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Therapeutic Class Overview Beta-Adrenergic Antagonists (Single-Entity)

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Therapeutic Class Overview Beta-Adrenergic Antagonists (Single-Entity) Therapeutic Class Overview Beta-adrenergic antagonists (single-entity) · Therapeutic Class Overview/Summary: The beta-adrenergic blocking agents (β-blockers) are Food and Drug Administration (FDA)-approved for the treatment of angina, arrhythmias, essential tremor, heart failure, hypertension, hypertrophic aortic stenosis, migraine prophylaxis, myocardial infarction, and pheochromocytoma.1-26 The β-blockers differ with regards to their adrenergic-receptor blocking, membrane stabilizing and intrinsic sympathomimetic activities, as well as lipophilicity.1-26 There are at least three distinct types of β receptors distributed throughout the body (β1, β2, and β3). β1-receptors are located predominantly in the heart and kidneys. β2-receptors are located in the lungs, gastrointestinal tract, liver, uterus, vascular smooth muscle, and skeletal muscle. β3-receptors are located in fat cells. β-blockers primarily exert their effects through a blockade of β1 and β2 receptor subtypes. Agents that have a greater affinity for β1 receptors are considered to be cardioselective. These agents may be safer in patients with asthma, chronic obstructive pulmonary disease, and peripheral vascular disease because they produce less inhibition of β2 receptors, which mediate vasoconstriction and bronchospasm. Cardioselectivity is dose dependent; therefore, β2 blockade can occur at higher doses. Carvedilol and labetalol also block α-adrenergic receptors. 27-28 Current clinical guidelines identify β-blockers as effective in many indications. Their place in therapy varies depending on indication and other patient specific factors. Specific treatment guidelines are summarized in Table 12.29-61 The beta-adrenergic blocking agents that are included in this review are listed in Table 1 and comparative information on cardioselectivity is highlighted in Table 2. This review encompasses all dosage forms and strengths for the single-entity products. A significant majority of these agents are available as a generic product. Table 1. Current Medications Available in the Therapeutic Class1-26 Generic Food and Drug Administration-Approved Dosage Generic (Trade Name) Indications Form/Strength Availability Management of ventricular premature Capsule: Acebutolol HCl ® beats; hypertension alone or in combination 200 mg a (Sectral *) with other antihypertensives 400 mg To decrease angina frequency and increase Tablet: exercise tolerance due to coronary 25 mg atherosclerosis; hypertension alone or in 50 mg Atenolol ® combination with other antihypertensives; 100 mg a (Tenormin *) hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality Hypertension alone or in combination with Tablet: Betaxolol HCl ® other antihypertensives 10 mg a (Kerlone *) 20 mg Bisoprolol Hypertension alone or in combination with Tablet: fumarate other antihypertensives 5 mg a (Zebeta®*) 10 mg Essential hypertension, alone or in Tablet: combination with other antihypertensives; 3.125 mg mild to severe chronic heart failure of 6.25 mg Carvedilol ischemic or cardiomyopathic origin to 12.5 mg ® a (Coreg *) increase survival and, also, to reduce the 25 mg risk of hospitalizations; reduce cardiovascular mortality in clinically stable patients who have survived the acute phase Page 1 of 10 Copyright 2015 • Review Completed on 8/3/2015 Therapeutic Class Overview: beta adrenergic antagonists (single entity) Generic Food and Drug Administration-Approved Dosage Generic (Trade Name) Indications Form/Strength Availability of a myocardial infarction and have a left ventricular ejection fraction of ≤40% (with or without symptomatic heart failure) Essential hypertension, alone or in Extended-release combination with other antihypertensives; capsule: mild to severe chronic heart failure of 10 mg ischemic or cardiomyopathic origin to 20 mg Carvedilol increase survival and, also, to reduce the 40 mg Phosphate (Coreg risk of hospitalizations; reduce 80 mg - CR) cardiovascular mortality in clinically stable patients who have survived the acute phase of a myocardial infarction and have a left ventricular ejection fraction of ≤40% (with or without symptomatic heart failure) Intraoperative and Postoperative Injection: Tachycardia and/or Hypertension that occur 10 mg/mL during induction and tracheal intubation, during surgery, on emergence from IV solution anesthesia and in the postoperative period; (Brevibloc®): Esmolol ® Supraventricular Tachycardia or 10 mg/mL a (Brevibloc *) Noncompensatory Sinus Tachycardia, short 20 mg/mL term control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances Hypertension alone or