beta adrenergic receptor antagonist (beta-blocker)
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Introduction
A molecule/drug that blocks the effect of catecholamines on beta adrenergic receptors, producing a decrease in heart rate & oxygen demand in the myocardium.
Indications
- coronary artery disease
- states of catecholamine excess
- thyrotoxicosis
- pheochromocytoma
- may leave alpha adrenergic effects unopposed
- tachyarrhythmias
- congenital long QT syndrome (may prevent episodes of torsades de pointes)
- neurocardiogenic syncope
- hypertension#
- treatment of heart failure
- hypertrophic cardiomyopathy[16]
- dissecting aortic aneurysm
- mitral valve prolapse
- esophageal varices
- migraine prophylaxis
- treatment of anxiety
- increased intraocular pressure, glaucoma
- essential tremor[16]
- use of beta-blockers is associated with less arthragias & less use of opioids & other analgesics for symptomatic large-joint osteoarthritis[18]
* no advantage of beta-blockers for preventing myocardial infarction or death when used to treat hypertension[9] or in patients with stable coronary artery disease or cardiovascular risk factors[14]
# not 1st line for uncomplicated hypertension[12]
Contraindications
- asthma, symptomatic reactive airways disease
- symptomatic bradycardia
- high degree AV block
- uncontrolled or unstable heart failure
- severe peripheral vascular disease
- Raynaud's phenomenon
- pheochromocytoma
- likely OK in 1st trimester of pregnancy[19]
Caution:
- when discontinuing beta blocker, taper over 1-2 weeks
- intermittent claudication
- may mask signs & symptoms of hypoglycemia
- use with caution in patients at risk for anaphylaxis
- may inhibit effects or epinephrine & make anaphylaxis more severe & difficult to treat[7]
Adverse effects
- bronchospasm
- bradycardia
- decreased cardiac output
- negative inotropic effects
- abrupt withdrawal may precipitate arrhythmia or angina
- may mask symptoms of hypoglycemia
- unopposed alpha adrenergic activity may potentiate coronary artery vasospasm
- lethargy
- confusion & diminished ability to concentrate
- impotence
- potentiation of Raynaud's phenomenon
- nightmares
- insomnia
- depression is[2], but is not[1][20], & might be[3] an adverse effect of beta-blockers
- may diminish effect of sulfonylureas
- hyperkalemia (extracellular shift of K+)
- metabolic alkalosis
- increased triglycerides
- diminished HDL cholesterol
- may exacerbate psoriasis[4]
- may increase risk of developing diabetes mellitus[5]
- increased cardiovascular mortality directly correlates with magnitude of heart rate slowing when used to treat hypertension[12]
- no fetal heart risk from Mom's beta-blocker usage[17]
- supportive therapy:
- IV access
- continuous cardiac monitoring
- bradycardia
- atropine generally not useful (not vagally mediated)
- glucagon 2-4 mg IV over 1-2 minutes, then start infusion at 2-5 mg/hr (do not exceed 10 mg/hr);
- may cause nausea/vomiting
- monitor for vagally-mediated bradycardia
- ventricular pacing
- hypotension
- calcium gluconate 3-9 g IV through peripheral line
- calcium chloride 1-2 g IV over 10 minutes through a central venous catheter is alternative (caution: sclerosing agent)
- high-dose insulin euglycemia therapy
- intra-aortic balloon pump
- drug adverse effects of beta-adrenergic receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
- alpha-1 adrenergic antagonists: orthostatic hypotension
- amiodarone: symptomatic bradycardia & sinus arrest
- sympathomimetics
- lidocaine serum levels may increase by 20-30%
- methacholine
- methyldopa (paradoxical hypertensive response to stress)
- NSAIDs may interfere with antihypertensive effect
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with thyroid hormone
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfinpyrazone
