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Agonists
A drug that binds to a receptor and activates it, mimicking the action of the body’s own signaling chemical.
Binds to and stimulates target tissue.
Most anesthetic agents and adjuncts
Analgesic
is a medication used to relieve pain by inhibiting pain pathways.
antagonists
A drug that binds to a receptor and blocks or reverses another drug’s effects
Competitively binds to the target tissue but doesn’t stimulate
Example: naloxone, atipamezole, flumazenil
Anesthetic
Used to induce a loss of sensation with or without unconsciousness
Antiemetic
A type of medication used to prevent or treat nausea and vomiting, often administered during or after surgery.
Neuroleptanalgesia
A profound state of sedation and analgesia induced by simultaneous administration of an opioid and a tranquilizer or sedative
Sedation used for minor procedures
Used for the Induction of general anesthesia in dogs, but not used in cats or in young, healthy dogs
Pharmacodynamics
The study of how drugs affect the body, including mechanisms of action, therapeutic effects, and side effects.
Pharmacokinetics
The path the drug takes through the body.
Drug movement
Sedation
Suppression of brain activity and awareness to prevent movement; animals are usually unaware of their surroundings and are drowsy
Tranquilization
Decreases anxiety without causing excessive sedation or drowsiness, animals are usually aware of their surroundings but do not appear to care
Partial agonists
Are opioids only
Partially stimulates opioid receptors
example: Buprenorphine
Agonist-Antagonists
Binds to more than one receptor, simultaneously stimulates one and blocks another.
Example: Butorphanol
Analgesia
Creates the absence of pain
Just because an animal is under anesthesia does not mean the perception of pain is eliminated
The most general anesthetics are not analgesics
Must provide analgesic per-,intra, and postoperatively
Inhalation anesthetics
Isoflurane, sevoflurane, and desflurane ( halogenated compounds) are used for inducing and maintaining anesthesia during surgical procedures.
Halogenated organic compounds
Isoflurane and sevoflurane are the most commonly used agents in this class
They are liquid at room temperature and become vaporized in oxygen that flows through the vaporizer
What are the effects of Halogenated organic compounds?
CNS effects
Has dose-related reversible CNS depression
Can cause hypothermia
Cardiovascular system effects
Depresses cardiovascular function
causes vasodilation
Respiratory system effects
has a dose-dependent ventilation depression
What is the mode of action for Halogenated organic compounds
The liquid anesthetic is vaporized and mixed with oxygen gas
The mixture is delivered to the patient via a mask or endotracheal tube
The mixture travels to the lungs (alveoli) and diffuses into the bloodstream
Diffusion rate is dependent on concentration gradient ( alveoli/ capillary and lipid solubility)
The anesthetic delivery to tissues ( brain) is dependent on the blood supply
What are the important properties of inhalational anesthetics?
The vapor pressure
partition coefficient
Minimum alveolar concentration ( MAC)
Isoflurane MAC%, Blood gas partition coefficient, and Vapor pressure STP
MAC %: 1.3-1.63%
Blood-Gas partition Coefficient: 1.46.
Vapor pressure STP: 240
This indicates that Isoflurane has a minimum alveolar concentration of 1.3-1.63%, meaning it is effective at that concentration for 50% of patients to not respond to surgical stimuli. The blood-gas partition coefficient of 1.46 suggests it requires moderate time to achieve equilibrium in the bloodstream.
Sevoflurane MAC% , Blood gas partition coefficient, and Vapor pressure STP:
MAC %: 2.34-2.58%
Blood gas partition: 0.68
Vapor pressure STP: 160
This indicates that Sevoflurane has a minimum alveolar concentration of 2.34-2.58%, meaning it is effective at that concentration for 50% of patients to not respond to surgical stimuli. The blood-gas partition coefficient of 0.68 suggests it achieves equilibrium in the bloodstream relatively quickly.
Vapor pressure
In a closed container, a liquid will reach equilibrium with its gaseous form. The pressure exerted by the gas is the vapor pressure.
It determines how readily an inhalation anesthetic will evaporate in the anesthetic machine vaporizer
It is temperature- and anesthetic-agent dependent
Vapor pressure determines vaporizer types
High vapor pressure Agents are volatile agents that are delivered from a precision vaporizer to control the delivery concentration
All precision vaporizers are made to deliver only one specific agent
Isoflurane, sevoflurane, desflurane, and halothane
Low vapor pressure
Nonvolatile agents are not used in vet med
Delivered from a non-precision vaporizer
blood-gas partition coefficient
The measure of the solubility of an inhalation anesthetic in blood as compared to alveolar gas
indicates the speed of induction and recovery for an inhalation anesthetic agent
A low blood-gas partition coefficient
agent is less soluble in blood than alveolar gas
faster expected induction and recovery
What does the blood-gas Partition coefficient determines?
