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ARCHIVED: Pharmacology for Nurse Anesthesia > Exam 2: ANS Pharmacology > Flashcards

Exam 2: ANS Pharmacology Flashcards

1
Q

Organs that are only innervated by SNS:

A 
Sweat glands 
Blood vessels (though they have M receptors)
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2
Q

Organs only innervated by PSNS:

A

Ciliary muscle of eye

Bronchial smooth muscle (though they have B2 receptors)

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3
Q

Receptors on skeletal muscle:

A

Nicotinic (Nm)

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4
Q

Receptors on blood vessels and other smooth muscle:

A

Adrenergic (alpha/beta)

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5
Q

Receptors on sweat glands:

A

Muscarinic (M1-5)

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6
Q

Receptors on adrenal medulla:

A

Nicotinic - preganglionic

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7
Q

Receptors on salivary glands etc:

A

Muscarinic

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8
Q

How is the adrenal medulla an anomaly?

A

Acts like a ganglia but releases NE/Epi as hormones

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9
Q

Norepi/epi % release:

A

Norepi 20%

Epi 80%

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10
Q

How are the sweat glands an anomaly?

A

Innervated by the SNS, but postganglionic neuron releases ACh onto a muscarinic ACh receptor

Sympathetic cholinergic!

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11
Q

How are the blood vessels an anomaly?

A

No PSNS innervation, although muscarinic ACh receptors present (require circulating ACh)

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12
Q

Name the endogenous catecholamines:

A

Epi
Norepi
Dopa

ENDogenous

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13
Q

Name the synthetic catecholamines:

A

Isoproterenol

Dobutamine

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14
Q

Name the indirect acting synthetic non-catecholamines:

A

Mephentermine
Ephedrine
Amphetamines

MEA culpa is an INDIRECT way of saying “my bad!”

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15
Q

Name the direct acting synthetic non-catecholamines:

A

Phenylephrine
Methoxamine

Don’t comment publicly, just PM me directly…

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16
Q

Name the selective α2 agonists:

A

Clonidine

Dexmedetomidine

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17
Q

Name the selective β2 agonists:

A

Abuterol
Terbutaline
Ritodrine

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18
Q

How do direct agonists work?

A

Either mimic the endogenous substance or directly activate the receptor

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19
Q

How do indirect agonists work?

A

Stimulate release of NTs

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20
Q

Structure of all sympathomimetics:

A

Beta-phenylethylamine derivatives

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21
Q

Chain of catecholamine formation:

A 
Tyrosine
DOPA
Dopamine
Norepinephrine
Epinephrine
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22
Q

Termination of effect of catecholamines:

A

Reuptake (I/II)
MAO
COMT
Lungs

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23
Q

Termination of effect of non-catecholamines:

A

MAO

Urinary excretion

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24
Q

Reuptake I vs II:

