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Pharmacology Block 2 > Adrenergic Agonists > Flashcards

Adrenergic Agonists Flashcards

1
Q

Where does the sympathetic NS arise from? Describe their pre/post ganglionic fibers

A

Thoracolumbar
Short preganglionic
Long postganglionic

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2
Q

Where does the parasympathetic NS arise from? Describe their pre/post ganglionic fibers

A

Craniosacral
Long preganglionic
Short postganglionic

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3
Q

How is the adrenal gland innervated by the autonomic NS?

A

Sympathetic preganglionic from thoracic spine directly to adrenal medulla to induce epinephrine hormone secretion

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4
Q

What kind of neurotransmitters are involved in the sympathetic nervous system and what are their receptors?

A

Pre: ACh => Binds Nicotinic receptors
Post: NE => Binds adrenergic receptors

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5
Q

W?hat kind of neurotransmitters are involved in the parasympathetic nervous system and what are their receptors?

A

Pre: Ach => binds Nicotinic Receptors
Post: Ach => binds nicotinic and muscarinic receptors

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6
Q

What are the exceptions to the sympathetic neurotransmitter properties?

A

Sweat glands + some skeletal mucle in smooth muscle vasculature

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7
Q

What are the effects of parasympathetic stimulation

A 
Miosis
Bradycardia
Bronchoconstriction
Increased GI motility
Increased bladder emptying
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8
Q

What are the effects of sympathetic stimulation?

A 
Mydriasis
Inc HR
Inc Inotropy
Bronchodilation
Vascular constriction/diliation
Decreasd GI motility
Decreased Bladder emptying
Increased blood sugar/glycogenolysis
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9
Q

What does Tyrosine Hydroxylase do?

A

Convert Tyrosine to Dopa, a precursor for Dopamine, which is a precursor for NE

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10
Q

Where is dopamine converted to NE?

A

In the synaptic vesicle

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11
Q

Where are a1 receptors found and what do they do?

A

Vascular Smooth Muscle: Vasoconstriction
Pupillary DIlator Muscle: Mydriasis
Pilomotor: Erect hair

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12
Q

Where are a2 receptors found and what do they do?

A

adrenergic/cholinergic nerve terminals: decrease neurotransmitter release
Some smooth muslce: Vasoconstriction

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13
Q

Where are B1 receptors found and what do they do?

A

Heart: Increase HR and Increase Inotropy
JGA: Increase Renin secretion

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14
Q

Where are B2 receptors found and what do they do?

A 
Lungs: Bronchodilations
Uterine/Vascular SMooth muscle: Relaxation
Liver: Increase glycogenolysis
Pancreatic B Cells: Increase insulin
Somatic Nerve Terminals: Tremor
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15
Q

Where are D1 receptors found and what do they do?

A

Renal + Sphlancnic Blood vessels : Relax and vasodilate

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16
Q

Where are D2 receptors found and what do they do?

A

Nerve Terminals: Inhibit Adenylyl Cyclase

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17
Q

What G protein is a1 receptor coupled to and how does it act?

A

Gaq : activates PLC -> cleave PIP2 -> inc IP3 + DAG -> Activate MLCK -> Phosphorylate light chain myosin -> contraction

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18
Q

What G protein is a2 receptor coupled to and what does it do?

A

Gai: decrease cAMP -> inhibit PKA -> inhibit voltage gated Ca2+ channels -> decrease neurotransmitter release

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19
Q

What G protein is B1 receptor coupled to and what does it do?

A

Gas: opposite of a2; Activate AC -> inc cAMP -> inc PKA -> phosphorylate Calcium channels

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20
Q

What G protein is B2 receptor coupled 2 and what does it do?

A

Gas: opposite of a1; inc cAMP -> inc PKA -> phosphorylate MLCK -> decrease enzyme activity on calmodulin -> decrease phosphorylation of myosin light chain -> relaxation

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21
Q

What are the nonselective direct acting adrenomimet

A

NE
Epi
Dopamine

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22
Q

What are the a1 selective adrenomimetics?

A

Phenylephrine

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23
Q

What are the a2 selective adrenomimetics?

A

Clonidine

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24
Q

What are the nonselective B agonists?

A

Isoproterenol

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25
Q

What are the B1 selective agonists?

A

Dobutamine

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26
Q

What are the B2 selective agonists?

A

Albuterol

Terbutaline

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27
Q

What are the indirect acting adrenomimetics that release endogenous compounds?

A

Ephedrine
Pseudoephedrine
Tyramine

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28
Q

What are the indirect acting adrenomimetics thatinhibit reuptake?

