Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Introduction to Pharmacology > Tranquilizers, Sedatives & Stimulants > Flashcards

Tranquilizers, Sedatives & Stimulants Flashcards

1
Q

What are tranquilizers/neuroleptics/sedatives?

A

medicine that calms the animal and promotes sleep (not necessarily induce it) —> analgesia, sedation, decreased sympathetic tone, euphoria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the mechanism of action of tranquilizers/sedatives?

A

affect the CNS at the basal ganglia, hypothalamus, limbic system, and brain stem to act as CNS depressants through dopamine, adrenergic, serotonin, opioid, and GABA receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What 4 common therapeutic uses are tranquilizers/sedatives used for?

A
  1. calm animals for easy handling
  2. pre-anesthetic medications
  3. anti-ementics
  4. anti-allergic
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What pharmacological effects do tranquilizers/sedatives have on the cardiovascular, respiratory, and GI systems?

A

CARDIOVASCULAR: bradycardia, hypotension, tachycardia

RESPIRATORY: hypoventilation

GI: decreased motility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the 5 major tranquilizers/sedatives?

A
  1. phenothiazine derivatives
  2. benzodiazepines
  3. α2-adrenergic agonists
  4. butyrophenone derivatives
  5. opioids
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How do phenothiazine derivatives work?

A

block dopamine action and reduce serotonin action

bind to dopamine receptors (D1-like, D2-like) to keep dopamine from binding and causing CNS activation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are 4 common phenothiazine derivatives used as tranquilizers?

A
  1. Chlorpromazine
  2. Aceptromazine (ACE)
  3. Promazine
  4. Triflupromazine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

How do phenothiazine derivatives cause their pharmacological effects? What is important to consider with the induced tranquilization?

A

depress brainstem and connections to the cerebral cortex, which decrease spontaneous motor activity, like grooming, rearing, and sniffing

NOT accompanied by analgesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What was the first drug developed with specific antipsychotic or tranquilizer actions?

A

Chlorpromazine —> phenothiazine derivative

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What pharmacological effects does Chlorpromazine have on the CNS and cardiovascular system?

A

CNS:
- sedation
- blocks release of FSH and LH, increases plasma prolactin
- inhibit other hormones

CARDIOVASCULAR:
- reduction of contractility of myocardium
- arrythmias

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What effect does Chlorpromazine have on the CNS of dogs, but not cats?

A

antagonizing effect on apomorphine-induced emesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What adverse effect is common in dogs and cats on Chlorpromazine? Horses?

A

DOGS/CATS: extrapyramidal effects (movement disorders)

HORSES: hyperesthesia (increased response to stimuli), marked excitement, penile prolapse

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

In what 4 situations is it contraindicated to used Chlorpromazine as a tranquilizer?

A
  1. patients with hypovolemia or shock
  2. use carefully in animals with hepatic dysfunction
  3. HORSES: may cause severe CNS excitation/depression, seizures,or death
  4. DOGS: bradycardia (use atropine combination)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

How does Acepromazine (ACE) affect compare to Chlorpromazine?

A

10-20x more potent —> mild to moderate sedation of shorter duration, with a smaller concentration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Why is there a fair volume of distribution of Acepromazine in horses?

A

highly protein bound

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are 2 common situations where Acepromazine is used?

A
  1. tranquilizer-sedative for controlling intractable animals and immobilizing large animals
  2. used before surgery, examinations/procedures, or grooming sessions with nervous/excitable animals
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

How does Promazine compare to Chlorpromazine?

A

structurally related, but 10-13x less potent to produce mild to moderate sedation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

When is Triflupromazine commonly used? What makes it unique compared to other phenothiazine derivatives?

A

sedation + antiemetic

higher risk of side effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the mechanism of action of benzodiazepines (BZDs) as tranquilizers?

A

bind to GABA receptors to enhance the inhibitory effect of GABA —> hyperpolarization!

(GABA-agonist to activate GABA-gated Cl- channel)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What 5 common benzodiazepines (BZDs) are used as tranquilizers?

