Abstract
In a model of bronchopulmonary aspergillosis terbinafine did not improve survival of experimental animals in doses up to 80 mg/kg/day despite adequate lung concentrations. Pretreatment and aerosolization of the compound were also ineffective. Terbinafine was markedly less active in vitro when serum was used instead of Yeast-Nitrogen-Glucose-broth. It is concluded that a lack of bioavailability in the presence of serum may explain the lack of activity of terbinafine in experimental aspergillosis.
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Stütz A, Petranyi G: Synthesis and antifungal activity of (E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1 naphthalene-methanamine (SF 86-327) and related allylamine derivatives with enhanced oral activity. Journal of Medical Chemistry 1984, 27: 1539–1543.
Ryder NS: Specific inhibition of fungalsterol biosynthesis by SF 86-327, a new allylamine antimycotic agent. Antimicrobial Agents and Chemotherapy 1985, 27: 252–256.
Ryder NS, Dupont MC: Inhibition of squalene epoxidase by allylamine antimycotic compounds. A comparative study of the fungal and mammalian enzymes. Biochemistry Journal 1985, 230: 765–770.
Ryder NS, Seidl G, Troke PF: Effect of the antimycotic drug naftifine on growth of and sterol biosynthesis inCandida albicans. Antimicrobial Agents and Chemotherapy 1984, 25: 483–487.
Shadomy S, Espinel-Ingroff A, Gebhart RJ: In vitro studies with SF 86-327, a new orally active allylamine derivative. Sabouradia 1985, 23: 125–132.
Clayton YM: The in vitro activity of terbinafine against uncommon fungal pathogens. In: Fromtling RA (ed): Recent trends in the discovery, development and evaluation of antifungal agents. Prous Science Publishers, Barcelona, 1987, p 433–439.
Petranyi G, Meingassner JG, Mieth H: Antifungal activity of the allylamine derivative terbinafine in vitro. Antimicrobial Agents and Chemotherapy 1987, 31: 1365–1368.
Schmitt HJ, Bernard EM, Andrade J, Edwards F, Schmitt B, Armstrong D: MIC and fungicidal activity of terbinafine against clinical isolates ofAspergillus spp. Antimicrobial Agents and Chemotherapy 1988, 32: 780–781.
Meyer RD, Young LS, Armstrong D, Yu BS: Aspergillosis complicating neoplastic disease. American Journal of Medicine 1973, 54: 6–15.
Karp JE, Burch PA, Merz WG: An approach to intensive antileukemia therapy in patients with previous invasive aspergillosis. American Journal of Medicine 1988, 85: 203–206.
Schmitt HJ, Bernard EM, Häuser M, Armstrong D: Aerosol amphotericin B is effective for prophylaxis and therapy in a rat model of pulmonary aspergillosis. Antimicrobial Agents and Chemotherapy 1988, 32: 1676–1679.
Häuser M, Schmitt HJ, Bernard EM, Armstrong D: A new bioassay for terbinafine. European Journal of Clinical Microbiology and Infectious Diseases 1988, 7: 531–533.
Petrany G, Stütz A, Ryder NS, Meingassner JG, Mieth H: Experimental antimycotic activity of naftifine and terbinafine. In: Fromtling RA (ed): Recent trends in the discovery, development and evaluation of antifungal agents. Prous Science Publishers, Barcelona, Spain 1987, p. 441–450.
Petrany G, Meingassner JG, Mieth H: Activity of terbinafine in experimental fungal infections of laboratory animals. Antimicrobial Agents and Chemotherapy 1987, 31: 1558–1561.
Petrany G, Stütz A, Ganzinger U: SF86-327, a new antifungal allylamine derivative: preclinical and preliminary clinical data. In: Spitzy KH, Karrer K (ed): Proceedings of the 13th International Congress of Chemotherapy. Egermann, Vienna, 1983, p. 21–30.
Niki Y, Bernard M, Schmitt HJ, Tong WP, Edwards FF, Armstrong D: Pharmacokinetics of aerosol amphotericin B in Rats. Antimicrobial Agents and Chemotherapy 1990, 34: 29–32.
Stephan A, Czok R, Maly O: Terbinafine — initial clinical results. In: Fromtling RA (ed): Recent trends in the discovery, development and evaluation of antifungal agents. Prous Science Publishers Barcelona, 1987, p. 511–520.
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Schmitt, H.J., Andrade, J., Edwards, F. et al. Inactivity of terbinafine in a rat model of pulmonary aspergillosis. Eur. J. Clin. Microbiol. Infect. Dis. 9, 832–835 (1990). https://doi.org/10.1007/BF01967386
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DOI: https://doi.org/10.1007/BF01967386