It determines the clinical use of the anesthetic agent
Questions to ask when using an anesthetic agent
Maintenance: how fast will the anesthetic depth change in response to changes in the vaporizer setting
Recovery: how long will the patient will sleep after anesthesia and how quickly the patient will recover from anesthesia.
How long does it take to see a change in a patient when using Isoflurane
it can take 10 minutes to see a change in a patient when using ISO
How long does it take to see a change in the patient when using Sevoflurane
Sevo takes much less time than ISO to see a change in a patient
A sevo patient wakes up faster
The lower the MAC the more BLANK the has is?
potent the anesthetic
Minimum Alveolar concentration (MAC)
The potency of the drug
The minimum inhalant concentration required to keep 50% of patients under anesthesia with the inhalant alone
The lower the MAC of an anesthetic is, the more potent the anesthetic agent, and the lower the vaporizer setting
What can MAC be altered by
It can be altered by age, metabolic activity, body temperature, disease, pregnancy, obesity, and other agents present
is MAC lower in dogs than in cats
yes it is lower in dogs than cats
Isoflurane MAC
1.3% to 1.63%
Why is Sevo faster than ISO
it has a lower blood-gas partition coefficient, meaning it dissolves less in the blood and moves more rapidly into and out of the brain
What are some adjuncts that lower the MAC
Acepromazine
Dexmedetomidine
ketamine
opioids
lidocaine
Gabapentin
trazodone
Injectable anesthetics
Can produce unconsciousness
Don’t provide analgesia
must be used with other agents to produce the complete effects of general anesthesia
Administered to effect IV
These are: propofol, etomidate, alfaxalone, and barbiturates
Propofol
an ultra-short-acting, nonbarbiturate anesthetic
commonly used to induce anesthesia in small animals
Other uses: IV bolus and CRI to treat status epilepticus in dogs and cats
Properties of Propofol
It is a highly fat-soluble drug
Its potency increases in animals with low plasma protein levels
Onset of action: 30- 60 seconds
Duration of action: 5- 10 minutes
complete recovery: 20 -30 minutes
When pushing propofol, wait 30- 60 seconds to prevent overdose in the patient
Propofol effects on the Central Nervous system
Has dose-dependent depression from sedation to general anesthesia
Transient excitement and muscle tremors (induction)
paddling, muscle twitching, nystagmus, opisthotonos
nystagmus: rapid involuntary eye movement
opisthotonos: a severe, involuntary spasm where an animal's head, neck, and back are rigidly arched backward
Propofol effects on the Cardiovascular system
Causes cardiac depression and transient hypotension
Propofol effects on the respiratory system
depressant with possible apnea
The use of propofol
Titrate IV slowly over 1-2 minutes to effect
IM produces mild sedation and ataxia only ( hurts when given IM)
Dose depends on premedication’s
It is a highly protein-bound drug and should not be used in patients with low albumin
Should not be used in hypoproteinemic animals
May cause excitement if given too slowly
Alfaxalone
Short duration of action
Wide margin of safety
Use IV for induction and maintenance anesthesia
Use IM in cats for deep sedation/light anesthesia
It is a Schedule IV controlled substance in the US
Not safer for cardiac patients
Alfaxalone effects on the central nervous system
Dose-dependent CNS depression
Alfaxalone effects on the cardiovascular system
heart rate, rhythm, blood pressure, and cardiac output are minimally affected
Alfaxalone’s effects on the respiratory system
apnea, especially if used with inhalants
Apnea: a temporary pause in breathing that lasts for at least 10 seconds
Alfaxalone’s effects on the musculoskeletal system
muscle relaxation with no excitement or twitching
Etomidate
Short-acting intravenous anesthetic agent
Minimal effect on the cardiovascular system
Administered only IV; painful on injection
adverse effects
vomiting
Muscle contractions minimized by premedication and slow administration
Not commonly used
Needs to be given over a long period of time, like an IV pump
Barbiturates
large class of controlled drugs
used as a general anesthetic declined due to new drug developments
has specific uses
short-acting pentobarbital (Barbiturate)
primary agent in euthanasia injectables
induce and maintain general anesthesia in lab animals
treat status epilepticus in small animals
Long-acting phenobarbital (Barbiturate)
seizure control
Dissociative anesthetics
Agents that induce dissociative anesthesia
characterized by, among other things, a cataleptoid state
unique CNS, cardiac, and respiratory effects
Ketamine hydrochloride, tiletamine (in telazol)
Guaifenisin
What are Dissociative anesthetics mode of action
Disrupts nerve transmission in some brain sections
Selective stimulation in parts of the brain
Decreases windup through NMDA inhibition
Induces a trance-like state
Animal appears awake
immobile and unaware of surroundings
Ketamine
Dissociative anesthetics
Peak action: 1-2 minutes after IV injection
Duration of action: 20-30 minutes
Metabolized:
Primarily metabolized in the liver or excreted unchanged in urine
Avoid use in animals with liver or kidney disease
Dissociative effects on the CNS
Cataleptoid state ( a condition that simulates or resembles catalepsy.)
