Preanesthetic medication Flashcards

(150 cards)

1
Q

Reasons for premed

A

To calm or sedate an excited, frightened or viscous animal
To minimize adverse effects of concurrently administered drugs
To reduce the required dose of concurrently administered agents
To produce smoother anesthetic inductions and recoveries
To decrease pain and discomfort before, during, and after surgery
To produce muscle relaxation

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2
Q

Pre-emptive analgesia is and why to utilize it

A

To provide analgesia before tissue injury, including surgery (and after)
Reasons to utilize pre-emptive analgesia
More effective analgesia and takes less medication than treating pain that already exists
Limiting pain before it occurs allows lowering overall amount of anesthetic required and therefore decreases drug risks
Speeds up recovery times

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3
Q

Considerations for selection of preanesthetic protocol

A

Species and breed
Temperament
Patient history
Physical status of patient
Availability and compatibility of drugs
Route available in that patient (PO,IV,IM,SQ)
Comfort with specific drugs
Procedure
Facilities available

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4
Q

Administering Premedication:

A

In general, time to effect of preanesthetic:
30-40 min before induction of SQ
10-20 min before induction if IM
3-10 minutes if given IV
Effects will be more pronounced and faster
More pronounced side-effects
Often requires an IV catheter
Patient to be left in quiet for drugs to have full effect
Excited patients require a higher dose of drug for equivalent sedation

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5
Q

Assessing sedation

A

Parasympathetic signs
prolapsed 3rd eyelid, drooling, constricted pupils
Ataxia
do not leave unattended; anxiety
Recumbency
Decrease in HR, RR, (BP)
Certain drugs can relax inhibitions and animals can become aggressive or exhibit other unusual behaviours

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6
Q

Preanesthetic precautions

A

Overdose can result in sufficient CNS depression to cause death
In very sick animals, recommended doses can cause lethal overdose
Horses that develop ataxia as a result of sedation can become anxious and enter “fight or flight”
Brachycephalic breeds should be continuously monitored under sedation
Relaxation of the elongated soft palate can cause the airway to close

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7
Q

3 main groups of premedications and would you mix them

A

Anticholinergics
Tranquilizers and sedatives
Phenothiazines
Benzodiazepines
Alpha 2-adrenoceptor agonists (alpha2-agonists)
Opioids
Usually used in combination of 2 or more of the above drugs
DO NOT MIX TWO OR MORE DRUGS UNLESS YOU HAVE A RELIABLE EVIDENCE IT IS SAFE TO DO SO!!

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8
Q

Anticholinergics work on what system and are they controlled

A

PSN and non controlled drug

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9
Q

Indications of anticholinergics

A

To counter the parasympathetic effects of many of the other drugs used in balanced anesthesia
Prevent and treat bradycardia
Decrease salivary secretions arising from parasympathetic stimulation (aids in intubation)
Mydriasis (prevents rolling of the eyeball and opens pupil for eye surgeries)

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10
Q

Routes of admin for anticholinergics

A

Im, SQ, IV and IT (intertracial)

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11
Q

Major effects and adverse effects of anticholinergics

A

Prevention of bradycardia
Increased HR
Cardiac arrhythmias
Reduction and thickening of resp secretions
Bronchodilation
Mydriasis
Reduction of GI, salivary,, and lacrimal secretions
Inhibition of peristalsis - colic horses

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12
Q

Tranquillisers and sedatives work by and act on what system

A

Centrally-acting
Cause depression of the CNS

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13
Q

Are tranquilizers and sedatives part of a balanced anesthesia plan and why

A

Part of balanced anesthesia
Smoother induction
Allows decreased dose of general anaesthetic
Patients recovery faster

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14
Q

Are tranquilizers and sedatives controlled drugs

A

Many are controlled drugs
Controlled drugs and narcotic act
Record! For inventory and with each individual use
Practice standards: lock and key, strict record of use

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15
Q

Indications of tranquilizers and sedatives

A

Tranquilizers = reduces anxiety but does not necessarily decrease awareness and wakefulness
Sedative = causes reduced mental activity
The effects of these drugs often overlap because they produce both effects to some degree, to the terms tranquilizer and sedative are often used interchangeably

