Amitriptyline, sold under the brand name Elavil among others, is a tricyclic antidepressant primarily used to treat cyclic vomiting syndrome, major depressive disorder and a variety of pain syndromes from neuropathic pain to fibromyalgia to migraine and tension headaches.
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Amitriptyline was discovered in the late 1950s by scientists at Merck and approved by the US Food and Drug Administration in 1961.
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Amitriptyline is effective for depression, but it is rarely used as a first-line antidepressant due to its higher toxicity in overdose and generally poorer tolerability.
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Amitriptyline is probably effective for the prevention of periodic migraine in adults.
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Amitriptyline is similar in efficacy to venlafaxine and topiramate but carries a higher burden of adverse effects than topiramate.
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Amitriptyline is not significantly different from placebo when used for the prevention of migraine in children.
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Amitriptyline is effective for the treatment of irritable bowel syndrome; however, because of its side effects, it should be reserved for select patients for whom other agents do not work.
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Amitriptyline can be used in the treatment of nocturnal enuresis in children.
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Amitriptyline should be used with caution in patients with epilepsy, impaired liver function, pheochromocytoma, urinary retention, prostate enlargement, hyperthyroidism, and pyloric stenosis.
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Amitriptyline can be used during pregnancy and lactation, in the cases when SSRI do not work.
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Amitriptyline is a non-selective blocker of multiple ion channels, in particular, voltage-gated sodium channels Nav1.
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Amitriptyline is metabolized mostly by CYP2C19 into nortriptyline and by CYP2D6 leading to a variety of hydroxylated metabolites, with the principal one among them being-10-hydroxynortriptyline, and to a lesser degree, by CYP3A4.
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Amitriptyline is prepared by reacting dibenzosuberone with 3propylmagnesium chloride and then heating the resulting intermediate product with hydrochloric acid to eliminate water.
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Amitriptyline was first developed by the American pharmaceutical company Merck in the late 1950s.
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Amitriptyline is the English and French generic name of the drug and its INN, BAN, and DCF, while amitriptyline hydrochloride is its USAN, USP, BANM, and JAN.
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