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Amitriptilien

chemiese verbinding

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Amitriptilien

Chemie
Chemiese formule C20H23N
IUPAC naam 3-(10,11-dihidro-5H-dibenso
[a,d]siklohepteen-5-ilideen)-
N,N-dimetielpropaan-1-amien
Molêre massa 277.411 g/mol
Smeltpunt 197.5 °C (387.5 °F)[1]
CAS-nommer 50-48-6
Farmakokinetika
Biobeskikbaarheid 45%[2]-53%[3]
Proteïengebonde 96%
Metabolisme Lewer (CYP2D6, CYP2C19,
CYP3A4)[4][3][5]
Metaboliete nortriptilien,
(E)-10-hidroksinortriptilien
Halfleeftyd 21 uur[2]
Uitskeiding Urine: 12–80% na 48 uur;[6]
fesies: nie ondersoek nie

Amitriptilien is 'n trisikliese antidepressant wat hoofsaaklik gebruik word vir die behandeling van ernstige depressiewe versteuring, 'n verskeidenheid pynsindrome soos neuropatiese pyn, fibromialgie, migraine en spanningshoofpyne.[7] As gevolg van die frekwensie en prominensie van newe-effekte, word amitriptilien oor die algemeen beskou as 'n tweede-lyn terapie vir hierdie aanduidings.[8][9][10][11]

Die mees algemene newe-effekte is 'n droë mond, lomerigheid, duiseligheid, hardlywigheid en massatoename. Van belang is seksuele disfunksie, wat hoofsaaklik by mans waargeneem word. Gloukoom, lewertoksisiteit en abnormale hartritmes is skaars maar ernstige newe-effekte. Bloedvlakke van amitriptilien verskil aansienlik van een persoon na 'n ander,[12] en amitriptilien is in wisselwerking met baie ander medikasie wat moontlik die newe-effekte daarvan kan vererger.

Amitriptilien is in die laat 1950's deur wetenskaplikes by Merck ontdek en in 1961 deur die Amerikaanse Voedsel- en geneesmiddeladministrasie (FDA) goedgekeur.[13] Dit is op die Wêreldgesondheidsorganisasie se lys van noodsaaklike medisyne.[14] Dit is beskikbaar as 'n generiese medikasie.[15] In 2020 was dit die 81ste mees voorgeskrewe medikasie in die Verenigde State, met meer as 9 miljoen voorskrifte.[16][17]

Mediese gebruike

wysig

Amitriptilien word aangedui vir die behandeling van ernstige depressiewe versteuring en neuropatiese pyn en vir die voorkoming van migraine en chroniese spanningshoofpyn. Dit kan gebruik word vir die behandeling van nagtelike enurese by kinders ouer as 6 nadat ander behandelings misluk het.[7]

Depressie

wysig

Amitriptilien is effektief vir depressie,[18] maar dit word selde as 'n eerste-linie antidepressant gebruik weens die hoër toksisiteit in oordosis en oor die algemeen swakker verdraagsaamheid.[19] Dit kan gebruik word vir depressie as 'n tweede-linie terapie, na die mislukking van ander behandelings.[20] Vir behandeling-weerstandige adolessente depressie[21] of vir kankerverwante depressie[22] is amitriptilien nie beter as plasebo nie. Dit word soms gebruik vir die behandeling van depressie in Parkinson se siekte,[23] maar ondersteunende bewyse daarvoor ontbreek.[24]

Pyn

wysig

Amitriptilien verlig pynlike diabetiese neuropatie . Dit word deur 'n verskeidenheid riglyne aanbeveel as 'n eerste- of tweedelynbehandeling.Kombinasiebehandeling van amitriptilien en pregabalien bied bykomende pynverligting vir mense wie se pyn nie voldoende met een medikasie beheer word nie, en is veilig.[25][26]

Lae dosisse amitriptilien verbeter slaapstoornisse matig en verminder pyn en moegheid wat verband hou met fibromialgie.[27]Kombinasies van amitriptilien en fluoksetien of melatonien kan fibromialgiepyn beter verlaag as enige medikasie op sy eie.[28]

