Clotrimazole2, a synthetic imidazole derivative, is primarily used locally in the treatment of vaginal and skin infections due to yeasts and dermatophytes. In vitro, it is most active against Candida spp., Trichophyton spp., Microsporum spp. and Malazzesia furfur (Pityrosporon orbiculare). In addition, it has some in vitro activity against certain Gram-positive bacteria, and at very high concentrations has activity against Trichomonas spp.
In the treatment of vaginal candidiasis, clotrimazole vaginal tablets have produced cure rates comparable with those of conventional nystatin vaginal tablets. There have been no published comparisons with nystatin vaginal cream or foaming vaginal tablets — nystatin dosage forms preferred by some clinicians. Clotrimazole has also been successful in patients who had failed to respond to other antifungal agents such as nystatin and amphotericin B. Results in trichomonal vaginitis are not impressive.
Skin infections caused by Candida or dermatophytes have been effectively treated with topical application of clotrimazole. In comparative trials, clotrimazole cream has been as effective as Whitfleld’s ointment and tolnaftate in the treatment of dermatophytoses, and as effective as nystatin in cutaneous candidiasis. Clotrimazole topical preparations are generally well tolerated, but local irritation has necessitated withdrawal of therapy in a few cases.
Candidal septicemia and urinary and pulmonary candidiasis have been cured with oral clotrimazole therapy. Results in other types of serious fungal infections, including pulmonary aspergillosis, have been disappointing. A limiting factor in oral clotrimazole therapy is the high incidence of gastro-intestinal disturbances and neurological reactions.
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Aal, H.A. and Moawad, M.K.: Clinical experience with Canesten cream (Bay b 5097) against dermatophytes in Egypt. Mykosen 16: 369 (1973).
Bewick, M. and Raper, D.A.: The diagnosis of systemic fungal infection in renal transplant patients and treatment with clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 34 (1974).
Bodenhoff, J.: A new antimycotic from Bayer AG, Bay b 5097. Acta Pathologica et Microbiologica Scandinavica 79: 345 (1971).
Bolt, H.M. and Kappus, H.: Effect of clotrimazole treatment on the demethylation of mestranol. Hormone and Metabolism Research 5: 234(1973).
Buchet, K.H.; Draber, W.; Regel, E. and Plempel, M.: Syntheses and properties of clotrimazole and other antimycotic 1-triphenylmethyl imidazoles. Drugs Made in Germany 75: 79 (1972).
Burgess, M.A. and Bodey, G.P.: Clotrimazole (Bay b 5097): in vitro and clinical pharmacological studies. Antimicrobial Agents and Chemotherapy 2: 423 (1972).
Cartwright, R.Y.: Clotrimazole in the treatment of acute and ‘resistant’ vaginal candidiasis. Postgraduate Medical Journal 50 (Suppl.1): 90(1974).
Cartwright, R.Y.; Shaldon, C. and Hall, G.H.: Urinary candidiasis after renal transplantation. British Medical Journal 2: 351 (1972).
Cho, N.; Saito, T.; Fukada, M.; Sato, I.; Kurakata, H. and Matsuhashi, K.: Clinical studies on clotrimazole as antifungal therapy in obstetrics and gynecology. Current Medical Research and Opinion 2: 1 (1974).
Clayton, Y.M. and Connor, B.L.: Clinical trial of clotrimazole in the treatment of superficial fungal infections. Postgraduate Medical Journal 50 (Suppl. 1): 66 (1974).
Cohen, M.; Harkness, R.A.; Renz, M. and Farquhar, J. W.: Trials of the use of clotrimazole in the treatment of oral candidiasis in newborn babies. Postgraduate Medical Journal 50 (Suppl. 1): 28(1974).
Comaish, J.S.: Double-blind comparison of clotrimazole with Whitfield’s and nystatin ointments. Postgraduate Medical Journal 50 (Suppl. 1): 73 (1974).
Couchman, J.M.: A preliminary report on a trial of clotrimazole against vaginal candidiasis in venereology. Postgrad. med. J. 50 (Suppl. 1): 93 (1974).
Crompton, G.K. and Milne, U.R.: Treatment of bronchopulmonary aspergillosis with clotrimazole. British Journal of Diseases of the Chest 67: 301 (1973).
David, L.M.; Veien, N.K.; Schmidt, J.D.; Murtishaw, W. and Smith E.B.: Topical clotrimazole in dermatophytosis. Current Therapeutic Research 15: 133 (1973).
