II. Medications: Azoles
- Background
- Azoles inhibit the synthesis of ergosterol (key component of fungal cell wall)
- Block sterol 14-a-dimethylase (microsomal Cytochrome P450-dependent enzyme)
- Azoles inhibit the synthesis of ergosterol (key component of fungal cell wall)
- Imidazoles (primarily used topically for candida and dermatophyte infections)
- Triazoles (primarily used orally for systemic fungal infections)
III. Medications: Allylamine
- Background
- Allylamines block Ergosterol synthesis (key component in the fungal cell wall)
- Inhibit squalene epoxidase, the enzyme that converts squalene to ergosterol
- Indicated in superficial dermatophyte infections resistant to imidazoles
- Allylamines block Ergosterol synthesis (key component in the fungal cell wall)
- Medications
- Naftifine (Naftin, topical)
- Terbinafine (Lamisil)
- Topical for resistant dermatophyte infections
- Oral Terbinafine is the preferred agent for Onychomycosis
IV. Medications: Polyene
- Background
- Polyenes bind to ergosterol within the fungal cell membrane
- Results in fungal cell Membrane Depolarization and increased permeability
- Fungal cell leaks key intracellular components, and ruptures
- Polyenes bind to ergosterol within the fungal cell membrane
-
Amphotericin B
- Preferred agent for deep fungal infections in pregnancy (long safety data record)
- Systemic, invasive, life-threatening fungal infections (including Meningitis, cystitis) and some Protozoa infections
- Largely replaced by newer, less toxic fungicides
- Candidemia
- Symptomatic candida cystitis or Pyelonephritis
- Cryptococcal Meningitis (HIV Infection, administered with Flucytosine)
-
Nystatin (topical or mucosal use)
- Cutaneous Candidiasis (topical Nystatin)
- Candida Diaper Dermatitis
- Candidal Intertrigo
- Oral Candidiasis (Thrush)
- First-line agent
- Cutaneous Candidiasis (topical Nystatin)
V. Medications: Echinocandin
- Background
- Echinocandins (Cyclic Lipopeptides) inhibit synthesis of beta-(1,3)-D-Glucan a key cell wall component
- Active against Candida species (including those resistant to Azole Antifungals) and some Aspergillus species
- Medications
- Caspofungin
- Micafungin
- Andulafungin
VI. Medications: Miscellaneous
-
Flucytosine (categorized as an antimetabolite)
- Flucytosine is a Fluorouracil prodrug, a fluorinated cytosine analog with Antifungal activity
- Within fungal cells, Flucytosine is deaminated to the active metabolite 5-Fluorouracil
- 5-Fluorouracil substitutes for the Pyrimidine uracil during RNA synthesis
- Inhibits fungal Protein synthesis
- Indications: Systemic Fungal Infections
- Used with Amphotericin (risk of induced resistance when used alone)
- Cryptococcal Meningitis
- CNS Candidiasis (HIV Infection)
- Candida Pyelonephritis
-
Griseofulvin (categorized as a Benzofuran)
- Antifungal derived first in 1958 from the mold Penicillium griseofulvum
- Inhibits microtubule function in Mitosis by binding tubulin in fungi
- Indications limited to Tinea Capitis as an alternative agent
VII. References
- (2012) Med Lett Drugs Ther 10(120): 61-8
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antifungal (on 8/23/2023 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ANTIFUNGAL 1% CREAM | Generic OTC | $0.10 per gram |
ANTIFUNGAL 1% TOPICAL CREAM | Generic OTC | $0.16 per gram |
ANTIFUNGAL 2% POWDER | Generic OTC | $0.05 per gram |
Ontology: Antifungal Agents (C0003308)
Definition (CHV) | a drug that kills fungus |
Definition (CHV) | a drug that kills fungus |
Definition (CHV) | a drug that kills fungus |
Definition (CHV) | a drug that kills fungus |
Definition (CHV) | a drug that kills fungus |
Definition (CHV) | a drug that kills fungus |
Definition (CHV) | a drug that kills fungus |
Definition (NCI) | Substances that treat systemic or topical infections caused by fungi. Antifungal agents kill or inhibit the growth of fungi, by various mechanisms. These mechanisms include inhibition of fungal mitosis, impairing synthesis or binding to ergosterol, inhibition of RNA or DNA synthesis, and interfering with other fungal metabolic processes. |
Definition (NCI_NCI-GLOSS) | Drugs that treat infections caused by fungi. |
Definition (MSH) | Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues. |
Definition (CSP) | substances that are destructive to fungi, suppress their reproduction or growth, or are effective against fungal infection. |
Concepts | Pharmacologic Substance (T121) |
MSH | D000935 |
SnomedCT | 282833001, 332848007, 289095006, 324643005, 373219008, 81491005 |
LNC | LP31435-8 |
