Rifaksimin

Rifaksimin
Klinički podaci
Prodajno imeFatroximin, Normix, Rifacol, Ritacol
Drugs.comMonografija
Način primeneOralno
Farmakokinetički podaci
Poluvreme eliminacije6 h
Identifikatori
CAS broj80621-81-4 ДаY
ATC kodA07AA11 (WHO), D06AX11
PubChemCID 6436173
DrugBankDB01220 ДаY
ChemSpider4940837 ДаY
ChEMBLCHEMBL1617 ДаY
Hemijski podaci
FormulaC43H51N3O11
Molarna masa785,879
SMILES
  • CO[C@H]1\C=C\O[C@@]2(C)OC3=C(C)C(O)=C4C(O)=C(NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)C1=C(N=C5C=C(C)C=CN15)C4=C3C2=O
InChI
  • InChI=1S/C43H51N3O11/c1-19-14-16-46-28(18-19)44-32-29-30-37(50)25(7)40-31(29)41(52)43(9,57-40)55-17-15-27(54-10)22(4)39(56-26(8)47)24(6)36(49)23(5)35(48)20(2)12-11-13-21(3)42(53)45-33(34(32)46)38(30)51/h11-18,20,22-24,27,35-36,39,48-51H,1-10H3,(H,45,53)/b12-11+,17-15+,21-13-/t20-,22+,23+,24+,27-,35-,36+,39+,43-/m0/s1 ДаY
  • Key:NZCRJKRKKOLAOJ-XRCRFVBUSA-N ДаY

Rifaksimin je organsko jedinjenje, koje sadrži 43 atoma ugljenika i ima molekulsku masu od 785,879 Da.[1][2][3][4][5]

Osobine

Osobina Vrednost
Broj akceptora vodonika 12
Broj donora vodonika 5
Broj rotacionih veza 3
Particioni koeficijent[6] (ALogP) 4,8
Rastvorljivost[7] (logS, log(mol/L)) -8,2
Polarna površina[8] (PSA, Å2) 198,4

Reference

  1. ^ Cottreau J, Baker SF, DuPont HL, Garey KW: Rifaximin: a nonsystemic rifamycin antibiotic for gastrointestinal infections. Expert Rev Anti Infect Ther. 2010 Jul;8(7):747-60. PMID 20586560
  2. ^ Williams R, Bass N: Rifaximin, a nonabsorbed oral antibiotic, in the treatment of hepatic encephalopathy: antimicrobial activity, efficacy, and safety. Rev Gastroenterol Disord. 2005;5 Suppl 1:S10-8. PMID 15976747
  3. ^ Koo HL, DuPont HL: Rifaximin: a unique gastrointestinal-selective antibiotic for enteric diseases. Curr Opin Gastroenterol. 2010 Jan;26(1):17-25. PMID 19881343
  4. ^ 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 Слободан приступ. PMID 21059682. doi:10.1093/nar/gkq1126.  уреди
  5. ^ 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 Слободан приступ. PMID 18048412. doi:10.1093/nar/gkm958.  уреди
  6. ^ 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. 
  7. ^ 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
  8. ^ 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

  • Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803. 
  • Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799. 

Spoljašnje veze

  • Rifaximin
  • p
  • r
  • u
Antifolati
(inhibira
purinski metabolizam,
i tim putem inhibira
DNK i RNK sintezu)
DR inhibitor
Sulfonamidi
(DS inhibitor)
Kratkotrajni
Srednje trajni
Dugotrajni
Drugi/negrupisani
Kombinacije
Inhibitori
topoizomeraze/
hinoloni/
(inhibiraju
DNK replikaciju)
1. generacija
Fluorohinoloni
2. generacija
3. generacija
4. generacija
Veterinarski
Srodni agenti (DG)
Anaerobni DNK
inhibitori
Nitro- imidazol derivati
Nitrofuran derivati
RNK sinteza
Rifamicinii/
RNK polimeraza
Rifampicin • Rifabutin • Rifapentin • Rifaksimin

M: INF

bact/virs/fung/para(a,e,c,h,r)

bact(+/-p/-o)/virs/fung/para(a,e,c,h,r), epon

bact(J1p,w,n,m)/virs(J5d,r,h)/fung/para(a,e,c,h,r),v,g


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Rifaksimin na srodnim projektima Vikipedije:
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