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pharm II > Neuroleptics > Flashcards

Neuroleptics Flashcards

1
Q

___________ is a phenothiazine derivative

A

Acepromazine

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2
Q

___________ are benzodiazepine derivative agonists

A
  1. Diazepam
  2. Midazolam
  3. Alprazolam
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3
Q

___________ are benzodiazepine derivative antagonists

A

Flumazenil

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4
Q

What is a neuroleptic?

A

Tranquilizer, anxiolytic

no analgesia (pain relief) or anesthesia when used alone

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5
Q

What parts of the pain pathway do benzodiazepine derivative agonists act on?

A

Perception and modulation

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6
Q

What are the main effects of neuroleptics?

A
  1. Sedation/hypnosis
  2. Emotional quiteness
  3. Dissociation from surroundings
  4. Centrally-mediated muscle relaxation
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7
Q

__________ is the most commonly used phenothiazine derivative neuroleptic

A

Acepromazine

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8
Q

Is there a reversal agent for neuroleptics?

A

Flumazenil - GABA receptor antagonist at the benzodiazepine binding site

only for benzodiazepines, NO REVERSAL FOR ACEPROMAZINE

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9
Q

What is the mode of action for benzodiazepine derivatives?

A

GABA receptor competitive agonist at the benzodiazepine binding site

(Diazepam, Midazolam, Alprazolam)

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10
Q

________ is the main inhibitory neurotransmitter in the CNS

A

GABA

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11
Q

Which of the following is false?

A. Midazolam and diazepam have a shorter duration of action than alprazolam

B. Diazepam can be give IV, IM, or TM in the case of a seizure

C. Splenomegaly can be seen following IV Acepromazine administration

D. Benzodiazepines can cross the BBB

A

B. Diazepam can be give IV, IM, and TM in the case of a seizure

DO NOT GIVE DIAZEPAM IM

  • Diazepam has slow absorption IM and is painful
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12
Q

What species differences need to be considered when using diazepam specifically?

A

Oral diazepam can cause hepatic necrosis in cats

oral diazepam in cats is contraindicated, IV or TM is okay

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13
Q

What route of admin can Midazolam be given?

A

IV or IM

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14
Q

What are the precautions of acepromazine use?

A
  1. Significant CV hypotension
  2. Penile prolapse in horses
  3. Aggression in dogs
  4. CNS stimulation (occasionally when used alone)
  5. Boxers/ MDR1 gene mutation have worse hypotension
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15
Q

What are the clinical indications for using acepromazine?

A
  1. Anti-emetic for motion sickness
  2. Neuroleptanalgesia - Preanesthetic agent when combined with opioids
    (Ex: ace + hydro)
  3. Pruritis due to allergic irritation (ace is an histamine antagonist)
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16
Q

True or False: Acepromazine can be reversed with flumazenil

A

FALSE, no reversal for phenothiazine derivatives

17
Q

Clinical indications for benzodiazepine derivatives?

A
  1. Pre med when combined w opioids, neuroleptanalgesia
    Ex: Diazepam + fentanyl
  2. Reduce anxiety (storms, etc)
  3. Anticonvulsant (acute treatment of seizures)
  4. Muscle relaxation
    Ex: Urinary tract antispasmodic (FLUTD)
  5. Appetite stimulation
18
Q

What parts of the pain pathway do phenothiazine derivative agonists act on?

A

Perception

Ex: Acepromazine

19
Q

MOA of Acepromazine?

A
  1. Central dopamine receptor competitive antagonist
  2. Variably blocks histamine, a1, and Ach
  3. Peripheral a1 receptor antagonist
    vasodilation leading to hypotension
  4. Central A2 antagonist
    CRTZ + Vomiting center - antiemetic
20
Q

What is true about PO Acepromazine?

A

Low oral bioavailability due to basic drug in acidic environment (more ionized)

  • have to use inc. dose when given PO
21
Q

Acepromazine onset of action is ________, and duration of action is _______

A

Slow, long

22
Q

What can be seen with large doses of acepromazine?

A

Extrapyramidal signs (rigidity, tremors)

23
Q

What animals are sensitive to acepromazine?

A
  1. Brachycephalics
  2. Boxers
  3. MDR-1 mutants
  4. Animals w liver disease
24
Q

Acepromazine has minimal depressive effects on the __________ system

A

Respiratory

25
Q

What can be seen on a radiograph after IV admin of acepromazine?

A

Splenomegaly

26
Q

Acepromazine is rarely used alone, except for _________

A

anti-motion sickness

27
Q

What can be seen in horses when using acepromazine?

A

Penile prolapse

28
Q

________ can sometimes be used to alleviate pruritic skin due to allergic irritation

A

Acepromazine

29
Q

Number 1 adverse effect of acepromazine?

A

Severe CV effects due to vasodilation and hypotension

30
Q

Benzodiazepines MOA?

A

GABA receptor competitive agonism at the benzo binding site

31
Q

Which benzodiazepine derivative has the longest duration of action?

A

Alprazolam

diazepam and midazolam have shorter duration of action

32
Q

Most common route of admin for Diazepam?

A

IV

33
Q

Diazepam should not be given ________ because of?

A

IM

slow absorption IM and painful due to propylene glycol

34
Q

Oral diazepam is contraindicated in _______

A

Cats

hepatic necrosis

35
Q

You want to reverse Diazepam, what drug do you pull up and how do you administer it?

A

Flumazenil IV

36
Q

Why are benzodiazepine derivatives not reliable for sedation when given alone?

A

Can cause paradoxical excitation

37
Q

Which of the following is least likely to be used as an antispasmodic for a blocked cat with FLUTD?

A. Alprazolam
B. Midazolam
C. Acepromazine
D. Diazepam

A

C. Acepromazine

38
Q

Which class of neuroleptics is better at achieving muscle relaxation?

A

Benzos > phenothiazine derivatives

39
Q

Which of the following neuroleptics have minimal effects on the CV and resp system?

A

Benzos

  1. Alprazolam
  2. Midazolam
  3. Diazepam

pharm II (23 decks)

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