Anti-fungal Medications Flashcards by ava mondschein

what are the classes of anti-fungal drugs?

Polyenes
Azoles
Pyrimidine analog
Echinocandins
Allylamines
Miscellaneous

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what are the drugs used for Dermatophytes?

Tolnaftate
Terbinafine
Clotrimazole
Fluconazole
Miconazole
Itraconazole
Ketoconazole

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what are the drugs used for Mucocutaneous Infections?

Amphotericin B
Nystatin
Fluconazole
Itraconazole
Clotrimazole
Miconazole
Oteseconazole
Ibrexafungerp

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what are the drugs used for systemic infections?

Amphotericin B
Caspofungin
Flucytosine
Micafungin
Fluconazole
Anidulafungin
Itraconazole
Voriconazole
Posaconazole
Isavuconazole

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what are the two polyene Antifungal drugs?

Amphotericin B
Nystatin

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what is the MOA for Amphotericin B?

targets ergosterol in the cell membrane and binds to it creating pores in the membrane leading to leakage and death

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what are the clinical uses for Amphotericin B?

potentially fatal systemic infections:
- Candida
- Cryptococcus
- Histoplasma
- Blastomyces
- Coccidioides
- Aspergillus
- Fusarium
- Mucor

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what are the pharmacokinetics for Amphotericin B?

Poor oral absorption → must be given by IV for systemic infections
Long half-life

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what are the adverse effects of Amphotericin B?

Nausea/vomiting, abdominal pain
Hypersensitivity causing flushing, chills, hypotension, headache, fever thrombophlebitis, seizures
Nephrotoxicity causing hypokalemia, hypocalcemia, hypomagnesemia, Anemia

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what are the formulations and administration routes for Amphotericin B?

Conventional Amphotericin B and Liposomal & Lipid Complex Forms (less nephrotoxicity)
Slow IV infusion for serious systemic infections, Topical use for eyes, ears and Local for bladder irrigation

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what is the MOA for Nystatin?

targets ergosterol in the cell membrane and binds to it creating pores in the membrane leading to leakage and death

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what are the clinical uses for Nystatin?

Candida infections of mucosa mouth-oral, esophagus, vaginal, skin, GI tract
**Natamycin –fungal eye infections (fungal keratitis).
**Candidicin – vaginal candidiasis (similar use as Nystatin)

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what are the pharmacokinetics for Nystatin?

Poorly absorbed from the gut which is why its used for topical or oral cavity infections

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what are the adverse effects of Nystatin?

Generally well tolerated
May cause:
- Mild local irritation or allergic reaction at the application site
- Mild GI upset

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what class of drug is Flucytosine?

pyrimidine antifungal

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what is the MOA for Flucytosine?

enters fungal cells using a fungus-specific enzyme→ Cytosine permease then is converted (deaminated) to: → 5-Fluorouracil (5-FU) which is then metabolized to:
- FUTP→ blocks RNA synthesis
- FdUMP→ inhibits thymidylate synthase which prevents DNA synthesis

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what is Flucytosine used to treat and how is it given?

Typically combined with other antifungals and given orally:
- Amphotericin B for Cryptococcal meningitis, systemic candidiasis, some Aspergillus
- Itraconazole for Pigmented fungi infections

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what are the adverse effects for Flucytosine?

GI: nausea, vomiting, diarrhea, rash.
Liver: hepatotoxic
Bone Marrow: anemia
Intestine: inflammation/necrosis

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what are the Azole Antifungal drugs used to treat?

candidiasis, dermatophytes, aspergillosis, cryptococcal meningitis

what are the adverse effects of all Azole Antifungals?

GI upset, headache, rash
Inhibit cP450
Inhibit steroid production
Hepatotoxic (low incidence)

what is the MOA for all Azoles?

Prevents conversion of lanosterol to ergosterol, weakening the cell membrane by inhibiting lanosterol demethylase

what are the Imidazole Antifungals (Azoles)?

