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Module 14 > Clinical Pharmacology of Sedatives > Flashcards

Clinical Pharmacology of Sedatives Flashcards

1
Q

what is a tranquilizer and examples

A

relieves anxiety without drowsiness

ex. phenothiazines, butyrophenones

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2
Q

what are neuroleptics and examples

A

tranquilizer used in treatment of psychoses

ex. penothiazines

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3
Q

what are sedatives and examples

A

calming effect with drowsiness

ex. alpha 2 adrenoreceptor agonists

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4
Q

what are hypnotics

A

induce sleep

ex. benzodiazepines, propofol

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5
Q

what is the mechanism of action of acepromazine

A

non-selective dopamine antagonism

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6
Q

what is the effect of acepromazine

A
  1. tranquilization/sedation
  2. anti-emesis
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7
Q

what other receptor types does acepromazine antagonize and what do these cause

A
  1. alpha 1 adrenergic receptors: vasodilation and hypotension
  2. muscarinic: decrease GIT motility
  3. histamine H1
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8
Q

what are the cardiovascular effects of acepromazine

A
  1. vasodilation leading to hypotension
  2. anti-arrhythmic action
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9
Q

why does acepromazine cause vasodilation and hypotension

A

alpha 1 adrenergic antagonist causes drop in BP initially

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10
Q

how does acepromazine cause ant-arrhythmic action

A

increases threshold for adrenaline/epinephrine induced arrhythmia

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11
Q

what are the respiratory effects of acepromazine

A

in bracycephalics sometimes causes an effect

sedation may worsen or improve the distress

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12
Q

what are the GI tract effects of acepromazine

A
  1. reduced smooth muscle activity
  2. anti-sialagogue action: reduced saliva
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13
Q

what are the other effects of acepromazine (4)

A
  1. hypothermia: peripheral vasodilation
  2. penile prolapse and/or priapism –> paramphimosis
  3. decrease in hematocrit
  4. mild anti-histamine activity
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14
Q

what are the routes of admin of acepromazine

A

IM (IV, SC)

oral pastes/tablets (20-55% oral bioavailability)

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15
Q

what is the duration of action of acepromazine

A

up to 4 hours or more

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16
Q

where is acepromazine metabolized

A

liver

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17
Q

what are potential drug interactions of acepromazine

A

potentiates effects of opioids, injectable and inhaled anethetics

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18
Q

what are the clinical indications of acepromazine (4)

A
  1. premedication prior to general anesthesia
  2. sedation
  3. motion sickness
  4. “calming” effects
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19
Q

what are the contra-indications of acepromazine

A
  1. hypovolemia
  2. breeding bulls and stallions
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20
Q

what are the cautions of acepromazine in some breeds (2)

A
  1. brachycephalic & giant breeds: increased sensitivity
  2. vasovagal syncope in boxers
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21
Q

what is vasovagal syncope in boxers caused by acepromazine

A

vasodilation leads to hypotension and then inappropriate bradycardia causing the dog to faint

