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Other Topical Agents
There are a number of topical agents used in treatment of superficial cutaneous mycoses, oropharyngeal candidiasis, and vulvovaginal candidiasis. The superficial cutaneous mycoses that respond to topical therapy include the localized infections of hair, nails, and epidermis due to the dermatophytes and Candida. While some of these topical agents are polyenes, azoles (imidazoles) or allylamines, others are of distinct chemical classes.
In addition to those used for treatment of cutaneous, oropharyngeal, and vulvovaginal fungal infections, an ophthalmic topical antifungal agent, pimaricin (natamycin) is also available. Pimaricin is a polyene used in treatment of keratomycosis. Its commercial formulation is an ophthalmic suspension available in USA (Natacyn™, Alcon Laboratories, Inc., Forthworth, TX). Following ophthalmic installation, pimaricin adheres to the corneal ulcer base very effectively and exerts favorable therapeutic efficacy. Pimaricin suspension is usually applied in concentrations of 2.5 to 5%. It may be used alone or in combination with topical or systemic azole preparations or amphotericin B, depending on the severity of the infection [462, 1139, 1866, 1963, 2223].
Pimaricin is effective mostly against moulds. While it is usually effective in vitro and in vivo against particularly Fusarium spp., clinical failure or in vitro resistance of this fungus against pimaricin has also been reported [861, 1899, 1973]. Similarly, its in vitro or in vivo activity in keratomycosis due to Pseudallescheria boydii may also vary [777, 1541, 1973].
Topical azoles are usually preferred in treatment of keratomycosis due to yeasts. Nevertheless, there are reports on favorable activity of pimaricin in cases due to yeasts as well. Concommittant therapy with pimaricin ointment and local amphotericin B injection to anterior chamber has been effective in keratomycosis due to Candida tropicalis [210].
Pimaricin is effective also against Exserohilum rostratum, Acremonium spp., and Cunninghamella spp.[73, 1973]. On the other hand, Aspergillus spp. , and dermatophytes are frequently resistant to pimaricin [1399, 1866].
The major characteristics of the currently available topical antifungal agents that are in general effective in treatment of superficial cutaneous mycoses and/or candidiasis are shown below [85, 899, 1274, 1744, 1886, 2057, 2092].
Agents which have limited applications and/or unclear efficacy are not included in the list. For more detailed information about clinical use of these agents, refer to the page on related infection. For detailed information on systemic use of polyenes, azoles, and allylamines, refer to the related pages.
Chemical Class
Generic Name |
Trade names |
Manufacturers |
Formulations |
Indications |
| Polyenes |
|
|
|
|
| Amphotericin B |
|
|
C, L, O |
CC |
| |
Fungizone |
Bristol MyersSquibb |
|
|
| Nystatin |
|
|
C, O, OS, P, VT, T |
CC, OC, VC |
| |
Mycostatin |
Bristol MyersSquibb |
|
|
| |
Nilstat |
Wyeth-Ayerst |
|
|
| |
Mykinac |
Alpharma |
|
|
| |
Pedi-Dri |
Pedinol Pharmacal |
|
|
| Azoles (Imidazoles) |
|
|
|
|
| Butoconazole |
|
|
C |
VC |
| |
Femstat |
Bayer |
|
|
| Clotrimazole |
|
|
C, L, S, T, VT |
D, CC, OC, VC |
| |
Fungoid |
Pedinol Pharmacal |
|
|
| |
Lotrimin |
Schering |
|
|
| |
Mycelex |
Bayer |
|
|
| |
Gyne-Lotrimin |
Schering |
|
|
| Econazole |
|
|
C |
D, CC |
| |
Spectazole |
Ortho Dermatological |
|
|
| Ketoconazole |
|
|
C, S |
D, CC |
| |
Nizoral |
Janssen Pharmaceu. |
|
|
| Miconazole |
|
|
C, L, S, P, VS |
D, CC, VC |
| |
Micatin |
McNeil |
|
|
| |
Monistat-Derm |
Ortho Dermatological |
|
|
| |
Monistat-7 |
Ortho Dermatological |
|
|
| |
Monistat-3 |
Ortho Dermatological |
|
|
| Oxiconazole |
|
|
C, L |
D, CC |
| |
Oxistat |
Glaxo Wellcome |
|
|
| Sulconazole |
|
|
C, S |
D, CC |
| |
Exelderm |
Westwood-Squibb |
|
|
| Terconazole |
|
|
C, VS |
VC |
| |
Terazole 3 |
Ortho McNeil |
|
|
| |
Terazole 7 |
Ortho McNeil |
|
|
| Tioconazole |
|
|
C, VO |
VC |
| |
Vagistat-1 |
Bristol-Myers Squibb |
|
|
| Allylamines and other non-azole ergosterol synthesis inhibitors |
|
|
|
|
| Amorolfine |
|
|
NL |
O |
| |
Loceryl |
Roche Laboratories |
|
|
| Butenafine HCl |
|
|
C |
D |
| |
Mentax |
Penederm |
|
|
| Naftifine |
|
|
C, O, P |
D |
| |
Naftin |
Allergan |
|
|
| Terbinafine |
|
|
C, S |
D |
| |
Lamisil |
Sandoz Pharmaceu. |
|
|
| Other agents |
|
|
|
|
| Ciclopirox olamine |
Loprox |
Hoechst Marion Roussel |
C, L |
D, CC |
| |
Penlac |
Dermic |
NL |
O |
| Haloprogin |
|
|
C |
D, CC |
| |
Halotex |
Westwood Squibb |
|
|
| Tolnaftate |
|
|
C, S, P |
D |
| |
Aftate |
Schering-Plough |
|
|
| |
NP-27 |
Thompson Medical |
|
|
| |
Tinactin |
Schering-Plough |
|
|
| |
Ting |
Fisons |
|
|
| Undecylenate |
|
|
C, P, O, S |
D |
| |
Cruex |
Fisons |
|
|
| |
Desenex |
Fisons |
|
|
C: cream L: lotion
NL: nail lacquer O: ointment
OS: oral suspension P: powder
S: solution/spray VO: vaginal ointment
VS: vaginal suppository T: troche VT: vaginal tablet
D: dermatophytosis CC: cutaneous candidiasis
OC: oropharyngeal candidiasis VC: vulvovaginal candidiasis
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References
73. Anandi, V., J. A. George, R. Thomas, K. N. Brahmadathan, and T. J. John. 1991. Phaeohyphomycosis of the eye caused by Exserohilum rostratum in India. Mycoses. 34:489-91.
