sedative hypnotics pharm

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cwhusker
ID:
171475
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sedative hypnotics pharm
Updated:
2012-11-14 17:27:03
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sedative hypnotics
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sedative hypnotics pharm
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  1. phenobarbital
    • long acting barbituate
    • MOA: binds the GABA A Cl channel on the beta subunit. increases the duration the channel is open. increases hyperpolarization
    • USES: seizures, rapid ability to alleviate fear and anxiety (but no longer used)
    • AE: sedation, high dependance, lethal in overdose, narrow TI
  2. thiopental
    • ultra short acting barbituate
    • MOA: binds to GABA A of Cl channel, increases the duration the channel is open. 
    • USES: anesthesia, IV b/c so short acting, not good for seizures
    • AE: sedation, high dependence, lethal overdose, narrow TI
    • induces p450 enzymes
  3. diazepam
    • long acting BZ (valium)
    • MOA: binds to GABA A on Cl channels. increases the frequency of the Cl channel opening
    • USES: anxiety b/c of the long t1/2 
    • AE: anterograde amnesia, won't cause coma or death with overdose.paradoxical excitement
    • don't use for more than 5 weeks
  4. chlordiazepoxide
    • long acting BZ
    • MOA: binds to GABA A on Cl channels. increases the frequency of the Cl channel opening
    • USES: anxiety b/c of the long t1/2
    • AE: anterograde amnesia, won't cause coma or death with overdose.
    • paradoxical excitementdon't use for more than 5 weeks
  5. oxazepam
    • intermediate acting BZ
    • MOA: increase the freq of the Cl channel opening
    • USES: anxiety b/c has a longer t1/2. 
    • has no toxic metabolites so can be used in the elderly
    • AE: amnesia, paradoxical excitment
  6. lorazepam
    • intermediate acting BZ
    • MOA: increases the freq of Cl channel opening
    • USES: insomnia b/c shorter t1/2, can be used in emergency situations b/c can be administered IV. 
    • AE: amnesia
  7. temazepam
    • intermediate acting BZ
    • MOA: increase the frequency of Cl channel opening, binds to GABA A. 
    • USES: insomnia
    • AE: amnesia
    • no toxic metabolites can be used in the elderly
  8. midazolam
    • ultra short acting BZ
    • MOA: increase the frequency of Cl channels opening, binds GABA A
    • USES: adjunct for anesthsia, used in emergencies b/c given IV
  9. flumazenil
    • BZ antagonist
    • MOA: competative BZ receptor antagonist
    • USES: used to counteract excessive effects of BZ
    • doesn't block the effects of other sedative hypnotics
    • doesn't produce sedation, confusion, or mental clouding
  10. buspirone
    • atypical sedative
    • MOA: partial agonist at 5 HT. acts as an agonist where 5 HT is low and as an antagonist where 5HT is high
    • USES: anxiolytic adjunct therapy for depression
    • onset 1-2 weeks
    • CI: MAOI's
  11. zaleplon
    • non-BZ, Z drug
    • MOA: agonist at GABA A, increases melatonin
    • USES: insomnia, rapid onset, used to fall asleep
    • AE: no tolerence, or rebound insomnia
  12. zolpidem
    • non-BZ, Z drug, Ambien
    • MOA: selective agonist at GABA A
    • USES: insomnia, shortens sleep latency, prolongs total sleep time. 
    • AE: tolerance and dependence are rare
  13. eszopiclone
    • non-BZ, Z drug, lunesta
    • MOA: agonist at GABA A
    • USES: insomnia, falling asleep and staying asleep, increases sleep time
    • effective for 6-12 months without dependence, fewer AE than BZ
    • only Z drug approved for long term use
  14. ramelteon
    • non-BZ, Z drug, Rozerem
    • MOA: melatonin agonist
    • USES: insomnia, shortens sleep latency
    • no tolerance or dependence
    • no abuse potential
  15. alprazolam
    • intermediate acting, BZ
    • MOA: increase the freq of Cl channel opening, alters the channel so that GABA binds more efficiently
    • USES: anti-anxiety, sedation, insomnia, anticonvulsants
    • AE: amnesia

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