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pharm III exam 1 > Opioids II > Flashcards

Opioids II Flashcards

1
Q

List the clinical uses of opioids

A
  1. analgesia
  2. acute pulmonary edema
  3. relief of cough
  4. diarrhea
  5. anesthesia
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2
Q

drug interaction: opioid + sedative hypnotics

A
  • increased CNS and respiratory depression
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3
Q

drug interaction: opioid + MAO inhibitors

A
  • high incidence of hyperpyrexic coma
    • meperidine and dextromethorphan are the worst
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4
Q

drug interaction: codeine, oxycodone, and hydrocodone + CYP2D6 inhibitors

A

inhibit metabolism of these compounds to thier active state

  • Fluoxetine is the worst for inhibition
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5
Q

contraindications to using opioids

A
  • use of partial agonist with full agonist
    • can impair analgesia and cause withdrawal
  • head injuries
  • pregnancy: especially at delivery
    • cross placenta barrier -> respiratory depression or drug dependence of fetus
  • impaired pulmonary function
  • impaired hepatic or renal function
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6
Q

MOA of Morphine

A
  • stimulates all opioid receptors: prototype
  • strong agonist : useful in severe pain
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7
Q

why is morphine more effective when injected than taken oraly

A
  • high first pass metabolism
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8
Q

where is morphine metabolized

A
  • liver by CYP2D6
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9
Q

Why should morphine not be given to patients with renal dysfunction

A
  • a major metabolite of morphine can cause adverse effects if it accumulates
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10
Q

Why is Hydromorphone better to use than morphine in patients with renal dysfunction

A

its metabolites don’t accumulate

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11
Q

Why is methadone traditionally used for maintenance treatment for addicts

A
  • long lasting, more slowly absorbed
  • low doses used to prevent withdrawal
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12
Q

MOA of methadone

A
  • stimulates mu receptors
  • block NMDA receptors
  • now commonly used in long term control of pain
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13
Q

MOA of Meperidine

A
  • Mu agonist
    • causes euphoria
  • inhibits NE/5-HT reuptake -> serotonin syndrome with MAOIs
  • blocks muscarinic receptors
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14
Q

adverse effects of Meperidine

A
  • should not be used for more than 48 hours, in high doses, or in renal failure due to accumulation of metabolite normeperidine
    • ​normeperidine -> seizures
  • tachycardia
  • pupil dilation
  • no cough suppression
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15
Q

MOA of Fentanyl

A
  • lipid soluble
  • Very potent
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16
Q

adverse effects of Fentanyl

A
  • high abuse potential
  • truncal rigitidy -> if given rapidly IV
  • metabolized by CYP3A4
17
Q

oxycodone + acetaminophen =

A

percoset

18
Q

oxycodone is metabolized by

A
  • CYP2D6
    • needed to be completely effective
19
Q

MOA of Oxymorphone

A
  • active metabolite of oxycodone, used for moderate to severe pain
    • does not need to be metabolized by CYP2D6
20
Q

hydrocodone + acetaminophen =

A

vicodin

21
Q

hydrocodone requires metabolism by what enzyme for full effect

A

CYP2D6

22
Q

codeine must be metabolized by what to be active

A
  • CYP2D6
  • codeine -> morphine
23
Q

codeine is used mainly for

A
  • cough suppressant
    • doses lower than for analgesia
    • shouldn’t be used in small children
24
Q

MOA of Pentazocine

A
  • kappa receptor agonist
  • Mu receptor partial agonist
25
Q

what is Pentazocine used for

A
  • moderate pain
    • may be less sedating than other opioids
    • Low abuse potential, may be good for addicts
26
Q

adverse effects of Pentazocine

A
  • dysphoria (kappa)
  • may cause withdrawal in patients dependent on opioids
27
Q

MOA of Buprenorphine

A
  • partial agonist on mu and maybe on kappa
    • ceiling to effect-doesn’t cause much euphoria
    • low abuse potential
28
Q

what is Buprenorphine used for

A
  • maintenance treatment of opioid addiction - decreases craving for drug
29
Q

why is Buprenorphine commonly combined with Naloxone

A
  • tablets are formulated together with naloxone (Suboxone), which is not absorbed sublingually; prevents dissolving the tablets in water and injecting the solution IV
30
Q

MOA of Tramadol

A
  • Weak Mu agonist -> mild to moderate pain
  • inhibits NE/5-HT reuptake -> contributes to analgesic effect
31
Q

tramadol + antidepressants lead to

A

seizures

32
Q

tramadol + MAOIs, TCAs, SSRIs may cause

A

serotonin syndrome

33
Q

MOA of Dextramethorphan

A
  • blocks NMDA receptors
  • decreases 5-HT reuptake
  • cough suppressant
  • not an analgesic
34
Q

Dextramethorphan + MAOIs will cause

A

serotonin syndrome

35
Q

DOC for opioid overdose

A
  • Naloxone (Narcan)
    • must be injected -> give until pupils dilate
    • short duration of action (2 hrs)
36
Q

use of Naltrexone

A
  • oral and long acting
  • used in tx of opioid addicts
    • if addict takes opioids, won’t have any effect
  • decreases craving in recovering alcoholics
37
Q

Route of admin Naltrexone

A

PO

pharm III exam 1 (11 decks)

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