Pain Management

Edit Answers
1234567891011121314151617181920212223242526272829303132333435363738394041424344454647484950
Across
  1. 4. Semisynthetic. Slightly more potent than morphine. Only in combination with non-opioids (e.g., Vicodin with acetaminophen).
  2. 7. Full μ-agonist. Highly variable pharmacokinetics, long duration of action.
  3. 8. Lubiprostone Not an opioid antagonist. CIC-2 chloride channel activator. Increases fluid secretion into GI lumen, softening stool. Used for OIC.
  4. 9. Bolus for PRN inpatient pain. Peak effect 1-15 min.
  5. 11. Tapentadol More potent μ-agonist than tramadol. Also inhibits NE reuptake. Primarily metabolized by O-glucuronidation.
  6. 12. brand name for Buprenorphine patches 7 days release. Steady-state in 3 days.
  7. 13. Ability to produce a maximal effect.
  8. 16. Full μ-agonist. More potent than morphine. Shorter duration of action despite similar half-life (requires greater accumulation for pain management, ↑ respiratory depression risk).
  9. 18. Endorphins, enkephalins, dynorphins are natural opioid receptor agonists.
  10. 19. Depression of cough reflex (medulla).
  11. 20. Diacetylmorphine Acetylation of morphine. Illicit, Schedule I. Not active itself. Increased lipophilicity allows rapid BBB penetration.
  12. 21. Fentanyl only (high potency, high lipophilicity). Avoids first-pass.
  13. 23. brand name for Fentanyl patches Drug-saturated adhesive, membrane controls diffusion. Heat increases delivery rate (fatal overdoses with heating pads).
  14. 25. hydromorphone ER Newer, avoids alcohol interaction.
  15. 29. Repeated dosing. Low patient comfort. 30-60 min to peak effect, rapid decline. Avoid if possible.
  16. 30. Medication or illegal substance causing insensibility/stupor (can refer to opioids or illicit substances).
  17. 31. Partial μ-agonist (antagonist at higher concentrations), κ-agonist. Mixed agonist-antagonist. Higher dysphoria than morphine (due to κ-activity). (Not available in US). Metabolized by CYP1A2.
  18. 33. Natural source from Papaver somniferum (poppy). Contains alkaloids, primarily morphine (~10%).
  19. 34. Most of dose systemically absorbed. Effective dose 10x intrathecal dose.
  20. 39. Hydromorphone Semisynthetic. More potent than morphine.
  21. 40. κ-agonist, partial μ-agonist (antagonist at higher concentrations). Mixed agonist-antagonist. Analgesia from μ-activity, CNS side effects (hallucinations, psychosis) from κ-activity.
  22. 42. Fully synthetic, different pharmacophore but similar 3D binding. Piperidine ring with 4-carbon substitution.
  23. 46. Meperidine Phenylpiperidine. One of the least potent opioids.
  24. 48. Oxymorphone Semisynthetic. More potent than morphine.
  25. 50. Direct to CSF.
Down
  1. 1. Narrower term, substances derived from Papaver somniferum or mimicking their effects. Endogenous peptides are not opiates.
  2. 2. Modifications to oxymorphone structure. Pure antagonists at all opioid receptors (greater μ-affinity). Bind tightly, block agonists, no receptor response (competitive antagonists).
  3. 3. Methylation of morphine's 3-hydroxy. Weak opioid activity, strong antitussive.
  4. 5. Any substance binding to opiate receptors or mimicking opiate effects (natural, semi-synthetic, synthetic non-peptides). (e.g., morphine, oxycodone, meperidine).
  5. 6. Bind to opiate receptors in CNS, periphery, GI, bladder. Analgesia primarily via μ receptors.
  6. 10. Cyclopropylmethyl group on nitrogen. Pure antagonist. High doses associated with hepatocellular injury (Black Box Warning). Cardiovascular (syncope) and GI adverse effects. Used as deterrent in addiction.
  7. 14. Chemically different from morphine but interact with same opioid receptors.
  8. 15. Dose required to produce a given effect.
  9. 17. decrease in pain intensity/eradication. Inhibition of ascending nociceptive transmission, activation of brain pain control circuits.
  10. 22. Naloxone Allyl group on nitrogen. Safer, widely used. Reverses opioid activity in overdose. Precipitates withdrawal in dependent patients. Low oral bioavailability (used with oral agonists as misuse deterrent).
  11. 24. Tramadol Weak opioid potency. O-demethylated by CYP2D6 to active metabolite (200x greater μ-affinity). Also inhibits NE/serotonin reuptake (neuropathic pain benefit, serotonin syndrome risk). C-IV. Lowers seizure threshold (avoid in epilepsy).
  12. 26. Semisynthetic. Slightly more potent than morphine. O-demethylated by CYP2D6 to oxymorphone (3x more potent than morphine).
  13. 27. Alvimopan Peripheral μ-antagonist. Limited to accelerating GI recovery after bowel resection surgery. Oral, 7 days max. Increased MI risk (REMS program).
  14. 28. Partial μ-agonist, weak κ-antagonist. High affinity, slow dissociation from μ-receptors (long-acting, less euphoria). Can precipitate withdrawal in opioid-dependent patients.
  15. 32. Morphine-like Classic 5-ring structure with ether bridge.
  16. 35. Preferred over IM for comfort. Intermittent boluses or continuous infusion.
  17. 36. Oliceridine IV only. Potent analgesia, designed to avoid respiratory depression by specific μ-opioid receptor conformational changes (G-protein selective activation, less β-arrestin activation).
  18. 37. Isolated from opium, chemically modified to yield diverse drugs. Most abundant alkaloid in opium. 5 chiral centers. Extraction more efficient than synthesis.
  19. 38. Partial μ-antagonist, κ-agonist. Can precipitate withdrawal.
  20. 41. Fentanyl oral transmucosal lozenge "Lollipop." Systemic absorption via oral mucosa.
  21. 43. hydromorphone ER Removed due to "dose dumping" with alcohol (fatal overdoses).
  22. 44. Anilidopiperidine. One of the most potent opioids (80-100x morphine, sufentanil 5-10x fentanyl). Highly lipophilic, rapid CNS distribution (useful anesthetic). Short duration due to redistribution.
  23. 45. Methylnaltrexone Selectively binds peripheral μ-receptors in GI tract, reducing constipation without affecting CNS analgesia. SC injection. Dose reduction for CrCl < 30 mL/min.
  24. 47. Local analgesia (epidural, intrathecal). Highly effective.
  25. 49. Extended pain control, good for swallowing issues/altered consciousness.