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MODULE 14 - Patient Support > PHARMACOLOGY - Sedative Drugs > Flashcards

PHARMACOLOGY - Sedative Drugs Flashcards

1
Q

What are the four main classifications of sedative drugs?

A

Phenothiazines
Butyrophenones
α2 adrenoreceptor agonists
Benzodiazepines

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2
Q

What is the mechanism of action for phenothiazines?

A

Phenothiazines are non-selective dopamine antagonists

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3
Q

What is the most commonly used phenothiazine used in veterinary medicine?

A

Acepromazine

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4
Q

What are the two desired effects that acepromazine has on the central nervous system (CNS)?

A

Sedation
Anti-emetic

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5
Q

What are the six side effects of acepromazine?

A

Hypotension
Anti-arrhythmic
Reduced gut motility
Antisialagogue
Hypothermia
Penile prolapse/Priapism

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6
Q

How does acepromazine cause hypotension?

A

Acepromazine is a non-selective antagonist meaning it will bind to other receptors other than dopamine, such as α1 adrenoreceptors on vascular smooth muscle which usually trigger vasoconstriction, however, if they are bound to by an anatagonist this will prevent vasoconstriction resulting in vasodilation and hypotension

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7
Q

How does acepromazine act as an anti-arrhythmic?

A

Acepromazine is a dopamine antagonist and thus reduces sympathetic nervous system activity which can protect against catecholamine driven arrhythmias

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8
Q

How does acepromazine reduce gut motility?

A

Acepromazine is a non-selective antagonist meaning it will bind to other receptors other than dopamine, such as muscarinic receptors. Through binding to these muscarinic receptors, acepromazine can inhibit the binding and action of acetylcholine which is important for stimulating gut motility

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9
Q

For which species’ is acepromazine liscenced?

A

Dogs
Cats
Horses

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10
Q

How is acepromazine administered?

A

Usually intramuscular injection but can be administered via subcutaneous injection

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11
Q

Why is oral administration of acepromazine unreliable?

A

Oral administration of acepromazine is unrealibale due to it’s variable bioavailability

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12
Q

(T/F) Acepromazine has a rapid onset and short duration of action

A

FALSE. Acepromazine has a slow onset and long duration of action

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13
Q

How does acepromazine interact with other drugs?

A

Acepromazine potentiates the effects of other sedative drugs as well as reduces the quantity of general anaesthetic required

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14
Q

What are the three main clinical indications for the use of acepromazine?

A

Sedative
Premedication
Antiemetic drug

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15
Q

What are the two main contraindications for the use of acepromazine?

A

Hypovolaemic patients
Breeding stallions

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16
Q

Why is acepromazine contraindicated in hypovolaemic patients?

A

Hypovolaemic patients have a reduced intravascular volume and thus already have hypotension which can be worsened by acepromazine administration as it will exacerbate the hypotension

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17
Q

Why is acepromazine contraindicated in breeding stallions?

A

Acepromazine is contraindicated in breeding stallions due to the risk of priapism (persistent erection)

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18
Q

In which breeds should lower doses of acepromazine be given?

A

Giant breeds
Brachycephalic
Herding breeds
Boxers

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19
Q

Why should lower doses of acepromazine be given to herding breeds?

A

Herding dog breeds often have a genetic mutation in the ABCB1 gene that allows certain drugs to cross the blood brain barrier (BBB) and accumulate in the brain

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20
Q

What side effect of acepromazine can be seen in boxers?

A

Vasovagal syncope

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21
Q

What is vasovagal syncope?

A

Acepromazine causes vasodilation which causes hypotension which can trigger an inappropriate vagally mediated bradycardia in boxers, exacerbating the hypotension resulting in syncope

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22
Q

How do you treat a vasovagal syncope episode?

A

Administer an antimuscarinic drug to block the vagal bradycardia

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23
Q

Give an example of an antimuscarinic drug

A

Atropine

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24
Q

How can you prevent a vasovagal syncope episode in boxers?

A

Administer a lower dose of acepromazine
Combine acepromazine with an antimuscarinic drug

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25
Q

What is the mechanism of action for butyrophenones?

