Adrenergic beta-antagonist

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Adrenergic beta-receptor blockaders (beta-blockers) are "drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety".[1]

Beta-blockers vary within the class regarding their properties. Beta-blockers that have low intrinsic sympathomimetic activity (ISA), low membrane stabilizing activity, high beta 1-selectivity, and high lipophilicity may be more effective.[2]

Pharmacogenomics

Regarding the treatment of heart failure, there is conflicting evidence whether beta-blockers are as effective in African-American patients as in Anglo patients.[3] This may be due to a polymorphism in African-American patients of the G-protein-coupled receptor kinase (GRK5) (OMIM) that confers a natural "genetic beta-blockade".[4]

Variation adrenergic receptor genotype may also influence effectiveness.[5]

Beta-blockers such as metoprolol that are metabolized by cytochrome P-450 2D6 allele and may have more drug interactions[6] and inherited variations in metabolism.[7]

Availability

Generically available beta-blockers include:[8][9]

Generic beta-blockers with beta 1-selectivity:[2]

Generic beta-blockers with intrinsic sympathomimetic activity (less resting bradycardia and lipid changes):[8]

  • Acebutolol
  • Pindolol

Generic beta-blockers with alpha blocking activity (more orthostatic hypotension):[8]

Clinical uses

The individual beta-blockers have been compared in the treatment of various diseases.[10]

Coronary heart disease

For more information, see: Coronary heart disease.

A meta-analysis has concluded that metoprolol may be the best beta-blocker for secondary prevention of myocardial infarction.[2]

Heart failure

For more information, see: Heart failure.

Two cohort studies suggest that atenolol and carvedilol may be more effect than metoprolol for the treatment of heart failure.[11][12]

References

  1. ↑ Anonymous (2024), Adrenergic beta-antagonist (English). Medical Subject Headings. U.S. National Library of Medicine.
  2. ↑ 2.0 2.1 2.2 Soriano JB, Hoes AW, Meems L, Grobbee DE (1997). "Increased survival with beta-blockers: importance of ancillary properties". Prog Cardiovasc Dis 39 (5): 445–56. PMID 9122425. [e]
  3. ↑ Shekelle PG, Rich MW, Morton SC, et al (2003). "Efficacy of angiotensin-converting enzyme inhibitors and beta-blockers in the management of left ventricular systolic dysfunction according to race, gender, and diabetic status: a meta-analysis of major clinical trials". J. Am. Coll. Cardiol. 41 (9): 1529–38. PMID 12742294. [e]
  4. ↑ Liggett, Stephen B et al. 2008. A GRK5 polymorphism that inhibits [beta]-adrenergic receptor signaling is protective in heart failure. Nat Med advanced online publication. http://dx.doi.org/10.1038/nm1750 (Accessed April 29, 2008).
  5. ↑ Zaugg M, Bestmann L, Wacker J, et al (July 2007). "Adrenergic receptor genotype but not perioperative bisoprolol therapy may determine cardiovascular outcome in at-risk patients undergoing surgery with spinal block: the Swiss Beta Blocker in Spinal Anesthesia (BBSA) study: a double-blinded, placebo-controlled, multicenter trial with 1-year follow-up". Anesthesiology 107 (1): 33–44. DOI:10.1097/01.anes.0000267530.62344.a4. PMID 17585213. Research Blogging.
  6. ↑ Onalan O, Cumurcu BE, Bekar L (May 2008). "Complete atrioventricular block associated with concomitant use of metoprolol and paroxetine". Mayo Clin. Proc. 83 (5): 595–9. PMID 18452693. [e]
  7. ↑ Nozawa T, Taguchi M, Tahara K, et al (November 2005). "Influence of CYP2D6 genotype on metoprolol plasma concentration and beta-adrenergic inhibition during long-term treatment: a comparison with bisoprolol". J. Cardiovasc. Pharmacol. 46 (5): 713–20. PMID 16220080. [e]
  8. ↑ 8.0 8.1 8.2 (June 2005) "Drugs for hypertension". Treat Guidel Med Lett 3 (34): 39–48. PMID 15912125. [e]
  9. ↑ (March 2008) "Nebivolol (Bystolic) for hypertension". Med Lett Drugs Ther 50 (1281): 17–9. PMID 18323772. [e]
  10. ↑ Dean L (2007). “Comparing Beta Blockers”, PubMed Clinical Q&A. Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information. “Based on http://www.ohsu.edu/drugeffectiveness/” 
  11. ↑ Kramer JM, Curtis LH, Dupree CS, et al (December 2008). "Comparative effectiveness of beta-blockers in elderly patients with heart failure". Arch. Intern. Med. 168 (22): 2422–8; discussion 2428–32. DOI:10.1001/archinternmed.2008.511. PMID 19064824. Research Blogging.
  12. ↑ Go AS, Yang J, Gurwitz JH, Hsu J, Lane K, Platt R (December 2008). "Comparative effectiveness of different beta-adrenergic antagonists on mortality among adults with heart failure in clinical practice". Arch. Intern. Med. 168 (22): 2415–21. DOI:10.1001/archinternmed.2008.506. PMID 19064823. Research Blogging.
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