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Narcotics: Pain Mgmt and Addiction > Pharm Lecture Opioids > Flashcards

Pharm Lecture Opioids Flashcards

1
Q

narcotics def

A

used to describe sleep agents originally now to describe highly addictive meds

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2
Q

opiates def

A

actual natural product from poppies

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3
Q

opioid def

A

lab version of natural papaver somniferum from opioids

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4
Q

MOA opioids

A
  • opioid receptor agonists
  • block release of pain NT
  • activate presynaptic receptors on GABA neuros inhibit GABA release
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5
Q

examples pain neurotransmitters

A
  • glutamate

- substance P

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6
Q

when opioids inhibit GABA release what is effect

A
  • dopaminergic neurons fire more
  • extra dopamine
    = more euphoria
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7
Q

morphine is a ___ agoinst

A

Mu receptor

  • found in brainstem
  • medial thalamus

(areas for analgesia, respiratory depression, euphoria, sedation, low GI motility, physical dependence)

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8
Q

Mu 1 receptor

A

peaceful: analgesia, euphoria, serenity

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9
Q

Mu 2 receptor

A 
respiratory depression 
pruritis 
prolactin release 
anorexia 
dependence 
histamin itch
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10
Q

kappa receptors are in what areas of brain?

A 
limbic 
brainstem 
spinal cord 
diencephalic areas 
aka OP2
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11
Q

delta receptors

A

located in brain effects not studied well

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12
Q

examples of full Mu receptor agonists

A
  • morphine
  • fentanyl
  • hydromorphone
  • codeine
  • oxycodone
  • methadone
  • heroin
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13
Q

partial mu agonists (has ceiling effect)

A

buprenorphine

butorphanol

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14
Q

mu receptor antagonists = block opioid response

A
  • naloxone (narcan)
  • naltrexone
  • suboxone (buprenorphine + naloxone)
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15
Q

when to perscribe a short acting opioid?

A
  • acute pain
  • incident pain
  • breathrough pain
  • for activity: travel / physical therapy
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16
Q

examples 7 of short acting opioid?

A
  • codeine
  • hydrocodone
  • hydromorphone (dilaudid)
  • morphine (MSIR, roxanol)
  • oxycodone
  • oxymorphone (opana)
  • fentanyl (actiq)
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17
Q

6 examples long acting opioids

A
  • fentanyl transdermal
  • levorphanol
  • methadone
  • morphine (MS contin, kadian, avinza)
  • oxycodone (oxycontin)
  • oxymorphone (opana ER)
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18
Q

when to use long term opioid?

A

chronic pain

moderate to severe pain

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19
Q

opioid OD triad

A

miosis
LOC
respiratory depression

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20
Q

opioid OD acute tx

A

narcan naloxone

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21
Q

rule of thumb with half lives and reaching a steady state

A

typically it takes 5 half lives for a drug to reach a half life and become fully effective

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22
Q

Common opioid ADR effects

A
  • sedation / lethargy
  • constipation
  • respiratory depression
  • N/V
  • pruritus / urticaria
  • can trigger bronchospasms
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23
Q

morphine half life

A

2 hours

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24
Q

codeine is a ___ agonist?

A

mu agonist

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25
Q

how potent codeine compared to morphine?

A

50% potency of morphine

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26
Q

half life codeine

A

2.5-3 hrs

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27
Q

codeine drug interactions

A

P450 CYP 2D6 substrate

  • inhibited by: cocaine, celecoxib, cimetidine, bupropion
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28
Q

codeine while nursing?

A

NO!

mom can be fine but baby ultra rapid metabolizer now in coma

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29
Q

what does ultra-rapid metabolizer mean in p450 lingo?

A
  • if drug is a prodrug that means more of the drug gets quickly turned into active form = more potent (ex codeine!)
  • if its is already active (morphine) then the drug will get metabolized quick and be less effective
30
Q

codeine prodrug morphine

A

yes! watch for ultra rapid metabolizer at 2D6 interaction! more potent!