85. Anonymous. 2000. Cicloprox (Penlac) nail lacquer for onychomycosis. The Medical Letter. 42:51.
210. Behrens-Baumann, W., R. Ruechel, O. Zimmermann, and M. Vogel. 1991. Candida tropicalis endophthalmitis following penetrating keratoplasty. Br. J. Opthalmol. 75:565.
462. Collier, L., A. Balows, and M. Sussman. 1998. Topley & Wilson's Microbiology and Microbial Infections, 9th ed, vol. 4. Arnold, London, Sydney, Auckland, New York.
777. Friedman, D. S., J. V. Schoster, J. P. Pickett, R. R. Dubielzig, C. Czuprynski, J. S. Knoll, and L. J. Wolfgram. 1989. Pseudallescheria boydii keratomycosis in a horse. J Am Vet Med Assoc. 195:616-8.
861. Goldblum, D., B. E. Frueh, S. Zimmerli, and M. Bohnke. 2000. Treatment of postkeratitis fusarium endophthalmitis with amphotericin B lipid complex [In Process Citation]. Cornea. 19:853-6.
899. Greenspan, D. 1994. Treatment of oropharyngeal candidiasis in HIV-positive patients. J. Amer. Acad. Dermatol. 31 (Suppl. 2):S51-S55.
1139. Jones, D. B. 1978. Therapy of postsurgical fungal endophthalmitis. Ophthalmology. 85:357-73.
1274. Kwon-Chung, K. J., and J. E. Bennett. 1992. Medical Mycology. Lea & Febiger, Philadelphia.
1399. Macura, A. B. 1993. In vitro susceptibility of dermatophytes to antifungal drugs: a comparison of two methods. Int. J. Dermatol. 32:533-6.
1541. Mills, R., and G. Garrett. 1992. Pseudallescheria boydii keratitis. Aust N Z J Ophthalmol. 20:253-6.
1744. Pelletier, R., J. Peter, C. Antin, C. Gonzalez, L. Wood, and T. J. Walsh. 2000. Emergence of resistance of Candida albicans to clotrimazole in human immunodeficiency virus-infected children: In vitro and clinical correlations. J Clin Microbiol. 38:1563-8.
1866. Rahman, M. R., G. J. Johnson, R. Husain, S. A. Howlader, and D. C. Minassian. 1998. Randomised trial of 0.2% chlorhexidine gluconate and 2.5% natamycin for fungal keratitis in Bangladesh. Br J Ophthalmol. 82:919-25.
1886. Reef, S. E., W. C. Levine, M. M. McNeil, S. Fisher-Hoch, S. D. Holmberg, A. Duerr, D. Smith, J. D. Sobel, and R. W. Pinner. 1995. Treatment options for vulvovaginal candidiasis. Background paper for development of 1993 STD treatment recommendations. Clin. Infect. Dis. 20 (Suppl. 1):S80-S90.
1899. Reuben, A., E. Anaissie, P. E. Nelson, R. Hashem, C. Legrand, D. H. Ho, and G. P. Bodey. 1989. Antifungal susceptibility of 44 clinical isolates of Fusarium species determined by using a broth microdilution method. Antimicrob. Agents Chemother. 33:1647-1649.
1963. Rosa, R. H., Jr., D. Miller, and E. C. Alfonso. 1994. The changing spectrum of fungal keratitis in south Florida. Ophthalmology. 101:1005-13.
1973. Rotowa, N. A., H. J. Shadomy, and S. Shadomy. 1990. In vitro activities of polyene and imidazole antifungal agents against unusual opportunistic fungal pathogens. Mycoses. 33:203-11.
2057. Schopf, R., O. Hettler, M. Brautigam, G. Weidinger, U. Kaben, P. Mayser, and V. Resl. 1999. Efficacy and tolerability of terbinafine 1% topical solution used for 1 week compared with 4 weeks clotrimazole 1% topical solution in the treatment of interdigital tinea pedis: a randomized, double-blind, multi-centre, 8-week clinical trial. Mycoses. 42:415-420.
2092. Sheehan, D. J., C. A. Hitchcock, and C. M. Sibley. 1999. Current and emerging azole antifungal agents. Clin. Microbiol. Rev. 12:40-79.
2223. Tanure, M. A., E. J. Cohen, S. Sudesh, C. J. Rapuano, and P. R. Laibson. 2000. Spectrum of fungal keratitis at Wills Eye Hospital, Philadelphia, Pennsylvania. Cornea. 19:307-12.
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