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Sedative And Anesthetics Flashcards

1
Q

______________induces a state of behavioral change where anxiety is relieved and the patient is relaxed, but aware of their surroundings

A

Tranquilizer (neuroleptic)

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2
Q

____________ induces a state characterized by CNS depression and drowsiness, decreased awareness of surroundings

A

Sedative

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3
Q

__________ induces sleep

A

Hypnotic

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4
Q

_____________ attenuated nocicpetive input leading to reduced rain

A

Analgesic

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5
Q

______________ decreases central sensitization to pain

A

Antihyperalgesics

do not block transmission of stimulus

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6
Q

_______________ diminishes ability to perceive pain

A

Antinocipcetion

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7
Q

____________ induces analgesia and stupor bordering on anesthesia

A

Narcotic

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8
Q

________________ causes analgesia and amnesiac state produced by admin of a neuroleptic and narcotic

A

Neuroleptanalgesia

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9
Q

________________ are drugs given before a medical, surgical, or invasive produced to induce sedation, analgesic, ad relieve anxiety

A

Premedication

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10
Q

What makes up the blood brain barrier?

A

Tight capillary endothelial junctions
Glial cells
Active transport for removal of organic acids or bases
CSF into venous drainage

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11
Q

What re the excitatory neurotransmitters?

A 
Glutamate (NMDA receptor) 
ACh 
Epi/ Norepi 
Dopamine
Serotonin 
Histamine
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12
Q

What are the inhibitory neurotransmitters?

A

GABA

Glycine (spinal cord)

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13
Q

Neuroleptics (tranquilizer) can be classified into

A

Phenothiazine derivative

Benzodiazepine derivative

Butyrophenone derivative

A2 agonists

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14
Q

What are the main effects of neuroleptics

A

Sedation and hypnosis
Emotional quietness
Dissociation from surroundings

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15
Q

What are the only group of neuroleptics to have analgesic effects?

A

A2 agonists

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16
Q

T/F: none of the neuroleptics have true anesthetic effects

A

T

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17
Q

What is the most common phenothiazine?

A

Acepromazine

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18
Q

What is the MOA of phenothiazines?

A

Competitively antagonize excitatory dopamine receptors in the CNS

Inhibit vomiting
Prolactin release
Muscle relaxation

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19
Q

How are phenothiazines administered?

A

IV, IM,SQ, PO

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20
Q

What is the oral bioavailability of phenothiazines in dogs?

A

Low

About 20%

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21
Q

Where are phenothiazines metabolized

A

Liver, excreted in urine

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22
Q

What effects do phenothiazines have in the CNS?

A

Sedation (dopamine receptor)
Decreased spontaneous motor activity
Hypothermia and hyperprolactinemia (hypothalamus)
Anti-emetic (alpha 2 receptor)

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23
Q

What are the effects of phenothiazines on the CVS?

A

Block alpha 1 receptor

Vasodilation-> hypotension ‘epinephrine reversal’

