Antifungal
Antifungal | |
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Drug class | |
Synonyms | antimycotic medication |
Legal status | |
In Wikidata |
An antifungal medication, also known as an antimycotic medication, is a
Routes of administration
Ocular
Indicated when the fungal infection is located in the eye. There is currently only one ocular antifungal available. This is Natamycin. However, various other antifungal agents could be compounded in this formulation.[2]
Intrathecal
Used occasionally when there's an infection of the central nervous system and other systemic options cannot reach the concentration required in that region for therapeutic benefit. Example(s): amphotericin B.[3]
Vaginal
This may be used to treat some fungal infections of the vaginal region. An example of a condition they are sometimes used for is candida vulvovaginitis which is treated with intravaginal Clotrimazole[4]
Topical
This is sometimes indicated when there's a fungal infection on the skin. An example is tinea pedis; this is sometimes treated with topical terbinafine.[5]
Oral
if the antifungal has good bioavailability, this is a common route to handle a fungal infection. An example is the use of ketoconazole to treat coccidioidomycosis.[6]
Intravenous
Like the oral route, this will reach the bloodstream and distribute throughout the body. However, it is faster and a good option if the drug has poor bioavailability. An example of this is IV amphotericin B for the treatment of coccidioidomycosis.[6]
Classes
The available classes of antifungal drugs are still limited but as of 2021 novel classes of antifungals are being developed and are undergoing various stages of clinical trials to assess performance.[7]
Polyenes
A
- Amphotericin B
- Candicidin
- Filipin – 35 carbons, binds to cholesterol (toxic)
- Hamycin
- Natamycin – 33 carbons, binds well to ergosterol
- Nystatin
- Rimocidin
Azoles
Imidazoles
- Bifonazole
- Butoconazole
- Clotrimazole
- Econazole
- Fenticonazole
- Isoconazole
- Ketoconazole
- Luliconazole
- Miconazole
- Omoconazole
- Oxiconazole
- Sertaconazole
- Sulconazole
- Tioconazole
Triazoles
- Albaconazole
- Efinaconazole
- Epoxiconazole
- Fluconazole
- Isavuconazole
- Itraconazole
- Posaconazole
- Propiconazole
- Ravuconazole
- Terconazole
- Voriconazole
Thiazoles
Allylamines
Echinocandins
Echinocandins inhibit the creation of glucan in the fungal cell wall by inhibiting 1,3-Beta-glucan synthase:
Echinocandins are administered intravenously, particularly for the treatment of resistant Candida species.[16][17]
Triterpenoids
Others
- Acrisorcin
- Amorolfine – a morpholine derivative used topically in dermatophytosis[18]
- Aurones – possess antifungal properties[19]
- Friar's Balsam, and Balsam of Peru[20]
- Carbol fuchsin (Castellani's paint)
- tinea versicolour.[21]
- Clioquinol
- Coal tar
- Copper(II) sulfate[22]
- topical antiseptic.[23]
- Chlorhexidine is a topical antibacterial and antifungal. It is commonly used in hospitals as an antiseptic. It is much more strongly antibacterial than antifungal, requiring at least a 10 times higher concentration to kill yeast compared to gram negative bacteria[24]
- Chlorophetanol
- Diiodohydroxyquinoline (Iodoquinol)
- Flucytosine (5-fluorocytosine) – an antimetabolite pyrimidine analog[25]
- Fumagillin
- Griseofulvin – binds to microtubules and inhibits mitosis[26]
- Haloprogin – discontinued due to the emergence of antifungals with fewer side effects[27]
- Miltefosine works by damaging fungal cell membranes [28]
- Nikkomycin – blocks formation of chitin present in the cell wall of fungus.
- Orotomide (F901318) – pyrimidine synthesis inhibitor[29][30]
- Piroctone olamine
- Pentanenitrile
- Potassium iodide – preferred treatment for lymphocutaneous sporotrichosis and subcutaneous zygomycosis (basidiobolomycosis). The mode of action is obscure.[31]
- Potassium permanganate - for use only on thicker, more insensitive skin such as the soles of the feet.
- Selenium disulfide
- Sodium thiosulfate
- Sulfur
- Tolnaftate – a thiocarbamate antifungal, which inhibits fungal squalene epoxidase (similar mechanism to allylamines like terbinafine)[medical citation needed]
- Triacetin – hydrolysed to acetic acid by fungal esterases[32]
- unsaturated fatty acid derived from natural castor oil; fungistatic, antibacterial, antiviral, and inhibits Candida morphogenesis[citation needed]
- Zinc pyrithione
Side effects
Incidents of liver injury or failure among modern antifungal medicines are very low to non-existent. However, some can cause allergic reactions in people.[33]
There are also many
Before oral antifungal therapies are used to treat nail disease, a confirmation of the fungal infection should be made.[36] Approximately half of suspected cases of fungal infection in nails have a non-fungal cause.[36] The side effects of oral treatment are significant and people without an infection should not take these drugs.[36]
Azoles are the group of antifungals which act on the cell membrane of fungi. They inhibit the enzyme 14-alpha-sterol demethylase, a microsomal CYP, which is required for biosynthesis of ergosterol for the cytoplasmic membrane. This leads to the accumulation of 14-alpha-methylsterols resulting in impairment of function of certain membrane-bound enzymes and disruption of close packing of acyl chains of phospholipids, thus inhibiting growth of the fungi. Some azoles directly increase permeability of the fungal cell membrane.[citation needed]
Resistance
Antifungal resistance is a subset of antimicrobial resistance, that specifically applies to fungi that have become resistant to antifungals. Resistance to antifungals can arise naturally, for example by genetic mutation or through aneuploidy. Extended use of antifungals leads to development of antifungal resistance through various mechanisms.[1]
Some fungi (e.g.
