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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
What are the B1 selective agonists?
Dobutamine
26
What are the B2 selective agonists?
Albuterol | Terbutaline
27
What are the indirect acting adrenomimetics that release endogenous compounds?
Ephedrine Pseudoephedrine Tyramine
28
What are the indirect acting adrenomimetics thatinhibit reuptake?
Methylphenidate Amphetamine Methamphetamine
29
What is the efficacy ranking of a1 receptors?
Epi > NE >>>> Isoproterenol
30
What is the efficacy ranking of a2 receptors?
Epi >= NE >>>>> Isoproterenol
31
What is the efficacy ranking of B1 receptors?
Isoproternol > Epi >>>> NE (not a full agonist)
32
What is the efficacy ranking of B2 receptors?
Isoproterenol > Epi =NE
33
Why do we see a decrease in diastolic BP with low dose Epi?
Activation of B2 receptors causing vasodilation
34
Why do we see an increase in diastolic BP with high dose epi?
Activation of a1 +a2 at increased levels override the effect of decreased diastolic bp from B2 receptor activation
35
What effects does Epi have?
Low dose: dec diastolic BP, inc CO High Dose: Inc TPR + CO Bronchodilaiton Dec bronchial secretions
36
What are the indications for EPi
Anaphylaxis Cardiac Arrest Bronchospasm
37
What are the contraindications of Epi?
Late term pregnancy
38
What are the toxicities of Epi?
Arrhythmias, Cerebral Hemorrhage, Pulmonary Edema
39
What are the cardiovascular effects of NE?
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
40
Why does the diastolic BP increase much more with NE than for Epi?
NE does not bind to B2 -> no counter to a1 + a2 effects -> leads to large increase in diastolic BP
41
What are the effectis of NE?
Inc CO and TPR Dec HR via baroreceptor reflex Inc MAP
42
What are the indications for NE?
Vasodilatory Shock
43
What are the toxicities for NE?
Ischemia, HTN, Arrythmias
44
What are the contraindications for NE?
Preexisting Vasoconstriciton/ischemia | Late term pregnancy
45
What are the effects of Dopamine?
Low Rates: Dec TPR (D1) and Inc CO (B1) | High Rates: Inc MAP + TPR (a1 +a2+B1)
46
What are the indications for dopamine?
Cardiogenic Shock
47
What are the toxicities for dopamine?
Hypotension at low rates due to D1 | Ischemia at high rates due to adrenergic stimulation
48
What are the contraindications for dopamine?
Tachyarrhythmias | V-Fib
49
What are the CV effects of isoproterenol?
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
What are the effects of isoproterenol?
Non selective B agonist | Dec TPR, Inc CO, Bronchodilation
51
What are the contraindications for Isoproterenol?
Angina with arrhythmias
52
What are the indications for isoproterenol?
Bradycardia/Heart block when TPR is high
53
What are the toxicities for isoproterenol?
Tachyarrhythmias
54
What effects does Dobutamine have?
Selective B1 agonist | Inc CO
55
What are the indications for dobutamine
Short term for CHF/Cardiogenic shock | B- Blockade
56
What are the toxicities for dobutamine?
Arrhythmias, Hypotension
57
What is unique about dobutamine?
Increases inotropy more than increase in chronotropy -> good for increasing perfusion No reflex tachycardia seen with isoproterenol due to limited B2 stimulation
58
What are the effects of Terbutaline/Albuterol?
Selective B2 agonists Bronchodilation Uterine relaxation
59
What are the indications for Terbutaline/Albuterol?
Bronchospasm | COPD
60
What are the toxicities for Terbutaline/Albuterol?
Tachycardia (at higher doses can activate B1) Muscle Tremor Tolerance
61
What are the effects of phenylephrine?
``` Selective a1 agonist Inc TPR/MAP Dec HR (Baroreflex) Pupillary dilation Dec bronchial/sinus secretions ```
62
What are the indications for phenylephrine?
Anesthesia Hypotension SV Tachycardia Mydriatic Agent NAsal decongestant
63
What are the contraindications for phenylephrine?