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24
Q

What breeds are more susceptible to the CVS effects of phenothiazines

A

Boxers/brachydephalics

Large breed dogs and sighthounds

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25
What effects do phenothiazines have on the respiratory system
Minimal at therapeutic dose | Depression at hight dose or with other opioids
26
What effects do phenothiazines have on skeletal muscle
Moderate relaxation
27
What are the precautions to using phenothiazines?
Boxers/brachycephalic/large dog/sighthounds.MDR1 mutations When vasodilation is contraindicated Stallions: penile prolapse Cattle: not approved ->ruminal regurgitation Aggressive dog: increase aggression Excited animals : reduced sedative effect Toxins: extrapyramial effect Liver disease: hepatotoxic Concurrent epinephrine use
28
What two phenothiazines are used as anti-emetics
Prochlorperazine and chlorpromazine
29
What phenothiazine is used as a antihistamine
Trimeprazine
30
What are the benzodiazepines
Agonists: Diazepam Midazolam Alprazolam Antagonist: Flumazenil Partial agonist: Imepitoin
31
What is the MOA of benzodiazepines?
Bind and active benzodiazepine binding site on GABA receptor to cause hyperpolarization of neurons (GABA is main inhibitory NT in CNS)
32
What is the distribution of benzodiazepine
Lipid soluble Wide distribution Cross BBB Protein bound
33
What benzodiazepine is given IV
Diazepam
34
What benzodiazepine is given IM
Midazolam
35
What benzodiazepine is given orally
Alprazolam (diazepam has short duration and can cause hepatic necrosis in cats)
36
What are the clinical uses for benzodiazepines?
Anxiolytics (behavioral modifiers) Anticonvulsant Premedication (combine with other agents) Sedation (not reliable on its own!) -> most reliable in ruminants Muscle relaxation -> central effect but short lived Appetite stimulation
37
What is used for specific reversal of benzodiazepines?
Flumazenil Competing antagonist on GABA receptor
38
What are contraindications to using benzodiazepine
CAT: hepatotoxicity with oral diazepam
39
What are precautions to use in benzodiazepine ?
Horse: muscle fasciculations seen (ataxia at high dose) Paradoxical excitement (fear/aggressive animals) Propylene glycol (diazepam injection-> pain IM and hypotension IV Pregnancy -teratogenic Hepatic and renal disease - altered metabolism and excretion
40
T/F: acepromazine has tranquilizer going and analgesic effects
F
41
What is the most important cardiovascular side effect of acepromazine ?
Hypotension
42
Why is oral diazepam contraindicated in cats
Hepatotoxicity
43
What are the A2 agonist neuroleptics
Dexmedatomidine Medetomidine Xylazine Yohimbine
44
Where is the pain pathway will A2 agonist have and effect
Perception Modulation Transmission
45
Dexmedetomidine is used in what species
Dogs Cat Exotic
46
Xylazine is used in what species
Horse, deer, elk
47
What is the reversal agent for dexmedetomidine
Atipamezole
48
What is the reversal agent to xylazine
Yohimbine
49
What is the MOA of Xylazine and dexmedetomidine ?
Competitive a2 agonism - > Brian (sedation) - > dorsal horn (analgesic and muscle relaxation) Competitive agonism of a1 receptors -> vasoconstriction
50
Activation of a2 receptors stimulates what pathway of action
G(inhibitory) protein receptor pathway - > negative coupling to reduce adenylyl cyclase and decrease cAMP - > increase outward flow of K+ Hyperpolarization Inhibit neurons Decrease NE release
51
What are the a2 agonists from most to least selective
Dexmedatomidine Romifidine Detomidine Xylazine
52
How are a2 agonists administered?
IV or IM Oral transmucosal Epidural
53
T/F: a2 agonists are widely distributed and can cross the BBB
T
54
How does the onset and duration of action differ between xylazine and medetomidine/detomidine?
Xylazine rapid onset (15min) sedation 1-2hrs analgesia 15-30min Medetomidine and detomidine have slightly longer action
55
What are the main effects of A2 agonists on the CNS
Sedation Pain modulation and analgesia Muscle relaxation Emesis
56
What is the emetic of choice in cats
Xylazine
57
What are the main effects of a2 agonists on the CVS?
Bi-phasic effect 1. peripheral phase (peripheral vasocontriction) Mediated by a1 receptors -systemic vascular resistance causes increase in BP=> reflex bradycardia (to maintain constant cerebral perfusion pressure) 2. Central phase Mediated by a2 receptors -decreased sympathetic tone -> heart rate stays low => hypotension AND bradycardia
58
When after giving A2 agonists, you see bradycardia and increased BP, should we give anticolinergics to help maintain HR?
No Phase 1 of biphasic effect Contraindicated because increased workload of heart against high vascular resistance will exacerbate pre-existing heart disease or worsen arrhythmias
59
When after giving A2 agonists, you see bradycardia and decreased BP, should we give anticolinergics to help maintain HR?
