10 Adrenergics I

Question 1

10 adrenergics I

which receptor when stimulated supplies parasympathetic activity to the heart?

Answer 1

M2 receptor.

Question 2

10 adrenergics I

Most organs/structures are innervated heavily by both the sympathetic and parasympathetic divisions. Which structures are solely sympathetic innervation?

Answer 2

1) blood vessels
2) sweat glands
3) liver
4) spleen
5) adrenal glands

Question 3

10 adrenergics I

where (generally) are adrenergic receptors found?

Answer 3

1) presynaptically (on postganglionic nerve terminals)

2) Postsynaptically (on target tissues)

Question 4

10 adrenergics I

which 2 adrenergic receptors are found on the nerve terminals of postganglionic nerves?

Answer 4

Alpha 2DA 2

Question 5

10 adrenergics I

T/F You find the Alpha 1, Beta 1, Beta 2, and DA 1 receptors on target tissues only?

Answer 5

True

Question 6

10 adrenergics I

What are the three catecholamines that are naturally occurring within the nervous system and clinically useful?

Answer 6

1) Norepinephrine
2) Epinephrine
3) Dopamine

Question 7

10 adrenergics I

what is considered the primary NT of adrenergic nerves?

Answer 7

Norepinepherine

Question 8

10 adrenergics I

Where does the major source of epi come from?

Answer 8

adrenal medulla

Question 9

10 adrenergics I

Where is dopamine released in the PNS?

Answer 9

By postganglionic sympathetic nerves of the renal and splanchnic vascular smooth muscle.

Question 10

10 adrenergics I

How is epinephrine made?

Answer 10

1) Tyrosine (tyrosine hydroxylase)
2) DOPA
3) Dopamine
4) Norepinephrine
5) Epinephrine

Question 11

10 adrenergics I

What controls the rate of epinephrine formation?

Answer 11

The rate of neuronal firing.

Question 12

10 adrenergics I

What is the rate limiting step in epinephrine synthesis?

Answer 12

Tyrosine to DOPA through tyrosine hydroxylase because it is controlled by negative feedback.

Question 13

10 adrenergics I

What is COMT? Where is it found? What does it do?

Answer 13

COMT= Catechol o methyltransferase.It is found mainly in the liver.It methylates catecholamines rendering them inactive.

Question 14

10 adrenergics I

what is MAO? Where is it found? what does it do?

Answer 14

1) MAO= Monoamine oxidase
2) found mainly in the liver, adrenergic nerve terminals, and brain.
3) Deaminates catecholamines.

Question 15

10 adrenergics I

Isoproterenol, dobutamine, and terbutaline are all adrenergic receptor agonists that have large alkyl moieties. What does the large alkyl moiety do for the drug?

Answer 15

It increases Beta activity. (note: the alkyl group is the very end ‘R’ group)

Question 16

10 adrenergics I

T/F Catecholamines have an OH at the 3/4 postition?

Answer 16

true

Question 17

10 adrenergics I

What happens when you loose the hydroxyl group on the catecholamine?

Answer 17

1) Decreased potency

2) increased duration of action because COMT cant metabolize it easily.

Question 18

10 adrenergics I

Metaraminol, phenylephrine, and ephedrine all act as long lasting adrenergic agonist because?

Answer 18

These drugs all have a substitution to the benzene ring such as the loss of a hydroxyl.

Question 19

10 adrenergics I

what happens when you form a drug (catecholamine agonist) that has a substitution on the alpha carbon?

Answer 19

You end up getting a long lasting catecholamine type reaction because MAO is not able act on the molecule easily.

Question 20

10 adrenergics I

Metaraminol and ephedrine can have substitutions to the benzene ring to extend their half lives. What else can these two drugs do to extend their lives?

Answer 20

Have a substitution on the alpha carbon. They have this substitution to help slow/prevent the breakdown from MAO.

Question 21

10 adrenergics I

Agonists for the alpha 1 adrenergic receptor have what function? What is the exception?

Answer 21

1) In general, contraction and constriction of smooth muscle. 2) It causes relaxation of intestinal smooth muscle

Question 22

10 adrenergics I

An agonist of the alpha 2 receptor would act where?

Answer 22

1) postganglionic sympathetic nerve terminals

Question 23

10 adrenergics I

What happens when the presynaptic nerve terminal is stimulated at the alpha 2 receptor?

Answer 23

negative feedback will inhibit the release of more NE from the postganglionic neuron.

Question 24

10 adrenergics I

phenylephrine, methoxamine, clonidine, and methyl-NE are all drugs that do what?

Answer 24

selective agonists for alpha adrenergic receptor (Note they can also activate beta but its much much less)

Question 25

# 10 adrenergics I Norepinephrine activates both alpha receptors equally. However, beta receptors are different. Which beta receptor is favored by NE?

