Repaglinid

Repaglinid
Klinički podaci
Robne marke GlucoNorm, Prandin
AHFS/Drugs.com Monografija
Identifikatori
CAS broj 135062-02-1
ATC kod A10BX02
PubChem[1][2] 65981
DrugBank DB00912
ChemSpider[3] 59377
KEGG[4] C07670 DaY
ChEMBL[5] CHEMBL1272 DaY
Hemijski podaci
Formula C27H36N2O4 
Mol. masa 452,586
SMILES eMolekuli & PubHem
Fizički podaci
Tačka topljenja 130-131 °C (-74 °F)
Farmakokinetički podaci
Poluvreme eliminacije 1 h
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

Repaglinid je organsko jedinjenje, koje sadrži 27 atoma ugljenika i ima molekulsku masu od 452,586 Da.[6][7][8]

Osobine

Osobina Vrednost
Broj akceptora vodonika 5
Broj donora vodonika 2
Broj rotacionih veza 10
Particioni koeficijent[9] (ALogP) 5,3
Rastvorljivost[10] (logS, log(mol/L)) -6,8
Polarna površina[11] (PSA, Å2) 78,9

Primena u lečenju šećerna bolesti [12]

Repaglinidi se primarno primenjeni u kod tip 2 šećerne bolesti. Kod bolesnika sa šećernom bolešću oni smanjuju vrednosti šećera u krvi, stimulišući sekreciju insulina vezivanjem za specifične receptore u membrani ćelija gušterače.

Kontraindikacije: Tip 1 šećerna bolest, trudnoća, dojenje, ketoacidoza, teška oštećenja jetre i bubrega, akutna infektivna stanja, trauma, koma, akutni infarkt miokarda, bolesnici mlađi od 18 godina i stariji od 75 godina.

Neželjeni efekti: Mučnina, povraćanje, bol u trbuhu, proliv, zatvor, alergijske reakcije uz osip po koži, retko porast jetrenih enzima.

Interakcije:

  • Lekovi koji pojačavaju dejstvo repaglinida su: ACE inhibitori, neselektivni blokatori, salicilati, anabolni steroidi, alkohol, antibiotici (eritromicin, klaritromicin), antimikotici, nesteroidni antiinflamatorni lijekovi.
  • Lekovi koji smanjuju dejstvo repaglinida su: oralni kontraceptivi, kortikosteroidi, tireoidni hormoni, barbiturati, troglitazon.

Neki od registrovanih repaglinida

  • NOVONORM tbl. od 0,5 mg., pakovanje 90 tbl.(Novo Nordisk),
  • NOVONORM tbl. od 1 mg., pakovanje 90 tbl.(Novo Nordisk),
  • NOVONORM tbl. od 2 mg., pakovanje 90 tbl.(Novo Nordisk).

Reference

  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.  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. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  6. Massi-Benedetti M, Damsbo P: Pharmacology and clinical experience with repaglinide. Expert Opin Investig Drugs. 2000 Apr;9(4):885-98. PMID 11060717
  7. 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. DOI:10.1093/nar/gkq1126. PMC 3013709. PMID 21059682.  edit
  8. David S. Wishart, Craig Knox, An Chi Guo, Dean Cheng, Savita Shrivastava, Dan Tzur, Bijaya Gautam, and Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Res 36 (Database issue): D901-6. DOI:10.1093/nar/gkm958. PMC 2238889. PMID 18048412.  edit
  9. Ghose, A.K., Viswanadhan V.N., and 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. 
  10. 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. DOI:10.1021/ci000392t. PMID 11749573.  edit
  11. 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. DOI:10.1021/jm000942e. PMID 11020286.  edit
  12. Ministarstvo zdravlja Republike Srbije. Nacionalni vodič dobre kliničke prakse Diabetes Mellitus Beograd, 2012. pp. 34-35

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