Biomaterial Database

Topical pharmacology of imidazole antifungals. 1976

R J Holt

Four imidazole derivatives have now undergone extensive open and comparative trials as topical agents in dermatomycoses and vaginal candidosis. They are chlormidazole (Chemie Grünenthal), clotrimazole (Bayer), miconazole (Janssen) and econazole (Janssen, Cilag-Chemie); all also have some antibacterial activity. Many other imidazoles have been marketed, usually as antiprotozoal or anthelminthic agents, and some of these have some antimycotic activity as well as other miscellaneous therapeutic properties. The mode of action of imidazole antimycotic agents is discussed; after prolonged topical application to animals and human subjects, systemic absorption is negligible. All four agents which are available as cream, powder, lotion or vaginal tablets have many sucessful studies to their credit, often with clinical and mycological cure rates of over 80% in a variety of dermatomycoses and in vaginal candidosis. The relative value of these topical agents is discussed, and it is suggested that in severe and extensive dermatomycoses consideration should be given to the systemic use of miconazole in support of topical therapy.

UI	MeSH Term	Description	Entries
D007093	Imidazoles	Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D008825	Miconazole	An imidazole antifungal agent that is used topically and by intravenous infusion.	Brentan,Dactarin,Miconasil Nitrate,Miconazole Nitrate,Monistat,R-14,889,Nitrate, Miconasil,Nitrate, Miconazole,R 14,889,R14,889
D002181	Candidiasis, Vulvovaginal	Infection of the VULVA and VAGINA with a fungus of the genus CANDIDA.	Moniliasis, Vulvovaginal,Vaginitis, Monilial,Candidiasis, Genital,Genital Vulvovaginal Candidiasis,Vaginal Yeast Infection,Vaginal Yeast Infections,Candidiasis, Genital Vulvovaginal,Genital Candidiasis,Infection, Vaginal Yeast,Infections, Vaginal Yeast,Monilial Vaginitis,Vulvovaginal Candidiasis,Vulvovaginal Candidiasis, Genital,Vulvovaginal Moniliasis,Yeast Infection, Vaginal,Yeast Infections, Vaginal
D003022	Clotrimazole	An imidazole derivative with a broad spectrum of antimycotic activity. It inhibits biosynthesis of the sterol ergostol, an important component of fungal CELL MEMBRANES. Its action leads to increased membrane permeability and apparent disruption of enzyme systems bound to the membrane.	Bay b 5097,Canesten,FB b 5097,Kanesten,Klotrimazole,Lotrimin,Mycelex
D003881	Dermatomycoses	Superficial infections of the skin or its appendages by any of various fungi.	Skin Diseases, Fungal,Dermatomycosis,Dermatophyte Infection,Fungal Skin Diseases
D004341	Drug Evaluation	Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals.	Evaluation Studies, Drug,Drug Evaluation Studies,Drug Evaluation Study,Drug Evaluations,Evaluation Study, Drug,Evaluation, Drug,Evaluations, Drug,Studies, Drug Evaluation,Study, Drug Evaluation
D005260	Female		Females
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000287	Administration, Topical	The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example.	Drug Administration, Topical,Administration, Topical Drug,Topical Administration,Topical Drug Administration,Administrations, Topical,Administrations, Topical Drug,Drug Administrations, Topical,Topical Administrations,Topical Drug Administrations
D000935	Antifungal Agents	Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues.	Anti-Fungal Agents,Antifungal Agent,Fungicides, Therapeutic,Antibiotics, Antifungal,Therapeutic Fungicides,Agent, Antifungal,Anti Fungal Agents,Antifungal Antibiotics