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16
Q

Different types of tranquilizers and sedatives

A

Phenothiazines
-Acepromazine
Benzodiazepines
-diazepam (Valium@)
-midazolam (Versed@)
Alpha2-adrenoceptor (alpha2-agonists)
-xylazine (Rompun@)
-dexmedetomidine (DexDomitor@)

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17
Q

Phenothiazines (tranquilizer and sedative) effects what system and is it controlled

A

Ex. acepromazine
Non-controlled (not technically Pr either)
Approved for horses, dogs and cats
Injectable and oral formulations
No reversal

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18
Q

major side effects and adverse effects of phenothiazines

A

Reduction of the seizure threshold
Tachycardia or bradycardia
Antiarrhythmic vasodilation
Hypotension
Antiemetic effects

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19
Q

Mechanism of action for phenothiazines

A

Blocks receptors in the basal ganglia→ CNS depression
Blocks alpha1 adrenergic receptors
Some antihistamine effects

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20
Q

Physiological effects of phenothiazines

A

Causes calming, reluctance to move and decreased interest in surroundings
Decreased spontaneous activity, ataxia
Vasodilation (due to blocking of alpha1-receptors
Suppressors chemoreceptor trigger zone (antiemetic)
Will slowly cross the placenta

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21
Q

Clinical use of phenothiazine

A

Anti-anxiety and sedation (relatively mild)
Chemical restraint ot ease handling
Travel
Decreased dose of general anesthetic
Eases induction and recovery
Blocks morphine-induced excitement in cat
Antispasmodic
Antiemetic (decreases vomiting when used together with hydromorphone as preanesthetic)

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22
Q

Common side effects of phenothiazines

A

Vasodilation (alpha1 receptor blockade); causes hypotension→ monitor BP
Hypothermia in small animals
Sequestering of RBCs in the spleen
Causes splenic enlargement and drops PVC
Caution in splenectomies, anemia
Overdose may cause rigidity or tremors
Ptosis, prolapsed 3rd eyelid in dogs and cats
Can cause aggression of excitement

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23
Q

Other considerations of phenothiazines

A

Bradycardia but less than many other agents
No analgesia
Antiemetic
Prevents histamine release and decreases allergic response
Worsens depressive effect of other drugs in the resp system
Metabolized by liver

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24
Q

Side effects specific to horses of phenothiazines

A

Penile prolapse
Facilitates sheath cleaning, examination
But can be irreversible
Caution in breeding stallions
Possible excitement, sweating, tachypnea