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22
Q

how is vasovagal syncope treated in boxers after acepromazine administration

A

anti-muscarinic drugs –> atropine +/- fluids

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23
Q

how do you prevent the vasovagal syncope in boxers after acepromazine

A

use lower doses

or combine with anti-muscarinic

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24
Q

what is the mechanism of action of butyrophenones

A

dopamine antagonism

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25
what are the effects of butyrophenones
1. sedation/tranquilization 2. anti-emesis
26
what are the side effects of butyrophenones
1. vasodilation & hypotension (a1 adrenergic antagonism) 2. hallucinations 3. agitation
27
what are examples of butyrophenones
1. azaperone (Stresnil) 2. fluanisone + fentanyl (Hypnorm)
28
what is azaperone used for
sedation, premedication or behavioural modificaiton in pigs
29
how is azaperone administered
deep IM
30
what are the side effects of azaperone
1. hypotension (mild) 2. hypothermia 3. priapism
31
what is hypnorm used for
sedation and premedication in mice, rats, rabbits, guinea pigs
32
how is hypnorm administered
IM or IP
33
what can hypnorm antagonize
fentanyl (ex. butorphanol)
34
what are examples of benzodiazepines
1. diazepam (Valium) 2. midazolam (Hypnovel)
35
what is the mechanism of action of benzodiazepines
potentiate activity of inhibitory neurotransmitter GABA
36
what are the effects of benzodiazepines
1. anxiolytic action 2. muscle relaxation 3. anticonvulsant properties
37
what are the side effects of benzodiazepines
1. minimal CV and respiratory depression suited to the sicker patient 2. hepatic failure in cats treated with oral diazepam
38
can you get predictable sedation with benzodiazepines
no not in healthy patients more reliable in sicker patients
39
what is the route of administration of benzodiazepines
IV (IM) or oral route (well absorbed orally)
40
what is the onset and duration of benzodiazepines
rapid onset short duration (injection)
41
how are benzodiazepines metabolized
liver active metabolites of diazepam
42
what are drug interactions with benzodiazepines
elimination impaired by microsomal enzyme inhibitors ex. cimetidine + diazepam and erythromycin + midazolam
43
what are the clinical uses of benzodiazepines
1. premed/hypnosis of sick animals 2. prevention/treatment of seizures 3. muscle relaxation 4. to induce eating in cats 5. occasionally to modify behaviour
44
what are the contraindications of benzodiazepines (2)
1. hepatic encephalopathy (portosystemic shunts) 2. early pregnancy (teratogenic)
45
what are the formulations of diazepam and midazolam
diazepam: insoluble in water --\> propylene glycol but irritant to veins (Valium), lipid emulsion but reduced bioavailability (Diazemuls) midazolam: water soluble
46
which is more potent midazolam or diazepam
midazolam \> diazepam (~2x)
47
what is diazepam licensed in
dogs and cats
48
what is midazolam licensed in
horses
49
what is the mechanism of action of alpha2-adrenoreceptor agonists
activate adrenergic receptors within the sympathetic nervous system
50
which receptors can alpha2-adrenoreceptor agonists act on
1. pre-synaptic a2 receptors 2. post-synaptic a2 receptors 3. post-synaptic a1 receptors
51
what are the effects of alpha2-adrenoreceptor agonists on pre-synaptic a2 receptors
reduce noradrenaline release --\> sympatholytic --\> decrease in sympathetic tone
52
what is the mechanism of action alpha2-adrenoreceptor agonists has on post-synaptic a2 receptors
mimic noradrenaline --\> sympathomimetic --\> increase sympathetic tone
53
what is the mechanism of action alpha2-adrenoreceptor agonists has on post-synaptic a1 receptors
mimic noradrenaline --\> sympathomimetic --\> increase sympathetic tone
54
what mechanism of action does alpha2-adrenoreceptor agonists have on the CNS
mainly act on pre-synaptic a2 receptors reduce central sympathetic tone --\> sympatholytic
55
what is the mechanism of action of alpha2-adrenoreceptor agonists on peripheral nervous system
post- (pre-) synaptic a2 receptors post-synaptic a1 receptors --\> sympathomimetic dominate form is post synaptic
56
what are the effects of alpha2-adrenoreceptor agonists on the CNS
1. sedation: mild to profound, more reliable than with tranquilizers 2. analgesia 3. muscle relaxation
57
what are the effects of alpha2-adrenoreceptor agonists on the cardiovascular system (2)
1. vasoconstriction 2. bradycardia & reduced CO
58
what does alpha2-adrenoreceptor agonists vasoconstriction in the blood vessels cause