intact reflexes
central dilated pupil
muscle tone
normal to muscle rigidity
counteract with concurrent tranquilizer
analgesia
potential for bizarre behavior
may produce nystagmus- more common in cats
catalepsy
a state of unresponsiveness and immobility, resembling a trance, where reflexes may remain intact.
Dissociative effects on the cardiovascular system
Stimulation of the sympathetic nervous system
Increase in HR
Increased cardiac output
Increased mean blood pressure
Puts a lot of strain on the cardiovascular
May decrease inotropy
Screen patients for heart disease
Can cause cardiac arrhythmias
Dissociative Effects on the respiratory system
Respiratory depression is usually insignificant
Apneustic respiration at a higher dose ( holding their breath)
Overdose may cause severe respiratory depression or arrest
Significant increase in salivation ( can cause airway obstruction)
Use of dissociative anesthetics
Administration: IM, IV, SQ or oral
Used in combination with other agents
Anesthetic induction for intubation
Chemical restraint/immobilization for short procedures
pain control
No effective reversal agent
What are the objectives of preanesthetic medication?
Reduce FAS
minimize adverse drug effects
reduce the dose of concurrent drugs
smoother anesthetic induction and recovery
analgesia
muscle relaxation
Allows for less propofol to be given
Acepromazine
Phenothiazines
Onset: 15 minutes IM ( takes too long to work)
Peak: 30-60 minutes
Duration: 4-8 hours, but highly variable in how long the sedation lasts; not good for wanting a patient to wake up quickly after a procedure
Can be administered IV or IM
There is no reversal agent
Metabolized by the liver
Will slowly cross the placenta
Acepromazine effects on the central nervous system
Calming effect
reluctance to move
decreased interest in surroundings
sedation less pronounced in cats
Acepromazine effects on the cardiovascular system
Peripheral vasodilation that leads to hypotension, increased Heart rate, and hypothermia
Acepromazine causes what to the veins
Vasodilation leading to increased blood flow and decreased blood pressure.
Acepromazine effects on the respiratory system
worsens the depressive effect of the other drugs
Acepromazine effects on the GI system
antiemetic
What does Acepromazine do to the spleen?
Acepromazine causes splenic engorgement, which can lead to increased blood volume in the spleen and potential effects on overall circulatory dynamics.
Causes a decrease in PCV
Acepromazine effects
Causes variable sedation
Vasodilation that leads to hypotension
anti-arrhythmic
anti-emetic
big spleen
There is no reversal
Benzodiazepines
A group of minor tranquilizers
Diazepam
Zolazepam- a combination drug
midazolam
has a rapid onset of action
A short duration of action
Is a DEA Schedule IV controlled substance
Benzodiazepines effects on the central nervous
has a calming and anti-anxiety effect only in old or ill patients
Disorientation and excitement in young and healthy dogs
Dysphoria and aggression in cats
Anticonvulsant use with animals having seizures ( does not prevent seizures)
Benzodiazepines effects on the cardiovascular and respiratory systems
has minimal effect with a high margin of safety
Benzodiazepines effects on the skeletal muscle
causes skeletal muscle relaxation
Benzodiazepines is a BLANK general anesthetic
a potentiate
allows for larger doses
Benzodiazepines is A BLANK for cats and ruminants
Appetite stimulant
What are the uses of Diazepam
Not a water-soluble medication; can’t be combined in a syringe with other drugs
Ketamine can be the exception to this
Commonly used with ketamine to induce anesthesia in small animals and horses
has to be administered IV slowly, or it can be given rectally for seizures
oral diazepam in cats can cause liver failure
IM administration can cause irritation and abscess
What are the uses for Midazolam?