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25
Relative contraindications of phenothiazine
Breeding stallions- penile prolapse BOXERS- may exacerbate underlying arrhythmias Also avoid in severely debilitated, neonates, geriatrics, preexisting hypotension (blood loss, shock, dehydration), CHF, liver disease, CRF Related to vasodilation and resultant hypotension Always use caution when sedating brachycephalic breeds
26
How to use acepromazine
Can also use alone for anti-anxiety and minor restraint Used in combination with other drugs for pre-anesthesia There is a mg/kg dose AND a maximum dose Increasing the dose does NOT increase sedation but does increase hypotension due to peripheral vasodilation Works better if not already excited; excitement can decrease the effect Lasts 4-8 hours Do not combine with dexmedetomidine No reversal. If overdose, provide supportive care Support BP-fluids Increase the sympathetic response
27
Butyrophenones is what
Azaperone/Stresnil@ Drug class: butyrophenones (similar to phenothiazines) Only used in pigs Very unpredictable results in other species Blocks dopamine and norepinephrine activity in the CNS
28
Clinical indications for azaperone
Decreases aggression/fighting during weaning and mixing Premedication and sedation (castrations) Antiemetic Decreases malignant hyperthermia Potentially fatal genetic condition; increased metabolic rate and muscle activity in response to isoflurane, transport/handling stress Most commonly occurs in pigs
29
Benzodiazepines is/when to use/ is it controlled
Ex. diazepam (Valium@), midazolam (Versed@) Controlled (schedule IV of the controlled drugs and substances act) Most not labelled for veterinary use therefore an example of ELDU Injectable and oral (tablets) formulas available
30
Major effects and adverse effects of benziodiazepines
Antianxiety and calming Anticonvulsant activity Disorientation and excitement in young, healthy dogs Dysphoria and aggression in cats Muscle fasciculation in horses Ataxia in recumbency in large animals Few cardiopulmonary effects Skeletal muscle relaxation No analgesia
31
Does benzodiazepines have a reversal agent
Reversal → flumazenil
32
Mechanism of action for benzodiazepines
Increase GABA levels in the brain GABA is an inhibitory neurotransmitter
33
Indications of benzodiazepines
As part of balanced anaesthesia Premed to smooth induction and recovery Can combine with ketamine for induction Other common indications Antianxiety to sedation; behavioural modifier Anticonvulsant for treating seizures Skeletal muscle relaxant (including urethral relaxation)
34
benefits of benzodiazepines
Minimal CV effects at appropriate dose Dose cause dose-dependent resp depression Smoother induction and recovery Decreases amount of inhalant GA required Increase skeletal muscle relaxation
35
Is benzodiazepine reversable
Reversible drug class In the event of overdose or adverse reaction, can give the reversal agent (aka antagonists or antidotes)
36
Precautions of benzodiazepines
Sedation is not always reliable when used alone in animals Dysphoria/excitement can occur May unmask latent aggression in some animals (animals lose inhibitions)
37
Precautions with horses on benzodiazepines
Muscle fasciculation Weakness, ataxia Do not give alone except for seizures in adults
38
Contraindications of benzodiazepines
AVOID in pregnancy/caesarean Will cross the placenta Causes similar to FLOPPY BABY SYNDROME Skeletal muscle relaxation in the neonate Asphyxiation form relaxation of resp muscle
39
Diazepam is what drug class and used on what
Benzodiazepine Commonly used Dog, cat, horse, pig
40
Clinical indications of diazepam
Anticonvulsant for emergency treatment of seizures Antianxiety (noise phobias) at lower dose Sedation in some patients at higher dose Must be used in combination with other drugs in cats and horses (and some dogs) or may cause excitement Skeletal muscle relaxant Relaxes urethral sphincter (blocked cats and dogs) Can mix with ketamine for induction (KetVal)
41
Indications of diazepam
Inexpensive Can be administered by many routes: IV solution- painful/unreliably absorbed if given IM/SQ Can give intrarectal if seizing patient Also available as oral tablets Dose varies depending on the route Lasts 30 min - 2h May cause a prolonged hangover effect Historically used as appetite stimulant in cats- doesn't really work-risky
42
handling and storage of diazepam
Controlled drug Not water soluble Will form precipitate if mixed with other drugs Never use if precipitate forms Only exception is KETAMINE (KetVal) Store IV solution in glass containers Drug binds to plastic with time Keep from light Flush IV lines immediately after administering Binds to plastic and will form precipitate if still present in line/verin when drug is administered
43
Adverse effects; contraindications of diazepam
Contradiction for caesarean Floppy baby syndrome Depressed, poor muscle tone, excessive sedation Aggressive dogs Can bring latent aggression Using alone in horses Excitement and ataxia Cats Can cause sudden liver failure- increase risk with increase doses Therefore avoid use as an appetite stimulant