increase in BP
59
why do alpha2-adrenoreceptor agonists cause vasoconstriction
**peripheral post-synaptic a2 receptors --\> vasoconstriction (dominate effect)** peripheral post-synaptic a1 receptors --\> vasoconstriction central pre-synaptic a2 receptors --\> vasodilation
60
how do alpha2-adrenoreceptor agonists cause bradycardia & reduced CO
baroreceptor mediated response --\> because of vasoconstriction to minimize the increase in BP central pre-synaptic a2 receptors (decrease sympathetic tone) --\> contributes to bradycardia
61
explain the effects after administration of alpha2-adrenoreceptor agonists (4)
1. initial vasoconstriction & increased BP 2. heart rate falls 3. BP returns to normal 4. heart rate remains low as central effects begin to dominate biphasic response (increase BP then decrease BP) described in humans but hypotension is not seen in animals
62
what are respiratory effects that alpha2-adrenoreceptor agonists cause (2)
1. mild to moderate depression (dose dependent) 2. arterial hypoxemia in ruminants (especially sheep)
63
what are the GIT effects alpha2-adrenoreceptor agonists cause (2)
1. vomiting in some species 2. reduced gut motility
64
what are the endocrine effects that alpha2-adrenoreceptor agonists cause (2)
1. inhibit ADH release --\> diuresis (increased production of dilute urine) 2. inhibit insulin release --\> hyperglycemia (be aware if getting a blood sample from a sedated animal)
65
what are the urogenital effects alpha2-adrenoreceptor agonists cause
1. uterine contraction
66
how are alpha2-adrenoreceptor agonists administered
IM, IV, SC & epidural routes
67
how are oral routes of alpha2-adrenoreceptor agonists metabolized
oral route - high 1st pass metabolism oral transmucosal route may be useful in aggressive patients
68
what can be used to antagonize alpha2-adrenoreceptor agonists
alpha2 antagonists they also antagonize analgesia
69
what are the drug interactions of alpha2-adrenoreceptor agonists
marked anesthesia-sparing effect act synergistically with opioids much greater sparing effect than ACP
70
what are clinical use of alpha2-adrenoreceptor agonists
1. sedation/premedication 2. analgesia 3. offset ketamine hypertonicity
71
what are alpha2-adrenoreceptor agonists licensed in
dogs, cats, horses and cattle
72
what are the contraindications of alpha2-adrenoreceptor agonists
generally reserved for use in healthy patients care with CV disease or in poor general health
73
what are authorized alpha2-adrenoreceptor agonists
xylazine, detomidine, romifidine, medetomidine, dexmedetomidine
74
what alpha2-adrenoreceptor agonists are licensed in dogs and cats
medetomidine, dexmedetomidine, (xylazine), atipamezole
75
what alpha2-adrenoreceptor agonists are licensed in horses
xylazine, detomidine, romifidine
76
what alpha2-adrenoreceptor agonists are licensed in cattle
xylazine, detomidine
77
what is the selectivity difference for a2,a1 receptors
a2:a1 ratio xylazine 160:1 detomidine 260:1 medetomidine 1620:1
78
79
what are the potency differences in different species of what alpha2-adrenoreceptor agonists
xylazine more potent in ruminants than horses detomidine approx equipotent in ruminants and horses pigs are relatively resistant to a2 agonists
80
what alpha2-adrenoreceptor agonists has the longest duration
xylazine \< detomidine/medetomidine \< romifidine
81
which alpha2-adrenoreceptor agonists is pro-arrhythmic
xylazine
82
which alpha2-adrenoreceptor agonists is anti-arrhythmic
medetomidine may be
83
which alpha2-adrenoreceptor agonist causes less ataxia in horses
romifidine --\> less ataxia than other alpha2-adrenoreceptor agonists
84
which alpha2-adrenoreceptor agonist causes uterine contraction
xylazine
85
which alpha2-adrenoreceptor agonist causes vomiting in dogs and cats
xylazine \> medetomidine
86
what is the difference between medetomidine and dexmedetomidine
medetomidine is a racemic mixture of 2 optical isomers dexmedetomidine is the active form and levomedetomidine is inactive (but may delay hepatic metabolism of other drugs)
87
what is vatinoxan
peripheral alpha2 antagonist
88
what does vatinoxan cause
1. acts peripherally to less CV effects --\> reduces vasoconstriction & resultant bradycardia/reduced CO 2. unable to cross blood-brain barrier --\> centrally mediated sedation, muscle relaxation and analgesia
89
how do you chose a sedative
1. side effects/"safety" 2. reliability of sedation 3. pharmacokinetics 4. legislation 5. potency 6. cost
90
which produces the most reliable sedation
alpha2 agonists \> ACP \> benzodiazepines

Module 14 (29 decks)

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