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

PHARMACOLOGY - Sedative Drugs Flashcards

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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 (ACP)

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4
Q

What are the effects and side effects of acepromazine?

A

Sedation
Antiemetic
Hypotension
Anti-arrhythmic
Reduced gut motility
Antisialagogue
Hypothermia
Penile prolapse/Priapism
Mild antihistamine effect
Increase seizure activity

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5
Q

How does acepromazine cause hypotension?

A

Acepromazine is a non-selective antagonist meaning it will bind to and have an antagonising effect on receptors other than dopamine, such as α1 receptors on vascular smooth muscle, resulting in vasodilation and hypotension

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6
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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7
Q

How does acepromazine reduce gut motility?

A

Acepromazine is a non-selective antagonist meaning it will bind to and have an antagonising effect on 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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8
Q

How does acepromazine have a mild antihistamine effect?

A

Acepromazine is a non-selective antagonist meaning it will bind to and have an antagonising effect on receptors other than dopamine, such as histamine 1 (H1) receptors

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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 and intravenous injection

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11
Q

What are the pharmacokinetic properties of acepromazine?

A

Variable bioavailability (unreliable for oral administration)
Slow onset and long duration of action

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12
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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13
Q

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

A

Sedative
Premedication
Antiemetic

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14
Q

What are the contraindications for acepromazine?

A

Hypovolaemia
Breeding stallions
History of seizures

There is limited evidence that ACP affects seizure patients

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15
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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16
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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17
Q

In which dog breeds should lower doses of acepromazine be given?

A

Giant breeds
Brachycephalic
Herding breeds
Boxers

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18
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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19
Q

What side effect of acepromazine can be seen in boxers?

A

Vasovagal syncope

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20
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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21
Q

How do you treat a vasovagal syncope episode?

A

Administer an antimuscarinic drug to block the vagal bradycardia

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22
Q

Give an example of an antimuscarinic drug

A

Atropine

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23
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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24
Q

What is the mechanism of action for butyrophenones?