Hoofpyn

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Amitriptilien is waarskynlik effektief vir die voorkoming van periodieke migraine by volwassenes. Amitriptilien is soortgelyk in doeltreffendheid aan venlafaksien en topiramaat, maar dra 'n groter las van nadelige effekte as topiramaat.[29] Vir baie pasiënte is selfs baie klein dosisse amitriptilien nuttig, wat moontlik kan maak vir die vermindering van newe-effekte.[30] Amitriptilien verskil nie beduidend van plasebo wanneer dit gebruik word vir die voorkoming van migraine by kinders nie.[31]

Amitriptilien kan die frekwensie en duur van chroniese spanningshoofpyn verminder, maar dit word geassosieer met erger nadelige effekte as mirtazapien. In die algemeen word amitriptilien aanbeveel vir die voorkoming van spanningshoofpyn, tesame met lewenstyladvies, wat vermyding van pynstillers en kafeïen moet insluit.[32]

Voorskrifneigings

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Tussen 1998 en 2017, saam met imipramien, was amitriptilien die mees algemeen voorgeskrewe eerste antidepressant vir kinders van 5-11 jaar in Engeland. Dit was ook die mees voorgeskrewe antidepressant (saam met fluoksetien) vir 12- tot 17-jariges.[33]

wysig

Die paar gerandomiseerde gekontroleerde proewe wat die doeltreffendheid van amitriptilien in eetversteuring ondersoek het, was ontmoedigend.[34]

