Adrenergic beta-antagonist
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 cell surface receptor kinase (GRK5) (OMIM) that confers a natural "genetic beta-blockade".[4]
Variation adrenergic receptor genotype may also influence effectiveness.[5]
Availability
Generically available beta-blockers include:[6][7]
- Betaxolol
- Nadolol
- Propranolol
- Timolol
Generic beta-blockers with beta 1-selectivity:[2]
- Atenolol (less lipid soluble; renally excreted)
- Bisoprolol
- Metoprolol (hepatically metabolized by cytochrome P-450 2D6 allele)
Generic beta-blockers with intrinsic sympathomimetic activity (less resting bradycardia and lipid changes):[6]
- Acebutolol
- Pindolol
Generic beta-blockers with alpha blocking activity (more orthostatic hypotension):[6]
- Carvedilol
- Labetalol
Clinical uses
The individual beta-blockers have been compared in the treatment of various diseases.[8]
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
Two cohort studies suggest that atenolol and carvedilol may be more effect than metoprolol for the treatment of heart failure.[9][10]
References
- ↑ Anonymous (2024), Adrenergic beta-antagonist (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ 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]
- ↑ 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]
- ↑ 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).
- ↑ 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.
- ↑ 6.0 6.1 6.2 (June 2005) "Drugs for hypertension". Treat Guidel Med Lett 3 (34): 39–48. PMID 15912125. [e]
- ↑ (March 2008) "Nebivolol (Bystolic) for hypertension". Med Lett Drugs Ther 50 (1281): 17–9. PMID 18323772. [e]
- ↑ 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/”
- ↑ 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.
- ↑ 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.