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Pharmacology II > Lecture 7: Sedative Drugs > Flashcards

Lecture 7: Sedative Drugs Flashcards

1
Q

Acepromazine produces ___

A

Sedation

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2
Q

Benzodiazepines produce __ and decrease ___

A

Sedation, anxiety

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3
Q

Alpha 2 agonists produce ___ and __

A

Sedation, analgesia

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4
Q

Opioids to decrease__ and increase__

A

Pain, sedation

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5
Q

Guaifenesin or methocarbomal for ___

A

Muscle relaxations

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6
Q

What receptor does acepromazine act on and what is result

A

D2 receptor in brain resulting in sedation

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7
Q

What can happen with high doses of acepromazine and why

A

Tremors and rigidity due to inhibition of striatal dopamine transmission

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8
Q

Beyond the D2 receptors what receptors do acepromazine block and what are effects

A

Muscarinic and alpha1- hypotension, bradycardia

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9
Q

What are some uses for acepromazine

A
  1. Preanesthetic to decrease anxiety or response to noise in dogs
  2. Sedation in horses
  3. Motion sickness in cats and dogs
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10
Q

Acepromazine is FDA approved for what species

A

Dogs, cats and horses

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11
Q

What are some side effects of acepromazine

A

Hypotension, agitation, ataxia, irreversible penile prolapse in horses

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12
Q

When would acepromazine be contraindicated

A
  1. Breeding horses-penile prolapse
  2. Hypovolemic, dehydrated, bleeding- d/t hypotension
  3. Collies
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13
Q

T or F: affects of acepromazine can be reversed

A

False

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14
Q

What does guaifenesin do and when can it be useful

A
  1. Relaxes laryngeal and pharyngeal muscles- easier intubation
  2. Mild sedation
  3. Muscle relaxation- helpful with surgical manipulation
  4. Combined with ketamine to decrease excitement during induction and recovery in horses
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15
Q

What are some adverse effects/contraindications for guaifenesin

A

Can produce sudden ataxia
MUST be given IV- causes perivascular damage
CI with AChE inhibitors

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16
Q

What is mechanism of action for dantrolene

A

Causes skeletal muscle relaxation by inhibiting releases of Ca2+ from endoplasmic reticulum

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17
Q

What are some indications for dantrolene

A
  1. Malignant hyperthermia- extreme muscle rigidity due to inhalants
  2. Function urethral obstruction in dogs and cats
  3. Horses with myosin is/equine exertional rhabdomylosiswhat a
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18
Q

What are some adverse effects of dantrolene

A

Sedation, weakness, nausea, increased urination

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19
Q

Post anesthetic uses of dantrolene can cause what in horses

A

Hyperkalemia and arrhythmias

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20
Q

What is the mechanism alpha2 agonists use to induce sedation

A

Stimulate presynaptic alpha 2 receptors to decrease the release of NE in both CNS and periphery, results in inhibition of Ca2+ depolarization

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21
Q

How do alpha2 agonists act to control pain and sedation

A

Activation of alpha2 receptors in spinal and supraspinal sites can analgesia and sedation by inhibiting glutamate release in ascending pain pathway

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22
Q

What are two major side effects of dexmedetomidine

A

Hypotension, bradycardia

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23
Q

What are the 4 alpha2 receptor subtypes

A

Alpha2A, alpha2B, alpha2C, alpha2D

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24
Q

Which alpha2 receptor could be responsible for xylazine toxicity in sheep that causes hpoxemia