44
midazolam/Versed@ is what type of drug class and used when
Benzodiazepines Very similar to diazepam Easier to use, but more expensive
45
How is midazolam different from diazepam
Twice as potente Shorter acting Compatible with many agents as it is water soluble Can give IM, SQ, IV CANNOT use alone Not used as anticonvulsant
46
Flumazenil is what drug class
Antagonsit
47
Flumazil works for what drugs
Reversal agent (aka antagonist) for benzodiazepines including diazepam and midazolam
48
How does flumazil work
Binds to and blocks GABA receptors More attraction for the GABA receptor then the benzodiazepines Therefore, knocks of any benzodiazepine drug already bound to the receptor Little to no effect on its own Solemn used because $$$$ and short duration of action of diazepam/midazolam
49
Is Alpha2 adrenergic agonists (tranquilizer and sedative) controlled
No
50
Alpha2 adrenergic agonists effects and adverse effects
Dose dependent sedation that can be profound Analgesia Agitation or aggression when touched Reaction to loud noises Muscle tremors in horses Cattle often lie down Initial hypertension, bradycardia, and pale MM followed by hypotension, decreased cardiac output, and a little further decrease in the heart rate Severe decrease in heart rate, BP, cardiac output, and tissue perfusion especially when high doses are given Respiratory depression that can be severe Muscle relaxation Vomiting in cats and dogs Adverse GI effects (bloat and colic) Hyperglycemia Hypothermia Increased urination Premature parturition in cattle Horses may sweat
51
Large animal apla2 adrenergic agonist
Xylazine (Rompun@) Detomidine (Dormosedan@) Romifidine (Sedivet@)
52
Small animal alpha2 adrenergic agonist
Dexmedetomidine (Dexodomitor@)
53
Is the drug class Alpd2 adrenergic agonist reversable
Yes
54
Mechanism of action of alpha2 adrenergic agonist
Drugs bind to alpha-2 adrenergic receptors Activation of alpha 2 receptors causes inhibition of release of norepinephrine and dopamine Decreases overall sympathetic response Metabolized by the liver; excreted by the kidneys
55
Physiological effect of alpa2-recptor activation
Overall CNS depression Decreased overall ability to respond to stimuli This action is enhanced if given together with an opioid or other sedative or tranquilizer Decreases sympathetic response Bradycardia- consistent, immediate, significant; as low as 12 bpm in a large dog Resp depression Increases parasympathetic nervous system Increased GI motility (except in ruminants)
56
Indications of alpha2 adrenergic agonist
Rapid and reversible sedation Mild analgesia on own Can be used for neuroleptanalgesia Occurs when alpha-2 agonist is combined with an opioid and given at a fairly high dose A state of lack of awareness associated with very heavy sedation combined with strong analgesia Used for minor procedures e.g. suturing lacerations in horses Centrally-mediated muscle relaxation
57
adverse effects of alpha 2 adrenergic agonist
Severe hypotension Can hyperventilate on room air Possible arrhythmias with some of the older drugs Increased risk if given too fast IV Increased risk if also given atropine Ataxia Cattle can become recumbent, decreased rumen motility, risk of bloat and may cause abortion Horses can become reactive to stimuli if give alone- noise, touch Emesis in cats
58
Why does alpha 2 adrenergic agonsit cause hypotension
Related to significant bradycardia Decreased pulse, MM become very pale Do not use with acepromazine in small animals
59
Why can animals hyperventilate on room air when under alpha 2 adrenergic agonist
Decreased RR and resp volume Enhances the resp depressant effect of other sedatives and anesthetics RESPIRATORY DISTRESS IN BRACHYCEPHALIC DOGS Ruminant very sensitive to resp effects
60
Warning and contraindications of alpha2 adrenergic agonist
Avoid or use extreme caution in pediatrics, geriatric Avoid if severely dehydrated, in shock, cardiovascular disease, severe resp disease, or severe renal disease Avoid if advanced liver disease Avoid or use extreme care with acepromazine Acpreomazine→ severe hypotension from combination of bradycardia and vasodilation; will plummet the BP and there is no way to bring it back other then reversal However it can be fail safe group IF you have reversal on hand MONITOR! MONITOR! MONITOR!
61
Using alpha2 adrenergic agonists
IM (15-20 min onset), IV (1-3 min onset) Duration of sedation is 30-60 min Don't give IV too fast or will enhance the resp and cardiac depression effects When using IV, should “give to effect” only until desired degree of sedation is achieved Avoid SQ Very lipophilic; drug will bind to fat and absorption will be unpredictable (can severely delay effect) Decreased effect if stressed or fearful
62
Indications of xylazine