A

Butyrophenones are non-selective dopamine antagonists

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26
Q

What are the two desired effects that butyrophenones have on the central nervous system (CNS)?

A

Sedation
Anti-emetic

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27
Q

Give two examples of butyrophenones

A

Azaperone (stresnil)
Fluanisone

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28
Q

For which species is azaperone (stresnil) liscenced?

A

Pigs

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29
Q

How is azaperone (stresnil) administered?

A

Intramuscular injection

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30
Q

What are the three clinical indicators for the use of azaperone (stresnil) in pigs?

A

Sedation
Premedication
Behaviour modification

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31
Q

What are three of the side effects of azaperone?

A

Hypotension
Hypothermia
Priapism

32
Q

What is Hyponorm?

A

Hyponorm is a mixture of fluanisone and
fentanyl

33
Q

For which species’ is Hyponorm licensced?

A

Small mammals

34
Q

How is Hyponorm administered?

A

Intramuscular injection
Intraperitoneal injection

35
Q

What are the two clinical indicators for the use of Hyponorm in small mammals?

A

Sedation
Premedication

36
Q

What is the mechanism of action for α2 adrenoreceptor agonists?

A

α2 adrenoreceptor agonists bind to adrenergic receptors within the sympathetic nervous system

37
Q

What are the effects of α2 adrenoreceptor agonists when they bind to presynaptic α2 adrenoreceptors?

A

α2 adrenoreceptor agonists have a sympatholytic effect when they bind to presynaptic α2 adrenoreceptors as this causes the inhibiton of adenylate cyclase which decreases cAMP and results in the inhibition of calcium influx into the cell, resulting in the inhibition of neurotransmitter release from the presynaptic terminal

38
Q

What are the effects of α2 adrenoreceptor agonists when they bind to postsynaptic α2 adrenoreceptors?

A

α2 adrenoreceptor agonists have a sympathomimetic effect when they bind to post-synaptic α2 adrenoreceptors as they mimic neurotransmitters, resulting in inceased sympathetic activity

39
Q

What are the effects of α2 adrenoreceptor agonists when they bind to postsynaptic α1 adrenoreceptors?

A

α2 adrenoreceptor agonists have a sympathomimetic effect when they bind to post-synaptic α1 adrenoreceptors as they mimic neurotransmitters, resulting in inceased sympathetic activity

40
Q

What are the three desired effects that α2 adrenoreceptor agonists have on the central nervous system (CNS)?

A

Sedation
Analgesia
Muscle relaxation

41
Q

(T/F) α2 adrenoreceptor agonists have the most reliable sedative effect

A

TRUE.

42
Q

What are the nine side effects of α2 adrenoreceptor agonists?

A

Transient hypertension followed by hypotension
Bradycardia
Mild to moderate respiratory depression
Artrial hypoxaemia in ruminants
Vomiting in some species
Reduced gut motility
Diuresis
Hyperglycaemia
Uterine contraction

43
Q

How do α2 adrenoreceptor agonists cause hypertension?

A

When α2 adrenoreceptor agonists bind to post-synaptic α adrenoreceptors on vascular smooth muscle, they have a sympathomimetic effect which will trigger vasoconstriction and thus hypertension

44
Q

How do α2 adrenoreceptor agonists cause bradycardia?

A

α2 adrenoreceptor agonists trigger hypertension which will stimulate baroreceptors to trigger a reflex bradycardia as a compensatory mechanism

45
Q

How do α2 adrenoreceptor agonists cause diuresis?

A

α2 adrenoreceptor agonists inhibit the release of antidiuretic hormone

46
Q

how α2 adrenoreceptor agonists cause hyperglycaemia?

A

α2 adrenoreceptor agonists inhibit insulin release

47
Q

How can α2 adrenoreceptor agonists be administered?

A

Intramuscular injection
Intravenous injection
Subcutaneous injection
Epidural injection

48
Q

What is oral administration of α2 adrenoreceptor agonists unreliable?

A

Oral administration of α2 adrenoreceptor agonists is unreliable due to first pass metabolism

49
Q

How do α2 adrenoreceptor agonists interact with other drugs?

