Econazole

Econazole is an antifungal agent that is used therapeutically for fungal infections of the skin, nails and mucous membranes. The topical application of the active ingredient is generally associated with little or no side effects.

What is econazole?

Econazole (also Econazolum) is an imidazole derivative and is assigned to the group of active ingredients imidazoles and triazoles, which act as topical azole antimycotics and have a fungistatic (fungicidal) effect and, in higher concentrations, fungicidal (fungicidal).

Accordingly, econazole is usually applied to dermatomycoses (fungal diseases of the skin, hair and nails) and mycoses of the mucous membranes, which are caused by fungi that are pathogenic to humans such as dermatophytes (thread fungi), molds and / or yeasts.

The active ingredient also shows an antibacterial effect against gram-positive bacteria and can be used for mixed infections (secondary infections). Econazole is a white powder that is almost insoluble in water and is usually present in medicinal products as econazole nitrate.

Pharmacological effect

How all imidazole derivatives work Econazole antifungal by inhibiting the biosynthesis of the ergosterol (a sterol) contained in the cell membrane of the fungi.

In particular, the 14-alpha-demethylase (an enzyme) required for C14-demethylation is inhibited (inhibited). As a result of the inhibited synthesis of ergosterol, the cell membrane of the fungi can no longer be synthesized and there is an accumulation of ergosterol precursors. Since econazole effectively inhibits CYPs (cytochrome 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 impair the liver to lead.

Econazole is, however, usually used locally or topically and externally, so that the absorption of the active ingredient into the circulation is low and usually no interactions are to be expected.

Medical application & use

Due to the wide range of effects of Econazole the drug can be used for almost all dermatomycoses. Econazole is used in particular in the treatment of fungal infections of the skin, nails and mucous membranes in the mouth and pubic area. 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 the event of an additional bacterial infection (mixed or secondary infection) with streptococci or staphylococci, as well as fungal infections caused by steroidal or antibiotic therapy measures. In addition, the active ingredient can treat a bran fungus (Pityriasis versicolor), which is caused by the yeast species Malassezia furfur.

Malassezia furfur usually belongs to the healthy skin flora. Hyperhidrosis (increased sweat production) as a result of a lack of evaporation, sporting activity and / or a hot and humid working environment can lead to increased fungal growth. Econazole can be applied topically as a lotion, cream, spray, solution or powder. In addition, the active ingredient can be used as a cream or vaginal suppository in the event of a vaginal infection by yeasts (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 yeast, especially for Balantis mycotica, as part of an antifungal therapy.

In general, the sexual partner of an affected person should also be treated to avoid a “ping-pong effect” (mutual re-infection).

Risks & side effects

In the presence of hypersensitivity to imidazoles, the use of Econazole contraindicated due to possible allergic reactions.

Therapy with econazole should also be excluded when a diaphragm containing latex is used for contraception. During pregnancy, Econazole should not be administered or only after medical consultation, as the agent is associated with impairment of fetogenesis in the first trimester (third of pregnancy) and increased labor and newborn mortality (foetotoxic effect) in the third trimester, especially at high doses .

In addition, local or topical use of econazole in the area of ​​the nipples (nipples) should be avoided during breastfeeding, as it has not yet been established whether the active ingredient can pass into breast milk.

In addition, when using Econazole, more frequent pruritus (itching), burning, stinging and reddening of the skin can be observed, while allergic reactions (contact dermatitis), skin rashes and inflammations, as well as angioedema (water retention in the subcutis or submucosa) and hives are less common. Econazole can cause irritation of the mucous membranes, especially in the vaginal area.

Finally, the tensile strength of condoms, especially latex condoms, can be negatively affected by econazole.