Bisoprolol

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Bisoprolol
Systematic (IUPAC) name
1-[4-[2-(1-methylethoxy)ethoxymethyl]
phenoxy]-3-(1-methylethylamino)propan-2-ol
Identifiers
CAS number 66722-44-9
ATC code C07AB07
PubChem 2405
DrugBank APRD00257
Chemical data
Formula C18H31NO4 
Mol. mass 325.443 g/mol
Pharmacokinetic data
Bioavailability >90%
Protein binding 30%[1]
Metabolism 50% Hepatic
Half life 10-12hours[2]
Excretion  ?
Therapeutic considerations
Licence data

US
Pregnancy cat.

C(AU) C(US)
Legal status

℞ Prescription only
Routes oral

Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type β1 adrenergic receptor blocker.

Contents

Pharmacology and biochemistry

β1 Selectivity

Bisoprolol has a higher degree of β1-selectivity compared to other β1-selective β-blockers such as atenolol, metoprolol and betaxolol.[3][4][5][6][7][8][9][10][11][12] However Nebivolol is approximately 3.5 times more β1-selective.[13][14]

Antihypertensive effect

Bisoprolol has a stronger antihypertensive effect than propranolol.[3]

Cardioprotection

Bisoprolol in animal models has been shown to be cardioprotective.[3]

Renin-angiotensin system

Bisoprolol inhibits renin secretion by about 65% and tachycardia by about 35%.[3]

Pharmacology of side-effects

In animal testing bisoprolol compared to propranolol has shown less sedative effects and only slightly reduced glucose tolerance.[15]

Indications

Bisoprolol (Concor,[16] Zebeta,[17] Concore,[18] Monocor[19]) can be used to treat cardiovascular diseases such as hypertension, coronary heart disease, arrhythmias, ischemic heart diseases and treatment of myocardial infarction after the acute event. Patients with compensated congestive heart failure may be treated with Bisoprolol as a comedication (usually together with an ACE inhibitor, a diuretic and a digitalis-glycosid, if indicated). In patients with congestive heart failure, it reduces the need for and the consumption of oxygen of the heart muscle. It is very important to start with low doses, as bisoprolol reduces also the muscular power of the heart, which is an undesired effect in congestive heart failure.

The drug is also used to treat other conditions, including dysautonomia, anxiety and hyperthyroidism (over active thyroid gland).

Bisoprolol will give a positive result in doping tests.[20]

References

  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. 
  2. ^ Leopold G (1986). "Balanced pharmacokinetics and metabolism of bisoprolol". J. Cardiovasc. Pharmacol. 8 Suppl 11: S16–20. PMID 2439789. 
  3. ^ a b c d Harting J, Becker KH, Bergmann R, et al (February 1986). "Pharmacodynamic profile of the selective beta 1-adrenoceptor antagonist bisoprolol". Arzneimittelforschung 36 (2): 200–8. PMID 2870720. 
  4. ^ Haeusler G, Schliep HJ, Schelling P, et al (1986). "High beta 1-selectivity and favourable pharmacokinetics as the outstanding properties of bisoprolol". J. Cardiovasc. Pharmacol. 8 Suppl 11: S2–15. PMID 2439793. 
  5. ^ Kaumann AJ, Lemoine H (October 1985). "Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency". Naunyn Schmiedebergs Arch. Pharmacol. 331 (1): 27–39. PMID 2866449. 
  6. ^ Klockow M, Greiner HE, Haase A, Schmitges CJ, Seyfried C (February 1986). "Studies on the receptor profile of bisoprolol". Arzneimittelforschung 36 (2): 197–200. PMID 2870719. 
  7. ^ Manalan AS, Besch HR, Watanabe AM (August 1981). "Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular myocardium and lung". Circ. Res. 49 (2): 326–36. PMID 6113900. 
  8. ^ Schliep HJ, Schulze E, Harting J, Haeusler G (April 1986). "Antagonistic effects of bisoprolol on several beta-adrenoceptor-mediated actions in anaesthetized cats". Eur. J. Pharmacol. 123 (2): 253–61. PMID 3011461. 
  9. ^ Schliep HJ, Harting J (1984). "Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and guinea pigs". J. Cardiovasc. Pharmacol. 6 (6): 1156–60. PMID 6084774. 
  10. ^ Schnabel P, Maack C, Mies F, Tyroller S, Scheer A, Böhm M (October 2000). "Binding properties of beta-blockers at recombinant beta1-, beta2-, and beta3-adrenoceptors". J. Cardiovasc. Pharmacol. 36 (4): 466–71. PMID 11026647. 
  11. ^ Smith C, Teitler M (April 1999). "Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors". Cardiovasc Drugs Ther 13 (2): 123–6. PMID 10372227. 
  12. ^ Wellstein A, Palm D, Belz GG (1986). "Affinity and selectivity of beta-adrenoceptor antagonists in vitro". J. Cardiovasc. Pharmacol. 8 Suppl 11: S36–40. PMID 2439796. 
  13. ^ Bundkirchen A, Brixius K, Bölck B, Nguyen Q, Schwinger RH (January 2003). "Beta 1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studies". Eur. J. Pharmacol. 460 (1): 19–26. doi:10.1016/S0014-2999(02)02875-3. PMID 12535855. 
  14. ^ Nuttall SL, Routledge HC, Kendall MJ (June 2003). "A comparison of the beta1-selectivity of three beta1-selective beta-blockers". J Clin Pharm Ther 28 (3): 179–86. PMID 12795776. 
  15. ^ Lettenbaur H. EMD 33 512 (Bisoprolol): Prüfung der Wirkung auf die Serumglukosekonzentration an Ratten im Vergleich zu Propranolol. Merck KGaA, Darmstadt, 1979.
  16. ^ Bisoprolol at Merck Serono [1]
  17. ^ "Prescription Drugs: Zebeta". Physicians' Desktop Reference. Retrieved on 2007-12-23.
  18. ^ "Pharmaceuticals". Merck Philippines. Retrieved on 2008-01-01.
  19. ^ "Products: Monocor". Biovail Corporation. Retrieved on 2007-12-23.
  20. ^ Ratiopharm packing slip, dated 03.08.2006

External links


v • d • e
Adrenergic antagonists
α
Non-selective α
reversible (Phentolamine) · irreversible (Phenoxybenzamine)
β
β1 selective
(cardioselective)
Atenolol · Acebutolol · Celiprolol · Betaxolol · Bisoprolol · Esmolol · Metoprolol · Nebivolol
Mixed α1/β

Wikipedia content modification information:

  • This page was last modified on 14 August 2008, at 19:52.

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