- drug interaction(s) of beta-adrenergic receptor antagonists with salicylate
- drug interaction(s) of beta-adrenergic receptor antagonists with rifampin
- drug interaction(s) of beta-adrenergic receptor antagonists with ampicillin
- drug interaction(s) of beta-adrenergic receptor antagonists with colestipol
- drug interaction(s) of beta-adrenergic receptor antagonists with cholestyramine
- drug interaction(s) of beta-adrenergic receptor antagonists with barbiturates
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium salts
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum carbonate
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum hydroxide
- drug interaction(s) of beta-adrenergic receptor antagonists with prazosin
- drug interaction(s) of beta-adrenergic receptor antagonists with lidocaine
- drug interaction(s) of beta-adrenergic receptor antagonists with ergot alkaloids
- drug interaction(s) of beta-adrenergic receptor antagonists with clonidine
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of beta-adrenergic receptor antagonists with quinidine
- drug interaction(s) of beta-adrenergic receptor antagonists with propafenone
- drug interaction(s) of beta-adrenergic receptor antagonists with phenothiazines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of beta-adrenergic receptor antagonists with loop diuretics
- drug interaction(s) of beta-adrenergic receptor antagonists with hydralazine
- drug interaction(s) of beta-adrenergic receptor antagonists with histamine H2 receptor antagonists
- drug interaction(s) of beta-adrenergic receptor antagonists with haloperidol
- drug interaction(s) of beta-adrenergic receptor antagonists with flecainide
- drug interaction(s) of beta-adrenergic receptor antagonists with oral contraceptives
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of spironolactone with beta blockers
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs & antihypertensives
Laboratory
Mechanism of action
- antagonism at beta-adrenergic receptor
- some are specific for the beta-1 adrenergic receptor
- beta-adrenergic receptor blockade leaves unbalanced alpha-adrenergic receptor activity (which tends to increase with age)
- polymorphism in the ADRB2 gene (C & G) alleles associated with different mortality when treated with beta-blocker after acute coronary syndrome
More general terms
More specific terms
- alprenolol
- beta-1 adrenergic receptor antagonist (beta-1 blocker)
- non-specific beta-adrenergic receptor antagonist (non-specific beta-blocker)
- oxprenolol (Coretal)
- vasodilating beta-blocker
Additional terms
Component of
References
- ↑ 1.0 1.1 Medical Knowledge Self Assessment Program (MKSAP) 11, 15, 16. American College of Physicians, Philadelphia 1998 2009, 2012
- ↑ 2.0 2.1 Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 158-59
- ↑ 3.0 3.1 Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 474-75, 491
- ↑ 4.0 4.1 The Washington Manual of Medical Therapeutics, 33rd edition Foster C et al (eds) Lippincott, Williams & Wilkins, Philadelphia, 2010, pg 969
- ↑ 5.0 5.1 Journal Watch 20(9): 72, 2000 Gress TW, Nieto FJ, Shahar E, Wofford MR, Brancati FL. Hypertension and antihypertensive therapy as risk factors for type 2 diabetes mellitus. Atherosclerosis Risk in Communities Study. N Engl J Med. 2000 Mar 30;342(13):905-12. PMID: https://www.ncbi.nlm.nih.gov/pubmed/10738048
- ↑ Prescriber's Letter 12(4): 2005 Comparison of Beta-Blockers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210410&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 Prescriber's Letter 12(7): 2005 Should Some Drugs Be Avoided in Patients at Risk of Anaphylaxis? Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210714&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Lanfear DE, Jones PG, Marsh S, Cresci S, McLeod HL, Spertus JA. Beta2-adrenergic receptor genotype and survival among patients receiving beta-blocker therapy after an acute coronary syndrome. JAMA. 2005 Sep 28;294(12):1526-33. PMID: https://www.ncbi.nlm.nih.gov/pubmed/16189366
