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Adrenergic Drugs

Pharmacology Exam 2

DrugMOASOASE / ADRsEK
Phenylephrine α1 agonist Blood vessels Eyes HTN, Burning & nasal discharge, rebound congestion Used as nasal decongestant and ophthalmics (mydriasis) Down-reg  rebound congestion Avoid in patients with HTN
Cocaine NE reuptake inhibitor CNS HTN, tachycardia, arrythmias, restlessness Used with Lidocaine to control arrythmias (Na+ channel blocker)
Dextroamphetamine & amphetamine (Adderall) Methylphenidate (Concerta, Ritalin) Lisdexamphetamine (Vyvanse) Dexmethylphenidate (Focalin) Stimulate pre-synaptic release of NE & DA CNS HTN, tachycardia, arrythmias, restlessness, loss of appetite Used for ADHD
Phenelzine Non-selective MOA-A & MOA-B irreversible antagonist CNS HTN, tachycardia, arrythmias, restlessness Inhibits breakdown of NE Serious ADR > HTN crisis due to dietary Tyramine
Selegiline Rasagiline SELECTIVE MAO-B irreversible antagonist CNS HTN, tachycardia, arrythmias, restlessness Inhibits breakdown of NE Used for depression & Parkinson’s
Prazosin Terazosin (Hytrin) Doxazosin (Cardura) Tamsulosin (Flomax) > alpha 1a SELECTIVE α1 antagonist reversible Brain Eye Nose Blood vessels Urethra Headache Blurred vision Orthostatic hypotension >reflex tachycardia Sexual dysfunction Used to treat HTN, BPH, and PTSD (prazosin only) Decrease preload and afterload (blood vessels)
Phenoxybenzamine Non-selective α1 & α2 antagonist irreversible Decrease peripheral resistance Brain Eye Nose Blood vessels Urethra GI Orthostatic hypotension >reflex tachycardia GI stimulation (α2 on PNS fiber blocked) Headache, Miosis Can be used for HTN crisis caused by phenelzine (short term control) Longer duration of action (irreversible> highest affinity for α1)
Mirtazapine (Remeron) NON-SELECTIVE α2 antagonist α1 antagonist Muscarinic antagonist H1 antagonist 5-HT 2a antagonist CNS Enhances release of NE & 5-HT (serotonin) Blocks H1 release>drowsiness Drowsiness, weight gain, increased cholesterol xerostomia, constipation, peripheral edema, HTN Used for MDD Rare side effect: agranulocytosis α2’s located in small blood vessels cause vasoconstrictio> antagonist will cause vasodilation> peripheral edema
Clonidine (Catapres) Brimonidine (Alphagan P) Tizanidine (Zanaflex) Guanfacine (Intuniv) Dexmedetomidine (Precedex) α2 agonist CNS Enhance inhibitory / suppress SNS Sedation, dry mouth, hypotension, bradycardia, sexual dysfunction, depression, constipation (activates GI inhibitory negative feedback pathway >less Ach) Hypertensive crisis can occur if taken off drug abruptly due to up-regulation of receptors
Dobutamine β1 agonist Heart Kidneys Brain Increased heart rate and contractility Tachycardia / arrythmias Increased RAAS CNS stimulation LOW dose: β1 selective HIGH dose: β1 > β2 > α1 Used in patients with systolic dysfunction and congestive heart failure
Metoprolol (Lopressor or Toprol) Atenolol (Tenormin) Nebivolol (Bystolic) “MAN” SELECTIVE β1 antagonist “β1 beta-blockers” Heart Kidneys Brain Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression
SABA: Albuterol (Ventolin) Levalbuterol (Xopenex) LABA: Salmeterol Formoterol β2 agonist Lungs Vasculature CNS Bronchial dilation Vasodilation Excitation
Propranolol (Inderal) Pindolol (PARTIAL AGONIST) Timolol (Betimol) NON-SELECTIVE Beta-blockers β1 & β2 antagonist Heart Kidneys Brain Lungs Vasculature Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression Mask symptoms of hypoglycemia  no nervousness / tremors Propranolol given at low dose for anxiety (target β1 in brain) Contraindicated for asthma pts
Carvedilol (Coreg) Labetalol (Trandate) β1 & β2 antagonist and α1 antagonist Heart Kidneys Brain Lungs Vasculature Decreased heart rate and contractility Fatigue / dizziness Bradycardia Decreased RAAS CNS depression Mask symptoms of hypoglycemia  no nervousness / tremors Contraindicated for asthma pts
Mirabegron β3 agonist Bladder Relief for overactive bladder Less side effects than muscarinic antagonists
Epinephrine β1, β2 agonist (blood vessels) Heart and vasculature Adrenergic receptors SNS activation Low dose: β1 & β2 High dose: everything Used for shock (life support) / anaphylaxis Patients must be weaned off due to down regulation of receptors
Norepinephrine (Levophed) α1, β1 agonist Heart & vasculature Increase TPR, heart rate, contractility Used for shock (life support)
Isoproterenol β1, β2 agonist (lungs) Heart & lungs Hyperglycemia Palpitations Tachycardia Arrythmias Used for asthma (not 1st line), bradycardia, and heart block (AV)
Created by: PharmacistJulian
 

 



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