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23 spring anesthesia > Test 1: 5 opioids > Flashcards

Test 1: 5 opioids Flashcards

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
Q

effects of opioids on the heart

A

Minimal effects in cardiac output, rhythm, and arterial blood pressure

some bradycardia can occur

26
Q

IV meperidine and morphine can cause

A

histamine release

vasodilation and hypotension

27
Q

opioids will do what to GI tract

A

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
Q

effects of opioids on urinary tract

A

may cause urinary retention
* Decrease detrusor contractility
* Decreased sensation of urge

Special caution for epidural administration

29
Q

woody chest is caused by

A

rare muscle rigidity with full opioid agonists

30
Q

what will opioids do to pupil size

A
  • Mydriasis – cats, horses, ruminants
  • Miosis – dogs, rabbits, rats
31
Q

what are some opioid antagonists

A

Naloxone

  • Naltrexone
  • Methylnaltrexone
  • Diprenorphine
32
Q

— is a partial μ agonist

A

Buprenorphine

opioid

33
Q

— are agonist- antagonist

A

Butorphanol
Nalbuphine

34
Q

— can cause histamine releases after fast IV administration

A

IV meperidine and morphine

35
Q

what opioid is used for epidural analgesia

A

morphine

Crosses BBB slower than synthetics opioids
* Persists in epidural space for 12 – 24h

36
Q

hydromorphone has a — duration

A

short 2-4 hr

morphine lasts 4-8 hrs
hydro 10 x more potent

37
Q

— can cause panting in dogs and hyperthermia in cats

A

hydromorphone

10 x more potent then morphine
shorter duration (2-4 hrs)

38
Q

methadone

A

Opioid agonist + NMDA antagonist – good for chronic / neuropathic pain

no vomiting!

potency, onset and duration similar to morphine

39
Q

— is an opioid used for chronic/ neuropathic pain

A

methadone
Opioid agonist + NMDA antagonist

No vomiting

NMDA is a glutamate receptor= excitatory

40
Q

meperidine

A
  • 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
Q

— is Highly lipid-soluble, short-acting synthetic opioid with 30 min duration

A

fentanyl

can be given as CRI or transdermal patches

100 x more potent then morphine

42
Q

what opioid is not metabolized by the liver

A

Remifentanil
Analog of fentanyl

200 x more potent then morphine

43
Q

— are high potency opioids used in large wildlife mammals

A

Carfentanil and Etorphine (M99)

Etorphine (3000x )
Carfentanil (10000x)

44
Q

Butorphanol

A

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
Q

— is an agonist at κ receptor and antagonist at μ receptor that is used in horses and birds

A

butorphanol

Minimal analgesia
Short duration – 1h
Mild sedation – better if combined with other sedatives

46
Q

— can be given tranmucosally in cats due to their high pH

A

buprenorphine

Partial μ agonist
short onset and long duration (6-12 hrs)

47
Q

— is a Partial μ agonist and the duration is —

A

buprenorphine

1hr onset, 6-12 hr duration

can be given IV, IM or SC
transmucosal in cats

48
Q

— will reverse opioids

A

nalaxone: duration 30-60 mins, may need to redose

naltrexone: long lasting for reversal of high potency opioids

49
Q

what is MAC reduction?

A

minimum alveolar concentration

will reduce the amount of inhalant required to maintain the anesthetic plan

opioids will cause a MAC reduction

50
Q

why use opioids with anesthesia

A
  • Sedation in premed – reduce patient stress
  • Analgesia
  • MAC Reduction-reduce amount of inhalant needed, improve cardiovascular stability

23 spring anesthesia (40 decks)

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