A
  1. Diazepam (Valium)
  2. Midazolam
  3. Clonazepam
  4. Zolazepam
  5. Alprazolam (Xanax)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are the 2 major pharmacological effects of benzodiazepines (BDZs)? What system do they have minimal effects on?

A
  1. depressed respiration
  2. muscular relaxation due to effects in spinal cord

minimal cardiovascular effect

22
Q

What are 3 major uses for benzodiazepines? How is the use of this drug different in other species?

A
  1. sedative, anti-anxiety, anti-panic
  2. anticonvulsant in all domestic species
  3. muscle relaxant when given with ketamine
  • BZDs alone are satisfactory in sheep, goats, and neonatal foals
  • NOT reliable in horses, dogs, or cats
23
Q

What is Diazepam most commonly used for? What else can it be used for?

A

benzodiazepine derivative used as a tranquilizer to sedate, reduce anxiety and panic, promote behavioral changes, and induce muscle relaxation

  • anticonvulsant
  • pre-anesthetic
  • increase appetite in cats
  • IV + opioids/anesthetics for general anesthesia
24
Q

What are 2 common adverse effects of Diazepam? 2 rare adverse effects?

A
  1. impaired coordination
  2. lethargy
  3. aggression and excitement
  4. hepatotoxicity in cats
25
Q

How do Clonazepam, Midazolam, and Zolazepam compare to Diazepam?

A

Clonazepam: stronger, but shorterd half-life

Midazolam: used in combination with opioids in older dos as a neuroleptanalgesic

Zolazepam: used exclusively with Tiletamine for anesthesia

26
Q

Why is Alprazolam (Xanax) not recommended for use in dogs?

A

strong liver and kidney effects and can be passed to offspring in milk/colostrum

27
Q

What are 3 common catecholamines? Where are they produced? When are they released?

A
  1. dopamine
  2. norepinephrine
  3. epinephrine

brain, nervous tissue, adrenal glands

in response to emotional or physcial stress —> fight or flight response (emergency stress)

28
Q

What do catecholamines do? What receptors do they bind to?

A

control metabolism, heart rate, blood pressure, and respiratory functions

G protein-coupled receptors: α- and β-adrenergic receptors

29
Q

How do α2-adrenergic agonists work as tranquilizers?

A

stimulate α2-adrenoreceptors, which inhibit NE release

30
Q

What are 5 common α2-adrenergic agonists used as tranquilizers?

A
  1. Xylazine (cats, dogs, horses, wild animals)
  2. Dexmedetomidine (Dexdomitor - most potent)
  3. Medetomidine
  4. Detomidine (horses)
  5. Clonidine
31
Q

What are 6 common pharmacological effects of α2-adrenergic agonists as tranquilizers?

A
  1. powerful sedation
  2. powerful analgesia
  3. skeletal muscle relaxation due to CNS effects
  4. emesis (cats)
  5. reduced GI motility and secretion
  6. hypertension followed by hypotension and bradycardia
32
Q

What are the 2 most common uses of α2-adrenergic agonists as tranquilizers? What combination should be avoided in geriatric, weak, and diseased animals?

A
  1. sedative, analgesic, immobilizing agent
  2. pre-anesthetic and anesthetic combination

Xylazine + Ketamine —> only use in young an healthy animals

33
Q

What is the most potent and selective α2-adrenergic agonist available for use in veterinary medicine?

A

Dexmedetomidine (Dexdomitor)

34
Q

Xylazine can be given IV in the jugular vein of horses. When do adverse effects happen?

A

immediate collapse, convulsions, and sudden death can occur is accidentally given in the carotid artery, which is very close to the jugular vein

35
Q

How can Xylazine cause hyperglycemia? What are 4 other adverse effects it has?

A

inhibits insulin release in horses

  1. cardiac aberrations
  2. renal insufficiency
  3. hepatic damage
  4. epilepsy
    (never give within the last month of pregnancy!)
36
Q

How do butyrophenone derivatives work as tranquilizers?

A

block dopamine D2 receptors

37
Q

What 2 butyrophenone derivatives are used as tranquilizers?

