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pharmacology > opiods > Flashcards

opiods Flashcards

1
Q

what are the 4 basic parts to the pathophys of pain

A
  1. transduction
  2. transmission
  3. modulation
  4. perception
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2
Q

what are the 3 receptor families that opiod receptors elicit effects on?

A

mu, kappa and delta

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3
Q

what does agonizing mu (u) receptors do?

A

Agonizing leads to analgesia, bradycardia, sedation, respiratory depression, euphoria, and physical dependence

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4
Q

what does agonizing kappa (k) receptors do?

A

Agonizing leads to analgesia and respiratory depression

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5
Q

what does agonizing delta (d) receptors do?

A

Agonizing leads to analgesia, respiratory depression, and sedation

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6
Q

Analgesia is produced when agents act as agonist on the three opioid receptors to inhibit the transmission of what?

A

nociceptive input and the perception of pain

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7
Q

what is the main MOA of opiods in regards to the mu opiod receptor?

A

Bind to mu opioid receptors in the

-CNS, GI TRACT and BLADDER causing inhibition of ascending pain pathway altering the perception of and response to pain

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8
Q

what are opiod receptors MOA in regards to kappa and delta receptors (less important that mu receptor MOA) ?

A

kappa- act in dorsal horn of spinal cord, inhibit substance P release
delta- inhibit release of excitatory neurotransmitters from nerve terminal

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9
Q

what is the benefit/downsides of transdermal patch preparation of opiod?

A

better longterm pain control but takes longer to work

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10
Q

benefit of using intranasal prep of opiod?

A

avoid 1st pass and dont need as high of a dose

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11
Q

what is the difference between a full and partial opiod agonist ?

A

full: no clinically relevant max response (no ceiling effect) - as dose is raised, analgesia effects increase until analgesia is achieved OR dose-limiting side effects occur
partial: produces less than a max response when fully-occupying receptors (ceiling effect)

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12
Q

what is a mixed agonist/antagonist?

A

Drug acts as a full agonist, but antagonist component binds to receptor without activating it to prevent increased binding of agonist. (ceiling effect)

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13
Q

what is a Naturally occurring opioid that is weak analgesic compared to morphine?

A

codeine

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14
Q

what is codeine used for?

A

use low for anti-tussive, then at higher doses for mild-moderate pain

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15
Q

codeine is contraindicated in children under age ____ or undergoing what procedures?

A

18

tonsillectomy/adenoidectomy

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16
Q

what do we need to worry about with the metabolism of codeine?

A

codeine is converted to morphine by CYP2D6…
rapid metabolizers: convert codeine to higher than usual levels of morphine causing toxicity

poor metabolizers: who when taking CYP2D6 inhibitors (ex. Fluoxetine) the cannot convert codeine to morphine and may not experience analgesic effect

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17
Q

what is a Semi-Synthetic opioid (means we tweaked a naturally occuring one and manufactured it) that is metabolized by CYP2D6 to hydromorphone?

A

hydrocodone (loratab)

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18
Q

what is the absorption and metabolism of morphine?

A

good abs, extensive 1st pass metabolism

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19
Q

what patient population do you need to be careful prescribing morphine for?

A

patients with renal insufficiency because of accumulation of toxic metabolite
(Patients have agitation, confusion, & delirium)

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20
Q

what are “abuse deterrent formulations” of morphine and oxycodone?

A

formulations that, when crushed/dissolved for injection either illicit NO EUPHORIC effects or illicit ADVERSE effects

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21
Q

what kind of drug is hydromorphone? strength compared to morphine?

A

semi-synthetic opiod, several times more potent than morphine (more lipophilic = faster abs)

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22
Q

what are the different formulations of hydromorphone?

A

IV, rectal, PO (short and long acting)

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23
Q

what would be a safer choice than morphine for someone with renal insufficiency?

A

hydromorphone

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24
Q

fentanyl is ___ times more powerful than morphine

A

100

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25
Q

Transdermal fentanyl should only be started after what?

