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Pharmacology II > Lecture 9: Opioid Analgesics > Flashcards

Lecture 9: Opioid Analgesics Flashcards

1
Q

What is nociception

A

Sensory processing and transmission of noxious stimuli

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2
Q

What are the affective components of pain (2)

A

Sensation and tissue damage

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3
Q

Opioids are effective at addressing both ___and ___

A

Pain transmission and affective components (sensation and tissue damage)

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4
Q

Opioids are the most effective analgesics available for ___

A

Tx of systemic acute pain

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5
Q

What is the pain transmission pathway

A
  1. Spinal nerves
  2. Spinal cord in dorsal horn
  3. Release substance P and glutamate
  4. Spinal cord—>brain
  5. Descending pathway
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6
Q

What 3 ways do opioids block pain

A

Inhibit perception, transduction and modulate the spinal pathway

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7
Q

Where are Mu receptors found

A

Brain and in the spinal cord in dorsal horn

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8
Q

What does activation of mu receptors result in

A

Sedation, supraspinal and spinal analgesia, miosis, respiratory depression, euphoria, inhibition of ACh and dopamine release, decrease GI motility

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9
Q

Where are kappa receptors found

A

Cerebral cortex, spinal cord and other brain regions

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10
Q

What is the result of activating kappa receptors

A

Spinal and supraspinal analgesia, mild sedation, inhibition of vasopressin, miosis

Less respiratory depression than mu

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11
Q

Where are delta receptors located

A

Limbic system, cerebral cortex and spinal cord

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12
Q

What is the result of activating delta receptors

A

Spinal and supraspinal analgesia, inhibition of dopamine release and cardiovascular depression

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13
Q

What is the mechanism of action of opioids

A
  1. Act on Gi proteins
  2. Decrease cAMP
  3. Close VG Ca2+ channels
  4. Decrease NT release- ACh, glutamate, substance P, NE
  5. Open presynaptic K+ channels (mu) causing hyperpolarization
  6. Promote release of endogenous opioids that further inhibit pain transmission
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14
Q

What are the two overall effects of opioids

A
  1. Inhibition of pain transmission
  2. Simulation of descending inhibitory neurons
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15
Q

The primary use for opioids is ___

A

Analgesia

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16
Q

What are the endogenous opioids

A

Endorphins, enkephalins, dynorphins

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17
Q

Release of endorphins causes ___

A

Euphoria

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18
Q

Release of enkephalins causes ___

A

Decreases our sensation and reaction to pain

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19
Q

Drugs that stimulate __ receptors produce profound analgesia

A

U receptors

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20
Q

What is the mechanism in which opioids provide analgesia

A

They decrease the transmission of pain in the spinal cord and the sensation of pain in the cerebral cortex, increase release of encephalin from PAG further reducing pain transmission

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21
Q

Opioid receptors undergo ___ and ___ which may lead to decrease effect overtime/ tolerance

A

Desensitization and downregulation

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22
Q

What effects do opioids have on the CNS

A

At low doses: sedation
At high doses: excitement
Horses and cats: excitement
Dogs: sedation

