Neuroleptics

Question 1

___________ is a phenothiazine derivative

Answer 1

Acepromazine

Question 2

___________ are benzodiazepine derivative agonists

Answer 2

1. Diazepam
2. Midazolam
3. Alprazolam

Question 3

___________ are benzodiazepine derivative antagonists

Answer 3

Flumazenil

Question 4

What is a neuroleptic?

Answer 4

Tranquilizer, anxiolytic

no analgesia (pain relief) or anesthesia when used alone

Question 5

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

Answer 5

Perception and modulation

Question 6

What are the main effects of neuroleptics?

Answer 6

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

Question 7

__________ is the most commonly used phenothiazine derivative neuroleptic

Answer 7

Acepromazine

Question 8

Is there a reversal agent for neuroleptics?

Answer 8

Flumazenil - GABA receptor antagonist at the benzodiazepine binding site

only for benzodiazepines, NO REVERSAL FOR ACEPROMAZINE

Question 9

What is the mode of action for benzodiazepine derivatives?

Answer 9

GABA receptor competitive agonist at the benzodiazepine binding site

(Diazepam, Midazolam, Alprazolam)

Question 10

________ is the main inhibitory neurotransmitter in the CNS

Answer 10

GABA

Question 11

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

Answer 11

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

Question 12

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

Answer 12

Oral diazepam can cause hepatic necrosis in cats

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

Question 13

What route of admin can Midazolam be given?

Answer 13

IV or IM

Question 14

What are the precautions of acepromazine use?

Answer 14

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

Question 15

What are the clinical indications for using acepromazine?

Answer 15

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)

Question 16

True or False: Acepromazine can be reversed with flumazenil

Answer 16

FALSE, no reversal for phenothiazine derivatives

Question 17

Clinical indications for benzodiazepine derivatives?

Answer 17

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

Question 18

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

Answer 18

Perception

Ex: Acepromazine

Question 19

MOA of Acepromazine?

Answer 19

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

Question 20

What is true about PO Acepromazine?

Answer 20

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

• have to use inc. dose when given PO

Question 21

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

Answer 21

Slow, long

Question 22

What can be seen with large doses of acepromazine?

Answer 22

Extrapyramidal signs (rigidity, tremors)

Question 23

What animals are sensitive to acepromazine?

Answer 23

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

Question 24

Acepromazine has minimal depressive effects on the __________ system

Answer 24

Respiratory

Question 25

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

Answer 25

Splenomegaly

Question 26

Acepromazine is rarely used alone, except for _________

Answer 26

anti-motion sickness

Question 27

What can be seen in horses when using acepromazine?

Answer 27

Penile prolapse

Question 28

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

Answer 28

Acepromazine

Question 29

Number 1 adverse effect of acepromazine?

Answer 29

Severe CV effects due to vasodilation and hypotension

Question 30

Benzodiazepines MOA?

Answer 30

GABA receptor competitive agonism at the benzo binding site

Question 31

Which benzodiazepine derivative has the longest duration of action?

Answer 31

Alprazolam *diazepam and midazolam have shorter duration of action*

Question 32

Most common route of admin for Diazepam?

Answer 32

IV

Question 33

Diazepam should not be given ________ because of?

Answer 33

IM slow absorption IM and painful due to propylene glycol

Question 34

Oral diazepam is contraindicated in _______

Answer 34

Cats **hepatic necrosis**

Question 35

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

Answer 35

Flumazenil IV

Question 36

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

Answer 36

Can cause paradoxical excitation

Question 37

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

Answer 37

C. Acepromazine

Question 38

Which class of neuroleptics is better at achieving muscle relaxation?

Answer 38

Benzos > phenothiazine derivatives

Question 39

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

Answer 39

Benzos 1. Alprazolam 2. Midazolam 3. Diazepam