A

Transdermal should only be started after initial titration with a short-acting opioid

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26
Q

exposing the fentanyl patch to heat (heating pad, exertion - exercise, or high fever) could increase risk for what?

A

increase release of drug and risk for respiratory depression

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27
Q

what is the proper disposal of fentanyl patch?

A

fold in half and flush

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28
Q

what formulations are there for oxycodone?

A

only oral

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29
Q

what kind of drug is oxycodone? compared to morphine?

A

semi-synthetic derivative of morphine, 1.5 times more powerful than morphine

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30
Q

hydrocodone and oxycodone are both often combined with what for acute pain?

A

acetaminophen

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31
Q

oxycodone for chronic pain?

A

extended release formulation

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32
Q

what kind of drug is oxymorphone? strength compared for morphine?

A

semi-synthetic opiod, metabolite of oxycodone

  • orally: 3 times more potent than morphine
  • IV : 10 times more potent than morphine
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33
Q

what is the 1/2 life of methadone? why is this significant?

A

very long, up to 5 days.

- Repeated doses can lead to accumulation of CNS depression without close monitoring during titration period

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34
Q

what do we need to know about switching from another opioid agonist to methadone?

A

NEEDs to be done by specialist b/c equianalgesic dose of methadone is not well established in opioid-tolerant patients

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35
Q

in addition to the accumulation –> CNS depression, what else might be a concern with dose-related effects of methadone?

A

dose-related QT prolongation

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36
Q

how often do you give methadone for chronic pain? for drug abuse withdrawal?

A

chronic pain: every 8 hours (great 1st line for cancer pain)
drug abuse: once daily

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37
Q

why is meperidine a “least favorite” drug of Dr. Cleveland?

A

Has metabolite, normeperidine (VERY TOXIC), with a 15-30 hour ½ life
extra info:
- CNS effects (if renal failure, elderly or on for a long time)
-antimuscarinic effects (pupils dilate & tachycardia)
- encephalopathy and death: If recent use of MAOI

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38
Q

meperidine should ONLY (if at all) be used when?

A 
short term (24-48 hrs), moderate-severe acute pain
- (rapid onset of axn and short acting)
39
Q

what are the 2 natural opiods?

A
  • codeine converted to morphine

- morphine

40
Q

what are the 4 semi-synthetic opiods?

A
  • hydrocodone converted to hydromorphone
  • hydromorphone
  • oxycodone converted to oxymorphone
  • oxymorphone
41
Q

what are our two mixed-mechanism opiod drugs?

what does this mean?

A
  1. tramadol
  2. tapentadol
    - these both target mu receptor and norepi and/or serotonin receptors as well.
42
Q

what is the MOA of tramadol?

A

mixed mechanism: Synthetic codeine analog

Weak morphine receptor agonist with NET and SERT activity

43
Q

what are the ADRs of tramadol? what are the upsides?

A
  • exacerbate seizures

- BUT less respiratory depression and constipation than other opiods

44
Q

what drugs lower seizure threshold? (maybe weeds)

A

TCAs (i.e. amytriptyline), SSRI, MAOI

anti-depressants

45
Q

what is the MOA of tapentadol?

A

mixed mechanism: Opioid receptor agonist and a norepinephrine reuptake inhibitor

46
Q

whats the one ADR we need to worry about with tapentadol?

A

serotonin syndrome (dont use with or w/on 14 day use of MAOI)

47
Q

what is the one partial agonist opioid drug?

A

buprenorphine : Drug binds to and activates opioid receptor to produce less than a full response when fully occupying their receptors

48
Q

what are the two uses of buprenorphine?

A

chronic pain and opiod use disorder

49
Q

opioid dosing, which will generally have higher dose- IV or oral?

A

oral

50
Q

30mg of oral morphine = ___ mg of hydrocodone = ___ mg of oral codeine = ____ (bl/buccal) of fentanyl

A

30mg hydrocodone
200mg - codeine
0.2 (sl/buccal) -fentanyl

51
Q

how do you calculate the total daily dose of an opioid? what is the goal to keep it under?

