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Intro to Pharmacology > Week 5 - Tranquilizers > Flashcards

Week 5 - Tranquilizers Flashcards

1
Q

Tranquilizers, Neuroleptics, and Sedatives are Medicines that _____ the animals and promote _____ but do not necessarily ______ sleep, even in ____ doses. Cause (4)?

A

calm, sleep, induce, high
analgesia, sedation, decreased sympathetic tone, euphoria

Immobilization?

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2
Q

Mechanism of action: affect the CNS at the (4)
CNS depressants acting through ?

A

basal ganglia, hypothalamus, limbic system, and brain stem
dopamine, α1-adrenergic, serotonin, opioid and GABA receptors

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3
Q

Therapeutic Uses: CNS tranquilizers are used to calm the animals for easy handling
as pre-anesthetic medications (allowing less general anesthetic)
anti-emetics
anti-allergi

A
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4
Q
A
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5
Q

Adverse Effects: _____, depending on ______ condition

A

various, existing

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6
Q

Phenothiazine derivatives - MOA:

A

Block Dopamine (DA) action and reduce action of serotonin.

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7
Q

Butyrophenone derivatives - MOA:

A

Block Dopamine (DA) receptors

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8
Q

Benzodiazepines: MOA

A

Enhance inhibitory effect of GABA

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9
Q

α2-adrenergic agonists: MOA

A

Stimulate α2-adrenoreceptors, which inhibit Norepinephrine (NE)/Noradrenaline release

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10
Q

Opioids: MOA

A

Stimulate opioid receptors [mu (μ), kappa (κ), and delta (Δ)

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11
Q

Phenothiazine derivatives block _____ and/or ______ receptors

A

dopamine, serotonin

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12
Q
A

Dopamine and serotonin are “happy” hormones. Produce similar feelings of wellbeing - alert, focused, motivated. We need to block the action of receptors to induce calmness. Pre-synaptic releases dopamine into cleft and then binds to DA receptor (agonists do the same thing). BUT, Dopamine antagonists have a different shape and therefore block the action of the receptor. Stops NT from binding to each receptor and sending a signal so we get a sedative effect.

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13
Q

Tranquilizers: Class of Phenothiazine Derivatives

A

 Chlorpromazine
 Acepromazine (Ace)
 Promazine
 Triflupromazine

KNOW THESE DRUG NAMES
Emphasis on the azine

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14
Q

Pharmacological Effects of Phenothiazine Derivatives
Effects are due to _______ of brain ____ and connections to the _______ ______.
* All phenothiazines decrease ______ _____ activity (3)
* The induced tranquilization is not accompanied by ________.

A

depression, stem, cerebral cortex, spontaneous motor, grooming, rearing, sniffing
analgesia

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15
Q

Chlorpromazine was the first drug developed with specific ______ or ______ action (year?)
* Appearance: _____ to slightly ______, _____, tasting crystalline _____
* Administration: ___ or ___, well absorbed and distributed throughout the body
* Rapidly absorbed after ____, undergoes extensive metabolism in the ____ and _____

A

antipsychotic, tranquilizer, 1950, white, creamy, odorless, bitter, powder, IM, IV, PO, liver, kidney

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16
Q

Chlorpromazine causes ______. When given IV gives –> ___-___ min
 Antagonizing effect on _______- induced ___ in dogs but not cats
 Endocrine effects: blocking release of ____ and ___, in plasma ____
 May ____ release of other hormones

A

sedation, 10-20 , apomorphine, emesis, FSH, LH, prolactin, inhibit

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17
Q

Chlorpromazine
Pharmacological effects - Cardiovascular

A

Effects on myocardium:
 Reduction of contractility
 Arrhythmias

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18
Q

Chlorpromazine Adverse Effects
Produces extrapyramidal signs in ___ and ___, such as ?
* May cause _______ and marked excitement in _____ and may cause _____ in the penis

A

cats, dogs, tremors, muscle contractions, hyperethesia, horses, prolapse

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19
Q

Chlorpromazine Contraindication (and other drugs in this class)
In patients with hypovolemia or shock, carefully used in animals with _____ dysfunction
* In horses, may cause ?
* In dogs, combination with atropine is recommended to overcome _______ effect

A

hepatic
severe CNS excitation/depression, seizures, death
bradycardia

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20
Q
A
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21
Q

Chlorpromazine

A
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22
Q

What is the color of Acepromazine (Ace)?

Does Ace have an odor? What does it taste like?

A

Yellow, odorless, bitter tasting water soluble powder

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23
Q

How can Ace be administered?

A

IM or IV

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24
Q

Ace is __-___ times more potent than chlorpromazine, produces ___ to ____ sedation of ____ duration.

A

10, 20, mild, moderate, shorter

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25
Q

Ace is highly ___ bound and has a __ volume of distribution in ___.