Equine and bovine Premed “Standing sedation” -For castrations, wound repairs, caesareans Sedates animal without becoming recumbent Colic -Excellent visceral analgesia 30 min of analgesia if given as an epidural Part of “Triple Drip” -Injectable GA, to be discussed with ketamine Two concentrations 20mg/ml or 100mg/ml -Lower concentration in cattle b/c of increased rep and GI effects IV “to effect” -IV has more pronounced heart and resp effects IM -Onset of action occurs 10-15 minutes after Im injection -Duration of action is approx. 30 min Epidural -Visceral analgesia Often combined with an opioid (ex. butorphanol) or valium for better sedation and longer duration
63
Adverse effects of xylazine
Cattle require 1/10 of dose compared to horse -Even at recommended dose can have severe resp effects, cause GI stasis (i.e., bloat) risk of aspiration pneumonia Horses -Sweating -Ataxia, wide-based stance -Horses can become excited if used alone -Never given intra-arterial in horse; will cause excitement/seizure/collapse -Avoid in neonatal foals as the lowered HR cannot maintain blood flow
64
detomidine/Dosmesdan@ are used in what and what drug class
Alpha2 adrenergic agonist labeled for horses
65
detmoidine works by/for
Similar to xylazine Visceral analgesia Give slowly IV to effect Can give alone or with opioid Severe hypotension and bradycardia Twice the duration and stronger sedation Used for standing sedation Never use with IV sulphonamides→ heart failure
66
romifidine/Sedivet@ is used for and why
Labelled for horses Similar to xylazine, detomidine Fast acting, long lasting Severe hypotension and bradycardia Sedative or pre med Can use at low dose Anxiolytic with minimal ataxia
67
dexmedetomidine/Dexdomitor@ is used for and when
Small animal Sedation (60-90 min); analgesia (30 min) Sedation Hip rads, minor procedures (with local anesthetic), quills Premed Sedation and pre-emptive analgesia On going sedation if given as CRI
68
Indications of dexmedetomidine
Usually given in combination with opioid Better analgesia Better sedation Dresses the mg/kg dose of dexmedetomidine required→ decreases adverse side effects Most commonly with butorphanol or buprenorphine Will see more resp depression is combined with hydromorphone
69
Dosing of dexedetomidine
The label dose is 10x to 20x what is used in clinic Label dose is intended for heavy sedation with dexmedetomidine alone When combined with opioids and/or with balanced anesthesia, only use at 1/10 to 1/20 the labelled dose Is also labelled for indication at higher doses (not usually done) As animal size increases, the mg/kg dose decreases
70
How to administer dexmedetomidine and how long does it work for
IM takes 15-20 min onset time NEVER give SQ- drug deposits in fat and releases unpredictably Give IV to effect Dog only Do NOT give to rapidly, can stop breathing 1-3 min onset Can give ½ IM, wait 15 min, give remainder IV to effect
71
Adverse effects of dexmedetomidine
Profound bradycardia and resp depression (much more noticeable in dogs) Monitor HR and BP HR will drop significantly; 16 (large K9), 40 (small K9) Monitor BP and pulse strength Monitor MM Will be pale; should never be cyanotic Monitor oxygenation Extend neck Place on flow-by 100% O2 if available Place IV catheter If in doubt, place ion IV fluid support
72
Caution and contraindications of dexmedetomidine
Do NOT use with atropine -Heart block, heart failure Extreme caution of avoid with acepromazine -Profound hypotension Extreme caution when followed by isoflurane in cats -Iso causes more extreme vasodilation then acepromazine Avoid if hypotensive dehydrated, geriatric, debilitated
73
Alpha2 antagonists is what type of drug
Reversal Reversals have a greater affinity for receptor then the agonist drug
74
Alpha-2 antagonist for LA
Yohimbine (Yobine®) Tolazoline (Tolazine®)
75
Alpha-2 antagonist for SA
Atipamezole (Antisedan®) Designed so you give equal VOLUME as Dexdomitor® for complete reversal
76
Alpha 2 antagonist works by
Effects specific to alpha2 agonist- does not affect other drugs Reversal of the sedative, cardiovascular AND analgesic effects of the corresponding agent Few adverse effects at clinical doses, but significant adverse effects if too much is given by increasing sympathetic tone GI, neurologic, and cardiovascular effects Excitement, muscle tremors, hypotension, tachycardia, salivation, vomiting, diarrhea
77
Opioids work as
Analgesia -Strongest analgesics available in vet med Preanesthetic -Pre-emptive analgesia – giving before pain occurs results in less post op analgesia required and shorter recovery times -Sedation -Decrease total dose of GA required Anesthetic induction -At higher doses, some opioids can produce unconsciousness (uncommon)
78
What are opioids used for
Majority have wide margin of safety at therapeutic dose (Higher Potency → Lower Therapeutic Index)
79
Where are opioids metabolized
Metabolized by liver with renal excretion, therefore Caution in very young, very old, debilitated Caution in very ill (including head trauma, shock, HBC) Caution if respiratory system is compromised
80
Are opioids controlled
Yes
81
Neuroleptanalgesia is and how to induce it
