Elimination and pharmacological effects following single oral doses of 50 and 75 mg of amitriptyline in man.

In a companion paper we described the disposition of a 75 mg single dose of amitriptyline in normal volunteers who were phenotyped as extensive or poor metabolizers of debrisoquine and bufuralol, and had a four-fold range in the oral clearance of the antidepressant, 50 mg of amitriptyline was also administered to the same volunteers. This paper compares the results after both doses and suggests that the disposition of amitriptyline is linear even in subjects with a low oral clearance. There was no relation between the pharmacokinetic data and the intensity of sedation or of psychomotor impairment.