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N929 - Anesthesia Pharmacology > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

(169 cards)

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1
Q

steps of neurotransmission

A
  • synthesis
  • storage
  • release
  • action at receptor
  • termination
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2
Q

what kind of receptor is a muscarinic cholinergic receptor

A

GPCR

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3
Q

how many types of muscarinic receptors are there?

A

5 subtypes, 2 subgroups

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4
Q

stimulatory muscarinic cholinergic receptors

A

M1, M3, M5

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5
Q

inhibitory muscarinic cholinergic receptors

A

M2, M4

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6
Q

endogenous ligand of muscarinic cholinergic receptor

A

ACh

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7
Q

autonomic effector tissues

A

heart, endothelium, smooth muscle, glands, and the CNS

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8
Q

M1

A

CNS

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9
Q

M2

A

heart

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10
Q

M3

A

smooth muscle, glands, endothelium, eye (circular and ciliary muscle)

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11
Q

M4

A

CNS

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12
Q

M5

A

CNS

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13
Q

nicotinic cholinergic receptor type

A

ligand-gated Na+ and K+ depolarizing channel

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14
Q

two subtypes of nicotinic receptor

A

NicN and NicM

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15
Q

location of nicotinic receptors

A

autonomic ganglia, skeletal muscle innervation, CNS

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16
Q

muscarinic cholinergic receptor transmission

A

ACh binds –> confirmational change –> g protein breaks off –> second messenger –> causes a cellular response

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17
Q

nicotinic cholinergic receptor transmission

A

ACh binds –> confirmational change –> channel opens and positively charged ions influx through channel

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18
Q

NicN

A

ANS ganglia (all), adrenal medulla, CNS

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19
Q

NicM

A

skeletal muscle NMJ

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20
Q

alpha adrenergic receptor type

A

GPCR

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21
Q

alpha adrenergic receptor ligand

A

NE; also EPI and Dopa in large doses

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22
Q

excitatory alpha adrenergic receptor

A

alpha1

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23
Q

alpha1 adrenergic receptor transmission

A

increase in calcium –> calmodulin activation –> increased actin/myosin interaction –> smooth muscle contraction