HTN | Vtach
64
What are the toxicities for phenylephrine?
HTN
65
What are the effects of clonidine?
Selective a2 agonist | Acute inc BP (peripheral ) => Dec BP (central)
66
What are the indicaitons for clonidine?
HTN due to sympathetic activation
67
What are the toxicities of clonidine?
Drymouth | HTN crisis after acute withdrawal
68
What are the effects of indirect acting sympathomimetics?
Inc TPR + Diastolic BP Inc Inotropy. chronotropy + systolic BP CNS stimulation
69
What are the indications for indirect acting sympathomimetics?
ADHD | Narcolepsy
70
What are the contraindications for indirect acting sympathetomimetics?
HTN Rx with MAO inhbiitors Atherosclerosis
71
What are the nonselective adrenergic antagonists?
propanolol timolol nadolol
72
What are the cardioselective antagonists?
B1 antagonists Atenolol Metroprolol
73
What are the partial adrenergic agonists?
B1 + B2 | Pindolol
74
What do all adrenergic antagonists do?
Decrease HR and force of contraction | Decrease renin
75
What needs to be considered when giving B-blockers?
Dont give to asthmatics | B-Blockers may mask sx of hypoglycemia
76
What are the effects of propanolol, timolol and nadolol?
Nonselective B-blockers Dec HR, contractility, renin Dec sympathetic activation Dec Aq humor production
77
What are the indications for propanolol, timolol, nadolol?
HTN Glaucoma Angina
78
What are the contraindications for propanolol, timolol, nadolol?
asthmatic bronchospasm Sinus bradycardia 2nd/3rd degree heart block Cardiogenic shock
79
What are the toxicities of propanolol, timolol, nadolol?
Bronchospasm Mask Hypoglycemia Bradycardia
80
Which nonselective B-Blocker has the longest half life?
Nadolol
81
What is timolol used for?
Opthalmic solution for glaucoma
82
What are the effects of metroprolol, atenolol, esmolol?
Cardiogenic B1 Blockers Dec HR, contractility, renin Dec sympathetic activation
83
What are the indications of metroprolol, atenolol, esmolol?
HTN, angina, arrhythmia
84
What are the contraindications for metroprolol, atenolol, esmolol?
Sinus bradycardia 2nd/3rd degree heart block Cardiogenic shock
85
What are the toxicities of metroprolol, atenolol, esmolol?
Hypotension | Bradycardia
86
Which cardiogenic B1 blockers can cross the BBB?
MEtroprolol | Atenolol does NOT cross BBB
87
What is esmolol used for?
Used in ER as cardiogenic B1 blocker to reverse arrhythmias
88
What does pindolol do?
Partial agonist of B receptors | Partially decrease BP, cotnractiliy, renin, sympathetic activation
89
What are the indications for pindolol?
HTN
90
What are the nonselective a receptor blockers?
Phentolamine | Phenoxybenzamine
91
What is the difference between phentolamine and phenoxybenzamine?
Both are nonselective a-receptor blockers Phentolamine is reversible phenoxybenzamine is irreversible
92
What are the effects of phentolamine/phenoxybenzamine?
Dec BP, Inc chronotropy + Inotropy
93
What are the indications for phentolamine/phenoxybenzamine?
HTN with pheochromocytoma | Extravasation from vasoconstriction
94
What are the contraindications for phenotlamine/phenoxybenzamine?
CAD
95
What are the toxicities of phentolamine/phenoxybenzamine?
Prolonged hypotension | Reflex Tachy
96
What are hte selective a1 receptor blockers?
Prazosin, Doxazosin Terazosin
97
What are the effects of prazosin, terazosin, doxazosin?
Inhibit vasoconstriction | Relax prostate smooth muscle
98
What are the indications for prazosin, terazosin, doxazosin?
HTN | BPH
99
What are the toxicities of prazosin, doxazosin, terazosin?
Orthostatic hypotension

Pharmacology Block 2 (6 decks)

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