Dogliotti, M. and Bisset, E.A.: Tinea capitis in black children. South African Medical Journal 48: 2215 (1974).
Drouchet, E.: Systemic mycoses — an acute diagnostic and therapeutic problem. Clinical Excerpts 35: 1219 (1973).
Duhm, B.; Maul, W.; Medenwald, H.; Patzche, K.; Wagner, L.A. and Oberste-Lehn, H.: Pharmacokinetics of topically applied Bis phenyl-(2-chlorophenyl)-1-imidazolyl-methane-[14C]. Drugs Made in Germany 15: 99 (1972).
Dunster, G.D.: Vaginal candidiasis in pregnancy — a trial of clotrimazole Postgraduate Medical Journal 50 (Suppl. 1): 86 (1974).
El Sheikh, M.: Laboratory and clinical experience with clotrimazole (Bay b 5097). Sabouraudia 10: 210 (1972).
El Zawahry, M. and Moawad, M.K.: Topical treatment of dermatomycoses with Canesten cream, and new antimycotic compound. Mykosen 16: 363 (1973).
Evans, E.G.V.; Watson, D.A. and Mathews, N.R.: Pulmonary aspergillomata in a child treated with clotrimazole. British Medical Journal 4: 599 (1971).
Fredriksson, T.: Topical treatment with Bay b 5097, a new broad spectrum antimycotic agent. British Journal of Dermatology 86: 628 (1972).
Freis, A.: The tolerance of clotrimazole on topical application. Drugs Made in Germany 15: 120 (1972).
Gillesberger, W. and Engelhardt, A.: An open trial of topical clotrimazole in dermatomycoses. Postgraduate Medical Journal 50 (Suppl. 1): 61 (1974).
Gip, L.: Topical treatment with clotrimazole in dermatomycosis. Current Therapeutic Research 16: 27 (1974a).
Gip, L.: The topical therapy of pityriasis versicolor with clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 59 (1974b).
Hall-Smith, P.: Dermatomycoses: a brief history of therapy and initial results with clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 70(1974).
Hamilton-Miller, J.M.T.: Physiological Properties of Mutagen-induced variants of Candida albicans resistant to polyene antibiotics. Journal of Medical Microbiology 5: 425 (1972).
Harkness, R.A. and Renz, M.: Endocrine effects of the antimycotic compound clotrimazole, and its related effects on enzymic activities in leucocytes. Brit. J. clin. Pharmacol. 1: 342 (1974).
Higton, B.K.: A trial of clotrimazole and nystatin in vaginal moniliasis. Journal of Obstetrics and Gynaecology of the British Commonwealth 80: 992 (1973).
Hirsch, A.; Szalmay, G. and Dedes, M.: Treatment of genital mycosis with clotrimazole (Bay b 5097 ). VIIth International Congress in Chemotherapy, Prague, 1971, p.253 (1971).
Holt, R.J. and Newman, R.L.: The treatment of urinary candidosis with the oral antifungal drugs 5-fluorosytosine and clotrimazole. Developmental Medicine and Child Neurology 14: 70 (1972a).
Holt, R.J. and Newman, R.L.: Urinary candidiasis after renal transplantation. Brit. med. J. 2: 714 (1972b).
Holt, R.J. and Newman, R.L.: Laboratory assessment of the antimycotic drug clotrimazole. Journal of Clinical Pathology 25: 1089 (1972c).
Holt, R.J.: Recent developments in antimycotic chemotherapy. Infection 2: 95 (1974).
Iwata, K.; Kanda, Y.; Yamaguchi, H. and Osumi, M.: Electronmicroscopic studies on the mechanism of action of clotrimazole on Candida albicans. Sabouraudia 11: 205 (1973b).
Iwata, K.; Yamaguchi, H. and Hiratani, T.: Mode of action of clotrimazole. Sabouraudia 11: 158 (1973a).
Jamieson, A. and Anderson, K.: Primary amoebic meningoencephalitis. Lancet 1: 261 (1974).
Jones, B.R.; Richards, A.B. and Clayton, Y.M.: Clotrimazole in the treatment of ocular infeciton by Aspergillus fumigatus. Postgraduate Medical Journal 50 (Suppl. 1): 39 (1974).
Keczkes, K.; Leighton, I. and Good, C.S.: Topical treatment of dermatophytoses and candidoses. Practitioner 214: 412 (1975).
