Abstract
A major pathway for the metabolism in man of the muscle relaxant and uricosuric drug, zoxazolamine, is via hydroxylation in the benzene ring to form 6-hydroxy-zoxazolamine which is excreted in urine as a glucuronide. Evidence is also presented for the excretion in urine of small amounts of a product (chlorzoxazone) formed by the substitution of the amino group of zoxazolamine for a hydroxyl group. 6-Hydroxy-zoxazolamine has little or no muscle relaxant properties whereas chlorzoxazone has muscle relaxant properties similar to those of zoxazolamine. Neither 6-hydroxy-zoxazolamine nor chlorzoxazone possesses uricosuric activity in gouty subjects.
The in vitro metabolism of zoxazolamine by TPN fortified liver homogenates has been described. It was found that the administration of 3,4-benzpyrene to rats markedly stimulates the activity of the enzyme system in liver which metabolizes zoxazolamine.
Footnotes
- Received September 11, 1959.
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