Adrenomimetic Drugs

Question 1

What do adrenergic drugs modulate?

Answer 1

Adrenergic transmission and primarily control the function of sympathetic nervous system

Question 2

Drugs activating adrenergic transmission (adrenomimetics or sympathomimetics) mimic or promote the effects of what?

Answer 2

Norepinephrine/epinephrine/dopamine at adrenergic receptors in the sympathetic NS

Question 3

Drugs inhibiting adrenergic transmission (sympatholytics or anti-adrenergic drugs) prevent the effects of what?

Answer 3

Norepinephrine/epinephrine/dopamine at adrenergic receptors in the sympathetic NS

Question 4

What are the types of a1 receptors?

Answer 4

a1A, a1B, a1D

Question 5

Which G protein is associated with a1 receptors?

Answer 5

Gq

Question 6

What are the effects of Gq binding to a1 receptors?

Answer 6

Increase IP3 and DAG common to all

Question 7

What are the types of a2 receptors?

Answer 7

a2A, a2B, a2C

Question 8

Which G protein is associated with a2 receptors?

Answer 8

Gi

Question 9

What are the effects of Gi binding to a2 receptors?

Answer 9

Decrease cAMP

Question 10

What are the types of B receptors?

Answer 10

B1, B2, B3

Question 11

Which G protein is associated with B receptors?

Answer 11

Gs which increases cAMP

Question 12

What are the types of dopamine receptors?

Answer 12

D1 and D2

Question 13

Which G protein is associated with D1 receptors?

Answer 13

Gs which increases cAMP

Question 14

Which G protein is associated with D2 receptors?

Answer 14

Gi which decreases cAMP

Question 15

Review

Answer 15

Signal transduction slides

Question 16

Direct acting adrenergic drugs produce their effects via what?

Answer 16

Direct interaction with adrenergic receptors

Ex. Adrenergic receptor agonists or antagonists

Question 17

Indirect acting adrenergic drugs produce their effects by doing what?

Answer 17

Increased or reducing the concentration of NE at target receptors
Work by altering neurotransmitter concentrations at target site

Question 18

What are the categories of direct adrenomimetics?

Answer 18

Alpha agonists, beta agonists, mixed alpha and beta agonists

Question 19

What are examples of alpha agonists?

Answer 19

Phenylephrine (a1) and clonidine (a2)

Question 20

What are examples of mixed alpha and beta agonists?

Answer 20

NE (a1 and a2 equally, B1 > B2) and epinephrine (all receptors equally)

Question 21

What are examples of beta agonists?

Answer 21

Dobutamine (B1), isoproterenol (B1 and B2 equally), albuterol (B2)

Question 22

Where are alpha-1 receptors found?

Answer 22

Most vascular smooth muscle (Innervated), pupillary dilator muscle, prostate and heart

Question 23

What are the actions of a1 receptors?

Answer 23

Vascular smooth muscle contraction
Contraction of pupillary dilator muscle (dilates pupil)
Contraction of the prostate
Increases force of contraction in the heart

Question 24

Where are a2 receptors found?

Answer 24

Neurons, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth muscle and fat cells

Question 25

What are the actions of a2 receptors?

Answer 25

Modulates transmitter release from neurons Platelet aggregation Inhibits transmitter release from adrenergic and cholinergic nerve terminals Contraction of some vascular smooth muscle Inhibits lipolysis

Question 26

Where are B1 receptors found?

Answer 26

Heart and juxtaglomerular cells

Question 27

What are the actions of B1 receptors?

Answer 27

Increases force and rate of heart contraction | Increases renin release

Question 28

Where are B2 receptors found?

Answer 28

Respiratory, urine, and vascular smooth muscle Skeletal muscle Human liver

Question 29

What are the actions of B2 receptors?

Answer 29

Promotes smooth muscle relaxation Promotes K+ uptake in skeletal muscle Activates glycogenolysis and gluconeogenesis

Question 30

Where are B3 receptors found?

Answer 30

Bladder and fat cells

Question 31

What are the actions of B3 receptors?

Answer 31

Relaxes detrusor muscle | Activates lipolysis

Question 32

Where are D1 receptors found?

Answer 32

Smooth muscle where it dilates renal blood vessels

Question 33

Where are D2 receptors found?

Answer 33

Nerve endings where it modulates transmitter release

Question 34

Which adrenomimetic drug can be used for hypotensive emergencies such as hemorrhagic shock, overdose of anti-hypertensives or CNS depressants?

Answer 34

NE and phenylephrine

Question 35

Which adrenomimetic drug can be used for Chronic hypotension?

Answer 35

Ephedrine

Question 36

Which adrenomimetic drug can be used for cardiogenic shock?

Answer 36

Dobutamine

Question 37

Which adrenomimetic drug can be used for heart failure?

Answer 37

Short term use of dobutamine in acute HF

Question 38

Which adrenomimetic drug can be used for HTN?

Answer 38

Alpha-2 agonists for the long term Tx

Question 39

Which adrenomimetic drug can be used for emergency the arepa for complete AV block and cardiac arrest?

Answer 39

Epinephrine and isoproterenol

Question 40

Which adrenomimetic drug can be used for depression?

Answer 40

Phenelzine and Selegiline

Question 41

Which adrenomimetic drug can be used for narcolepsy?

Answer 41

Amphetamines and methylphenidate

Question 42

Which adrenomimetic drug can be used for ADHD?

Answer 42

Methylphenidate

Question 43

Which adrenomimetic drug can be used for obesity?

Answer 43

Ephedrine | Amphetamines

Question 44

Which adrenomimetic drug can be used for bronchial asthma?

Answer 44

Albuterol

Question 45

Which adrenomimetic drug can be used for decongestion of mucous membranes?

Answer 45

Phenylephrine and ephedrine

Question 46

Which adrenomimetic drug can be used for anaphylaxis?

Answer 46

Epinephrine (effective at both respiratory (bronchospasm) and cardiovascular (severe hypotension, cardiac depression) components

Question 47

Which adrenomimetic drug can be used for ophthalmic applications?

Answer 47

Examination of retina - induction of mydriasis —> phenylephrine Glaucoma —> alpha 2 selective agonists

Question 48

Which adrenomimetic drug can be used for stress urinary incontinence?

Answer 48

Ephedrine