A

Methylphenidate
Amphetamine
Methamphetamine

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29
Q

What is the efficacy ranking of a1 receptors?

A

Epi > NE&raquo_space;» Isoproterenol

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30
Q

What is the efficacy ranking of a2 receptors?

A

Epi >= NE&raquo_space;»> Isoproterenol

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31
Q

What is the efficacy ranking of B1 receptors?

A

Isoproternol > Epi&raquo_space;» NE (not a full agonist)

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32
Q

What is the efficacy ranking of B2 receptors?

A

Isoproterenol > Epi =NE

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33
Q

Why do we see a decrease in diastolic BP with low dose Epi?

A

Activation of B2 receptors causing vasodilation

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34
Q

Why do we see an increase in diastolic BP with high dose epi?

A

Activation of a1 +a2 at increased levels override the effect of decreased diastolic bp from B2 receptor activation

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35
Q

What effects does Epi have?

A

Low dose: dec diastolic BP, inc CO
High Dose: Inc TPR + CO
Bronchodilaiton
Dec bronchial secretions

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36
Q

What are the indications for EPi

A

Anaphylaxis
Cardiac Arrest
Bronchospasm

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37
Q

What are the contraindications of Epi?

A

Late term pregnancy

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38
Q

What are the toxicities of Epi?

A

Arrhythmias, Cerebral Hemorrhage, Pulmonary Edema

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39
Q

What are the cardiovascular effects of NE?

A

Increased CO and Systolic BP from B1 receptor activation
Vasoconstriction leading to inc diastolic BP from a1+a2

Inc diastolic BP -> Baroreceptor reflex-> dec HR

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40
Q

Why does the diastolic BP increase much more with NE than for Epi?

A

NE does not bind to B2 -> no counter to a1 + a2 effects -> leads to large increase in diastolic BP

41
Q

What are the effectis of NE?

A

Inc CO and TPR
Dec HR via baroreceptor reflex
Inc MAP

42
Q

What are the indications for NE?

A

Vasodilatory Shock

43
Q

What are the toxicities for NE?

A

Ischemia, HTN, Arrythmias

44
Q

What are the contraindications for NE?

A

Preexisting Vasoconstriciton/ischemia

Late term pregnancy

45
Q

What are the effects of Dopamine?

A

Low Rates: Dec TPR (D1) and Inc CO (B1)

High Rates: Inc MAP + TPR (a1 +a2+B1)

46
Q

What are the indications for dopamine?

A

Cardiogenic Shock

47
Q

What are the toxicities for dopamine?

A

Hypotension at low rates due to D1

Ischemia at high rates due to adrenergic stimulation

48
Q

What are the contraindications for dopamine?

A

Tachyarrhythmias

V-Fib

49
Q

What are the CV effects of isoproterenol?

A

Inc CO (B1) and Dec Diastolic BP (B2)

Systolic initially goes up but decreases as diastolic bp decreases => widened pulse pressure

Inc HR due to reflex tachycardia from decreased diastolic BP

50
Q

What are the effects of isoproterenol?

A

Non selective B agonist

Dec TPR, Inc CO, Bronchodilation

51
Q

What are the contraindications for Isoproterenol?

A

Angina with arrhythmias

52
Q

What are the indications for isoproterenol?

A

Bradycardia/Heart block when TPR is high

53
Q

What are the toxicities for isoproterenol?

A

Tachyarrhythmias

54
Q

What effects does Dobutamine have?

A

Selective B1 agonist

Inc CO

55
Q

What are the indications for dobutamine

A

Short term for CHF/Cardiogenic shock

B- Blockade

56
Q

What are the toxicities for dobutamine?

A

Arrhythmias, Hypotension

57
Q

What is unique about dobutamine?

A

Increases inotropy more than increase in chronotropy -> good for increasing perfusion

No reflex tachycardia seen with isoproterenol due to limited B2 stimulation

58
Q

What are the effects of Terbutaline/Albuterol?

A

Selective B2 agonists
Bronchodilation
Uterine relaxation

59
Q

What are the indications for Terbutaline/Albuterol?

A

Bronchospasm

COPD

60
Q

What are the toxicities for Terbutaline/Albuterol?

A

Tachycardia (at higher doses can activate B1)
Muscle Tremor
Tolerance

61
Q

What are the effects of phenylephrine?

A 
Selective a1 agonist
Inc TPR/MAP
Dec HR (Baroreflex)
Pupillary dilation
Dec bronchial/sinus secretions
62
Q

What are the indications for phenylephrine?