Verwysings

wysig
  1. ↑ Blessel KW, Rudy BC, Senkowski BZ (1974). "Amitriptyline Hydrochloride". Analytical Profiles of Drug Substances. 3: 127–148. doi:10.1016/S0099-5428(08)60066-0. ISBN 9780122608032.
  2. ↑ 2,0 2,1 Schulz P, Dick P, Blaschke TF, Hollister L (1985). "Discrepancies between pharmacokinetic studies of amitriptyline". Clin Pharmacokinet. 10 (3): 257–68. doi:10.2165/00003088-198510030-00005. PMID 3893842. S2CID 41881790.
  3. ↑ 3,0 3,1 McClure EW, Daniels RN (Februarie 2021). "Classics in Chemical Neuroscience: Amitriptyline". ACS Chem Neurosci. 12 (3): 354–362. doi:10.1021/acschemneuro.0c00467. PMID 33438398. S2CID 231596860.
  4. ↑ Breyer-Pfaff U (Oktober 2004). "The metabolic fate of amitriptyline, nortriptyline and amitriptylinoxide in man". Drug Metab Rev. 36 (3–4): 723–46. doi:10.1081/dmr-200033482. PMID 15554244. S2CID 25565048.
  5. ↑ Venkatakrishnan K, Schmider J, Harmatz JS, Ehrenberg BL, von Moltke LL, Graf JA, Mertzanis P, Corbett KE, Rodriguez MC, Shader RI, Greenblatt DJ (Oktober 2001). "Relative contribution of CYP3A to amitriptyline clearance in humans: in vitro and in vivo studies". J Clin Pharmacol. 41 (10): 1043–54. doi:10.1177/00912700122012634. PMID 11583471. S2CID 27146286.
  6. ↑ Schulz P, Balant-Gorgia AE, Kubli A, Gertsch-Genet C, Garrone G (1983). "Elimination and pharmacological effects following single oral doses of 50 and 75 mg of amitriptyline in man". Arch Psychiatr Nervenkr (1970). 233 (6): 449–55. doi:10.1007/BF00342785. PMID 6667101. S2CID 20844722.
  7. ↑ 7,0 7,1 "Amitriptyline Tablets BP 50mg – Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Actavis UK Ltd. 24 Maart 2013. Geargiveer vanaf die oorspronklike op 3 Desember 2013. Besoek op 1 Desember 2013.
  8. ↑ Hitchings A, Lonsdale D, Burrage D, Baker E (2015). Top 100 drugs : clinical pharmacology and practical prescribing. p. 50. ISBN 978-0-7020-5516-4.
  9. ↑ Alam U, Sloan G, Tesfaye S (Maart 2020). "Treating Pain in Diabetic Neuropathy: Current and Developmental Drugs". Drugs. 80 (4): 363–384. doi:10.1007/s40265-020-01259-2. PMID 32040849. S2CID 211074023.
  10. ↑ Macfarlane GJ, Kronisch C, Dean LE, Atzeni F, Häuser W, Fluß E, Choy E, Kosek E, Amris K, Branco J, Dincer F, Leino-Arjas P, Longley K, McCarthy GM, Makri S, Perrot S, Sarzi-Puttini P, Taylor A, Jones GT (Februarie 2017). "EULAR revised recommendations for the management of fibromyalgia". Ann Rheum Dis. 76 (2): 318–328. doi:10.1136/annrheumdis-2016-209724. PMID 27377815.
  11. ↑ Silberstein SD, Holland S, Freitag F, Dodick DW, Argoff C, Ashman E (April 2012). "Evidence-based guideline update: pharmacologic treatment for episodic migraine prevention in adults: report of the Quality Standards Subcommittee of the American Academy of Neurology and the American Headache Society". Neurology. 78 (17): 1337–45. doi:10.1212/WNL.0b013e3182535d20. PMC 3335452. PMID 22529202.
  12. ↑ Tfelt-Hansen P, Ågesen FN, Pavbro A, Tfelt-Hansen J (Mei 2017). "Pharmacokinetic Variability of Drugs Used for Prophylactic Treatment of Migraine". CNS Drugs. 31 (5): 389–403. doi:10.1007/s40263-017-0430-3. PMID 28405886. S2CID 23560743.
  13. ↑ Fangmann P, Assion HJ, Juckel G, González CA, López-Muñoz F (Februarie 2008). "Half a century of antidepressant drugs: on the clinical introduction of monoamine oxidase inhibitors, tricyclics, and tetracyclics. Part II: tricyclics and tetracyclics". Journal of Clinical Psychopharmacology. 28 (1): 1–4. doi:10.1097/jcp.0b013e3181627b60. PMID 18204333. S2CID 31018835.
  14. ↑ World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  15. ↑ "Amitriptyline Hydrochloride". Drugs.com. The American Society of Health-System Pharmacists. Geargiveer vanaf die oorspronklike op 24 September 2014. Besoek op 25 September 2014.
  16. ↑ "The Top 300 of 2020". ClinCalc.com. Besoek op 7 Oktober 2022.
  17. ↑ "Amitriptyline – Drug Usage Statistics". ClinCalc.com. Besoek op 7 Oktober 2022.
  18. ↑ Leucht C, Huhn M, Leucht S (Desember 2012). "Amitriptyline versus placebo for major depressive disorder". Cochrane Database Syst Rev. 12: CD009138. doi:10.1002/14651858.CD009138.pub2. PMID 23235671.
  19. ↑ Rossi, S, red. (2013). Australian Medicines Handbook (2013 uitg.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.
