Subacute toxicity and maximum tolerable dose of sertaconazole in repeated administration studies.
28-Day oral and dermal subacute toxicity studies of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl) ethoxy-methyl] benzo [b] thiophene (sertaconazole, FI-7045, CAS 99592-32-2), were carried out. The oral studies included the evaluation of subacute toxicity in rat (dose levels of 50, 150 and 300 mg/kg) and maximum tolerable dose in repeated administration in ferrets (consecutive dose levels in accordance with a geometric progression of 50, 75, 112.5, 168 and 250 mg/kg), which were the animal species intended for chronic toxicity studies. The dermal studies included the evaluation of subacute toxicity in rats and rabbits (1 ml/kg of a 2% cream). The results, in general, have shown low toxic effects, which can be summarized as a slight non-significant hepatomegalia in the rat with increased gamma-GTP and alkaline phosphatase values and a high urinary pH value; no histopathological changes were observed. These effects are characteristic of azole derivatives and are therefore common to other antifungals with this chemical group.
Romero
A
A
Research Centre, Ferrer Group, Barcelona, Spain.
Villamayor
F
F
Grau
M T
MT
Sacristán
A
A
Ortíz
J A
JA
D000284:Administration, Oral; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000633:toxicity*; D004435:Eating / Q000187:drug effects; D005260:Female; D005289:Ferrets; D006160:Guanosine Triphosphate / Q000494:pharmacology; D007093:Imidazoles / Q000008:administration & dosage / Q000633:toxicity*; D007271:Injections, Intradermal; D008099:Liver / Q000187:drug effects; D008297:Male; D009929:Organ Size / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012737:Sex Factors; D013876:Thiophenes / Q000008:administration & dosage / Q000633:toxicity*
D000935:Antifungal Agents; D007093:Imidazoles; D013876:Thiophenes; C061131:sertaconazole; D006160:Guanosine Triphosphate