Yes Phase 2 of Biphasic response Clinical for cardiovascular depression
60
What effect will A2 agonists have on the respiratory system?
Decreased respiratory rate (cats may be more sensitive) Sheep, goat, and horse > increase respiratory rate and airway pressure=> increased CO2
61
What effect with A2 agonist have on the GI system
Decrease motility | Decrease acid secretion
62
What effects can a2 have on the uterus
Stimulate myometrial contractions -> may cause abortion in ruminants
63
What effect will A2 have on blood sugar
Hyperglycemia Decrease insulin release (transient) More pronounced in horse and ruminant
64
Clinically, what are a2 agonists used for?
Sedation Pre-anesthetic/premedication Analgesia Emetic Behavioral Chemical ejaculation in stallions
65
What are precautions to using A2 agonists ?
``` Cardiovascular disease/instability Emesis Liver disease Kidney disease Seizure disorder (increased ICP) Intra-arterial injection Late pregnancy in cattle and sheep ```
66
When is A2 agonist use contraindicated?
Critically ill and patients with shock
67
How should I administer competitive A2 antagonist (reversal agents)
IM -> greater possibility of side effects when give IV
68
What are the main effects of A2 antagonists?
CNS effects reversed (sedation and analgesia) Cardiovascular depression reversed Respiratory depression reversed GI side effect: salivation and diarrhea
69
When should I use A2 antagonists?
To reverse a2 agonist toxicity Mitoban toxicity Amitraz tick collars
70
What drug is the most selective to the A2 receptor
Dexmedetomidine
71
Alpha 2 agonists often cause bradycardia and bradyarrhythmias, what is the most common arrhythmia it causes?
Atrioventricular block
72
What is anesthesia
Drug induced central CNS depression in unconsciousness in which the patient cannot be arose by painful stimuli, and sensory motor and autonomic reflex functions are attenuated
73
What is dissociated anesthesia ?
Drug induced dissociation of the thalamocrotical and limbic systems in a catatonic state
74
What are the stages of anesthesia?
Analgesia -> voluntary motor excitement and state of analgesia Excitement phase -> characterized by involuntary excitation or delirium Surgical anesthesia -> plane of surgical anesthetic depth is reached Medullary paralysis -> characterized by paralysis of vital centers in medulla Death -> respiratory failure and collapse of resuscitative
75
What are the depths of surgical anesthesia
Consciousness, pain sensation and most neuromuscular reflexes are abolished 1 and 2 => light 1 and 3=> deep
76
What is the MOA of dissociative anesthetics
Non competitive NMDA receptor antagonist Inhibits activation by glutamate of ligand-gated ion channels
77
What part of the pain pathway does dissociative anesthetics work?
Modulation
78
What is the distribution of anesthetics?
Wide Lipid soluble Crosses BBB
79
How are anesthetics excreted?
Urine Cats have more renal excretion than other species -> caution in renal insufficiency
80
What is the onset, duration and recovery of anesthetics??
Induction - fast Duration - 20-45min Recovery - 2-10hrs (very long)
81
What are the main effects of dissociative anesthetics on the CNS?
1. depress thalamocortical system (sensory ) 2. activate limbic system -> dissociation (emotion/behavioral/memory) Anesthesia, amnesia, and catalepsy
82
What is catalepsy?
Muscle tone maintained to hypertonic -> need to be used in combo with muscle relaxant
83
What are the main effects of dissociative anesthetics on the CVS?
Centrally mediated CV stimulation Increase sympathetic tone (positive inotrope). Decreased parasympathetic tone
84
What are the main effects of dissociative anesthetics on the respiratory system?
Stimulate respiration (low dose) Bronchodilation (good for asthmatic patients) Increased secretions Depress respiration (very high dose)
85
What is the main effect dissociative anesthetics will have on the GI system
Stimulate salivary secretion
86
At low doses, ketamine primarily will act on?
CNS hypersensitization (suppress)
87
Can ketamine be used as a sole analgesic
No | Used at subanesthetic dose in combo with opioid to manage acute main
88
What is the recovery time for tiletamine/Zolazepam and what part of it is reversible
Tiletamine -> dissociative Zolazepam (benzodiazepine ) ``` LONG recovery (hours) Only the zolazepam is reversible ```
89
What are the clinical uses for dissociative anesthetics?
Chemical restrain and anesthetic for minor procedure Induction of anesthesia Part of triple drip in large animals Analgesia (CRI)
90
What is 'Kitty magic' for induction of anesthesia ?
Ketamine + Dexmedtomidine + Buprenorphine
91
What is the triple drip in large animals?
Form of total intravenous anesthetia (TIVA) Guaifenesin + Xylazine + Ketamine
92
What is used in combination to a dissocative anesthetic to produce analgesic effects
Fentanyl + Lidocaine + Ketamine (FLK) Morphine + Lidocaine + Ketamine (MLK)
93
What role does a dissociative anesthetic play in acute pain
