Effects of butenafine hydrochloride, a new benzylamine derivative, on experimental dermatophytosis in guinea pigs.
Butenafine hydrochloride, N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethylamine hydrochloride (butenafine), is a novel antifungal agent of the class of benzylamine derivatives. Butenafine was investigated for its activity against guinea pig dermatophytosis caused by Trichophyton mentagrophytes or Microsporum canis in comparison with those of naftifine, tolnaftate, clotrimazole, and bifonazole. Topical butenafine showed excellent efficacy against dermatophytosis when it was applied once daily, and the effect was superior to those of all four reference drugs. When applied once at 24 or 48 h before infection, the drug exhibited excellent prophylactic efficacy against experimental T. mentagrophytes infection. The concentrations of butenafine in animal skin at 24 and 48 h after application of 0.2 ml of a 1% solution were several hundred times higher than those required to kill T. mentagrophytes and M. canis. The good efficacy of butenafine against dermatophytosis may be attributable to its fungicidal activity and long retention in the skin after topical application.
Arika
T
T
Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Tokyo, Japan.
Yokoo
M
M
Hase
T
T
Maeda
T
T
Amemiya
K
K
Yamaguchi
H
H
D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D001596:Benzylamines / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D003881:Dermatomycoses / Q000188:drug therapy* / Q000382:microbiology / Q000517:prevention & control; D008401:Gas Chromatography-Mass Spectrometry; D006168:Guinea Pigs; D008297:Male; D008826:Microbial Sensitivity Tests; D008864:Microsporum / Q000187:drug effects; D009281:Naphthalenes / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D012867:Skin / Q000737:chemistry; D014249:Trichophyton / Q000187:drug effects
D000935:Antifungal Agents; D001596:Benzylamines; D009281:Naphthalenes; C067594:butenafine