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Metabolism of Aminoglutethimide in Humans: Quantification and Clinical Relevance of Induced Metabolism

Metabolism of Aminoglutethimide in Humans: Quantification and Clinical Relevance of Induced Metabolism

P E Goss, M Jarman, L J Griggs

Br J Cancer. 1985 Feb;51(2):259-62.

PMID: 3838134

Abstract:

Hydroxylaminoglutethimide [3-ethyl-3-(4-hydroxylaminophenyl)piperidine-2,6-dione] (HxAG), aminoglutethimide [3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione] (AG) and N-acetyl-aminoglutethimide (N-AcAG) have been quantified by high performance liquid chromatography using m-aminoglutethimide (metaAG) as the internal standard in serial 24 h urine collections from a patient on chronic AG therapy without steroid supplementation. HxAG is the product of a major AG-induced metabolic pathway since the ratio [HxAG]/[AG] rises with time. In contrast the ratio [N-AcAG]/[AG] decreases with time. A rapid, simple colorimetric assay has been used to quantify HxAG in urine from both male and female patients receiving a range of doses of AG and to show that induced metabolism is a general phenomenon even at low doses (125 mg twice daily). AG therapy is known to alter the metabolic rate and plasma half-life of a number of coadministered compounds including dexamethasone and warfarin. Clinicians should remain alerted to this phenomenon.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP83417112	m-Aminoglutethimide		83417-11-2	Price

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