Pharmacology Exam 4

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Rx2013
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49371
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Pharmacology Exam 4
Updated:
2010-11-14 00:56:24
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Sedative hypnotic anxiolytic drugs
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Sedative hypnotic and anxiolytic drugs
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  1. BZDs & newer hypnotics vs. older sedative hypnotics
    greater margin of safety/therapeutic index
  2. required for sedative hypnotic activity of BZDs
    substituent in the 7 position such as a halogen or nitro group
  3. alprazolam
    depression
  4. chlordiazepoxide
    alcohol withdrawl syndromes
  5. clonazepam
    • convulsion
    • panic disorder
    • muscle relaxation
  6. Clorazepate
    convulsion
  7. Diazepam
    • status epilepticus
    • most commonly used
  8. triazolam
    early morning insomnia
  9. Pharmacologic properties of BZDs
    • no general anesthesia
    • increases sedative effects of other CNS depressants
  10. Sedation and hypnotic effects of BZDs
    • decreases latency
    • increases time of non-REM sleep
    • decreases duration of NREM sleep
    • decrease duration of REM sleep
  11. sedation and hypnosis with BZDs
    • cause sedation and hypnosis as dose increases
    • GABAa
  12. Muscle relaxation with BZDs
    neuromuscular blockade at very high doses
  13. Anterograde amnesia with BZDs
    preanesthetic medication or diagnostic/operative prodecure
  14. Anticonvulsant BZDs
    • clonazepam
    • lorazepam
    • diazepam
  15. peripheral effects of BZDs
    coronary vasodilation
  16. Mechanism of action for BZD
    • binds alosteric site on GABAa receptor
    • increases frequency of channel opening events
  17. Difficult to differentiate anxiolytic properties of BZSs from sedative hypnotic properties because...
    drus which control anxiety are also sedatives
  18. impairment of motor performance with BZDs
    • lightheadedness
    • lassitude
    • incoordination
    • ataxia
    • mental slowing
  19. Abuse and dependance with BZDs
    • less problematic than with barbituates and alcohol
    • dependance is reported
  20. chronic use and abrupt withdrawl of BZDs
    • rebound anxiety
    • insomnia
    • agitation
    • panic, paranoia, myalgia, muscle twitches, convulsions
  21. Interactions of BZDs with other drugs
    • ethanol increases absorption of BZDs
    • BZDs + valproate = psychosis
  22. 4 classifications of BZDs
    • ultra short acting BZDs
    • short acting
    • intermediate acting
    • long acting
  23. short acting BZDs T1/2 =
    less than 6 hours
  24. intermediate acting BZDs T1/2 =
    6-24 hours
  25. long acting BZDs T1/2 =
    greater than 24 hours
  26. intermediate acting BZDs
    • alprazolam
    • chlordiazepoxide
    • lorazepam
    • oxazepam
    • temazepam
  27. short acting BZDs
    triazolam
  28. long acting BZDs
    • clorazepate
    • diazepam
    • flurazepam
  29. BZDs with no active metabolites
    oxazepam and lorazepam
  30. Buspirone
    • partial 5HT agonist
    • affinity with D2 receptors
    • selective anxiolytic effects
    • slow onset of action
    • no rebound anxiety or withdrawl symptoms
  31. Zolpidem, Zaleplon, Eszopiclone
    • selectively bind alpha 1 subtype of GABAa
    • antagonized by flumazenil
    • minimal muscle relaxing and anticonvulsant effects
    • rapid onset
    • less tolerance and dependance
  32. zaleplon for
    those awake early
  33. dose reductions of sleep aids in patients with...
    • hepatic dysfunction
    • elderly patients
    • pt. taking cimetidine or rifampin
  34. Flumazenil
    • competative antagonist of BDZs
    • rapid action, short half life
    • extensive 1st pass metabolism (less than 25% passes)
  35. Taper off BDZs at
    10% or less per day over 10 to 14 days
  36. Barbituates
    • non-selective CNS depressants
    • cause unconsciousness at high doses
    • narrower margin of safety
    • limited use
  37. Factors affecting onset and duration of barbituate actions
    • lipid solubility
    • tissue redistribution and affinity for plasma proteins
    • liver enzyme metabolism
    • renal excretion
  38. barbituates in order of duration of action long to short
    • phenobarb
    • amobarb
    • pentobarb
    • secobarb
    • thiopental
  39. Pharmacological properties of Barbituates and sleep
    • decrease REM time
    • prolonged use causes rebound insomnia, restlessness, anxiety and nightmares
  40. pharmacological properties of barbituates in anesthesia
    thiobarbiturates and shortacting oxybarbiturates used for anesthesia
  41. anticonvulsant properties of barbiturates
    • phenobarb has selective anticonvulsant action
    • generalized tonic-clonic seizures
  42. barbiturates and respiration
    depression of medullary respiratory center
  43. barbiturates and cardiovascular system
    • decreased cardiac output
    • decreased renal plasma flow
    • increased total peripheral resistence
  44. barbiturates and GI
    decreased GI muscle tone
  45. barbiturates and uterus
    • decreased force and frequency of contractions
    • fetal respiratory suppression
  46. mechanism of action for barbiturates
    • increase duration of GABA gated CL channel openings
    • GABA mimetic and high concentrations
    • inhibit excitatory AMPA receptors
  47. Adverse effects of Barbiturates
    • CNS depression
    • overt excitement
    • hypersensitivity
  48. contraindications of barbiturates
    • acute intermittent porphyria
    • pulmonary insufficiency
    • cardiovascular disease
  49. uses of barbiturates
    • sedative/hypnotic
    • anesthetics
    • anticonvulsants
    • hyperbilirubinemia and kernicterus
  50. Chloral hydrate
    • short acting sedative hypnotic
    • does not affect REM
    • less hangover than BDZs or barbs
  51. Glutethimide and methyprylon
    • methyprolon = shroter duration of action
    • significant anticholinergic effects
  52. Meprobamate
    • anxiolytic agent
    • causes widespread CNS depression
    • anticonvulsant action

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