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Pharmacology Test 2 > Sedatives and Analgesics Part 4 > Flashcards

Sedatives and Analgesics Part 4 Flashcards

1
Q

Name the drugs that are neuroleptic (tranquilizers)?

A 
 Acepromazine 
 Diazepam
 Midazolam
 Alprazolam
 Flumazenil*
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2
Q

Name the drugs that are alpha 2 agonists?

A 
 Dexmedetomidine 
 Medetomidine
 Xylazine
 Atipamezole*
 Yohimbine*
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3
Q

Name the term:

Induces a state of behavioral change wherein anxiety is relieved and the patient is relaxed although aware of their surroundings No analgesia or anesthesia when used alone

A

Tranquilizer (neuroleptic, anxiolytic):

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4
Q

Name the term:

Induces a state characterized by CNS depression and drowsiness, decreased awareness of surroundings

A

Sedative

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5
Q

Name the term:

Induces sleep

A

Hypnotic

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6
Q

Name the term:

Attenuate nociceptive input leading to reduction in pain sensation. True analgesics stop transduction and transmission of pain signals.

A

Analgesic

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7
Q

Name the term:

Decrease central sensitization to pain. They do not block the transmission of the stimulus

A

Antihyperalgesics

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8
Q

Name the term:

Diminished ability to perceive pain

A

Antinociception

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9
Q

Name the term:

Induces analgesia & stupor bordering on general anesthesia

A

Narcotic

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10
Q

Name the term:

Analgesia & amnesic state produced by administration of a neuroleptic + narcotic
Deep sedation achievable, unconsciousness may occur

A

Neuroleptanalgesia:

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11
Q

Name the term:

Drug(s) given before a medical, surgical, or invasive procedure to induce sedation, analgesia, and relieve anxiety

A

Pre-medication

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12
Q

4 steps to create a sedation and premedication plan

A
  1. Anti-convulsant
  2. Sedation
  3. Muscle Relaxation
  4. Analgesia
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13
Q

Name the 2 excitatory neurotransmitters (2)?

A

Glutamate (NMDA receptor)

Acetylcholine

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14
Q

Name the 2 inhibitory Neurotransmitters?

A
  • GABA

- Glycine (spinal cord)

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15
Q

Name the Phenothiazine derivative drug?

A

Acepromazine

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16
Q

Name the Benzodiazepine derivative?

A
  • Diazepam
  • Midazolam
  • Alprazolam
  • Flumazenil
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17
Q

Name the alpha 2 agonists?

A
  • Dexmedetomidine
  • Medetomidine
  • Xylazine
  • Yohimbine
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18
Q

Main effects of the neuroleptic tranquilizers?

A

 Sedation & hypnosis

 Emotional quietness

 Dissociation from surroundings

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19
Q

Only ____ agonists have analgesic effects? the other classes of tranquilizers do not have any pain relief properties when used alone

A

A2-agonists

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20
Q

Most common phenothiazine?

A

Acepromazine

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21
Q

Mechanism of action for Phenothiazine?

A

Competitively antagonize excitatory dopamine receptors in the CNS

Also variably blocks histamine, alpha-1 and Acetylcholine (muscarinic) receptors

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22
Q

Phenothiazines like acepromazine inhibit vomiting by?

A

Inhibition of alpha-2 receptors to the Chemoreceptor Trigger Zone (CRTZ) that effects Vomiting

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23
Q

Phenothiazine drugs increase _____ release usually that’s usually inhibited by dopamine?

A

Prolactin

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24
Q

Phenothiazines also have a minimal _____ relaxation effect?

A

muscle

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25
Q

Route of administration for phenothiazine?

A

Can be given IV, IM, SQ or PO

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26
Q

With dogs, the route of administration of Phenothiazines (Acepromazine) has this effect?

A

Oral bioavailability in dogs is low (~20%)

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27
Q

Do Phenothiazines cross the blood brain barrier?

A

Yes

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28
Q

Phenothiazines are metabolized in the?

A

liver and excreted in the urine

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29
Q

What are the Phenothiazines effects on the CNS?

A
  • Sedation
  • Decreased spontaneous motor activity
  • Anti-emetic (CRTZ)
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30
Q

Phenothiazines effects on the cardiovascular system?

A

Blocks Alpha-1 receptors

-Vasodilation/hypotension

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31
Q

What breeds are more sensitive to cardiovascular effects of phenothiazines?

A

Boxers/brachycephalics, MDR1 mutants, large breed dogs and sighthounds may be more sensitive to the cardiovascular effects than other breeds so you might need to dose reduce

32
Q

If Acepromazine is used in large doses with opioids, what kind if effects can we see?

A

Respiratory depression

33
Q

Acepromazine effects on skeletal muscle?

A

Moderate muscle relaxation

34
Q

What can be seen with the spleen with acepromazine?

A

Reduced hematocrit due to splenic sequestration ie. splenomegaly

35
Q

When should we not use phenothiazines? Think of serious contraindications you might not want to increase?

A

Do not use any time vasodilation is contraindicated

Cardiac dz, hypovolemia/dehydration, epidural, etc

36
Q

What are some adverse effects with stallions using acepromazine?

A

Penile prolapse and injury (paraphimosis)

37
Q

What are the adverse effects with cattle using acepromazine?

A

Not approved in food animals, ruminal regurgitation can be seen

38
Q

What can be seen with aggressive dogs using acepromazine?

A

May startle more easily, increased aggression and CNS stimulation sometimes seen.

39
Q

What can be seen with excited patients using acepromazine?

A

reduced sedation

40
Q

At larger doses or chronic doses what can be seen using acepromazine?