Answer 25

NE favors Beta 1 >>Beta 2

Question 26

# 10 adrenergics I T/F Epinepherine favors Beta 2 over Beta 1?

Answer 26

False. Beta 1=Beta 2 Also, Alpha 1=Alpha 2

Question 27

# 10 adrenergics I Dobutamine, isoproterenol, albuterol, terbutaline, and metaproterenol are what type of drugs?

Answer 27

They are Beta agonists.

Question 28

# 10 adrenergics I Where do you find Beta 1 receptors (Mainly)?

Answer 28

heart and adipose tissue

Question 29

# 10 adrenergics I stimulation of Beta 1 receptors leads to?

Answer 29

``` increased: heart rate contractility C.O. lipolysis ```

Question 30

# 10 adrenergics I What effects will you see with activation of the beta 2 receptor?

Answer 30

1) vasodilation in skeletal muscle 2) relaxation of smooth muscle 3) decreased intraocular pressure

Question 31

# 10 adrenergics I what does the beta 3 receptor do?

Answer 31

Increases glycogenolysis in the liver and skeletal M.

Question 32

# 10 adrenergics I Activation of the dopamine (D1 receptor) causes what? Where?

Answer 32

1) vasodilation | 2) kidney and mesenteric

Question 33

# 10 adrenergics I Where do you find the D2 receptor? What do they do?

Answer 33

1) Presynaptic nerve terminal | 2) The D2 receptor acts as a negative feedback loop to prevent too much NE from being released.

Question 34

# 10 adrenergics I Fenoldopam is a drug that does what?

Answer 34

Dopamine agonist. D1>>D2

Question 35

# 10 adrenergics I What is NET?

Answer 35

AKA Amine 1 transport. Its a NE reuptake system located on the postganglionic nerve terminal.

Question 36

# 10 adrenergics I what percent of NE is recycled back into the postganglionic nerve terminal? What about the rest of the NE?

Answer 36

50%The rest of the NE is degraded by MAO and COMT

Question 37

# 10 adrenergics I What is the target of cocaine and tricyclic antidepressants?

Answer 37

They inhibit the function of Amine 1 transport

Question 38

# 10 adrenergics I T/F vasoconstriction, tachycardia, and mydriasis are 3 symptoms associated with cocaine use. Why does this occur?

Answer 38

Cocaine block amine 1 transport (NET) and therefore causes further activation of the sympathetic nervous system.

Question 39

# 10 adrenergics I What is DMI?

Answer 39

DMI=Desmethylimipramine | A tricyclic antidepressant that blocks NET.

Question 40

# 10 adrenergics I what effects will you see with and alpha 2 and DA 2 antagonist?

Answer 40

Increased sympathetic activation. This is because the release of NE from the postganglionic synapse is not allowing for negative feedback.

Question 41

# 10 adrenergics I T/F For Alpha 2 receptors, clinically relevant drugs are lacking?

Answer 41

True

Question 42

# 10 adrenergics I T/F Antiphychotic drugs such as haloperidol and chlorpromazine act as antagonists to the D2 receptors and also elicit peripheral side effects?

Answer 42

True

Question 43

# 10 adrenergics I NE is taken back into the synaptic terminal by NET (amine 1 transport). What other drugs/chemical does NET transport back into the nerve terminal?

Answer 43

dopamine tyramine ephedrine amphetamine

Question 44

# 10 adrenergics I Domamine, tyramine, ephedrine, and amphetamines all increase sympathetic responses. How do they do this?

Answer 44

They are all taken up through NET, and once inside the nerve terminal, they displace NE from storage vesicles causing NE to be released into the synapse.

Question 45

# 10 adrenergics I Where can you get exogenous tyramine? When does this present as a problem?

Answer 45

1) cheeses, sausage, smoked products. | 2) This only becomes an issue if you have problems with MAO.

Question 46

# 10 adrenergics I How do amphetamines work?

Answer 46

They stimulate alpha 1 and beta 1 receptors, act as a NE releasing factor, and are vasopressors.

Question 47

# 10 adrenergics I How does ephedrine act on the body?

Answer 47

It directly stimulates alpha 1 and beta 1 receptors, and acts as a releasing factor for NE.(Note: mild Beta 2 can occur=dilate bronchial/nasal decongestant)

Question 48

# 10 adrenergics I where are alpha 1 receptors found?

Answer 48

most smooth muscle and elicit constriction/contraction(Exception: Inhibits the GI smooth muscle)

Question 49

# 10 adrenergics I Where are beta 1 receptors found?

Answer 49

``` heart (increase) adipose tissue (Lipolysis) ```

Question 50

# 10 adrenergics I where are beta 2 receptors found? what do they do?

Answer 50

1) bronchioles, intestines, uterus, arterioles of heart and skeletal muscle. 2) They all promote relaxation of smooth muscle. Ex: vasodilation.

Question 51

# 10 adrenergics I What happens when you activate a DA 1 receptor?

Answer 51

You get increased blood flow to kidney and mesentary because of vasodilation to these structures.

