Inactivity of terbinafine in a rat model of pulmonary aspergillosis.
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.
Schmitt
H J
HJ
Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, New York.
Andrade
J
J
Edwards
F
F
Niki
Y
Y
Bernard
E
E
Armstrong
D
D
D000336:Aerosols; D000666:Amphotericin B / Q000627:therapeutic use; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001228:Aspergillosis / Q000188:drug therapy*; D001231:Aspergillus flavus / Q000187:drug effects; D001232:Aspergillus fumigatus / Q000187:drug effects; D001234:Aspergillus niger / Q000187:drug effects; D001682:Biological Availability; D004195:Disease Models, Animal; D008168:Lung / Q000378:metabolism; D008172:Lung Diseases, Fungal / Q000188:drug therapy*; D008297:Male; D009281:Naphthalenes / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051381:Rats; D011919:Rats, Inbred Strains; D000077291:Terbinafine
D000336:Aerosols; D000935:Antifungal Agents; D009281:Naphthalenes; D000666:Amphotericin B; D000077291:Terbinafine