narcotics Flashcards
which opioids bind mu-opioid receptors but it has low receptor affinity (thus a weak analgesic) BUT also have some NE/5HT uptake inhibition (which results in what bc of this particular action?)
codeine
all opioids bind to which receptor?
Mu-opioid receptor
which opioid is a weak analgesic in itself, but it demethylates to morphine and is found in many cough meds?
codeine
SE of all opioids?
major: miosis, constipation, respiratory depression
Dry mouth, N/V, sedation, sweating, dreams, dysphoria, delirium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
which opioid has M3 and M6 metabolites? Which metabolite is more potent/active?
morphine; M6
which opioid gives you mood alteration in addition to providing analgesia for severe pain? what are some of the other effects of this drug?
morphine; severe analgesia, mood alteration, antitussive, sedation
which drug may have SE in caucasians w/o drug effect? (cannot be converted to active)
codeine
synthetic codeine analog
tramadol
for:
1. severe analgesia
2. moderate analgesia
3. moderate to severe analgesia
- morphine
- codeine, tramadol
- oxycodone, fentanyl
list all the opioids (10)
- morphine
- codeine
- tramadol
- fentanyl
- methadone
- oxycodone
- meperidine
- propoxyphene
- loperamide
- diphenoxylate
2 opioids for tx diarrhea
loperamide and diphenoxylate
slows peristalsis via opioid receptors in intestine, possible decrease GI secretion
loperamide and diphenoxylate
meperidine congener (2)
loperamide and diphenoxylate
which opioid can be administered IV or via transdermal (intraspinal possible) and has a long T1/2 (cannot change dose more than 1/week)
fentanyl
which opioid is highly lipid-soluble
fentanyl
which opioid is for tx chronic, severe pain as well as heroin and opioid addicts?
methadone
mostly bound to plasma protein and accumulates in tissues (thus, extended duration of action, thus do not change dose more than 1/wk (long T1/2))
methadone
for moderate to severe pain, oxycontin is the extended release form
oxycodone
not supposed to use this opioid because it makes normeperidine metabolite (causes AMS, seizures, in addition to miosis, resp depression, constipation)
meperidine
dont use this opioid bc it makes norpropoxyphene (CNS toxicity), which has a long T1/2. but this drug is a weak mu-opioid receptor agonist
propoxyphene
2 opioids to tx diarrhea?
loperamide and diphenoxylate
2 opioid antagonists?
- naloxone
2. naltrexone
what drug is a competitive mu, delta, and kappa-opioid receptor ANTAGONIST?
naloxone
what drug is used to tx alcoholism?
naltrexone
mu-opioid antagonist
naltraxone
- can precipitate w/d (flu-like sx of n/v/d, piloerection, yawning, irritability);
- need continuous prn infusion bc only lasts 15-30min. (oral form is completely metabolized by liver)
- pt has normal mental status
naloxone
may produce prolonged w/d state (n/v/yawning, piloerection)
naltrexone
