Gabapentin enakarbil (Horizant) prolek je gabapentina. On se koristi za lečenje sindroma nemirnih nogu (RLS) i posterpetske neuralgije (PHN) kod odraslih osoba.[1][2][3]

Gabapentin enakarbil
Klinički podaci
Drugs.comenacarbil.html Monografija
Način primeneOralno
Farmakokinetički podaci
Poluvreme eliminacije5,1 - 6,0 h
IzlučivanjeRenalno (94%)
Identifikatori
CAS broj478296-72-9 ДаY
ATC kodNone
PubChemCID 9883933
DrugBankDB08872 ДаY
ChemSpider8059607 ДаY
ChEBICHEBI:68840 ДаY
Hemijski podaci
FormulaC16H27NO6
Molarna masa329.389
  • CC(C)C(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O
  • InChI=1S/C16H27NO6/c1-11(2)14(20)22-12(3)23-15(21)17-10-16(9-13(18)19)7-5-4-6-8-16/h11-12H,4-10H2,1-3H3,(H,17,21)(H,18,19) ДаY
  • Key:TZDUHAJSIBHXDL-UHFFFAOYSA-N ДаY

Osobine уреди

Osobina Vrednost
Broj akceptora vodonika 7
Broj donora vodonika 2
Broj rotacionih veza 9
Particioni koeficijent[4] (ALogP) 3,5
Rastvorljivost[5] (logS, log(mol/L)) -3,9
Polarna površina[6] (PSA, Å2) 105,4

Reference уреди

  1. ^ Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. PMID 15146029
  2. ^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.  уреди
  3. ^ David S. Wishart; Craig Knox; An Chi Guo; Dean Cheng; Savita Shrivastava; Dan Tzur; Bijaya Gautam; Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic acids research. 36 (Database issue): D901—6. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.  уреди
  4. ^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o. 
  5. ^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t.  уреди
  6. ^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e.  уреди

Literatura уреди

Spoljašnje veze уреди