Tramadol

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Tramadol
(IUPAC) ime
(1R,2R)-rel-2-[(dimetilamino)metil]- 1-(3-metoksifenil)cikloheksanol
Klinički podaci
Identifikatori
CAS broj 27203-92-5
ATC kod N02AX02
PubChem[1][2] 33741
DrugBank APRD00028
ChemSpider[3] 31105
UNII 39J1LGJ30J YesY
Hemijski podaci
Formula C16H25NO2 
Mol. masa 263.4 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 68–72% (povećava se sa ponovljenim doziranjem.)
Vezivanje za proteine plazme 20%
Metabolizam hepatički demetilacija i glukuronidacija
Poluvreme eliminacije 5–7 časova
Izlučivanje renalno
Farmakoinformacioni podaci
Trudnoća C(AU) C(US)
Pravni status Samo na recept (S4) (AU) POM (UK) -only (SAD) Prescription only
Način primene oralno, IV, IM, rektalno, sablingualno, intranazalno

Tramadol (Ultram, Tramal) je centralno delujući analgetik i koristi se u lečenju umerenog do umereno jakog bola. Lek ima širok spektar delovanja, uključujući i tretman za sindrom nemirnih nogu, gastroezofagealni refluks, i fibromijalgiju. Razvila ga je farmaceutska kompanija Grünenthal GmbH krajem 70-ih godina 20. veka.[4]

Tramadol dejstvuje kao slab agonist na μ-opioidnom receptoru, oslobađa serotonin, i inhibira reapsorpciju norepinefrina.[5][6][7][8][9][10][11]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. US patent 3652589, Flick, Kurt; Frankus, Ernst, "1-(m-Substituted Phenyl)-2-Aminomethyl Cyclohexanols", granted 28. 3. 1972.  
  5. Dayer, P; Desmeules, J; Collart, L (1997). "Pharmacology of tramadol". Drugs. 53 Suppl 2: 18–24. PMID 9190321. doi:10.2165/00003495-199700532-00006. 
  6. Lewis, KS; Han, NH (1997). "Tramadol: a new centrally acting analgesic". American journal of health-system pharmacy 54 (6): 643–52. PMID 9075493. 
  7. WO patent 2007070779, Singh, Chandra, "A Method to Treat Premature Ejaculation in Humans", granted 21. 6. 2007.  
  8. Driessen B, Reimann W (January 1992). "Interaction of the central analgesic, tramadol, with the uptake and release of 5-hydroxytryptamine in the rat brain in vitro". British Journal of Pharmacology 105 (1): 147–51. PMC 1908625. PMID 1596676. 
  9. Bamigbade TA, Davidson C, Langford RM, Stamford JA (September 1997). "Actions of tramadol, its enantiomers and principal metabolite, O-desmethyltramadol, on serotonin (5-HT) efflux and uptake in the rat dorsal raphe nucleus". British Journal of Anaesthesia 79 (3): 352–6. PMID 9389855. 
  10. Reimann W, Schneider F (May 1998). "Induction of 5-hydroxytryptamine release by tramadol, fenfluramine and reserpine". European Journal of Pharmacology 349 (2-3): 199–203. PMID 9671098. doi:10.1016/S0014-2999(98)00195-2. 
  11. Gobbi M, Moia M, Pirona L et al. (September 2002). "p-Methylthioamphetamine and 1-(m-chlorophenyl)piperazine, two non-neurotoxic 5-HT releasers in vivo, differ from neurotoxic amphetamine derivatives in their mode of action at 5-HT nerve endings in vitro". Journal of Neurochemistry 82 (6): 1435–43. PMID 12354291. doi:10.1046/j.1471-4159.2002.01073.x. 

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