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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
Q

Which alpha 2 receptor subtype is responsible for producing sedation, analgesia and anxiolysis

A

Alpha2A

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26
Q

Which alpha2 receptor subtype can cause vasoconstriction

A

Alpha2B

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27
Q

What are some peripheral effects of alpha2 agonists

A
  1. Initial hypertension
    2.reflex bradycardia and vasodilation- hypotension
  2. Hypoxemia in sheep
  3. Diuresis
  4. Decrease GI
  5. Hyperglycemia
  6. Emesis- xylazine
  7. Dry eyes
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28
Q

What species is the most sensitive to alpha 2 sedation effects

A

Ruminants

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29
Q

What alpha2 agonist causes the most sedation

A

Dexmedetomidine

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30
Q

What alpha2 agonists cause the least sedation

A

Romifidine, and detomidine

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31
Q

What alpha2 agonist has some muscle relaxation affects and could be used in horses to cause least likelihood of ataxia

A

Romifidine

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32
Q

What alpha2 agonist causes marked emesis in cats

A

Xylazine

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33
Q

Which alpha2 agonist has the greatest chance of causing aggression and which receptor does it act on

A

Xylazine- alpha 1

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34
Q

What species is very sensitive to xylazine and is not recommended

A

Cattle

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35
Q

What species is xylazine fatal in

A

Sheep

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36
Q

How is xylazine fatal in sheep

A

Produce hypoxemia
Activate pulmonary macrophages, produce bronchoconstriction, and cause intra-alveolar edema and hemorrhage

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37
Q

What species is detomidine approved in

A

Horses

38
Q

What alpha2 agonist has the longest duration of action

A

Detomidine

39
Q

What is an adverse effect of detomidine in horses

A

Penile prolapse

40
Q

Detomidine may cause ___when co-administered with sulfonamides in horses

A

Fatal dysrhythmias

41
Q

What is medetomidine used for

A

Produce sedation for surgery and decrease emergence delirium

42
Q

What species is medetomidine approved for

A

Dogs

43
Q

What does medetomidine/vatinoxan do and what is the benefit vs medetomidine

A

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
Q

What species is dexmedetomidine approved for

A

Dogs and cats

45
Q

What is the most potent alpha 2 agonists

A

Dexmedetomidine

46
Q

What is dexmedetomidine used for

A

Sedation for short procedures/exams or pre-anesthetic sedation

47
Q

What are some adverse effects of dexmedetomidine

A

Ataxia, vomiting, hyperglycemia, bradycardia, hypotension

48
Q

What alpha2 agonist is less likely to produce diuresis

A

Dexmedetomidine

49
Q

What drug can be used to revere dexmedetomidine

A

Atipamezole

50
Q

What species is Romifidine approved for

A

Horses

51
Q

Why is romifidine a good alpha2 agonist in horses

A
  1. Less ataxia
  2. Long lasting so decreases attempts to stand during recovery so provides better outcome
52
Q

Romifidine causes ___ in dogs and cats

A

Cardiovascular depression

53
Q

Romifidine can be used in cats and dogs for __, potentiates the effects of ___

A

Analgesia, potentiates morphine and lidocaine

54
Q

What are some adverse effects of alpha2 agonists

A
  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
Q

Alpha 2 agonists are contraindication in dogs with

A

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
Q

What alpha2 is contraindicated in sheep

A

Xylazine

57
Q

What alpha2 is contraindicated in horses with colic because it may mask pain and respiratory or cardiac changes

A

Detomidine

58
Q

What are some other contraindications for alpha 2 agonists

A

Seizure disorders, pregnancy

59
Q

What interactions do alpha 2 agonists have

A
  1. CNS depressants (opioids, anesthetic, sedatives)
  2. Epinephrine- will worsen cardiac effects
60
Q

What is atipamezole

A

Alpha 2 competitive antagonist used to reverse sedation effects

61
Q

Atipmazole can cause __, ___, and ___ and can cause profound __ in reptiles

A

Delirium, anxiety, and aggression, profound hypotension in reptiles

62
Q

How can atipamezole cause hypotension

A

Histamine release, prior to we have vasoconstriction and high vagal tone rapidly go to vasodilation and bradycardia- decrease CO too much

63
Q

What species is atipamezole labeled for and not labeled for

A

Labeled: cats and dogs
Not FDA approved for food producing animals

64
Q

What is yohimbine

A

Alpha 2 antagonists that can only reverse xylazine and detomidine

65
Q

What are 2 negative side effects of yohimbine

A

CNS excitement, tachycardia

66
Q

What species is yohimbine labeled for

A

Dogs

67
Q

What is tolazoline and what species is it labeled for

A

Non-selective alpha2 antagonist, labeled for horses

68
Q

What is the major inhibitor NT in the brain

A

GABA

69
Q

What is the result of stimulation of GABA a receptors

A

Cl- channels open causing hyper polarization and inhibition of neurotransmission

70
Q

Stimulation of GABA a receptors decreases what

A

Anxiety, vigilance, muscle tension, seizures, and causes sedation

71
Q

Benzodiazepines do what to GABA a receptor

A

Increase opening of Cl- Chanel

72
Q

What are benzodiazepines used for

A

Sedation, anxiolytic effects

73
Q

Are they slow or rapid onset

A

Rapid

74
Q

What are some fearful reactions benzodiazepines can be useful for

A

Submissive urination, storm phobia, separation anxiety, fear without aggression, foal rejection in mares, feather plucking in birds

75
Q

Benzodiazepines should not be used when what behavioral issue is present

A

Aggression because it will potentiates it

76
Q

___can be used as appetite stimulant

A

Benzodiazepines

77
Q

Benzos have an __potential and are a schedule __ drug

A

Abuse, IV

78
Q

What is the t/12 life of diazepam in dogs, horses and cats

A

Dogs: 2-3hrs
Horses:7-22
Cats: 5.5

79
Q

Diazepam may decrease inhibition and increase ___behavior

A

Aggressive

80
Q

Diazepam May cause __ in horses

A

Ataxia

81
Q

Diazepam is contraindicated in ___

A

Pregnant animals- crosses placenta may be tetragenic

82
Q

What is the t1/2 life of midazolam in dogs

A

30 minutes

83
Q

What is midazolam used for

A

Induction of anesthesia in combination with other anesthetic
Control seizures

84
Q

What are some side effects of benzodiazepines

A

Sedation, ataxia, muscle relaxation, increase appetite, anxiety, dysphoria, aggression

85
Q

Oral diazepam in cats can cause

A

Idiopathic hepatic necrosis

86
Q

What is the treatment for overdose on benzos

A
  1. Supportive therapy
  2. Activated charcoal
  3. Vomiting in cats-xylazine
  4. Flumazenil- benzodiazepine receptor antagonist
87
Q

What is flumazenil

A

Benzodiazepine receptor antagonist

88
Q

Administration of flumazenil can have what negative consequence

A

Seizures

89
Q

What is the mechanism of action of Trazodone

A

5HT2A/2C antagonist and inhibits 5TH uptake

90
Q

Trazodone provides __ and __

A

Sedation and decrease anxiety

91
Q

What is the mechanism of action for gabapentin

A

Decreases excitatory transmitter release in overactive nerves

92
Q

What is gabapentin used for

A

Adjunct analgesic, some sedation and anti anxiety effects

Pharmacology II (36 decks)

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