Acebutolol

Acebutolol
(IUPAC) ime
	(RS)-N-(3-acetil-4-[2-hidroksi-3-(propan-2-ilamino)propoksi]fenil)butanamid
Klinički podaci
Robne marke	Sectral
AHFS/Drugs.com	Monografija
MedlinePlus	a687003
Identifikatori
CAS broj	37517-30-9
ATC kod	C07AB04
PubChem	1978
DrugBank	DB01193
ChemSpider	1901
UNII	67P356D8GH
KEGG	D02338
ChEBI	CHEBI:2379
ChEMBL	CHEMBL642
Hemijski podaci
Formula	C18H28N2O4
Mol. masa	336,426 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C18H28N2O4/c1-5-6-18(23)20-14-7-8-17(16(9-14)13(4)21)24-11-15(22)10-19-12(2)3/h7-9,12,15,19,22H,5-6,10-11H2,1-4H3,(H,20,23) ; Key: GOEMGAFJFRBGGG-UHFFFAOYSA-N
Fizički podaci
Tačka topljenja	121 °C (250 °F)
Farmakokinetički podaci
Bioraspoloživost	40% (opseg 35 do 50%)
Metabolizam	Hepatički
Poluvreme eliminacije	3-4 sata (lek); 8-13 sata (aktivni metabolit)
Izlučivanje	Renalno: 30%; Bilijarno: 60%
Farmakoinformacioni podaci
Licenca	US FDA:link
Trudnoća	C(AU) B(US)
Pravni status	℞ Prescription only
Način primene	oralno, iv

Acebutolol (Sektral, Prent) je beta blokator za tretman hipertenzije i aritmija.^[6]^[7]

Farmakologija

Acebutolol je kardioselektivni beta blokator sa intrinsičnom simpatomimetičkom aktivnošću. On je stoga podesniji od beta blokatora koji nisu kardioselektivni za primenu kod pacijenata sa astmom ili hroničnam opstruktivnom bolešću pluća. U dozama manjim od 800 mg dnevno njegovi konstrikcini efekti na bronhijalnom sistemu i glatkim mišićima krvnih sudova su samo 10% do 30% nivoa izazvanih propranololskim tretmanom. Postoje eksperimentalni podaci da se kardioselektivna svojstva gube pri dozama od 800 mg/dan i većim.

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
↑ Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
↑ Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.

Literatura

Spoljašnje veze

	Portal Medicina
	Portal Hemija

AHFS Database

[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

[Goodman_Gilman-6] Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.

[PDR-7] Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.

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