Karvedilol

Karvedilol
(IUPAC) ime
	(±)-[3-(9H-karbazol-4-iloksi)-2-hidroksipropil][2-(2-metoksifenoksi)etil]amin
Klinički podaci
Robne marke	Koreg
AHFS/Drugs.com	Monografija
MedlinePlus	a697042
Identifikatori
CAS broj	72956-09-3
ATC kod	C07AG02
PubChem	2585
DrugBank	DB01136
ChemSpider	2487
UNII	0K47UL67F2
KEGG	D00255
ChEBI	CHEBI:3441
ChEMBL	CHEMBL723
Hemijski podaci
Formula	C24H26N2O4
Mol. masa	406,474
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3 ; Key: OGHNVEJMJSYVRP-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	25–35%
Vezivanje za proteine plazme	98%
Metabolizam	Jetra (CYP2D6, CYP2C9)
Poluvreme eliminacije	7–10 sata
Izlučivanje	Urin (16%), Izmet (60%)
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Karvedilol je neselektivni beta blokator/alfa-1 blokator koji se koristi za tretman kongestivnog zatajenja srca. On je u prodaji pod brojnim imenima uključujući Karvil, Koreg, Dilatrend, Koronis, Eukardik, i Karlok kao generički lek,^[6]. Karvedilol ima znatnu ulogu u tretmanu kongestivnog zatajenja srca.

Farmakologija

Karvedilol je beta blokator (β₁, β₂) i alfa blokator (α₁):

Norepinefrin stimuliše nerve koji kontrolišu mišiće srca vezivanjem za β₁- i β₂-adrenergičke receptora. Karvedilol blokira vezivanje tih receptora,^[7] čime se usporava srčani ritam i redukuje sila kojom srce pumpa. Time se snižava krvni pritisak, te se umanjuje količina rada srca.
Norepinefrin se takođe vezuje za α₁-adrenergičke receptore na krvnim sudovima, uzrokujući njihovu konstrikciju i povišenje krvnog pritiska. Karvedilol blokira vezivanje agonista za α₁-adrenergičke receptore,^[8] čime dodatno snižava krvni pritisak.

Reference

↑ 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
↑ Press Release, FDA Approves First Generic Versions of Coreg, U.S. Food and Drug Administration, Sep. 5, 2007
↑ Stafylas PC, Sarafidis PA (2008). „Carvedilol in hypertension treatment”. Vasc Health Risk Manag 4 (1): 23–30. DOI:10.2147/vhrm.2008.04.01.23. PMC 2464772. PMID 18629377.
↑ Othman AA, Tenero DM, Boyle DA, Eddington ND, Fossler MJ (2007). „Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate”. AAPS J 9 (2): E208–18. DOI:10.1208/aapsj0902023. PMC 2751410. PMID 17614362. Arhivirano iz originala na datum 2012-10-15. Pristupljeno 2014-04-05.

Literatura

Subhashis Chakraborty, Dali Shukla, Brahmeshwar Mishra & Sanjay Singh.Clinical updates on carvedilol: a first choice beta-blocker in the treatment of cardiovascular diseases. Expert Opin Drug Metab Toxicol. 2010 Feb;6(2):237-50. DOI 10.1517/17425250903540220, PMID 20073998

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Coreg CR official website Arhivirano 2013-02-16 na Wayback Machine-u
Physicians Desk Reference Info on Carvedilol

[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] Press Release, FDA Approves First Generic Versions of Coreg, U.S. Food and Drug Administration, Sep. 5, 2007

[pmid18629377-7] Stafylas PC, Sarafidis PA (2008). „Carvedilol in hypertension treatment”. Vasc Health Risk Manag 4 (1): 23–30. DOI:10.2147/vhrm.2008.04.01.23. PMC 2464772. PMID 18629377.

[pmid17614362-8] Othman AA, Tenero DM, Boyle DA, Eddington ND, Fossler MJ (2007). „Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate”. AAPS J 9 (2): E208–18. DOI:10.1208/aapsj0902023. PMC 2751410. PMID 17614362. Arhivirano iz originala na datum 2012-10-15. Pristupljeno 2014-04-05.

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