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23
Q

Opioids may cause ___ in dogs

A

Dysphoria

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24
Q

Opioids may cause ___ and ___ in cats

A

Dysphoria and increased motor activity

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25
What are the effects of opioids on the pupils
Miosis in most species Mydriasis in cats and horses
26
What effects do mu receptor agonists have on respiratory system
They are respiratory depressants, increase arterial CO2 and decrease arterial O2 and pH Result in panting in dogs and resetting hypothalamic temperature set point
27
What are the effects of opioids on the cardiovascular system
Bradycardia Hypotension- vasodilation due to histamine release
28
What opioid is most likely to cause vasodilation from histamine release
Morphine
29
____ and ____ in cats from histamine may become dangerous
Pruritis and excoriation
30
What are the GI effects from opioids
1. Stimulate CRTZ- vomiting 2. Aspiration from vomiting 3. Decrease GI-constipation and decrease gastric empty 4. Anti-diarrhea
31
What receptors does morphine act on
Full mu receptor agonist High doses stimulate kappa receptors
32
What species is morphine typically used in
Cats, dogs, and horses
33
___can induce vomiting in dogs by stimulating CRTZ
Morphine
34
How is morphine metabolized in cats vs dogs
Cats: sulfate conjugation Dogs: glucoronidation
35
What are the uses for morphine
Tx for acute pain in dogs, cats and horses
36
What can morphine cause in horses and what would should be given with it
Excitement, give with xylazine, acepromazine, diazepam
37
What are some adverse effects of morphine
Hyperexcitation, hypotension (d/t histamine), cerebral hemorrhage and edema (increase cerebral BF and ICP- don’t use with head injuries) , hyperthermia in dogs and rabbits, hyperthermia in cats, horses and ruminants
38
What are the doses of morphine that produce excitation in dogs, cats and horses
Dogs: 20mg/kg Cats: 5-10mg/kg Horses: 0.66mg/kg
39
What receptor does methadone act
Synthetic u agonist
40
Methadone can be used as an alternative to ___in dogs and cats. Why?
Morphine- reduce vomiting, nausea and defecation
41
What is methadone used for
Pre-anesthetic or analgesia in dogs or cats
42
Does methadone have a long or short half life and duration of action
Long
43
What are some adverse effects of methadone
Sedation, respiratory depression
44
What receptors do oxymorphone and hydromorphone act on
U agonists
45
Hydromorphone and oxymorphone have less___than morphine
Vasodilation/histamine release
46
What are some side effects of oxymorphone, hydromorphone
Panting in dogs, bradycardia, sedation, and hyperthermia in cats
47
What is oxymorphone, hydromorphone used for
1. Analgesia in dogs, cats and horses 2. Preanesthetic administration 3. Neurleptanalgesia 4. Anesthesia in swine combined with ketamine and xylazine
48
Hydromorphone combined with ___can decrease vomiting and panting in dogs
Acepromazine
49
Hydrocodone is converted to hydromorphone and can be used as a __in dogs
Antitussive
50
What receptor does fentanyl act on
U agonist
51
What are some uses for fentanyl
1. Anesthetic induction regimen 2. Control intra-op and post-op pain 3. Chronic pain
52
What are some adverse effects of fentanyl
1. Auditory stimuli may evoke motor response 2. Panting, defecating, flatulence 3. Bradycardia and hypersalivation
53
What are the benefits of fentanyl patch
Provide long lasting pain relief for up to 4 days
54
What receptor does alfentanil act on
U receptor agonist
55
What is alfentanil used for
1. Analgesic and sedative 2. Adjunctive for anesthesia particularly in cats
56
What receptor does sufentanil act on
U receptor agonist (more potent than fentanyl)
57
What is sufentanil used for
Adjunctive anesthesia, epidural analgesia, post-op analgesic
58
What are some adverse effects of sufentanil
Sedation, respiratory depression, bradycardia
59
What is carfentanil used for
Labeled for IM to immobilize large/wild animals
60
What are some adverse effects of carfentanil
1. Disruption of body temperature- hyper/hyporthermia that can be fatal in field 2. Respiratory and CNS depression
61
What is the reversal agent for carfentanil
Naltrexone
62
What receptors does tramadol act on
1. Weak u receptor agonist 2. Inhibits reuptake of serotonin and NE 3. Stimulates alpha2 receptors via NE
63
What is tramadol used for
Analgesia, antitussive
64
What are some adverse effects of tramadol
Seizures if given with other antidepressants/ fluoxetine
65
What receptors does buprenorphine act on
Partial agonist on u receptors and antagonist on k receptors
66
Buprenorphine is resistant to antagonism by what reversal
Naloxone
67
What is buprenorphine used for
Pre-op and post-op analgesia in small animals and analgesia in horses
68
What are some adverse effects of buprenorphine
Respiratory depression, excitement, mydriasis in cats, sedation
69
What receptors does butorphanol act on
K receptor agonist, partial agonist or antagonist for u receptors
70
Butorphanol can be used as a reversal for what receptor and what does it reverse and what is maintained
Reverse effects of u agonist- sedation, respiratory depression while maintaining analgesia from k effect
71
What is butorphanol labeled for
1. Antitussive in dogs from chronic upper respiratory infections 2. Analgesia in cats 3. Visceral pain in horses with colic 4. Analagesia and chemical restraint in cattle combined with ketamine 5. Mild to moderate pain 6. Anti-emetic for chemo patients
72
What are some adverse effects of butorphanol
1. Head bobbing in horses, ataxia, sedation or excitement 2. P-gp metabolism so decrease does 25% in heterozygous MRD1 mutations and 50% in homozygous
73
What receptors does nalbuphine act on
K receptor agonist, u receptor antagonist
74
What are the uses for nalbuphine
1. IM to control mild to moderate pain or pre surgery protocol 2. Topical administration for pain from corneal ulcers
75
What receptors does Naloxone act on
High affinity u receptor antagonist, low affinity for k
76
What are the uses for Naloxone
Reverse opioid induced sedation, respiratory depression, dysphoria
77
What are some adverse effects of Naloxone
1. Reversal of analgesia 2. Nausea, vomiting, hypotension, tachycardia
78
What receptors does naltrexone act on
U receptor antagonist
79
What is naltrexone used for
1. Reverse opioid induced immobilization of large animals 2. Oral administration to tx behavioral problems in dogs

Pharmacology II (36 decks)

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