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CHAPTER 18 Adrenergic Drugs Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. Adrenergic Drugs Drugs that stimulate the sympathetic nervous system (SNS) Also known as: Adrenergic agonists Sympathomimetics Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 2 Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 3 Characteristics Mimic the effects of SNS neurotransmitters (catecholamines) Norepinephrine (NE) Epinephrine (EPI) Dopamine Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 4 Adrenergic Receptors Located throughout the body Are receptors for the sympathetic neurotransmitters Alpha-adrenergic receptors Beta-adrenergic receptors Dopaminergic receptors: respond only to dopamine Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 5 Alpha-Adrenergic Receptors Divided into alpha1 and alpha2 receptors Differentiated by their location on nerves Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 6 Alpha1-Adrenergic Receptors Located on postsynaptic effector cells (the cell, muscle, or organ that the nerve stimulates) Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 7 Alpha2-Adrenergic Receptors Located on presynaptic nerve terminals (the nerve that stimulates the effector cells) Control the release of neurotransmitters Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 8 Alpha-Adrenergic Agonist Responses Vasoconstriction CNS stimulation Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 9 Beta-Adrenergic Receptors All are located on postsynaptic effector cells Beta1-adrenergic receptors—located primarily in the heart Beta2-adrenergic receptors—located in smooth muscle of the bronchioles, arterioles, and visceral organs Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 10 Beta-Adrenergic Agonist Responses Bronchial, GI, and uterine smooth muscle relaxation Glycogenolysis Cardiac stimulation Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 11 Dopaminergic Receptors An additional adrenergic receptor Stimulated by dopamine Causes dilation of the following blood vessels, resulting in increased blood flow Renal Mesenteric Coronary Cerebral Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 12 Responses to Stimulation Location Cardiovascular Receptor Response Blood vessels Cardiac muscle alpha1 beta2 beta1 AV Node beta1 SA Node beta1 Constriction Dilation Increased contractility Increased heart rate Increased heart rate Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 13 Responses to Stimulation (cont’d) Location Gastrointestinal Receptor Response Muscle beta2 and alpha Sphincters alpha1 Decreased motility Constriction Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 14 Responses to Stimulation (cont’d) Location Genitourinary Receptor Response Bladder sphincter Penis Uterus alpha1 Constriction alpha1 alpha1 beta2 Ejaculation Contraction Relaxation Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 15 Responses to Stimulation (cont’d) Location Respiratory Receptor Response Bronchial muscles beta2 Dilation Liver beta2 Glycogenolysis Pupils alpha1 Dilation Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 16 Catecholamines Substances that can produce a sympathomimetic response Endogenous Epinephrine, norepinephrine, dopamine Synthetic Dobutamine, phenylephrine Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 17 Mechanism of Action Direct-acting sympathomimetic Binds directly to the receptor and causes a physiologic response Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 18 Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 19 Mechanism of Action (cont’d) Indirect-acting sympathomimetic Causes release of catecholamine from storage sites (vesicles) in nerve endings Catecholamine then binds to receptors and causes a physiologic response Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 20 Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 21 Mechanism of Action (cont’d) Mixed-acting sympathomimetic Directly stimulates the receptor by binding to it and Indirectly stimulates the receptor by causing the release of stored neurotransmitters from vesicles in the nerve endings Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 22 Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 23 Drug Effects Stimulation of alpha-adrenergic receptors on smooth muscles results in Vasoconstriction of blood vessels Relaxation of GI smooth muscles (decreased motility) Constriction of bladder sphincter Contraction of uterus Male ejaculation Contraction of pupillary muscles of the eye (dilated pupils) Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 24 Drug Effects (cont’d) Stimulation of beta1-adrenergic receptors on the myocardium, AV node, and SA node results in cardiac stimulation Increased force of contraction (positive inotropic effect) Increased heart rate (positive chronotropic effect) Increased conduction through AV node (positive dromotropic effect) Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 25 Drug Effects (cont’d) Stimulation of beta2-adrenergic receptors on the airways results in Bronchodilation (relaxation of the bronchi) Other