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Neuro Pharm Quiz > Opioids Module > Flashcards

Opioids Module Flashcards

1
Q

MOA of Codeine

potency

A
  • full MOR agonist

0. 01

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2
Q

MOA of Morphine

potency

A
  • full MOR agonist

1

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3
Q

MOA of Hydrocodone

potency

A
  • full MOR agonist

1

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4
Q

MOA of Oxycodone

potency

A
  • full MOR agonist

1. 5

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5
Q

MOA of heroin

potency

A
  • full MOR agonist

2

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6
Q

MOA of Buprenorphine

used for

negative effects

when do we give it

A
  • partial MOR agonist (more potent)
  • full kappa and delta antagonist
  • reduces withdrawal symptoms without producing same level of addictive effects
  • more potent and will displace opioids from receptor if taken at the same time precipitating withdrawal symptoms
  • after withdrawal symptoms begin
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7
Q

MOA of Nalbuphine

A
  • partial MOR agonist

- full kappa agonist

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8
Q

MOA of Methadone

potency

used for/benefits

negative effects

A
  • full MOR agonist

1

  • reduce withdrawal symptoms and ease detox
  • long biological half life (24 hours)
  • can be addictive
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9
Q

MOA of Meperidine

potency

A
  • full MOR agonist

0. 1

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10
Q

MOA of fentanyl

potency

A
  • full MOR agonist

100

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11
Q

MOA of Remifentanil

potency

A
  • full MOR agonist

200

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12
Q

MOA of carfentanil

potency

A
  • full MOR agonist

10000

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13
Q

MOA of Butorphanol

A
  • partial MOR agonist

- full kappa agonist

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14
Q

MOA of methylnaltrexone

what does it treat

A
  • neutral MOR antagonist
  • inhibit effects of other opioids through competition for receptor binding
  • opioid induced constipation
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15
Q

MOA of pentazocine

A
  • neutral MOR antagonist

- full kappa agonist

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16
Q

MOA of Naltrexone

used for

A
  • inverse MOR agonist
  • inhibit basal, opioid-independent activity of the receptor
  • treat acute opioid overdoses
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17
Q

MOA of Naloxone

used for

A
  • inverse MOR agonist
  • inhibit basal, opioid-independent activity of the receptor
  • treat acute opioid overdoses
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18
Q

what happens in transduction step of pain

A
  • nociceptors increase rate of depolarization in response to noxious stimulus
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19
Q

what happens in the modulatory step of pain

A
  • descending pathway of nerve impulse modules pain perception
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20
Q

both the ascending and descending pathway intersect where

what is this the site of

A
  • in the dorsal horn of the spinal cord
  • summation of intensity of pain
  • site of opioid action
21
Q

endorphins act on which opioid receptor

A
  • mu
22
Q

enkephalins act on which opioid receptor

A
  • delta
23
Q

dynorphins act on which opioid receptor

A
  • kappa
24
Q

opioids produce analgesia by agonizing receptors in the

A
  • brain and spinal cord

- peripheral nociceptor neurons

25
Q

opioids produce sedation and respiratory depression by acting on receptors in the

A
  • brain
26
Q

opioids produce constipation by acting on receptors in the

A
  • myenteric/submucosal plexus of the enteric nervous system in the GI tract
27
Q

can partial agonists produce full analgesia

A
  • no, but still clinically useful
28
Q

oral administration of opioids subjects them to the ____-

A
  • first pass effect
29
Q

opioids are metabolized by what reactions

what is the product

eliminated by

significance of the product

A
  • phase I/phase II
  • highly polar glucuronidated metabolites
  • eliminated by kidneys
  • can have more potent analgesic effects or more toxicity
30
Q

some opioids can be metabolized into ______ drugs through ______ mediated reactions

which ones

A
  • more potent
  • CYP2D6
  • codeine, hydrocodone, and oxycodone
31
Q

what opioids are okay to use in a patient with renal dysfunction

A
  • fentanyl
  • methadone
  • burprenoprhine
32
Q

MORs are found on the ___-synaptic nociceptor neuron terminal and ____-synaptic cell membrane

A
  • presynaptic nociceptor neuron terminal

- postsynaptic cell membrane

33
Q

MOA of opioid-activated MORs in presynaptic neuron

A
  • inhibit opening of Ca2+ channels during depolarization
  • reduce influx of Ca2+
  • slow release of neurotransmitters
34
Q

MOA of opioid-activated MORs in postsynaptic neuron

A
  • stimulate opening of K+ channels
  • increase K+ efflux
  • hyper polarize the neuron
35
Q

opioid action on descending modulatory pathway

A
  • block release of GABA

- disinhibit modulatory neurons

36
Q

toxicities of acute opioid use

how

A
  • respiratory depression
  • constipation
  • sedation
37
Q

toxicities of chronic opioid use

how

A
  • hyperalgesia - increase sensitivity to noxious stimuli
  • tolerance - inactivated receptor
  • dependence - release dopamine into nucleus accumbens in mesolimbic pathway. (inhibit release of GABA that negatively regulates this process)
  • withdrawal
38
Q

how do opioids cause respiratory depression

A
  • MORs on respiratory control centers of pons and medulla.
  • reduce signaling to diaphragm and intercostal muscles
  • slow rate of breathing
39
Q

how do opioids cause sedation

A
  • bind to MORs in brain and cause sedation
40
Q

how do opioids cause constipation

can be beneficial in patients with

A
  • bind to MORs on myenteric and submucosal plexus in the GI tract which coordination smooth muscle contraction
  • inhibit transmission and reduce GI smooth muscle contraction
  • diarrhea
41
Q

what is cross tolerance

A
  • tolerance to one opioid producing tolerance to others
42
Q

what is opioid rotation

A
  • switch to a different opioid after tolerance develops from previous one
43
Q

peak symptoms of opioid withdraw begin to subside by

A
  • 3-4 days
44
Q

importance of naloxone being administered nasally

A
  • increases rate of absorption

- minimizes onset time

45
Q

Suboxone combines

MOA

how is it given

A
  • buprenorphine with naxolone
  • block effects of drug being abused
  • mitigate symptoms of withdrawal
  • sublingual
46
Q

drugs that inhibit/induce _____ or ____ can have drug reactions with opioids

A
  • CYP3A4/2D6
47
Q

drugs that inhibit CYP3A4/2D6

A
  • cardiac drugs (amiodarone, diltaizem, verapamil)
  • behavioral drugs (bupropion, SSRIs)
  • GI drugs (cimetidine)
  • antibiotics (fluoroquinolones)
48
Q

drugs that induce CYP3A4/2D6

A
  • anticonvulsants (barbiturates, phenytoin)
  • anti-inflammatories (corticosteroids)
  • behavioral drugs (duloxetine)

Neuro Pharm Quiz (5 decks)

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