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17 Cards in this Set

  • Front
  • Back
morphine
- strong μ agonist
- moderate/severe acute/chronic pain, or sedation
- active metabolite (M6G) is more potent than morphine itself and has analgesic effects
- metabolized in liver to make the active metabolite
codeine
- moderate μ agonist
- can be combined with non-opioid analgesic for mild/moderate pain
- metabolized to morphine (low) and inactive metabolite (high)
- antitussive and antidiarrheal activity
hydromorphone
- moderate/strong μ agonist
- moderate/severe pain
- similar to morphine, fewer severe side effects
oxycodone
- moderate/strong μ agonist
- severe pain (cancer, post-op)
- similar analgesic effect as morphine
- fewer side effects
hydrocodone
- moderate μ agonist
- moderate/severe pain, can be combined with non-opioid in tablet or liquid form
- antitussive effects
- when given with acetaminophen, be careful with high dose, causing liver toxicity b/c of acetaminophen metabolism
meperidine
- moderate-strong μ agonist
- active metabolite (normeperidine) can accumulate, has long t1/2 and can cause CNS problems (seizures) thus recommended short-term dosage only
- CI with MAO inhibitors (causes serotonin syndrome)
- CI for chronic pain due to risk of seizure
fentanyl
(sufentanil, alfentanil, remifentanil)
- very strong μ agonist (80x morphine), also κ agonist
- faster absorption than morphine across BBB
- short t1/2 and duration
- useful as anesthetic adjuvant b/c of fast acting
methadone
- strong μ agonist, some anti-NMDA
- good oral bioavailability, so can be given through mouth
- long t1/2 (good for chronic pain)
- commonly used to help with opiate withdrawal programs
propoxyphene
- weak μ agonist
- mild analgesic
- high dosages may be toxic
tramadol
- weak μ agonist
- also blocks pain signals by inhibiting NE/serotonin reuptake
- good for short-term severe pain, use with NSAID for osteoarthritis, or replacement for addictive analgesics
pentazocine
- mixed partial μ and κ agonist
- moderate/severe pain
- less potent than morphine (shorter t1/2 and less respiratory depression)
- can cause hallucinations, anxiety attacks
buprenorphine
- partial μ agonist (mixed)
- for moderate/severe pain
- slow dissociation from μ receptor, so has longer duration than morphine
naloxone
- competitive antagonist at all three receptors (stronger at μ site)
- short t1/2
- low oral bioavailability (use IV, subcut, IM)
- mostly no side effects
naltrexone
- competitive antagonist at all sites (stronger at μ site)
- longer t1/2 than naloxone
- good oral availablity
- has side effects
loperamide
- antidiarrheal
- for acute diarrhea or chronic diarrhea from inflammatory bowel disease
- no CNS actions (cannot cross BBB)
- interferes with peristalsis
diphenoxylate
- antidiarrheal
- for acute diarrhea and chronic diarrhea from IBS
- stays mostly inside the GI
- inhibits GI motility, slows GI propulsion
dextromethorphan
- antitussive
- for chronic, nonproductive cough