A

I: Neuronal (80%)
II: Extraneuronal

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25
How do MAO inhibitors cause problems with sympathomimetics?
Non-catecholamines are unable to be broken down and have an increased effect
26
Relative receptor activation of α-agonists:
Phenylephrine: α1 > α2 Clonidine: α2 > α1
27
Relative receptor activation of mixed α/β agonists:
Norepi: α1=α2; β1 >>> β2 Epi: α1=α2; β1=β2 Equal Epi Nonequal Norepi
28
Relative receptor activation of β-agonists:
Dobutamine: β1 > β2 Isoproterenol: β1 = β2 Terbutaline/albuterol: β2 > β1
29
Relative receptor activation of dopamine agonists:
Dopamine: D1 = D2 Fenoldopam: D1 >> D2
30
MoA of epinephrine:
α and β receptor activation | Most potent α receptor activator!
31
PK of epinephrine:
Very poorly lipid soluble (no CNS effect) IV onset: 1-2 min Duration: 5-10 min
32
Indications for epinephrine:
Bronchial asthma Acute allergic rxn Cardiac arrest/asystole Vfib unresponsive to defib
33
Resuscitation dose of epinephrine:
10mcg/kg IV
34
Infusion dose of epinephrine:
1-2mcg/min: β2 for bronchospasm 4-5mcg/min: β1 for ↑ contractility 10-20 mcg/min: α (more prominent as dose ↑) and β
35
CV effects of epinephrine:
``` BP regulation is major role α1: Vasoconstriction, ↑BP / CVP / work α2: Negative feedback ↓ BP β1: ↑ contractility, HR, CO, BP β2: Peripheral vasodilation ↓ BP ``` At moderate doses: SBP increases DBP decreases MAP stays the same
36
Cerebral effects of epinephrine:
Minimal vasoconstriction | ↑ CBF
37
Ocular effects of epinephrine:
Dilation of pupils/mydriasis (α1) | Increased humoral outflow (α1/α2), production of aquaous humor (β1)
38
Respiratory effects of epinephrine:
Bronchodilation (β2) Decreased histamine release (β2) Reduced mucosal secretions (α1) Good for treating bronchospasm, anaphylaxis
39
GI effects of epinephrine:
Decreased digestive secretions (α2) Decreased peristalsis (α, β2) Decreased blood flow (α1)
40
GU effects of epinephrine:
Renal blood flow dramatically reduced! (α1) Increased renin release (β1) Contraction of urethral sphincter (α1) and bladder relaxation (β2) Inhibition of labor (β2)
41
Metabolic effects of epinephrine:
↑ glycogenesis, insulin release (β2) - inhibition of release by α2, but minor Peri-op pts need *more* insulin than usual
42
Hypotension dosing for norepi:
4-16mcg/min
43
Indications for norepi perioperatively:
Hemorrhage (redistribute remaining blood) | Septic shock last line
44
Effects of norepi:
``` Intense vasoconstriction (α1 with no β2 to balance!!) ↑ BP activates baroreceptors so ↓ HR ```
45
Dosing of dopamine:
1-3 mcg/kg/min: D1 receptor dominates 3-10 mcg/kg/min: β1 receptor dominates > 10 mcg/kg/min: α receptor dominates
46
Effects of dopamine:
↑ contractility, renal BF, UOP, GFR ↑ endogenous norepi release Inhibition of carotid bodies / altered response to hypoxia ↑ ocular pressure
47
Dopamine and dobutamine:
Synergistic; reduces afterload, improves CO
48
MoA of isoproterenol:
β1 and β2 agonist
49
Effects of isoproterenol:
↑ HR, contractility | ↓ SVR means ↑ SBP, ↓ DBP, ↓ MAP
50
Dosing of isoproterenol for block/dysrhythmias:
1-5 mcg/min
51
PK of isoproterenol:
Rapidly metabolized by COMT (need to infuse)
52
Why increased MI risk with isoproterenol?
↑ HR means ↓ O2 delivery to the myocardium
53
Dosing for dobutamine:
2-10 mcg/kg/min
54
Receptors targeted by dobutamine:
β1 selective at < 5 mcg/kg/min | Weak a1 stimulation > 5 mcg/kg/min
55
Effects of dobutamine:
↑ CO without increasing HR/BP | Coronary artery vasodilator
56
MoA of ephedrine:
Indirect agonist at α and β receptors
57
Indications for ephedrine:
Hypotension with bradycardia
58
Dosing for ephedrine:
10-25 mg IV | 10-50 mg IM