Question 52

# 10 adrenergics I T/F Beta 1 and beta 2 receptors are 10x more sensitive to Epi than are alpha 1 and alpha 2 receptors?

Answer 52

True

Question 53

# 10 adrenergics I Epi stimulates which receptors?

Answer 53

all alpha, all beta (beta mainly)

Question 54

# 10 adrenergics I NE stimulates which receptors?

Answer 54

all alpha, Beta 1 only.

Question 55

# 10 adrenergics I Dopamine stimulates which receptors?

Answer 55

all dopamine, alpha 1, beta 1

Question 56

# 10 adrenergics I Only 50% of the NE is recycled back into the nerve terminal. How does the nerve make up for the lost NE?

Answer 56

It transports tyrosine into the nerve terminal and converts tyrosine into DOPA--> dopamine--> NE

Question 57

# 10 adrenergics I How does NE get into the vesicle ready to be released?

Answer 57

VMAT (vesicular monoamine transporter)

Question 58

# 10 adrenergics I What triggers NE release?

Answer 58

Ca+ influx derived from an action potential.

Question 59

# 10 adrenergics I Upon excitation of the adrenal medulla from the sympathetic nervous system, what is released?

Answer 59

80% Epi | 20% NE

Question 60

# 10 adrenergics I what is pheochromocytoma?

Answer 60

A tumor of the adrenal gland that secretes a bunch of Epi and NE into the body. This causes an overwhelming sympathetic response.

Question 61

# 10 adrenergics I Will you get excessive sweating with a pheochromocytoma?

Answer 61

Yes but only non thermoregulatory apocrine sweat glands will be stimulated.

Question 62

# 10 adrenergics I Dopamine in the PNS is mainly secreted for what?

Answer 62

Activation of the DA 1 receptor in renal and splanchnic vasculature. (At high doses it can also stimulate alpha 1 and beta 1 receptors)

Question 63

# 10 adrenergics I Why is dopamine used for shock?

Answer 63

increased vasoconstriction (alpha 1) increased HR/contractability (Beta 1) increased blood flow (DA 1)

Question 64

# 10 adrenergics I Norepinephrine has its major effects on which receptors?

Answer 64

all alpha, beta 1 (It has little to no effect of beta 2)

Question 65

# 10 adrenergics I what is Isoproterenol?

Answer 65

a very potent beta agonist. (very little alpha activity) 1) increased C.O. with beta 1 2) decreased M.A.P. with beta 2

Question 66

# 10 adrenergics I what is considered the most potent vasopressor?

Answer 66

Epi because it has both full alpha and beta activity.

Question 67

# 10 adrenergics I what is a vasopressor?

Answer 67

a vasoconstrictor

Question 68

# 10 adrenergics I what happens when you give epi in low doses? high dose? bolus?

Answer 68

1) low dose (beta 1 and beta 2 dominate) 2) high dose (beta1, beta 2 and alpha 1 dominate) 3) bollus (Drop in MAP because due to vasovagal response)

Question 69

# 10 adrenergics I what do you generally see with infusion of NE?

Answer 69

NE infusion increased MAP and decreases HR. | MAP increases because NE lacks Beta 2 receptor activity which would cause vasodilation( smooth muscle relaxation).

Question 70

# 10 adrenergics I which 3 drugs are used to overcome hypotensive crisis?

Answer 70

NE, Phenylephrine, methoxamine

Question 71

# 10 adrenergics I which 2 drugs are used to overcome chronic orthostatic hypotension?

Answer 71

midodrine, ephedrine

Question 72

# 10 adrenergics I which 1 drug is great for treating shock and why?

Answer 72

Dopamine. alpha 1, beta 1, and DA 1 activity.

Question 73

# 10 adrenergics I which 2 drugs are great at slowing/stopping blood flow during surgery?

Answer 73

epinephrine, cocaine

Question 74

# 10 adrenergics I which 3 drugs are useful to help prevent diffusion of local anesthetics?

Answer 74

Epi, NE, phenylephrine

Question 75

# 10 adrenergics I which 3 drugs help with reducing congestion of mucous membranes?

Answer 75

phenylephrine, ephedrine, pseudoephrine

Question 76

# 10 adrenergics I which 1 drug is useful for rescuing cardiac function during a heart block of cardiac arrest?

Answer 76

epinephrine

Question 77

# 10 adrenergics I which 1 drug is useful for rescuing cardiac function during heart failure?

Answer 77

dobutamine

Question 78

# 10 adrenergics I metaproterenol, terbutaline, and albuterol are all beta 2 selective drugs designed to treat what?

Answer 78

bronchial asthma.

Question 79

# 10 adrenergics I what is anaphylaxis and how do you treat it?

Answer 79

1) bronchospasm 2) mucous membrane congestion 3) angioedema 4) hypotension(treated with epi)

Question 80

# 10 adrenergics I which type of drug is used to treat glaucoma?

Answer 80

Beta antagonists generally.

Question 81

# 10 adrenergics I terbutaline does what for the pregant woman?

Answer 81

relax pregnant uterus

Question 82

# 10 adrenergics I ephedrine is used in the genitourinay tract to do what?

Answer 82

correct stress incontinence.