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Pharm Block 10 > Adrenergic Agonists > Flashcards

Adrenergic Agonists Flashcards

1
Q

Synthesis of NE

A
  • starts with tyrosine
  • tyrosine transformed into DOPA in neuron, rate limiting step
  • formed into dopamine in the neuron
  • goes into vesicles
  • turns into NE inside the vesicle
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2
Q

What is the rate limiting step in NE synthesis

A

Tyrosine into DOPA in the neuron

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3
Q

Where is NE formed?

A

Inside the vesicle

-from dopamine

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4
Q

Release of NE

A
  • similar to Ach
  • depolarize
  • Ca2+ channels open
  • Ca2+ rushes in
  • vesicles go to membrane
  • NE released into synapse
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5
Q

What are the fates of NE once it is released into the synapse?

A
  1. Bind to alpha or beta
  2. Metabolized by COMT
  3. NE reuptake into neuron
  4. Negative feedback binding to presynaptic
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6
Q

What does NE bind to

A

Alpha or beta

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7
Q

What is NE metabolized by

A

COMT

-turned into inactive metabolites, just like Ach is with acetylcholinesterase

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8
Q

NE reuptake into neuron

A
  • very rapid
  • goes back into the presynaptic neuron without being degraded (differnt for Ach)
  • reason for short half life
  • clears synapse even better than COMT
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9
Q

What is the major reason for short half life of NE

A

Rapid reuptake into the presynaptic neuron

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10
Q

What clears the synapse better, NE reuptake or COMT?

A

Reuptake

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11
Q

What receptor does NE bind to presynaptic ally for negative feedback on the neuron

A

A2

  • low CAMP
  • closes Ca2+ channels
  • vesicle wont migrate
  • wont release NE
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12
Q

Alpha 2 agonist

A
  • stops NE release

- lowers BP

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13
Q

Alpha 2 antagonist

A

Increases NE release

Increases BP

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14
Q

COMT inhibitor

A

Increase NE in synapse

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15
Q

Cocaine and NE

A

Blocks reuptake
Blocks major pathway to clear NE
Stimulant effect

Na/K ATPase is what gets blocked by cocaine

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16
Q

TCA (tricyclic antidepressants) and NE

A

Work like cocaine

-block reuptake of NE

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17
Q

MAO

A
  • Monamine oxidase inhibitor
  • Metabolizes amines in the cytoplasm (dopamine, NE, dopamine safe from it in the vesicle)
  • when there is reuptake of NE, MAO waits for it in the cytoplasm and limits NE in the neuron by degrading excess of it
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18
Q

MAOI (MAO inhibitor)

A

Increase recycling, increase NE

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19
Q

What is the enzyme responsible for the rate limiting step of NE synthesis

A

Tyrosine hydroxylase

-tyrosine into DOPA

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20
Q

there is one more step to NE synthesis that is not made int sympathetic nerves

A

NE into epi. This is done in adrenal medulla. Sympathetic nerves do not have the enzyme necessary to do this

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21
Q

A1 receptor

A

Gq

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22
Q

A2 receptors

A

Gi

23
Q

B receptors

A

Gs

24
Q

Tissues and receptor types

A

Different tissues have differnt receptors

25
Q

Catecholamines

A

Epinephrine
NE
Dopamine

26
Q

Duration of action of epi, NE, and dopamine

A

They are rapidly metabolized by COMT and MAO, so they have a short duration of action

27
Q

Epi, NE, and dopamine given as drugs and the CNS

A

Not much penetration into the CNS

28
Q

What type if receptors are found in most vascular smith muscle and what are the actions of it

A

A1

Contracts, vasconstricts, increase TPR, increase BP

29
Q

What kind of receptors are in pupillary radial muscle and what is the action

A

A1

Contracts (mydriasis)

30
Q

What kind of receptor is in the prostate and what does it do

A

A1a!!!!

Contracts and decreases urine output

31
Q

What kind of drug should be given for BPH (benign prostate hyperplasia)

A

A1 antagonsit

32
Q

What kind of drugs should be avoided in someone with BPH (benign prostate hyperplasia)

A

A1 agonist

M blockers

33
Q

What kind of receptors are on adrenergic and cholinergic nerve terminals and what do they do

A

A2
Inhibits transmitter release via negative feedback

Don’t worry too much about the cholinergic part

34
Q

What kind of receptors are on pancreatic Bcells and what do they do

A

A2
Inhibits insulin release
Want to use nutrients in fight or flight, not store them

35
Q

What kind of receptors are on the heart and what do they do

A

B1

Stimulates rate and force

36
Q

What kind of adrenoreceptors are on the juxtaglomerular cells and what do they do?

A

B1
Stimulates renin release
Activates RAAS

37
Q

What drug can inhibit sympathetic induced renin release

A

B1 blocker

38
Q

What kind of adrenorecptors are on respiratory, uterine, and vascular smooth muscle and what do they do?

A 
B2
Relaxes 
-bronchodilate 
-can stop premature labor 
-vasodilator BV and decrease TPR and BP
39
Q

What kind of drugs are good to give for asthma

A

B2 agonists and M antagonists

40
Q

What is a good drug to give someone going into premature labor?

A

B2 agonist

41
Q

What does a B2 agonist do to blood vessels and blood pressure

A

Vasodilate, decreases TPR and BP

42
Q

Which adrenoreceptor is not innervated?

A

B2

43
Q

What adrenorecptor is on the liver and what does it do

A

B2
Stimulates glycogenolysis
-need glucose quick for fight or flight

44
Q

What adrenorecptor is on voluntary muscle and what does it do

A

B2
Causes tremor
-they dont do much because they are not innervated. We dont expect a tremor, but when someone takes a B2 agonist for asthma way more than they need, they get a tremor because of decreased BP. Usually systemic. A premature labor patient would have a tremor too

45
Q

What adrenorecptors are found on fat cells and what do they do

A

B3

Stimulates lipolysis

46
Q

What adrenoreceptors are found on renal and other splanchnic blood vessels and what do they do

A

D1
Relaxes (reduces resistance)
Vasodilate in renal BV

47
Q

CNS effects of catecholamines

A

They do not enter the CNS effectively
-amphetamines are an example of sympathmimetics which do enter the CNS and can cause reduced fatigue, euphoria, and insomnia

48
Q

What kind of sympathomimetic can get into the CNS

A

Amphetamines

49
Q

Effects of adrenorecptors on the eye

A

The radial muscle responds to a1 agonists with mydriasis

50
Q

Effects of adrenoreceptors on the bronchi

A

The smooth muscle of the bronchi relax in response to B2 agonists

51
Q

GI tract effect of adrenorecptors

A

A1 and b2 both mediate smooth muscle relaxation

52
Q

Effect of adrenorecptors on genitourinry tract

A

A1 receptors in the bladder mediate contraction of the sphincter, B3 agonists relax detrusor muscle

53
Q

A1 agonists in the vascular system

A

Constrict skin and splanchnic blood vessels and increase peripheral vascular resistance nad venous pressure; since these drugs increase BP they evoke a compensatory reflex bradycardia

Response on heart is opposite of blood pressure

Increased BP=decreased HR

54
Q

A2 agonists on the vascular system

A

When given orally, they accumulate in the CNS and reduce sympathetic outflow and blood pressure
-would get reflected tachycardia

Pharm Block 10 (6 decks)

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