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Pharm > opioids > Flashcards

opioids Flashcards

1
Q

what are the three opioid receptors?

A

mu, kappa, delta

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2
Q

agonizing mu leads to what body responses?

A

analgesia, respiratory depression, sedation (plus bradycardia, euphoria, and physical dependence)

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3
Q

agonizing kappa leads to what body responses?

A

analgesia and respiratory depression

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4
Q

agonizing delta leads to what body responses?

A

analgesia, respiratory depression, and sedation

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5
Q

what three places are the mu receptors? what does binding cause?

A

CNS, GI, urinary bladder

causes inhibition of ascending pain pathway (alters perception and response to pain)

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6
Q

where are kappa receptors? what does binding cause?

A

dorsal horn of spinal cord

decrease release of substance P

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7
Q

binding of opioid receptors cause what two things?

A

inhibit release of excitatory NT from nerve terminal (dec Ca influx) AND increases amount of K leaving post synaptic cell

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8
Q

7 forms of opioid preparations

A

oral, injectable, rectal suppository, transdermal patch, intranasal spray, buccal transmucosal, PCA

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9
Q

need to remove transdermal patch before what procedure and why?

A

before MRI because can get burns

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10
Q

compare use of MSContin and MSIR oral preps

A

MSContin- slow release which gives longer and more stable pain control but doesnt work fast
MSIR- quick release which gives faster relief for breakthrough pain

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11
Q

intranasal spray is used for what type of relief? what are two advantages?

A

QUICK relief

avoids first pass metabolism and don’t need to give as high of a dose

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12
Q

what are the three types of opioid action on receptors?

A

full agonist, partial agonist, mixed agonist/antagonist

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13
Q

a full agonist binds to what receptor? produces what kind of response?

A

binds to mu receptor and produces a maximal response

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14
Q

describe analgesia effect with full agonist

A

NO ceiling effect- can keep increasing dose to increase pain relief
stop when analgesia is reached or dose limiting side effects are reached

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15
Q

a partial agonist binds to what receptor? and produces what type of response?

A

binds to opioid receptor and produces a less-than-full response when fully occupying the receptors

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16
Q

how do mixed agonist/antagonists work?

A

drug acts as full agonist but antagonist binds to receptors as well (without activation) to prevent agonist from binding = LESS THAN FULL EFFECT

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17
Q

full agonist medications (12)

A 
Codeine
Morphine
Hydrocodone
Hydromorphone
Oxycodone
Oxymorphone
Methadone
Meperidine/Demerol
Fentanyl
Sufentanyl, alfentanyl, remifentanyl (RAS-nyls)
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18
Q

what is our partial agonist drug?

A

buprenorphine

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19
Q

tramadol is a synthetic analog of what drug? it is a weak morphine receptor agonist with ______ and ______. what level of controlled substance?

A

codeine; NET and SERT; 4

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20
Q

what can tramadol cause in some patients?

A

cause or exacerbate seizures (esp people who are already taking meds that lower seizure threshold- TCAs, SSRI, MAOI

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21
Q

Nucynta is what type of receptor agonist and what type of inhibitor?

A

opioid agonist and NE reuptake inhibitor

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22
Q

what significant ADR can you get while using Nucynta with an MAOI?

A

serotonin syndrome (too much serotonin in body)- don’t use within 14 days of taking MAOI

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23
Q

what can having no ceiling effect cause?

A

respiratory depression

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24
Q

how do you calculate total daily dose of opioids? 3 steps

A

1) . determine total amount of EACH opioid taken per day
2) . multiply each dose by conversion factor to get MME
3) . add MMEs together

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25
Q

above 50 on MME score means patient is at an increased risk of what?

A

respiratory depression

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26
Q

how to dose opioids when stopping use?

A

TAPER- avoid ADRs and seizures this way

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27
Q

oral opioids are metabolized how? how does this impact dose?

A

significant first pass effect for oral opioids (this VARIES per person)- important because oral dose might be a lot higher than parenteral

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28
Q

describe distribution for oral opioids

A

rapidly leave blood compartment and localize in highly perfused tissues (LARGE volume of distribution)

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29
Q

what three forms of opioids are absorbed well?

A

IM, SQ, PO

30
Q

morphine is metabolized to what 2 things?

A

M3G and M6G

31
Q

Hydromorphone is metabolized to what?

A

H3G

32
Q

what two metabolites have neuroexcitatory properties and can cause seizures? what pt pop do you need to watch these in?

A

M3G and H3G; watch in renal failure (CNS side effects) pts or pts on morphine/hydromorphone for a LONG time

33
Q

what does M6G accumulation cause?

A

over-sedation and respiratory depression

34
Q

Meperidine becomes what metabolite?

A

normeperidine

35
Q

what does normeperidine cause?

A

TOXIC metabolite- seizures in patients with renal failure, elderly, or on a high dose for a long time

36
Q

oxymorphone goes through what type of metabolism?

