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SMP Block 2 > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Alpha 1 receptor subtype location

A

a - prostate

radial muscles, bladder sphincters, skin, blood vessels

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2
Q

Dopamine receptor location

A

Renal and mesenteric blood vessels

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3
Q

Alpha 1 receptor stimulation effect

A

Constriction

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4
Q

Dopamine receptor stimulation effect

A

Dose dependent
Low dose - vasodilation
High dose - stimulation of alpha 1 and beta 1 receptors - increase cardiac output and contractility, increase NE release at heart synapse by blocking reuptake

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5
Q

Alpha 1 receptor mechanism

A

Gq - phospholipase C coupling (PIP2 to IP3 and DAG) - increase Ca2+

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6
Q

What cholinergic receptor has the same mechanism as the adrenergic alpha 1 receptors?

A

M3

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7
Q

Alpha 2 receptor subtype location

A

a - vasomotor center, SNS and PSNS postganglionic fibers

b - vascular smooth muscle

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8
Q

Alpha 2 receptor subtype mechanism

A

Gi - inhibition of adenylyl cyclase, decrease CAMP levels

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9
Q

Dopamine receptor mechanism

A

Gs - stimulate adenylyl cyclase, increase CAMP levels

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10
Q

Alpha 2a receptor effect

A
  1. Vasomotor center - decrease SNS outflow to heart (decrease contractility), vasculature (decrease TPR), and adrenal medulla (decrease levels of epi/norepi)
  2. Postsynaptic SNS ganglionic fibers - feedback inhibition through NE hyperpolarization which decreases further NE release
  3. Postsynaptic SNS-PSNS meets - “collaterols” NE on alpha 2a on cholinergic fibers decreases ACh release and Ach on muscarinic on adrenergic fibers decreases NE release
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11
Q

What receptors ensure that the SNS and the PSNS are not exerting opposing effects at the same time?

A

Alpha 2a

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12
Q

Beta 1 receptor location

A

Heart and kidney

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13
Q

Alpha 2 receptor NT affinity

A

E»>NE

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14
Q

Beta 1 receptor NT affinity

A

E=NE

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15
Q

Beta 2 receptor NT affinity

A

E»>NE

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16
Q

Beta 3 receptor NT affinity

A

NE»>E

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17
Q

Beta 3 receptor NT affinity

A

NE»>E

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18
Q

Beta 1 receptor mechanism

A

Gs - stimulate adenylyl cyclase, increase CAMP levels

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19
Q

Beta 2 receptor mechanism

A

Gs - stimulate adenylyl cyclase, increase CAMP levels

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20
Q

Beta 3 receptor mechanism

A

Gs - stimulate adenylyl cyclase, increase CAMP levels

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21
Q

Beta 1 receptor effect

A

Increase heart contractility

Increase renin production to increase blood volume and therefore increase blood pressure

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22
Q

Beta 2 receptor location

A

Skeletal and liver blood vessels
Skeletal muscle
Bronchi
Liver

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23
Q

Beta 2 receptor effect

A

Skeletal and liver blood vessels - dilation
Skeletal muscle - potassium uptake, glycogen breakdown
Bronchi - dilation
Liver - glycogen breakdown

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24
Q

Beta 3 receptor location

A

Bladder

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25
Q

Beta 3 receptor effect

A

Relaxation of detrusor - urinary retention

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26
Q

Explain the effects of increase CAMP levels by location. What receptors are involved?

A

Cardiac muscle - Beta 1 or Beta 2 - contraction

Smooth muscle - Beta 2, Beta 3, Dopamine - relaxation

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27
Q

Which adrenergic receptors are not innervated?

A

Beta 2

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28
Q

What role does phosphodiesterase play in the adrenergic system?

A

Breakdown to CAMP

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29
Q

What is the general effect of PDE inhibitors?

A

Increase effect of CAMP:
Increase cardiac contractility
Bronchodilation
Vasodilation

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30
Q

How can you inhibit the synthesis of catecholamines?

A

Metyrosine - competitive inhibitor of tyrosine hydroxylase

NE - feedback inhibition of TH

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31
Q

Describe 3 mechanisms by which catecholamine effect is terminated

A

Reuptake - NET transporter (into cytoplasm) and VMAT (into vesicle)
Degradation - MAO (presynaptic terminal) and COMT (end organ)
Inhibition - alpha 2a

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32
Q

What receptor does phenylephrine work on?

A

alpha 1 agonist

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33
Q

What is the effect of histamine?

A

Vasodilation

34
Q

What 3 drugs can be used to impact catecholamine synthesis?

