds to fungal microtubules
–> Interferes with mitosis
AE:
- Photosensitivity
Caspofungin
Antifungal Agent (Echinocandins)
Characteristics:
- Synthetic modified echinocandin B
MOA:
- Inhibit 1,3-beta-glucan synthase
–> Impairs 1,3-beta-glucan production
–> Interfering with the structural integrity of fungal cell walls
Anidulafungin
Antifungal Agent (Echinocandins)
Characteristics:
- Synthetic modified echinocandin B
MOA:
- Inhibit 1,3-beta-glucan synthase
–> Impairs 1,3-beta-glucan production
–> Interfering with the structural integrity of fungal cell walls
Micafungin
Antifungal Agent (Echinocandins)
Characteristics:
- Synthetic modified echinocandin B
MOA:
- Inhibit 1,3-beta-glucan synthase
–> Impairs 1,3-beta-glucan production
–> Interfering with the structural integrity of fungal cell walls
AE:
- Hepatotoxicity
Ketoconazole
Antifungal Agent
(Azoles)
Characteristics:
- Broad-spectrum fungistatic
MOA:
- Inhibits fungal cytochrome P450 3A enzyme (Lanosine 14alpha-demethylase)
–> Prevents ergosterol formation from lanosterol
–> Impairs replication
AE:
- Interferes with Amphotericin as Ergosterol is needed for binding
- Gynecomastia (Inhibits adrenal cortex, interferes with steroid and testosterone –> Development of breasts)
PK:
- HL = 8 hours
- Absorbed well in GI tract
Fluconazole
Antifungal Agent
(Azoles)
Characteristics:
- Broad-spectrum fungistatic
MOA:
- Inhibits fungal cytochrome P450 3A enzyme (Lanosine 14alpha-demethylase)
–> Prevents ergosterol formation from lanosterol
–> Impairs replication
AE:
- Interferes with Amphotericin as Ergosterol is needed for binding
- Stevens-Johnson Syndrome
PK:
- HL = 25 hours
- Oral/IV
Itraconazole
Antifungal Agent
(Azoles)
Characteristics:
- Broad-spectrum fungistatic
MOA:
- Inhibits fungal cytochrome P450 3A enzyme (Lanosine 14alpha-demethylase)
–> Prevents ergosterol formation from lanosterol
–> Impairs replication
AE:
- Interferes with Amphotericin as Ergosterol is needed for binding
- Stevens-Johnson Syndrome
PK:
- 36 hours
- Highly lipid soluble
Miconazole
Antifungal Agent
(Azoles)
Characteristics:
- Broad-spectrum fungistatic
MOA:
- Inhibits fungal cytochrome P450 3A enzyme (Lanosine 14alpha-demethylase)
–> Prevents ergosterol formation from lanosterol
–> Impairs replication
AE:
- Interferes with Amphotericin as Ergosterol is needed for binding
Flucytosine
Antifungal Agent
Characteristics:
- Orally active antifungal
- Given with Amphotericin
MOA:
- Converted into 5-fluorouracil (only in fungal cells)
–> Inhibits thymidylate synthetase preventing DNA synthesis
AE:
- Neutropenia
- Alopecia
- Hepatitis
Terbinafine
Antifungal Agent
Characteristics:
- Lipophilic fungicidal
MOA:
- Inhibits squalene epoxidase
–> Prevents synthesis of ergosterol to squalene
AE:
- Decreased efficacy of amphotericin
- Arthralgia & Myalgia
- Hepatitis
Naftifine
Antifungal Agent
Characteristics:
- Lipophilic fungicidal
MOA:
- Inhibits squalene epoxidase
–> Prevents synthesis of ergosterol to squalene
AE:
- Decreased efficacy of amphotericin
- Arthralgia & Myalgia
- Hepatitis
