Ch 17: Adrenergic Agonists

Question 1

Adrenergic agonists are often referred to as…

Answer 1

…sympathomimetics.

p. 143

Question 2

Drugs can activate adrenergic receptors by 4 basic mechanisms:

Answer 2

1) direct receptor binding
2) promotion of release of norepinephrine (NE)
3) blockade of reuptake of NE
4) inhibition of inactivation of NE

(p. 143)

Question 3

What are the 2 major classes of adrenergic agonists?

Answer 3

catecholamines and noncatecholamines

p. 144

Question 4

What are 3 major characteristics that all catecholamines have in common?

Answer 4

1. they cannot be used orally
2. they have a brief duration of action
3. they cannot cross the blood-brain barrier

(p. 144)

Question 5

Albuterol is highly _________, acting at ____ _ receptors only.

Answer 5

selective, beta 2

p. 144

Question 6

Which adrenergic receptor subtypes do epinephrine affect?

Answer 6

Beta 1, beta 2, alpha 1, and alpha 2

p. 144

Question 7

At low or therapeutic doses, selectivity of adrenergic drugs is _______. As dosage increases, selectivity ________.

Answer 7

maximal
declines

(p. 145)

Question 8

What are the 3 major adverse affects of alpha 1 activation?

Answer 8

hypertension
necrosis
bradycardia

(p. 147)

Question 9

There are __ ___________ ____________ related to activation of peripheral alpha 2 receptors.

Answer 9

no therapeutic applications

p. 147

Question 10

Activation of alpha 2 receptors in the CNS cause:

What important drug has this effect?

Answer 10

1) reduction of sympathetic outflow to the heart and blood vessels
2) relief of severe pain

clonidine (pp. 147, 168)

Question 11

What 5 drugs are capable of activating alpha 1 receptors? (Hint: 3 are catecholamines and 2 are noncatecholamines)

Answer 11

1) epinephrine
2) norepinephrine
3) dopamine

4) ephedrine
5) phenylephrine

(p. 146)

Question 12

What are 2 of the drugs capable of activating alpha 2 receptors?

Answer 12

epinephrine and norepinephrine

p. 147

Question 13

Beta 1 receptors can be activated by what 6 drugs? (Hint: 5 are catecholamines and 1 is a noncatecholamine)

Answer 13

1) epinephrine
2) norepinephrine
3) isoproterenol
4) dobutamine
5) dopamine

6) ephedrine
(p. 147)

Question 14

What is the effect of beta 2 activation in the uterus?

Answer 14

relaxation of uterine smooth muscle

p. 148

Question 15

What is the most common side effect of beta 2 agonists?

Answer 15

tremors – because activation of beta 2 receptors in skeletal muscle enhances contraction

(p. 148)

Question 16

Anaphylaxis is characterized by what 3 features?

Answer 16

hypotension
bronchoconstriction
edema of the glottis

(p. 148)

Question 17

What 2 enzymes inactivate catecholamines resulting in their very short half-lives?

Answer 17

Monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT)

(p. 144)

Question 18

Which adrenergic receptors are activated by epinephrine?

Answer 18

Alpha 1, alpha 2, beta 1, and beta 2

p. 146

Question 19

Which adrenergic receptors are activated by norepinephrine?

Answer 19

alpha 1, alpha 2, beta 1

p. 146

Question 20

Which adrenergic receptors are activated by isoproterenol?

Answer 20

beta 1, beta 2

p. 146

Question 21

Which adrenergic receptors are activated by dobutamine?

Answer 21

beta 1

p. 146

Question 22

Which adrenergic receptors are activated by dopamine?

Answer 22

alpha 1, beta 1, dopamine

p. 146

Question 23

Which adrenergic receptors are activated by phenylephrine?

Answer 23

alpha 1

p. 146