A
  1. determine total daily amount of each opioid the person takes
  2. you convert each drug to the MME (morphine mg equivalent) ( multiple each by the conversion factor)
  3. add together
    GOAL: under 50 total
    definitely keep under 120 (dangerous level!)
52
Q

opiods: all formulations have good abs, but which has significant first pass metabolism? why is this important to know?

A

abs well in all forms: IM, SQ or PO
1st pass: oral
- oral dose may need to be much higher than parenteral
- but amount of 1st pass varies from individual to individual

53
Q

what is the distribution like for opiods?

A

LARGE volume of distribution
( they rapidly leave the blood compartment and localize in high concentrations in highly perfused tissue (brain, lungs, liver, kidneys & spleen)

54
Q

Morphine is metabolized to ____ and ____

Hydromorphone is metabolized to ___

A

morphine: M3G & M6G
hydromorphone: H3G

55
Q

morphine metabolite- M3G and hydromorphone metabolist H3G can both accumulate and cause what ADRs? what patients do we need to worry about this with?

A

neuroexcitatory & potential to cause seizures

(renal failure patients)

56
Q

morphine metabolite M6G can accumulate and cause what?

A

oversedation & respiratory depression

57
Q

the metabolite of merpiridine, normepiridine can cause what major ADR?

A

Can cause seizures in patients with renal failure , elderly or on a high dose for a long time

58
Q

what is the only opiod that doesnt go through phase 1 CYP450? what does it go through? (maybe weeds)

A

oxymorphone: only goes through phase 2 (gluconization)

59
Q

dose-related respiratory depression with opioids, why is this a major concern if someone has had head trauma?

A

Dose related respiratory depression leading to increased PCO2 (when you have this buildup = vasodilation. if head trauma… increase in cerebral pressure)

60
Q

what are the 6 CNS effects of opioid-receptor stimulation?

A
  1. euphoria
  2. sedation w/out amnesia
  3. respiratory depression
  4. cough suppression (codeine)
  5. miosis
  6. N/V activation of chemoreceptor trigger zone
61
Q

possible peripheral effects of opioid receptor activation

first 2 important, last 4 less important

A
  1. cardiovascular - possible HYPOtension
  2. GI- mu receptor- constipation
  3. gallbladder - smooth muscle contraction- pain with GB disease
  4. GU- urine retation
  5. Uterus- potentially prolong labor
  6. skin- urticaria, pruritis, flushing & warm skin (histamine release)
62
Q

what are the possible cardiovascular effects of opioids? what is the one outlier for these effects?

A

usually well tolerated unless someone has CV stress

  • if CV disease or is hypovolemic narcotics –> blood vessel dilatation & hypotension
  • outlier : Meperidine (anticholinergic effects) –> tachycardia
63
Q

tolerance usually begins to develop after ___ - ___ wks of chronic therapeutic narcotics

A

2-3 weeks

64
Q

what is the progression of tolerance? (maybe weeds)

A

reduced ADRs –> shorter duration of analgesia –> decrease effectiveness with each dose

65
Q

Tolerance occurs to analgesic effects and all other effects EXCEPT ____, _____ , and ______

A

miosis, seizures & constipation

- these effects will ALWAYS be there

66
Q

4 opioid-induced constipation txts (weeds)

A

Methylnaltrexone (Relistor)
Naloxegol (Movantik)
Naldemedine (Symproic)
Alvimopan (Entereg)

67
Q

what is opioid rotation?

