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PHARM II > Opiates, Opioids > Flashcards

Opiates, Opioids Flashcards

1
Q

Opiates are made from ___

A

plants

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2
Q

Opioids are made from ___

A

labs

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3
Q

Active compounds of poppies (2)

A

Morphine, codeine (prodrug of morphine)

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4
Q

what was soldier’s disease?

A

opium abuse

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5
Q

opioid MOA

A

opioid receptor agonist:

  • block release of pain neurotransmitters from nociceptive fibers (glutamate, substance P, and calcitonin gene-related peptide)
  • activate presynaptic receptors on GABA neurons (inhibit GABA release)
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6
Q

morphine MOA

A

Mu agonist

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7
Q

where are Mu receptors located?

A

primarily brainstem and medial thalamus

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8
Q

what is subtype Mu1 associated w/?

A

Mu1 related to analgesia, euphoria, and serenity

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9
Q

what is subtype Mu2 associated w/?

A

Mu2 is related to respiratory depression, pruritus, prolactin release, dependence, anorexia, and sedation. These are also called OP3 or MOR (morphine opioid receptors).

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10
Q

where are kappa (OP2, KOR) located?

A

limbic and other diencephalic areas, brain stem, and spinal cord

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11
Q

delta receptors, located mostly in the brain, are associated w/ what?

A

not well studied, maybe psychomimetic and dysphoric effects

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12
Q

name some full opioid agonists

A 
Morphine
Fentanyl
Hydromorphone
Codeine
Oxycodone
Methadone 
Heroin
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13
Q

name 2 opioid partial agonists

A 
Buprenorphine
Butorphanol (Stadol)
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14
Q

name 2 opioid antagonists

A

Naloxone (Narcan)

Naltrexone

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15
Q

name a combo opioid partial agonist/antagonist

A

Suboxone (buprenorphine + naloxone)

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16
Q

name some short-acting opioids

A 
Codeine
Hydrocodone 
Hydromorphone (Dilaudid)
Morphine (MSIR, Roxanol)
Oxycodone
Oxymorphone (Opana)
Fentanyl (Actiq)
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17
Q

list some uses for short-acting opioids

A

Acute pain
Incident pain
Breakthrough pain
Activity (PT, travel)

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18
Q

list some long-acting opioids

A 
Fentanyl (transdermal)
Levorphanol
Methadone
Morphine (MS Contin, Kadian, Avinza)
Oxycodone (Oxycontin)
Oxymorphone (Opana ER)
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19
Q

what are some uses for long-acting opioids?

A

Chronic pain

Moderate to severe pain

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20
Q

DEA scheduling 1-5 is ___ to ___ addictive

A

most to least

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21
Q

opioid ADRs

A 
Sedation, lethargy
Constipation
Respiratory depression
N/V
Pruritus/urticaria (direct histamine response, can also cause bronchospasm)
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22
Q

triad of opioid OD

A

Miosis
Loss of consciousness
Respiratory depression

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23
Q

opioid OD antidote

A

naloxone (Narcan)

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24
Q

what is something that can exacerbate and opioid OD?

A

EtOH (or other CNS depressants)

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25
Q

does morphine cross the BBB?

A

yes

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26
Q

T/F there are a lot of drug int’s w/ morphine

A

False

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27
Q

morphine ADRs

A 
Direct histamine release
Respiratory depression
Orthostasis
Constipation
N/V
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28
Q

is codeine a strong or weak Mu agonist?

A

weak

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29
Q

when codeine is metabolized to morphine, it’s potency is ___% that of morphine

A

50%

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30
Q

codeine metabolism

A

CYP 2D6 substrate
Inhibited by bupropion, cimetidine, celecoxib, cocaine
Warning for ultra-rapid metabolizers (nursing infants)

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31
Q

Oxycodone (roxicodone, oxycontin, percocet, etc.) is active at what receptors?

A

mu and kappa receptors

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32
Q

what enzyme metabolizes oxycodone?

A

CYP 2D6

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33
Q

fun facts about oxycodone

A

High potency analgesia
t1/2 = 2.5 - 3 hrs
Highly abused

34
Q

what is the most commonly used opioid?

A

hydrocodone

35
Q

T/F, hydrocodone has weak activity at mu receptor

36
Q

what enzyme metabolizes hydrocodone?

A

CYP 2D6 (to hydromorphone)

37
Q

name some combo hydrocodone meds

A

hydrocodone/acetaminophen (Lortab, Lorcet, Vicodin)

Hydrocodone/ibuprofen (Vicoprofen)

38
Q

Hydromorphone (Dilaudid, Exalgo) works at which receptors?

A

mu and delta receptors

39
Q

T/F, hydromorphone is more potent than morphine

40
Q

Oxymorphone (Opana) is ___ x more potent than morphine

41
Q

T/F, oxymorphone is a P450 drug

42
Q

name 2 opioids that are NOT metabl by 450

A

oxymorphone & hydromorphone

43
Q

Fentanyl (Actiq, Duragesic) is a strong/weak mu agonist

44
Q

fentanyl is __ x more potent than morphine

45
Q

what enzyme metabolizes fentanyl

46
Q

what do we worry about for the fentanyl transdermal patch?

A

heat - causes dose dumping

47
Q

Can you give fentanyl to a patient with a codeine allergy?

A

they are structurally different, so theoretically, yes

48
Q

can you reverse effects of meperidine (demerol) w/ narcan?

49
Q

meperidine (demerol) is a neurotoxic metabolite that can cause what?

A

Anxiety, tremors, seizures

50
Q

pts taking meperidine should avoid taking what?

