Econazole is an antifungal agent that is used therapeutically for fungal infections of the skin, nails, and mucous membranes. Topical application of the active ingredient is generally associated with no or minor side effects.
What is econazole?
Econazole is an antifungal agent used therapeutically for fungal infections of the skin, nails, and mucous membranes. Econazole (also econazolum) is an imidazole derivative and is assigned to the imidazole and triazole group of active ingredients, which act as topical azole antifungals fungistatically (inhibiting fungi) and in higher concentrations fungicidally (killing fungi). Accordingly, econazole is generally applied in dermatomycoses (fungal diseases of the skin, hair and nails) and mycoses of the mucous membranes caused by human pathogenic fungi such as dermatophytes (filamentous fungi), molds and/or yeasts. The active ingredient also exhibits antibacterial activity against Gram-positive bacteria and can be used to treat mixed infections (secondary infections). Econazole is a white powder that is almost insoluble in water and is generally present in drugs as econazole nitrate.
Pharmacologic action
Like all imidazole derivatives, econazole has an antifungal effect by inhibiting the biosynthesis of ergosterol (a sterol) contained in the cell membrane of fungi. In particular, 14-alpha-demethylase (an enzyme), which is required for C14 demethylation, is inhibited. As a result of inhibited ergosterol synthesis, the fungal cell membrane can no longer be synthesized and an accumulation of ergosterol precursors occurs. Since econazole effectively inhibits CYPs (cytochromes P450), metabolizing enzymes that are particularly active in the liver and participate in the metabolism of drugs, fatty acids, steroids, bile acids, and vitamins, among other things, systemic application in high doses could lead to liver impairment. However, econazole is generally applied locally or topically and externally, so absorption of the active ingredient into the circulation is low and no interactions are usually expected.
Medicinal use and application
Due to the broad spectrum of activity of econazole, the drug can be used for almost all dermatomycoses. In particular, Econazole is used in the treatment of fungal infections of the skin, nails, and mucous membranes of the mouth and pubic area. Thus, the application of Econazole is indicated for infections caused by dermatophytes (including Epidermophyton, Trichophyton and/or Microsporum species), yeasts (including Candida albicans) or molds (including Cladosporium, Aspergillus species). Econazole can also be used in cases of additional bacterial infection (mixed or secondary infection) with streptococci or staphylococci, as well as fungal infections caused by steroidal or antibiotic therapy. In addition, the active ingredient can be used to treat pityriasis versicolor, a fungal infection caused by the yeast species Malassezia furfur. Malassezia furfur usually belongs to the healthy skin flora. Hyperhidrosis (increased sweat production) due to a lack of evaporation, athletic activity, and/or a hot and humid work environment may result in increased fungal growth. Econazole can be applied topically as a lotion, cream, spray, solution or powder. In addition, the active ingredient can be applied as a cream or vaginal suppository for vaginal infections caused by yeast fungi (including Candida albicans). The use of the imidazole derivative is also indicated for secondary bacterial infections of the vagina. Econazole is also applied locally as a vaginal cream for infections of the male penis or genital area with yeasts, especially Balantis mycotica, as part of an antifungal therapy. In general, the sexual partner of an affected person should be co-treated to avoid a “ping-pong effect” (mutual re-infection).
Risks and side effects
In the presence of hypersensitivity to imidazoles, use of econazole is contraindicated because of possible allergic reactions. Similarly, therapy with econazole should be excluded when using a latex-containing diaphragm for contraception.Econazole should not be used during pregnancy, or only after consultation with a physician, as the drug is associated with impaired fetogenesis in the first trimester (third trimester) and increased labor activity and neonatal mortality (fetotoxic effect) in the third trimester, especially at high doses. In addition, local or topical application of econazole in the area of the nipples should be avoided during breastfeeding, as it is not yet certain whether the active ingredient can pass into breast milk. In addition, pruritus (itching), burning, stinging and reddening of the skin are more frequently observed with the use of econazole, while allergic reactions (contact dermatitis), skin rashes and inflammations as well as angioedema (water retention in the subcutis or submucosa) and hives are less frequently observed. Especially in the vaginal area, econazole may cause mucosal irritation. Finally, the tear strength of condoms, especially latex condoms, may be negatively affected by econazole.