Pharm Lecture Opioids Flashcards
narcotics def
used to describe sleep agents originally now to describe highly addictive meds
opiates def
actual natural product from poppies
opioid def
lab version of natural papaver somniferum from opioids
MOA opioids
- opioid receptor agonists
- block release of pain NT
- activate presynaptic receptors on GABA neuros inhibit GABA release
examples pain neurotransmitters
- glutamate
- substance P
when opioids inhibit GABA release what is effect
- dopaminergic neurons fire more
- extra dopamine
= more euphoria
morphine is a ___ agoinst
Mu receptor
- found in brainstem
- medial thalamus
(areas for analgesia, respiratory depression, euphoria, sedation, low GI motility, physical dependence)
Mu 1 receptor
peaceful: analgesia, euphoria, serenity
Mu 2 receptor
respiratory depression pruritis prolactin release anorexia dependence histamin itch
kappa receptors are in what areas of brain?
limbic brainstem spinal cord diencephalic areas aka OP2
delta receptors
located in brain effects not studied well
examples of full Mu receptor agonists
- morphine
- fentanyl
- hydromorphone
- codeine
- oxycodone
- methadone
- heroin
partial mu agonists (has ceiling effect)
buprenorphine
butorphanol
mu receptor antagonists = block opioid response
- naloxone (narcan)
- naltrexone
- suboxone (buprenorphine + naloxone)
when to perscribe a short acting opioid?
- acute pain
- incident pain
- breathrough pain
- for activity: travel / physical therapy
examples 7 of short acting opioid?
- codeine
- hydrocodone
- hydromorphone (dilaudid)
- morphine (MSIR, roxanol)
- oxycodone
- oxymorphone (opana)
- fentanyl (actiq)
6 examples long acting opioids
- fentanyl transdermal
- levorphanol
- methadone
- morphine (MS contin, kadian, avinza)
- oxycodone (oxycontin)
- oxymorphone (opana ER)
when to use long term opioid?
chronic pain
moderate to severe pain
opioid OD triad
miosis
LOC
respiratory depression
opioid OD acute tx
narcan naloxone
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
Common opioid ADR effects
- sedation / lethargy
- constipation
- respiratory depression
- N/V
- pruritus / urticaria
- can trigger bronchospasms
morphine half life
2 hours
codeine is a ___ agonist?
mu agonist
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
