Butenafine, a derivative of
benzylamine with potent fungicidal activity is a new generation of antimycotic compound that has shown to be extremely effective against experimentally-induced
tinea pedis in the guinea-pig, a situation that resembles synergetic pathology similar to that of
tinea pedis in humans.
Butenafine, (N-4-tert-butylbenzyl-N-methyl-1-naphthalenemethyl-amine hydrochloride) with a chemical structure and mode of action similar to those of the allylamines, demonstrates superior fungicidal activity in vitro against dermatophytes and superior fungistatic activity toward Candida albicans that of
naftifine and
terbinafine. In vitro, pharmacodynamic data has shown that the geometric mean of minimum inhibitory concentration values for
butenafine were comparatively lower than those of
naftifine and
clotrimazole against clinical isolates for many dermatophytes. It inhibits
sterol synthesis by blocking the
squalene epoxidation stage in fungi. In phramacokinetic assessments
butenafine achieves and maintains high concentrations and long retention time in skin, with associated anti-inflammatory activity in vivo. In controlled clinical trials when applied topically,
butenafine appears to be well tolerated with a subjective mild burning sensation at the application site. There were no withdrawals from the study.
Butenafine is sparingly soluble in water but readily soluble in
methanol,
ethanol,
dichloromethane and
chloroform. If incorporated properly in semisolid topical preparations, with a balanced vehicle,
butenafine hydrochloride potentially exhibits as a promising alternative antimycotic agent for the treatment of
tinea pedis.