Bisoprolol

Bisoprolol
(IUPAC) ime
	(RS)-1-(4-[(2-izopropoksietoksi)metil]fenoksi)-; 3-(izopropilamino)propan-2-ol
Klinički podaci
Robne marke	Zebeta
AHFS/Drugs.com	Monografija
MedlinePlus	a693024
Identifikatori
CAS broj	66722-44-9
ATC kod	C07AB07
PubChem	2405
DrugBank	DB00612
ChemSpider	2312
UNII	Y41JS2NL6U
KEGG	D02342
ChEBI	CHEBI:3127
ChEMBL	CHEMBL645
Hemijski podaci
Formula	C18H31NO4
Mol. masa	325,443 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3 ; Key: VHYCDWMUTMEGQY-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	>90%
Vezivanje za proteine plazme	30%
Metabolizam	50% Hepatički
Poluvreme eliminacije	10–12 sata
Farmakoinformacioni podaci
Licenca	US FDA:link
Trudnoća	C(AU) C(US)
Pravni status	℞ Prescription only
Način primene	oralno

Bisoprolol je lek iz grupe beta blokatora, klase lekova koji se prvenstveno koriste za tretiranje kardiovaskularnih bolesti. On je selektivan za tip β1 adrenergičkog receptora. FDA je odobrila zahtev kompanije Duramed farmaceuti za Zebeta oralne tablete (Bisoprolol fumarat) 31. jula 1992. Od tog vremena niz drugih kompanija su dobile odobrenje za proizvodnju ovog leka.^[8]

Klinička upotreba

Bisoprolol se koristi za tretiranje: visokog krvnog pritiska (hipertenzije), redukovanog protoka krvi do srca i kongestivnog zatajenja srca. On služi kao preventivni tretman pre, i kao primarni tretman nakon srčanog udara. Njime se umanjuju šanse od ponovnog udara.^[9]^[10]^[11] U slučaju srčane ishemije lek se koristi za redukovanje aktivnosti srčanog mišića i stoga umanjenje potražnja za kiseonikom i nutrijentima, tako da redukovano snabdevanje krvi još uvek može da bude dovoljno.^[12]^[13]^[14]

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
↑ Bühring KU, Sailer H, Faro HP, Leopold G, Pabst J, Garbe A (1986). „Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans”. J. Cardiovasc. Pharmacol. 8 Suppl 11: S21–8. PMID 2439794.
↑ Leopold G (1986). „Balanced pharmacokinetics and metabolism of bisoprolol”. J. Cardiovasc. Pharmacol. 8 Suppl 11: S16–20. PMID 2439789.
↑ „Bisoprolol Official FDA information, side effects and uses.”. Pristupljeno 2012-03-17.
↑ Rosenberg, J.; Gustafsson, F. (2008). „Bisoprolol for congestive heart failure”. Expert Opinion on Pharmacotherapy 9 (2): 293–300. DOI:10.1517/14656566.9.2.293. PMID 18201151.
↑ Amabile, G.; Serradimigni, A. (1987). „Comparison of bisoprolol with nifedipine for treatment of essential hypertension in the elderly: Comparative double-blind trial”. European heart journal 8 Suppl M: 65–69. PMID 2967187.
↑ Thadani, U. (2004). „Current medical management of chronic stable angina”. Journal of cardiovascular pharmacology and therapeutics 9 Suppl 1: S11–S29; quiz S29–9. PMID 15378129.
↑ „A randomized trial of beta-blockade in heart failure. The Cardiac Insufficiency Bisoprolol Study (CIBIS). CIBIS Investigators and Committees”. Circulation 90 (4): 1765–1773. 1994. PMID 7923660.
↑ Konishi, M.; Haraguchi, G.; Kimura, S.; Inagaki, H.; Kawabata, M.; Hachiya, H.; Hirao, K.; Isobe, M. (2010). „Comparative effects of carvedilol vs bisoprolol for severe congestive heart failure”. Circulation journal : official journal of the Japanese Circulation Society 74 (6): 1127–1134. PMID 20354334.
↑ Castagno, D.; Jhund, P. S.; McMurray, J. J. V.; Lewsey, J. D.; Erdmann, E.; Zannad, F.; Remme, W. J.; Lopez-Sendon, J. L. i dr.. (2010). „Improved survival with bisoprolol in patients with heart failure and renal impairment: An analysis of the cardiac insufficiency bisoprolol study II (CIBIS-II) trial”. European Journal of Heart Failure 12 (6): 607–616. DOI:10.1093/eurjhf/hfq038. PMID 20354032.

Vanjske veze

Monocor Prescribing information Arhivirano 2009-02-10 na Wayback Machine-u (PDF)

[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

[pmid2439794-6] Bühring KU, Sailer H, Faro HP, Leopold G, Pabst J, Garbe A (1986). „Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans”. J. Cardiovasc. Pharmacol. 8 Suppl 11: S21–8. PMID 2439794.

[pmid2439789-7] Leopold G (1986). „Balanced pharmacokinetics and metabolism of bisoprolol”. J. Cardiovasc. Pharmacol. 8 Suppl 11: S16–20. PMID 2439789.

[8] „Bisoprolol Official FDA information, side effects and uses.”. Pristupljeno 2012-03-17.

[r31-9] Rosenberg, J.; Gustafsson, F. (2008). „Bisoprolol for congestive heart failure”. Expert Opinion on Pharmacotherapy 9 (2): 293–300. DOI:10.1517/14656566.9.2.293. PMID 18201151.

[r22-10] Amabile, G.; Serradimigni, A. (1987). „Comparison of bisoprolol with nifedipine for treatment of essential hypertension in the elderly: Comparative double-blind trial”. European heart journal 8 Suppl M: 65–69. PMID 2967187.

[r32-11] Thadani, U. (2004). „Current medical management of chronic stable angina”. Journal of cardiovascular pharmacology and therapeutics 9 Suppl 1: S11–S29; quiz S29–9. PMID 15378129.

[PMID7923660-12] „A randomized trial of beta-blockade in heart failure. The Cardiac Insufficiency Bisoprolol Study (CIBIS). CIBIS Investigators and Committees”. Circulation 90 (4): 1765–1773. 1994. PMID 7923660.

[PMID20354334-13] Konishi, M.; Haraguchi, G.; Kimura, S.; Inagaki, H.; Kawabata, M.; Hachiya, H.; Hirao, K.; Isobe, M. (2010). „Comparative effects of carvedilol vs bisoprolol for severe congestive heart failure”. Circulation journal : official journal of the Japanese Circulation Society 74 (6): 1127–1134. PMID 20354334.

[PMID20354032-14] Castagno, D.; Jhund, P. S.; McMurray, J. J. V.; Lewsey, J. D.; Erdmann, E.; Zannad, F.; Remme, W. J.; Lopez-Sendon, J. L. i dr.. (2010). „Improved survival with bisoprolol in patients with heart failure and renal impairment: An analysis of the cardiac insufficiency bisoprolol study II (CIBIS-II) trial”. European Journal of Heart Failure 12 (6): 607–616. DOI:10.1093/eurjhf/hfq038. PMID 20354032.

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