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Heiman.pharm.HTN.7

Beta Blockers

QuestionAnswer
Beta-1 receptors Increased rate and force of cardiac contraction. Increased renin secretion in the kidney
Beta-2 receptors Constriction of vascular, coronary arteriole, uterine, and skeletal smooth muscle. Bronchial dilation. Increased gluconeogenesis in liver.
Mechanism Blockage of the beta-receptors leading to: Vasodilation. Decreased HR Decreased force of contraction of cardiac muscle. Decreased renin secretion.
Selectivity Selective beta – 1 blockade Atenolol Metoprolol Acebutolol Betaxolol Bisoprolol Dose dependent Increased beta – 2 blockade at higher doses
Intrinsic Sympathomimetic Activity Partial agonist activity May decrease bradycardia, bronchoconstriction Not beneficial for arrhythmias May negate effectiveness of beta-blockers in secondary prevention of MI Carteolol Penbutolol Pindolol
Kinetics Good absorption Some with large first pass effect Propranolol High lipid solubility Propranolol Penbutolol Hepatic metabolism Renal excretion Labetalol High protein binding Propranolol Penbutolol Carvedilol
Adverse Effects Hypotension Bradycardia Depression Impotence Arrhythmias Elevated liver enzymes Dizziness, fatigue Hyperlipidemia
Cautions Hepatic or renal impairment CHF May decrease contractility Heart block Bronchospastic disease May mask signs and symptoms of hypoglycemia
Drug Interactions Other hepatically metabolized drugs Increased levels of flecainide, clonidine Increased levels of beta-blockers caused by: Antiarrhythmiacs Calcium channel blockers Fluoroquinolones Cimetidine
Names Propranolol (Inderal)‏ Carteolol (Cartol)‏ Nadolol (Corgard)‏ Penbutolol (Levatol)‏ Pindolol (Visken)‏ Sotalol (Betapace, Sotacor, Betapace AF)‏ Used only for arrhythmias Timolol (Blocadren)‏ Atenolol (Tenormin)‏ Metoprolol (Lopressor, Toprol)‏
Names Acebutolol (Sectral)‏ Betaxolol (Kerlone)‏ Bisoprolol (Zebeta)‏ Esmolol (Brevibloc)‏ Only IV
Names Carvedilol (Coreg)‏ Has beta and alpha blocking properties Labetalol (Normodyne, Trandate)‏ Has beta and alpha blocking properties Nebivolol (Bystolic) Highly beta – 1 selective
Created by: DianaB
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