Test 1: 5 opioids Flashcards

(50 cards)

1
Q

classes of opioid receptors

A

μ
κ
δ

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2
Q

effects of μ opioid receptor

A

analgesia

bradycardia
↓breathing
↓GI motlility
vomiting
↓urine production

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3
Q

effects of kappa opioid receptors

A

analgesia
↑urine production

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4
Q

effects of delta opioid receptor

A

analgesia
↓breathing

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5
Q

where are opioid receptors

A

brain, spinal cord, periphery

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6
Q

where are the opioid sites in the brain

A
  • Rostral ventromedial medulla (RVM)
  • Midbrain Periaqueductal gray (PAG)
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7
Q

what will opioids do in the brain

A
  • Enhances descending inhibition
  • Decreases descending facilitation
  • Influences nociceptive processing (perception)
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8
Q

where are opioid receptors in the spinal cord

A

dorsal horn of the spinal cord

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9
Q

how does opioids work in the spinal cord

A
  • Reduce the release of excitatory neurotransmitters
  • Reduce the excitability of neurons that carry pain signals
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10
Q

where are opioid receptors in the periphery

A

nerve endings

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11
Q

how does opioids work in the periphery

A
  • Inhibit afferent nociceptive transmission
  • Upregulated with inflammation
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12
Q

why use κ agonist

A

will be μ antagonist

will wake up patient

butorphanol

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13
Q

efficacy vs potency

A

efficacy: how well the drug works: The maximum response achievable from an applied or dosed agent

potency: how much drug you need: Measurement of drug activity in terms of the amount required to produce an effect of given intensity

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14
Q

Measurement of drug activity in terms of the amount required to produce an effect of given intensity

A

potency

Comparisons are made to morphine

  • “How much drug you need”
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15
Q

The maximum response achievable from an applied or dosed agent

A

efficacy

how well the drug works

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16
Q

The extent or fraction to which a drug binds to receptors at any given concentration

A

affinity

“How strong is the binding with receptor”

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17
Q

what are some ways to give an opioid

A
  • IV – 100% bioavailability, IM/SC – well absorbed
  • Oral – variable bioavailability, 1st pass effect, formulation/species dependent
  • Oral Transmucosal – pH of the mouth x pKa of the drug
  • Transdermal – lipophilic with low molecular weight, but VERY variable absorption
  • Epidural – lipophilicity affects onset and duration
  • Longer action with low lipid solubility = morphine
  • Spinal/ Subarachnoid – lower dose than epidural
  • Topical – cornea – peripheral μ opioid receptors
  • Intraarticular – opioid receptors upregulated in inflamed joints
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18
Q

how are opioids metabolized

A

in the liver

CYP450 and/or glucuronidation

(opioids can last longer in cats= no glucuronidation)

except Remifentanil- metabolized by plasma esterase

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19
Q

which opioid is broken down by plasma esterases

A

Remifentanil

can be used in liver failure patients

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20
Q

how does opioids cause sedation

A

species dependent (Dogs > cats/ horses)

  • Increase effects of other sedatives (phenothiazines, alpha-2)

can cause excitement in cats at high doses, and cause excitement in horses without pain

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21
Q

what happens to horse if you give opioids without pain

A

will cause excitement

22
Q

other than sedation, what will opioids do to the brain

A

Reduce cerebral metabolic rate
maintain cerebral blood flow and intracranial pressure

can cause vomiting and stop cough

dogs ↓temp
cats, ruminants and pigs ↑temp

23
Q

opioids will do what to thermoregulation

A

Species-specific effects

Dogs – Hypothermia
* Reset thermoregulatory point in hypothalamus = pant at normal body temperature

Cats, ruminants, pigs - Hyperthermia

24
Q

what will opioids do to respiratory center

A

dose dependent depressent

direct effect in the respiratory center

Decreased responsiveness of chemoreceptors to CO2 and hypoxia

humans and primates can stop breathing and die with overdose

25
effects of opioids on the heart
**Minimal effects** in cardiac output, rhythm, and arterial blood pressure some bradycardia can occur
26
IV meperidine and morphine can cause
histamine release vasodilation and hypotension
27
opioids will do what to GI tract
decrease motility * Mediated by μ and δ receptors in the myenteric plexus * Predispose to ileus and constipation * Colic in horses and tympany in ruminants
28
effects of opioids on urinary tract
may cause urinary retention * Decrease detrusor contractility * Decreased sensation of urge Special caution for epidural administration
29
woody chest is caused by
rare muscle rigidity with full opioid agonists
30
what will opioids do to pupil size
* Mydriasis – cats, horses, ruminants * Miosis – dogs, rabbits, rats
31
what are some opioid antagonists
Naloxone * Naltrexone * Methylnaltrexone * Diprenorphine
32
--- is a partial μ agonist
Buprenorphine ## Footnote opioid
33
--- are agonist- antagonist
Butorphanol Nalbuphine
34
--- can cause histamine releases after fast IV administration
IV meperidine and morphine
35
what opioid is used for epidural analgesia
morphine Crosses BBB slower than synthetics opioids * Persists in epidural space for 12 – 24h
36
hydromorphone has a --- duration
short 2-4 hr ## Footnote morphine lasts 4-8 hrs hydro 10 x more potent
37
--- can cause panting in dogs and hyperthermia in cats
hydromorphone ## Footnote 10 x more potent then morphine shorter duration (2-4 hrs)
38
methadone
Opioid agonist + NMDA antagonist – good for chronic / neuropathic pain **no vomiting!** potency, onset and duration similar to morphine
39
--- is an opioid used for chronic/ neuropathic pain
methadone Opioid agonist + NMDA antagonist No vomiting NMDA is a glutamate receptor= excitatory
40
meperidine
* Route: IM, SC * Duration: 1-4h * No vomiting and less bradycardia * Market **histamine release** * Analgesia (0.1) not profound as morphine – short procedures / mild pain
41
--- is Highly lipid-soluble, short-acting synthetic opioid with 30 min duration
fentanyl can be given as CRI or transdermal patches ## Footnote 100 x more potent then morphine
42
what opioid is not metabolized by the liver
Remifentanil Analog of fentanyl ## Footnote 200 x more potent then morphine
43
--- are high potency opioids used in large wildlife mammals
Carfentanil and Etorphine (M99) ## Footnote Etorphine (3000x ) Carfentanil (10000x)
44
Butorphanol
Agonist at κ receptor and antagonist at μ receptor short duration 1 hr Can be used to partially antagonize full opioid drugs Mild sedation – better if combined with other sedatives Commonly used in **horses and birds**
45
--- is an agonist at κ receptor and antagonist at μ receptor that is used in horses and birds
butorphanol Minimal analgesia Short duration – 1h Mild sedation – better if combined with other sedatives
46
--- can be given tranmucosally in cats due to their high pH
buprenorphine Partial μ agonist short onset and long duration (6-12 hrs)
47
--- is a Partial μ agonist and the duration is ---
buprenorphine 1hr onset, 6-12 hr duration can be given IV, IM or SC transmucosal in cats
48
--- will reverse opioids
**nalaxone**: duration 30-60 mins, may need to redose **naltrexone**: long lasting for reversal of high potency opioids
49
what is MAC reduction?
minimum alveolar concentration will reduce the amount of inhalant required to maintain the anesthetic plan opioids will cause a MAC reduction
50
why use opioids with anesthesia
* Sedation in premed – reduce patient stress * Analgesia * MAC Reduction-reduce amount of inhalant needed, improve cardiovascular stability