opiates and receptors Flashcards
what do endogenous opiates have similarities in?
AA sequence
(T/F) some endogenous opiates are derived from the same precursor molecule?
T
what receptor does morphine act on?
mu
what receptor does ketocyclazocine act on?
kappa
is the sigma receptor an opioid receptor?
no
which three receptors have some identical AA sequences?
mu, delta, kappa
what three drugs make up the phenanthrene class?
codeine, morphine, dihydromorphone
what 2 drugs make up the levorphanol class?
levorphanol and dextrorphan
what 3 drugs make up the fentanyl class?
fentanyl, alfentanyl, sufentanyl
what three drugs make up the methadone class?
methadone, LAAM, propoxyphene
what type of opiate agonists are the agents?
direct acting agonists
what drug is the gold standard opioid agonist?
morphine
(T/F) opioid agonists have reuptake blockers and degredation inhibitors
F
(T/F) opioid agonists have synthesis inhibitors and precursors
F
(T/F) opioid agonists do not have neuron activators or releasors
T
where are the main effects of mu opioid agonists?
CNS
what is the main effect of opioid mu receptor agonists on the CNS?
analgesia without anesthesia
(T/F) mu receptor agonists cause anethesia
F
what are the 6 minor effects on the CNS by mu receptor agonists?
sedation, respiratory depression, nausea, anti-tussive, miosis, neuroendocrine effects
what is the difference between NSAIDs and morphine?
NSAIDS relieve the pain and morphine the pain is still there but not bothersome
what type of pain is morphine affective towards: dull/throbbing or sharp/cutaneous?
dull/throbbing
do opiates work at the source of pain?
no
where is the primary source of pain relief from opiates?
reduced appreciation of pain by CNS
(T/F) opiates are anti-inflammatory
F
A patient with inflammation would benefit from ____
NSAIDs
a patient who had surgery and has bone pain would benefit from ____
opiates
where is supraspinal analgisa?
PAG (brain)
where is spinal analgisa?
spinal cord dorsal horn and spinothalamic tract
morphine produces CNS _____
depression
the most common cause of death in opioid OD is ___
respiratory depression
where are the mu receptors?
medulla
what does respiratory depression do to PCO2 levels?
inc
what does respiratory depression do to RR, minute volume, and tidal exchange?
dec
what is a consequence with nausea side effect from opioids?
choking on the nausea
what is miosis?
constricted pupil
is miosis from excitation on the parasympthetic or sympathetic nervous system?
miosis is excitation on the parasympathetic nervous system innervating pupil
what happens upon anoxia?
mydriasis
what two hormones are inc with morpine?
GH and PRL
other than the CNS, where at the 3 places morphine can act?
cardiovascular, GI, smooth muscle
what happens to SNS tone and reflexes from morphine?
dec
what happens to vascular resistance from morphine?
dec, vasodilation
what happens to baroreceptor reflex from morphine?
blunted
what happens to gastric emptying and motility of the GI with morphine?
dec
what impact does morphine have on the bowel movement?
constipation
do nonpropulsive contractions increase or decrease with morphine?
inc, lead to spasms
do propulsive contractions increase or decrease with morphine?
dec, lead to stasis
what happens to anal sphincter tone with morphine?
inc
what happens to bladder external sphincter tone with morphine?
inc
what happens to bladder volume and voiding with morphine?
bladder volume inc
voiding dec
what happens to biliary pressure with morphine?
10x fold increase in pressure
there is _____ worsening of gall stone/kidney stone pain
paradoxical
what causes the worsening of the gall/kidney stone pain?
increases smooth muscle contraction by morphine acting on mu receptor squeezing on stone
are young or old more sensitive to morphine?
both
what is responsible for skin flushing?
morphine histamine response
acute overdose problem includes?
opiate triad
what are the 3 parts of the opiate triad?
respiratory depression, comatose, miosis
how do you treat the opioid triad?
naloxone iv
what are the three chronic treatment issues?
dependence, addiction, tolerance
what has a higher effect morphine or codeiene?
morphine
what CYP does codeiene get metabolized by?
2D6
what is morphine’s prodrug?
codeiene
heroin is _____ morphine
diacetyl
heroine has _____ CNS entry
fast
heroine is a _____ of morphine
prodrug
in OD, what is the marker for heroin use?
