Labetalol

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	3869
DrugBank	DB00598
ChemSpider	3734
UNII	R5H8897N95
KEGG	D08106
ChEBI	CHEBI:6343
ChEMBL	CHEMBL429
Hemijski podaci
Formula	C19H24N2O3
Mol. masa	328,406 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24) ; Key: SGUAFYQXFOLMHL-UHFFFAOYSA-N
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 | uredi kod]

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 | uredi kod]

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
CAS-Nummer: 75659-07-3	CAS-Nummer: 83167-24-2
CAS-Nummer: 83167-32-2	CAS-Nummer: 83167-31-1

Reference[uredi | uredi kod]

↑ 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
↑ 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.
↑ 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
↑ 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.
↑ 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
↑ 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. DOI:10.1186/1754-9493-2-13. PMC 2429901. PMID 18505576.
↑ 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.
↑ Katzung, Bertram G. (2006). Basic and clinical pharmacology. New York: McGraw-Hill Medical. str. 170. ISBN 0-07-145153-6.
↑ 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 | uredi kod]

Spoljašnje veze[uredi | uredi kod]

	Portal Medicina
	Portal Hemija

Molimo Vas, obratite pažnju na važno upozorenje u vezi tema o zdravlju (medicini).

[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

[pmid18505576-6] 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. DOI:10.1186/1754-9493-2-13. PMC 2429901. PMID 18505576.

[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.

[katzung10-8] 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.

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