Kobayashi, T. and Amenomori, Y.: Results of a clinical investigation of clotrimazole (‘Canesten’), a new anti-mycotic substance, in the therapy of vaginal fungal infections. Journal of International Medical Research 2: 366 (1974).
Legal, H-P.: The treatment of trichomonas and Candida vaginitis with clotrimazole vaginal tablets. Postgraduate Medical Journal 50 (Suppl. 1): 81 (1974).
Liljedahl, SO.; Frisk, Å. and Wickman, K.: Successful treatment of Candida septicaemia in severely burned patients with a new antimycotic, clotrimazole (Bay b 5097 ). Injury: The British Journal of Accident Surgery 4: 157(1972).
Lohmeyer, H.: Treatment of candidiasis and trichomoniasis of the female genital tract. Postgraduate Medical Journal 50 (Suppl. 1): 78 (1974).
Male, O.: A double-blind comparison of clotrimazole and tolnaftate therapy of superficial dermatophytoses. Postgrad, med. J.50 (Suppl. 1): 75 (1974).
Marget, W. and Adam, D.: Bay b 5097, a new orally applicable antifungal substance with broadspectrum activity. Acta paediat. scand. 60: 341 (1971).
Marks, H.J.: A double-blind comparison of clotrimazole and nystatin vaginal tablets in Candida vaginitis. Postgrad. med. J. JO (Suppl. 1): 105 (1974).
Marks, M.I.; Steer, P. and Eickhoff, T.C.: In vitro sensitivity of Torulopsis glabarata to amphotericin B, 5-fluorocytosine and clotrimazole (Bay 5097). Applied Microbiology 22: 93 (1971).
Masterton, G.; Henderson, J.; Napier, I.R. and Moffet, M.: Six-day clotrimazole therapy in vaginal candidosis. Current Medical Research and Opinion 3: 83 (1975).
Meinhof, W. and Günther, D.: Treatment of chronic mucocutaneous candidiasis of children (candida granuloma) with clotrimazole. Archives for Dermatological Research 242: 293 (1972).
Milne, L.J.R.: Mycologjcal studies in the use of clotrimazole in bronchopulmonary aspergillosis and neonatal and vaginal candidiasis. Postgraduate Medical Journal 50 (Suppl. 1): 20 (1974).
Nakama, T.: A clinical investigation of clotrimazole (Bay b 5097) cream on skin candidiasis. Kurume Medical Journal 19: 259 (1972).
Nishimoto, K.: Clinical experiences on the treatment of dermatomycoses with Bay b 5097 cream and solution. J. West-Japan Derm. 34: No.6 (1972).
Oates, J.K. and Davidson, F.: Treatment of vaginal candidiasis with clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 99 (1974).
Oberste-Lehn, H.: Ideal properties of a modern antifungal agent — the therapy of mycoses with clotrimazole. Postgrad. med. J. 50 (Suppl. 1): 51 (1974).
Oberste-Lehn, H.; Baggesen, I. and Plempel, M.: Preliminary clinical studies of a new oral antimycotic agent in systemic mycosis. Deutsche Medizinische Wochenschrift 14: 1361 (1969).
Plempel, M. and Bartman, K.: Experimental studies on the antimycotic action of clotrimazole (Canesten) in vitro and after local application in vivo. Drugs Made in Germany 15: 103 (1972).
Polemann, G.: Clinical experience in the local treatment of dermatomycoses with clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 54 (1974).
Renz, M.; Farquhar, J.W.; Cohen, M. and Harkness, R.A.: Elevation of myeloperoxidase activity in infants with oral candidiasis treated with clotrimazole. Postgrad. med. J. 50 (Suppl. 1): 30 (1974).
Schnell, J.D.: The incidence of vaginal Candida and trichomonas infections and treatment of trichomonas vaginitis with clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 79 (1974).
Shadomy, S.: In vitro antifungal activity of clotrimazole (Bay b 5097). Infect. Immun. 4: 143 (1971a).
Shadomy, S.: In vivo studies with Bay b 5097. Antimicrob. Agents Chemother. — 1970: 169 (1971b).
Smith, E.B.; David, L.M. and Knox, J.M.: Topical clotrimazole in dermatophytosis in a prison environment. Postgrad. med. J.50 (Suppl. 1): 64 (1974).