Reduce post-op pain hypersensitivity Reduce short term tolerance to opioids Prevent opioid-induced hyperalgesia Reduce dose in post operative opioids
94
What are disadvantages to using ketamine?
Irreversible Cannot be used alone -> use with opioid Inappropriate in cardiac disease patient Increase ICP Pain with IM injection Risk of corneal ulceraction and substance abused
95
That are precautions to using dissociative anesthetics ?
Pain with IM injection (good in cats but less good IM in dogs) Eyes remain open-> lubricate /blink Respiratory depression at high dose
96
When should ketamine not be used
If increased ICP or IOP is contraindicated Seizure Myelography Certain cardiac disease or hyper tension Hepatic insufficiency Renal disease/failure in cats
97
What is the sequence of dose dependent sedation induced by GABA agonists
Sedation -> hypnosis -> anesthesia -> coma -> death
98
What part of the pain pathway do GABA agonist analgesics have an effect?
General anesthesia -> perception | Anticonvulsant -> modulation
99
What is the MOA of GABA agonists
Bind GABA receptor Barbiturates: Increase the amount of time that GABA remains on the binding site and at high doses are reported to be able to activate chloride channels without GABA present Main effect -> sedation and hypnosis
100
What are the GABA agonist drugs?
Barbiturates : Thiopental Non-barbiturates : Propofol Alflaxalone Etomidate
101
How are barbiturates administered?
IV and Oral. Not SQ or IM -> injection causes tissue damage
102
How are barbiturates metabolized?
Hydroxylation in the liver Thiobarbituaes are inactivated in the brain and the kidney
103
What is the main effect of barbiturates on the CNS?
Nonselective dose-dependent depression Sedation, hypnosis, and anesthesia Poor analgesia unless anesthetized Anticonvulsant Decrease ICP Increase threshold for spinal reflex
104
Why are barbiturates good for head trauma cases?
Barbiturates decrease brain metabolism -> neuroprotective for a poorly perfused brain
105
What are the main effects of barbiturates on the cardiovascular system
Hypotension ( due to cardiac depression) -> reflex tachycardia Thiobarbituates sensitize myocardium to catecholamine-induced arrhythmias Intra-arterial injection causes vasoconstriction and gangrene
106
What are the main effects of barbiturates on the respiratory system?
Dose dependent respiratory depression (cats are more sensitive) VERY important -> most common cause of death due to poor dosing/monitoring
107
What effect with barbiturates have on skeletal muscle
Inhibit sensitivity of motor endplate to ACH | Abdominal relaxation incomplete
108
What effect with barbiturates have on body temp?
Hypothermia -> decreased basal metabolic rate
109
What effect with barbiturates have on the kidney?
Oliguria and Anura due to decreased blood pressure -> reduced GFR Stimulate ADH
110
Repeated use of propoflo can cause what in cats?
Blood dyscrasia | Heinz body anemia
111
Propoflo is administered how?
IV
112
What is the distribution of propoflo?
``` Widely distributed (lipid soluble) Redistributed to muscle then fat ```
113
What are the main effects of propofol on CNS
Dose dependent CNS depression
114
What are the main effects of propofol on the cardiovascular system?
Vasodialation without reflex tachycardia | Splenic engorgement cab be observed
115
What are the main effects of propofol on the respiratory system
Dose dependent depression | Rate dependent apnea
116
_________________ GABA agonist is an analog of progesterone
Alfaxalone neurosteroid
117
How is alfaxalone administered?
Labeled IV only | Sometimes used IM (unlike propofol)
118
T/F: alfaxalone and propofol provide significant analgesia
F
119
Myoclonus can be seen during induction (and by non-IV on recovery) with admin of what drug?
Alfaxalone
120
What is the MOA of Etomidate
Depress the CNS by enhancing GABA
121
What anesthetic is indicated in patients with significant cardiac disease?
Etomidate | -> least amount of cardiac depression
122
T/F: etomidate has no analgesic effects
T
123
What are the main effects of etomidate
Sedative, hypnotic and anesthetic effects Dose dependent respiratory depression Decreased ICP and IOP Inhibits cortisol synthesis Rapid recovery with no accumulation
124
Use of ___________ in animals with hypoadreanal cortisol crisis is contraindicated
Etomidate | Causes relative adrenal insufficiency by inhibiting cortisol synthesis by the adrenal gland -> critical illness
125
What anesthetic should be avoided in patients with traumatic brain injury?
Ketamine | -> increased ICP
126
``` Which of the following is not considered and IV anesthetic induction agent? Ketamine Propofol Alfaxalone Fentanyl ```
Fentanyl
127
``` Which of the following causes the least amount of cardiovascular depression Ketamine Propofol Etomidate Alfaxalone ```
Ketamine -> causes cardiac stimulation

RUSVM Pharmacology (18 decks)

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