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24
Q

inhibitory alpha adrenergic receptor

A

alpha 2

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25
alpha2 adrenergic receptor transmission
decrease in cAMP --> decrease in NE release
26
alpha1
excitatory; smooth muscle, GU sphincters (esp. bladder), most vascular smooth muscle (skin, splanchic), eye (radial muscle), heart, liver
27
alpha 2
inhibitory; pre-synaptic nerve terminal, platelets, pancreatic beta cells
28
beta adrenergic receptor type
GPCR
29
beta adrenergic receptor ligand
NE, Epi
30
beta adrenergic receptor transmission
activation of adenyl cyclase --> increase in cAMP --> increase in kinase activation and phosphorylation of protein
31
beta adrenergic receptor tissues
heart, kidney, liver, smooth muscle, skeletal muscle, fat cells
32
beta1
heart, kidney (JG cells - cause renin release)
33
beta2
smooth muscle (bronchiolar, uterine, etc.), vascular smooth muscle (skeletal muscle beds), liver, skeletal muscle, heart
34
beta3
adipose tissue
35
PSNS action
rest and digest
36
PSNS origin
``` cranial nerves (III, VII, IX, X) and sacral region vagus nerve 90% ```
37
PSNS ganglia location
target organ
38
PSNS preganglionic length and NT
long, ACh
39
PSNS postganglionic length and NT
short, ACh
40
divergence of PSNS
discrete; this is because postganglionic neurons are not branched, but are directed to a specific target organ
41
PSNS receptor on postganglionic neuron
cholinergic
42
SNS action
fight or flight
43
SNS origin
thoracolumbar region of spinal cord; T1-T12 and L1-L5
44
SNS ganglia location
sympathetic chain ganglion or paravertebral chain
45
SNS preganglionic length and NT
short, ACh
46
SNS postganglionic length and NT
long, NE
47
divergence of SNS
diffuse; because postganglionic neurons may innervate more than one organ
48
SNS receptor on postganglionic neuron
adrenergic
49
exceptions to dual innervation
- adrenal medulla (SNS) - most sweat glands (SNS) - kidney (SNS) - blood vessels (SNS) - piloerector muscle (SNS)
50
eye iris radial muscle
SNS - alpha1 - contracts (mydriasis)
51
eye iris circular muscle
PSNS - M3 - contracts (miosis)
52
eye ciliary muscle
SNS - beta2 - relaxes (far vision) | PSNS - M3 - contracts (near vision)
53
SA node
SNS - beta1 - accelerates (increased HR) | PSNS - M2 - decelerates (decreased HR)
54
ectopic pacemakers
SNS - beta1 - accelerates (increased HR)
55
contractility of myocardium
SNS - beta1 - increases (increased force of contraction) | PSNS - M2 - decreases (atria, decreased force of contraction)
56
skin, splanchnic blood veseels
SNS - alpha1 - contracts (vasoconstriction)
57
skeletal muscle blood vessels
SNS - beta2 - relaxes (vasodilation)
58
bronchiolar smooth muscle
SNS - beta2 - relaxes (bronchodilation) | PSNS - M3 - contracts (bronchoconstriction)
59
GI walls
SNS - alpha2, beta2 - relaxes | PSNS - M3 - contracts
60
GI sphincters
SNS - alpha1 - contracts | PSNS - M3 - relaxes
61
GI secretion
SNS - alpha2 - decreases | PSNS - M3 - increases
62
GU bladder wall
SNS - beta2 - relaxes | PSNS - M3 - contracts
63
GU Sphincter
SNS - alpha1 - contracts | PSNS - M3 - relaxes
64
Uterus (pregnant)
SNS - beta2 - relaxes SNS - alpha1 - contracts PSNS - M - contracts
65
Penis seminal vesicles
SNS - alpha1 - ejaculation | PSNS - M - erection
66
pilomotor smooth muscles
SNS - alpha1 - contracts
67
sweat glands eccrine
SNS - M - increases
68
sweat glands apocrine (stress)
SNS - alpha - increases
69
liver
SNS - beta2, alpha - gluconeogenesis, glycogenolysis
70
fat cells
SNS - beta3 - lipolysis
71
kidney
SNS - beta1 - renin release from JG cells
72
cholinergic muscarinic agonist drugs
- acetylcholine - muscarine - pilocarpine - bethanechol
73
cholinergic muscarinic agonist MOA
Receptor agonist | -acts directly on the muscarinic receptor
74
cholinergic muscarinic agonist clinical uses
- eye (glaucoma, contract ciliary body, increase outflow of aqueous humor) - GI/GU (post op ileus, post op urinary retention, xerostomia)
75
cholinergic muscarinic agonist adverse affects
``` CV: -decreased HR -decreased CO and arterial pressure -vasodilation via NO (produced by endothelial cells) GI: increased motility Bladder: contracts Lungs: bronchoconstriction Secretions: -increased sweat -increased salivation -increased lacrimation -increased bronchial Eye: -miosis -accommodation for near vision -decreased intraocular pressure Toxicity antidote --> atropine ```
76
cholinergic nicotinic agonist drugs
- Succinylcholine - Varenicline - Acetylcholine - Nicotine