Tamura, S.; Kwamoto, H.; Yamada, T.; Majima, H. and Miyamoto, H.: Therapy of candida vaginitis and Candida vulvovaginitis with a new antimycotic substance, clotrimazole. Current Medical Research and Opinion 1: 540 (1973).
Tan, C.G.; Good, C.S.; Milne, L.J.R. and Loudon, J.D.O.: A comparative trial of six day therapy with clotrimazole and nystatin in pregnant patients with vaginal candidiasis. Postgraduate Medical Journal 50 (Suppl. 1): 102 (1974).
Tettenborn, D.: Acute toxicity and local tolerance of clotrimazole. Drugs Made in Germany 15: 94 (1972).
Tettenborn, D.: Toxicity of clotrimazole. Postgraduate Medical Journal 50 (Suppl 1): 17(1974).
Von Kunicki, A.: Ergebnisse der clotrimazol-therapie bei Candida- und Trichomonas-infektionen. Arzneimittel-Forschung (Drug Research) 24: 534 (1974).
Von Lachenicht, P. and Potel, J.: Untersuchungen zur lokalen Chemotherapie und zur epidemiologie der weiblichen genitalmykose. Arzneimittel-Forschung (Drug Research) 24: 525 (1974).
Wahlberg, J.E.: Irritation threshold, tolerance and cross-reactions with clotrimazole applied to skin. Postgraduate Medical Journal 50 (Suppl.1): 53 (1974).
Waitz, J.A.; Moss, E.L. and Weinstein, M.J.: Chemotherapeutic evaluation of clotrimazole (Bay b 5097, l(o-chloro-α-α-diphenylbenzyl) imidazole). Applied Microbiology 22: 891 (1971).
Weingartner, L.; Sitka, U.; Patsch, R. and Grundig, C.: Studies on the activity of a new antimycotic (Bay b 5097) in children. International Journal of Clinical Pharmacology, Therapy and Toxicology 6: 358 (1972).
Weuta, H.: Clotrimazole vaginal tablets — clinical investigation in an open study. Drugs Made in Germany 15: 121 (1972).
Weuta, H.: Clinical studies with oral clotrimazole. Postgraduate Medical Journal 50 (Suppl. 1): 45 (1974).
Widholm, O.: An open trial of local therapy with clotrimazole for vaginal candidiasis. Postgraduate Medical Journal 50 (Suppl. 1): 85 (1974).
Woutters, A.: Comparison of activity of various trichomonacides in vitro. International Symposium on Diagnosis and Chemotherapy of Urinary and Genital Infections due to Protozoa — Fungi and Bacteria, Florence, May 1971.
Yamaguchi, H; Kanda, Y.; Iwata, K. and Osumi, M.: Electronmicroscopical studies on the fungitoxicity of bisphenyl-[2-chlorophenyl]-1-imidazolyl methane (Bay b 5097): preferential effect on the nuclear envelope in Candida albicans cells. Journal of Electron Microscopy 22: 167 (1973).
See subject index in each issue for further indexing terms.
‘Canesten (Bayer)’; ‘Lotrimin’(Delbay)
Manuscript reviewed by: Dr M. Bewick, Department of Surgery, Guy’s Hospital, London, England; Dr R. Carruthers, Consultant Dermatologist, Launceston, Australia; Dr N. Cho, Department of Obstetrics and Gynaecology, Showa University, Tokyo, Japan; Dr G. Dennerstein, Consultant Gynaecologist, Melbourne, Australia; Dr R.J. Holt, Department of Microbiology, Queen Mary’s Hospital for Children, Surrey, England; Prof. G. Medoff, Washington University, St. Louis, Mo., USA; Dr H. ObersteLehn, Ferdinand Sauerbruch Clinic, Wuppertal-Elberfeld, West Germany; Dr R.G. Park, Consultant Dermatologist, Wellington, New Zealand; Dr J.H.S. Pettit, Consultant Dermatologist, Kuala Lumpur, Malaysia; Dr R.J. Seddon, Postgraduate School of Obstetrics and Gynaecology, The University of Auckland, New Zealand; Dr J.P. Utz, Georgetown University, Washington, D.C., USA; Dr K.O. Wong, Consultant Dermatologist, Hong Kong.
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Sawyer, P.R., Brogden, R.N., Pinder, K.M. et al. Clotrimazole: A Review of its Antifungal Activity and Therapeutic Efficacy. Drugs 9, 424–447 (1975). https://doi.org/10.2165/00003495-197509060-00003
- Antifungal agents