Bisoprolol

Bisoprolol
IUPAC ime
	(RS)-1-(4-[(2-izopropoksietoksi)metil]fenoksi)-; 3-(izopropilamino)propan-2-ol
Klinički podaci
Prodajno ime	Zebeta
Drugs.com	Monografija
MedlinePlus	a693024
Podaci o licenci	US FDA: Bisoprolol;
Kategorija trudnoće	AU: C ; US: C (Mogući rizik) ; ;
Način primene	oralno
Pravni status
Pravni status	Rx-only;
Farmakokinetički podaci
Bioraspoloživost	>90%
Vezivanje proteina	30%
Metabolizam	50% Hepatički
Poluvreme eliminacije	10–12 sata
Identifikatori
CAS broj	66722-44-9
ATC kod	C07AB07 (WHO)
PubChem	CID 2405
DrugBank	DB00612
ChemSpider	2312
UNII	Y41JS2NL6U
KEGG	D02342
ChEBI	CHEBI:3127
ChEMBL	CHEMBL645
Hemijski podaci
Formula	C18H31NO4
Molarna masa	325,443 g/mol
	SMILES O(c1ccc(cc1)COCCOC(C)C)CC(O)CNC(C)C; ;
	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 ;

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.^[3]

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.^[4]^[5]^[6] 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.^[7]^[8]^[9]

Reference

^ 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.”. Приступљено 17. 03. 2012.
^ Rosenberg, J.; Gustafsson, F. (2008). „Bisoprolol for congestive heart failure”. Expert Opinion on Pharmacotherapy. 9 (2): 293—300. PMID 18201151. doi:10.1517/14656566.9.2.293.
^ 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.; Lechat, P. (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. PMID 20354032. doi:10.1093/eurjhf/hfq038.

Spoljašnje veze

Monocor Prescribing information (PDF)

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid2439794-1] 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.

[pmid2439789-2] Leopold G (1986). „Balanced pharmacokinetics and metabolism of bisoprolol”. J. Cardiovasc. Pharmacol. 8 Suppl 11: S16—20. PMID 2439789.

[3] „Bisoprolol Official FDA information, side effects and uses.”. Приступљено 17. 03. 2012.

[r31-4] Rosenberg, J.; Gustafsson, F. (2008). „Bisoprolol for congestive heart failure”. Expert Opinion on Pharmacotherapy. 9 (2): 293—300. PMID 18201151. doi:10.1517/14656566.9.2.293.

[r22-5] 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.

[r32-6] 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.

[pmid7923660-7] „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.

[pmid20354334-8] 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.

[pmid20354032-9] Castagno, D.; Jhund, P. S.; McMurray, J. J. V.; Lewsey, J. D.; Erdmann, E.; Zannad, F.; Remme, W. J.; Lopez-Sendon, J. L.; Lechat, P. (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. PMID 20354032. doi:10.1093/eurjhf/hfq038.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]