77
cholinergic nicotinic agonist MOA
Receptor agonist - acts directly on the nicotinic receptor - NN – stimulation of post ganglionic neuronal activity (Autonomic NS); CNS stimulation - NM – activation of NM endplates; contraction
78
cholinergic nicotinic agonist clinical uses
- NN – smoking cessation (NRT, nicotine replacement therapy) (varenicline) - NM – depolarizing skeletal muscle paralysis (succinylcholine)
79
cholinergic nicotinic agonist adverse effects
NN - CNS stimulation - skeletal muscle depolarization/blockade - HTN - increased HR - N/V/D
80
AChE inhibitor (reversible) drugs
- Edrophonium - Neostigmine - Pyridostigmine - Physostigmine - Donepezil
81
AChE inhibitor (reversible) MOA
- binds to active site and inhibits activity of AChE; undergoes hydrolysis; acidic portion slowly released and prevents ACh from binding - increase in ACh - amplifies effects at cholinergic synapses - indirect stimulant of nicotinic and muscarinic receptors by increased ACh
82
edrophonium PK/PD
- alcohol - short acting - very polar - onset 30-60 seconds - DOA – 10 min
83
neostigmine PK/PD
- carbamate - intermediate acting - moderately polar - onset 10-30 min - DOA – 2-4 hours
84
physostigmine PK/PD
- intermediate acting - nonpolar - crosses BBB - onset 3-8 min - DOA – 1 hour
85
AChE inhibitors (reversible) clinical uses
- reversal of NM blockade by non-depolarizing drug - myasthenia gravis diagnosis and treatment - glaucoma - GI-ileus - post op urinary retention - Alzheimer’s disease (donepezil)
86
AChE inhibitors (reversible) adverse effects
Autonomic: -increased secretions (salivary, lacrimal, bronchial, GI) -increased GI motility -bronchoconstriction -bradycardia -hypotension -miosis; accommodation for near vision NMJ: -reverses NM block by non-depolarizing blocker -improves transmission (myasthenia gravis) -large doses – depolarizing block CNS: -therapeutic (dementia treatment) -toxicity (excitation = possible convulsion; depression follows = unconscious) Toxicity antidote --> atropine; pralidoxime
87
AChE inhibitor (irreversible) drugs
- Echothiophate | - Organophosphate insecticides
88
AChE inhibitor (irreversible) PK/PD
long duration
89
AChE inhibitor (irreversible) clinical uses
- reversal of NM blockade by non-depolarizing drug - myasthenia gravis diagnosis and treatment - glaucoma - GI-ileus - post op urinary retention - non-therapeutic insecticide (organophosphate insecticide)
90
AChE inhibitor (irreversible) adverse effects
Autonomic: -increased secretions (salivary, lacrimal, bronchial, GI) -increased GI motility -bronchoconstriction -bradycardia -hypotension -miosis; accommodation for near vision NMJ: -reverses NM block by non-depolarizing blocker -improves transmission (myasthenia gravis) -large doses – depolarizing block CNS: -therapeutic (dementia treatment) -toxicity (excitation = possible convulsion; depression follows = unconscious)
91
muscarinic antagonist drugs
- atropine - glycopyrrolate - scopolamine
92
muscarinic antagonist MOA
competitively blocks ACh from binding to the receptor and producing its effects
93
muscarinic antagonist clinical uses
``` CV: -tx of bradycardia CNS: -motion sickness (scopolamine) -Parkinson’s (boost dopamine and decrease ACh) Eye: -eye exam requiring mydriasis and cycloplegia Resp: -decreased secretions -COPD/asthma (inhalation) GI/GU: -GI hypermotility -urinary urgency (newer M3 selective) Other: -anesthetic premedication -cholinergic poisoning -AChE inhibitor toxicity ```
94
muscarinic antagonist adverse effects
``` CV: -increased HR Resp: -bronchodilation GI/GU: -decreased secretions/activity Glands/Sweat glands: -decreased secretions Eye: -mydriasis -increase intraocular pressure -cycloplegia (paralysis of accommodation) CNS: -sedation ```
95
atropine MOA
- tertiary amine - lipophilic - crosses BBB
96
atropine PK/PD
- half-life 4 hours (prolonged in elderly to 10 hours | - eye effects last for days
97
atropine clinical uses
- ophthalmic - tx of bradycardia - antidote for cholinergic agonists - preoperative inhibition of secretions - adjunct for NMBD reversal
98
scopolamine MOA
- tertiary amine - crosses BBB - more lipophilic than atropine - +++ CNS effects (amnesia) - +++ sedation
99
scopolamine PK/PD
- half-life 1-4 hours - onset 10 min - duration about 2 hours
100
scopolamine clinical uses
- motion sickness - PONV - preoperative for amnesia, sedation, or decrease secretions
101
glycopyrrolate MOA
- quaternary amine | - less CNS effects (b/c polar so unable to cross BBB)