A

antcholinergics & MAOIs

51
Q

Propoxyphene (Darvon, Darvocet) is/is not reversible w/ narcan

A

is; can cause neuro & cardiotoxicity

52
Q

methadone MOA

A

NMDA antagonist, Serotonin-norepinephrine reuptake inhibitor (SNRI) - Neuropathic pain

53
Q

methadone has a long half-life because it is

A

highly lipophilic

54
Q

serious ADR of methadone

A

cardiotoxicity; torsades des pointes

titrate slowly

55
Q

metab enzymes of methadone

A

CYP3A4 and 2D6

56
Q

buprenorphine MOA & use

A

Mu receptor partial agonist, Kappa receptor antagonist
Used for opioid/heroin addiction
(3A4 metab)

57
Q

buprenorphine ADR

A

Sedation
N/V
Dizziness, HA
Respiratory depression

58
Q

Butorphanol (Stadol)

Levorphanol general info

A

Used for moderate to severe pain
Respiratory depression
Euphoria
Typical opioid ADRs

59
Q

naloxone (narcan) ADRs

A

headache, myalgia, increased B/P, opioid withdrawal

60
Q

naloxone (narcan) MOA, ind

A

mu receptor antagonist (admin IM, subQ, IV, intranasal)
Reverses respiratory depression, sedation, hypotension
(Works in 2 – 5 min, Lazarus effect)

Used as a reversal agent for opioid OD

61
Q

Tramadol (Ultram, Ultracet, Ryzolt, Rybix) MOA

A

Synthetic codeine analog
Weak Mu receptor agonist
Inhibits NE and 5HT uptake (SNRI)

62
Q

Tramadol (Ultram, Ultracet, Ryzolt, Rybix) warning

A

Warning for seizure risk at recommended and increased doses (higher incidence with SSRIs, TCAs, opioids, MAOI)

63
Q

Tramadol (Ultram, Ultracet, Ryzolt, Rybix) serious ADRs

A

Suicide risk

Serotonin syndrome risk

64
Q

Tramadol (Ultram, Ultracet, Ryzolt, Rybix) ind

A

As effective as morphine for mild to moderate pain, labor pain - less effective for severe or chronic pain

65
Q

Tramadol (Ultram, Ultracet, Ryzolt, Rybix) ADRs

A

Dizziness, vertigo, nausea, constipation, headache, somnolence, vomiting, pruritus
Supposedly less respiratory depression than morphine

66
Q

Tramadol (Ultram, Ultracet, Ryzolt, Rybix) drug int

A

CYP2D6 and CYP3A4 inhibitors
Serotonergic drugs
Carbamazepine

67
Q

Tapentadol (Nucynta, Nucynta ER) gen info

A

Mu opioid agonist, NE reuptake inhibitor
1st opioid specifically approved for diabetic neuropathy
Stronger than tramadol
No P450 metabolism
Potentially fatal if taken with EtOH
DEA CSA: CII
Same drowsiness/dizziness as oxycodone (less N/V and constipation)

68
Q

opioid conversion guidelines

A

Calculate 24 hr total dose
Divide by dosing schedule
Reduce dose by 30% - 50%
Titrate to goal

69
Q

warning signs of opioid addiction/abuse

A

Early refills
Requesting higher doses
Prescriber hopping

70
Q

define opioid addiction

A

Use of medication outside normally accepted standard for the drug
Cravings and preoccupation with the drug
Loss of control of use
phys vs psych

71
Q

opioid dependence parameters

A

> 3 behaviors over a 12-month period

72
Q

signs & sx of opioid withdrawal

A 
Mood lability -> irritability, anxiety, restlessness
Chills, sweating
Abdominal pain, nausea, diarrhea
Sneezing, rhinorrhea, dilated pupils
Muscle weakness, pains
Insomnia
73
Q

time line of opioid withdrawl

A

8-16 hrs after last dose (peak 2 – 4 days)
resolves 7 – 14 days
Not life-threatening

74
Q

red flags of dependency/addiction

A

post-op
requesting specific med/increased dose
don’t want PE, testing

75
Q

what is the CAGE questionnaire used for?

A

alcohol & drug dependency quick eval

76
Q

opioid dependence tx

A

Detoxification (necessary for long-term abstinence)
can be slow (tapering via methadone) or rapid (via reversal med or d/c of opioids; naltrexone/buprenorphine, clonidine, anti-diarrheal, NSAIDs, muscle relaxants)

77
Q

goals of opioid withdrawal tx

A

Prevent or reduce withdrawal symptoms
Prevent or reduce cravings
Avoid relapse
Restore normal physiological functions caused by opioid dep.
Improve impairments created by opioid dep

78
Q

non-pharm withdrawal tx

A

Support groups (Narcotics Anonymous), psychotherapy, pain contracts, TROSA, family counseling

79
Q

pharm withdrawal tx

A

Methadone
Buprenorphine
Naltrexone

80
Q

2016 CDC Chronic Pain Guidelines when pain lasts > 1 yr

A

Nonopioid & nonpharm tx preferred
Consider opioids when benefit outweigh risk
Est tx goals before starting opioids
Discuss risks & realistic benefits
Start with IR opioids & lowest effective dosage (3 – 7 days for acute pain)
Evaluate treatment q 1-4 wks after starting or increasing dose; if dosing stable, evaluate q3 months
If harm > benefit, taper and d/c
Evaluate risk for harms
Sleep disorders, pregnancy, renal/liver insufficiency, 65 or older
Review history of controlled substance prescriptions
Urine drug testing prior to initiation and annually thereafter
Avoid concomitant use of BZDs
Arrange tx for opioid-use disorders

PHARM II (3 decks)

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