Source: Health Products Regulatory Authority (ZA) Revision Year: 2022 Publisher: Strides Pharma SA (Pty) Ltd, 106 16th Road, Building 2, Midrand
Category and Class: A 1.2 Psychoanaleptics (antidepressants). Pharmacotherapeutic group: Antidepressants – Non-selective monoamine reuptake inhibitor (tricyclic antidepressant)
ATC code: N06AA09
Amitriptyline is a tricyclic antidepressant. It has marked anticholinergic and sedative properties. It prevents the re-uptake, and hence the inactivation of noradrenaline and serotonin at nerve terminals. Re-uptake prevention of these monoamine neurotransmitters potentiate their action in the brain. This appears to be associated with the antidepressant activity.
Amitriptyline is absorbed after oral administration, reaching its maximum plasma concentration approximately 6 hours after administration.
Amitriptyline and nortriptyline are widely distributed throughout the body with a high binding to plasma proteins and tissues. An elimination half-life ranging from 9-25 hours has been estimated.
Amitriptyline and nortriptyline pass across the placental barrier. In nursing mothers, amitriptyline and nortriptyline, are excreted in the 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.
Amitriptyline is excreted as glucuronide or conjugate sulfate metabolites and little medicine appears unchanged in the urine.
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