A profound state of sedation and analgesia Induced by simultaneous administration of an opioid and a sedative Ex. Dexmedetomidine + hydromorphone; xylazine + fentanyl Commonly given for minor procedures or indication Causes CNS depression to state of borderline unconsciousness Can be aroused by extreme stimulation, noise
82
Routes of administration of opioids
IM SQ IV PO Rectal Transdermal Subarachnoid Intraarticular (joints) Epidural Neurolepetangelasia , when given IV, must be done so slowly to avoid CNS stimulation
83
Mode of action of opioids
Drugs work by binding to opioid receptors Although opioid receptors found on neurons throughout the body, analgesic and sedative effects are primarily the result of their action on receptors located in the brain and spinal cord Brain- sedation and analgesia Spinal cord-analgesia Smooth muscle of the rep tract, GI tract, urinary tract
84
Major types of opioid receptors
Mu (μ) Kappa (κ) Delta (δ)
85
Mu opioid receptor works for
Supraspinal analgesia Moderate to severe pain Sedation Resp depression Bradycardia Miosis (mydriasis in cats) Hypothermia (hyperthermia in cats) Euphoria /dysphoria GI stasis (constipation) Urinary retention CRTZ (chemoreceptor trigger zone) for vomiting Antiemetic at the vomiting center
86
Kappa opioid receptor works for
Spinal analgesia Mild to moderate pain Miosis Mild sedation Little resp depression Diuresis
87
Classes of opioids
Pure agnostic Partial mu-agonist Agonist-antagonist Pure antagonists
88
What determines the class the opioid is in
Opioids are placed into “classes” based on which receptor they bind and whether binding causes the receptor to be turned on (agonist), partially turned on (partial agonist) or turned off (antagonist)
89
Pure agonists work by
Drugs bind to and turn on the mu-receptor May also turn on kappa-receptor Provides the best analgesia (treats moderate to severe pain) Mu-antagonist provides the best analgesia. Drugs with a higher affinity for the mu-receptor provide more analgesia Also produces sedation Highest risk of addiction Morphine, hydromorphone, oxymorphone, fentanyl, meperidine, hydrocodone, tramadol
90
Pure agonists side effects
Side effects as listed for the mu receptor (resp depression, GI stasis, hypothermia, occasional hyperthermia in cats); analgesia and sedation are better if also has kappa activity
91
Partial mu-agonsits work by
Binds to and partially activates the mu-receptor
92
Partial mu-agonists physiological effect compared to pure agonists
Less analgesia Less resp depression Less GI stasis Less euphoria Less hypothermia
93
When to use partial mu-agnosists
Indicated for slight to moderate pain Also used to “partially” block the effects of a pure mu-agonist that is given at the same time; i.e., acts as a partial reversal Buprenorphine (partial mu-agonist; kappa antagonist)
94
Agonist-antogonist opioids work by
Simultaneously turns on kappa-receptor (kappa-agonist) while blocking mu-receptor (mu-antagonist)
95
Physiological effects of agonist-antagonist opioids
Mild analgesia Sedation Less resp depression and less GI effects than the pure or partial agonists May cause dysphoria
96
When to use agonist-antagonist opioids
Can be used to “completely block” either mu-agonist or partial mu-agonist activity Butorphanol (kappa-agonist; mu-antagonist)
97
Pure antagonists work by
Binds to both mu-receptors and kappa-receptors but does not produce any activity Effectively acts as a block “Reversals” Naloxone Naltrexone Direnorphine (M-50) is the reversal agent specifically created for etorphine (M-99)
98
Major side effects of opioids
Resp depression Most common cause of death in case of OD Centrally-mediated; decreases RR and tidal volume Also inhibits the CO2-drive that stimulates breathing Ventilation should be monitored and O2 available Bradycardia Hypothermia in all species Occasional hyperthermia in certain cats is due to a mu-receptor response especially hydromorphone and can be fatal if not treated Caution using in patients with brain trauma or cerebral edema; can increase brain swelling Sedation
99
Non-life-threatening side effects of opioids
Vomiting GI stasis (constipation) Dysphoria, excitement, hallucinations, startle response in cats Addiction
100
Why does opioids induce vomiting
Activates the chemoreceptor trigger zone in the brain Often with first dose of mu-agonists in healthy pain free animals Can block/decrease with acepromazine or diazepam
101
Why does opioids cause GI stasis
More likely with chronic use Avoid or caution in colic, bloat, FB surgeries (enterotomies)
102
Why does opioids cause addiction
Mu-receptor mediated Receptor down-regulation means may need to increase dose or dosing frequency to manage chronic pain
103
Variable side effects of opioids
Variable effects may or may not occur depending on the specific opioid, dosage, route of administration and species Antitussive (codeine, hydrocodone, butorphanol; to treat cough) Vomit (apomorphine; IM hydromorphone) Diarrhea and flatulence Miosis in dogs; mydriasis in cats and horses Excitement, dysphoria, whine/bark (dogs), increased motor activity (horse), increased sensitivity to noise Hypotension/hypertension Changes in urination Excess salivation Panting in dogs Hyperthermia in cats Sweating in horses