It is water-soluble, so it can be mixed with other medications
Administered IM or SC
Excellent sedative for swine, ferrets, rabbits, and birds
Excellent per-med when combined with opioids in older, compromised patients
Causes excitement in younger patients
Summary of Benzodiazepines
Is a mild sedative
heart safe
anticonvulsant
Causes hyperactivity in young patients
Reversible with flumazenil
Alpha2-adrenoceptor agonists
A non-controlled agent
acts on the alpha receptors of the sympathetic nervous system
Decreases release of norepinephrine
No fight-or-flight response
Metabolized in the liver; excreted in the urine
rapid sedation that has a 1- 2 hour duration
duration of effect typically longer in dogs than in cats
readily reversed with alpha-2 antagonists
Medications that are in the alpha 2- agonists class
Dexmedetomidine ( Dexdomitor)
Xylazine ( rompun,anaSed)
Medetomidine-vatinoxan (Zenalpha)
detomidine (Dormosedan)
Romifidine ( Sedivet)
The effects of Alpha 2 agonists on the cardiovascular system in the early phase
Dose-dependent vasoconstriction and hypotension ( causes a dramatic vasoconstriction of everything)
bradycardia
Cardiac arrhythmias, such as 2nd-degree AV block, can reduce cardiac output due to decreased heart rate.
The effects of Alpha 2 agonists on the cardiovascular system in the late phase
Decreased cardiac output
hypotension and further bradycardia
The effects of Alpha 2 agonists on the Central nervous system
Has a dose-dependent sedative effect
The analgesia is short-acting (Dexdom should not be used by itself, as it does not provide proper pain relief)
hypothermia
Aggressive behavior ( alpha-1) does not happen often
Why should dexdom be used with other medications
to provide adequate pain relief and prevent inadequate analgesia.
The effects of Alpha 2 agonists on the respiratory system
dose-dependent depression
More severe if given with other drugs
What are some other effects of alpha 2 agonists
causes MAC-reduction
muscle relaxation
vomiting: immediate response seen in cats and dogs, but seen more often when given IM or SQ
How to used Dexmedetomidine
2 to 5 mcg/kg when used as part of a multimodal protocol
Can be given IM or IV
Likely to cause vomiting if given SQ
Dexmedetomidine works synergistically with opioids, reducing the dose requirements of each ( allows for much smoother sedation)
Needs to be avoided in cardiac patients, geriatric, diabetic, pregnant, neonatal, or profoundly ill patients.
Alpha 2- antagonists
Reverses all effects of alpha-2 agonists
Beneficial and detrimental effects
zenalpha is a combo agonist-antagonist ( the medetomidine can still be reversed)
Administered IM
What are the effects of an overdose of an Alpha2-antagonists
Neurological: excitement and muscle tremors
Cardiovascular: hypotension and tachycardia
Gastrointestinal: salivation and diarrhea
a summary of Alpha2 effects
Sedation
bradycardia
emetic
vasoconstriction
some analgesia
reversible
Opioids
Produce analgesia and sedation effects
Anesthetic induction when combined with other drugs
classified as agonists, partial agonists, agonists-antagonists, or antagonists
Sevoflurane is expected to provide a more rapid anesthetic induction than isoflurane due to its lower ________________.
blood-gas partition coefficient
Which of the following statements is INCORRECT?
A morbidly obese dog will require more anesthetic per unit body weight than a dog of the same breed with a healthy body condition score.
NMDA receptor antagonist used to induce dissociative anesthesia
Ketamine
Sedative medication that is contraindicated in abdominal surgery due to causing splenomegaly
acepromazine
Local anesthetic also used to treat ventricular arrhythmias
lidocaine
Fast-acting injectable anesthetic delivered in a lipid emulsion
Propofol
Commonly used inhalant anesthetic agent known for rapid induction and recovery
sevoflurane
Potent sedative that cause vasoconstriction and bradycardia in its initial phase
dexmedetomidine
Which physical parameter is assessed by lightly tapping the skin near the medial or lateral canthus?
palpebral reflex
When performing chest compressions using the thoracic pump method, the chest should be compressed to ________________________ .
1/3 to 1/2 the width of the chest