Bisoprolol: Wikis

  

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Bisoprolol
Systematic (IUPAC) name
(RS)-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-
3-(isopropylamino)propan-2-ol
Identifiers
CAS number 66722-44-9
ATC code C07AB07
PubChem 2405
DrugBank APRD00257
ChemSpider 2312
Chemical data
Formula C 18H31NO4  
Mol. mass 325.443 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability >90%
Protein binding 30%[1]
Metabolism 50% Hepatic
Half life 10–12 hours[2]
Excretion  ?
Therapeutic considerations
Licence data

US FDA:link

Pregnancy cat. C(AU) C(US)
Legal status Prescription only
Routes oral
 Yes check.svgY(what is this?)  (verify)

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

Clinical use

Bisoprolol is a beta-adrenoceptor blocking drug (beta-blocker).

Many beta-blockers are now available and in general they are all equally effective. There are, however, differences between them which may affect choice in treating particular diseases or individual patients.

Beta-blockers with a relatively short duration of action have to be given two or three times daily. Many of these are, however, available in modified-release formulations so that administration once daily is adequate for hypertension. For angina twice-daily treatment may sometimes be needed even with a modified-release formulation. Some beta-blockers such as atenolol, bisoprolol, carvedilol, celiprolol, and nadolol have an intrinsically longer duration of action and need to be given only once daily.

Cautions

Beta-blockers can precipitate asthma and this effect can be dangerous. Beta-blockers should be avoided in patients with a history of asthma or bronchospasm; if there is no alternative, a cardioselective beta-blocker can be used with extreme caution under specialist supervision. Atenolol, bisoprolol, metoprolol, nebivolol, and (to a lesser extent) acebutolol, have less effect on the beta2 (bronchial) receptors and are, therefore, relatively cardioselective, but they are not cardiospecific. They have a lesser effect on airways resistance but are not free of this side-effect.

Side effects

Beta-blockers are also associated with fatigue, coldness of the extremities (may be less common with those with ISA, see above), and sleep disturbances with nightmares (may be less common with the water-soluble beta-blockers, see above).

Indications

Bisoprolol (Concor,[3] Zebeta,[4] Concore,[5] Monocor[6]) 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.[7]

Pharmacology and biochemistry

Selectivity of various β-blockers

β1 Selectivity

Bisoprolol has a higher degree of β1-selectivity compared to other β1-selective β-blockers such as atenolol, metoprolol and betaxolol.[8][9][10][11][12][13][14][15][16][17] However Nebivolol is approximately 3.5 times more β1-selective.[18][19]

Antihypertensive effect

Bisoprolol has a stronger antihypertensive effect than propranolol.[8]

Cardioprotection

Bisoprolol in animal models has been shown to be cardioprotective.[8]

Renin-angiotensin system

Bisoprolol inhibits renin secretion by about 65% and tachycardia by about 35%.[8]

Pharmacology of side-effects

In animal testing bisoprolol compared to propranolol has shown less sedative effects and only slightly reduced glucose tolerance.[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. ^ Bisoprolol at Merck Serono [1]
  4. ^ "Prescription Drugs: Zebeta". Physicians' Desktop Reference. http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=Zeb1667.html&contentName=Zebeta&contentId=651. Retrieved 2007-12-23.  
  5. ^ "Pharmaceuticals". Merck Philippines. http://www.merck.ph/index.php?option=com_content&task=view&id=23&Itemid=48. Retrieved 2008-01-01.  
  6. ^ "Products: Monocor". Biovail Corporation. http://www.biovail.com/english/products/default.asp?s=1&product=10&viewer=patient&state=displayProduct&country=Canada. Retrieved 2007-12-23.  
  7. ^ Ratiopharm packing slip, dated 03.08.2006
  8. ^ 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.  
  9. ^ 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.  
  10. ^ 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.  
  11. ^ 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.  
  12. ^ 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.  
  13. ^ 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. doi:10.1016/0014-2999(86)90666-7. PMID 3011461.  
  14. ^ 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. doi:10.1097/00005344-198406060-00024. PMID 6084774.  
  15. ^ 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. http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0160-2446&volume=36&issue=4&spage=466.  
  16. ^ 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. doi:10.1023/A:1007784109255. PMID 10372227. http://www.kluweronline.com/art.pdf?issn=0920-3206&volume=13&page=123.  
  17. ^ 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.  
  18. ^ 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.  
  19. ^ 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. doi:10.1046/j.1365-2710.2003.00477.x. PMID 12795776.  
  20. ^ Lettenbaur H. EMD 33 512 (Bisoprolol): Prüfung der Wirkung auf die Serumglukosekonzentration an Ratten im Vergleich zu Propranolol. Merck KGaA, Darmstadt, 1979.

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