Amitriptylinoxide Explained

Amitriptylinoxide (brand names Amioxid, Ambivalon, Equilibrin), or amitriptyline N-oxide, is a tricyclic antidepressant (TCA) which was introduced in Europe in the 1970s for the treatment of depression.[1]

Amitriptylinoxide is both an analogue and metabolite of amitriptyline, and has similar effects as well as equivalent efficacy as an antidepressant.[2] [3] [4] [5] However, it has a faster onset of action and fewer adverse effects, including reduced drowsiness, sedation, anticholinergic symptoms like dry mouth, sweating, and dizziness, orthostatic hypotension, and cardiotoxicity.[2] [3] [4] [5] [6] [7]

In receptor binding assays, amitriptylinoxide was found to have generally equivalent pharmacology to amitriptyline, acting as a serotonin and norepinephrine reuptake inhibitor, serotonin receptor antagonist, and H1 receptor antagonist, among other properties, but with approximately 60-fold lower affinity for the α1-adrenergic receptor, and the weakest affinity of any of the TCAs analyzed for the muscarinic acetylcholine receptors.[8] [9] [10]

Amitriptylinoxide has been said to be a prodrug of amitriptyline.[11]

See also

Notes and References

  1. Book: Swiss Pharmaceutical Society . Index Nominum 2000: International Drug Directory (Book with CD-ROM) . Medpharm Scientific Publishers . Boca Raton . 2000 . 49 . 3-88763-075-0 .
  2. Rapp W . Comparative trial of amitriptyline-N-oxide and amitriptyline in the treatment of out-patients with depressive syndromes . Acta Psychiatrica Scandinavica . 58 . 3 . 245–55 . September 1978 . 360779 . 10.1111/j.1600-0447.1978.tb06936.x. 12666498 .
  3. Tegeler J, Klieser E, Lehmann E, Heinrich K . Double-blind study of the therapeutic efficacy and tolerability of amitriptylinoxide in comparison with amitriptyline . Pharmacopsychiatry . 23 . 1 . 45–9 . January 1990 . 2179974. 10.1055/s-2007-1014481. 956047 .
  4. Godt HH, Fredslund-Andersen K, Edlund AH . [Amitriptyline N-oxide. A new antidepressant. A clinical double-blind trial in comparison with amitriptyline] . da . Nordisk Psykiatrisk Tidsskrift. Nordic Journal of Psychiatry . 25 . 3 . 237–46 . 1971 . 4945956 . 10.3109/08039487109094663.
  5. Book: Aronson, Jeffrey Kenneth . Meyler's Side Effects of Psychiatric Drugs (Meylers Side Effects) . Elsevier Science . Amsterdam . 2008 . 30 . 978-0-444-53266-4 .
  6. Wenzl H, Graf E, Sieck A . Central nervous effects of a new tricyclic antidepressant (amitriptylinoxide) . Arzneimittel-Forschung . 28 . 10b . 1874–9 . 1978 . 261811.
  7. Dencker SJ . [Clinical trial with imipramine-N-oxide and amitriptyline-N-oxide] . sv . Nordisk Psykiatrisk Tidsskrift. Nordic Journal of Psychiatry . 25 . 5 . 463–70 . 1971 . 4947298 . 10.3109/08039487109094696.
  8. Borbe HO, Zierenberg O . Amitriptylinoxide: receptor-binding profile compared with other antidepressant drugs . Pharmacopsychiatry . 18 . 5 . 314–9 . September 1985 . 2996040. 10.1055/s-2007-1017388. 31927039 .
  9. Maj J, Vetulani J, Michaluk J, Rogóz Z, Skuza G . Jerzy Vetulani . Central action of amitriptyline N-oxide . Pharmacopsychiatria . 15 . 6 . 187–91 . November 1982 . 6185962 . 10.1055/s-2007-1019536. 25823571 .
  10. Hyttel J, Christensen AV, Fjalland B . Neuropharmacological properties of amitriptyline, nortriptyline and their metabolites . Acta Pharmacologica et Toxicologica . 47 . 1 . 53–7 . July 1980 . 7395525 . 10.1111/j.1600-0773.1980.tb02025.x.
  11. Book: Pavel Anzenbacher. Ulrich M. Zanger. Metabolism of Drugs and Other Xenobiotics. 23 February 2012. John Wiley & Sons. 978-3-527-64632-6. 302–.

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