Tranquilizers Flashcards
What is a synonym of tranquilizer?
Neuroleptics and sedatives
What is a tranquilizer?
Medicines that calm the animals and promote sleep but do not necessarily induce sleep, even in high doses. Cause analgesia, sedation, decreased sympathetic tone, euphoria.
What is the mechanism of action of tranquilizers?
They affect the CNS at the basal ganglia, hypothalamus, limbic system, and brain stem though acting with dopamine, α1-adrenergic, serotonin, opioid and GABA receptors
What are the therapeutic uses of tranquilizers?
CNS tranquilizers are used to calm the animals for easy handling as pre-anesthetic medications (allowing less general anesthetic)
anti-emetics
anti-allergic
What are the pharmacological effects of tranquilizers on the cardiovascular system, respiratory system, gastrointestinal system?
Are there adverse effects to tranquilizers?
various, depending on existing condition
What are the different categories of tranquilizers, and their mechanism of action?
What are some phenothiazine derivatives we use?
❖ Chlorpromazine ❖ Acepromazine (Ace) ❖ Promazine ❖ Triflupromazine
What are the pharmacological effects of phenothiazine derivatives?
- Effects are due to depression of brain stem and connections to the cerebral cortex * All phenothiazines decrease spontaneous motor activity (grooming, rearing, sniffing)
- The induced tranquilization is not accompanied by analgesia
What is Chlorpromazine? What is its pharmacologic effects? What are the adverse effects of chlorpromazine? When is its use contraindicated?
What is Acepromazine? What is its characteristics of the drug? When is it used? What is important to note about its potency? What are the routes of administration?
What is Promazine? What is its characteristics of the drug? When is it used? What is important to note about its potency? What are the routes of administration/ duration?
What is triflupromazine? What is it used for? What is important to know about its side effects?
How do benzodiazepines interact with gaba gated cl- channels? What does this cause within the membrane. What effect does it cause? How commonly prescribed is this medication
What are the types of commonly used benzodiazapines in veterinary medicine?
❖ Diazepam (ValiumR) ❖ Midazolam ❖ Clonazepam ❖ Zolazepam ❖ Alprazolam (xanax)
What are the types of commonly used benzodiazepines in veterinary medicine?
❖ Diazepam (ValiumR) ❖ Midazolam ❖ Clonazepam ❖ Zolazepam ❖ Alprazolam (xanax)
What are the pharmacologic effects of benzodiazepines? What are the uses of them?
When are benzodiazepines good alone as a tranquilizer?
Sheep, goats, neonatal foals
When must benzodiazepines be used with other drugs for sedative effect?
Horses, dogs, cats
Why are benzodiazepines used over other drugs?
Minimal cardiovascular effects
What is Valium ( or diazepam)? What is its pharmacokenetic properties? What is it used for? How can it be administered?
What are the adverse effects of giving diazepam?
How is clonazepam in comparison to diazepam?
❖ Clonazepam (stronger than diazepam but has shorter t1/2 )
How can midazolam be used to make it a neuroleptanalgesic?
❖ Midazolam (used in combination with an opioid in older dogs as a neuroleptanalgesic)
How is zolazepam used?
❖ Zolazepam (used exclusively with Tiletamine for anesthesia)(approved for animal use)
What animal should we not use alprazolam? What is its trade name? Why shouldnt we use it in that animal?
-> Do not use in dogs
-> Strong side effects in kidney and liver
-> Can accumulate in milk of lactating bitches and harm puppies.
-> Can harm pregnant animals
What is the MOA of alpha 2 adrenergic agonists?
Stimulate α2-adrenoreceptors causing decrease in NE release
How do a2-adrenergic agonists decrease NE release?
a2 agonists block presynaptic a2 receptors resulting in suppression of norepinephrine release -> this in turn causes a negative feedback loop further suppressing norepinephrine release
Where in the body are their a2 receptors?
heart and blood vessels
What are examples of a2 adrenergic agonists used as tranquilizers in veterinary medicine?
❖ Xylazine (cat, dog, horse, and wild animals)
❖ Medetomidine
❖ Detomidine (horses, IM and IV)
❖ Dexmedetomidine (most potent and selective α2-agonist in Vet Med)
❖ Clonidine
What are the pharmacologic effects of a2- adrenergic agonists? aa
What are uses for a2-adrenergic agonists? When should use be avoided?
What animals is xylazine hydrochloride most commonly used to sedate? Which animals is it not used for? How safe is it? What additional parameter should be monitored during the procedure?
Which a2 adrenergic agonist is more potent than Xylazine, but less potent than dexmedetomadine? What is dose dependent in this drug?
