Sedatives Flashcards

1
Q

What are the 2 mechanisms of action of sedatives?

A

Antagonise excitatory neurotransmitters

Potentiate inhibitory neurotransmitters

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2
Q

Name the 4 groups of sedatives and give examples of drugs from each class

A

Phenothiazines - ACP
Alpha 2 agonists - Medetomidine, Dexmedatomidine, Xylazine
Benzodiazepines - Diazdepam, Midazolam
Butyrophenones - Azaperone, Hypnorm

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3
Q

Describe the mechanism of action of ACP

A

Non-selective dopamine antagonist causing tranquilisation/sedation and anti-emesis
no analgesia

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4
Q

Describe the pharmacokinetics of ACP

A
Solution for injection IM, IV, SC
Oral paste in horses
Duration of action - 4hrs
Hepatic metabolism
Potentiates opioids, injectable and inhaled anaesthetics
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5
Q

What are the effects of ACP?

A

CV - vasodilation (due to alpha 1 antagonist), hypotension, variable effect on HR, antiarrhythmic (increases the threshold for adrenaline induced arrhythmias)
RESP - min direct effect
GIT - decreases smooth muscle activity, antisialogogue
Hypothermia, priapism, decreased PCV

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6
Q

What are the clinical indications for using ACP?

A

Premed, sedation, motion sickness

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7
Q

What are the contraindications for using ACP?

A

Hypovolaemia , breeding bulls/stallions, giant breeds have an increased sensitivity to lower doses

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8
Q

Describe the mechanism of action of the alpha 2 agonists

A

Agonise alpha 2 adrenergic receptors.
CNS - presynaptic - reduce noradrenaline release
Peripheral - act on pre and postsynaptic receptors

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9
Q

Describe the pharmacokinetics of alpha 2s

A

IM, IV, SC, epidural, transmucosal
High first pass metabolism with oral admin
Can give antagonists to reverse action
Marked anaesthetic sparing effect

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10
Q

What are the effects of the alpha 2s?

A

CNS - sedation is mild-profound, analgesia has a shorter duration than sedation, muscle relaxation
CVS - peripheral vasoconstriction, increased blood pressure, arrthymias (sinus and AV block)
RESP -mild-mod depression, arterial hypoxaemia in ruminants
GIT - v+, decreased motility
Endocrine - inhibits ADH and insulin release
Uterine contraction

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11
Q

What are the clinical indications for using alpha 2s?

A

Premed, sedation, analgesia, offset ketamine hypertonicity

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12
Q

What are the contradindications associated with using alpha 2s?

A

Reserved for use in young, healthy patients, cases with CV dysfunction

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13
Q

Describe the differences between different alpha 2 drugs

A

Duration: xylazine

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14
Q

What are the differences between detomidine and medetomidine

A

Medetomidine is a racemic mixture
May delay hepatic metabolism of other drugs
May decrease activity of dexmedetomidine
May contribute to undesirable cardiac effects
Dex is more potent

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15
Q

Describe the mechanism of action of benzodiazepines

A

Potentiates activity of inhibitory NT GABA

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16
Q

Describe the pharmacokinetics of the benzodiazepines

A

IV, IM, oral (gd absorption)
Rapid onset, short duration
Hepatic metabolism
Elimination impaired by microsomal enzyme inhibitors e.g. Cimetidine and Diazepam, Erythromycin and Midazolam

17
Q

What are the effects and side effects of the benzodiazepines?

A

Anxiolytic - may get paradoxical excitement in healthy patients and sedation in sick
Min. CVS and resp depression
Anticonvulsant
Muscle relaxation

18
Q

What are the indications for using benzodiazepines?

A
Premed/hypnosis of sick animals
Prevention/tx of seizures
Muscle relaxation
Induce eating in cats
Occasionally to modify behaviour
19
Q

What are the contraindications associated with benzodiazepines?

A

Hepatic encephalopathy (PSS), early pregnancy (tetratogenic)

20
Q

Describe the mechanism of action of the butyrophenones

A

Dopamine receptor antagonist

Tranquilisation, sedation and anti-emesis

21
Q

What are the effects/side effects of butyrophenones?

A

Vasodilation and hypotension, hallucinations, agitation

Azaperone = hypotension, hypothermia, priapism

22
Q

What are the indications for using butyrophenones?

A
Azaperone =  sedation, premed, behavioural modification in pigs, IM then leave undisturbed for 5 mins
Hypnorm = sedation and premed, small furries, IM/IP, prolonged recovery times