A

protein, fair, horses,

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26
Q

It is used as a _____- _____ for controlling intractable animals and to ______ large animals. It is also used before _____ or veterinary ______ and procedures or _____ sessions with ______/_______ animals

A

tranquilizer, sedative, immobilize, surgery, examinations, grooming, nervous, excitable

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27
Q

Acepromazine (Ace)

A
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28
Q

Promazine
* Structurally related to ________
* Administration: ____ and ____
* 10-13 times less ______ than chlorpromazine, produces mild to moderate _______
* Duration is ____-dependent and can vary within __-___ hr

A

chlorpromazine, IM, IV, potent, sedation, dose, 4-6

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29
Q

Promazine

A
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30
Q

Triflupromazine is used occasionally in animals for ______ and as an ______ agent. Has ______ risk of side effects than other _______ derivatives

A

sedation, antiemetic, higher, phenothiazine

31
Q

Triflupromazine

A
32
Q

Tranquilizers: Benzodiazepines (BZDs)

A

GABA NT binds to site of GABA-A receptor.
Ligand gated ion channels allow for hyper-polarization of the membrane and inhibition of action potential happens.
Gaba agonist does the same thing as GABA NT.

33
Q

Tranquilizers: Benzodiazepine (BZD) derivatives

A

 Diazepam (ValiumR)
 Midazolam
 Clonazepam
 Zolazepam

34
Q

Tranquilizers: Benzodiazepine (BZD) derivatives
Pharmacological Effects

A

Minimal cardiovascular effects = good
* Depressed respiratory effects
* Muscular relaxation due to effects in spinal cord

35
Q

Tranquilizers: Benzodiazepine (BZD) derivatives Uses

A

As anticonvulsants in all the domestic species
* As muscle relaxant when given together with ketamine
* BZD alone: satisfactory in sheep, goats, neonatal foals
NOT reliable in horses, dogs, or cats

36
Q

Diazepam (ValiumR)
* PK: highly ____ soluble, widely distributed throughout the body, crosses _______, ____ metabolism
* Used in Vet Med to ?
* Also used as an anticonvulsant (dogs and horses)
* Can be prescribed to what species?
* Use as ______ in horses
* Can be used ____ in combination with ______ or _____ for general anesthesia
* Administration: ?

A

lipid, BBB, liver
sedate, reduce anxiety, panic, promote behavioral changes, or induce muscle relaxation
dogs, cats, reptiles, sheep, horses, and goat scan

sedative, IV, opioids, anesthetics

oral, IV, or rectal

37
Q

Diazepam (Valium) - Adverse Effects

A

Impaired coordination Alprazolam (Xanax)
* Lethargy
* Rare: aggression and excitement
* Rare: hepatotoxicity in cats

38
Q

Clonazepam is stronger than _____ but has shorter ___ )

A

diazepam, t1/2

39
Q

Midazolam is used in combination with an ____ in older dogs as a __________.

A

opioid, neuroleptanalgesic

40
Q

Zolazepam is used exclusively with _____ for anesthesia.(approved for animal use)

A

Tiletamine

41
Q

In pre-synaptic and post-synaptic and nerves
Focus more on pre-synaptic
alpha2 agonists in pre-synaptic nerve; negative feedback mechanism in place which suppresses releases adrenaline goes down.

A
42
Q

Tranquilizers: α2- Adrenergic Agonists

A

 Xylazine (cat, dog, horse, and wild animals)
 Medetomidine
 Detomidine (horses, IM and IV)
 Dexmedetomidine (most potent and selective α2-agonist in Vet Med)
 Clonidine

43
Q

Xylazine can be used in what species?

A

Dogs, cats, horses, and wild animals.

44
Q

Detomidine can be used in ______ and is administered ___ or ___.

A

Horses, IV, IM

45
Q

Tranquilizers: α2- Adrenergic Agonists - Pharmacological Effects
Powerful ______
* Powerful _____ (she emphasized this)
* _____ muscle relaxation due to effects in the CNS
* ______ (cats, less in dogs)
* Reduced both ___ ____ and ____ (control of diarrhea)
* _______ followed by hypotension, ______

A

sedation
analgesia
Skeletal
Emesis
GI motility, secretion
Hypertension
bradycardia

46
Q

Tranquilizers: α2- Adrenergic Agonists
Uses

A

As a sedative, analgesic, and immobilizing agent
* As a pre-anesthetic, and as a part of the anesthetic combination
* Xylazine-ketamine combo should be avoided in geriatric, weak, and diseased small animals

47
Q
A
48
Q

Xylazine can lead to what side effects in horses?

A

Contraindications:
* Cardiac aberrations, renal insufficiency, hepatic impairment
* Epilepsy
* Immediate collapse, convulsions, and sudden death can occur in horse given Xylazine into carotid artery
* Xylazine inhibits insulin release in horses leading to hyperglycemia
* Accidental? Jugular?