A

Functional liver disease

41
Q

Main drug used in the Phenothiazine class?

A

Acepromazine

42
Q

Sedative effects of Acepromazine?

A
  • Yes – good, reliable sedation, but little indication for use on its own
  • Combine with analgesic
43
Q

Acepromazine effects on muscle relaxation?

A

Moderate muscle relaxation

44
Q

Acepromazine analgesic effects?

A

none

45
Q

Acepromazine this is the #1 adverse effect for cardiovascular effects?

A

Hypotension

46
Q

Acepromazine reversal agent?

A

None, once given you must ride out clinical effects (2-4 hours, generally)

47
Q

Name the 3 Benzodiazepine agonists?

A

Diazepam (Valium®)

Midazolam (Versed®)

Alprazolam (Xanax®)

48
Q

Name the Benzodiazepine competitive antagonist?

A

Flumazenil

49
Q

Benzodiazepine partial agonist?

A

Imepitoin

50
Q

Mechanism of action for Benzodiazepine?

A

Bind & activate benzodiazepine binding site on GABAA receptor to cause hyperpolarization of neurons

51
Q

GABA is the main….?

A

GABA is the main inhibitory neurotransmitter in the CNS, higher threshold and therefore less likely to fire, chloride ion channels

52
Q

Benzodiazepine are ____solube so that means? And are excreted /metabolized by?

A 
Lipid soluble (wide distribution, cross
BBB, protein bound)
  • Metabolized in liver to active metabolites
  • Excreted in the urine primarily
53
Q

Diazepams most common route of administration is? Name the adverse effects

A

-Most common route, give slowly IV
(avoid hypotension)

-Slow/poor absorption IM, painful injection (propylene glycol)

54
Q

Midazolam most common route of administration is? Name the adverse effects

A

Midazolam IM (or IV): can be an irritant IM

Can think of it as the ‘version of
diazepam that you can give IM’

55
Q

Describe oral administration for the benzodiazepine? Name who you can’t give orally to certain species!!

A

Generally good oral absorption

Diazepam has short duration, alprazolam often used instead

Note: Oral diazepam can cause hepatic necrosis in cats!!

56
Q

Transmucosal (intranasal, rectal) administration for benzodiazepine?

A

Diazepam has decent bioavailability in dogs via these routes

57
Q

Clinical uses of Benzodiazepines?

A
  • Anxiolytics (behavioral modifiers) Ex. thunder storm anxiety /alprazolam works well for this
  • Anticonvulsants: Emergency treatment of seizures and status epilepticus
  • Premedication: Combined with other agents. Neuroleptanalgesia
  • Sedation: (Mild) NOT reliable on its own. May have paradoxical excitation (cat on ceiling scenario). Most reliable as sedative in ruminants

Muscle relaxation: Central effects, profound, but short-lived. Urinary tract antispasmodic

Appetite stimulation: Considered more of a side effect

58
Q

WHO IS USED FOR SPECIFIC REVERSAL OF BENZODIAZEPINE? Describe how it works?

A

Flumazenil for specific reversal

  • Competitive antagonist
  • Binds to benzodiazepine receptor on GABA
59
Q

What do we worry about with oral diazepam to cats? What can we use instead?

A

Cats: Hepatotoxicity can be seen with oral diazepam! -CONTRAINDICATED

Does not seem to be a problem with oral alprazolam

60
Q

What do we worry about with horses with Benzodiazepine?

A

Muscle fasciculations have been seen, ataxia at high doses

61
Q

What do we worry about with excitatory effects with Benzodiazepine?

A

Paradoxical excitement sometimes seen:

  • Usually combine with other agents
  • Caution with fear-aggressive animals (disinhibition)
62
Q

What can we seen with diazepam injections?

A

Propylene glycol: Pain with IM injection, hypotension with rapid IV injection, hemolysis with large IV doses

63
Q

Adverse effects with pregnancy of benzodiazepine?

A

May be teratogenic – FDA category D for humans, category C for animals. Distributed into milk and can affect nursing neonates

64
Q

Benzodiazepine can cause ____ and _____ disease?

A

Hepatic & Renal Disease:

Altered/delayed drug metabolism & excretion)

65
Q

Benzodiazepine is Often the MOST reliable sedatives used in these categories of animals?

A

very young, very old, or very sick patients

66
Q

True or False?

Acepromazine has tranquilizing and analgesic effects?

A

False (Only tranquilizing)

67
Q

What is the most important cardiovascular side effect of acepromazine?

A

Hypotension

68
Q

Why is oral diazepam contraindicated in cats?

A

Hepatotoxicity

69
Q

What are the 3 main receptors for acepromazine?

A
  1. CNS effect ( competitive antagonism of the excitatory central dopamine = neurolepsis)
  2. Alpha-1 antagonism (peripheral vasodilation- hypotension)
  3. Alpha-2 antagonism in CNS causes vomiting inhibition
70
Q

Name the main mechanism of action for Acepromazine?

A

competitive antagonism of the dopamine receptors in the CNS

71
Q

Most common routes of administration for acepromazine?

A

Oral tablets most common

IV, IM, SubQ

72
Q

Name the most common tranquilizer?

A

Acepromazine

73
Q

Name the Benzodiazepines?

A

Dizepam, Midazalam, Alprazolam

74
Q

Name the benzodiazepines receptor?

A

Bind and activate benzodiazepine binding site on Gaba receptor = hyperpolarization of neurons

75
Q

GABA is?? what if you agonize it what does it do?

A

if you agonize Gaba = depress the CNS

main inhibitory transmitter for CNS

Pharmacology Test 2 (7 decks)

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