A

α2 adrenoreceptor agonists potentiate the effects of other sedative drugs as well as reduce the quantity of general anaesthetic required

50
Q

What can be used to reverse the effects of α2 adrenoreceptor agonists?

A

α2 adrenoreceptor antagonists

51
Q

Give an example of an α2 adrenoreceptor antagonist

A

Atipamezole

52
Q

What are the four clinical indicators for the use of α2 adrenoreceptor agonists?

A

Sedation
Premedication
Analgesia
Offset ketamine hypertonicity

53
Q

What are the contraindications for the use of α2 adrenoreceptor agonists?

A

Take care administering α2 adrenoreceptor agonists to any patient with cardiovascular disease or in poor general health due to the extensive side effects

54
Q

Give three examples of α2 adrenoreceptor agonists licensed in dogs and cats

A

Xylazine
Medetomidine
Dexmedetomidine

55
Q

Give two examples of α2 adrenoreceptor agonists licensed in cattle

A

Xylazine
Detomidine

56
Q

Give three examples of α2 adrenoreceptor agonists licensed in horses

A

Xylazine
Detomidine
Romifidine

57
Q

Why should you use lower doses of xylazine in cattle compared to horses?

A

Xylazine is more potent in cattle compared to horses so a lower dose is required

58
Q

Which species is relatively resistant to α2 adrenoreceptor agonists?

A

Pigs

59
Q

What are the main differences between medetomidine and dexmedetomidine?

A

Dexmedetomidine is more potent but has a slightly shorter duration of action than medetomidine

60
Q

Which α2 adrenoreceptor agonists are most specific to α2 adrenoreceptors and thus have fewer side effects?

A

Medetomidine
Dexmedetomidine

61
Q

Which α2 adrenoreceptor agonists are least specific to α2 adrenoreceptors and thus have the most side effects?

A

Xylazine

62
Q

Which α2 adrenoreceptor agonists has the longest duration of action?

A

Romifidine

63
Q

Which α2 adrenoreceptor agonist has the shortest duration of action?

A

Xylazine

64
Q

Which α2 adrenoreceptor agonist is best for sedating standing horses?

A

Romifidine as is has the least muscle relaxing properties which reduces ataxia in standing horses

65
Q

What is the mechanism of action for benzodiazepines?

A

Benzodiazepines potentiate the activity of inhibitory GABAa receptors

66
Q

Give two examples of benzodiazepines

A

Diazepam
Midazolam

67
Q

Which species’ is diazepam liscensed in?

A

Dogs
Cats

68
Q

Which species is midazolam liscensed in?

A

Horses

69
Q

What are the four desired effects that benzodiazepines have on the central nervous system (CNS)?

A

Sedation
Anxiolytic effect
Antiepileptic
Muscle relaxant

70
Q

How are benzodiazepines administered?

A

Intravenous injection
Intramuscular injection
Orally

71
Q

Why is midazolam better for intravenous administration compared to diazepam?

A

Diazepam is insoluble in water so tends to be dissolved in solvents that can irritate the veins or in lipid emulsions resulting in poor bioavailability, however midazolam is soluble in water and thus can be given IV without irritating the veins

72
Q

How do benzodiazepines interact with other drugs?

A

Benzodiazepines are eliminated through the action of microsomal hepatic enzymes and thus this elimination can be affected by drugs that act as microsomal enzyme inhibitors

73
Q

Give an example of a drug that acts as a microsomal enzyme inhibitor

A

Erythromycin

74
Q

What are the four main clinical indicators for the use of benzodiazepines?

A

Premedication in sick animals
Muscle relaxation
Antiepileptic
Offset ketamine hypertonicity

75
Q

Why are benzodiazepines not very effective premedications in healthy animals?

A

Benzodiazepines by themselves produce little sedation in healthy animals and can even cause paradoxical excitement in healthy animals. However, they can be useful for premedication in sick animals as they have less side effects compared to other sedatives

76
Q

What are the two main contraindications for the use of benzodiazepines?

A

Patients with severe hepatic disease and/or hepatic encephalopathy
Animals in early pregnancy

77
Q

Why are benzodiazepines contraindicated in patients in early pregnancy?

A

Benzodiazepines can cross the placenta

MODULE 14 - Patient Support (25 decks)

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