- ↑ 9.0 9.1 Lindholm LH, Carlberg B, Samuelsson O. Should beta blockers remain first choice in the treatment of primary hypertension? A meta-analysis. Lancet. 2005 Oct 29-Nov 4;366(9496):1545-53. PMID: https://www.ncbi.nlm.nih.gov/pubmed/16257341
Beevers DG. The end of beta blockers for uncomplicated hypertension? Lancet. 2005 Oct 29-Nov 4;366(9496):1510-2. No abstract available. PMID: https://www.ncbi.nlm.nih.gov/pubmed/16257329 - ↑ Khan N and McAlister FA, Re-examining the efficacy of beta blockers for treatment of hypertension. A meta-analysis. CMAJ 2006; 174:1737 PMID: https://www.ncbi.nlm.nih.gov/pubmed/16754904
- ↑ Prescriber's Letter 14(8): 2007 CHART: AHA Blood Pressure Goals and Treatments Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230801&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 12.0 12.1 12.2 Bangalore S et sl, Relation of beta-blocker-induced heart rate lowering and cardioprotection in hypertension. J Am Coll Cardiol 2008 52:1482 PMID: https://www.ncbi.nlm.nih.gov/pubmed/19017516
Kaplan NM Beta-blockers in hypertension: Adding insult to injury. J Am Coll Cardiol 2008 52:1490 PMID: https://www.ncbi.nlm.nih.gov/pubmed/19017517 - ↑ Prescriber's Letter 14(8): 2007 Comparison of Oral Beta-Blockers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250302&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 14.0 14.1 Bangalore S et al. for the REACH Registry Investigators. beta-blocker use and clinical outcomes in stable outpatients with and without coronary artery disease. JAMA 2012 Oct 3; 308:1340. PMID: https://www.ncbi.nlm.nih.gov/pubmed/23032550
- ↑ Prescriber's Letter 19(12): 2012 CHART: Comparison of Oral Beta-Blockers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=281221&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 16.0 16.1 16.2 Deprecated Reference
- ↑ 17.0 17.1 Boyles S No Fetal Heart Risk from Mom's Beta-Blocker Use - More complete data point finger at maternal confounders. MedPage Today. April 18, 2017
Duan L, Ng A, Chen W et al beta-Blocker exposure in pregnancy and risk of fetal cardiac anomalies. JAMA Intern Med. 2017 Apr 17 PMID: https://www.ncbi.nlm.nih.gov/pubmed/28418448 - ↑ 18.0 18.1 Valdes AM, Abhishek A, Muir K et al Association of Beta-Blocker Use With Less Prevalent Joint Pain and Lower Opioid Requirement in People With Osteoarthritis. Arthritis Care Res (Hoboken). 2017 Jul;69(7):1076-1081. PMID: https://www.ncbi.nlm.nih.gov/pubmed/27696728
- ↑ 19.0 19.1 Bateman BT, Heide-Jorgensen U, Einarsdottir K et al beta-Blocker Use in Pregnancy and the Risk for Congenital Malformations: An International Cohort Study. Ann Intern Med. 2018. Oct 16. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/30326014 <Internet> http://annals.org/aim/article-abstract/2707333/blocker-use-pregnancy-risk-congenital-malformations-international-cohort-study
Ray JG To beta of Not to beta? Very likely K to beta. Ann Intern Med. 2018. Oct 16. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/30326080 <Internet> http://annals.org/aim/article-abstract/2707335/very-likely-ok - ↑ 20.0 20.1 Riemer TG, Villagomez Fuentes LE, Algharably EAE et al Do beta-Blockers Cause Depression? Hypertension. 2021. March 15 PMID: https://www.ncbi.nlm.nih.gov/pubmed/33719510 https://www.ahajournals.org/doi/10.1161/HYPERTENSIONAHA.120.16590
- ↑ DeWitt CR, Waksman JC. Pharmacology, pathophysiology and management of calcium channel blocker and beta-blocker toxicity. Toxicol Rev 2004; 23:223 PMID: https://www.ncbi.nlm.nih.gov/pubmed/15898828