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Amorolfine
Amorolfine is a morpholine derivative which is used topically as an antifungal agent. It has a broad spectrum of activity, including dermatophytes, various filamentous and dematiaceous fungi, yeasts and dimorphic fungi. Its activity is fungicidal for most species [451, 984, 1818]. It penetrates into the nail rapidly and achieves concentrations higher than the MICs obtained for most of the fungi causing onychomycosis. [1002, 1817, 2246]. Its clearance is slow following topical application [1962]. Amorolfine has been ineffective when administered orally to animals with systemic fungal infections. This lack of activity may be due to protein binding and/or rapid metabolism of the drug [1818, 1890].
Amorolfine has 5% nail lacquer formulation. It is being manufactured by Roche Laboratories and its trade name is Loceryl™.
The most significant advantage of nail lacquer formulation is that it builds a non-water soluble film on the nail plate which remains at the application site for a week. This film acts as a depot for the drug [1809]. Cream, vaginal tablet and spray formulations of amorolfine were once available but no longer appear to be manufactured.
Amorolfine blocks delta 14 reduction and delta 7-8 isomerisation, resulting in depletion of ergosterol and accumulation of ignosterol in fungal cytoplasmic membrane. Fungal cell wall becomes thicker and chitin deposits are formed inside and ouside the cell wall [1818].
Amorolfine exerts fungicidal activity on dermatophytes. It is also active against other filamentous fungi that cause onychomycosis, such as Scytalidium spp. and Scopulariopsis spp. [451]. It yields relatively low MICs also for various dematiaceous fungi [1682]. Its in vitro spectrum appears broad when tested against various fungi [541]. However, in vitro susceptibility testing parameters for amorolfine remain yet variable, due to the lack of a standard methodology for testing dermatophytes and data reported so far are limited [541].
For amorolfine MICs, see susceptibility patterns and the susceptibility database.
Amorolfine 5% nail lacquer is applied once or twice weekly for up to 6 months in onychomycosis [1302, 1890].
In various superficial dermatomycoses, amorolfine cream has previously been used once daily on the infected area for up to 6 weeks [984].
Topical amorolfine is well-tolerated and minor local adverse reactions are observed rarely. Burning sensation, dryness of skin, scaling, itching, erythema and weeping have been reported [553, 984, 1651, 1652].
Amorolfine is available for topical administration in 5% nail lacquer formulation.
The most significant indication for amorolfine treatment is mild onychomycosis without nail matrix involvement [613]. While amorolfine achieves clinical cure in around 40 to 55% of patients with mild onychomycosis, those with severe onychomycosis involving the nail bed require systemic treatment [984, 1005].
Amorolfine appeared effective also in treatment of various superficial dermatomycosis [553, 554, 984, 1652]. Its activity in dermatomycosis appeared similar to that of topical bifonazole in terms of clinical and mycological cure rates [551]. Also, single dose treatment of vulvovaginal candidiasis with 50 mg or 100 mg of amorolfine vaginal tablets yielded favorable activity, except in cases due to Candida glabrata [557]. However, cream and vaginal tablet formulations of amorolfine are not available anymore.
The role of topical amorolfine in combination with a systemic antifungal agent has not been fully defined. However, amorolfine appears synergistic with ketoconazole, griseofulvin, and terbinafine in vitro. Moreover, in a murine model of dermatophytosis, amorolfine combined with griseofulvin, terbinafine, itraconazole or fluconazole appeared more active than monotherapy with any of the agents [1816].
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References
451. Clayton, Y. M. 1994. Relevance of broad-spectrum and fungicidal activity of antifungals in the treatment of dermatomycoses. Br J Dermatol. 130 (Suppl 43):7-8.
541. de Vroey, C., P. Desmet, Z. Q. Li, P. Mukamurangwa, and C. Raes-Wuytack. 1996. Further studies on the in vitro antifungal activity of amorolfine. Mycoses. 39:41-44.
551. del Palacio-Hernanz, A., S. Lopez-Gomez, P. Moreno-Palancar, and F. Gonzalez-Lastra. 1989. A clinical double-blind trial comparing amorolfine cream 0.5% (RO-14-4767) with bifonazole cream 1% in the treatment of dermatomycosis. Clin Exp Dermatol. 14:141-144.