102
glycopyrrolate PK/PD
- half-life 1 hour - onset 1 min - duration 7 hours
103
glycopyrrolate clinical uses
- pre-op cardiac dysrhythmia (vagal reflex) | - reversal of NM blockade with neostigmine
104
nicotinic N antagonist (ganglionic blocker)
hexamethonium
105
hexamethonium facts
- blocks ganglionic output - hypertensive emergency - not used anymore
106
nicotinic M antagonist drugs
- Atracurium - Cisatracurium - Vecuronium - Rocuronium - Pancuronium
107
nicotinic M antagonist MOA
competitively binds to nicotinic receptor at NMJ to block the action of ACh
108
nicotinic M antagonist clinical use
skeletal muscle relaxation for surgical intubation or ventilation control
109
alpha agonist drugs
- Norepinephrine (alpha 1, alpha 2) - Phenylephrine (alpha 1) - Clonidine (alpha 2) - Dexamethasone (alpha 2)
110
alpha agonist MOA
directly binds to activates the alpha receptor
111
alpha agonist clinical uses
``` Alpha 1: -Shock, systemically because of ability to vasoconstrict -decongestant -ophthalmic hyperemia Alpha 2: -hypertension (central effects) ```
112
alpha agonist adverse effects
``` Alpha1: -vasoconstriction -smooth muscle contraction (except GI) -trophic effect BPH -GI/GU sphincters contract -mydriasis Alpha2: -decrease NE release (presynaptic) -CNS inhibition of sympathetic outflow from VMC in the brain -platelet aggregation -decrease in insulin secretion ```
113
beta agonist drugs
- Isoproterenol (beta 1 and beta 2) - Dobutamine (beta 1) - Albuterol (beta 2)
114
beta agonist MOA
directly binds to and activates the beta receptor
115
beta agonist clinical uses
``` Beta 1: -acute heart failure (increases CO and BP) Beta 2: -asthma -COPD -pre-term labor (to relax uterus) ```
116
beta agonist adverse effects
``` Beta1: -increased HR and contractility -increase in renin release -trophic effect in heart (hypertrophy, used for chronic stable HF) Beta2: -bronchodilation -vasodilation (esp skeletal muscle beds) -most smooth muscle relaxes -skeletal muscle contracts (hypokalemia, increased K+ uptake) -GI/GU – relaxation -uterine smooth muscle relaxation -glycogenolysis (liver to raise BG) ```
117
mixed alpha/beta agonist drugs
- epi | - NE
118
mixed alpha/beta agonist MOA
- directly bind to and activate the alpha and beta receptors - which is activated depends on substance affinity for receptor
119
mixed alpha/beta agonist PK/PD
- rapid onset - brief duration - no oral admin because polar - poor CNS penetration
120
NT releaser (indirect acting) drugs
Amphetamine | Ephedrine
121
Amphetamine MOA
- displaces/releases stored catecholamine NT | - secondary – inhibitis catecholamine reuptake (NET, DAT)
122
amphetamine clinical uses
uses in ADHD, narcolepsy, appetite suppression
123
ephedrine MOA
- displaces/releases stored catecholamine NT | - some agonist activity at alpha and beta adrenergic receptors
124
ephedrine PK/PD
extended duration, because not a catecholamine
125
NE reuptake inhibitor (indirect acting) drugs
- Cocaine | - Serotonin-Norepinephrine Reuptake Inhibitors (SNRI)
126
Cocaine MOA
- blocks NE reuptake by inhibiting the action of NET & DAT transporters - blocks sodium channels, so local anesthetic actions
127
SNRI MOA
block NE reuptake by inhibiting NET transporter
128
MAO Inhibitor (indirect acting) drugs
- Tranylcypromine (non-selective A & B) | - Selegiline (selective B)
129
MAOI MOA
- prevent breakdown of catecholamines in presynaptic terminal so catecholamine accumulates in vesicles - MAO A – metabolizes NE - MAO B – metabolizes DA
130
alpha receptor blocker drugs
- Phenoxybenzamine (alpha 1, alpha 2) - Phentolamine (alpha 1, alpha 2) - Prazosin (alpha 1) - Yohimbine (alpha 2)
131
alpha receptor blocker MOA
Competitively binds to the alpha receptor and blocks activity of endogenous ligand
132
alpha receptor blocker clinical uses
- HTN (later agent, not used a lot anymore) - BPH - pheochromocytoma (non-selective)
133
alpha receptor blocker adverse effects
- smooth muscle relaxation - decreased peripheral vascular resistance - decreased BP
134
beta receptor blocker drugs
- Propranolol (beta 1, beta 2) - Metoprolol (beta 1) - Esmolol (beta 1)
135
beta receptor blocker MOA
Competitively binds to the beta receptor and blocks activity of endogenous ligand
136
beta receptor blocker clinical uses
- HTN - angina pectoris - arrythmia - MI - thyrotoxicosis - heart failure – chronic stable only and only select agents - other – infantile hemangioma, glaucoma, migraine prophylaxis, anxiety