A

Anesthesia Hypotension
SV Tachycardia
Mydriatic Agent
NAsal decongestant

63
Q

What are the contraindications for phenylephrine?

64
Q

What are the toxicities for phenylephrine?

65
Q

What are the effects of clonidine?

A

Selective a2 agonist

Acute inc BP (peripheral ) => Dec BP (central)

66
Q

What are the indicaitons for clonidine?

A

HTN due to sympathetic activation

67
Q

What are the toxicities of clonidine?

A

Drymouth

HTN crisis after acute withdrawal

68
Q

What are the effects of indirect acting sympathomimetics?

A

Inc TPR + Diastolic BP
Inc Inotropy. chronotropy + systolic BP
CNS stimulation

69
Q

What are the indications for indirect acting sympathomimetics?

A

ADHD

Narcolepsy

70
Q

What are the contraindications for indirect acting sympathetomimetics?

A

HTN
Rx with MAO inhbiitors
Atherosclerosis

71
Q

What are the nonselective adrenergic antagonists?

A

propanolol
timolol
nadolol

72
Q

What are the cardioselective antagonists?

A

B1 antagonists
Atenolol
Metroprolol

73
Q

What are the partial adrenergic agonists?

A

B1 + B2

Pindolol

74
Q

What do all adrenergic antagonists do?

A

Decrease HR and force of contraction

Decrease renin

75
Q

What needs to be considered when giving B-blockers?

A

Dont give to asthmatics

B-Blockers may mask sx of hypoglycemia

76
Q

What are the effects of propanolol, timolol and nadolol?

A

Nonselective B-blockers
Dec HR, contractility, renin
Dec sympathetic activation
Dec Aq humor production

77
Q

What are the indications for propanolol, timolol, nadolol?

A

HTN
Glaucoma
Angina

78
Q

What are the contraindications for propanolol, timolol, nadolol?

A

asthmatic bronchospasm
Sinus bradycardia
2nd/3rd degree heart block
Cardiogenic shock

79
Q

What are the toxicities of propanolol, timolol, nadolol?

A

Bronchospasm
Mask Hypoglycemia
Bradycardia

80
Q

Which nonselective B-Blocker has the longest half life?

81
Q

What is timolol used for?

A

Opthalmic solution for glaucoma

82
Q

What are the effects of metroprolol, atenolol, esmolol?

A

Cardiogenic B1 Blockers
Dec HR, contractility, renin
Dec sympathetic activation

83
Q

What are the indications of metroprolol, atenolol, esmolol?

A

HTN, angina, arrhythmia

84
Q

What are the contraindications for metroprolol, atenolol, esmolol?

A

Sinus bradycardia
2nd/3rd degree heart block
Cardiogenic shock

85
Q

What are the toxicities of metroprolol, atenolol, esmolol?

A

Hypotension

Bradycardia

86
Q

Which cardiogenic B1 blockers can cross the BBB?

A

MEtroprolol

Atenolol does NOT cross BBB

87
Q

What is esmolol used for?

A

Used in ER as cardiogenic B1 blocker to reverse arrhythmias

88
Q

What does pindolol do?

A

Partial agonist of B receptors

Partially decrease BP, cotnractiliy, renin, sympathetic activation

89
Q

What are the indications for pindolol?

90
Q

What are the nonselective a receptor blockers?

A

Phentolamine

Phenoxybenzamine

91
Q

What is the difference between phentolamine and phenoxybenzamine?

A

Both are nonselective a-receptor blockers
Phentolamine is reversible
phenoxybenzamine is irreversible

92
Q

What are the effects of phentolamine/phenoxybenzamine?

A

Dec BP, Inc chronotropy + Inotropy

93
Q

What are the indications for phentolamine/phenoxybenzamine?

A

HTN with pheochromocytoma

Extravasation from vasoconstriction

94
Q

What are the contraindications for phenotlamine/phenoxybenzamine?

95
Q

What are the toxicities of phentolamine/phenoxybenzamine?

A

Prolonged hypotension

Reflex Tachy

96
Q

What are hte selective a1 receptor blockers?

A

Prazosin,
Doxazosin
Terazosin

97
Q

What are the effects of prazosin, terazosin, doxazosin?

A

Inhibit vasoconstriction

Relax prostate smooth muscle

98
Q

What are the indications for prazosin, terazosin, doxazosin?

99
Q

What are the toxicities of prazosin, doxazosin, terazosin?

A

Orthostatic hypotension

Pharmacology Block 2 (6 decks)

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