Week 5 - Tranquilizers Flashcards by Christine Parascandola

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

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

Immobilization?

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

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

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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

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Adverse Effects: _____, depending on ______ condition

various, existing

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Phenothiazine derivatives - MOA:

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

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Butyrophenone derivatives - MOA:

Block Dopamine (DA) receptors

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Benzodiazepines: MOA

Enhance inhibitory effect of GABA

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α2-adrenergic agonists: MOA

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

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Opioids: MOA

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

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Phenothiazine derivatives block _____ and/or ______ receptors

dopamine, serotonin

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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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Tranquilizers: Class of Phenothiazine Derivatives

 Chlorpromazine
 Acepromazine (Ace)
 Promazine
 Triflupromazine

KNOW THESE DRUG NAMES
Emphasis on the azine

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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 ________.

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

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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 _____

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

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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

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

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Chlorpromazine
Pharmacological effects - Cardiovascular

Effects on myocardium:
 Reduction of contractility
 Arrhythmias

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

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

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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

hepatic
severe CNS excitation/depression, seizures, death
bradycardia

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Chlorpromazine

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What is the color of Acepromazine (Ace)?

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

Yellow, odorless, bitter tasting water soluble powder

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How can Ace be administered?

IM or IV

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

10, 20, mild, moderate, shorter

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

protein, fair, horses,

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

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

Acepromazine (Ace)

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

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

Promazine

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

sedation, antiemetic, higher, phenothiazine

Triflupromazine

Tranquilizers: Benzodiazepines (BZDs)

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.

Tranquilizers: Benzodiazepine (BZD) derivatives

 Diazepam (ValiumR)  Midazolam  Clonazepam  Zolazepam

Tranquilizers: Benzodiazepine (BZD) derivatives Pharmacological Effects

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

Tranquilizers: Benzodiazepine (BZD) derivatives Uses

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

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: ?

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

Diazepam (Valium) - Adverse Effects

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

Clonazepam is stronger than _____ but has shorter ___ )

diazepam, t1/2

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

opioid, neuroleptanalgesic

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

Tiletamine

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.

Tranquilizers: α2- Adrenergic Agonists

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

Xylazine can be used in what species?

Dogs, cats, horses, and wild animals.

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

Horses, IV, IM

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, ______

sedation analgesia Skeletal Emesis GI motility, secretion Hypertension bradycardia

Tranquilizers: α2- Adrenergic Agonists Uses

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

Xylazine can lead to what side effects in horses?

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?

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

young, healthy

Xylazine should not be given within the ____ month of pregnancy

last

Tranquilizers: Butyrophenone derivatives

Butyrophenone derivatives: Block central dopamine D2 receptor

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

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

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

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

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

 Morphine  Oxymorphine  Fentanyl  Carfentanil

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

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

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

DA, NE, dopamine, NE

What is the MOA of CNS Stimulants (Analeptics)?

MOA: Promotion of neurotransmission

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

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

CNS Stimulants (Analeptics) - Doses

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

CNS Stimulants (Analeptics) - Adverse Effects

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

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

CNS stimulant

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

respiration, direct, medullary, respiratory, carotid, aortic

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 ______.

inhalant, parenteral, overdose, neonate, endotracheal, ventilation

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

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

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

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

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

methylphenidate, atomoxetine (ADD)

What medications are used in humans to treat Narcolepsy?

modafinil

Armodafinil, amphetamines, ecstasy are CNS ?

Stimulants

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

mood, alertness, energy, sociability, sexual

What are the side effects of CNS Stimulant ingestion?

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

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

dopamine, blocking, dopamine, Dopamine, NE, serotonin

Abused: Cocaine, MDMA: “ecstasy” MDMA

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

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