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[[File:Butriptyline.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]</div> | [[File:Butriptyline.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]</div> | ||
__NOTOC__ | __NOTOC__ | ||
{{SI}} | {{SI}} | ||
{{CMG}} | {{CMG}} | ||
==Overview== | ==Overview== | ||
'''Butriptyline''' ('''Evadene''', '''Evadyne''', '''Evasidol''', '''Centrolese''') is a [[tricyclic antidepressant]] (TCA) which has been used in [[Europe]] since 1974.<ref name="isbn3-527-31058-4">{{cite book | author = José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens | title = Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application | publisher = Wiley-VCH | location = Weinheim | year = 2007 | page = 180 | isbn = 3-527-31058-4 | oclc = | doi = | url = http://books.google.com/books?id=yXD4QA-Y_Z0C&lpg=PA180&dq=butriptyline&as_brr=3&pg=PA180#v=onepage&q=&f=false}}</ref><ref name="isbn3-88763-075-0">{{cite book | author = Swiss Pharmaceutical Society | title = Index Nominum 2000: International Drug Directory (Book with CD-ROM) | publisher = Medpharm Scientific Publishers | location = Boca Raton | year = 2000 | pages = | isbn = 3-88763-075-0 | oclc = | doi = | url = http://books.google.com/books?id=5GpcTQD_L2oC&lpg=PA1205&pg=PA154#v=onepage&q=&f=false}}</ref><ref name="isbn0-8155-1144-2">{{cite book | author = Sittig, Marshall | title = Pharmaceutical manufacturing encyclopedia | publisher = Noyes Publications | location = Park Ridge, N.J., U.S.A | year = 1988 | page = 213 | isbn = 0-8155-1144-2 | oclc = | doi = | url = http://books.google.com/books?id=X2EyLsG4bcUC&lpg=PA213&dq=butriptyline&as_brr=3&pg=PA213#v=onepage&q=&f=false}}</ref><ref name="isbn0-412-54090-8">{{cite book | author = | title = Dictionary of organic compounds | publisher = Chapman & Hall | location = London | year = 1996 | page = 1157 | isbn = 0-412-54090-8 | oclc = | doi = | url = http://books.google.com/books?id=zNZfxR-CsYcC&lpg=PA1157&dq=butriptyline&lr=&as_brr=3&pg=PA1157#v=onepage&q=&f=false}}</ref><ref name="isbn0-89862-674-9">{{cite book | author = Paykel, Eugene S. | title = Handbook of affective disorders | publisher = Guilford Press | location = New York | year = 1992 | page = 339 | isbn = 0-89862-674-9 | oclc = | doi = | url = http://books.google.com/books?id=r003DuAeZhIC&lpg=PA339&dq=butriptyline&lr=&as_brr=3&pg=PA339#v=onepage&q=&f=false}}</ref> It is the [[isobutyl]] [[side chain]] [[homology (chemistry)|homologue]] of [[amitriptyline]] and produces similar effects to it, but with less marked [[side effect]]s like [[sedation]] and [[drug interaction|interactions]] with [[adrenergic]] drugs.<ref name="isbn3-527-31058-4"/><ref name="isbn0-89862-674-9"/><ref name="isbn0-444-53266-8">{{cite book | author = Aronson, Jeffrey Kenneth | title = Meyler's Side Effects of Psychiatric Drugs (Meylers Side Effects) | publisher = Elsevier Science | location = Amsterdam | year = 2008 | pages = | isbn = 0-444-53266-8 | oclc = | doi = | url = http://books.google.com/books?id=s0XYvuPVgaAC&lpg=PA31&pg=PA31#v=onepage&q=&f=false}}</ref> | '''Butriptyline''' ('''Evadene''', '''Evadyne''', '''Evasidol''', '''Centrolese''') is a [[tricyclic antidepressant]] (TCA) which has been used in [[Europe]] since 1974.