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Pharm Ch9

Adrenergic Pharm

QuestionAnswer
Inhibitors of Catecholamine Synthesis (inhibits tyrosine hydroxylase (TH) and used to Tx: HTN (pheochromocytoma)) α-Methyltyrosine
Inhibitors of Catecholamine Storage: irreversibly damages VMAT, no longer used d/t ADRs of psychotic depression Reserpine
Inhibitors of Catecholamine Storage: found in red wine & aged cheese, processed by MAO; CI in people taking MAOI’s (causes HTN crisis d/t displaced NE) Tyramine (metabolite is Octopamine)
Inhibitors of Catecholamine Storage: displaces NE, inhibits cardiac sympathetic nerves (reduces CO) and treats uncontrolled HTN Guanethidine Guanadrel
Inhibitors of Catecholamine Storage: 1) displaces catecholamines from vesicles, 2) weakly inhibits MAO, 3) blocks reuptake by NET & DAT; ADRs: fatigue/depression after CNS stimulation Tx: depression & narcolepsy, suppresses appetite Amphetamine
Inhibitors of Catecholamine Storage: Restricted use in US; one is used widely as OTC decongestant Ephedrine Pseudoephedrine Phenylpropanolamine
Inhibitors of Catecholamine Storage: ADRs: ↑BP, restlessness, dizziness, tremor, irritability, confusion, aggression, ED, anxiety, paranoid hallucinations, panic, suicidal Tx: ADHD in children (CNS stimulant) Methylphenidate (Ritalin)
Inhibitors of Catecholamine Storage: “crank”, “crystal meth” is a major drug of abuse Methamphetamine
Inhibitors of Catecholamine Reuptake (sympathomimetic): inhibitor of NET drug of abuse Tx: local anesthetic Cocaine
Inhibitors of Catecholamine Reuptake (sympathomimetic): inhibits NET, blocks NE, 5HT, histamine/muscarinic R; Latency period of weeks before improvement is seen in depression; ADRs: postural hypotension, sinus tachycardia, arrhythmia Imipramine, Amitriptyline (TCAs)
Inhibitors of Catecholamine Reuptake (sympathomimetic): mixed 5HT & NE reuptake inhibitor Duloxetine
Inhibitors of Catecholamine Metabolism (MAOIs): nonselective (all MAOIs CI w/ SSRIs d/t serotonin syndrome - tremors, seizures, coma, death) Phenelzine Iproniazid Tranylcypromine
Inhibitors of Catecholamine Metabolism: MAO-AI Clorgyline
Inhibitors of Catecholamine Metabolism: MAO-BI that potentiates DA to treat Parkinson’s Selegiline
Inhibitors of Catecholamine Metabolism: reversible MAO-AI Brofaromine Befloxatone Moclobemide
systemic α1-agonist to treat shock Methoxamine
topical α1-agonist to treat nasal congestion, opthalmic hyperemia, shock Phenylephrine Oxymetazoline Tetrahydrazoline (Afrin, Visine)
α2-agonist treats HTN, drug withdrawal (sympatholytic); ADRs: bradycardia, dry mouth, sedation Clonidine Guanabenz, Guanfacine (both rarely used)
α2-agonist DOC for HTN in pregnancy, ADRs: rare hepatotoxicity, autoimmune hemolytic anemia α-Methyldopa
β-Adrenergic Agonists: nonselective treats asthma bronchoconstriction; ADRs: unwanted cardiac side effects Isoproterenol
β1-agonist, +inotrope, ↑CO treats heart failure Dobutamine
β2-agonist treats obstructive airway disease, acute bronchospasm Metaproterenol Terbutaline Albuterol
long-acting β2-agonist (12 hrs) Salmeterol
nonselective, irreversible; Block α1: ↓peripheral resistance, ↑CO, Tx: pre-op pheochromocytoma Phenoxybenzamine
α-Adrenergic Antagonists: nonselective, reversible Tx: pre-op pheochromocytoma Phentolamine
α1-antagonist treats HTN Prazosin
α1-antagonist has longer half-life Terazosin Doxazosin
α1A-antagonist has less ADRs of orthostatic hypotension Tamsulosin
α1-antagonist ↑insulin release & treats ED Yohimbine
β-Adrenergic Antagonists: nonselective ADRs: sedation, decreased libido, Tx: HTN, angina, glaucoma Propranolol Nadolol Timolol
Blocks α1, β1, β2, weak partial agonist at β2, ↓BP (vasodilation, prevention of reflex sympathetic ↑HR), Tx: HTN, ADRs: liver damage (do LFTs!) Labetalol Carvedilol
antagonist & partial agonist β1, β2 causes smaller decreases in HR & BP; Tx: HTN Pindolol
partial agonist β1, Tx: HTN Acebutolol
selective β1 blocker, very short half-life (3-4 min) Tx: thyroid storm Esmolol
selective β1 blocker, intermediate half-life (3-4 hrs), Tx: mild HF, first MI Metoprolol Atenolol
selective β1 blocker, β2-agonist Celiprolol
Created by: fmuralid
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