in combination with Injection: other antihypertensives (tablet); 5 mg/mL Hypertension, control of blood pressure in Labetalol HCl ® severe hypertension (injection) Tablet: a (Trandate *) 100 mg 200 mg 300 mg Angina, long-term maintenance treatment; Injection: Hypertension alone or in combination with 5 mg/5 mL other antihypertensives; Hemodynamically Metoprolol tartrate stable patients with definite or suspected Tablet: ® a (Lopressor *) acute myocardial infarction to reduce 25 mg cardiovascular mortality 50 mg 100 mg Angina, long-term maintenance treatment; Extended-release Hypertension alone or in combination with tablet: other antihypertensives; Stable, 25 mg Metoprolol symptomatic (NYHA Class II or III) heart 50 mg succinate (Toprol failure of ischemic, hypertensive, or a ® 100 mg XL *) cardiomyopathic origin; Hemodynamically 200 mg stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality Nadolol Angina, long-term maintenance treatment; Tablet: ® a (Corgard *) Hypertension alone or in combination with 20 mg Page 2 of 10 Copyright 2015 • Review Completed on 8/3/2015 Therapeutic Class Overview: beta adrenergic antagonists (single entity) Generic Food and Drug Administration-Approved Dosage Generic (Trade Name) Indications Form/Strength Availability other antihypertensives 40 mg 80 mg Hypertension alone or in combination with Tablet: other antihypertensives 2.5 mg Nebivolol HCl ® 5 mg - (Bystolic *) 10 mg 20 mg Mild to moderate arterial hypertension alone Tablet: Penbutolol sulfate ® or in combination with other 20 mg - (Levatol ) antihypertensives Hypertension alone or in combination with Tablet: Pindolol other antihypertensives 5 mg a 10 mg To decrease angina frequency and increase capsule: exercise tolerance due to coronary 60 mg atherosclerosis (24-hour capsule); 80 mg Persistent premature ventricular 120 mg extrasystoles that impair the well-being of 160 mg the patient and do not respond to conventional measures (injection); Short- Injection: term treatment of supraventricular 1 mg/mL tachycardia, including Wolff-Parkinson- White syndrome and thyrotoxicosis, to Oral solution: decrease ventricular rate (injection); To 20 mg/5 mL abolish tachyarrhythmias due to excessive 40 mg/5 mL catecholamine action during anesthesia when other measures fail (injection); To control ventricular rate in life-threatening Oral Solution Propranolol HCl digitalis-induced arrhythmias (injection); To (Hemangeol®): (Hemangeol®, control ventricular rate in patients with atrial 4.28 mg/mL ® Inderal LA *, fibrillation and a rapid ventricular a Inderal XL®, response(tablet); Hypertension alone or in Tablet: Innopran XL®) combination with other antihypertensives; 10 mg Improves NYHA functional class in 20 mg symptomatic patients with hypertropic 40 mg subaortic stenosis (24-hour capsule); 60 mg Reduce cardiovascular mortality in patients 80 mg who have survived the acute phase of myocardial infarction and are clinically stable (tablet); Adjunct to alpha-adrenergic blockade to control blood pressure and reduce symptoms of catecholamine- secreting tumors (tablet); Familial or hereditary essential tremor (injection); Treatment of proliferating infantile hemangioma requiring systemic therapy (oral solution); Prophylaxis of migraine headache (24-hour capsule) Sotalol HCl Documented ventricular arrhythmias that in Injection: (Betapace®*, the judgement of the physician are life- 150 mg/10 mL ® a Betapace AF *, threatening; Maintenance of normal sinus Sotylize®, rhythm in patients with symptomatic atrial Oral Solution Page 3 of 10 Copyright 2015 • Review Completed on 8/3/2015 Therapeutic Class Overview: beta adrenergic antagonists (single entity) Generic Food and Drug Administration-Approved Dosage Generic (Trade Name) Indications Form/Strength Availability Sorine®†) fibrillation/atrial flutter who are currently in (Sotylize®): sinus rhythm 5 mg/mL Tablet: 80 mg 120 mg 160 mg 240 mg Hypertension alone or in combination with Tablet: other antihypertensives; Reduce 5 mg cardiovascular mortality and reinfarction in 10 mg Timolol Maleate a patients who have survived the acute phase 20 mg of myocardial infarction and are clinically stable; Prophylaxis of migraine headache HCl=hydrochloride * Generic available in at least one formulation † Branded generic product Evidence-based Medicine · Despite the extensive experience with β-blockers in clinical practice, there have been no studies suggesting that any of these agents have major advantages or disadvantages in relation to the others for the treatment of many cardiovascular diseases. When any available β-blocker is titrated properly, it can be effective in patients with an arrhythmia, hypertension, or angina pectoris and other indications.63-185 · The safety and efficacy of sotalol hydrochloride oral
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