  20. ↑ Hitchings A, Lonsdale D, Burrage D, Baker E (2015). Top 100 drugs : clinical pharmacology and practical prescribing. p. 50. ISBN 978-0-7020-5516-4.
  21. ↑ Zhou X, Michael KD, Liu Y, Del Giovane C, Qin B, Cohen D, Gentile S, Xie P (November 2014). "Systematic review of management for treatment-resistant depression in adolescents". BMC Psychiatry. 14: 340. doi:10.1186/s12888-014-0340-6. PMC 4254264. PMID 25433401.
  22. ↑ Riblet N, Larson R, Watts BV, Holtzheimer P (2014). "Reevaluating the role of antidepressants in cancer-related depression: a systematic review and meta-analysis". Gen Hosp Psychiatry. 36 (5): 466–73. doi:10.1016/j.genhosppsych.2014.05.010. PMID 24950919.
  23. ↑ "Parkinson's disease". merckmanuals.com. Merck Sharp & Dohme Corp. Augustus 2007. Geargiveer vanaf die oorspronklike op 18 November 2013. Besoek op 22 Desember 2013.
  24. ↑ Seppi K, Weintraub D, Coelho M, Perez-Lloret S, Fox SH, Katzenschlager R, Hametner EM, Poewe W, Rascol O, Goetz CG, Sampaio C (Oktober 2011). "The Movement Disorder Society Evidence-Based Medicine Review Update: Treatments for the non-motor symptoms of Parkinson's disease". Mov Disord. 26 (Suppl 3): S42–80. doi:10.1002/mds.23884. PMC 4020145. PMID 22021174.
  25. ↑ "Combination therapy for painful diabetic neuropathy is safe and effective". NIHR Evidence (in Engels). 6 April 2023. doi:10.3310/nihrevidence_57470.
  26. ↑ Tesfaye S, Sloan G, Petrie J, White D, Bradburn M, Julious S, et al. (Augustus 2022). "Comparison of amitriptyline supplemented with pregabalin, pregabalin supplemented with amitriptyline, and duloxetine supplemented with pregabalin for the treatment of diabetic peripheral neuropathic pain (OPTION-DM): a multicentre, double-blind, randomised crossover trial". Lancet. 400 (10353): 680–690. doi:10.1016/s0140-6736(22)01472-6.
  27. ↑ Sommer C, Alten R, Bär KJ, Bernateck M, Brückle W, Friedel E, Henningsen P, Petzke F, Tölle T, Üçeyler N, Winkelmann A, Häuser W (Junie 2017). "[Drug therapy of fibromyalgia syndrome : Updated guidelines 2017 and overview of systematic review articles]". Schmerz (in Duits). 31 (3): 274–284. doi:10.1007/s00482-017-0207-0. PMID 28493231.
  28. ↑ Thorpe J, Shum B, Moore RA, Wiffen PJ, Gilron I (Februarie 2018). "Combination pharmacotherapy for the treatment of fibromyalgia in adults". Cochrane Database Syst Rev. 2 (2): CD010585. doi:10.1002/14651858.CD010585.pub2. PMID 29457627.
  29. ↑ Silberstein SD, Holland S, Freitag F, Dodick DW, Argoff C, Ashman E (April 2012). "Evidence-based guideline update: pharmacologic treatment for episodic migraine prevention in adults: report of the Quality Standards Subcommittee of the American Academy of Neurology and the American Headache Society". Neurology. 78 (17): 1337–45. doi:10.1212/WNL.0b013e3182535d20. PMC 3335452. PMID 22529202.
  30. ↑ Loder E, Rizzoli P (November 2018). "Pharmacologic Prevention of Migraine: A Narrative Review of the State of the Art in 2018". Headache. 58 (Suppl 3): 218–229. doi:10.1111/head.13375. PMID 30137671. S2CID 52071815.
  31. ↑ Oskoui M, Pringsheim T, Billinghurst L, Potrebic S, Gersz EM, Gloss D, Holler-Managan Y, Leininger E, Licking N, Mack K, Powers SW, Sowell M, Victorio MC, Yonker M, Zanitsch H, Hershey AD (September 2019). "Practice guideline update summary: Pharmacologic treatment for pediatric migraine prevention: Report of the Guideline Development, Dissemination, and Implementation Subcommittee of the American Academy of Neurology and the American Headache Society". Neurology. 93 (11): 500–509. doi:10.1212/WNL.0000000000008105. PMC 6746206. PMID 31413170.
  32. ↑ Ghadiri-Sani M, Silver N (Februarie 2016). "Headache (chronic tension-type)". BMJ Clin Evid. 2016. PMC 4747324. PMID 26859719.
  33. ↑ Jack RH, Hollis C, Coupland C, Morriss R, Knaggs RD, Butler D, et al. (Julie 2020). Hellner C (red.). "Incidence and prevalence of primary care antidepressant prescribing in children and young people in England, 1998–2017: A population-based cohort study". PLOS Medicine. 17 (7): e1003215. doi:10.1371/journal.pmed.1003215. PMC 7375537. PMID 32697803.
  34. ↑ Flament MF, Bissada H, Spettigue W (Maart 2012). "Evidence-based pharmacotherapy of eating disorders". International Journal of Neuropsychopharmacology. 15 (2): 189–207. doi:10.1017/S1461145711000381. PMID 21414249.
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