Flashcards in Opioid Analgesics and Antagonists Deck (81):
fentanyl, sufentanil, hydromorphone, meperidine, morphine, methadone, buprenorphrine, oxymorphone
pentazocine, nalbuphine, butorphanol
naloxone, naltrexone, nalmefene
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?
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 ...?
kappa and delta
fast Adelta fibers
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?
effects of morphine binding at kappa?
effects of buprenorphine binding at mu?
effects of buprenorphine binding at kappa?
effects of buprenorphine binding at delta?
effects of pentazocine binding at mu?
effects of pentazocine binding at kappa?
effects of nalbuphine binding at mu?
effects of nalbuphine binding at kappa?
effects of nalaxone binding at mu?
effects of nalaxone binding at kappa?
effects of nalaxone binding at delta?
which semi synthetic opioid drug is 40x more potent than morphine?
which synthetic opioid drug can be given to those who need pain managed for awhile?
codeine is only ... as potent as morphine?
CNS depression of Morphine is enhanced by ...
sedative-hypnotics, antipsychotic drugs, antidepressants
... may interfere with opioid induced analgesia?
opioids (esp. meperidine) are contraindicated with ...
CNS effect of morphine?
analgesia, euphoria, stupor or tupor
morphine: respiratory center depression or excitation?
True or False: cough reflex center is depressed by morphine
True or false: miosis by morphine
1/10 potency of morphine; cough suppression; mild to moderate pain?
1/2 the potency of morphine; mild to moderate pain and antitussive?
moderate to severe pain; 2x potency of morphine; high abuse potential; bioavailability 80%?
combo of oxycodone w/ acetaminophen?
severe pain relief (acute pain); high potency (7-10x ) at Mu receptor sites?
severe pain relief; 7x more potent than morphine?
first fully synthetic; 1/10 potency of morphine; respiratory depression in neonates?
nor-meperidine is ...?
moderate to severe pain relief (traditional use); opiate dependence treatment?
buprenorphine and naloxone?
severe pain relief; fully synthetic; most potent opioid?
moderate to severe pain; mainstay of opiate dependence treatment; fully synthetic?
moderate to severe pain; fully synthetic; atypical opioid; partially blocked by naloxone; inhibits reuptake of NE and 5-HT?
opioid receptor antagonist; short duration of action; only injectable?
opioid receptor antagonist; long duration of action?
opioid receptor antagonist; long duration of action; long duration of action; reduces craving?
routes of admin of fentanyl?
IM, IV, transdermal
duration of action of fentanyl?
elimination half life of fentanyl?
does fentanyl have active metabolite?
routes of admin of methadone?
oral and parenteral
duration of action of methadone?
elimination half life of methadone?
does methadone have active metabolite?
route of admin of propoxyphene?
duration of action of propoxyphene?
elimination half life of propoxyphene?
does propoxyphene have active metabolite?
route of admin of naloxone?
duration of action of naloxone?
elimination half life of naloxone?
does naloxone have active metabolite?
route of admins of naltrexone?
duration of action of naltrexone?
elimination half life of naltrexone?
does naltrexone have active metabolite?