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PHARMA - SEDATIVES AND HYPNOTICS
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1. Sedatives should induce drowsiness and encourage
the onset the maintenance of sleep, while hypnotics reduce anxiety and has a calming effect 2. Hypnotic effects involve a more pronounced depression of the CNS than sedation. (T/F) 3. How can hypnotic effects be achieved? 4. What drug class are the most widely used anxiolytics? 5. What is the prototype of barbiturates? 6. What is a prodrug that is first converted to its active form desmethyldiazepam in the stomach? 7. Which enzyme metabolizes most of the sedatives/hypnotics? 8. Which 2 drugs have metabolites that have shorter half life, which are considered more as hypnotics than anxiolytics? 9. What is the only barbiturate that has a significant portion not metabolized? 10. What is the elimination half life of phenobarbital? 11. Patients with renal insufficiency should never be given phenobarbital (T/F) 12. Most S/H are given with caution in patients with hepatic problems, which phenobarbital as the exception (T/F) 13. Newer hypnotics have phase 1 and phase 2 metabolism (T/F) 14. If patient is given rifampicin along with zolpidem, bioavailability increases. (T/F) 15. What is a strategy to lower serum phenobarbital levels during toxicity? What is the rationale behind it? 16. Sedative hypnotics have affinity to both GABAa and GABAb receptors (T/F) 17. What happens when bdz’s bind to GABAa receptors? 18. Benzodiazepines increase FREQUENCY of channel opening, while barbiturates prolong DURATION of opening (T/F) 19. Barbiturates, although binds to GABA receptors mainly, can also bind glutaminergic receptors. (T/F) 20. What is the reason for the greater CNS/anesthetic effects of barbiturates? 21. Benzodiazepines, at low doses, have an anxiolytic effect (T/F) 22. Why are benzodiazepines addictive? 23. At high doses, barbs and bzd’s become hypnotic agents (T/F) 24. Describe all stages of the sleep cycle (tangina) 25. At what stage of the sleep cycle does the body first go into deep sleep? 26. At what stage of the sleep cycle does the body make repairs? 27. At what stage of the sleep cycle does the brain become more active, and where a person dreams? 28. Sleep progresses in a sequential manner (T/F) 29. Benzos and older drugs reduce sleep onset latency, increase stage 2 NREM sleep, and increases duration of REM sleep (T/F) 30. What is the effect of newer agents when it comes to sleep? 31. Which newer agent decreases REM, and has minimal effect on slow wave sleep? 32. Which newer agent decreases sleep onset latency, but has minimum effect on total sleep time? 33. Which newer agent increases total sleep time, especially stage 2? 34. What is the REM-rebound? 35. Eszopiclone, at high doses, is associated with rebound insomnia (T/F) 36. Anesthetic agents should preferably be long acting rather than short acting (T/F) 37. What drug do you give to reverse the respiratory depression brought about by anesthesia use? 38. What drugs are used to relieve muscle spasm? 39. The newer agents lack anticonvulsant action (T/F) 40. As long as someone is healthy and have no problems with CV function, sedative hypnotics do not cause any detrimental effects (T/F) 41. What is the phenomenon of reduced drug response due to repeated exposure to sedative hypnotics? 42. Tolerance is not observed with newer agents (T/F) 43. The mechanism of tolerance may be due to increase in what? 44. Tolerance also can be explained by the upregulation of receptors (T/F) 45. What is the only benzodiazepine antagonist available in the market? 46. Flumazenil works as an allosteric inhibitor of benzodiazepine receptors (T/F) 47. If a patient is taking both a benzo and a tca, once you give flumazenil, it can cause arrhythmias or convulsions (T/F) 48. Flumazenil can be used for the treatment of benzodiazepine addiction (T/F) 49. Melatonin agonist drugs (anything with -mel) are present in which part of the brain? 50. Melatonin agonists have a direct effect on GABAergic transmission (T/F) 51. Melatonin agonists have withdrawal symptoms when discontinued (T/F) 52. Which enzymes converts melatonin agonists to active metabolites? 53. Benzodiazepines and barbiturates can be used for long term management (T/F) explain the rationale behind the correct answer 54. For immediate relief of anxiety, what class of drugs do you give? 55. Anxiety attacks are managed with benzodiazepines for how many weeks? 56. If you are tapering benzodiazepines, what do you overlap it with? 57. Which is safer, benzodiazepines or barbiturates? 58. Benzos have amnestic effects (T/F) 59. In the context of sedatives and hypnotics, the largest dosing should be during the day, and the minority should be at night. (T/F) 60. Hypnotics can be used for long term treatment (T/F) 61. Abrupt discontinuation of hypnotics have no effects of rebound insomnia (T/F) 62. At hypnotic doses, there is anterograde amnestic effects (T/F)