[Metabolism of o,p'-DDD (mitotane) in human and animals. Actual notions and practical deductions (author's transl)].
The metabolism of o,p'-DDD (mitotane), a well-known inhibitor of adrenal steroidogenesis in man and animal, is reviewed. Following oral administration, about 65% of the ingested drug were found to pass in the stool. The drug appeared in the urine in metabolized forms: o,p'-DDA and mono-and dihydroxylated derivatives of o.p'-DDA. These latters were found as well in the stools. An unsaturated metabolite, o,p'-DDE was described in plasma and tissues in man. Serum specimens of treated patients were analyzed for o,p'-DDD during various phases of therapy: the levels and the rate of rise during treatment were very variable (5 to 90 microng/ml). Tissue levels were obtained from animals (rats, dogs) or men (biopsy as well as autopsy): o,p'-DDD was primarily found stored in adipose tissue and fat-containing tissues, essentially adrenals. Practical conclusions can be drawn from these results: there is no correlation between the dose of o,p'-DDD administered and its blood level; there is no correlation between blood levels and the patient's responsiveness to the drug; there is a possibility that the molecule transformed in an active metabolite through its metabolism.
D000818:Animals; D003634:DDT / Q000378:metabolism; D003633:Dichlorodiphenyl Dichloroethylene / Q000378:metabolism; D003632:Dichlorodiphenyldichloroethane / Q000378:metabolism; D005243:Feces / Q000032:analysis; D006801:Humans; D007536:Isomerism; D008939:Mitotane / Q000097:blood / Q000378:metabolism*; D013045:Species Specificity; D013329:Structure-Activity Relationship
D003633:Dichlorodiphenyl Dichloroethylene; D008939:Mitotane; D003634:DDT; D003632:Dichlorodiphenyldichloroethane
Métabolisme de l'o,p'-DDD (mitotane) chez l'homme et l'animal. Données actuelles et déductions pratiques