A
  1. Azaperone
  2. Droperidol
38
Q

What effect does Azaperone have? What receptors does it act on? What animals is it commonly used on?

A

sedative and antiemetic

potent D2 antagonist with some α1-adrenergic, muscarinic-cholinergic, and histamine receptor activity

pigs/swine as a pre-anesthetic before general anesthesia and C-sections or as a behavior modifying agent

39
Q

What receptors does Droperidol work on? How does it compare to the phenothiazine derivatives, Chlorpromazine and Promazine?

A

potent D2 antagonist with some histamine and serotonin antagonist activity

more potent in dogs

40
Q

What drug should Droperidol never be used with? How can it be used to induce neuroleptanalgesia? What is it most commonly used for?

A

epinephrine

Droperidol + fentanyl (opioid)

chemical restraining agent in aggressive dogs

41
Q

How do opioids work as tranquilizers? What 4 are commonly used?

A

stimulate opioid receptors (μ, κ, δ)

  1. Morphine - μ+++, κ+
  2. Oxymorphone - μ+++, κ+, δ+ (10x more potent)
  3. Fentanyl - μ+++ (100x more potent)
  4. Carfentanil - μ+++ (100,000x more potent)
42
Q

What are CNS stimulants (Analeptics)? What is their mechanism of action?

A

medicines that stimulate the brain, speeding up both mental and physical processes, which increases energy and metabolism, improves attention and alertness, and elevates blood pressure, heart rate, body temperature, and respiratory rate

promotes neurotransmission —> Amphetamines enhance the release of dopamine and norepinephrine onto the synaptic gap by blocking reuptake and allowing accumulation

43
Q

What are 3 common times CNS stimulants (Analeptics) are typically used? What are 3 possible adverse effects?

A
  1. in emergency situations during anesthesia
  2. decrease respiratory depressant effects of opiates and barbituates
  3. treat Attention Deficit Hyperactivity Disorder (ADHD) or hyperkinesis in dogs
  4. high doses may induce seizures
  5. hypertension, arrhythmias, hyperventilation
  6. hepatotoxicity
44
Q

What is the most frequently used CNS stimulant in veterinary medicine? What is its mechanism of action?

A

Doxapram

stimulates respiration through direct stimulation of the medullary respiratory centers and activation of carotid and aortic chemoreceptors

45
Q

What therapeutic use is Doxapram used for? When is it not usually effective?

A

to arouse animals from inhalant and parenteral anesthesia or anesthetic overdose

in severely depressed neonates
not a good substitute for ET intubation/ventilation

46
Q

What are 2 common adverse effects of Doxapram?

A
  1. high doses may induce seizures
  2. hypertension, arrythmias, hyperventilatio, and seizures can lead to respiratory alkalosis (low level of CO2 in the blood)
47
Q

What are 7 signs and symptoms of accidental ingestion and intoxication of CNS stimulants?

A
  1. agitation
  2. increased heart rate
  3. panting
  4. tremors
  5. increased body temperature
  6. vomiting, diarrhea
  7. seizures
48
Q

How are CNS stimulants used in humans? What pharmacological effect do they have?

A

treats ADD and narcolepsy —> methylphenidate, atomoxetine, modafinil, armodafinil (amphetamines, ecstasy)

stimulant effects on mood and alertness, enhances energy, sociability, and sexual arousal

49
Q

What are some common side effects on CNS stimulants in humans?

A
  • headache
  • insomnia
  • irritability, elation, agitation, confusion
  • palpitations, tachycardia
  • nasal stuffiness
  • decreased appetite
  • liver injury
  • addictive qualities
50
Q

What are 2 common CNS stimulants abused by humans? How do they work?

A
  1. COCAINE: binds to dopamine transporter, blocking the removal of dopamine from the synapse, allowing it to accumulate and produce an amplified signal (also affects NE and serotonin neurotransmission)
  2. MDMA: indirect serotonin agonist, increased the amount of serotonin released into synapse

Introduction to Pharmacology (39 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions