Source: Health Products Regulatory Authority (ZA) Revision Year: 2017 Publisher: PHARMACARE LIMITED, Healthcare Park, Woodlands Drive, Woodmead 2191
A 1.2 Psychoanaleptics (antidepressants)
Amitriptyline is a tricyclic antidepressant that inhibits the membrane pump mechanism responsible for re-uptake of noradrenaline into adrenergic neurons. This interference with reuptake of noradrenaline is believed to result in the antidepressant activity of amitriptyline. The precise mechanism of action in man has not been confirmed.
After oral intake, peak plasma concentrations occur within about 6 hours of oral administration.
Amitriptyline and nortriptyline are widely distributed throughout the body and are highly bound to plasma and tissue protein. The estimated half-life of amitriptyline is 9 to 25 hours. It crosses the placental barrier and is excreted in breast milk.
Amitriptyline is extensively demethylated in the liver to its primary active metabolite, nortriptyline. The metabolism pathway includes N-oxidation and conjugation with glucuronic acid.
It is excreted in urine in the form of metabolites.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.