A

Metyrosine
L-Dopa
Reserpine

35
Q

Describe metyrosine including the mechanism, effect, and what purpose it is used for

A

Decrease catecholamine synthesis by competitively inhibiting tyrosine hydroxylase
Treatment of pheochromocytoma (catecholamine-secreting tumor of adrenal medulla)

36
Q

Describe L-Dopa including the mechanism, effect, and what purpose it is used for

A

Increase catecholamine synthesis

Treatment of Parkinson’s (can cross BBB) and TH deficiency

37
Q

What is a consideration when using L-Dopa as a treatment?

A

Dopamine in periphery would cause renal vasodilation - give in conjunction with carbidopa which prevents peripheral conversion of L-Dopa to Dopamine

38
Q

Describe reserpine including the mechanism, effect, and what purpose it is used for

A

Disrupts VMAT - dopa, NE, epi, serotonin do not go into vesicles, destruction by MAO
Treatment of HTN and psychosis historically but caused risk of SI

39
Q

Describe Clonidine including the mechanism, effect, and what purpose it is used for

A

alpha 2a and 2c agonist, decreases NE via vasomotor center, reduces SNS tone
Treatment of HTN, Tourette’s, withdrawl

40
Q

Describe botulinum toxin including the mechanism, effect, and what purpose it is used for

A

Blocks VAMP and SNAP coupling to block ACh release and prevents muscle contraction
Treatment of muscle spasticity and wrinkles

41
Q

Describe tetanus toxin including the mechanism, effect, and what purpose it is used for

A

Prevents GABA release by blocking VAMP and SNAP coupling

Not used in any treatment of disease - causes seizures and prolonged muscle contraction

42
Q

Describe amphetamines including the mechanism, effect, and what purpose it is used for (2 mechanisms)

A

Blocks VMAT and MAO, which increases cytoplasmic concentration of NE, dopa, and serotonin, prolonging their action - reuptake (NET) transporter reverses and releases NTs
Also prevents reuptake via NET transporter prolonging action of NE, dopa, serotonin
Treatment of ADHD, narcolepsy, and acts as a general stimulant
Potential for abuse due to prolonged dopamine action

43
Q

What is ritalin an example of?

A

Amphetamine

44
Q

Describe ephedrine including the mechanism, effect, and what purpose it is used for

A

Increases non-physiologic NE release and weakly stimulates beta receptors
Pseudophedrine (sudafed) is used at OTC nasal decongestant - constricts nasal blood vessels but can lead to rebound hyperemia

45
Q

Why is ephedrine closely regulated over the counter?

A

Similar to methamphetamine in structure - can be used to make meth

46
Q

Describe tyramine including the mechanism, effect, and what purpose it is used for

A

Increases non-physiologic NE release - usually is degraded by MAO
Causes HTN in patients on MAO inhibitors
Found in aged foods - cheese, beer, wine

47
Q

Describe cocaine including the mechanism, effect, and what purpose it is used for

A

Blocks NET transporter which reuptakes NTs - prolongs action of dopa, NE, and serotonin

48
Q

Why is cocaine abuse so dangerous?

A

Abuse due to effects on dopamine

Toxicity due to NE overstimulation of the heart

49
Q

Describe desipramine including the mechanism, effect, and what purpose it is used for

A

Tricyclic anti-depressant
Prolongs NE and serotinin action via inhibition of reuptake but does not affect dopa - less potential for abuse and used as anti-depressant

50
Q

What is an important consideration for patients on MAO inhibitors?

A

Avoid tyramine-rich foods

51
Q

Name 3 dangerous drug interactions with MAO inhibitors

A
  1. Opioids - potentially fatal via unknown mechanisms
  2. Stimulants, anti-depressants, and decongestants - potentially dangerously high levels of NE
  3. Serotonin syndrome - excessive serotonin levels in the body
52
Q

Describe phenelzine including the mechanism, effect, and what purpose it is used for

A

Non-selective MAO inhibitor

Treatment of depression

53
Q

Describe selegiline including the mechanism, effect, and what purpose it is used for

A

MAO-B inhibitor - increases dopamine levels

Used as an adjunctive treatment for Parkinson’s

54
Q

What is another name for selegiline?

A

Deprenyl

55
Q

What is another name for deprenyl?

A

Selegiline

56
Q

What drugs behave similarly to phenelzine?

A

Isocarboxazid

Tranylcypromine

57
Q

What are two specific PDE enzymes and what second messengers do the affect primarily?

A

PDE-4: breaks down CAMP

PDE-5: breaks down CGMP

58
Q

Describe aminophylline including the mechanism, effect, and what purpose it is used for

A

Non-selective PDE inhibitor

Historical uses in Asthma and COPD (bronchiolar relaxation) but not used anymore due to cardiac side effects

59
Q

What is another name for aminophylline?

A

Theophylline

60
Q

What is another name for theophylline?

A

Aminophylline

61
Q

Describe sildenafil including the mechanism, effect, and what purpose it is used for

A

Selective PDE5 inhibitor - increases levels of CGMP, which promotes smooth muscle relaxation
Treatment of erectile dysfunction - blood to penis
Pumlonary HTN - lung vasodilation
Potential future uses for dementia through increasing cerebral blood flow

62
Q

What are two other drugs that behave similarly to sildenafil?

A

Vardenafil

Tadalafil

63
Q

Which adrenergic agonist increases perfusion without increasing HR and why?

A

Norepi increases perfusion by increasing TPR (DBP) as well as cardiac contractility (SBP) but does not increase HR because the baroreceptor reflex works to counteract increases in HR

64
Q

Why is epi so useful in cardiac arrest and anaphylactic shock?

A

Acts on B2 receptors in addition to all NE effects - overall decreases in TPR (DBP) with increase in cardiac contractility (SBP) so mean blood pressure remains the same and the baroreceptor reflex is not activated - this significantly increases cardiac output and perfusion

65
Q

Describe the effects of isoproterenol?

A

Only acts on beta receptors - exaggerated epi response - greater decrease in TPR due to no alpha activation - this actually causes an increase in HR due to baroreceptor reflex, which GREATLY increases CO

66
Q

Describe dobutamine including the mechanism, effect, and what purpose it is used for

A

Beta 1 agonist - used in acute heart failure by increasing cardiac output - decrease TPR and heart rate - makes the heart more efficient

67
Q

Describe albuterol including the mechanism, effect, and what purpose it is used for

A

Beta 2 agonist - used in asthma for bronchodilation without severe cardiac effects (only 20% heart is beta 2)

68
Q

What class of drugs was investigated for potential effects in uterine contractions and what was the implication?

A

Beta 2 agonist - highlighted hormonal expression of receptors

69
Q

Describe phenylephrine including the mechanism, effect, and what purpose it is used for

A

Alpha 1 agonist - increases BP through vasoconstriction and lowers HR via baroreceptor reflex

70
Q

Describe brimonidine including the mechanism, effect, and what purpose it is used for

A

Alpha 2 agonist - decreases intra-ocular pressure by decreasing production of aqueous humor
Treatment of glaucoma

71
Q

Describe phentolamine including the mechanism, effect, and what purpose it is used for

A

Non-selective, reversible alpha antagonist

**NOT used in HTN because it lowers BP too much and subsequently raises HR via baroreceptor reflex

72
Q

Describe phenoxybenzamine including the mechanism, effect, and what purpose it is used for

A

Non-selective, IRreversible alpha antagonists

No common uses

73
Q

Describe prazosin including the mechanism, effect, and what purpose it is used for

A

Selective alpha 1 antagonist

Treatment of HTN

74
Q

What suffix is commonly used for alpha 1 selective antagonists

A

-osin

75
Q

Describe tamsulosin including the mechanism, effect, and what purpose it is used for

A

Selective alpha 1 antagonist

Treatment of benign prostatic hyperplasia

76
Q

Describe yohimbine including the mechanism, effect, and what purpose it is used for

A

Selective alpha 2 antagonist

Used in muscle building and enhanced sexual function

77
Q

What suffix is commonly used for beta antagonists

A

-ol

78
Q

Describe propanolol including the mechanism, effect, and what purpose it is used for

A

Non-selective beta-blocker

79
Q

Describe metorpolol including the mechanism, effect, and what purpose it is used for

A

Beta 1 antagonist - prevent heart and kidney effects (contractility and BP) while maintaining B2 effects of vasodilation, K+ uptake
Especially useful in treating diabetics due to glycogenolysis effects of Beta 2 in liver and skeletal muscle

80
Q

Describe pindolol including the mechanism, effect, and what purpose it is used for

A

Non-selective beta-blocker and partial agonist to intrinsic sympathetic activity
Treatment of HTN in runners where you would not want to further decrease HR

81
Q

Describe carvedilol including the mechanism, effect, and what purpose it is used for

A

Combined alpha 1 and beta antagonist

Treatment of chronic heart failure - prevents hypertrophy of the heart by blocking alpha 1

82
Q

Describe Labetalol including the mechanism, effect, and what purpose it is used for

A

Combined alpha 1 and beta antagonist

Treatment of HTN in pregnancy as well as hypertensive emergencies

SMP Block 2 (4 decks)

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