effects of beta2-adrenergic stimulation Uterine relaxation Glycogenolysis in the liver Increased renin secretion in the kidneys Relaxation of GI smooth muscles (decreased motility) Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 26 Indications Treatment of asthma and bronchitis Bronchodilators: drugs that stimulate beta2adrenergic receptors of bronchial smooth muscles, causing relaxation, resulting in bronchodilation Examples: albuterol, ephedrine, epinephrine, formoterol, levalbuterol, metaproterenol, pirbuterol, salmeterol, and terbutaline* * Used to stop premature labor—causes relaxation of uterine smooth muscle Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 27 Indications (cont’d) Reduction of intraocular pressure and dilation of pupils: treatment of open-angle glaucoma Alpha-adrenergic receptors Examples: epinephrine and dipivefrin Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 28 Indications (cont’d) Temporary relief of conjunctival congestion (eyes) Alpha-adrenergic receptors Examples: epinephrine, naphazoline, phenylephrine, tetrahydrozoline Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 29 Indications (cont’d) Treatment of nasal congestion Intranasal (topical) application causes constriction of dilated arterioles and reduction of nasal blood flow, thus decreasing congestion Alpha1-adrenergic receptors Examples: epinephrine, ephedrine, naphazoline, oxymetazoline, phenylephrine, and tetrahydrozoline Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 30 Vasoactive Adrenergics (Pressors, Inotropes) Also called cardioselective sympathomimetics Used to support the heart during cardiac failure or shock; various alpha and beta receptors affected Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 31 Vasoactive Sympathomimetics (Pressors, Inotropes): Examples Dobutamine Ephedrine Fenoldopam Methoxamine Others Dopamine Epinephrine Phenylephrine Norepinephrine Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 32 Alpha-Adrenergic Adverse Effects CNS Cardiovascular Headache, restlessness, excitement, insomnia, euphoria Palpitations (dysrhythmias), tachycardia, vasoconstriction, hypertension Other Loss of appetite, dry mouth, nausea, vomiting, taste changes (rare) Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 33 Beta-Adrenergic Adverse Effects CNS Cardiovascular Mild tremors, headache, nervousness, dizziness Increased heart rate, palpitations (dysrhythmias), fluctuations in BP Other Sweating, nausea, vomiting, muscle cramps Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 34 Interactions Anesthetic drugs Tricyclic antidepressants MAOIs Antihistamines Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 35 Interactions (cont’d) Thyroid preparations Antihypertensives Will directly antagonize another adrenergic drug, resulting in reduced effects Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 36 Nursing Implications Assess for allergies and history of hypertension, cardiac dysrhythmias, or other cardiovascular disease Assess renal, hepatic, and cardiac function before treatment Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 37 Nursing Implications (cont’d) Perform baseline assessment of vital signs, peripheral pulses, skin color, temperature, and capillary refill; include postural blood pressure and pulse Follow administration guidelines carefully Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 38 Nursing Implications (cont’d) Intravenous administration Check IV site often for infiltration Use clear IV solutions Use an infusion pump Infuse drug slowly to avoid dangerous cardiovascular effects Monitor cardiac rhythm Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 39 Nursing Implications (cont’d) With chronic lung disease Instruct patients to avoid factors that exacerbate their condition Encourage fluid intake (up to 3000 mL/day) if permitted Educate patients about proper dosing, use of equipment (MDI, spacer, nebulizer), and equipment care Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 40 Nursing Implications (cont’d) Salmeterol is indicated for prevention of bronchospasms, not management of acute symptoms Overuse of nasal decongestants may cause rebound nasal congestion or ulcerations Avoid over-the-counter or other medications because of possible interactions Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 41 Nursing Implications (cont’d) Administering two adrenergic drugs together may precipitate severe cardiovascular effects such as tachycardia or hypertension Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 42 Nursing Implications (cont’d) Monitor for therapeutic effects (cardiovascular uses) Decreased edema Increased urinary output Return to normal vital signs Improved skin color and temperature Increased LOC Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 43 Nursing Implications (cont’d) Monitor for therapeutic effects (asthma) Return to normal respiratory rate Improved breath sounds, fewer crackles Increased air exchange Decreased cough Less dyspnea Improved blood gases Increased activity tolerance Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. 44