Opioid Analgesics and Antagonists Flashcards
Strong agonists?
fentanyl, sufentanil, hydromorphone, meperidine, morphine, methadone, buprenorphrine, oxymorphone
Moderate agonists?
codeine, oxycodone
Weak agonists?
propoxyphene, tramadol
Mixed agonists/antagonists?
pentazocine, nalbuphine, butorphanol
Antagonists?
naloxone, naltrexone, nalmefene
Antitussives?
codeine, dextromethorphan, levopropoxyphene
opium resin contains 3 major alkaloids?
morphine, codeine, thebaine
a 30 amino acid long peptide released from a precursor called POMC protein?
B-endorphin
2 pentapeptides (enkephalins)?
Met-enkephalin and Leu-enkephalin
dynorphin A and dynorhpin B are produced from pro-dynorphin in ….?
the pituitary, hypothalamus, midbrain and striatum
opioid bind to ….?
mu, delta and kappa receptors
morphine and other pure agonists have greater affinity for … and lower affinity for …?
mu
kappa and delta
neospinothalamic?
fast Adelta fibers
paleospinothalamic?
slow C fibers
CNS distribution of mu and kappa receptors?
cerebral cortex, striatum, hippocampus, dorsal horn, midbrain
How is CNS distribution of delta receptor different?
amygdala instead of midbrain
pharmacologic functions of mu receptors?
analgesia, sedation, miosis, euphoria, constipation, respiratory depression, pruritus
pharmacologic functions of kappa receptors?
analgesia, sedation, miosis, dysphoria, micturition, diuresis, hallucinations
pharmacologic functions of delta receptors?
analgesia, emotion/reward, seizures (?)
prototypic ligands of mu receptors?
morphine, methadone, endorphin
prototypic ligands of kappa receptors?
dynorphin A and ethylketocyclazocine
prototypic ligands of delta receptors?
enkephalins and deltorphin II
effects of morphine binding at mu?
agonist
effects of morphine binding at kappa?
agonist (weak)
effects of buprenorphine binding at mu?
mixed agonist/antagonist
effects of buprenorphine binding at kappa?
antagonist
effects of buprenorphine binding at delta?
antagonist
effects of pentazocine binding at mu?
antagonist (weak)
effects of pentazocine binding at kappa?
agonist
effects of nalbuphine binding at mu?
antagonist
effects of nalbuphine binding at kappa?
agonist
effects of nalaxone binding at mu?
antagonist
effects of nalaxone binding at kappa?
antagonist
effects of nalaxone binding at delta?
antagonist (weak)
which semi synthetic opioid drug is 40x more potent than morphine?
buprenorphine
which synthetic opioid drug can be given to those who need pain managed for awhile?
fentanyl
codeine is only … as potent as morphine?
half
CNS depression of Morphine is enhanced by …
sedative-hypnotics, antipsychotic drugs, antidepressants
… may interfere with opioid induced analgesia?
sedative-hypnotics
opioids (esp. meperidine) are contraindicated with …
MAOI antidepressants
CNS effect of morphine?
analgesia, euphoria, stupor or tupor
morphine: respiratory center depression or excitation?
depression
True or False: cough reflex center is depressed by morphine
true
True or false: miosis by morphine
true
1/10 potency of morphine; cough suppression; mild to moderate pain?
codeine
1/2 the potency of morphine; mild to moderate pain and antitussive?
hydorcodone/dihydrocodone
moderate to severe pain; 2x potency of morphine; high abuse potential; bioavailability 80%?
oxycodone
combo of oxycodone w/ acetaminophen?
percoset
severe pain relief (acute pain); high potency (7-10x ) at Mu receptor sites?
hydromorphone
severe pain relief; 7x more potent than morphine?
oxymorphone
first fully synthetic; 1/10 potency of morphine; respiratory depression in neonates?
meperidine
nor-meperidine is …?
neurotoxic
moderate to severe pain relief (traditional use); opiate dependence treatment?
buprenorphine
buprenorphine and naloxone?
suboxone
severe pain relief; fully synthetic; most potent opioid?
fentanyl
moderate to severe pain; mainstay of opiate dependence treatment; fully synthetic?
methadone
moderate to severe pain; fully synthetic; atypical opioid; partially blocked by naloxone; inhibits reuptake of NE and 5-HT?
tramadol
opioid receptor antagonist; short duration of action; only injectable?
naloxone
opioid receptor antagonist; long duration of action?
nalmefene
opioid receptor antagonist; long duration of action; long duration of action; reduces craving?
naltrexone
routes of admin of fentanyl?
IM, IV, transdermal
duration of action of fentanyl?
1 hr
elimination half life of fentanyl?
4 hrs
does fentanyl have active metabolite?
No
routes of admin of methadone?
oral and parenteral
duration of action of methadone?
8 hrs
elimination half life of methadone?
24 hrs
does methadone have active metabolite?
No
route of admin of propoxyphene?
oral
duration of action of propoxyphene?
4 hrs
elimination half life of propoxyphene?
9 hrs
does propoxyphene have active metabolite?
Yes
route of admin of naloxone?
parenteral
duration of action of naloxone?
2 hrs
elimination half life of naloxone?
4 hrs
does naloxone have active metabolite?
No
route of admins of naltrexone?
oral
duration of action of naltrexone?
24 hrs
elimination half life of naltrexone?
12 hrs
does naltrexone have active metabolite?
Yes
two opioid receptor agonists with no analgesic effects and used mainly as antidiarrheal?
diphenoxylate and loperamide