Antithyroid action of ketoconazole: in-vitro studies and rat in-vivo studies.
Inspection of the chemical structure of ketoconazole indicates that it may have antithyroid activity. The antithyroid action of this drug was demonstrated in-vitro and in-vivo. In-vitro, it was found to form a complex with iodine (formation constant Kc 141 L mol-1), and to inhibit lactoperoxidase (IC50 2 x 10(-4) M). Its effects in-vivo in the rat were assessed by assay of circulating-thyroxine, and from the histological appearance of the thyroid gland. Thyroid gland weight was increased in rats treated with ketoconazole.
Comby
F
F
Laboratoire de Chimie Thérapeutique et Chimie Organique, Faculté de Pharmacie, Limoges, France.
Lagorce
J F
JF
Buxeraud
J
J
Raby
C
C
D000818:Animals; D013956:Antithyroid Agents / Q000494:pharmacology*; D066298:In Vitro Techniques; D007455:Iodine / Q000737:chemistry; D007654:Ketoconazole / Q000737:chemistry / Q000494:pharmacology*; D007784:Lactoperoxidase / Q000037:antagonists & inhibitors; D008297:Male; D008713:Methimazole / Q000494:pharmacology; D008954:Models, Biological; D009929:Organ Size / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D013961:Thyroid Gland / Q000187:drug effects*; D015430:Weight Gain / Q000187:drug effects
D013956:Antithyroid Agents; D008713:Methimazole; D007455:Iodine; D007784:Lactoperoxidase; D007654:Ketoconazole