Amitriptilien

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]

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} Verwysingfout: Invalid <ref> tag; no text was provided for refs named pmid3893842
3. ↑ ^{3,0 3,1} Verwysingfout: Invalid <ref> tag; no text was provided for refs named pmid33438398
4. ↑ Verwysingfout: Invalid <ref> tag; no text was provided for refs named pmid15554244
5. ↑ Verwysingfout: Invalid <ref> tag; no text was provided for refs named pmid11583471
6. ↑ Verwysingfout: Invalid <ref> tag; no text was provided for refs named pmid6667101
7. ↑ "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.