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Kaplan Pharmacology: Autonomic Pharm > Chapter 3: Adrenergic Pharmacology > Flashcards

Chapter 3: Adrenergic Pharmacology Flashcards

1
Q

What is the main way NE leaves synaptic cleft?

A

through NE reuptake

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2
Q

What is the main transporter by which NE reuptaken?

A

through NaCl - NE co-transporter driven by the sodium gradient and maintained by Na+/K+ ATPase

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3
Q

Where are a1 receptors found and what do they do?

A

`

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4
Q

Where are the a2 receptors located and what is the response?

A
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5
Q

Where are the B1 receptors located and what is their response?

A
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6
Q

Where are the B2 receptors located and what is their response?

A
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7
Q

Where are the B3 receptors located and what is their response?

A
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8
Q

Where are the D1 (peripheral) located and what is their response?

A
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9
Q

Which cells mediate release of renin from kidneys via B1 activation?

A

JG cells

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10
Q

Fenoldopam use and MOA.

A

D1 agonist used for severe hypertension

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11
Q

DA can affect which adrenergic receptors. (List from most affected by lower doses to higher doses)

A

D1

B1

a1

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12
Q

What G-protein coupled receptor pathway does a1 follow?

A

Gq > increased phospholipase C > IP3, DAG > inc. Ca 2+

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13
Q

What G protein coupled receptor pathway does a2 follow?

A

Gi coupled

Gi> dec adenylyl cyclase > dec. cAMP

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14
Q

What G-protein receptor pathway does B1 follow?

A

Gs
inc adenylyl cyclase > inc. cAMP

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15
Q

What G protein coupled receptor pathway does B2 follow?

A

inc adenylyl cyclase > inc. cAMP

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16
Q

What G protein coupled receptor pathway does D1 follow?

A

inc adenylyl cyclase > inc. cAMP

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17
Q

Clinical use of phenylephrine.

A

nasal decongestant and ophthalmologic use (mydriasis without cyclopegia), hypotensive states

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18
Q

MOA of phenylephrine.

A

a1 agonist

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19
Q

What are the prototype a2 agonist?

A

E=MC2
methyldopa
clonidine

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20
Q

What are the β agonist drugs we discussed?

A
  • Isoproterenol (β1=β2)
  • Dobutamine ( β1> β2) congestive heart failure CHF
  • Selective β2 agonists: salmeterol, albuterol, terbutaline (asthma and premature labor)
  • Selective β3 agonist: mirabegron (overactive bladder)
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21
Q

What are the mixed receptor acting adrenergic agonist neurotransmitters?

A

NE and Epi

22
Q

Trick to remember some Beta2 agonists?

A

terol for B2 agonists

23
Q

What are the effects of epinephrine on BP and HR?

A

depends on dose

low dose mimics isopreteronol
high dose mimics NE

24
Q

How would you distinguish between isoproterenol and Epi on a trace diagram?

A

if gave more of the dose then graph would change unlike in isoproterenol in which it would not change

25
Q

How do you differentiate between high dose Epi and NE.

A

Administer alpha blocker

In NE if do this the BP returns do baseline

In Epi BP won’t return to baseline because of B2 activity

26
Q

Some metabolic effects of B2 agonists?

A

increased glycogenolysis (muscle and liver)

inc. gluconeogenesis

mobilization of fat

27
Q

What are some major uses of NE and Epi?

A
  • cardiac arrest because of B1 benefit
  • adjunct to local anesthetics because of epi a1 benefit
  • hypotension because of a1 benefit
  • anaphylaxis (epi only) strong B2 benefit
  • Asthma (mostly epi used) B2 benefit
28
Q

Name some indirect acting adrenergic receptor agonists considered releasers.

A

tyramine
amphetamines
pseudoephedrine

29
Q

Clinical use of pseudoephedrine?

A

cold medication

30
Q

Clinical use amphetamines like methylphenidate?

A

narcolepsy and ADHD

31
Q

If given an MAO-A inhibitor what should a patient not eat?

A

red wine, cheese

32
Q

MAO type A found mainly where? What does it metabolize?

A

liver but Anywhere

NE, 5HT and tyramine

33
Q

Where is MAO type B found? What does it metabolize?

A

Brain

Metabolizes DA

34
Q

Name some reuptake inhibitors that are indirect-acting adrenergic receptor agonists?

A

cocaine
tricyclic antidepressants

35
Q

Major uses of alpha receptor antagonist?

A

HTN
pheochromocytoma (use of nonselective a blocker to control BP before surgery)
BPH: selective a1 blocker

36
Q

List drugs considered non-selective alpha receptor antagonist.

A

phentolamine (competitive inhibitor)
phenoxybenzamine (noncompetitive inhibitor)

37
Q

List the drugs that are selective a1 blockers?

A

prazosin, doxazosin, terazosin, tamsulosin

38
Q

Trick to remember the selective a1 blockers?

A

“zosins” mostly

39
Q

MOA of tamsulosin? How does this pertain to clinical use? (benefits)

A

acts on alpha 1a receptor blockers; therefore only affects BPH not BP

40
Q

Which has the longer half-life? Phentolamine or phenoxybenzamine?

A

phenoxybenzamine

41
Q

B2 blockers have what metabolic effects?

A

block glycogenolysis, and gluconeogenesis
inc. LDLs, TGs

42
Q

Reproduce this chart on Beta blockers

A
43
Q

How do you remember the B1 selective blockers?

A

A-M olol B1 selective
N-Z olol B1 non selective

44
Q

How do you remember what is a B blocker and something else?

A

olol B blocker only
ilol or alól B blocker and something else

45
Q

Carvedilol and labetalol have what adrenergic blocking activities?

A

alpha - 1 and B-blocking activity

46
Q

Clinical use of carvedilol and labetalol?

A

CHF and Hypertensive emergencies (respectively)

47
Q

Benefit of labetalol over carvedilol?

A

consistent decrease in HR.

48
Q

What is the mechanism of action of sotalol?

A

K+ channel blockade and B-blocking activity

49
Q

What are some general uses of beta- blockers?

A

angina, HTN, post-MI

antiarrhythmics (class II: propranolol, acebutolol, esmolol)

glaucoma (timolol)

migraine, thyrotoxicosis, performance anxiety, essential tremor (propranolol)

50
Q

Yohimbine MOA and clinical use.

A

a2 antagonist

postural hypotension

51
Q

Mirtazapine MOA?

A

a2 antagonist

Kaplan Pharmacology: Autonomic Pharm (4 decks)

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