104
Pure mu agonists examples
Morphine Fentanyl Hydromorphone Methadone Meperidine Sufentanil Cerfentanil
105
Indications of morphine
Mu and kappa agonist Indications “Opioid standard of reference) All other opioids are compared to morphine Mild to moderate sedation dose dependant Analgesia for moderate to severe pain
106
Routes and duration of morphine
IV, IM, SQ, PO, intra articular, epidural Duration of action 3-4 hours
107
Side effects of morphine
Excitement or dysphoria in cats, horses Mydriasis in cats, horses Drowsiness in dogs Severe resp depression with high doses Nausea/vomiting GI stasis (oral form is worse) Histamine release can cause systemic vasodilation
108
Fentanyl indications and potency
Mu and kappa agonist 50-100x the potency of morphine Indications Neuroleptanalgesia Induction Analgesia (provided frequent administration)
109
Routes and duration of action of fentanyl
IV bolus CRI (preferred IV method) Slow release transdermal patch Epidural Duration of action 1-2 min onset; 10 min duration of action IV Usually CRI or slow release transdermal patch for analgesia
110
Side effects of fentanyl
Defecation or constipation Resp depression Bradycardia Hypothermia Panting, drooling Dysphoria, agitation Sedation Not approved for food animals
111
Hydromorphone indications
Mu and kappa agonist Indications 5-10x the potency of morphine Moderate to severe pain (visceral and somatic) Pre, peri and postoperative pain control More sedation than morphine Rarely used in large animals because of lack of info about efficacy or adverse side effects
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Duration of action by route for hydromophone
IV 1-2 hours IM 2-4 hours in dogs, longer in cats SQ up to 6-8h Epidural 8 hrs
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Side effects of hydromorphone
Reliable emetic with first dose, especially if SQ/IM Diarrhea with first dose; constipation with chronic use Pant, drool Mydriasis in cats and horse Excitement /hallucinations in cats and horses
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Adverse effects of hydromorphone
Resp depression Use with caution or contraindicated if severe resp disease Most common cause of fatality Bradycardia Hypothermia in all species Can cause occasional hyperthermia in cats which can be fatal In the event of a severe adverse reaction, can partially reverse with buprenorphine or butorphanol; can completely reverse with naloxone, naltrexone
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methadone indications
Mu and kappa agonist Indications 5-10x the potency of morphine Moderate to severe pain (visceral and somatic) Low incidence of vomiting (compared to morphine or hydromorphone); other side effects similar to other pure mu agonists Excellent article summarising methadone released in the CVJ last year
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Duration of action for methadone
Duration of action ~4hrs This is slightly longer than morphine and hydromorphone
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What can you use methadone on
Methadone is relatively new in canada Currently only licensed for use in cats; however, it is licensed for use in cats and dogs on other areas (Australia, New Zealand countries within the UN and EU) as an analgesic and preanesthetic agent Licensed in Canada: 0.5mg/kg IM in cats prior to spay or neuter. Extra-label: commonly used 0.2-0.5mg/kg administered IV, IM or SC
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meperidine/Demerol@ indications
Mu and kappa agonist Indications 1/10x morphine Mild to moderate pain
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meperidine/Demerol@ route of action and duration
Routes IM injection, NOT IV or SQ Histamine release with IV use Duration of action 30-90 min
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Side effects of meperidine
No vomiting or bradycardia Use as premedication when no vomiting required
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Sufentanil works on what receptor
Super mu-agonist” 500-1000X the power of morphine But shorter acting than fentanyl
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Indications of sufentanil
Intraoperative analgesia in dogs and cast as an infusion Induction
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Carfentanil works on what receptor
“Super mu-agonist” 10,000-100,000X the power of morphine
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Indications of carfentanil
Wildlife capture and immobilization
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Why is carfentanil super dangerous for people
Potentially fatal if handler scratches/injects self Use with extreme caution Wear double gloves when handling closed bottle
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Reversal of carfentanil
Requires naltrexone for reversal Draw up BEFORE handling carfentanil
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Partial mu agonists is
Buprenorphine -Partial mu agonist, kappa antagonist