<ref name="isbn3-527-31058-4">{{cite book | author = José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens | title = Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application | publisher = Wiley-VCH | location = Weinheim | year = 2007 | page = 180 | isbn = 3-527-31058-4 | oclc = | doi = | url = http://books.google.com/books?id=yXD4QA-Y_Z0C&lpg=PA180&dq=butriptyline&as_brr=3&pg=PA180#v=onepage&q=&f=false}}</ref><ref name="isbn3-88763-075-0">{{cite book | author = Swiss Pharmaceutical Society | title = Index Nominum 2000: International Drug Directory (Book with CD-ROM) | publisher = Medpharm Scientific Publishers | location = Boca Raton | year = 2000 | pages = | isbn = 3-88763-075-0 | oclc = | doi = | url = http://books.google.com/books?id=5GpcTQD_L2oC&lpg=PA1205&pg=PA154#v=onepage&q=&f=false}}</ref><ref name="isbn0-8155-1144-2">{{cite book | author = Sittig, Marshall | title = Pharmaceutical manufacturing encyclopedia | publisher = Noyes Publications | location = Park Ridge, N.J., U.S.A | year = 1988 | page = 213 | isbn = 0-8155-1144-2 | oclc = | doi = | url = http://books.google.com/books?id=X2EyLsG4bcUC&lpg=PA213&dq=butriptyline&as_brr=3&pg=PA213#v=onepage&q=&f=false}}</ref><ref name="isbn0-412-54090-8">{{cite book | author = | title = Dictionary of organic compounds | publisher = Chapman & Hall | location = London | year = 1996 | page = 1157 | isbn = 0-412-54090-8 | oclc = | doi = | url = http://books.google.com/books?id=zNZfxR-CsYcC&lpg=PA1157&dq=butriptyline&lr=&as_brr=3&pg=PA1157#v=onepage&q=&f=false}}</ref><ref name="isbn0-89862-674-9">{{cite book | author = Paykel, Eugene S. | title = Handbook of affective disorders | publisher = Guilford Press | location = New York | year = 1992 | page = 339 | isbn = 0-89862-674-9 | oclc = | doi = | url = http://books.google.com/books?id=r003DuAeZhIC&lpg=PA339&dq=butriptyline&lr=&as_brr=3&pg=PA339#v=onepage&q=&f=false}}</ref> It is the [[isobutyl]] [[side chain]] [[homology (chemistry)|homologue]] of [[amitriptyline]] and produces similar effects to it, but with less marked [[side effect]]s like [[sedation]] and [[drug interaction|interactions]] with [[adrenergic]] drugs.<ref name="isbn3-527-31058-4"/><ref name="isbn0-89862-674-9"/><ref name="isbn0-444-53266-8">{{cite book | author = Aronson, Jeffrey Kenneth | title = Meyler's Side Effects of Psychiatric Drugs (Meylers Side Effects) | publisher = Elsevier Science | location = Amsterdam | year = 2008 | pages = | isbn = 0-444-53266-8 | oclc = | doi = | url = http://books.google.com/books?id=s0XYvuPVgaAC&lpg=PA31&pg=PA31#v=onepage&q=&f=false}}</ref> | ||
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{{Antidepressants}} | {{Antidepressants}} | ||
[[Category:Tricyclic antidepressants]] | [[Category:Tricyclic antidepressants]] | ||
[[Category:Drug]] | [[Category:Drug]] | ||
Latest revision as of 18:27, 18 August 2015
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
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
- ↑ 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.
- ↑ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 3-88763-075-0.
- ↑ Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. p. 213. ISBN 0-8155-1144-2.
- ↑ Dictionary of organic compounds. London: Chapman & Hall. 1996. p. 1157. ISBN 0-412-54090-8.
- ↑ 5.0 5.1 Paykel, Eugene S. (1992). Handbook of affective disorders. New York: Guilford Press. p. 339. ISBN 0-89862-674-9.
- ↑ Aronson, Jeffrey Kenneth (2008). Meyler's Side Effects of Psychiatric Drugs (Meylers Side Effects). Amsterdam: Elsevier Science. ISBN 0-444-53266-8.
- ↑ 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.
- ↑ 8.0 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.
- ↑ 9.0 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.