Amitriptyline inhibits the re-uptake of noradrenaline at the noradrenergic nerve endings and the re-uptake of serotonin (5-hydroxy tryptamine) at the serotoninergic nerve endings in the central nervous system. These two effects are considered to be the likely base of the antidepressant effect of amitriptyline. The drug also has a strong anticholinergic effect and serves as an antagonist on a1 and H1 receptors.

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