Sedatives Flashcards

1
Q

What is a sedative?

A

A drug that makes you calm, drowsy and not very responsive to external stimuli

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2
Q

What does high sedation cause?

A

Sleep, but can be roused (unlike anaesthesia)

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3
Q

What are the types of sedation?

A

Neuroleptic

Neuroleptanalgsia

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4
Q

What is neuroleptic sedation?

A

Sedation with effects of phenothiazines or butyrophenones on the CNS

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5
Q

What is neuroelepotanalgesia?

A

Combination of a neuroleptic and an opioid

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6
Q

What is tranquilliser?

A

Makes you calm, but alert and responsive

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7
Q

What does a high dose of tranquilliser cause? What is this?

A

Catalepsy

Altered state of consciousness, can be hyper

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8
Q

What is an anxiolytic?

A

Drug that reduces anxiety, makes calm

Normal stressful responses doesn’t result in stress response (increased cortisol)

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9
Q

What are the 4 classes of sedatives?

A

Alpha 2 agonists
Phenothiazines
Butyrophenones
Benzodiazepines

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10
Q

Which classes of sedatives are licensed?

A

All except benzodiazepines

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11
Q

How do alpha 2 agonists work? What do they cause?

A

Bind to a2 receptors
Cause sympathomimetic peripheral effects (e.g. vasoconstriction)
Cause sympatholytic CNS effects (e.g. sedation)

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12
Q

How are alpha 2 agonists administered?

A

Water soluble injection so IV or IM

Molecules lipid soluble so can be orally, SC or epidural

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13
Q

What are the main effects of alpha 2 agonists?

A

Sedation, analgesia (1/3 of sedation duration), muscle relaxation
= anaesthetic sparing agent

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14
Q

What are the side effects of alpha 2 agonists?

A
Vasoconstriction causes increased after load on heart
Diuresis
Hyperglycaemia
Muscle relaxation 
Sweating
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15
Q

What are the advantages to alpha 2 agonists?

A

Analgesic for some of anaesthetic = anaesthetic sparing agent
Has antagonist available

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16
Q

Atipamezole is the antagonist to alpha 2 agonists. What is a disadvantage of using this antagonist?

A

Antagonises all effects including analgesia

Overdose causes excitement and hyperalgesia

17
Q

Give an example of an alpha 2 agonist

A

Romfidine

18
Q

Give an example of the only licensed phenothiazine.

A

Acepromazine

19
Q

Phenothiazines are antagonists to many receptors. Give examples of some of these receptors and what their antagonist binding causes

A

A1 adrenoreceptors - vasodilation
Dopamine receptors -sedation
Histamine receptors - anti-emetic and reduced hypersensitivity
Serotonin receptors - anxiolytic
Muscarinic (cholinergic) receptors - reduced parasympathetic tone

20
Q

How can phenothiazines be administered?

A

Water soluble injectable = IM, IV

Lipid soluble molecules = SC, orally

21
Q

Which is the least reliable route for acepromazine and why?

A

Orally

Least bioavailability

22
Q

What are the effects of acepromazine/phenothiazinines?

A

Sedation (less reliable than a2 agonists)

Muscle relaxation

23
Q

What are the disadvantages of acepromazine?

A

No analgesia

No anatagonist

24
Q

What are the side effects of acepromazine/phenothiazines?

A

Vasodilation
Syncope
Antihistamine
Long lasting

25
Q

What is syncope?

A

Temporary unconsciousness
Lack of blood to brain
Common in brachycephalic and excited animals

26
Q

What is the MOA of butyrophenones?

A

Similar to phenothiazines - antagonist to lots of receptors

27
Q

What are the main effects of butryophenones?

A

Sedation (least reliable)
Muscle relaxation
Anti-emetic, anti-histamien
Long lasting

28
Q

What are the side effects of butyrophenones?

A

Long lasting
Vasodilation (less than acepromazine)
NO ANALGESIA OR ANTAGONIST

29
Q

Give an example of a butyrophenone

A

Fluanisone

azaperone

30
Q

How do benzodiazepines work?

A

Bind to GABA receptor (inhibitory neurotraasmitter)

31
Q

Give 2 examples of benzodiazepines. Are either of these licensed?

A

Diazepam
Midazolam
No licensed benzodiazipin!

32
Q

Why is diazepam not used as much as midazolam?

A

IV solution expensive

Emulsion form even more expensive

33
Q

What is a side effect of benzodiazepines?

A

Causes excitement if used alone

Overdose causes excitement

34
Q

Which is the only group of sedatives to have analgesic effects?

A

Alpha 2 agonists

Only for 1/3 of sedative effect

35
Q

Which are the 2 groups of sedatives to have antagonists?

A

Alpha 2 agonists

Benzodiazepines