- opioid receptor agonists - block release of pain NT - activate presynaptic receptors on GABA neuros inhibit GABA release

Pharm Lecture Opioids Flashcards by Rose Clousing

narcotics def

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

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opiates def

actual natural product from poppies

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opioid def

lab version of natural papaver somniferum from opioids

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MOA opioids

opioid receptor agonists
block release of pain NT
activate presynaptic receptors on GABA neuros inhibit GABA release

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examples pain neurotransmitters

glutamate

- substance P

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when opioids inhibit GABA release what is effect

dopaminergic neurons fire more
extra dopamine
= more euphoria

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morphine is a ___ agoinst

Mu receptor

found in brainstem
medial thalamus

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

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Mu 1 receptor

peaceful: analgesia, euphoria, serenity

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Mu 2 receptor

respiratory depression 
pruritis 
prolactin release 
anorexia 
dependence 
histamin itch

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kappa receptors are in what areas of brain?

limbic 
brainstem 
spinal cord 
diencephalic areas 
aka OP2

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delta receptors

located in brain effects not studied well

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examples of full Mu receptor agonists

morphine
fentanyl
hydromorphone
codeine
oxycodone
methadone
heroin

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partial mu agonists (has ceiling effect)

buprenorphine

butorphanol

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mu receptor antagonists = block opioid response

naloxone (narcan)
naltrexone
suboxone (buprenorphine + naloxone)

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when to perscribe a short acting opioid?

acute pain
incident pain
breathrough pain
for activity: travel / physical therapy

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examples 7 of short acting opioid?

codeine
hydrocodone
hydromorphone (dilaudid)
morphine (MSIR, roxanol)
oxycodone
oxymorphone (opana)
fentanyl (actiq)

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6 examples long acting opioids

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

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when to use long term opioid?

chronic pain

moderate to severe pain

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opioid OD triad

miosis
LOC
respiratory depression

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opioid OD acute tx

narcan naloxone

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rule of thumb with half lives and reaching a steady state

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

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Common opioid ADR effects

sedation / lethargy
constipation
respiratory depression
N/V
pruritus / urticaria
can trigger bronchospasms

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morphine half life

2 hours

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codeine is a ___ agonist?

mu agonist

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how potent codeine compared to morphine?

50% potency of morphine

half life codeine

2.5-3 hrs

codeine drug interactions

P450 CYP 2D6 substrate - inhibited by: cocaine, celecoxib, cimetidine, bupropion

codeine while nursing?

NO! | mom can be fine but baby ultra rapid metabolizer now in coma

what does ultra-rapid metabolizer mean in p450 lingo?

- 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

codeine prodrug morphine

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

MOA oxycodone

mu and kappa receptor agonist

t/f oxycodone is prodrug

true | gets metabolized to oxymorphone

common combo products with oxycodone

- oxycodone/ APAP - percocet - roxicet - tylox

t/f oxycodone abused

YES high abuse | - companies make pills so you can't crush them turn into gel etc

MC used opioid

hydrocodone

half life hydrocodone

4 hours

hydrocodone is prodrug of

hydromorphone

hydrocodone / APAP common brands

lortab Lorcet Vicodin

Vicodin is

hydrocodone / APAP

hydromorphone MOA

agonist at mu and delta receptors

t/f hydromorphone drug interactions

false not as many metabolized by glucuronidation not p450 - same pathway as APAP

dilaudid is

hydromorphone

oxymorphone is __

10x more potentn than morphine - FDA trying to remove from market

adr oxymorphone

thrombotic angiography

fentanyl is __ times more potent morphine

80x

fentanyl metabolism

CYP3A4 metabolism

fentanyl patch pharmokinetics

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!)

meperidine ___x morphine

only 10% potency of morphine

meperidine ADR

- anticholinergic properties do not use in elderly | - neurotoxic metabolite (anxiety, tremors sz etc) that not reversible with naloxone

propoxyphene brand

darvon, darvocet

use darvon darvocet in elderly?

NO!

main ADR propoxyphene (darvocet, darvon)

cardiotoxicitiy

methadone is a __?

- SNRI - NMDA blocker - high affinity mu agonist

methadone pharmokinetics

- 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

buprenorphine MOA

mu partial agonist - ceiling effect - kappa blocker - treats opioid addiction often with naloxone (suboxone) 3A4 metabolism

butorphanol / levorphanol moa

mu agonist | for mod to severe pain

narcan generic

naloxone

naloxone MOA

mu receptor blocker | - reverses opioid intoxication

naloxone ADR

headache, myalgia, increased BP withdrawl sx

naltrexone brand

vivitrol

naltrexone MOA

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

tramadol brands (4)

- ultram - ultracet - ryzolt - rybix

tramadol is a ___ analog

synthetic codeine week mu receptor agonists blocks NE and 5ht uptake (SNRI) as effective as morphine for mild to mod pain (labor)

tramadol t/f less effective for severe or chronic pain

true

tramadol warning

- increase risk for seizures (esp with SSRI, TCA, opioids, MAOI) - serotonin syndrome risk - suicide risk

tramadol interactions

any serotonin drugs carbamazepine 2D6 and 3A4

first opioid for diabetic neuropathy

tapentadol

tapentadol MOA

mu agonist NE reuptake inhibitor stronger than tramadol

tapentadol and ETOH

FATAL NO ALCOHOL WHILE ON THIS MED

t/f opioid and BZD

do not co perscribe | increases risk of resp depression

things to make sure of prior to start rx

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