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ANESTHESIA PHARM 2 > OPIOIDS > Flashcards

OPIOIDS Flashcards

1
Q

what is the source of nociceptive somatic pain?

A

tissues (skin, muscle, joints, bones, ligaments)

often known as musculoskeletal pain

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2
Q

what is the source of nociceptive visceral pain?

A

internal organs of the main body cavities (thorax, abdomen, pelvis)

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3
Q

characterize somatic nociceptive pain vs. visceral pain

A
  • somatic pain – sharp and well localized, can be reproduced by touching or moving the area/tissue involved
  • visceral pain –poorly localized, dull pain (ache, cramping). frequently produces referred pain to the back
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4
Q

differentiate useful medications for somatic vs. visceral pain

A
  • somatic pain – may respond to combinations of weak or strong opioids AND NSAIDS
  • visceral pain – very responsive to weak and strong opioids
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5
Q

name a natural opioid

A

morphine

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6
Q

name a synthetic opioid

A

fentanyl

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7
Q

name a semisynthetic opioid

A

heroin

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8
Q

name an opioid agonist

A

morphine

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9
Q

name an opioid agonist/antagonist

A

nalbuphine

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10
Q

name an opioid antagonist

A

naloxone

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11
Q

what is the mechanism of action of opioids?

A

bind specific G protein-coupled receptors (in brain and spinal cord regions) involved in transmission and modulation of pain

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12
Q

where do opioid agonists work?

A
  • opioid receptors in the pre/post-synaptic CNS

* peripheral afferent nerves

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13
Q

what endogenous ligands do opioids mimic the effects of?

A
  • enkaphalins
  • endorphins
  • dynorphins
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14
Q

what neurotransmitters are released in response to pain (release is decreased with opioids)

A

acetylcholine, dopamin, norepi, substance p

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15
Q

which opioid receptor’s 1º action is analgesia, produces N/V, pruritits, and bradycardia, and has low abuse potential?

A

Mu1

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16
Q

which opioid receptor is found only in the spinal cord (as opposed to spinal AND supraspinal)?

A

Mu2

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17
Q

Mu1 and Mu2 both produce euphoria. which one also produces sedation?

A

Mu2

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18
Q

which opioid receptors are responsible for physical dependence?

A

Mu2 and delta

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19
Q

which opioid receptor does not produce respiratory depression?

A

Mu1

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20
Q

which opioid receptor is responsible for dysphoria and diuresis?

A

kappa

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21
Q

which opioid receptor is the principle site for agonist-antagonists, and is highly resistant to high intensity pain?

A

kappa

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22
Q

where does nalbuphine work?

A

nalbuphine is an agonist-antagonist opioid – agonist at kappa receptors, and an antagonist at mu receptors

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23
Q

three opioid receptors modulate the body’s ability to retain or excrete urine. describe the two

A
  • kappa receptors produced diuresis (increase excretion)

* delta and Mu1 receptors produce urinary retention

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24
Q

which receptors are responsive to endorphins, morphine, and synthetic opioids?

A

Mu1 and Mu2

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25
Q

which receptors are responsive to dynorphins?

A

kappa

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26
Q

which receptors are responsive to enkaphalins?

A

delta

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27
Q

where are the targets of neuraxial opioids?

A

mu receptors in substantia gelatinosa of spinal cord

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28
Q

what kind of pain are neuraxial opioids designed to suppress?

A

visceral pain

29
Q

what are the 4 classic side effects of neuraxial opioids?

A

pruritis, N/V, urinary retention, ventilatory depression

30
Q

what are the dosing recommendations for morphine (IV, epidural, intrathecal)

A

10mg IV, 1mg epidural, 0.1mg intrathecal (1/10 ratio; very hydrophilic)

31
Q

what are the dosing recommendations for hydromorphone (IV, epidural, intrathecal)

A

1mg IV, 0.2mg epidural, 0.04mg intrathecal (1/5 ratio; intermediate hydro-/lipo-philicity

32
Q

what are the dosing recommendations for fentanyl (IV, epidural, intrathecal)

A

100mcg IV, 33mcg epidural, 6-10mcg intrathecal (1/3 – 1/5 ratio; very lipophilic)

33
Q

how well are opioids absorbed?

A
  • well absorbed by many routes

* some have high first pass metabolism (PO)

34
Q

how well are opioid distributed?

A
  • rapidly leave blood compartment for highly perfused areas

* muscle and fat act as a reservoir

35
Q

describe the metabolism of opioids

A
  • converted to polar metabolites then excreted by kidneys
  • morphine-6-glucoronide (4-6x analgesic potency than morphine – morphine is a prodrug)
  • tissue esterases (heroin, remifentanil)
  • normeperidine (demerol)
36
Q

what are the cardiovascular side effects of opioids?

