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Anesthesia Fast Facts > Pain & Opioids > Flashcards

Pain & Opioids Flashcards

1
Q

Semi-synthetic opioids

A
  • chemical modification of the morphine molecule

- heroin (diacetylmorphine), thebaine, oxycodone, hydrocodone, hydromorphone

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2
Q

Synthetic opioids

A

-manufactured by synthesis rather than chemical modification of the morphine molecule

  • morphine derivative: levorphanol, nalbuphine
  • benzomorphan methadone derivatives
  • benzomorphan derivatives: pentazocine
  • phenylpiperidine derivatives: meperidine, fentanyl, alfentanil, sufentanil, remifentanil
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3
Q

Opioid receptors

A

-all 4 are G protein receptor and inhibit adenylate cyclase and cyclic adenosine monophosphate (cAMP) production

Mu-1, Mu-2
Delta
Kappa

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4
Q

Mu receptors

A

Mu 1 - analgesia

Mu 2 - hypoventilation, physical dependence

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5
Q

Generalized effects of exogenous opioids at the Mu-1 receptors include which two of the following? (supraspinal, spinal analgesia, physical dependence, constipation)

A

supraspinal, spinal analgesia

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6
Q

The respiratory depressant effects of the opioid agonists are produced by action at which receptor?

A

Mu2

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7
Q

Which opioid does NOT have an active metabolite? (Fentanyl, Meperidine, Morphine, Oxycodone)

A

Fentanyl

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8
Q

Which opioid receptor is responsible for shivering postoperatively?

A

Kappa

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9
Q

Which opioid receptor is involved in the physical dependence of opioid addiction?

A

Primiarly Mu 2 (also detla)

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10
Q

Of the opioid medications which one has constant clearance and is unaffected by liver or renal disease?

A

Remifentanil

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11
Q

Match opioid receptors with endogenous opioids:

[mu, delta, kappa] to [endomorphins, endorphins, enkephalins, dynorphins]

A

Mu: endomorphins, endorphins, enkephalins

Delta: endorphins and enkephalins

kappa: dynorphins

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12
Q

2 chemical classes of opioid alkaloids?

A
  1. phenanthrenes

2. benzylisoquinolines

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13
Q

Opioid MOA

A
  • Done largely by presynaptic inhibition via Ca++ ch inactivation & reduced Ca++ influx which reduces NT release (Ach, D, NE, SubP).
  • increased K+ conductance (hyperpolarizes and prevents neuronal excitation/propagation)
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14
Q

metabolism & excretion of opioids is via

A

hepatic metabolism for ALL (except remifentanil which is metabolized by non-specific esterases)

renal excretion for ALL (with some biliary, morphine)

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15
Q

CYP enzymes inovlved

A

CYP 2D6, 3A4, 2B6

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16
Q

active metabolite of morphine

A

morphine 6 gucuronide M6G

accounts for about 10% of morphine’s metabolism

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17
Q

Opioid effects: CNS

A

analgesia, sedation, euphoria/dysphoria

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18
Q

Opioid effects: CV

A

decreased tone & vasodilation

bradycardia

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19
Q

Opioid effects: Pulm

A
  • depresses RR and rhythm (slow/deep) primarily through Mu2 in the brainstem
  • decreased responsiveness to hypercarbia
  • decrease cough
20
Q

Opioid effects: ridgiidty

A
  • cause skeletal muscle rigidity, especially thoracic and abdominal muscles (may involve actions with central mu receptors interacting with dopaminergic and GABA pathways)
  • decrease in chest-wall compliance and constriction of pharyngeal and laryngeal muscles can become difficult to ventilate
21
Q

opioid effects: GI

A

PONV
GI constipation or ileus
increase biliary pressure, spasm of sphincter of oddi

22
Q

Naturally occurring opioids

A

morphine

codeine

23
Q

opioid partial agonists or agonist/antagonists

A

buprenorphine
butorphanol
nalbuphine

24
Q

opioid antagonists

A

naloxone
nalmefene
naltrexone

25
Q

synthetic codeine analog

A

tramadol

26
Q

non-narcotic analgesics

A

NSAIDS (ketorolac, ibuprofen)

acetaminophen

27
Q

receptor activation causes presynaptic inhibition of NTs release (what NTs are involved)

A

Ach
Dopamine
norepi
substance P

28
Q

all opioid receptors are what type?

A

G-protein receptors and inhibit adenylate cyclase and cyclic adenosine monophosphate (cAMP) production

29
Q

True/False: naloxone and other opioid antagonists work at all 4 opioid receptors?

A

True

30
Q

Which opioid receptor is responsible for dysphoria and sedation?

A

kappa

31
Q

Which opioid receptors are responsible for miosis?

A

Mu1

Kappa

32
Q

Which opioid receptor is responsible for bradycardia and hypothermia?

A

Mu1

33
Q

Which opioid receptor is responsible for euphoria?

A

Mu1

34
Q

Which opioid receptor is responsible for urinary retention?

A

Mu1

Delta

35
Q

Opioid effects: cutaenous changes

A

flushed, warm, urticaria, puritis

36
Q

Order the context-sensitive half-time for a 4 hr infusion from shortest to longest (alfentanil, fentanyl, remifentanil, sufentanil)

A 
Shortest
1. Remifentanil
2. sufentanil
3. alfentanil
4. fentanyl 
Longest
37
Q

Anesthesia’s uses for opioids

A
  • analgesia
  • blunting SNS response to intubation or surgical stimulation
  • sedation
  • reduces the amount of VA needed for MAC

Meperidine - post-op` shivering

38
Q

Fentanyl IV push dose for analgesia

A

dose: 25-150 mcg
onset: 3-5 min

39
Q

Fentanyl infusion rate

A

1-2 mcg/kg/hr

40
Q

Alfentanil loading dose & maintenance rate

A

loading dose: 35-70 mcg/kg (1500-5000 mcg in 70kg pt)

onset: 1-2 min
maintenance: 0.25-0.5 mcg/kg/min

41
Q

Remifentanil loading dose & maintenance rate

A

loading dose: 1-2 mcg/kg (70-140 mcg in 70kg pt)

onset: 1 min
maintenance: 0.05-0.25 mcg/kg/min

42
Q

Order of onset/peak for bolus injection, fastest to longest(alfentanil, fentanyl, remifentanil, sufentanil)

A 
Fastest
1. Remifentanil
2. alfentanil
3. Fentanyl
4. sufentanil
5. morphine
Longest
43
Q

most common pharmacokinetic interaction in opioid pharmacology?

A

combined IV opioids and propofol

-due to hemodynamic changes induced by propofol and their impact on pharmacokinetic processes, opioid concentrations may be larger when given with continuous propofol

44
Q

most common pharmacodynamic interaction in opioid pharmacology?

A

synergistic interaction that occurs when opioids are given combined with sedatives

  • ex: when given with volatile anesthetics, they reduce the MAC of the VA. (MAC reduction can be substantial, but not complete)
  • can also be given with propofol or other hypnotics
45
Q

effects of increased age on opioids

A

-in general older patients have lower central clearance and higher potency (lower EC50)

Anesthesia Fast Facts (24 decks)

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