Drugs Affecting Adrenergic Function Autonomic Nervous System Involuntary system responsible for control of smooth muscles Bronchi Blood vessels GI tract Cardiac muscles Exocrine (gastric, sweat, and salivary) SNS and PSNS Effects on the Body Medication function Pharmacological drugs work on the receptors by either: Increase (Agonist) Decrease (Antagonists)(anti) Neurotransmitters of ANS Acetylcholine DopamineNorepinephrine Epinephrine Adrenergic Agonists These drugs mimic the action of the sympathetic nervous system 2 groups Catecholamineo Short duration actiono Cannot be given orallyo They do not cross the blood brain barrier Non-catecholamine Classified according to their selectivity Nonselective-acting Selective-acting Adrenergic Receptors Alpha 1 Alpha 2 Beta 1 Beta 2Fight or Flight System Adrenergic Receptors Alpha 1: Arteries/Veins Bladder Eyes Male Sex Organs Alpha 2: Inhibits Norepinephrine Release Adrenergic Receptors Beta 1: Heart & Kidney Beta 2: Bronchi Skeletal Muscle Arterioles Uterus Dopamine: Kidneys Non-Selective Prototype Epinephrine: Pharmacotherapeutics: Wide variety of indications-- asthma, shock, anaphylactic reaction, ventricular fibrillation. Pharmacokinetics: Adminstered—parenterally, topically, or by inhalation. Metabolized in the liver and excreted through the kidneys. Pharmacodynamics: It stimulates all adrenergic receptors except dopaminergic and causes the greatest adverse effects in the cardiovascular system and CNS. Epinephrine Contraindications and precautions Absolute contraindications to epinephrine include hypersensitivity, sulfite sensitivity, closed-angle glaucoma, and its use during labor. Adverse effectshypertensive crisis cardiac arrhythmias angina elevated serum glucose cerebral hemorrhage J Drug interactions Beta blockers Selective-adrenergic agonists Nonselective-acting Activate both alpha and beta receptors Selective- acting Alpha 1 Arteries- veins, bladder, eyes, Male sex organ Alpha-2 Inhibits norepinephrine release Beta-1 Heart & Kidney Beta-2 Arterioles, Bronchi, liver, skeletal muscles Uterus Dopamine-1 Dopamine-2 Epinephrine Maximizing therapeutic effects/Minimizing adverse effects Requires close monitoring of vital signs and careful monitoring for adverse effects. Take as prescribed. When treating anaphylactic shock, monitor blood pressure. Assisting the patient with menu planning may help to promote appetite and counteract the anorectic influence of epinephrine. Alpha-1 Adrenergic Agonist Prototype: Phenylephrine (Allerest, Sudafed PE, Neo-Synephrine, Preparation H) Remember where Alpha 1 receptors are located???? Phenylephrine Pharmacotherapeutics Used parenterally for vascular failure in shock. Used topically and orally to shrink tissues for relief of nasal mucosal congestion, hemorrhoids. Pharmacokinetics Administered: parenterally or topically because of poor absorption from GI tract Metabolized by liver Excreted in urine. Phenylephrine Pharmacodynamics A powerful alpha-1 adrenergic agonist Very little activity on beta receptors Vasoconstrictor Predominant actions are in vascular system Phenylephrine Contraindications Hypersensitivity, severe hypertension, ventricular tachycardia, closed angle glaucoma, sulfite sensitivity Use Cautiously with: Hyperthyroidism, pregnancy, asthma, myocardial disease, arteriosclerosis, diabetes, asthma Phenylephrine Adverse Effects Headache, Restlessness, Excitability, Reflex bradycardia (following increase in B/P) Rebound congestion Drug interactions Antihypertensive Meds, Antidepressants (MAOI/Tricyclic) Oxytocics Phenylephrine Maximizing Therapeutic Effects/Minimizing Adverse Effects Correct blood loss/fluid deficits Proper technique for administration Use as prescribed Phenylephrine Minimizing Adverse Effects/Maximizing Adverse Effects Administer through large vein Frequent IV site assessment Avoid driving at night Good sleep hygiene Watch for drug-drug interactions Safety Watch for rebound congestion Alpha 2 Agonist Prototype: clonidine (catapres) Remember alpha 2 receptors?? Clonidine Pharmacotherapeutics Antihypertensive Symptoms of withdrawal ADHD Pain Pharmacokinetics Administered: parenterally, topically, or orally. Clonidine Pharmocodynamics: Inhibits release of norepinephrine- opposite effect- vasodilation Clonidine Contraindications and precautions Coronary insufficiency Recent MI Recent CVA Adverse effects Clonidine Maximizing Therapeutic Effects/Minimizing Adverse Effects Monitor B/P Safety Client education Avoid abrupt discontinuationdry mouth sedationdizziness constipation Beta-Adrenergic Agonists Beta-adrenergic agonists Stimulates beta receptors Selective versus non-selective Mimic action of the SNS Terms you should know: Inotropic: strength of contraction Chronotropic: increased heart rate Beta-Adrenergic Agonists Prototype: Dopamine (Intropin) Stimulation of beta-1 receptors Increased HR Increased force of contraction Increased cardiac output Dopamine PharmacotherapeuticsUsed to correct the hemodynamic imbalances present in shock. Also used at low dose to improve renal function PharmacokineticsIV only- Onset: 5 minutes. Duration: 10 minutes.Metabolized: Liver, kidneys, & plasmaExcreted in the urinePharmacodynamics Has the capability to stimulate all adrenergic receptors Strong beta-1 stimulation Dopamine Contraindications and precautions Uncorrected tachyarrhythmias, Ventricular fibrillation Adverse effectsEctopic beats dyspneanausea and vomiting headachetachycardia hypotensionangina vasoconstrictionpalpitation DopamineMaximizing Therapeutic Effects/Minimizing Adverse Effects Administer IV dopamine via infusion pump Start at low doses Monitor B/P, UOP, CO, PWP Monitor IV
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