A
  • decreased sympathetic tone
  • decreased BP
  • decreased HR
  • minimal contractility effects
37
Q

what are the cardiovascular side effects of demerol?

A

anti-muscarinic effect (like atropine) – increase HR

38
Q

what are the respiratory effects of opioids?

A
  • respiratory depression due to agonist effect at Mu2
  • dose dependent depression of ventilatory response to CO2
  • increased PaCO2 (almost becomes an anesthetic)
  • decreased RR
  • increased tidal volume
  • decreased minute ventilation
  • cough suppression (dextramethorphan – no analgesia or ventilatory depression)
39
Q

what are the CNS effects of opioids?

A
  • sedation and analgesia vs. euphoria
  • reduces MAC
  • decreased CBF and CMRO2
  • increases ICP with hypoventilation
  • seizures with meperidine use (normeperdine buildup)
  • miosis (edinger-wetphal nucleus of oculomotor nerve – no developed tolerance)
40
Q

describe biliary colic side effect of opioids

A
  • spasm of sphincter of Odi (can present similarly to angina)
  • less with meperidine
  • naloxone relieves pain
  • glucagon 2mg IV reverses
41
Q

how are opioid side effects expressed in the GI?

A
  • N/V
  • constipation
  • delayed gastric emptying
  • biliary colic
42
Q

how are opioid side effects expressed in the GU?

A
  • urinary retention due to increase in tone of ureter and vesicle sphincter
43
Q

how do opioids affect histamine release?

A

increase histamine release – flushing, itching (more with morphine and meperidine)

44
Q

describe side effects observed in the thoracic cavity

A

truncal rigidity

45
Q

for which side effects do pts develop tolerance?

A

tolerance to depression of ventilation

46
Q

what is the onset, peak effect, and duration times of morphine?

A
  • onset: 15-30min
  • peak effect: 45-90min
  • duration: 3-4hr
47
Q

how is morphine metabolized?

A

metabolized via conjugation with glucuronic acid in hepatic, extra hepatic, and kindneys

48
Q

what is the active metabolite of morphine?

A

morphine-6-glucaronide

* accumulation of morphine and metabolite in kidney failure pts leading to prolonged narcosis and ventilatory depression

49
Q

how potent is meperidine compared to morphine?

A

0.1 potency of morphine

50
Q

meperidine peak effect, duration

A
  • peak effect: 5-7min

* duration: 2-4hr

51
Q

describe the local/atropine-like side effects of demerol

A
  • block Na channels

* tachycardia, dry mouth, mydriasis

52
Q

how is demerol most of used?

A

Tx for post op shivering (12.5-25mg)

53
Q

fentanyl peak effect, duration

A
  • peak effect 3-5min

* duration 30-60min

54
Q

how much fentanyl undergoes 1st pass pulmonary uptake?

A

75% (metabolized in lungs, not liver)

55
Q

what characteristic of fentanyl makes it last so long?

A

highly lipid soluble and protein bound

56
Q

which opioid is hemodynamically stable?

A

fentanyl

57
Q

induction dose – fentanyl

A

2-6mcg/kg with a sedative hypnotic

58
Q

what is the infusion rate of fentanyl

A

0.5-5mcg/kg/hr

59
Q

how potent is sufentanil compared to fentanyl?

A

10X as potent as fentanyl (greater affinity for opioid receptor – great for neurosurgery)

60
Q

peak, duration – sufentanil

A

same as fentanyl — peak 3-5min, duration 30-60min

61
Q

what is the dosing of sufentanil?

A
  • 0.3-1.0mcg/kg 1-3min before DL

* 0.5mcg/kg followed by 0.5mcg/kg/hr

62
Q

how potent is alfentanyl compared to fentanyl?

A

1/10 as potent as fentanyl

63
Q

what procedures is alfentanyl good for?

A

anesthetic for RBB, DL

* 5-10mcg/kg provide good analgesia with rapid recovery

64
Q

how potent/long acting is remifentanyl compared to fentanyl?

A

similar potency to fentanyl, short duration (~10min)

65
Q

where is remifentanyl metabolized?

A

plasma and tissue esterases

66
Q

compare dilaudid to morphine

A
  • 8x more potent than morphine but shorter acting (~2hr)
  • more sedation but less euphoria
  • less histamine release
67
Q

what are opioid antagonists useful for?

A

Tx overdose, respiratory depression

68
Q

what is the duration of opioid antagonists?

A

30-45min

69
Q

what is the dose of opioid antagonists?

A

1-4mcg/kg

ANESTHESIA PHARM 2 (4 decks)

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