CNS Depressants

  1. are drugs that can be used to slow down the functions of the CNS
    CNS depressants
  2. are used in the symptomatic tx of thought disorder
    antipsychotic drugs
  3. antipsychotic drug is previously known as
    • neuroleptic drugs
    • antischizoprenic drugs
    • major tranquilizer
  4. are highly effective anxiolytic and hypnotic agents
  5. nonbenzodiazepine drugs (Z Drugs)
    • imidazopyridine (Zolpidem)
    • Pyrazolopyrimidine ( Zaleplon)
  6. are confined to anesthesia and tx of epilepsy
  7. depress the CNS producing calming or drowsiness, sleep, unconsciousness, surgical anesthesia, coma, and death from respiratory and cadriovascular depression
    sedative-hypnotic drugs
  8. pharmacokinetics of hypnotic drugs
    • absorbed well from GI tract
    • good distribution to brain
    • cross the placental barrier during pregnancy
    • detectable in breast milk
  9. is a partial 5-HT1A receptor agonist and an anxiolytics. less sedative and less abuse potential
  10. first line therapy for some anxiety disorders in 1990s because they are not as addictive as benzodiazepine
    SSRI (escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
  11. antidepressant drugs
    • trazodone
    • doxepin
    • mirtazapine
  12. used as sleeping pills for wakeful children
  13. notable as a benzodiazepine marketed exclusively for use of insomnia
    flurazepam HCl USP Dalmane
  14. is a benzodiazepine metabolized by N-dealkylation
  15. is a benzodiazepine that is an active metabolite of chloradiazepoxide and diazepam
    oxazepam USP
  16. is a benzodiazepine that is the 2-chloro derivative of oxazepam thus increases activity
    Lorazepam USP
  17. highly potent anxiolytic on mg basis
    alprazolam USP
  18. ultra short acting hypnotic
    gained popularity as sleep inducer in elderly patients because it causes less daytime sedation
    triazolam USP
  19. via IV as a short acting sedative hypnotic and as an induction anesthetic
  20. are nonBZD introduced as short and moderate acting hypnotics
    zolpidem and eszopiclone
  21. rapid onset of action of 1.6 hrs and bioavailability of 72%
  22. zolpidem has a onset of action of ____ and bioavailability of ____
    1.6 hrs and 72%
  23. was originally marketed as racemic mixture
  24. Zopiclone was originally marketed as
    racemic mixture
  25. half life of zopiclone
    6 hrs
  26. 3 melatonin receptor antagonist
    • MT1
    • MT2
    • MT3
  27. MT1 receptor results to sleepines
    MT2 receptor related to circadian rhythm
    MT3 repceptor related to intra ocular pressure
  28. an endogenous ligand referred to as the hormone of darkness
    melatonin (N-acetyl-5-methoxytryptamine)
  29. - is N-acetylated and O-acetylated product of serotonin found in the pineal gland
    - biosynthesized and released at night
    - play a role in the circadian rhythm of humans
    - promoted commerciallt as a sleep aid by the food supplement industry
    melatonin (N-acetyl-5-methoxytryptamine)
  30. - is 8 times more tna that of MT2 receptor
    - no addiction liability and tx of insomnia
    ramelteon (Rozerem)
  31. - is metabolically N-demethylated to phenobarbital
    - anticonvulsant
    mephobarbital USP
  32. is a long acting sedative and hypnotic
    phenobarbital USP
  33. long duration of action of barbiturates
    more than 6 hrs
  34. intermediate duration of action of barbiturates
    3-6 hrs
  35. ex. of barbiturates with intermediate duration of action
    • amobarbital USP
    • amobarbital sodium USP
    • butabarbital sodium USP
  36. can produce sedation and hypnosis resembling those produced by the barbiturates
    chemical structures (imides, amide, alcohol)
  37. is one of the most active nonbarbiturates hypnotics that is structurally similar to the barbiturates esp. phenobarbital
    Glutethimide USP
  38. is a mild sedative hypnotic with a quick onset and short duration of action (t¹/2=5.6 hrs) (alcohol)
    ethchlorvynol USP
  39. is officially indicated as an antianxiety agent (alcohol)
    meprobamate usp
  40. is the mono N- isopropyl-substituted relative of meprobamate
    Carisoprodol USP
  41. is the p-chloro substituted and 1 carbamate derivative of the lead compound in the development of this group of agents, mephenesin
    chlorphenesin carbamate
  42. is an aldehyde hydrate stable enough to be isolated
    chloral hydrate usp
  43. is recognizable as the cyclic trimer of acetaldehyde
    paraldehyde usp
  44. first phenothiazine compound introduced into therapy
    chlorpromazine HCl USP
  45. has a greater mg potency as an antipsychotic, higher EPS but lower sedative and hypotensive effect than chlorpromazine (phenothiazine)
    triflupromazine HCl usp
  46. a phenothiazine that has a relatively low tendency to produce EPS
    thioridazine HCl usp
  47. a phenothiazine that shares many properties with thioridazine
    mesoridazine besylate usp
  48. a phenothiazine characterized by high mg antipsychotic potency, high prevalence of ESP and low sedative and autonomic effect
    prochlorperazine maleate usp
  49. a phenothiazine act as antipsychotic and antiemetic
    perphenazine USP
  50. is a fluorobutyrophenone that is a potent antipsychotic useful in schizo and in psychoses associated with brain damage
    haloperidol usp
  51. is a fluorobutyrophenone that is used alone as preanesthetic neuroleptic or antiemetic
    droperidol usp
  52. is a fluorobutyrophenone that has a structural features of a hybrid molecule between a butyrophenone antipsychotic and a trazodone like depressant
  53. is not used because of its hygroscopic nature and it is more irritating than the carbonate or citrate to the GI tract
    Lithium Chloride
  54. lithium salts used in US
    • Lithium Carbonate (Eskalith, Lithane)
    • Citrate (Cibalith-S)
Card Set
CNS Depressants