English | Agents, Antifungal, Fungicides, Therapeutic, Therapeutic Fungicides, Antifungal preparation, THER FUNGICIDES, FUNGICIDES THER, ANTIFUNGALS, antifungal agents, antifungal agents (medication), Antifungal Agent [TC], [AM700] ANTIFUNGALS, Antifungal Agent, antifungal drugs, antifungals, antifungal drug, drugs fungicidal, Antifungal drugs (substance), Fungicidal drug (product), Antifungal preparation (product), Antifungal agents, antifungal, Antifungal drugs, Fungicidal drug, Antifungal, Antifungal (substance), Antifungal agent, Antifungal drugs (product), antifungal agent, Antifungal agent, NOS, Fungicidal drug (substance), Antifungal preparation (substance), Antifungal Agents, Antifungal Drug, Antifungals |
French | Anti-fongiques, Fongicides, Anti-fungiques, Agents antifongiques, Médicaments antifongiques, Antimycosiques, Antifongiques, Antifungiques |
Swedish | Svampmedel |
Czech | antimykotika, antifungální látky |
Finnish | Sienilääkkeet |
Italian | Fungicidi terapeutici, Antimicotici |
Russian | PROTIVOGRIBKOVYE SREDSTVA, FUNGITSIDNYE SREDSTVA, ANTIBIOTIKI PROTIVOGRIBKOVYE, АНТИБИОТИКИ ПРОТИВОГРИБКОВЫЕ, ПРОТИВОГРИБКОВЫЕ СРЕДСТВА, ФУНГИЦИДНЫЕ СРЕДСТВА |
Polish | Leki przeciwgrzybicze, Antybiotyki przeciwgrzybicze |
Croatian | ANTIMIKOTICI, ANTIFUNGICI |
Japanese | 抗真菌性抗生物質, 抗かび性抗生物質, 抗真菌抗生物質, 抗カビ性抗生物質, 抗真菌剤, 抗生物質-抗真菌性, 抗カビ抗生物質, 抗かび薬, 抗真菌薬, 抗黴剤, 殺真菌薬, 治療用殺真菌薬, 防黴剤, 抗カビ剤, 抗黴薬, 防カビ剤 |
Portuguese | Antifúngicos, Antimicóticos, Agentes Antifúngicos, Agentes Antimicóticos, Fungicidas Terapêuticos |
Spanish | Antifúngicos, preparación antifúngica, fármaco fungicida, preparación antifúngica (producto), agente antifúngico, fármaco fungicida (producto), Agentes Antimicóticos, Agentes Antifúngicos, Antimicóticos, agente antimicótico, antifúngico (sustancia), antifúngico, antimicótico, drogas antimicóticas (producto), drogas antimicóticas (sustancia), drogas antimicóticas, fármacos antifúngicos, Fungicidas Terapéuticos |
German | Antimykotika, Antipilzmittel, Fungizide, therapeutische, Pilzmittel |
Ontology: Azole antifungal (C0360363)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
SnomedCT | 350195009, 373236000 |
English | azole agents, azole agents (medication), azole antifungal, antifungals azole, antifungals azoles, Azole antifungal, Azole antifungal (product), Azole antifungal (substance), Azole Antifungals |
Spanish | antimicótico azólico (producto), antimicótico azólico (sustancia), antimicótico azólico, azol antimicótico (producto), azol antimicótico (sustancia), azol antimicótico |
Ontology: Imidazole antifungal (C0360364)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
SnomedCT | 350196005, 372631007 |
English | Imidazole antifungal, Imidazole antifungal (product), Imidazole antifungal (substance) |
Spanish | antifúngico imidazol, antimicótico imidazol (sustancia), antimicótico imidazol, antimicótico imidazólico (producto), antimicótico imidazólico, imidazol antimicótico (sustancia) |
Ontology: Triazole antifungal (C0360380)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
SnomedCT | 350208007, 372632000 |
Spanish | antifúngico triazólico (sustancia), antifúngico triazólico, antifúngicos triazólicos (sustancia), antifúngicos triazólicos, antimicótico triazólico (producto), antimicótico triazólico, triazol antimicótico (producto), triazol antimicótico (sustancia), triazol antimicótico |
English | Triazole antifungals, Triazole antifungals (product), Triazole antifungals (substance), Triazole antifungal (substance), Triazole antifungal |
Ontology: Echinocandins (C1268551)
Definition (MSH) | Cyclic hexapeptides of proline-ornithine-threonine-proline-threonine-serine. The cyclization with a single non-peptide bond can lead them to be incorrectly called DEPSIPEPTIDES, but the echinocandins lack ester links. Antifungal activity is via inhibition of 1,3-beta-glucan synthase production of BETA-GLUCANS. |
Concepts | Pharmacologic Substance (T121) |
MSH | D054714 |
SnomedCT | 129473008, 373570003 |
English | Echinocandins, Echinocandins [Chemical/Ingredient], echinocandin, echinocandins, Echinocandin (product), Echinocandin (substance), Echinocandin, Glucan synthesis inhibitor |
Portuguese | Equinocandinas |
Spanish | Equinocandinas, equinocandina (producto), equinocandina (sustancia), equinocandina, inhibidor de la síntesis de glucano |
Finnish | Ekinokandiinit |
French | Échinocandines |
German | Echinocandine, Echinokandine |
Italian | Echinocandine |
Russian | ЭХИНОКАНДИНЫ, EKHINOKANDINY |
Japanese | エキノカンジン, エキノカンジン類 |
Czech | echinokandiny |
Swedish | Echinocandiner |
Polish | Akuletacyny, Echinokandyny, Mulundokandyny, Pneumokandyny |
Ontology: Polyene Antifungal [EPC] (C1579365)
Concepts | Pharmacologic Substance (T121) |
English | Polyene Antifungal [EPC], Polyene Antifungal |
Ontology: Echinocandin Antifungal [EPC] (C2266974)
Concepts | Pharmacologic Substance (T121) |
English | Echinocandin Antifungal [EPC], Echinocandin Antifungal |
Ontology: Allylamine Antifungal [EPC] (C3537228)
Concepts | Pharmacologic Substance (T121) |
English | Allylamine Antifungal [EPC], Allylamine Antifungal |