59
Negative effect of ephedrine:
Tachyphylaxis d/t norepi depletion
60
PK of ephedrine:
Excreted unchanged in urine Metabolized by MAO and conjugated in liver Et1/2: 3 hrs
61
MoA of phenylephrine:
Direct α1 agonist
62
Effects of phenylephrine:
Venoconstriction ( > arterial) ↑ BP, SVR ↓ HR, CO
63
Indications for phenylephrine:
Hypotension (not d/t hypovolemia)
64
Dosing for phenylephrine:
50-200 mcg IV | Infusion: 20-50 mcg/min
65
Overdose of phenylephrine or epinephrine:
``` Give phentolamine (α1 antagonist) or NTG/NTP NOT a β-blocker, which will ↓ contractility and rate and leave massive vasoconstriction ```
66
Indications for β2 agonists:
Premature labor, asthma, COPD
67
Side effects of β2 agonists:
Tremor | Reflex tachycardia
68
Indications for albuterol:
Asthmatic bronchospasm
69
Dosing of albuterol:
100mcg/puff 2 puffs q4-6hr Nebulization: 15mg/hr for 2 hours
70
Side effects of albuterol:
Tachycardia, hypokalemia
71
Indications for terbutaline:
Asthma | Premature labor
72
Difference between salmeterol and albuterol:
Salmeterol duration > 12 hrs
73
Indication for ritordine:
Premature labor
74
Side effects of ritordine:
↑ HR/CO d/t β1 activity | Can cause pulmonary edema
75
MoA and indication for midodrine:
α1 agonist | Postural hypotension
76
Effects of amphetamine:
↑ release of norepi, dopamine, 5HT Blocks reuptake Blocks vesicular transport Inhibits MAO
77
Difference between amphetamine and methamphetamine:
Methamphetamine has higher CNS effects
78
MoA of cocaine:
Prevents reuptake of catecholamines (norepi, dopamine, 5HT)
79
MoA of reserpine:
Vesicles lose ability to store norepi/dopamine/5HT
80
CV effects of α1 antagonism:
Vasodilation ↓ PVR, BP | Postural hypotension
81
CV effects of α2 antagonism:
↑ norepi release by blocking negative feedback
82
GI effects of α-antagonism:
Muscle relaxation and easier urination
83
ENT effects of α-antagonism:
Miosis | Nasal congestion
84
Competitive α-antagonists:
Phentolamine Prazosin Yohimbine
85
Covalently binding α-antagonist:
Phenoxybenzamine
86
MoA of phentolamine:
Nonselective α-blocker
87
Effects of phentolamine:
Vasodilation ↓BP ↑HR, CO
88
Indications for phentolamine:
``` Hypertensive emergencies (pheochromocytoma, ANS dysreflexia) Extravascular infiltration of sympathomimetics ```
89
Dosing/timing of phentolamine for HTN crisis:
30-70 mcg/kg IV Onset: 2 min Duration: 10-15 min
90
Dosing of phentolamine for extravasation:
2.5 - 5mg in 10ml NS
91
MoA of phenoxybenzamine:
Binds covalently to α1 receptors
92
Effects of phenoxybenzamine:
↓ SVR, vasodilation
93
PK of phenoxybenzamine:
Pro-drug Onset: 1hr Et1/2: 24 hrs
94
Indications for phenoxybenzamine:
Pheochromocytoma | Raynaud's disease
95
MoA of prazosin:
Selective α1 antagonist
96
MoA of yohimbine:
Selective α2 antagonist
97
Indications for yohimbine:
Orthostatic hypotension | Impotence
98
MoA and indications for terazosin and tamulosin:
α1 antagonists for BPH
99
Effects of β antagonists:
``` Improve O2 supply/demand Can provoke bronchospasm Vasoconstriction in skeletal muscles ↓ renin release ↓ insulin release ```
100
MoA of β antagonists:
Competitive and reversible inhibition of β receptors
101
Chronic use of β antagonists:
Upregulation in receptors | *MUST* take β-blocker on DOS or ↑ risk of intra-op MI
102
Non-selective β antagonists:
Propranolol Nadalol Timolol Pindolol Not Too Particularly Picky
103
Cardioselective/β1 antagonists:
``` Metoprolol Atenolol Acebutolol Betaxolol Esmolol ``` MAABE they're block your receptor, but they're selective
104
Receptor activity of propranolol:
β1 = β2
105
MoA of propranolol:
Lacks sympathomimetic activity; pure antagonist
106
CV effects of propranolol:
