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beta adrenergic receptor antagonist (beta-blocker)

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: 1) coronary artery disease a) myocardial infarction* b) angina pectoris, unstable angina c) secondary prevention in patients with cardiovascular disease 2) states of catecholamine excess a) thyrotoxicosis b) pheochromocytoma c) may leave alpha adrenergic effects unopposed 3) tachyarrhythmias a) supraventricular tachycardia 1] atrial fibrillation 2] atrial flutter 3] sinus tachycardia b) ventricular tachycardia (sotalol) 4) congenital long QT syndrome (may prevent episodes of torsades de pointes) 5) neurocardiogenic syncope 6) hypertension# 7) treatment of heart failure - left ventricular dysfunction 8) hypertrophic cardiomyopathy [16] 9) dissecting aortic aneurysm 10) mitral valve prolapse 11) esophageal varices 12) migraine prophylaxis 13) treatment of anxiety 14) increased intraocular pressure, glaucoma 15) essential tremor [16] 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: 1) asthma, symptomatic reactive airways disease 2) symptomatic bradycardia - high degree AV block - third degree AV block 3) uncontrolled or unstable heart failure - cardiogenic shock 4) severe peripheral vascular disease 5) Raynaud's phenomenon 6) pheochromocytoma 7) likely OK in 1st trimester of pregnancy [19] Caution: 1) when discontinuing beta blocker, taper over 1-2 weeks 2) intermittent claudication 3) may mask signs & symptoms of hypoglycemia 4) use with caution in patients at risk for anaphylaxis - may inhibit effects or epinephrine & make anaphylaxis more severe & difficult to treat [7] Adverse effects: 1) bronchospasm 2) bradycardia 3) decreased cardiac output 4) negative inotropic effects 5) abrupt withdrawal may precipitate arrhythmia or angina 6) may mask symptoms of hypoglycemia 7) unopposed alpha adrenergic activity may potentiate coronary artery vasospasm 8) lethargy 9) confusion & diminished ability to concentrate 10) impotence 11) potentiation of Raynaud's phenomenon 12) nightmares 13) insomnia 14) depression is [2], but is not [1,20], & might be [3] an adverse effect of beta-blockers 15) may diminish effect of sulfonylureas 16) hyperkalemia (extracellular shift of K+) 17) metabolic alkalosis 18) increased triglycerides 19) diminished HDL cholesterol 20) may exacerbate psoriasis [4] 21) may increase risk of developing diabetes mellitus [5] 22) increased cardiovascular mortality directly correlates with magnitude of heart rate slowing when used to treat hypertension [12] 23) no fetal heart risk from Mom's beta-blocker usage [17] Overdose: 1) supportive therapy: a) IV access b) continuous cardiac monitoring 2) bradycardia a) atropine generally not useful (not vagally mediated) b) glucagon 2-4 mg IV over 1-2 minutes, then start infusion at 2-5 mg/hr (do not exceed 10 mg/hr); 1] may cause nausea/vomiting 2] monitor for vagally-mediated bradycardia c) ventricular pacing 3) hypotension a) calcium gluconate 3-9 g IV through peripheral line b) calcium chloride 1-2 g IV over 10 minutes through a central venous catheter is alternative (caution: sclerosing agent) c) high-dose insulin euglycemia therapy d) intra-aortic balloon pump Drug interactions: 1) alpha-1 adrenergic antagonists: orthostatic hypotension 2) amiodarone: symptomatic bradycardia & sinus arrest 3) sympathomimetics 4) lidocaine serum levels may increase by 20-30% 5) methacholine 6) methyldopa (paradoxical hypertensive response to stress) 7) NSAIDs may interfere with antihypertensive effect Laboratory: - beta-blocker in hair - beta-blocker in body fluid - beta-blocker in blood - beta-blocker in serum/plasma Mechanism of action: 1) antagonism at beta-adrenergic receptor a) some are specific for the beta-1 adrenergic receptor b) beta-adrenergic receptor blockade leaves unbalanced alpha-adrenergic receptor activity (which tends to increase with age) 2) polymorphism in the ADRB2 gene (C & G) alleles associated with different mortality when treated with beta-blocker after acute coronary syndrome

Interactions

drug interactions drug adverse effects (more general classes)

Related

beta adrenergic receptor beta adrenergic receptor antagonist contraindications

Specific

alprenolol beta-1 adrenergic receptor antagonist (beta-1 blocker) non-specific beta-adrenergic receptor antagonist (non-specific beta-blocker) oxprenolol (Coretal) vasodilating beta-blocker

General

adrenergic receptor antagonist

Properties

References

  1. Medical Knowledge Self Assessment Program (MKSAP) 11, 15, 16. American College of Physicians, Philadelphia 1998 2009, 2012
  2. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 158-59
  3. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 474-75, 491
  4. The Washington Manual of Medical Therapeutics, 33rd edition Foster C et al (eds) Lippincott, Williams & Wilkins, Philadelphia, 2010, pg 969
  5. 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: 10738048
  6. Prescriber's Letter 12(4): 2005 Comparison of Beta-Blockers Detail-Document#: 210410 (subscription needed) http://www.prescribersletter.com
  7. Prescriber's Letter 12(7): 2005 Should Some Drugs Be Avoided in Patients at Risk of Anaphylaxis? Detail-Document#: 210714 (subscription needed) http://www.prescribersletter.com
  8. 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: 16189366
  9. 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: 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: 16257329
  10. Khan N and McAlister FA, Re-examining the efficacy of beta blockers for treatment of hypertension. A meta-analysis. CMAJ 2006; 174:1737 PMID: 16754904
  11. Prescriber's Letter 14(8): 2007 CHART: AHA Blood Pressure Goals and Treatments Detail-Document#: 230801 (subscription needed) http://www.prescribersletter.com
  12. Bangalore S et sl, Relation of beta-blocker-induced heart rate lowering and cardioprotection in hypertension. J Am Coll Cardiol 2008 52:1482 PMID: 19017516 - Kaplan NM Beta-blockers in hypertension: Adding insult to injury. J Am Coll Cardiol 2008 52:1490 PMID: 19017517
  13. Prescriber's Letter 14(8): 2007 Comparison of Oral Beta-Blockers Detail-Document#: 250302 (subscription needed) http://www.prescribersletter.com
  14. 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: 23032550
  15. Prescriber's Letter 19(12): 2012 CHART: Comparison of Oral Beta-Blockers Detail-Document#: 281221 (subscription needed) http://www.prescribersletter.com
  16. Deprecated Reference
  17. 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: 28418448
  18. 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: 27696728
  19. 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. PMID: 30326014 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. PMID: 30326080 http://annals.org/aim/article-abstract/2707335/very-likely-ok
  20. Riemer TG, Villagomez Fuentes LE, Algharably EAE et al Do beta-Blockers Cause Depression? Hypertension. 2021. March 15 PMID: 33719510 https://www.ahajournals.org/doi/10.1161/HYPERTENSIONAHA.120.16590
  21. DeWitt CR, Waksman JC. Pharmacology, pathophysiology and management of calcium channel blocker and beta-blocker toxicity. Toxicol Rev 2004; 23:223 PMID: 15898828

Component-of

polypill (Polycap)