Prukaloprid

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Prukaloprid
(IUPAC) ime
4-Amino-5-hloro-N-[1-(3-metoksipropil)piperidin-4-il]-2,3-dihidro-1-benzofuran-7-karboksamid
Klinički podaci
Robne marke Resolor, Resotran
AHFS/Drugs.com Internacionalno ime leka
Identifikatori
CAS broj 179474-81-8
ATC kod A03AE04
PubChem[1][2] 3052762
UNII 0A09IUW5TP YesY
Hemijski podaci
Formula C18H26ClN3O3 
Mol. masa 367,870 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Licenca

EU EMEA:link

Trudnoća ?
Pravni status Prescription only
Način primene Oralno

Prukaloprid (Resolor) je lek koji deluje kao selektivni agonist visokog afiniteta za 5-HT4 receptor.[3] On poboljšava umanjeni motilitet creva koji je tipičan za hroničnu konstipaciju, i proizvodi normalnije pražnjenje creva.[4][5][6][7][8][9] Prukaloprid je odobren za upotrebu u Evropi 2009[10] i u Kanadi (Resotran) 2011[11], dok u SAD-u nije odobren. Ovaj lek se ispituje za moguću primenu u tretmanu hronične intestinalne pseudoopstrukcije.[12][13]

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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  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. Briejer, M. R.; Bosmans, J. P.; Van Daele, P.; Jurzak, M.; Heylen, L.; Leysen, J. E.; Prins, N. H.; Schuurkes, J. A. (2001). „The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound”. European Journal of Pharmacology 423 (1): 71–83. DOI:10.1016/S0014-2999(01)01087-1. PMID 11438309. 
  4. Clinical Trials NCT00793247
  5. Emmanuel, A. V.; Kamm, M. A.; Roy, A. J.; Kerstens, R.; Vandeplassche, L. (2012). „Randomised clinical trial: The efficacy of prucalopride in patients with chronic intestinal pseudo-obstruction - a double-blind, placebo-controlled, cross-over, multiple n = 1 study”. Alimentary Pharmacology & Therapeutics 35 (1): 48–55. DOI:10.1111/j.1365-2036.2011.04907.x. PMID 22061077. 
  6. Smart, C. J.; Ramesh, A. N. (2011). „The successful treatment of acute refractory pseudo-obstruction with Prucalopride”. Colorectal Disease: no. DOI:10.1111/j.1463-1318.2011.02929.x. 
  7. Bouras, E. P.; Camilleri, M.; Burton, D. D.; McKinzie, S. (1999). „Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans”. Gut 44 (5): 682–686. DOI:10.1136/gut.44.5.682. PMC 1727485. PMID 10205205. //www.ncbi.nlm.nih.gov/pmc/articles/PMC1727485/. 
  8. Bouras, E. P.; Camilleri, M.; Burton, D. D.; Thomforde, G.; McKinzie, S.; Zinsmeister, A. R. (2001). „Prucalopride accelerates gastrointestinal and colonic transit in patients with constipation without a rectal evacuation disorder”. Gastroenterology 120 (2): 354–360. DOI:10.1053/gast.2001.21166. PMID 11159875. 
  9. Tack, J.; Van Outryve, M.; Beyens, G.; Kerstens, R.; Vandeplassche, L. (2008). „Prucalopride (Resolor) in the treatment of severe chronic constipation in patients dissatisfied with laxatives”. Gut 58 (3): 357–365. DOI:10.1136/gut.2008.162404. PMID 18987031. 
  10. European Medicines Agency -EPAR
  11. Health Canada, Notice of Decision for Resotran
  12. Briejer, M. R.; Prins, N. H.; Schuurkes, J. A. (2001). „Effects of the enterokinetic prucalopride (R093877) on colonic motility in fasted dogs”. Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society 13 (5): 465–472. DOI:10.1046/j.1365-2982.2001.00280.x. PMID 11696108. 
  13. Oustamanolakis, P.; Tack, J. (2012). „Prucalopride for chronic intestinal pseudo-obstruction”. Alimentary Pharmacology & Therapeutics 35 (3): 398. DOI:10.1111/j.1365-2036.2011.04947.x. 

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