Adrenergic beta-antagonist: Difference between revisions
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Beta-blockers vary within the class regarding their properties. Beta-blockers that have low intrinsic sympathomimetic activity (ISA), low membrane stabilizing activity, high [[Adrenergic receptor|beta 1-selectivity]], and high lipophilicity may be more effective.<ref name="pmid9122425">{{cite journal |author=Soriano JB, Hoes AW, Meems L, Grobbee DE |title=Increased survival with beta-blockers: importance of ancillary properties |journal=Prog Cardiovasc Dis |volume=39 |issue=5 |pages=445–56 |year=1997 |pmid=9122425 |doi= |url=http://linkinghub.elsevier.com/retrieve/pii/S0033-0620(97)80039-4 |issn=}}</ref> A [[meta-analysis]] has concluded that [[metoprolol]] may be the best beta-blocker for [[secondary prevention]] of [[myocardial infarction]].<ref name="pmid9122425"/> | Beta-blockers vary within the class regarding their properties. Beta-blockers that have low intrinsic sympathomimetic activity (ISA), low membrane stabilizing activity, high [[Adrenergic receptor|beta 1-selectivity]], and high lipophilicity may be more effective.<ref name="pmid9122425">{{cite journal |author=Soriano JB, Hoes AW, Meems L, Grobbee DE |title=Increased survival with beta-blockers: importance of ancillary properties |journal=Prog Cardiovasc Dis |volume=39 |issue=5 |pages=445–56 |year=1997 |pmid=9122425 |doi= |url=http://linkinghub.elsevier.com/retrieve/pii/S0033-0620(97)80039-4 |issn=}}</ref> A [[meta-analysis]] has concluded that [[metoprolol]] may be the best beta-blocker for [[secondary prevention]] of [[myocardial infarction]].<ref name="pmid9122425"/> | ||
==Pharmacogenomics== | |||
Regarding he treatment of heart failure, there is conflicting evidence whether [[beta-blocker]]s are as effective in African-American patients as in Anglo patients.<ref name="pmid12742294">{{cite journal |author=Shekelle PG, Rich MW, Morton SC, ''et al'' |title=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 |journal=J. Am. Coll. Cardiol. |volume=41 |issue=9 |pages=1529–38 |year=2003 |pmid=12742294 |doi=}}</ref> This may be due to a polymorphism in African-American patients of the G protein–coupled [[cell surface receptor]] kinase (GRK5) ([http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=600870 OMIM]) that confers a natural "genetic beta-blockade".<ref name="doi10.1038/nm1750">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).</ref> | |||
==Availability== | ==Availability== | ||
Revision as of 07:47, 3 November 2008
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] A meta-analysis has concluded that metoprolol may be the best beta-blocker for secondary prevention of myocardial infarction.[2]
Pharmacogenomics
Regarding he 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]
Availability
Generically available beta-blockers include:[5][6]
- 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)
Generic beta-blockers with intrinsic sympathomimetic activity (less resting bradycardia and lipid changes):[5]
- Acebutolol
- Pindolol
Generic beta-blockers with alpha blocking activity (more orthostatic hypotension):[5]
- Carvedilol
- Labetalol
Clinical uses
The individual beta-blockers have been compared in the treatment of various diseases.[7]
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).
- ↑ 5.0 5.1 5.2 (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/”