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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
What does the G protein dictate? What are the 3 types of G proteins in adrenergic receptors?
Downstream effects Gq, Gs, Gi
26
Which G protein goes with the a1 adrenergic receptor?
Gq
27
What is the effect of Gq?
Gq -> phospholipase C -> IP3
28
Which G protein goes with the a2 adrenergic receptor?
Gi
29
Which G protein goes with the B1 adrenergic receptor?
Gs
30
What is the effect of Gs and Gi?
Gs -> adenylyl cylase -> cAMP
31
Pharmacological actions and adverse reactions of adrenergic agonists are both _________ of physiological responses of the __________
extensions; SNS
32
What are the physiological and pharmacological responses to SNS/adrenergic agonists?
Increased HR Increased contractility Increased AV conduction
33
What are the adverse reactions when there is too much SNS/adrenergic agonist?
Tachycardia Palpitations Arrhythmias Increased O2 demand (ischemia)
34
Where are a1 adrenergic receptors (Gq) located? What are the effects on these organs?
Blood vessels (vasoconstriction) Pupillary muscles (dilation) Bladder sphincter (contraction) Liver (increased glucose and glucagon)
35
Where are a2 adrenergic receptors (Gi) located? What is the effect on this organ?
CNS - in presynaptic terminals (inhibits NE release)
36
Where are B1 (Gs) adrenergic receptors located? What is the effect on this organ?
Heart (increase HR, contractility, AV conduction)
37
Where are B2 adrenergic receptors located? What are the effects on these organs?
Lungs (bronchodilation) GI (decreased motility, inhibits labor) Blood vessels (vasodilation)
38
Where are B3 adrenergic receptors located? What are the effects on these organs?
Adipose tissue (increased lypolysis and free fatty acids) Bladder wall (relaxation)
39
What are the 3 naturally occurring adrenergic agonists (catecholamines)?
NE Epinephrine Dopamine (A mean cat named Ned)
40
What are the drug name endings for most adrenergic agonists?
-ephrine -edrine -zoline -terol Amphetamine
41
What are the general therapeutic uses for adrenergic agonists?
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
What are the 3 types of adrenergic agonists?
1. Directing acting (receptor binding) 2. Indirect acting (modulation of endogenous catecholamines via synthesis, metabolism, transport) 3. Mixed acting
43
What are the uses for epinephrine?
Local anesthesia Hemostasis (stops bleeding) Anaphylaxis Allergic reactions (hypersensitivity)
44
How does epinephrine work in local anesthesia?
Delay absorption into blood Prolonged action Minimize systemic effects
45
What are the 2 life-threatening symptoms of anaphylaxis?
Airway - trouble breathing, wheezing, chest tightness, swelling of throat, hoarseness, "scratchy" throat Cardiovascular system - chest pain, low BP, rapid HR, weak pulse
46
How does epinephrine reverse the effects of anaphylaxis?
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
What are the a1-selective adrenergic receptor agonists (drugs)?
Phenylephrine Midodrine
48
What is Phenylephrine (a1-selective adrenergic receptor agonist) used for?
Contraction of vascular SM (vasoconstriction increases BP) Temp. relief from nasal congestion - edema (vasoconstriction decreases edema)
49
What is Midodrine (a1-selective adrenergic receptor agonist) used for?
Postural hypotension (vasoconstriction increases BP)
50
What are the a2-selective adrenergic receptor agonists (drugs)?
Clonidine Methyldopa
51
What effects do a2-selective adrenergic receptor agonists (Clonidine, Methyldopa) have?
Sympatholytic
52
Clonidine (2-selective adrenergic receptor agonist) is ________ acting, so it is used for ________ feedback.
centrally; negative
53
What is Clonidine (a2-selective adrenergic receptor agonist) used for?
Anti-hypertension Withdrawal symptoms of opioid addiction (blocks nausea, vomiting, sweating, diarrhea)
54
What is Methyldopa (a2-selective adrenergic receptor agonist) used for?
Anti-hypertension
55
What is the B1-selective adrenergic receptor agonist (drug)?
Dobutamine
56
Dobutamine (B1-selective adrenergic receptor agonist) is a synthetic analog of _________
dopamine (but has no effect on dopamine receptors)
57
What is Dobutamine (B1-selective adrenergic receptor agonist) used for?
Increasing contractility, cardiac output, and HR Short term tx of acute myocardial insufficiency (congestive heart failure, myocardial infarction, cardiac surgery)
58
What is the B2-selective adrenergic receptor agonist (drug)?
Albuterol
59
What is Albuterol (B2-selective adrenergic receptor agonist) used for?
Bronchospasm (asthma, COPD) Preventing breathing difficulties during exercise
60
What are common side effects of Albuterol (B2-selective adrenergic receptor agonist)? Why?
Tremor Tachycardia Palpitations B2 agonists will also activate B1 receptors at high doses!!
61
What are the indirect acting agonists (stimulants)?
Amphetamines (adderall) Methylphenidate (Ritalin) Cocaine
62
What are the mixed acting agonists?
Ephedrine Pseudoephedrine (Sudafed)
63
Describe the mechanism of Amphetamine (indirect acting agonist)
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
What is Amphetamine (indirect acting agonist) used to treat?
ADHD Narcolepsy
65
Describe the mechanism of Ephedrine (mixed acting agonist)
1. Directly binds to and activates adrenergic receptors (both a and B) 2. Stimulates release of NE
66
What is Ephedrine (mixed acting agonist) used to treat?
Nasal congestion Hypotension (it is vasoconstrictor)
67
What are the other effects of Ephedrine (mixed acting agonist)?
Bronchodilation (via B2) Increased HR (via B1) CNS stimulation
68
What are the problems with indirect acting and mixed acting agonists?
Acute tolerance (tachyphylaxis) Repeated administrations (depletion of neurotransmitter)
69
What drugs do indirect acting and mixed acting agonists interact with?
TCAs MAOIs
70
What is dopamine?
CNS neurotransmitter
71
Where else can dopamine receptors be located?
Peripheral tissue (causing peripheral effects)
72
What are the dopamine receptors?
D1-D5 GPCRs
73
What do low infusion rates of dopamine on peripheral organs affect? What is the result?
Vasodilation of visceral vasculature Result = increased urinary flow/renal blood flow
74
What do intermediate rates of dopamine on peripheral organs affect? What is the result?
Stimulation of myocardial contractility Increased conductivity Result = increased cardiac output
75
What do higher doses of dopamine on peripheral organs affect? What is the result?
Vasoconstriction Increased BP (via a1, B1, B2) Result = poor peripheral circulation
76
Adverse reactions of adrenergic (sympathomimetic) agents on the brain vs on the heart
Brain: anxiety, tremors, restlessness Heart: palpitations, arrhythmias, increased BP
77
Contraindications of adrenergic (sympathomimetic) agents
Uncontrolled hypertension Angina (chest pain from ischemia) Hyperthyroidism (adrenergic system in overdrive)

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