II. Medications: Azoles

  1. Background
    1. Azoles inhibit the synthesis of ergosterol (key component of fungal cell wall)
      1. Block sterol 14-a-dimethylase (microsomal Cytochrome P450-dependent enzyme)
  2. Imidazoles (primarily used topically for candida and dermatophyte infections)
    1. Clotrimazole
    2. Miconazole
    3. Ketoconazole
  3. Triazoles (primarily used orally for systemic fungal infections)
    1. Fluconazole
    2. Isavuconazole
    3. Itraconazole
    4. Voriconazole
    5. Posaconazole

III. Medications: Allylamine

  1. Background
    1. Allylamines block Ergosterol synthesis (key component in the fungal cell wall)
      1. Inhibit squalene epoxidase, the enzyme that converts squalene to ergosterol
    2. Indicated in superficial dermatophyte infections resistant to imidazoles
  2. Medications
    1. Naftifine (Naftin, topical)
    2. Terbinafine (Lamisil)
      1. Topical for resistant dermatophyte infections
      2. Oral Terbinafine is the preferred agent for Onychomycosis

IV. Medications: Polyene

  1. Background
    1. Polyenes bind to ergosterol within the fungal cell membrane
      1. Results in fungal cell Membrane Depolarization and increased permeability
      2. Fungal cell leaks key intracellular components, and ruptures
  2. Amphotericin B
    1. Preferred agent for deep fungal infections in pregnancy (long safety data record)
    2. Systemic, invasive, life-threatening fungal infections (including Meningitis, cystitis) and some Protozoa infections
      1. Largely replaced by newer, less toxic fungicides
      2. Candidemia
      3. Symptomatic candida cystitis or Pyelonephritis
      4. Cryptococcal Meningitis (HIV Infection, administered with Flucytosine)
  3. Nystatin (topical or mucosal use)
    1. Cutaneous Candidiasis (topical Nystatin)
      1. Candida Diaper Dermatitis
      2. Candidal Intertrigo
    2. Oral Candidiasis (Thrush)
      1. First-line agent

V. Medications: Echinocandin

  1. Background
    1. Echinocandins (Cyclic Lipopeptides) inhibit synthesis of beta-(1,3)-D-Glucan a key cell wall component
    2. Active against Candida species (including those resistant to Azole Antifungals) and some Aspergillus species
  2. Medications
    1. Caspofungin
    2. Micafungin
    3. Andulafungin

VI. Medications: Miscellaneous

  1. Flucytosine (categorized as an antimetabolite)
    1. Flucytosine is a Fluorouracil prodrug, a fluorinated cytosine analog with Antifungal activity
    2. Within fungal cells, Flucytosine is deaminated to the active metabolite 5-Fluorouracil
      1. 5-Fluorouracil substitutes for the Pyrimidine uracil during RNA synthesis
      2. Inhibits fungal Protein synthesis
    3. Indications: Systemic Fungal Infections
      1. Used with Amphotericin (risk of induced resistance when used alone)
      2. Cryptococcal Meningitis
      3. CNS Candidiasis (HIV Infection)
      4. Candida Pyelonephritis
  2. Griseofulvin (categorized as a Benzofuran)
    1. Antifungal derived first in 1958 from the mold Penicillium griseofulvum
    2. Inhibits microtubule function in Mitosis by binding tubulin in fungi
    3. Indications limited to Tinea Capitis as an alternative agent

VII. References

  1. (2012) Med Lett Drugs Ther 10(120): 61-8

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Related Studies

Cost: Medications

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