6MAM
what three phenanthrenes are alagesics?
hydrocodone, oxycodone, hydromorphine
is immediate release or XR preferred?
immediate release
you should avoid opioids in combo with _____
benzos
with acute pain, you start with a ___ dose
low
what is levorphanol’s efficacy in relation to morphines?
same efficacy
what is dextrorphan’s use?
anti-tussive
is dextrorphan an opioid?
non-opiate
what receptor does dextrorphan interact with?
NMDA
what is meperidine’s efficacy in relation to morphine’s?
lower efficacy
what happens with convulsions on merperidine?
inc
which version of merperidine is responsible for convulsions?
normerperidine
is merperidine used?
no
what is normerperidine’s efficacy compared to merperidine?
1/2 as effective as merperidine
what is normerperidine’s toxicity in comparison to merperidine?
2x as toxic as merperidine
when combined with _____ normerperidine’s toxicity increases
SSRI
what is common with serotonin syndrome
normerperidine toxicity symptoms + fever
what are the 4 common normerperidine toxicity manifestations?
seizure, irritability, tremor, myoclonus
diphyloxylate and loperamide are used for?
diarrhea
merperidine begins as….
MPTP
MPTP becomes____ when enters the brain
MPP+
MPP+ finally converts to…
DA
neuron death leads to _____ syndrome
parkinsons
what is fentanyls potency and efficacy compared to morphine?
higher
fentanyl is a ____ opioid
synthetic
fentanyl is used for 2 purposes _____ and ______
anesthesia + analgesia
three fentanyl analogs are…
alentanil, sulfentanil, remifentanil
(T/F) fentanyl is often used as an additive to make something more potent
T
“designer drug” lead to passing of which act?
controlled substance analog act
what is methadone’s efficacy compared to morphine?
same
what happens to methadone’s t1/2 with repeat doses?
inc
LAAM’s efficacy is similiar to ___
methadone
propoxyphene’s efficacy is lower than ______
codeiene
fentanyl has a ____ efficacy
superior
morphine and methadone have a ____ efficacy
high
codeiene has ____ efficacy
good
propoxyphene has ____ efficacy
low
efficacy as an analgesic correlates with efficacy to produce ____
euphoria
you should use the ____ efficacy possible for the pain
lowest
two liabilities with mu agonists are…
OD and abuse liability
a mu selective agonist is…
methadone
the ligand selectivity is based on…
receptor binding
analgesia, euphoria, and respiratory depression are common to which receptor subtypes?
mu
analgesia, dysphoria, and NO respiratory depression are common to which receptor subtypes?
kappa
opiate mixed agonist/antagonist combine actions at which two receptors?
mu and kappa
nalorphine MOA
mu antagonist/ kappa agonist
nalorphine had ____ abuse liability
no (mu antagonizing)
nalorphine had ____ analgesic action
good (kappa agonist)
pentazocine MOA?
mu partial agonist/kappa weak agonist
is pentazocine abuse -free?
no
Nalbuphine MOA?
weak mu antagonist/weak kappa agonist
butorphanol MOA?
partial mu agonist/weak kappa agonist
buprenorphine MOA?
partial mu agonist/weak kappa antagonist
how fast does buprenorphine leave the mu receptor?
slow offset from mu receptor
the maximum number of drug-receptor transduction effects is greater if drugs leave receptors ____ after producing effect
fast
narcan has a ___t1/2
short
naltrexone has a ____t1/2
long
naltrexone can be given ___ form
oral
narcan (naloxone) is given ___ form
iv
what does it mean if a small dose of iv naloxone is given and some reversal?
opioid involvement
(T/F) naloxone can cause withdrawal
T
narcan has two forms… they are ___ and ___
nasal and iv
the two full antagonists are…
vivitrol + narcan
what happens to the endogenous opiates as a result of vivitrol?
they are blocked too so no “normal good feelings”
vivitrol is active in the ____ form
po
(T/F)spinal intrathecal administration is addictive
F
rate the following opioid agonist/antagonist mixed compounds from most to least efficient? nalorphine, pentazocine, buprenorphine
buprenorphine >
pentazocine >
nalorphine
which opiate is available as sustained release?
oxycontin
