Adrenergic Receptors Agonists/Antagonists

Question 1

Norepinephrine

Answer 1

Non-selective agonist. Agonist: α1, α2, β1 treats: Hypotension. SE: Hypertension; arrythmias; headache

Question 2

Epinephrine

Answer 2

Non-selective agonist. Agonist: α1, (α2), β1, β2 Anaphylactic shock; combined with local anesthetics; glaucoma. SE: Palpitation; arrhythmias; headache; tremor

Question 3

Amphetamine

Answer 3

Indirect acting Increases release of NE. Treats ADHD, narcolepsy, recreation. SE: Hypertension, insomnia, anxiety, arrhythmias

Question 4

Isoproterenol

Answer 4

Non-selective β agonist. Agonist: β1, β2. Treats Bronchodilator/asthma; shock; heart block. SE: Palpitation; tachyarrhythmia; headache

Question 5

Dobutamine

Answer 5

β1-selective β agonist. Agonist: β. Treats Cardiac decompensation; shock; heart block. SE: Tachyarrythmias; hypertension

Question 6

Albuterol

Answer 6

β2-selective β agonist. Brochodilation. Treats: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD. SE: Can mask progressively severe inflammation Tachycardia, muscle tremor. 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal

Question 7

Terbutaline

Answer 7

β2-selective β agonist. Brochodilation. Treats: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD; early labor. SE: Can mask progressively severe inflammation Tachycardia, muscle tremor. 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal

Question 8

Phenylephrine

Answer 8

α1-selective α agonist. Mech: Vasoconstriction. Treats: Nasal congestion; postural Hypotension. SE: Hypertension; reflex bradycardia

Question 9

Clonidine

Answer 9

α2-selective α agonist. Decrease sympathetic outflow from CNS. Treats: Hypertension; shock; withdrawal from drug dependence. SE: Sedation

Question 10

alpha-methyldopa

Answer 10

α2-selective α agonist. Decreases synthesis of NE (by going through entire pathway instead of dopa); end-product (a-methylnorepinephrine) activates a2 inhibitors. Treats: Hypertension, shock, withdrawal from drug dependence. SE: Sedation. Prodrug; crosses BBB

Question 11

Fenoldopam

Answer 11

Selective dopamine agonist. Vasodilation. Treats: Increase blood flow at renal, mesenteric, and cerebral arteries. ~10 minute half-life

Question 12

Dopamine

Answer 12

Mixed acting (direct/indirect). Agonist: D1, α1, β1 TreatsL Shock, renal failure, hypotension. SE: Vasoconstriction (@ high doses). “Low dose = Direct @ D1 Receptors; Medium dose = Direct @ Beta 1, some Indirect; High dose = Direct @ Alpha 1, some Indirect”

Question 13

Phentolamine

Answer 13

Non-selective α-antagonist. Antagonist: α1, α2. Treats: Pheochromocytoma, Raynaud’s, frostbite SE: Postural hypotension; inhibit ejaculation

Question 14

Phenoxybenzamine

Answer 14

Non-selective α-antagonist. Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor). Treats: Pheochromocytoma, Raynaud’s, frostbite. SE: Postural hypotension; inhibit ejaculation

Question 15

Prazosin

Answer 15

α1-selective antagonist. Vasodilation. Treats: Primary HTN, BPH. SE:Postural hypotension (usually 1st dose)

Question 16

Terazosin

Answer 16

α1-selective antagonist. Vasodilation. Treats: Primary HTN, BPH. SE: Postural hypotension (usually 1st dose)

Question 17

Propranolol

Answer 17

Non-selective β-antagonist (1st generation). Antagonist: β1, β2. Treats: Angina, Hypertension, Arrythmias. SE: Bradycardia, Bronchoconstriction, Sexual Dysfunction. Workhorse by which all the rest are judged

Question 18

Timolol

Answer 18

Non-selective β-antagonist (1st generation) Antagonist: β1, β2. Treats: Angina, Hypertension, Arrythmias, Glaucoma. SE: Bradycardia, Bronchoconstriction, Sexual Dysfunction

Question 19

Metoprolol

Answer 19

β1-selective antagonist (2nd generation). Decrease heart rate, contractility, CO. Treats: HTN, Angina, Arrythmias, CHF. SE: Bradycardia, Sexual Dysfunction

Question 20

Atenolol

Answer 20

β1-selective antagonist (2nd generation) Decrease heart rate, contractility, CO. Treats: HTN, Angina, Arrythmias, CHF. SE: Bradycardia, Sexual Dysfunction

Question 21

Bisoprolol

Answer 21

β1-selective antagonist (2nd generation) Decrease heart rate, contractility, CO. Treats: HTN, Angina, Arrythmias, CHF. SE: Bradycardia, Sexual Dysfunction

Question 22

Carvedilol

Answer 22

Non-selective β-antagonist (3rd generation “A”) Antagonist: β1, β2. Treats: CHF, HTN. SE: Bradycardia, Fatigue

Question 23

Labetalol

Answer 23

Non-selective β-antagonist (3rd generation “A”) Antagonist: β1, β2. Treats: CHF, HTN. SE: Bradycardia, Fatigue

Question 24

Betaxolol

Answer 24

β1-selective antagonist (3rd generation “B”). Decrease heart rate, CO. Treats: CHF, HTN. SE: Bradycardia

Question 25

Tyramine

Answer 25

Indirect acting. Mech: Increases cytoplasmic NE release. Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out

Question 26

Cocaine

Answer 26

Prevents NE reuptake

Question 27

Guanethidine

Answer 27

Mech: False neurotransmitter (vesicles become full of guanethidine rather than NE). Treats: Antihypertensive. SE: Many and serious . Don’t really use this in US; doesn’t cross BBB

Question 28

Reserpine

Answer 28

Mech: Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it). Treats: Older antihypertensive. SE: Many and serious (depression and suicide are major ones). Cheap! (used abroad, not here)

Question 29

alpha-me-tyrosine

Answer 29

Mech: Inhibit tyrosine hydroxylase (decreases NE synthesis). Treats:Pheochromocytoma. SE: Many and serious. Still used for this

Question 30

Ephedrine

Answer 30

Nasal decongestion, anorexic