49
Q

Xylazine with ketamine should be use only in _____ and _________ animals

A

young, healthy

50
Q

Xylazine should not be given within the ____ month of pregnancy

A

last

51
Q

Tranquilizers: Butyrophenone derivatives

A

Butyrophenone derivatives: Block central dopamine D2 receptor

52
Q

Azaperone is a _______ ______ with ____ and _____ effects
* Potent ___ antagonist with some (3) receptors
* Used as a __-________ agent prior to general _____ or ______ section.
* Occasionally used as a _____ modifying agent
* Mainly used in ___ and ___

Block ______ pathway

A

Butyrophenone neuroleptic, sedative, antiemetic, D2, α1-adrenergic, muscarinic-cholinergic and histamine, pre-anesthetic, anesthesia, caesarean, behavior, pigs, swine,
dopamine

53
Q

Droperidol is a potent ___ antagonist with some _____ and _____ antagonist activity
* More potent than _______ and ______ in dogs
* Should not be used with _____
* Used in combination with ____ (opioid) for induction of _______
* Chemical restraining agent in _______ ___

Block ______ pathway

A

D2, histamine, serotonin, chlorpromazine, promazine, epinephrine, fentanyl, neuroleptanalgesia, aggressive, dogs, dopamine

54
Q

Opioids: MOA: Stimulate opioid receptors [mu (μ), kappa (κ), and delta (Δ)]

Name the common Opiods

A

 Morphine
 Oxymorphine
 Fentanyl
 Carfentanil

55
Q

CNS Stimulants (_________) are medications that stimulate the brain, speeding up both _______ and ______ processes.
They increase ______, improve _______ and ________, and elevate _______ ________, _______ rate and ______ rate

A

Analeptics, mental, physical, energy, attention, alertness, blood pressure, heart, respiratory

56
Q

Amphetamines enhance release of ___ and ____ onto the synaptic gap by blocking _____ and/or ___ reuptake

A

DA, NE, dopamine, NE

57
Q

What is the MOA of CNS Stimulants (Analeptics)?

A

MOA: Promotion of neurotransmission

58
Q

CNS Stimulants Analeptics - Pharmacological Effects
CNS stimulants are used primarily in _______ situations during anesthesia or to decrease the _______ _______ effects of opiates and barbiturates; to treat _____ or _______ in dogs

A

emergency, respiratory depressant, Attention Deficit Hyperactivity Disorder (ADHD), hyperkinesis

59
Q

CNS Stimulants (Analeptics) - Doses

A

1-5 mg/kg, IV, in dogs and cats
0.5 -1 mg/kg. IV in adult horses
0.02-0.05 mg/kg/min, IV in young animal

60
Q

CNS Stimulants (Analeptics) - Adverse Effects

A

Adverse Effects: High doses may induce seizures
Hypertension, arrhythmias, and hyperventilation
Hepatotoxicity

61
Q

Doxapram: Is used most frequently in Veterinary Medicine as a _____ ______

A

CNS stimulant

62
Q

Doxapram MOA:
MOA: stimulates ______ through ____ stimulation of the _______ ________ centers and activation of _____ and _____ chemoreceptors

A

respiration, direct, medullary, respiratory, carotid, aortic

63
Q

Doxapram Therapeutic uses:
To arouse animals from _____ and ______ anesthesia or anesthetic ________. Not effective in severely depressed _______ and is not a good substitute for ________ intubation and ______.

A

inhalant, parenteral, overdose, neonate, endotracheal, ventilation

64
Q

Doxapram Adverse Effects
High doses may induce _____
* (4) –> may lead to respiratory alkalosis [a?]

A

seizures, Hypertension, arrhythmias, hyperventilation, and seizures , low level of carbon dioxide (CO2) in the blood

65
Q

Accidental Ingestion and Intoxication in Pets
Signs and symptoms of toxicity in dogs

A

Agitation
* Increased heart rate
* Panting
* Tremors
* Increased body T
* Vomiting, Drooling
* Seizures
Accidental Ingestion and Intoxication in Pets

66
Q

What medications are used in humans to treat ADD?
Medical use in humans: ADD and narcolepsy.
modafinil (narcolepsy),

A

methylphenidate, atomoxetine (ADD)

67
Q

What medications are used in humans to treat Narcolepsy?

A

modafinil

68
Q

Armodafinil, amphetamines, ecstasy are CNS ?

A

Stimulants

69
Q

The pharmacological effects of CNS Stimulants:
Stimulant effect ____ and _____, enhance ___, _____, and ______ arousal

A

mood, alertness, energy, sociability, sexual

70
Q

What are the side effects of CNS Stimulant ingestion?

A

Side Effects:
* Headache, insomnia, irritability, elation, agitation, confusion, palpitations, tachycardia,
nasal stuffiness, and decreased appetite
* Liver injury
* Addictive qualities

71
Q

Abused: Cocaine, MDMA: “ecstasy”
Cocaine binds to ____ transporter, _______ the removal of _____ from the synapse. ______ accumulates in the synapse to produce amplified signal. Affects also ____ and ______ neurotransmission

A

dopamine, blocking, dopamine, Dopamine, NE, serotonin

72
Q

Abused: Cocaine, MDMA: “ecstasy”
MDMA

A

(MethyleneDioxyMetamphetAmine): is an indirect serotonin agonist,
increasing the amount of serotonin released into the synapse

73
Q
A
74
Q

What are the side effects and clinical signs of Cocaine/Crack users?

A

Intro to Pharmacology (31 decks)

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