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D1 Spring > Pharmacology - Adrenergic Agonists (Exam 2) > Flashcards

Pharmacology - Adrenergic Agonists (Exam 2) Flashcards

1
Q

Autonomic nervous system is responsible for which bodily functions? Name 4 examples

A

Bodily functions NOT consciously directed

  1. Airways
  2. Heartbeat
  3. GI activity
  4. Blood pressure
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2
Q

What do autonomic drugs activate?

A
  1. Airways
  2. Heartbeat
  3. GI activity
  4. Blood pressure
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3
Q

What do autonomic drugs inhibit?

A
  1. Using bathroom
  2. Tear production
  3. Saliva production
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4
Q

What does the SNS and PNS innervate?

A

Most peripheral organs/tissues (they usually innervate the same ones)

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5
Q

T/F the SNS and PNS often produce opposite effects

A

True

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6
Q

Which 2 drugs affect the SNS? What are their effects?

A

Adrenergic (increase heart rate + airway)

Anti-adrenergic (decrease heart rate + airway)

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7
Q

Which 2 drugs affect the PNS? What are their effects?

A

Cholinergic (decrease heart rate + airway)

Anti-cholinergic (increase heart rate + airway)

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8
Q

Which 2 drugs are used to treat asthma?

A

Adrenergic (increase heart rate + airway)

Anti-cholinergic (increase heart rate + airway)

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9
Q

Which system is responsible for dilated pupils?

A

SNS

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10
Q

What is the SNS neurotransmitter?

A

NE

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11
Q

What is the SNS receptor?

A

Adrenergic

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12
Q

What is the PNS neurotransmitter?

A

ACh

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13
Q

What is the PNS receptor?

A

Muscarinic

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14
Q

What does a parasympathomimetic and sympathomimetic do?

A

Parasympathomimetic: increases parasympathetic response
Sympathomimetic: increases sympathetic response

(“-mimetic” = mimicking)

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15
Q

What does a parasympatholytic and sympatholytic do?

A

Parasympatholytic: decreases parasympathetic response
Sympatholytic: decreases sympathetic response

(-“lytic” = inhibiting)

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16
Q

Cholinergic = ?

Neurotransmitter = ?

A

Parasympathomimetic

ACh

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17
Q

Adrenergic = ?

Neurotransmitter = ?

Hormone = ?

A

Sympathomimetic

NE

Adrenaline (epinephrine)

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18
Q

2 other names for adrenergic drug

A

Sympathomimetic drug
Adrenergic agonist

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19
Q

2 other names for anti-adrenergic drug

A

Sympatholytic drug
Adrenergic antagonist

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20
Q

2 other names for cholinergic drug

A

Parasympathomimetic drug
Muscarinic drug

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21
Q

2 other names for anti-cholinergic drug

A

Parasympatholytic drug
Anti-muscarinic drug

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22
Q

What controls the adrenal gland? What is found in the adrenal gland?

A

Controlled by SNS

NE and adrenaline (epinephrine)

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23
Q

What are the 5 adrenergic receptors?

A

a1
a2
B1
B2
B3

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24
Q

What kind of receptors are adrenergic receptors?

A

GPCRs

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25
Q

What does the G protein dictate? What are the 3 types of G proteins in adrenergic receptors?

A

Downstream effects

Gq, Gs, Gi

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26
Q

Which G protein goes with the a1 adrenergic receptor?

A

Gq

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27
Q

What is the effect of Gq?

A

Gq -> phospholipase C -> IP3

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28
Q

Which G protein goes with the a2 adrenergic receptor?

A

Gi

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29
Q

Which G protein goes with the B1 adrenergic receptor?

A

Gs

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30
Q

What is the effect of Gs and Gi?

A

Gs -> adenylyl cylase -> cAMP

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31
Q

Pharmacological actions and adverse reactions of adrenergic agonists are both _________ of physiological responses of the __________

A

extensions; SNS

32
Q

What are the physiological and pharmacological responses to SNS/adrenergic agonists?

A

Increased HR
Increased contractility
Increased AV conduction

33
Q

What are the adverse reactions when there is too much SNS/adrenergic agonist?

A

Tachycardia
Palpitations
Arrhythmias
Increased O2 demand (ischemia)

34
Q

Where are a1 adrenergic receptors (Gq) located? What are the effects on these organs?

A

Blood vessels (vasoconstriction)
Pupillary muscles (dilation)
Bladder sphincter (contraction)
Liver (increased glucose and glucagon)

35
Q

Where are a2 adrenergic receptors (Gi) located? What is the effect on this organ?

A

CNS - in presynaptic terminals (inhibits NE release)

36
Q

Where are B1 (Gs) adrenergic receptors located? What is the effect on this organ?

A

Heart (increase HR, contractility, AV conduction)

37
Q

Where are B2 adrenergic receptors located? What are the effects on these organs?

A

Lungs (bronchodilation)
GI (decreased motility, inhibits labor)
Blood vessels (vasodilation)

38
Q

Where are B3 adrenergic receptors located? What are the effects on these organs?

A

Adipose tissue (increased lypolysis and free fatty acids)
Bladder wall (relaxation)

39
Q

What are the 3 naturally occurring adrenergic agonists (catecholamines)?

A

NE
Epinephrine
Dopamine

(A mean cat named Ned)

40
Q

What are the drug name endings for most adrenergic agonists?

A

-ephrine
-edrine
-zoline
-terol
Amphetamine

41
Q

What are the general therapeutic uses for adrenergic agonists?

A
  1. Local vasoconstriction (nasal decongestion)
  2. Tx of hypotension and shock
  3. Ophthalmic uses
  4. Tx of allergic states
  5. CNS stimulation
  6. Tx of hypertension (a2 agonists)
42
Q

What are the 3 types of adrenergic agonists?

A
  1. Directing acting (receptor binding)
  2. Indirect acting (modulation of endogenous catecholamines via synthesis, metabolism, transport)
  3. Mixed acting
43
Q

What are the uses for epinephrine?

A

Local anesthesia
Hemostasis (stops bleeding)
Anaphylaxis
Allergic reactions (hypersensitivity)

44
Q

How does epinephrine work in local anesthesia?

A

Delay absorption into blood
Prolonged action
Minimize systemic effects

45
Q

What are the 2 life-threatening symptoms of anaphylaxis?

A

Airway - trouble breathing, wheezing, chest tightness, swelling of throat, hoarseness, “scratchy” throat

Cardiovascular system - chest pain, low BP, rapid HR, weak pulse

46
Q

How does epinephrine reverse the effects of anaphylaxis?

A

Epinephrine is a vasoconstrictor that increases BP, so it can reverse the low BP (hypotension) during anaphylaxis

Epinephrine is a bronchodilator via B2 adrenergic receptors, so it can reverse the airway constriction during anaphylaxis

47
Q

What are the a1-selective adrenergic receptor agonists (drugs)?

A

Phenylephrine
Midodrine

48
Q

What is Phenylephrine (a1-selective adrenergic receptor agonist) used for?

A

Contraction of vascular SM (vasoconstriction increases BP)

Temp. relief from nasal congestion - edema (vasoconstriction decreases edema)

49
Q

What is Midodrine (a1-selective adrenergic receptor agonist) used for?

A

Postural hypotension (vasoconstriction increases BP)

50
Q

What are the a2-selective adrenergic receptor agonists (drugs)?

A

Clonidine
Methyldopa

51
Q

What effects do a2-selective adrenergic receptor agonists (Clonidine, Methyldopa) have?

A

Sympatholytic

52
Q

Clonidine (2-selective adrenergic receptor agonist) is ________ acting, so it is used for ________ feedback.

A

centrally; negative

53
Q

What is Clonidine (a2-selective adrenergic receptor agonist) used for?

A

Anti-hypertension

Withdrawal symptoms of opioid addiction (blocks nausea, vomiting, sweating, diarrhea)

54
Q

What is Methyldopa (a2-selective adrenergic receptor agonist) used for?

A

Anti-hypertension

55
Q

What is the B1-selective adrenergic receptor agonist (drug)?

A

Dobutamine

56
Q

Dobutamine (B1-selective adrenergic receptor agonist) is a synthetic analog of _________

A

dopamine

(but has no effect on dopamine receptors)

57
Q

What is Dobutamine (B1-selective adrenergic receptor agonist) used for?

A

Increasing contractility, cardiac output, and HR

Short term tx of acute myocardial insufficiency (congestive heart failure, myocardial infarction, cardiac surgery)

58
Q

What is the B2-selective adrenergic receptor agonist (drug)?

A

Albuterol

59
Q

What is Albuterol (B2-selective adrenergic receptor agonist) used for?

A

Bronchospasm (asthma, COPD)

Preventing breathing difficulties during exercise

60
Q

What are common side effects of Albuterol (B2-selective adrenergic receptor agonist)? Why?

A

Tremor
Tachycardia
Palpitations

B2 agonists will also activate B1 receptors at high doses!!

61
Q

What are the indirect acting agonists (stimulants)?

A

Amphetamines (adderall)
Methylphenidate (Ritalin)
Cocaine

62
Q

What are the mixed acting agonists?

A

Ephedrine
Pseudoephedrine (Sudafed)

63
Q

Describe the mechanism of Amphetamine (indirect acting agonist)

A
  1. Amphetamine is lipophilic, so crosses BBB to produce CNS effects
  2. Competes w/ dopamine at dopamine transporter
  3. Inhibits vesicular monoamine transporter
  4. Increased dopamine level at synapse
  5. Similar action of NE
64
Q

What is Amphetamine (indirect acting agonist) used to treat?

A

ADHD
Narcolepsy

65
Q

Describe the mechanism of Ephedrine (mixed acting agonist)

A
  1. Directly binds to and activates adrenergic receptors (both a and B)
  2. Stimulates release of NE
66
Q

What is Ephedrine (mixed acting agonist) used to treat?

A

Nasal congestion
Hypotension

(it is vasoconstrictor)

67
Q

What are the other effects of Ephedrine (mixed acting agonist)?

A

Bronchodilation (via B2)
Increased HR (via B1)
CNS stimulation

68
Q

What are the problems with indirect acting and mixed acting agonists?

A

Acute tolerance (tachyphylaxis)
Repeated administrations (depletion of neurotransmitter)

69
Q

What drugs do indirect acting and mixed acting agonists interact with?

A

TCAs
MAOIs

70
Q

What is dopamine?

A

CNS neurotransmitter

71
Q

Where else can dopamine receptors be located?

A

Peripheral tissue (causing peripheral effects)

72
Q

What are the dopamine receptors?

A

D1-D5
GPCRs

73
Q

What do low infusion rates of dopamine on peripheral organs affect? What is the result?

A

Vasodilation of visceral vasculature

Result = increased urinary flow/renal blood flow

74
Q

What do intermediate rates of dopamine on peripheral organs affect? What is the result?

A

Stimulation of myocardial contractility
Increased conductivity

Result = increased cardiac output

75
Q

What do higher doses of dopamine on peripheral organs affect? What is the result?

A

Vasoconstriction
Increased BP (via a1, B1, B2)

Result = poor peripheral circulation

76
Q

Adverse reactions of adrenergic (sympathomimetic) agents on the brain vs on the heart

A

Brain: anxiety, tremors, restlessness
Heart: palpitations, arrhythmias, increased BP

77
Q

Contraindications of adrenergic (sympathomimetic) agents

A

Uncontrolled hypertension
Angina (chest pain from ischemia)
Hyperthyroidism (adrenergic system in overdrive)

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