What alpha 2 adrenergic agonist is used primarily in horses aside from xylazine? What systems can it affect?
What is the most potent and most selective a2-adrenergic agonist available for use in vet med? What is it used for? What is the benefits of its use?
What is important to note about giving xylazine in horses? What is its contraindications/ when should it not be used in horses?
Do not use if patient has:
* Cardiac aberrations, renal insufficiency, hepatic impairment
* Epilepsy
* Combinations with ketamine should be use only in young and healthy animals
* Should not be given within the last month of pregnancy
* Immediate collapse, convulsions, and sudden death can occur in horse given Xylazine into carotid artery
* Xylazine inhibits insulin release in horses leading to hyperglycemia
- USE CAUTION DURING ADMINISTRATION DUE TO COLLAPSE CONVULSION AND DEATH THAT CAN OCCUR IF IT GOES INTO CAROTID ARTERY. JUGULAR VEIN IS SUPER CLOSE!
What is the MAO of Butyrophenone derivatives?
Block central dopamine D2 receptors
What are the 2 main types of Butyrophenone derivatives used in veterinary medicine?
- Azaperone
- Droperidol
What is azaperone used for usually? What can it be used for sometimes? What animal is it typically used in? When is it used? What receptors does it affect?
What is droperidol used for usually? What animal is it typically used in? When is it used? What receptors does it affect?
What drug should droperidol not be used with?
Epinephrine
What is the MOA of opioids?
Opioids: MOA: Stimulate opioid receptors [mu (µ), kappa (κ), and delta (Δ)]
What is the MOA of Benzodiazepines?
❑ Benzodiazepines (BZDs):
Bind to GABA receptors and enhance inhibitory effect of GABA
What is the MOA of phenothiazine derivatives?
Block dopamine and/or serotonin receptors
What are examples of opioids?
❖ Morphine
❖ Oxymorphine
❖ Fentanyl
❖ Carfentanil
What are the catecholamines?
Where are catecholamines produced?
Production: in the brain, nerve tissues, and adrenal glands
When are catecholamines released? What do they control? What are their receptors?
What are CNS stimulants ( analeptics?
Medicines that stimulate the brain, speeding up both mental and physical processes.
They increase energy, improve attention and alertness, and elevate blood pressure, heart rate and respiratory rate
What is the MOA of analeptics (CNS stimulants)?
MOA: Promotion of neurotransmission
Amphetamines enhance release of DA and NE onto the synaptic gap by blocking dopamine and/or NE reuptake .
What are the pharmacologic effects of CNS Stimulants (analeptics)?
What are the adverse effects of CNS Stimulants?
Adverse Effects: High doses may induce seizures
Hypertension, arrhythmias, and hyperventilation Hepatotoxicity
What is Doxapram? What is its MOA?
Doxapram: Is used most frequently in Veterinary Medicine as a CNS stimulant MOA: stimulates respiration through direct stimulation of the medullary respiratory centers and activation of carotid and aortic chemoreceptors
What is the Therapeutic uses of Doxapram? When is it not very helpful?
Therapeutic uses:
*To arouse animals from inhalant and parenteral anesthesia or anesthetic overdose
* Not effective in severely depressed neonate and is not a good substitute forendotracheal intubation and ventilation
What are the Adverse effects of doxapram?
Adverse effects:
* High doses may induce seizures
* Hypertension, arrhythmias, hyperventilation, and seizures may lead to respiratory alkalosis [a low level of carbon dioxide (CO2) in the blood]
What are signs and symptoms of accidental intoxication of analeptics in pets?
Signs and symptoms of toxicity in dogs:
* Agitation
* Increased heart rate
* Panting
* Tremors
* Increased body Temp
* Vomiting, Drooling
* Seizures
What is the medical use in humans of analeptics? What are some examples of medications used in this way?
Medical use in humans: ADD and narcolepsy. methylphenidate, atomoxetine (ADD), modafinil (narcolepsy), armodafinil, amphetamines, ecstasy
What are the pharmacological effects seen in pets that have accidental intoxication of CNS Stimulant medications?
Pharmacological effects: Simulant effects on mood and alertness, enhance energy, sociability, and sexual arousal
What are the side effects of CNS stimulant ingestion and intoxication in dogs?
What is cocaine? What is its MOA? What can it affect?
❖ Cocaine: Binds to dopamine transporter, blocking the removal of dopamine from the synapse.
- Dopamine accumulates in the synapse to produce amplified signal.
Affects also NE and serotonin neurotransmission
- illegal substance
What is MDMA? What is its MOA?
❖ MDMA (MethyleneDioxyMetamphetAmine): is an indirect serotonin agonist,
increasing the amount of serotonin released into the synapse
- illegal substance
