21 Opioids III Flashcards
What are the routes of administration available for hydromorphone?
IV, PO
Why does hydromorphone have a faster onset than morphine?
it is more lipid soluble
Is hydromorphone or morphine more potent?
hydromorphone is 5x more potent
what is vicodin?
hydrocodone + acetaminophen
what is hydrocodone metabolized to? What enzyme catalyzes this conversion?
hydromorphone, CYP2D6
what is percocet?
oxycodone + acetaminophen
what is oxycodone metabolized to? What enzyme catalyzes this conversion?
oxymorphone, CYP2D6
Why are opioids sometimes administered in combination with acetaminophen (eg vicodin, percocet)
Formulations of opioids with acetaminophen provide
additional pain relief while avoiding severe opioid side
effects.
What is the name of the prodrug that is converted to morphine by CYP2D6?
codeine
What prodrug is converted to monoacetyl morphine and morphine in the brain?
heroin
what opioid is used for maintenance of opioid drug addiction?
methadone
what is the half life of methadone?
Very long; 15 - 60 hours
is meperidine slower or faster onset than morphine?
faster, because it is more lipid soluble
is meperidine more or less potent than morphine?
1/10 as potent
in what type of patient does nor-meperidine have a prolonged half life?
patients with renal failure, due to decreased elimination
What are the signs and symptoms of serotonin syndrome?
- Neuromuscular hyperactivity; tremor, clonus, myoclonus,
hyper-reflexia and (in the advanced stage) pyramidal
rigidity. - Autonomic hyperactivity; diaphoresis, fever, tachycardia
and tachypnea. - Altered mental status; agitation, excitement and (in the
advanced stage) confusion.
which opioid can cause serotonin sydrome, particularly when combined with SSRIs and MAOIs?
meperidine
Which two drugs are partial mu agonists?
tramadol and tapentadol
what metabolizes tramadol?
CYP2D6 (produces active metabolite) and CYP3A4
what metabolizes tapentadol?
CYP2C9, CYP2C19, and a little by CYP2D6
what do pentazocrine, butorphanol, and nalbuphine have in common?
they all act at opioid k receptors but also mu partial agonist/antagonist
what receptors does buprenorphine act on?
partial mu receptor agonist and kappa agonist
What is buprenorphine used for?
treating drug abuse and addiction
What percentage of the us population are rapid metabolizers of CYP2D6?
4-5%
which opioid agonists are used as antidiarrheals?
diphenoxylate and loperamide
which opioid antagonists are used to antagonize the GI side effects of opiates?
alvimopan and methylnaltrexone
What is a REMS?
Risk Evaluation and Mitigation strategy, strategy used to manage known or potential serious risks associated with a drug product; required by the RDA to ensure that the benefits of a drug outweigh the risks
