Glucuronidation of Amitriptyline in Manin Vivo

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Abstract
The urinary excretion of amitriptyline (AT) as N‐glucuronide was studied in healthy volunteers after single oral doses of AT and in patients on continuous treatment with AT. In the volunteers, 8±3% of a 25 mg dose of AT was recovered in urine as glucuronide during 108 hr. No difference between slow and rapid debrisoquine hydroxylators with respect to the excretion of AT glucuronide was seen. 0.08 to 1.68% of the given AT dose was recovered in urine in unchanged form. The excretion of unchanged AT correlated with the debrisoquine metabolic ratio (rg=0.61; pin vivoboth after single low doses and during continuous treatment with therapeutic doses.

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