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There are two types of antifungals: local and systemic. Local antifungals are usually administered topically or vaginally, depending on the condition being treated. Systemic antifungals are administered orally or intravenously.
A polyene is a molecule with multiple conjugated double bonds. A polyene antifungal is a macrocyclic polyene with a heavily hydroxylated region on the ring opposite the conjugated system. This makes polyene antifungals amphiphilic. The polyene antimycotics bind with sterols in the fungal cell membrane, principally ergosterol. This changes the transition temperature (Tg) of the cell membrane, thereby placing the membrane in a less fluid, more crystalline state. (In ordinary circumstances membrane sterols increase the packing of the phospholipid bilayer making the plasma membrane more dense.) As a result, the cell's contents including monovalent ions (K+, Na+, H+, and Cl-), small organic molecules leak and this is regarded one of the primary ways cell dies. Animal cells contain cholesterol instead of ergosterol and so they are much less susceptible. However, at therapeutic doses, some amphotericin B may bind to animal membrane cholesterol, increasing the risk of human toxicity. Amphotericin B is nephrotoxic when given intravenously. As a polyene's hydrophobic chain is shortened, its sterol binding activity is increased. Therefore, further reduction of the hydrophobic chain may result in it binding to cholesterol, making it toxic to animals.
Ciclopirox - (ciclopirox olamine) - is a hydroxypyridone antifungal that interferes with active membrane transport, cell membrane integrity, and fungal respiratory processes. It is most useful against tinea versicolour.
Apart from side effects like altered estrogen levels and liver damage, many antifungal medicines can cause allergic reactions in people. For example, the azole group of drugs is known to have caused anaphylaxis.
Before oral antifungal therapies are used to treat nail disease, a confirmation of the fungal infection should be made. Approximately half of suspected cases of fungal infection in nails have a non-fungal cause. The side effects of oral treatment are significant and people without an infection should not take these drugs.
Azoles are the group of anti fungals which act on the cell membrane of fungus. They inhibit the enzyme 14 - alpha-sterol demethylase, a microsomal CYP, which is required for biosynthesis of Ergosterol for cytoplasmic membrane. This leads to accumulation of 14-alpha-methylsterols resulting in impairment of function of certain membrane bound enzymes and disruption close packing of acyl chains of phospholipids, thus inhibiting growth of the fungi. Some azoles directly increase permeability of fungal cell membrane.
^Chang, Chia-Hsuin; Young-Xu, Yinong; Kurth, Tobias; Orav, John E.; Chan, Arnold K. (2007). "The Safety of Oral Antifungal Treatments for Superficial Dermatophytosis and Onychomycosis: A Meta-analysis". The American Journal of Medicine. 120 (9): 791-798.e3. doi:10.1016/j.amjmed.2007.03.021. ISSN0002-9343.
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^"Haloprogin". DrugBank. University of Alberta. November 6, 2006. Retrieved .
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. PMID10626104.
Antifungal Drugs - Detailed information on antifungals from the Fungal Guide written by R. Thomas and K. Barber