Ketoconazole
Clotrimazole
Miconazole

what is Clotrimazole used for and what are its adverse effects?

topical/topical oral treatment for dermatophytes, ringworm, molds oropharyngeal, skin, vaginal candidiasis
*can cause burning, itching, redness

what is Miconazole used for and what are its adverse effects?

Cutaneous candidiasis, vulvovaginitis, dermatophytes
*can cause burning, itching, redness

what is Ketoconazole used for and what are its adverse effects?

topical secondary treatment for dermatophytes, shampoo for dandruff * can cause nausea, vomiting, diarrhea headache, gynecomastia

what are the Triazole Antifungals (Azoles)?

Fluconazole Itraconazole Voriconazole Posaconazole Isavuconazole Oteseconazole Efinaconazole

what is Fluconazole used for and what are its adverse effects?

oral and IV treatment for mucocutaneous candidiasis, cryptococcal meningitis, oral (thrush), esophageal, vaginal, UTIs * can cause GI upset, hepatoxic (rare), inh. cP450

what is Itraconazole used for and what are its adverse effects?

used to treat dermatophytes, onychomycosis, etc (oral), histoplasmosis, aspergillus (IV) * can cause GI upset, hepatoxic (rarely liver failure), inh. P450, pain on IV

what is Voriconazole used for and what are its adverse effects?

oral or IV treatment for aspergillosis, candidiasis, histoplasmosis * can cause GI upset, rash, photosensitivity, alter liver enzymes, prolong QT, inh. P450

what is Posaconazole used for and what are its adverse effects?

oral or IV treatment of aspergillosis, candidiasis, histoplasmosis, mucormycosis * can cause GI upset, headache, hepatotoxic

what is Oteseconazole used for?

oral treatment of recurrent vulvovaginal candidiasis

what is Isavuconazole used for and what are its adverse effects?

oral or IV treatment for aspergillosis, candidiasis, histoplasmosis, mucormycosis * causes GI upset, headache, hypokalemia

what is Efinaconazole used for?

Topical for onychomycosis

what are the Eichinocandins Antifungals?

Caspofungin Micafungin Anidulafungin Rezafungin

what is the MOA for the Eichinocandins Antifungals?

Inhibits synthesis of β-glucans, a major component of the fungal cell wall by inhibiting the 1,3 β-glucan synthase enzyme

what are the clinical uses for the Eichinocandins Antifungals?

IV treatment for disseminated candida and invasive aspergillosis

what are the adverse effects of the Eichinocandins Antifungals?

well-tolerated but - GI upset, flushing, headache, urticaria, pruritis

what is the MOA for Ibrexafungerp?

semisynthetic derivative antifungal which acts similarly to echinocandin by inhibiting 1,3 β-glucan synthase

what is Ibrexafungerp used for and what are its adverse effects?

1-day oral therapy used to treat vulvovaginal candidiasis (fungicidal) * can cause GI upset, dizziness, rash

what are the Allylamine Antifungal drugs?

Terbinafine Naftifine Butenafine

what are the Allylamine Antifungals used for and what are its adverse effects?

oral for onychomycosis (terbinafine) and topical for dermatophytes (ring worm, tinea) * can cause GI upset, headache, rash, (hepatotoxicity-rare)

what is the MOA for the Allylamine Antifungals?

Blocks conversion of squalene to lanosterol, by inhibiting squalene epoxidase enzyme leading to a toxic buildup of squalene and a lack of ergosterol

what is Roflumilast?

a PDE4 (phosphodiesterase-4) inhibitor that works by increasing levels of cAMP, which helps reduce the production of proinflammatory cytokines

what is Roflumilast used for and what are its adverse effects?

used as a topical treatment for seborrheic dermatitis (first line: topical antifungals; corticosteroids) (also, plaque psoriasis) * can cause nausea, headache, nasopharyngitis

what are the oral and topical drugs used to treat Onycomycosis?

Oral: Terbinafine, Itraconazole Topical: Ciclopirox, Tavaborole (inh t-RNA synthetase), Efinaconazole