Opioid and Non-Opioid Analgesics Flashcards

1
Q

Which analgesics effect transduction?

A
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2
Q

Which analgesics target transmission?

A
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3
Q

Which analgesics target modulation?

A
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4
Q

Which analgesics target perception?

A
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5
Q

The most important site of pain modulation is:

A

the substantia nigra in the dorsal horn

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6
Q

Pain signals are transmitted on a three-neuron pathway:

A

First-order neuron: Periphery to dorsal horn

Second-order neuron: dorsal horn to thalamus

Third-order neuron: thalamus to cerebral cortex

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7
Q

Pain is inhibited when:

A
  1. spinal neurons release GABA and Glycine
  2. The descending pathway releases NE, serotonin, and endorphins
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8
Q

What happens when an opioid binds to its receptor?

A
  1. Adenylate cyclase activity is decreased
  2. cAMP is decreased
  3. Ca conductance is decreased
  4. K conductance is increased (hyperpolarizes the membrane)
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9
Q

In the brain, where are opioid receptors located?

A

Periaqueductal gray
locus coeruleus
Rostral Ventral Medulla

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10
Q

In the spinal cord, where are opioid receptors located?

A

Afferent neurons in the dorsal horn

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11
Q

In the periphery, where are opioid receptors located?

A

Sensory neurons and immune cells

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12
Q

What are the cardiovascular effects of opioid administration?

A

Just bradycardia

The only exception is demerol, because of its atropine-like ring

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13
Q

What are the neurological effects of opioids?

A
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14
Q

What are the cardiovascular effects of opioids?

A
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15
Q

What are the GI effects of opioids?

A
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16
Q

How do opioids impact thermoregulation?

A

They reset the hypothalamic set point, resulting in decreased body temperature

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17
Q

What are the immunologic effects of opioids?

A

Histamine release (morphine, demerol, codeine)

Inhibition of cellular and humoral function

Suppression of natural killer cell function

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18
Q

Tolerance develops to nearly all the side effects of opioids EXCEPT:

A

miosis and constipation. Those are neve attenuated

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19
Q

Rank the opioids in order of potency

A
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20
Q

When does heroin withdrawal begin?

A

Onset 6-18 hrs
Peak 36-72 hours
Duration 7-10 days

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21
Q

Which opioids undergo hepatic biotransformation?

A

All of them except remifentanil

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22
Q

Which opioids have active metabolites?

A

Morphine
Demerol
Maybe hydromorphone

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23
Q

Morphine is conjugated into:

A

Morphine-3-gluconuride
Morphine-6-gluconuride

24
Q

Compared to morphine, is M-6-G more or less water soluble?

A

It is more water soluble, meaning it is less likely to cross the BBB

25
Q

Why are renal patients more prone to complications from morphine?

A

M-6-G accumulates in quantities large enough to cross the BBB

26
Q

Morphine is ______ in the liver

A

conjugated

27
Q

Demerol is ______ in the liver

A

demethylated

28
Q

What metabolite is produced from demerol?

A

Normeperidine, which is about 50% as potent as meperidine

29
Q

What are the side effects of normeperidine?

A

Myoclonus
Seizures

30
Q

Remifentanil is metabolized by:

A

tissue esterases and erythrocytes
NOT PSEUDOchE

31
Q

Remifentanil is always dosed using:

A

LBW

32
Q

Which opioid is associated with anticholinergic side effects?

A

Demerol

It has an atropine-like ring

33
Q

Which opioid receptors does demerol stimulate?

A

mu and kappa

34
Q

Meperidine is the only opioid that ______

A

reduces shivering

35
Q

Meperidine should never be given to patients taking:

A

MAOIs

Can cause serotonin syndrome

36
Q

What is the benefit of alfentanil?

A

It has a rapid onset

37
Q

Why does alfentanil have a rapid onset?

A

It has a pKa of 6.5 and it’s a weak base. This means it exists almost entirely in a non-ionized, lipid-soluble form, which makes it easier for it to cross the BBB

38
Q

Alfentanil is useful for:

A

blunting SNS response to brief, intense stimulation like intubation or a retrobulbar block

39
Q

Which drugs can be used to attenuate hyperalgesia from Remifentanil?

A

Ketamine and Mag

40
Q

Which opioid receptors does remifentanil agonize?

A

Mu

41
Q

Can remifentanil be used in neuraxial anesthesia?

A

NO! it contains glycine, which can cause skeletal muscle weakness

42
Q

Methadone reduces pain through three mechanisms:

A
  1. Mu receptor agonism
  2. NMDA antagonism
  3. MAO reuptake inhibition
43
Q

How does methadone impact ECGs?

A

It can prolong the QT

44
Q

What is the best treatment for muscle stiffness d/t opioid administration?

A

Paralysis and intubation

45
Q
A
46
Q

Name three partial opioid agonists

A

Buprenorphine
Nalbuphine
Butorphanol

47
Q

Which partial agonist can be administered nasally?

A

Butorphanol

48
Q

Which partial agonist can be administered transdermally?

A

Buprenorphine

49
Q

Name two partial agonists that provide BETTER analgesia than morphine

A

Buprenorphine
Butorphanol

50
Q

What is the dose for naloxone?

A

20-40 mcg at a time

51
Q

What is the duration of naloxone?

A

30-45 min

52
Q

What are the side effects of naloxone in the dependent patient?

A

Tachycardia
Pulmonary Edema
Cardiac dysrhythmias
Sudden death

53
Q

What is methylnaltrexone?

A

Its an opioid antagonist that cannot cross the BBB. It can relieve systemic symptoms of opioid use

54
Q

Which opioid antagonist does NOT reverse respiratory depression?

A

Relistor, because it does not cross the BBB

55
Q

Which opioid inhibits nerve conduction?

A

Meperedine, because it’s also structurally similar to LAs

56
Q
A