A

Alpha2D

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25
Which alpha 2 receptor subtype is responsible for producing sedation, analgesia and anxiolysis
Alpha2A
26
Which alpha2 receptor subtype can cause vasoconstriction
Alpha2B
27
What are some peripheral effects of alpha2 agonists
1. Initial hypertension 2.reflex bradycardia and vasodilation- hypotension 3. Hypoxemia in sheep 4. Diuresis 5. Decrease GI 6. Hyperglycemia 7. Emesis- xylazine 8. Dry eyes
28
What species is the most sensitive to alpha 2 sedation effects
Ruminants
29
What alpha2 agonist causes the most sedation
Dexmedetomidine
30
What alpha2 agonists cause the least sedation
Romifidine, and detomidine
31
What alpha2 agonist has some muscle relaxation affects and could be used in horses to cause least likelihood of ataxia
Romifidine
32
What alpha2 agonist causes marked emesis in cats
Xylazine
33
Which alpha2 agonist has the greatest chance of causing aggression and which receptor does it act on
Xylazine- alpha 1
34
What species is very sensitive to xylazine and is not recommended
Cattle
35
What species is xylazine fatal in
Sheep
36
How is xylazine fatal in sheep
Produce hypoxemia Activate pulmonary macrophages, produce bronchoconstriction, and cause intra-alveolar edema and hemorrhage
37
What species is detomidine approved in
Horses
38
What alpha2 agonist has the longest duration of action
Detomidine
39
What is an adverse effect of detomidine in horses
Penile prolapse
40
Detomidine may cause ___when co-administered with sulfonamides in horses
Fatal dysrhythmias
41
What is medetomidine used for
Produce sedation for surgery and decrease emergence delirium
42
What species is medetomidine approved for
Dogs
43
What does medetomidine/vatinoxan do and what is the benefit vs medetomidine
Used for sedation but does not produce the peripheral effects (increase HR, arrhyhtmias) like metomidine does because vatinoxan is a peripheral alpha 2 blocker so only get central sedation effects and not peripheral cardiac effects
44
What species is dexmedetomidine approved for
Dogs and cats
45
What is the most potent alpha 2 agonists
Dexmedetomidine
46
What is dexmedetomidine used for
Sedation for short procedures/exams or pre-anesthetic sedation
47
What are some adverse effects of dexmedetomidine
Ataxia, vomiting, hyperglycemia, bradycardia, hypotension
48
What alpha2 agonist is less likely to produce diuresis
Dexmedetomidine
49
What drug can be used to revere dexmedetomidine
Atipamezole
50
What species is Romifidine approved for
Horses
51
Why is romifidine a good alpha2 agonist in horses
1. Less ataxia 2. Long lasting so decreases attempts to stand during recovery so provides better outcome
52
Romifidine causes ___ in dogs and cats
Cardiovascular depression
53
Romifidine can be used in cats and dogs for __, potentiates the effects of ___
Analgesia, potentiates morphine and lidocaine
54
What are some adverse effects of alpha2 agonists
1. Hypertension 2. Bradycardia and AV block 3. Respiratory depression 4. Vomiting 5. Penile prolapse 6. Muscle tremors 7. Urination, 8. Startle 9. Hypothermia
55
Alpha 2 agonists are contraindication in dogs with
Cardiovascular disease, respiratory disorders, liver or kidney dysfunction, shock, dehydration, loss of blood volume, severe debilitation, stress due to extreme heat, cold or fatigue
56
What alpha2 is contraindicated in sheep
Xylazine
57
What alpha2 is contraindicated in horses with colic because it may mask pain and respiratory or cardiac changes
Detomidine
58
What are some other contraindications for alpha 2 agonists
Seizure disorders, pregnancy
59
What interactions do alpha 2 agonists have
1. CNS depressants (opioids, anesthetic, sedatives) 2. Epinephrine- will worsen cardiac effects
60
What is atipamezole
Alpha 2 competitive antagonist used to reverse sedation effects
61
Atipmazole can cause __, ___, and ___ and can cause profound __ in reptiles
Delirium, anxiety, and aggression, profound hypotension in reptiles
62
How can atipamezole cause hypotension
Histamine release, prior to we have vasoconstriction and high vagal tone rapidly go to vasodilation and bradycardia- decrease CO too much
63
What species is atipamezole labeled for and not labeled for
Labeled: cats and dogs Not FDA approved for food producing animals
64
What is yohimbine
Alpha 2 antagonists that can only reverse xylazine and detomidine
65
What are 2 negative side effects of yohimbine
CNS excitement, tachycardia
66
What species is yohimbine labeled for
Dogs
67
What is tolazoline and what species is it labeled for
Non-selective alpha2 antagonist, labeled for horses
68
What is the major inhibitor NT in the brain
GABA
69
What is the result of stimulation of GABA a receptors
Cl- channels open causing hyper polarization and inhibition of neurotransmission
70
Stimulation of GABA a receptors decreases what
Anxiety, vigilance, muscle tension, seizures, and causes sedation
71
Benzodiazepines do what to GABA a receptor
Increase opening of Cl- Chanel
72
What are benzodiazepines used for
Sedation, anxiolytic effects
73
Are they slow or rapid onset
Rapid
74
What are some fearful reactions benzodiazepines can be useful for
Submissive urination, storm phobia, separation anxiety, fear without aggression, foal rejection in mares, feather plucking in birds
75
Benzodiazepines should not be used when what behavioral issue is present
Aggression because it will potentiates it
76
___can be used as appetite stimulant
Benzodiazepines
77
Benzos have an __potential and are a schedule __ drug
Abuse, IV
78
What is the t/12 life of diazepam in dogs, horses and cats
Dogs: 2-3hrs Horses:7-22 Cats: 5.5
79
Diazepam may decrease inhibition and increase ___behavior
Aggressive
80
Diazepam May cause __ in horses
Ataxia
81
Diazepam is contraindicated in ___
Pregnant animals- crosses placenta may be tetragenic
82
What is the t1/2 life of midazolam in dogs
30 minutes
83
What is midazolam used for
Induction of anesthesia in combination with other anesthetic Control seizures
84
What are some side effects of benzodiazepines
Sedation, ataxia, muscle relaxation, increase appetite, anxiety, dysphoria, aggression
85
Oral diazepam in cats can cause
Idiopathic hepatic necrosis
86
What is the treatment for overdose on benzos
1. Supportive therapy 2. Activated charcoal 3. Vomiting in cats-xylazine 4. Flumazenil- benzodiazepine receptor antagonist
87
What is flumazenil
Benzodiazepine receptor antagonist
88
Administration of flumazenil can have what negative consequence
Seizures
89
What is the mechanism of action of Trazodone
5HT2A/2C antagonist and inhibits 5TH uptake
90
Trazodone provides __ and __
Sedation and decrease anxiety
91
What is the mechanism of action for gabapentin
Decreases excitatory transmitter release in overactive nerves
92
What is gabapentin used for
Adjunct analgesic, some sedation and anti anxiety effects

Pharmacology II (36 decks)

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