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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 |
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codeine
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- 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 |
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hydromorphone
|
- moderate/strong μ agonist
- moderate/severe pain - similar to morphine, fewer severe side effects |
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oxycodone
|
- moderate/strong μ agonist
- severe pain (cancer, post-op) - similar analgesic effect as morphine - fewer side effects |
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hydrocodone
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- 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 |
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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 |
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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 |
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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 |
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propoxyphene
|
- weak μ agonist
- mild analgesic - high dosages may be toxic |
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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 |
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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 |
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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 |
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naltrexone
|
- competitive antagonist at all sites (stronger at μ site)
- longer t1/2 than naloxone - good oral availablity - has side effects |
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loperamide
|
- antidiarrheal
- for acute diarrhea or chronic diarrhea from inflammatory bowel disease - no CNS actions (cannot cross BBB) - interferes with peristalsis |
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diphenoxylate
|
- antidiarrheal
- for acute diarrhea and chronic diarrhea from IBS - stays mostly inside the GI - inhibits GI motility, slows GI propulsion |
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dextromethorphan
|
- antitussive
- for chronic, nonproductive cough |