A

if experiencing decreasing effectiveness of one opioid analgesic regimen they are “rotated” to a different opioid analgesic (to prevent tolerance and dose escalation)
=significantly improved analgesia at a reduced over-all equivalent dosage

-changed drugs = change receptor types and therefore get greater affect from the new receptors

68
Q

physical dependence with opiods: phase 1 (timeline- hours without the drug, and effects)

A

up to 8 hrs

-anxiety and drug craving

69
Q

physical dependence with opiods: phase 2 (hours without the drug and effects)

A

8-24 hours

  • anxiety & insomnia
  • GI upset
  • rhinorrhea & diaphoresis
  • mydriasis (dilation of pupil)
70
Q

physical dependence with opiods: phase 3 (timeline- hours without the drug and effects)

A

up to 3 days

  • tachycardia, hypertension
  • N/V, diarrhea
  • fever, chills
  • seizure, tremors, muscle spasm
71
Q

taking someone off an opioid you want to taper __% at a time (maybe weeds)

A

10%

72
Q

All opioids are controlled (scheduled) drugs…

full vs partial agonist (which is more addictive, what is the correlating schedule) ?

A 
Full agonists tend to be more addictive (higher schedule, lower number, 2) 
partial agonists (lower schedule, high number 3 or 4)
73
Q

Pregnant women dependent on opioids should switch to

______ or ______

A

buprenorphine or methadone

74
Q

increased risk of respiratory depression with opioids + what other drugs? (maybe weeds)

A

Alcohol, general anesthetics, phenothiazines (anti-emetic promethazine), benzodiazepines (xanax, adivan, etc), TCA

75
Q

opioid withdrawal for mothers/newborns is associated with what?

A

spontaneous abortion and premature labor… better to taper them both off.

76
Q

which 5 drugs have increased risk of serotonin syndrome with MAOIs ? (maybe weeds)

A

tramadol, tapentadol, methadone, meperidine, and fentanyl

77
Q

which 7 drugs have CYP34A metabolism substrate? (maybe weeds)

A

Buprenorphine, fentanyl, hydrocodone, meperidine, methadone, oxycodone, and tramadol

78
Q

which 3 drugs have CYP2D6 metabolism substrate? (maybe weeds)

A

Codeine, methadone, hydrocodone

79
Q

WHO analgesic ladder: mild pain

A

non-opiod (acteaminophen (i.e. paracetamol), ASA, NSAID)

+/- adjuvant

80
Q

WHO analgesic ladder: mild to moderate pain

A

opioid (codeine, tramadol, etc,)
+/- non-opiod
+/-adjuvant

81
Q

WHO analgesic ladder: moderate to severe pain

A

opioid (morphine, fentanyl, etc,)
+/- non-opiod
+/-adjuvant

82
Q

what agents may you use for localized pain? (maybe weeds)

A

Topical agents – diclofenac gel/patch or lidocaine creams/patch

83
Q

what kind of opioids are you using for severe pain? what dose for how long?

A

Immediate release opioids
Lowest effective dose for shortest duration of time
Preferred less than 7 days

84
Q

when would you use opioids for neuropathic pain?

A

only if antiepileptics (“gabas and carbas” , antidepressants and topicals dont work

85
Q

why might you use morphine for pulmonary edema? what would you try first?

A

IV morphine decreases SOB by decreasing anxiety, dyspnea, preload and afterload
Works well if having an MI with chest pain & pulmonary edema
*try loops (furosemide) first, but if they still have pain then add morphine

86
Q

if a patient HAS to have MME over 50, what else might you do to prevent ADRs? (maybe weeds)

A

add opioid antagonist

87
Q

txt of diarrhea, diphenoxylate combined with ______ to prevent addiction (weeds)

A

atropine

88
Q

what is naloxone (narcan) used for?

A

to save someone who ODed. Bind to but do not stimulate the narcotic receptor and end up blocking effects of other agonists

89
Q

what if you give narcan to someone who doesnt have an opioid in the system?

A

nothing happens, it just sits on the opiod receptor and does nothing

90
Q

how long does it take narcan to work?

A

1-2 minutes (fast acting)

91
Q

what is the half life of narcan? why is this significant?

A

Half life - 2 hours

May wear off before all opioids metabolized – patient may relapse

92
Q

what are the formulations for narcan? why?

A

naloxone- undergoes 1st pass metabolism so it NEEDS to be intranasal or IV

93
Q

what is the difference between naloxone (narcan) and naltrexone?

A

naltrexone: longer DOA, up to 48 hours. used for maintenance programs to block heroine effects

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