Adrenergic Agonists/antagonists

Question 1

Norepinephrine

Mech
Tx
Side Eff

Answer 1

Non-selective Agonist: α1, α2, β1

Tx: Acute Hypotension

Hypertension; arrythmias; headache

Question 2

Epinephrine

Mech
Tx
Side Eff

Answer 2

Non-selective Agonist: α1, (α2), β1, β2

Tx: Anaphylactic shock; combined with local anesthetics; glaucoma

Palpitation; arrhythmias; headache

Question 3

Amphetamine

Mech
Tx
Side Eff

Answer 3

Increases NorEpi Release

Tx: ADHD, narcolepsy, recreation

Hypertension, insomnia, anxiety, arrhythmias

Question 4

Isoproterenol

Mech
Tx
Side Eff

Answer 4

Non-selective β agonist
Agonist: β1, β2

Tx: shock; heart block

Palpitation; tachyarrhythmia; headache

Question 5

Dobutamine

Mech
Tx
Side Eff

Answer 5

β1-selective β agonist
Agonist: β1

Tx: Cardiac decompensation; shock; heart block

Tachyarrythmias; hypertension

Question 6

Albuterol

Mech
Tx
Side Eff

Answer 6

β2-selective β agonist
Agonist: β2

Tx: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD

Can mask progressively severe inflammation
Tachycardia, muscle tremor

Question 7

Terbutaline

Mech
Tx
Side Eff

Answer 7

β2-selective β agonist
Agonist: β2

Tx: Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD

Can mask progressively severe inflammation
Tachycardia, muscle tremor

Question 8

Phenylephrine

Mech
Tx
Side Eff

Answer 8

α1-selective α agonist
Agonist: α1

Tx: Nasal congestion; postural Hypotension

Hypertension; reflex bradycardia

Question 9

Clonidine

Mech
Tx
Side Eff

Answer 9

α2-selective α agonist
Agonist: CNS α2

Tx: Hypertension; shock; withdrawal from drug dependence

Sedation

Question 10

α-methyldopa

Mech
Tx
Side Eff

Answer 10

α2-selective agonist
Crosses BBB- activates CNS a2 receptors

Tx: Hypertension

Sedation

Question 11

Fenoldopam

Mech
Tx
Side Eff

Answer 11

Selective dopamine agonist
Agonist: D1 only

Tx: Increase blood flow at renal, mesenteric, and cerebral arteries

Question 12

Dopamine

Mech
Tx
Side Eff

Answer 12

Mixed acting (direct/indirect)
Agonist: D1, α1, β1

Low dose = Direct @ D1 Receptors
Medium dose = Direct @ Beta 1, some Indirect
High dose = Direct @ Alpha 1, some Indirect

Vasoconstriction (@ high doses)

Question 13

Phentolamine

Mech
Tx
Side Eff

Answer 13

Non-selective α-antagonist
Antagonist: α1, α2

Tx: Pheochromocytoma, Raynaud’s, frostbite

Postural hypotension; inhibit ejaculation

Question 14

Phenoxybenzamine

Mech
Tx
Side Eff

Answer 14

Non-selective α-antagonist
Antagonist: α1, α2;
non-competitive blocker

Tx: Pheochromocytoma, Raynaud’s, frostbite

Postural hypotension; inhibit ejaculation

Question 15

Prazosin

Mech
Tx
Side Eff

Answer 15

α1-selective antagonist
Antagonist: α1

Tx: Primary HTN, BPH

Postural hypotension (usually 1st dose)

Question 16

Terazosin

Mech
Tx
Side Eff

Answer 16

α1-selective antagonist
Antagonist: α1

Tx: Primary HTN, BPH

Postural hypotension (usually 1st dose)

Question 17

Propranolol

Mech
Tx
Side Eff

Answer 17

Non-selective β-antagonist (1st generation)
Antagonist: β1, β2

Tx: Angina, Hypertension, Arrythmias

Bradycardia, Bronchoconstriction, Sexual Dysfunction

Question 18

Timolol

Mech
Tx
Side Eff

Answer 18

antagonist (1st generation)
Antagonist: β1, β2

Tx: Glaucoma

Bradycardia, Bronchoconstriction, Sexual Dysfunction

Question 19

Metropolol

Mech
Tx
Side Eff

Answer 19

β1-selective antagonist (2nd generation)
Antagonist: β1

Tx: HTN, Angina, Arrythmias, CHF

Bradycardia, Sexual Dysfunction

Question 20

Atenolol

Mech
Tx
Side Eff

Answer 20

β1-selective antagonist (2nd generation)
Antagonist: β1

Tx: HTN, Angina, Arrythmias, CHF

Bradycardia, Sexual Dysfunction

Question 21

Bisoprolol

Mech
Tx
Side Eff

Answer 21

β1-selective antagonist (2nd generation)
Antagonist: β1

Tx: HTN, Angina, Arrythmias, CHF

Bradycardia, Sexual Dysfunction

Question 22

Carvedilol

Mech
Tx
Side Eff

Answer 22

Non-selective β-antagonist
Antagonist: β1, β2
3rd gen

Tx: CHF, HTN

Bradycardia, Fatigue

Question 23

Labetalol

Mech
Tx
Side Eff

Answer 23

Non-selective β-antagonist
Antagonist: β1, β2
3rd gen

Tx: CHF, HTN

Bradycardia, Fatigue

Question 24

Betoxolol

Mech
Tx
Side Eff

Answer 24

β1-selective antagonist Antagonist: β1
3rd gen

Tx: CHF, HTN

Bradycardia

Question 25

Tyramine

Mech
Tx
Side Eff

Answer 25

Indirect acting agonist
Increases cytoplasmic NE release

No Tx

Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out

Question 26

Cocaine

Mech
Tx
Side Eff

Answer 26

Prevents NE reuptake

Tx: Local anesthetic, vasoconstrictor

Insomnia, anxiety, arrhythmias

Question 27

Guanethidine

Mech
Tx
Side Eff

Answer 27

Nerve ending blocker
False neurotransmitter (vesicles become full of guanethidine rather than NE)

Tx: Antihypertensive

Many and serious
Don’t really use this in US; doesn’t cross BBB

Question 28

Reserpine

Mech
Tx
Side Eff

Answer 28

Nerve ending blocker
Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it)

Tx: Older antihypertensive

Many and serious (depression and suicide are major ones)
Cheap! (used abroad)

Question 29

α-me-tyrosine

Mech
Tx
Side Eff

Answer 29

Nerve ending blocker
Inhibit tyrosine hydroxylase (decreases NE synthesis)

Tx: Pheochromocytoma

Many and serious

Question 30

Ephedrine

Mech
Tx
Side Eff

Answer 30

Mixed, direct (β2)/indirect agonist

Nasal decongestion, anorexic