↓ HR, contractility, CO Especially during exercise ↑ PVR, coronary VR O2 demand lowered Sodium retention d/t ↓ renin
107
PK of propranolol:
``` Significant first pass effect Highly protein bound (90-95%) Metabolized in liver Et1/2: 2-3 hrs ↓ clearance of amide LAs ↓ pulmonary first pass effect of Fentanyl ```
108
Indications for timolol:
Glaucoma
109
Indications for nadolol:
Long-term tx; preferred d/t daily dosing Et1/2: 20-40 hrs!
110
MoA of metoprolol:
Selective β1 antagonist
111
Effects of metoprolol:
Prevents inotropy, chronotropy
112
PK of metoprolol:
60% first pass effect | Et1/2: 3-4 hrs
113
Dosing of metoprolol:
1-15 mg (1mg at a time)
114
MoA of atenolol:
Most selective β1 antagonist with the least CNS effects
115
PK of atenolol:
Not metabolized in liver; excreted via renal system (VERY polar) Et1/2: 6-7 hrs
116
Indications for atenolol:
Cardiac patients with CAD
117
MoA of betaxolol:
Selective β1 antagonist
118
Et1/2 and indications for betaxolol:
Et1/2: 11-22 hrs Daily dose for HTN Topical for glaucoma with less bronchospastic risk
119
MoA of esmolol:
Selective β1 antagonist
120
PK of esmolol:
Rapid onset Et1/2: 9 min Short duration (< 15 min) Hydrolyzed by plasma esterases
121
Indications for esmolol:
Controlled hypotension Tourniquet pain Short noxious stimuli Wakeups
122
Dosing for esmolol:
0.5 mg/kg IV Infusion: 50-300 mcg/min
123
Side effects of β blockers:
``` ↓ HR, contractility, BP Exacerbation of PVD Bronchospasm Inhibit uptake of K+ into muscles ↓ BP with inhaled agents Fatigue, lethargy N/V/D ```
124
Relative contraindications for β blockers:
Heart block or cardiac failure Asthma DM w/o BG monitoring Hypovolemia
125
Indications for β blockers:
``` HTN Angina Post-MI Tachyarrythmias ↓ SNS tone ```
126
MoA of labetalol:
α1, β1, β2 antagonist | β blockade 7x higher
127
PK of labetalol:
Conjugation metabolism Very little in the urine Et1/2: 5-8 hrs
128
Effects of labetalol:
↓ BP, SVR, HR - maximum drop 5-10 mins after administration
129
Dose of labetalol:
0.1 - 0.5 mg/kg Usually 5mg/time for HTN in OR
130
Side effects of labetalol:
``` Orthostatic hypotension Bronchospasm Heart block CHF Bradycardia ```
131
Which muscarinic receptor most affects the heart?
M2
132
MoA of antimuscarinics:
Competitively, reversibly antagonize ACh at muscarinic receptors
133
Tertiary amines vs. quaternary ammonium antimuscarinics:
Tertiaries: atropine, scopolamine Quaternary: glycopyrrolate Tertiary will cross BBB, quarternary will not
134
PK of IV atropine:
Onset 1 minute Duration 30-60 min Et1/2: 2.3 hours 18% unchanged, rest hydrolysed
135
PK of IV glycopyrrolate:
Onset 2-3 min Duration 30-60 min Et1/2: 1.25 hrs 80% unchanged via urine
136
PK of scopolamine:
Extensively metabolized
137
Indications for antimuscarinics:
``` Antisialogogue Sedation PONV prevention Bradycardia Reversal of NMB (with anticholinesterase) Amnesia promotion in unstable pts Bronchodilation Mydriasis Reduce biliary/ureteral spasm ```
138
Dosing for ipratropium:
40-80 mcg/puff 2 puffs 0.25 - 0.5 mg via nebulizer Not fast onset - 30-90 min
139
Scopolamine dosing:
Pre-op: 0.3 - 0.5 mg | 1.5 mg transdermal for 72 hours' N/V prevent
140
Atropine dosing:
0.2 - 0.4 mg IV pre-op 0.4 - 1.0 mg IV for bradycardia 2 mg in 5ml NS nebulized for bronchodilation
141
Glycopyrrolate dosing:
0.1 - 0.2 mg IV pre-op or bradycardia
142
S/s of central anticholinergic syndrome:
``` Restlessness Hallucinations Somnolence Unconsciousness Delayed emergence ```
143
Tx for central anticholinergic syndrome:
Physostigmine (anticholinesterase) 15-60 mg/kg IV PRN q1-2hrs

ARCHIVED: Pharmacology for Nurse Anesthesia (20 decks)

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