Unlike resistance to antibacterials, antifungal resistance can be driven by antifungal use in agriculture. Currently there is no regulation on the use of similar antifungal classes in agriculture and the clinic.[1][37]
The emergence of Candida auris as a potential human pathogen that sometimes exhibits multi-class antifungal drug resistance is concerning and has been associated with several outbreaks globally. The WHO has released a priority fungal pathogen list, including pathogens with antifungal resistance.[38]
References
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- ^ Sobel J. "Candida vulvovaginitis: Treatment". UpToDate. Archived from the original on 15 May 2023. Retrieved 21 May 2023.
- PMID 35448582.
- ^ a b Carver P. Pharmacotherapy: a pathophysiological approach (11th ed.).
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- PMID 19689243.
- PMID 9880474.
- ^ from the original on 12 July 2023, retrieved 2 December 2022
- ^ PubChem. "Imidazole". pubchem.ncbi.nlm.nih.gov. Archived from the original on 10 May 2023. Retrieved 2 December 2022.
- PMID 20347663.
- ^ "As Fungal Infections Expand, so Does Market | GEN Magazine Articles | GEN". GEN. 15 February 2012. Archived from the original on 6 September 2015. Retrieved 17 October 2015.
- ^ "Research and Markets: Global Antifungal Therapeutics (Polyenes, Azoles, Echinocandins, Allylamines) Market:Trends and Opportunities (2014-2019) | Business Wire". www.businesswire.com. 28 August 2014. Archived from the original on 4 March 2016. Retrieved 17 October 2015.
- ^ "Tinea Cruris". nurse-practitioners-and-physician-assistants.advanceweb.com. Archived from the original on 1 September 2017. Retrieved 17 October 2015.
- ^ "Echinocandins for the treatment of systemic fungal infection | Canadian Antimicrobial Resistance Alliance (CARA)" (PDF). Archived (PDF) from the original on 9 October 2021. Retrieved 9 May 2015.
- S2CID 32016049.
- PMID 6635894.
- PMID 28094180.
- ISBN 0-7817-3481-9. Archivedfrom the original on 14 January 2023. Retrieved 8 November 2020.
- ^ Long SF. "Anti-Fungals". Southwestern Oklahoma State University. Archived from the original on 17 June 2008.
- PMID 26361585.
- PMID 2272286.
- ISBN 9780429195648.
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- PMID 30726008. Retrieved 22 June 2021.
- ^ "Haloprogin". DrugBank. University of Alberta. 6 November 2006. Archived from the original on 1 January 2007. Retrieved 17 February 2007.
- S2CID 206011501.
- PMID 27791100.
- PMID 28830945.
- ^ "Systemic Therapy". Rook's Textbook of Dermatology. Vol. 4 (8th ed.). 2010. p. 74.48.
- ISBN 978-3527306732.
- S2CID 43198078.
- ^ a b Lewis RE. "Antifungal Drug Interactions". doctorfungus. Archived from the original on 19 June 2010. Retrieved 23 January 2010.
- ^ Research Cf (24 August 2022). "Drug Development and Drug Interactions | Table of Substrates, Inhibitors and Inducers". FDA. Archived from the original on 4 November 2020. Retrieved 17 April 2023.
- ^ ABIM Foundation. American Academy of Dermatology. Archivedfrom the original on 1 December 2013. Retrieved 5 December 2013., which cites
- Roberts DT, Taylor WD, Boyle J (March 2003). "Guidelines for treatment of onychomycosis". The British Journal of Dermatology. 148 (3): 402–10. S2CID 33750748.
- Mehregan DR, Gee SL (December 1999). "The cost effectiveness of testing for onychomycosis versus empiric treatment of onychodystrophies with oral antifungal agents". Cutis. 64 (6): 407–10. PMID 10626104.
- Roberts DT, Taylor WD, Boyle J (March 2003). "Guidelines for treatment of onychomycosis". The British Journal of Dermatology. 148 (3): 402–10.
- S2CID 253052170.
- ISBN 978-92-4-006024-1. Archived from the original on 26 October 2022. Retrieved 27 October 2022.)
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External links
- Antifungal Drugs – Detailed information on antifungals from the Fungal Guide written by R. Thomas and K. Barber
- "Clotrimazole". Clotrimazole (Canesten). Bayer Philippines.