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Indications of buphenorphine
1/20x morphine Mild to moderate pain Less sedation Onset of action ~30 min
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Routes and duration of action for bupernorphine
IV, IM, SQ, epidural or trans mucosal (in cats) Place in the buccal cavity or sublingual and allow absorption through the oral mucosa Will NOT work if swallowed Duration of action 6-8 hours in dogs and cats 2 hrs in sheep
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Side effects of buprenorphine
Fewer side effects than hydromorphone due to partial mu-activity Slightly dysphoria
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Reversal of buprenorphine
Higher affinity than naloxone, therefore requires much high doses or infusion of naloxone to reverse buprenorphine
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What drug is a Agonist- antagonist (kappa agonists, mu antagonist)
Butrophanol/Turbugesic@
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indications of butrophanol
½ to 1x morphine Mild to moderate pain Analgesia and sedation are via the kappa-receptor Ex, colic Sedation Antitussive Reversal of hydromorphone SA (0.5mg/ml) and LA (10mg/ml) concentrations
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Routes used for butrophanol
IV, IM, SQ, PO
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Side effects of butrophanol
No mu-receptor mediated side effects Less resp depression No excitement No GI stasis No panting in dogs
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How does butrophanol work as a reversal
Binds to and blocks mu-receptor Activation of kappa receptor produces mild to moderate analgesia and some sedation If butorphanol and hydromorphone are both present, butorphanol will bind to the receptor because it has 30X the affinity for the receptor compared to hydromorphone. Result is to kick out the hydromorphone and/or prevent the hydromorphone from binding to the receptor
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Opioid antagonists (reversal) indication
Reversal of desirable and undesirable effects of opioid agonists, partial agonist, or agonist-antagonist including sedation and analgesia CNS and resp depression
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Routes of admin for opioid antagonists
IM, slow IV
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major effects and adverse effects of opioid antagonsits
Reversal of desirable and undesirable effects Sedation, dysphoria, panting, resp depression, hypotension, bradycardia, GI effects and analgesia The action of opioid antagonists if often dramatic, causing patient to appear nearly unaffected shortly after administration
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Naxalone is what type or reversal
Pure antagonist
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Naloxone indications
Complete reversal of both mu and kappa agonists Will lose all adverse effects and all analgesia Dog, cat, horses, exotics, people 1 drop under tongue of neonates after C-section to reverse resp depression of opioid given to the mother
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Duration of action and time of onset of naloxone
Duration of action 30-40 min; will need to top up Time of onset 2 min IV Aggressive use can cause catecholamine related cardiac arrhythmias and vasoconstriction leading to pulmonary edema
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Naltrexone indications and duration of action
(pure antagonist) Both mu and kappa antagonist More potent than naloxone Used to reverse carfentanil in wild life Can be used intranasally Duration of action Long lasting (hours)
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Butorphanol/Torbugesic@ (Partial antagonist)
Kappa agonists, mu antagonist Only blocks mu activity; adds to kappa activity Not very strong reversal Leaves sedation and some analgesia Will reverse resp depression and hypo/hyperthermia
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What drugs are pure antagonist
Naloxone * Naltrexone * Diprenorphine (M-50) is the reversal agent specifically created for etorphine (M-99)
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What drugs are pure mu agonists
Morphine Fentanyl Hydromorphone Methadone Meperidine/demerol Sufentanil Cerfentanil
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What drugs are partial mu agonsits
Buprenorphine
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What drugs are kappa agonists and mu antagonist
Butorphanol/Turbugesic
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Side effects of Mu receptor opioid
Resp depression Bradycardia Miosis (mydriasis in cats) Hypothermia (hyperthermia in cats) Euphoria /dysphoria GI stasis (constipation) Urinary retention CRTZ (chemoreceptor trigger zone) for vomiting Antiemetic at the vomiting center
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Side effects of kappa receptor opioids
Miosis Mild sedation Little resp depression Diuresis