553. del Palacio, A., L. Gip, A. Bergstraesser, and M. Zaug. 1992. Dose-finding study of amorolfine cream (0.125%, 0.25%, 0.5%) in the treatment of dermatomycoses. Clin Exp Dermatol. 17 (Suppl 1):50-55.
554. del Palacio, A., S. Lopez-Gomez, M. Garcia-Bravo, S. Cuetara, L. Iglesias-Diez, and A. Rodriguez-Noriega. 1992. Experience with amorolfine in the treatment of dermatomycoses. Dermatology. 184 (Suppl 1):25-29.
557. del Palacio, A., F. Sanz, M. Garcia-Bravo, C. Gimeno, S. Cuetara, P. Miranda, and A. R-Noriega. 1991. Single dose treatment of vaginal candidosis: randomized comparison of amorolfine (50 mg and 100 mg) and clotrimazole (500 mg) in patients with vulvovaginal candidosis. Mycoses. 34:85-91.
613. Downs, A. M. R., J. T. Lear, and C. B. Archer. 1999. Scytalidium hyalinum onychomycosis succesfully treated with 5% amorolfine nail lacquer. Br. J. Dermatol. 140:555.
984. Haria, M., and H. M. Bryson. 1995. Amorolfine: a review of its pharmocological properties and therapeutic potential in the treatment of onychomycosis and other superficial fungal infections. Drugs. 49:103-120.
1002. Hay, R. J. 1994. Antifungal drugs on the horizon. J Am Acad Dermatol. 31 (3 pt 2):S82-S86.
1005. Hay, R. J. 1992. Treatment of dermatomycoses and onychomycoses- - state of the art. Clin Exp Dermatol. 17 (Suppl 1):2-5.
1302. Lauharanta, J. 1992. Comparative efficacy and safety of amorolfine nail lacquer 2% versus 5% once weekly. Clin Exp Dermatol. 17 (Suppl 1):41-43.
1651. Nolting, S., D. Reinel, G. Semig, R. Reckers-Czaschka, M. Bergstraesser, and M. Zaug. 1993. Amorolfine spary in the treatment of foot mycoses (a dose-finding study). Br J Dermatol. 129:170-174.
1652. Nolting, S., G. Semig, H. K. Friedrich, M. Dietz, R. Reckers-Czaschka, M. Bergstraesser, and M. Zaug. 1992. Double-blind comparison of amorolfine and bifonazole in the treatment of dermatomycoses. Clin Exp Dermatol. 17 (Suppl 1):56-60.
1682. Okeke, C. N., and H. C. Gugnani. 1987. In vitro sensitivity of environmental isolates of pathogenic dematiaceous fungi to aqzole compounds and a phenylpropyl-morpholine derivative. Mycopathologia. 99:175-181.
1809. Pittrof, F., J. Gerhards, W. Erni, and G. Klecak. 1992. Loceryl nail lacquer --realization of a new galenical approach to onychomycosis therapy. Clin Exp Dermatol. 17 (Suppl 1):26-28.
1816. Polak, A. 1993. Combination of amorolfine with various antifungal drugs in dermatophytosis. Mycoses. 36:43-49.
1817. Polak, A. 1993. Kinetics of amorolfine in human nails. Mycoses. 36:101-103.
1818. Polak, A. 1992. Preclinical data and mode of action of amorolfine. Dermatology. 184 (Suppl 1):3-7.
1890. Reinel, D., and C. Clarke. 1992. Comparative efficacy and safety of amorolfine nail lacquer 5% in onychomycosis, once-weekly versus twice-weekly. Clin Exp Dermatol. 17 (Suppl 1):44-49.
1962. Roncari, G., C. Ponelle, R. Zumbrunnen, A. Guenzi, J. Dingemanse, and J. H. Jonkman. 1992. Percutaneous absorption of amorolfine following a single topical application of an amorolfine cream formulation. Clin Exp Dermatol. 17 (Suppl 1):33-36.
2246. Torres-Rodriguez, J. M. 1993. New topical antifungal drugs. Arch Med Res. 24:371-375.
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