A

phase 2- converts drug into more water soluble INACTIVE metabolites

37
Q

CNS effects that occur when stimulating opioid receptors (6)

A

1) . euphoria
2) . sedation without amnesia
3) . dose related resp depression with inc PCO2 (inc cerebral pressure)
4) . cough suppression with codeine
5) . Miosis (pupil constriction)- no tolerance
6) . nausea/vomiting activation of chemoreceptor zone

38
Q

how does cough suppression with codeine use lead to airway obstruction?

A

other opioids may allow accumulation of secretions so by decreasing cough, secretions could block airway

39
Q

what do you always want to make sure of in a pt who is taking codeine?

A

that they can metabolize it into morphine

40
Q

in what two cases can opioids affect BP?

A

if pt has CV disease or in a hypovolemic state, opioids can cause blood vessel dilation and hypotension

41
Q

what effect does meperidine have on CV system?

A

binds to M2 receptor as an antagonist and increase HR

42
Q

what opioid receptor causes constipation when activated?

A

MU

43
Q

opioid receptor activation causes what in pts with gallbladder dz?

A

contraction of biliary smooth muscle, increasing pain

44
Q

opioids have what effect on the bladder?

A

increase bladder tone and can lead to urinary retention

45
Q

opioids can have what effect on the uterus?

A

it can decrease uterine tone and potentially prolong labor (still used tho)

46
Q

opioids in what form can cause pruritis?

A

parenteral- due to histamine release

47
Q

tolerance of opioids develops how fast?

A

in 2-3 weeks if chronically exposed

48
Q

what three ADRs of opioids do you never develop tolerance to?

A

miosis, seizures, and constipation

-tolerance to analgesia and other effects

49
Q

what are four opioid constipation treatments?

A

relistor, movantik, symproic, entereg

50
Q

how does opioid rotation work for tolerance?

A

switch pt off current opioid to different one AND at a lower dose

51
Q

what two things will make opioid withdrawal worse?

A

higher the dose and longer the pt has been taking it

52
Q

which class of opioids are more addictive?

A

full agonists

53
Q

pregnant women dependent on opioids should switch to what two specific types?

A

buprenorphine or methadone

54
Q

what are four pt populations who opioids are contraindicated in?

A

1) . Head injuries- opioids inc PCO2 by inc cerebral blood flow
2) . Pregnancy
3) . COPD/lung dz- opioids dec resp drive
4) . hepatic/renal impairment (accumulation of metabolites)

55
Q

always prescribe what with a benzo prescription?

A

narcam (or other antagonist)

56
Q

5 drugs classes that increase respiratory depression when used with opioids

A

alcohol, general anesthetics, phenothiazines, benzos (Ativan/valium), TCAs

57
Q

avoid what type of drugs with opioid use so that you don’t get urinary retention or constipation

A

anticholinergics

58
Q

which drugs increase risk for serotonin syndrome?

A

MAO inhibitors, methadone, meperidine, fentanyl, nucynta

59
Q

WHO ladder-
Mild pain
moderate pain
severe pain

A

mild- non opioid (Tylenol, aspirin, NSAID), +/- adjuvant
moderate- opioid (codeine/tramadol), +/- non opioid, +/- adjuvant
severe- opioid (morphine/fentanyl), +/- non opioid, +/- adjuvant

60
Q

Acute pain management: what to use for
mild-moderate pain
localized pain
severe pain

A

mild-moderate: nonopioids- asp, Tylenol, NSAIDs

localized: topical (diclofenac gel or lidocaine)
severe: immediate release opioids ONLY ( lowest effective dose and no more than 7 days)

61
Q

how to treat chronic non cancer pain

A

use non pharm tx first (PT, acupuncture, chiropractor, CBT) and then agents for acute pain until pain is relieved

62
Q

what do you give pts with chronic cancer pain?

A

FULL AGONISTS- not worried about addiction in these people; inc dose if tolerance is developed; give immediate release products for breakthrough pain

63
Q

how to tx neuropathic pain (4)

A

1) . antidepressants- TCAs, SNRIs
2) . antiepileptics- gabapentin, pregabalin, zepines
3) . topicals- lidocaine, diclofenac
4) . opioids if nothing else works

64
Q

what opioid might you use with acute pulmonary edema?

A

morphine (MONA-B)- decreases SOB (usually Lasix is 1st line)

65
Q

what opioid should you use if pt is having acute pain from an MI?

A

morphine

66
Q

should Plavix be taken with morphine?

A

no, decreases Plavix levels so patient would clot faster

67
Q

how do you use opioids for cough/diarrhea? what two agents should be used?

A

at much lower doses (not like pain doses); dextromethorphan (OTC cough suppressant) or diphenoxylate paired with atropine for diarrhea

68
Q

how long do opioid antagonists take to work? what are our two agents?

A

1-3 minutes; naloxone and naltrexone (revia/vivitrol)

69
Q

naltrexone blocks what opioid and its effects?

A

heroin effects for up to 48 hours

70
Q

opioids are not prescribed to people younger than….

A

18 years old

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