A

Butyrophenones are non-selective dopamine antagonists

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25
What are the effects and side effects of butyrophenones?
Sedation Antiemetic Hypotension Hypothermia Priapism
26
Give two examples of butyrophenones
Azaperone (stresnil) Fluanisone
27
Which species is azaperone (stresnil) liscenced in?
Pigs
28
How is azaperone (stresnil) administered?
Intramuscular injection
29
What are the clinical indicators for azaperone (stresnil) in pigs?
Sedation Premedication Behaviour modification
30
What is Hyponorm?
Hyponorm is a mixture of fluanisone and fentanyl
31
Which species' is Hyponorm licensced for?
Small mammals
32
How is Hyponorm administered?
Intramuscular injection Intraperitoneal injection
33
What are the clinical indicators for the use of Hyponorm in small mammals?
Sedation Premedication
34
(T/F) Hyponorm has a rapid recovery
FALSE. Hyponorm has a prolonged recovery
35
What is the mechanism of action for α2 adrenoreceptor agonists?
α2 adrenoreceptor agonists bind to adrenergic receptors within the sympathetic nervous system
36
What are the effects of α2 adrenoreceptor agonists when they bind to presynaptic α2 adrenoreceptors?
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
37
What are the effects of α2 adrenoreceptor agonists when they bind to postsynaptic α2 adrenoreceptors?
α2 adrenoreceptor agonists have a sympathomimetic effect when they bind to post-synaptic α2 adrenoreceptors as they mimic neurotransmitters, resulting in inceased sympathetic activity
38
What are the effects of α2 adrenoreceptor agonists when they bind to postsynaptic α1 adrenoreceptors?
α2 adrenoreceptor agonists have a sympathomimetic effect when they bind to post-synaptic α1 adrenoreceptors as they mimic neurotransmitters, resulting in inceased sympathetic activity
39
(T/F) α2 agonists have the most reliable sedative effect
TRUE.
40
What are the effects and side effects of α2 agonists?
Sedation Analgesia Muscle relaxant Hypertension Bradycardia Arrhythmogenic in horses Mild to moderate respiratory depression Artrial hypoxaemia in ruminants Pulmonary oedema in small ruminants Tachypnoea in pyrexic horses Worsens airway obstruction in horses Vomiting in some species Reduced gut motility Diuresis Hyperglycaemia Uterine contraction
41
How do α2 adrenoreceptor agonists cause hypertension?
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
42
How do α2 adrenoreceptor agonists cause bradycardia?
α2 adrenoreceptor agonists trigger hypertension which will stimulate baroreceptors to trigger a reflex bradycardia as a compensatory mechanism
43
How do α2 adrenoreceptor agonists cause diuresis?
α2 adrenoreceptor agonists inhibit the release of antidiuretic hormone
44
How do α2 adrenoreceptor agonists cause hyperglycaemia?
α2 adrenoreceptor agonists inhibit insulin release
45
How can α2 adrenoreceptor agonists be administered?
Intramuscular injection Intravenous injection Subcutaneous injection Epidural injection
46
What is oral administration of α2 adrenoreceptor agonists unreliable?
Oral administration of α2 adrenoreceptor agonists is unreliable due to first pass metabolism
47
How do α2 adrenoreceptor agonists interact with other drugs?
α2 adrenoreceptor agonists potentiate the effects of other sedative drugs as well as reduce the quantity of general anaesthetic required
48
What can be used to reverse the effects of α2 adrenoreceptor agonists?
α2 adrenoreceptor antagonists
49
Give an example of an α2 adrenoreceptor antagonist
Atipamezole
50
(T/F) Atipamezole is licensed in food producing animals
FALSE. Atipamezole is not licensed in food producing animals
51
What are the four clinical indicators for the use of α2 adrenoreceptor agonists?
Sedation Premedication Analgesia Offset ketamine hypertonicity
52
What are the contraindications for the use of α2 adrenoreceptor agonists?
Take care administering α2 adrenoreceptor agonists to any patient with cardiovascular disease or in poor general health due to the extensive side effects
53
Which α2 agonists are licensed in dogs and cats?
Xylazine Medetomidine Dexmedetomidine
54
Which α2 agonists are licensed in cattle?
Xylazine Detomidine
55
Which α2 agonists are licensed in horses?
Xylazine Detomidine Romifidine
56
Why should you use lower doses of xylazine in cattle compared to horses?
Xylazine is more potent in cattle compared to horses so a lower dose is required
57
Which species is relatively resistant to α2 adrenoreceptor agonists?
Pigs
58
What are the main differences between medetomidine and dexmedetomidine?
Dexmedetomidine is more potent but has a slightly shorter duration of action than medetomidine
59
Which α2 adrenoreceptor agonists are most specific to α2 adrenoreceptors and thus have fewer side effects?
Medetomidine Dexmedetomidine
60
Which α2 adrenoreceptor agonists are least specific to α2 adrenoreceptors and thus have the most side effects?
Xylazine
61
Which α2 adrenoreceptor agonists has the longest duration of action?
Romifidine
62
Which α2 adrenoreceptor agonist has the shortest duration of action?
Xylazine
63
Which α2 adrenoreceptor agonist is best for sedating standing horses?
Romifidine as is has the least muscle relaxing properties which reduces ataxia in standing horses
64
What is the mechanism of action for benzodiazepines?
Benzodiazepines potentiate the activity of inhibitory GABAa receptors
65
Give two examples of benzodiazepines
Diazepam Midazolam
66
Which species' is diazepam liscensed in?
Dogs Cats
67
Which species is midazolam liscensed in?
Horses
68
What are the four desired effects that benzodiazepines have on the central nervous system (CNS)?
Sedation Anxiolytic effect Antiepileptic Muscle relaxant
69
How are benzodiazepines administered?
Intravenous injection Intramuscular injection Orally
70
Why is midazolam better for intravenous administration compared to diazepam?
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
71
How do benzodiazepines interact with other drugs?
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
72
Which drugs act as microsomal enzyme inhibitors?
Erythromycin Cimetidine
73
What are the clinical indicators for the use of benzodiazepines?
Premedication in sick animals Muscle relaxation Antiepileptic
74
Why are benzodiazepines not very effective premedications in healthy animals?
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
75
What are the contraindications for the use of benzodiazepines?
Hepatic encephalopathy Early pregnancy
76
Why are benzodiazepines contraindicated in patients with hepatic encephalopathy?
Benzodiazepines are contraindicated in patients with hepatic encephalopathy as they are metabolised by the liver and thus can cause strong sedation in patients with liver dysfunction
77
Why are benzodiazepines contraindicated in patients in early pregnancy?
Benzodiazepines can cross the placenta
78
Which factors should you consider when determining which sedative you should choose for premedication?
1. How much sedation is needed *(consider patient temperament and the procedure taking place)* 2. Patient health *(any contraindications, or alternatively any side effects that may benefit the patient)* 3. Pharmacokinetics 4. Controlled drug legislation and veterinary medicine register 5. Affordability for the client
79
What are the aims of premedication?
To provide a calming or sedative effect To provide analgesia To reduce dose of other drugs required To counteract other unwanted drug affects To provide a more smooth induction and recovery

MODULE 14 - Patient Support (24 decks)

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