Opioids / NSAIDS NB
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Created by:
firefighternate on November 20, 2011
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34 terms
Terms | Definitions |
|---|---|
 opiate | morphine like chemical |
| opioid | morphine like (pharmacological axn), includes antagonist drugs (mimics or antagonize) |
| Endorphin | endogenous opioid peptides -enkephalins, dynorphins, etc.) |
| narcotic | narcosis, stupor, sleep inducing (legal term) |
| Opioid effects | CNS: euphoria, sedation, resp depress, cough suppression, miosis, emesis, constipation, constriction of oddi, |
| Mu receptor | morphine preferring, spinal and supraspinal analgesia |
| Kappa receptor | receptor in spinal cord |
| Delta receptor | spinal and supraspinal analgesia |
| K channels | agonists open channels causing neuronal hyper-polarization. more neg, harder for an AP |
| Ca channels | agonist reduce opening, inhibiting calcium dependent neurotransmitter release. -inhibits presynaptic release of neurotransmitter |
| morphine | low bioavailability (20%) Significant 1st pass metabolism IM or IV |
| codeine | good bioavailability (60%) low potency good anti-tussive metabolized to morphine |
| heroin | rapid entry into brain metabolized to morphine |
| oxycodone | semi-synthetic orally active combo with NSAIDs |
| Naloxone | pure antagonist IV only, zero bioavailability short half life |
| Naltrexone | bioavailable antagonist used to maintain addicts in a drug free state reduces cravings of an alcoholic |
| Meperidine (demerol) | variable bioavailability less GI than morphine AE: severe interaction with MAOI |
| diphenoxylate | low solubility antidiarrheal |
| methadone | similar analgesic efficacy as morphine longer half life blunts heroin high |
| pentazocine | structurally similar to apiates mixed agonist/antagonist -kapp receptor agonist -lower abuse potential |
| dextromethorphan | d-isomer of codeine no analgesic effect good anti-tussive |
| NSAIDs | COX inhibitors |
| COX-1 | stomach, colon, kidney, vascular smooth muscle, and platelets |
| COX-2 | inflammatory responses, fever and algesia |
| anti-inflammatory effect of NSAIDs | requires significantly higher dose -2xs |
| Acetylsalicylic acid (ASA) | NON-reversible inhibits platelet cyclo-oxygenase SE: GI distress, prolonged bleeding, TINNITUS |
| salicylic acid | REVERSIBLE inhibitin of cyclo-oxygenase |
| ibuprofen | non-selective/non-salicylate -inhibits COX -1, 2 |
| naproxen | non-selective/non-salicylate -inhibits COX-1,2 -longer half life |
| celecoxib | COX-2 selective inhibitor -8-10 fold selectivity |
| acetaminophen | anti-pyretic and analgesic *no anti-inflammatory effects AE: hepatotoxic OD: tx with acetylcysteine |
| acetylcysteine | Tx for OD of acetaminophen |
| ASA combo with NSAIDs | use ASA first |
| NSAIDs on kidneys | COX-1,2: can increase and decrease Na retention (natriuresis predominates) -increase BP b/c more Na -hypovolemic at risk for renal ischemia |
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