Econazole (e kon’na zole) is a broad spectrum topical antifungal used to treat tinea pedis, tinea cruris, tinea corporis, and tinea versicolor caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Microsporum canis, Microsporum audouini, Microsporum gypseum, and Epidermophyton floccosum. As well as being antimycotic its also has some action against Gram positive bacteria. It first was patented in 1968 and used since in 1974.
Econazole nitrate is available as a 1% topical cream with most formulations being in a water-miscible base that generally consists of benzoic acid, butylated hydroxytoluene, mineral oil, oleoyl polyoxylglycerides PEG-6-32 stearate/glycol stearate and water.
Mechanism of action:
Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme to inhibit lanosterol converting to ergosterol resulting in increased cellular permeability that causes cell death from leakage of cellular contents.
Pharmacokinetics:
Systemic absorption of econazole nitrate is extremely low after topical application to the skin.
Half-life: unknown
Bioavailability: unknown
Metabolism: Hepatic
Excretion: unknown
Econazole nitrate packaging from Taro Pharmaceuticals (USA)
Adverse effects:
Affect ~3%.
Burning, irritation, pruritic rash and redness at the site of application.
Contraindications:
Allergy or hypersensitivity to econazole or any of the ingredients used in the formulation.
Dosage:
Applied once or twice daily to the affected area.
Precautions:
External use only. Not for ophthalmic use.
No studies on use during pregnancy; it has not been shown to be teratogenic when administered orally to mice, rabbits or rats.
It is not known if econazole nitrate is excreted in human milk; oral administration of large doses of econazole nitrate to lactating rats found econazole or its metabolites in the excreted in milk.
Interactions:
Due to very low systemic absorption, clinical interactions are extremely rare.
Those on oral anticoagulants (eg warfarin, acenocoumarol) use with caution and monitor anticoagulant effect more frequently, especially if econazole used under occlusion (econazole can enhance anticoagulation effect).
Brand names: Pevaryl; Spectazole; Ecostatin; Ecoza; and others
Chemical formula: C18H15Cl3N2O
Systematic chemical name: 1-[2-{(4-chloro-phenyl) methoxy}-2-(2,4-dichlorophenyl)ethyl]-1H-imidazole mononitrate
Other anti-fungal drugs:
| Antibiotics | Polyenes: | Nystatin | Amphotericin B | Hamycin | |
| Heterocyclic benzofuran: | Griseofulvin | ||||
| Echinocandins: | Caspofungin | Micafungin | Anidulafungin | ||
| Azoles: | Imidazoles: | Topical: | Clotrimazole | Econazole | Miconazole |
| Bifonazole | |||||
| Systemic: | Ketoconazole | ||||
| Triazoles: | Fluconazole | Itraconazole | Voriconazole | Posaconazole | |
| Efinaconazole | Fosravuconazole | ||||
| Morpholines: | Amorolfine | ||||
| Allylamines: | Terbinafine (oral) | Terbinafine (topical) | |||
| Other topical agents: | Tolnaftate | Benzoic acid | Butenafine | Sodium thiosulfate | Quiniodochlor |
| Undecylenic acid | Ciclopirox olamine | Gentian Violet |
In Australia, econazole is on the National Podiatry Scheduled Medicines List.
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