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Terbinafine
Terbinafine is an allylamine structurally related to naftifine. It is a synthetic antifungal agent. It is highly lipophilic in nature and tends to accumulate in skin, nails, and fatty tissues [656, 1934].
Terbinafine has oral and topical (cream) formulations. Oral preparation has been first introduced in 1991 in United Kingdom and approved for clinical use in 1996 in USA [950, 1014]. It is being manufactured by Novartis Pharmaceuticals. Its trade name is Lamisil.
As with the other allylamines, terbinafine inhibits ergosterol biosynthesis via inhibition of squalene epoxidase. This enzyme is part of the fungal sterol synthesis pathway that creates the sterols needed for the fungal cell membrane.
Terbinafine is mainly effective on a specific group of fungi, dermatophytes. However, a standard in vitro susceptibility testing methodology is not yet available for this group. Studies to address this to question are in progress. One of the parameters under investigation is the standard medium to be used in the test. This medium should enhance conidium formation in dermatophytes. Although as yet unstandardized, the in vitro activity of terbinafine has been tested against various dermatophytes. Terbinafine yields lower MICs compared to fluconazole, itraconazole, and griseofulvin [1121]. The meaning and clinical significance of these data demand further investigations and development of a standard in vitro susceptibility testing method.
Terbinafine has in vitro activity also against most Candida spp., Aspergillus spp., Sporothrix schenckii [1119], Penicillium marneffei [1489], Malassezia furfur [1767], Cryptococcus neoformans [1991], Trichosporon spp. and Blastoschizomyces [1990].
For terbinafine MICs obtained for various types of fungi, see susceptibility patterns and the susceptibility database.
The typical dose of terbinafine is 250 mg/day [617].
Adverse reactions to terbinafine are in general transient and mild. The incidence of these reactions has been found to be 10.5% in a large scale study. Most involve the gastrointestinal system and the skin [971]. Reversible agranulocytosis has been reported as a rare side effect [1694].
Terbinafine is available for oral and topical administrations. Topically, 1% cream and solution formulations are used.
Terbinafine is one of the mainstays of treatment of dermatophytosis. Compared to the previously existing antifungal agent, griseofulvin, it is more effective, as well as being significantly less toxic. Moreover, the required duration of therapy is also shorter with terbinafine.
This property is of interest, particularly in cases of onychomycosis where prolonged courses of therapy are needed [114]. Terbinafine is a safe and efficacious agent in treatment of this clinical setting [617, 1014], as well as other dermatophytosis. It appears to be similarly or more effective than its alternative, itraconazole [522, 1934] and also fluconazole [1001].
Terbinafine, when combined with fluconazole, has occasionally been successful in treatment of oropharyngeal infections due to fluconazole-resistant Candida spp. [833]. An even more recent report suggests a possible role for terbinafine alone against azole-resistant oropharyngeal infections [2298].
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References
114. Arenas, R., J. Dominguez-Cherit, and L. M. Fernandez. 1995. Open randomized comparison of itraconazole versus terbinafine in onychomycosis. Int. J. Dermatol. 34:138-43.
522. De Backer, M., C. De Vroey, E. Lesaffre, I. Scheys, and P. De Keyser. 1998. Twelve weeks of continuous oral therapy for toenail onychomycosis caused by dermatophytes: A double-blind comparative trial of terbinafine 250 mg/day versus itraconazole 200 mg/day. J. Amer. Acad. Dermatol. 38:S57-S63.
617. Drake, L. A., N. H. Shear, J. P. Arlette, R. Cloutier, F. W. Danby, B. E. Elewski, S. Garnis-Jones, J. M. Giroux, D. Gratton, W. Gulliver, P. Hull, H. E. Jones, M. Journet, A. L. Krol, J. J. Leyden, S. C. Maddin, J. B. Ross, R. C. Savin, R. K. Scher, G. R. Sibbald, N. H. Tawfik, N. Zaias, M. Tolpin, S. Evans, J. E. Birnbaum, and et al. 1997. Oral terbinafine in the treatment of toenail onychomycosis: North American multicenter trial. J. Amer. Acad. Dermatol. 37:740-745.
656. Elewski, B. E. 1998. Onychomycosis: Pathogenesis, diagnosis, and management. Clin. Microbiol. Rev. 11:415-429.
833. Ghannoum, M. A., and B. Elewski. 1999. Successful treatment of fluconazole-resistant oropharyngeal candidiasis by a combination of fluconazole and terbinafine. Clin Diagn Lab Immunol. 6:921-923.
950. Gupta, A. K., and N. H. Shear. 1997. Terbinafine: an update. J. Amer. Acad. Dermatol. 37:979-988.
971. Hall, M., C. Monka, P. Krupp, and O. S. D. 1997. Safety of oral terbinafine: results of a postmarketing surveillance study in 25,884 patients. Arch. Dermatol. 133:1213-1219.
1001. Havu, V., H. Heikkila, K. Kuokkanen, M. Nuutinen, T. Rantanen, S. Saari, S. Stubb, R. Suhonen, and K. Turjanmaa. 2000. A double-blind, randomized study to compare the efficacy and safety of terbinafine (Lamisil (R)) with fluconazole (Diflucan (R)) in the treatment of onychomycosis. Brit J Dermatol. 142:97-102.
1014. Hecker, D. 1997. Current trends in onychomycosis therapy: a literature review. Mount Sinai Journal of Medicine. 64:399-405.
1119. Jessup, C. J., N. S. Ryder, and M. A. Ghannoum. 2000. An evaluation of the in vitro activity of terbinafine. Med Mycol. 38:155-159.
1121. Jessup, C. J., J. Warner, N. Isham, I. Hasan, and M. A. Ghannoum. 2000. Antifungal susceptibility testing of dermatophytes: Establishing a medium for inducing conidial growth and evaluation of susceptibility of clinical isolates. J Clin Microbiol. 38:341-344.
1489. McGinnis, M. R., N. G. Nordoff, N. S. Ryder, and G. B. Nunn. 2000. In vitro comparison of terbinafine and itraconazole against Penicillium marneffei. Antimicrob. Agents Chemother. 44:1407-1408.
1694. Ornstein, D. L., and P. Ely. 1998. Reversible agranulocytosis associated with oral terbinafine for onychomycosis. J Amer Acad Dermatol. 39:1023-1024.
1767. Petranyi, G., J. G. Meingassner, and H. Mieth. 1987. Antifungal activity of the allylamine derivative terbinafine in vitro. Antimicrob. Agents Chemother. 31:1365-1368.
1934. Roberts, D. T. 1994. Oral therapeutic agents in fungal nail disease. J. Amer. Acad. Dermatol. 31:S78-81.
1990. Ryder, N. S. 1999. Activity of terbinafine against serious fungal pathogens. Mycoses. 42:115-119.
1991. Ryder, N. S., S. Wagner, and I. Leitner. 1998. In vitro activities of terbinafine against cutaneous isolates of Candida albicans and other pathogenic yeasts. Antimicrob. Agents Chemother. 42:1057-1061.
2298. Vazquez, J., A. Lamaraca, R. Schwartz, R. Ramirez, L. Smith, R. Pollard, J. Gill, A. Fothergill, L. Ince, J. Wirzman, A. Perez, and J. Felser. 2000. Management of fluconazole-refractory oropharyngeal candidiasis with high-dose terbinafine in patients with AIDS. 40th Interscience Conference on Antimicrobial Agents and Chemotherapy, Abstract No.
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