Celekoksib

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Celekoksib
Celecoxib.svg
Celecoxib-3D-spacefill.png
Klinički podaci
Prodajno imeCelebra, Celebrex
Drugs.comMonografija
Način primeneOralno
Farmakokinetički podaci
Poluvreme eliminacije11 h
IzlučivanjeRenalno, fekalno
Identifikatori
CAS broj169590-42-5 ДаY
ATC kodL01XX33 (WHO), M01AH01
PubChemCID 2662
DrugBankDB00482 ДаY
ChemSpider2562 ДаY
KEGGC07589 ДаY
ChEBICHEBI:3520 ДаY
ChEMBLCHEMBL118 ДаY
Hemijski podaci
FormulaC17H14F3N3O2S
Molarna masa381,372
Fizički podaci
Tačka topljenja158 °C (316 °F)

Celekoksib je COX-2 selektivni nesteroidni anti-inflamatorni lek. Jedno od imena pod kojima se prodaje je Celebrex.

Hemiske osobine[уреди]

Celekoksib je organsko jedinjenje, koje sadrži 17 atoma ugljenika i ima molekulsku masu od 381,372 Da.[1][2][3][4][5][6][7][8]

Osobine[уреди]

Osobina Vrednost
Broj akceptora vodonika 3
Broj donora vodonika 1
Broj rotacionih veza 4
Particioni koeficijent[9] (ALogP) 4,4
Rastvorljivost[10] (logS, log(mol/L)) -6,4
Polarna površina[11] (PSA, Å2) 86,4

Reference[уреди]

  1. ^ Malhotra S, Shafiq N, Pandhi P: COX-2 inhibitors: a CLASS act or Just VIGORously promoted. MedGenMed. 2004 Mar 23;6(1):6. PMID 15208519
  2. ^ Silverstein FE, Faich G, Goldstein JL, Simon LS, Pincus T, Whelton A, Makuch R, Eisen G, Agrawal NM, Stenson WF, Burr AM, Zhao WW, Kent JD, Lefkowith JB, Verburg KM, Geis GS: Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study. JAMA. 2000 Sep 13;284(10):1247-55. PMID 10979111
  3. ^ Solomon SD, McMurray JJ, Pfeffer MA, Wittes J, Fowler R, Finn P, Anderson WF, Zauber A, Hawk E, Bertagnolli M: Cardiovascular risk associated with celecoxib in a clinical trial for colorectal adenoma prevention. N Engl J Med. 2005 Mar 17;352(11):1071-80. Epub 2005 Feb 15. PMID 15713944
  4. ^ Yelland MJ, Nikles CJ, McNairn N, Del Mar CB, Schluter PJ, Brown RM: Celecoxib compared with sustained-release paracetamol for osteoarthritis: a series of n-of-1 trials. Rheumatology (Oxford). 2007 Jan;46(1):135-40. Epub 2006 Jun 15. PMID 16777855
  5. ^ Bertagnolli MM, Eagle CJ, Zauber AG, Redston M, Solomon SD, Kim K, Tang J, Rosenstein RB, Wittes J, Corle D, Hess TM, Woloj GM, Boisserie F, Anderson WF, Viner JL, Bagheri D, Burn J, Chung DC, Dewar T, Foley TR, Hoffman N, Macrae F, Pruitt RE, Saltzman JR, Salzberg B, Sylwestrowicz T, Gordon GB, Hawk ET: Celecoxib for the prevention of sporadic colorectal adenomas. N Engl J Med. 2006 Aug 31;355(9):873-84. PMID 16943400
  6. ^ Sandberg M, Yasar U, Stromberg P, Hoog JO, Eliasson E: Oxidation of celecoxib by polymorphic cytochrome P450 2C9 and alcohol dehydrogenase. Br J Clin Pharmacol. 2002 Oct;54(4):423-9. PMID 12392591
  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. PMC 3013709Слободан приступ. PMID 21059682. doi:10.1093/nar/gkq1126. 
  8. ^ 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 2238889Слободан приступ. PMID 18048412. doi:10.1093/nar/gkm958. 
  9. ^ 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. 
  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. PMID 11749573. doi:10.1021/ci000392t. 
  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. PMID 11020286. doi:10.1021/jm000942e. 

Literatura[уреди]

Spoljašnje veze[уреди]

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