Bisoprolol

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Bisoprolol
200px
Systematic (IUPAC) name
(RS)-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-
3-(isopropylamino)propan-2-ol
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration		 oral
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability >90%
Protein binding 30%[1]
Metabolism 50% Hepatic
Biological half-life 10–12 hours[2]
Identifiers
CAS Number 66722-44-9
ATC code C07AB07 (WHO)
PubChem CID 2405
DrugBank APRD00257
ChemSpider 2312
Chemical data
Formula C18H31NO4
Molar mass 325.443 g/mol[[Script error: No such module "String".]]
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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.

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

File:Bisoprolol selectivity.svg
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]

Overdosage

Acute overdosage is often manifested by nausea, emesis, asthenia, diarrhea, bradycardia and hypotension. Plasma, serum or blood concentrations of bisoprolol may be measured to confirm a diagnosis of poisoning in hospitalized patients or to aid in the medicolegal investigation of fatalities.[21]

References

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External links

de:Bisoprolol

es:Bisoprolol fr:Bisoprolol hr:Bisoprolol hu:Bizoprolol nl:Bisoprolol pl:Bisoprolol pt:Bisoprolol ru:Бисопролол fi:Bisoprololi

uk:Бісопролол
  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. Retrieved 2007-12-23. 
  5. ↑ "Pharmaceuticals". Merck Philippines. Retrieved 2008-01-01. 
  6. ↑ "Products: Monocor". Biovail Corporation. Retrieved 2007-12-23. 
  7. ↑ Ratiopharm packing slip, dated 03.08.2006
  8. ↑ 8.0 8.1 8.2 8.3 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  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. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  11. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  12. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  13. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  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. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  16. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  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. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  19. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  20. ↑ Lettenbaur H. EMD 33 512 (Bisoprolol): Prüfung der Wirkung auf die Serumglukosekonzentration an Ratten im Vergleich zu Propranolol. Merck KGaA, Darmstadt, 1979.
  21. ↑ R. Baselt, Disposition of Toxic Drugs and Chemicals in Man, 8th edition, Biomedical Publications, Foster City, CA, 2008, pp. 165-166.
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