31
Q

MOA oxycodone

A

mu and kappa receptor agonist

32
Q

t/f oxycodone is prodrug

A

true

gets metabolized to oxymorphone

33
Q

common combo products with oxycodone

A
  • oxycodone/ APAP
  • percocet
  • roxicet
  • tylox
34
Q

t/f oxycodone abused

A

YES high abuse

- companies make pills so you can’t crush them turn into gel etc

35
Q

MC used opioid

A

hydrocodone

36
Q

half life hydrocodone

A

4 hours

37
Q

hydrocodone is prodrug of

A

hydromorphone

38
Q

hydrocodone / APAP common brands

A

lortab
Lorcet
Vicodin

39
Q

Vicodin is

A

hydrocodone / APAP

40
Q

hydromorphone MOA

A

agonist at mu and delta receptors

41
Q

t/f hydromorphone drug interactions

A

false not as many
metabolized by glucuronidation not p450

  • same pathway as APAP
42
Q

dilaudid is

A

hydromorphone

43
Q

oxymorphone is __

A

10x more potentn than morphine

  • FDA trying to remove from market
44
Q

adr oxymorphone

A

thrombotic angiography

45
Q

fentanyl is __ times more potent morphine

A

80x

46
Q

fentanyl metabolism

A

CYP3A4 metabolism

47
Q

fentanyl patch pharmokinetics

A

6-12 hr analgesic onset

  • steady state 3-6 days
  • after patch removed clear up to 24 hrs after
  • watch out heat = dose dump = death! (heated water beds etc!)
48
Q

meperidine ___x morphine

A

only 10% potency of morphine

49
Q

meperidine ADR

A
  • anticholinergic properties do not use in elderly

- neurotoxic metabolite (anxiety, tremors sz etc) that not reversible with naloxone

50
Q

propoxyphene brand

A

darvon, darvocet

51
Q

use darvon darvocet in elderly?

A

NO!

52
Q

main ADR propoxyphene (darvocet, darvon)

A

cardiotoxicitiy

53
Q

methadone is a __?

A
  • SNRI
  • NMDA blocker
  • high affinity mu agonist
54
Q

methadone pharmokinetics

A
  • analgesic 4-8hr
  • half life 12-50 hr
  • watch out lipophilic can linger in periphery
  • cardiotoxicity long QT, torsades de points

not ethical use
needs close monitoring

55
Q

buprenorphine MOA

A

mu partial agonist

  • ceiling effect
  • kappa blocker
  • treats opioid addiction often with naloxone (suboxone)

3A4 metabolism

56
Q

butorphanol / levorphanol moa

A

mu agonist

for mod to severe pain

57
Q

narcan generic

A

naloxone

58
Q

naloxone MOA

A

mu receptor blocker

- reverses opioid intoxication

59
Q

naloxone ADR

A

headache, myalgia, increased BP

withdrawl sx

60
Q

naltrexone brand

A

vivitrol

61
Q

naltrexone MOA

A

opioid blocker
CI in pts usng opioids
can help in ETOH abuse decrease cravings

62
Q

tramadol brands (4)

A
  • ultram
  • ultracet
  • ryzolt
  • rybix
63
Q

tramadol is a ___ analog

A

synthetic codeine
week mu receptor agonists

blocks NE and 5ht uptake (SNRI)

as effective as morphine for mild to mod pain (labor)

64
Q

tramadol t/f less effective for severe or chronic pain

A

true

65
Q

tramadol warning

A
  • increase risk for seizures

(esp with SSRI, TCA, opioids, MAOI)

  • serotonin syndrome risk
  • suicide risk
66
Q

tramadol interactions

A

any serotonin drugs
carbamazepine

2D6 and 3A4

67
Q

first opioid for diabetic neuropathy

A

tapentadol

68
Q

tapentadol MOA

A

mu agonist
NE reuptake inhibitor
stronger than tramadol

69
Q

tapentadol and ETOH

A

FATAL NO ALCOHOL WHILE ON THIS MED

70
Q

t/f opioid and BZD

A

do not co perscribe

increases risk of resp depression

71
Q

things to make sure of prior to start rx

A
  • no pregnancy
  • renal liver fxn
  • elderly ..prob not great idea
  • respiratory depression concern

Narcotics: Pain Mgmt and Addiction (8 decks)

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