137
beta receptor blocker adverse effects
- decreased HR - decreased force of contraction - decreased renin - anti-dysrhythmic effects (some) - bronchoconstriction - arrythmia, bradycardia - sedation (for those that cross BBB) - decreased sexual function - DM – blocking of glycogenolysis + blocks s/s of hypoglycemia so be careful!!
138
Cholinergic Crisis Toxicity Mnemonic: (DUMBBELSS)
* Diarrhea, Diaphoresis * Urination * Miosis * Bradycardia * Bronchoconstriction * Excitation (skeletal muscle, or CNS) * Lacrimation * Salivation * Sweating
139
Muscarinic Agonist Mnemonic: (SLUDGE)
* Salivation * Lacrimation * Urination * Diarrhea * GI Upset * Emesis
140
Anticholinergic Memory Aid
* Dry as a bone * Hot as a pistol * Red as a beet * Blind as a bat * Mad as a hatter
141
Epinephrine
Naturally occurring catecholamine – last in the chain of synthesis
142
Epinephrine receptor/MOA
Alpha1, alpha2, beta1, beta2, beta3 -low doses – beta effects -high doses – alpha effects Highest affinity for beta receptors
143
Epinephrine PK/PD
- metabolized in liver by CYP450 - excreted in urine - half-life < 5 min
144
Epinephrine dosing
1-20 mcg/min
145
Epinephrine clinical uses
- anaphylaxis - in combination with local anesthetics - cardiac arrest - some shock states that involve poor tissue oxygen delivery and hypotension
146
Epinephrine effects
- positive inotropic, chronotropic, dromotropic actions - increase in myocardial oxygen consumption - potential for arrythmia (dt dromotropic action) - bronchodilation - vasodilation - decrease in histamine release from mast cells - LOW dose – decreases SVR - HIGH dose – increase SVR
147
Norepinephrine
Derived from dopamine in chain of catecholamine synthesis
148
Norepinephrine receptor/MOA
Alpha1, beta1 | -little effect on beta 2
149
Norepinephrine PK/PD
- metabolized in liver, kidney, plasma by CYP450 - excreted in urine - half-life 1 min
150
Norepinephrine dosing
1-20 mcg/min
151
Norepinephrine clinical uses
- shock | - generally used in patients with adequate CO but low SVR
152
Norepinephrine effects
- decrease in vital organ flow due to combo of alpha/beta stimulation - coronary artery perfusion increased d/t increase in DBP - increased renal vascular resistance, so decrease UOP - increase preload - caution in patients with peripheral tissue perfusion issues (NE may exacerbate) - decrease in insulin production - other effects usually due to potent vasoconstrictive effects
153
Isoproterenol receptor/MOA
Beta1, beta2 | No alpha activity
154
Isoproterenol PK/PD
- metabolized in liver by CYP450 - excreted in urine - unknown half-life
155
Isoproterenol dosing
2-20 mcg/min
156
Isoproterenol clinical uses
- acute asthma (not as much anymore) - cardiac stimulant - occasional use for treatment of bradycardia with heart block or torsades de pointes - post heart transplant for chronotropic support
157
Isoproterenol effects
- positive inotropic and chronotropic effects - decrease SVR, increase CO - increase myocardial oxygen consumption - bronchodilation - pulmonary vascular bed vasodilation - excessive tachycardia - myocardial ischemia (dt decreased DBP) - arrythmias
158
Dopamine
derived from dopa in chain of catecholamine synthesis
159
Dopamine receptor/MOA
- low dose – D1 in renal, mesenteric, coronary vascular beds - med dose – beta1 - high dose – alpha1
160
Dopamine PK/PD
- metabolized in liver, kidney, plasma by CYP450 - 25% metabolized to NE - excreted urine - half-life 2 min
161
Dopamine dosing
1-4 mcg/kg/min 5-10 mcg/kg/min 11-20 mcg/kg/min
162
Dopamine clinical uses
- shock - HF - increase blood flow to kidneys
163
Dopamine effects
- indirect sympathomimetic effect via release of NE from beta1 stimulation - increase RBF, so increase GFR and UOP - can cause severe limb ischemia (esp. in peds, DM, atherosclerosis, Reynaud’s)
164
Dobutamine
synthetic sympathomimetic amine derived from isoproterenol
165
Dobutamine receptor/MOA
Beta1
166
Dobutamine PK/PD
- metabolized in liver by CYP450 - excreted urine - half-life 2 min
167
Dobutamine dosing
1-20 mcg/kg/min
168
Dobutamine clinical uses
- acute HF - cardiogenic/septic shock - heart stimulation for cardiac stress testing
169
Dobutamine effects
- strong inotropic response (but minimal chronotropy) - can increase or maintain BP dt increase CO and slight decrease in SVR - no longer used for inotropic support in surgery dt significant adverse effects

N929 - Anesthesia Pharmacology (12 decks)

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