Labetalol

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Labetalol
(IUPAC) ime
(RS)-2-hidroksi-51-hidroksi-2-[(1-metil-3-fenolpropil)amino]etil}benzamid
Klinički podaci
Robne marke Trandat
AHFS/Drugs.com Monografija
MedlinePlus a685034
Identifikatori
CAS broj 36894-69-6
ATC kod C07AG01
PubChem[1][2] 3869
DrugBank DB00598
ChemSpider[3] 3734
UNII R5H8897N95 YesY
KEGG[4] D08106 YesY
ChEBI CHEBI:6343 YesY
ChEMBL[5] CHEMBL429 YesY
Hemijski podaci
Formula C19H24N2O3 
Mol. masa 328,406 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 25%
Vezivanje za proteine plazme 50%
Metabolizam hepatički
Poluvreme eliminacije Tableta: 6-8 sati; IV: 5.5 sati
Izlučivanje urin
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Prescription only
Način primene oralno iv

Labetalol (Normodin, Trandat) je mešoviti alfa/beta adrenergički antagonist, koji se koristi za tretiranje visokog krvnog pritiska.[6]

Indikcije[uredi - уреди | uredi izvor]

Koristi se kao tretman trudnoćom indukovanu hipertenziju koja je često vezana za preeklampsiju.[7] On se takođe koristi za tretiranje hronične i akutne hipertenzije feohromocitoma i hipertenzivne krize.[8][9]

Stereokemija[uredi - уреди | uredi izvor]

Labetalol sadrži dva stereogena centra i sastoji se od četiri stereoizomera. Ovo je mješavina ("R", "R") -, ("S", "R") -, ("R", "S" ) - i ( S , S ) - oblik:

Stereoizomeri Labetalola
(RR)-Labetalol Structural Formula V1.svg
CAS-Nummer: 75659-07-3
(SS)-Labetalol Structural Formula V1.svg
CAS-Nummer: 83167-24-2
(RS)-Labetalol Structural Formula V1.svg
CAS-Nummer: 83167-32-2
(SR)-Labetalol Structural Formula V1.svg
CAS-Nummer: 83167-31-1

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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 20331846. doi:10.1186/1758-2946-2-3.  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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. Fahed S, Grum DF, Papadimos TJ (2008). "Labetalol infusion for refractory hypertension causing severe hypotension and bradycardia: an issue of patient safety". Patient Saf Surg 2: 13. PMC 2429901. PMID 18505576. doi:10.1186/1754-9493-2-13. 
  7. C. J. Pickles, E. M. Symonds, F. Broughton Pipkin (January 1989). "The fetal outcome in a randomized double-blind controlled trial of labetalol versus placebo in pregnancy-induced hypertension". BJOG: An International Journal of Obstetrics & Gynaecology 96 (1): 38–43. doi:10.1111/j.1471-0528.1989.tb01574.x. 
  8. Katzung, Bertram G. (2006). Basic and clinical pharmacology. New York: McGraw-Hill Medical. str. 170. ISBN 0-07-145153-6. 
  9. D A Richards, J Tuckman, and B N Prichard (October 1976). "Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol". Br J Clin Pharmacol 3 (5): 849–855. PMC 1428931. PMID 9968. 

Literatura[uredi - уреди | uredi izvor]

Spoljašnje veze[uredi - уреди | uredi izvor]

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