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Reliable, easy-to-read patient information on common medical conditions — written in plain language, free of jargon, and grounded in current evidence. Browse the most frequent diagnoses, understand what they mean for everyday life, and learn which steps and questions help you have a focused conversation with your doctor.

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Butriptyline

Introduction

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Overview

Overview

Butriptyline (Evadene, Evadyne, Evasidol, Centrolese) is a tricyclic antidepressant (TCA) which has been used in Europe since 1974.[1][2][3][4][5] It is the isobutyl side chain homologue of amitriptyline and produces similar effects to it, but with less marked side effects like sedation and interactions with adrenergic drugs.[1][5][6]

In vitro, butriptyline is a strong antihistamine and anticholinergic, moderate 5-HT2 and α1-adrenergic receptor antagonist, and weak serotonin reuptake inhibitor, with negligible affinity for the norepinephrine and dopamine transporters.[7][8][9] These actions appear to confer a profile similar to that of iprindole and trimipramine with serotonin-blocking effects as the predominant mediator of mood-lifting efficacy.[10][11][12]

However, in clinical trials, using similar doses, butriptyline was found to be even more effective than amitriptyline as an antidepressant, despite the fact that amitriptyline is much, much stronger as both a 5-HT2 antagonist and serotonin-norepinephrine reuptake inhibitor.[7][8][9][13] As a result, it may be that butriptyline, in vivo, functions as a prodrug to a metabolite with more appreciable pharmacodynamics.

References

References

  1. ↑ 1.0 1.1 José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. p. 180. ISBN 3-527-31058-4.
  2. ↑ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 3-88763-075-0.
  3. ↑ Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. p. 213. ISBN 0-8155-1144-2.
  4. ↑ Dictionary of organic compounds. London: Chapman & Hall. 1996. p. 1157. ISBN 0-412-54090-8.
  5. ↑ 5.0 5.1 Paykel, Eugene S. (1992). Handbook of affective disorders. New York: Guilford Press. p. 339. ISBN 0-89862-674-9.
  6. ↑ Aronson, Jeffrey Kenneth (2008). Meyler’s Side Effects of Psychiatric Drugs (Meylers Side Effects). Amsterdam: Elsevier Science. ISBN 0-444-53266-8.
  7. ↑ 7.0 7.1 Richelson E, Nelson A (July 1984). “Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro”. The Journal of Pharmacology and Experimental Therapeutics. 230 (1): 94–102. PMID 6086881.
  8. ↑ 8.0 8.1 Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). “Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro”. European Journal of Pharmacology. 132 (2–3): 115–21. doi:10.1016/0014-2999(86)90596-0. PMID 3816971.
  9. ↑ 9.0 9.1 Tatsumi M, Groshan K, Blakely RD, Richelson E (December 1997). “Pharmacological profile of antidepressants and related compounds at human monoamine transporters”. European Journal of Pharmacology. 340 (2–3): 249–58. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821.
  10. ↑ Jaramillo J, Greenberg R (February 1975). “Comparative pharmacological studies on butriptyline and some related standard tricyclic antidepressants”. Canadian Journal of Physiology and Pharmacology. 53 (1): 104–12. doi:10.1139/y75-014. PMID 166748.
  11. ↑ Randrup A, Braestrup C (August 1977). “Uptake inhibition of biogenic amines by newer antidepressant drugs: relevance to the dopamine hypothesis of depression”. Psychopharmacology. 53 (3): 309–14. doi:10.1007/BF00492370. PMID 408861.
  12. ↑ Richelson E, Pfenning M (September 1984). “Blockade by antidepressants and related compounds of biogenic amine uptake into rat brain synaptosomes: most antidepressants selectively block norepinephrine uptake”. European Journal of Pharmacology. 104 (3–4): 277–86. doi:10.1016/0014-2999(84)90403-5. PMID 6499924.
  13. ↑ Guelfi JD, Dreyfus JF, Delcros M, Pichot P (1983). “A double-blind controlled multicenter trial comparing butriptyline with amitriptyline”. Neuropsychobiology. 9 (2–3): 142–6. doi:10.1159/000117952. PMID 6353270.

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]