extraneuronal uptake of amines
Non-selective (1st generation)
Decrease in heart rate Decrease in contractility Decrease in cardiac output Slow conduction in atria and AV node Increase refractory period, AV node Bronchoconstriction Prolonged hypoglycemia Decrease in plasma FFA Reduction in HDL
cholesterol Increase in LDL cholesterol and triglycerides Hypokalemia
(2nd generation) Atenolol Bisoprolol Esmolol Metoprolol
Angina pectoris Hypertension Cardiac arrhythmias CHF
Hypertropic obstructive cardiomyopathy Hyperthyroidism Migraine prophylaxis Acute panic symptoms Substance abuse withdrawal Variceal bleeding in portal hypertension
Bradycardia Negative inotropic effect Decrease in cardiac output Bradyarrhythmias Reduction in
AV conduction Bronchoconstriction Fatigue
(insomnia, nightmares) Prolongation of hypoglycemia Sexual dysfunction in men Drag interactions
Prazosin and related quinazolines are selective for a1 receptors but not among a1 subtypes Tamsulosin exhibits some selectivity for a1A receptors
Pharmacological effects depend largely on degree of sympathoadrenal tone Bronchoconstriction (of concern in asthmatics and COPD) Hypoglycemia (concern in hypoglycemics and diabetics) Membrane stabilizing effect (propranolol, acebutolol, carvedilol, and betaxolol only) ISA (strong for pindolol; weak for penbutolol, carteolol, labetalol, and betaxolol)
Summary of Adrenergic Agonists and Antagonists (Continued)
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