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15 Cards in this Set
- Front
- Back
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Flurazepam
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BZD; T1/2 = 50-100 hr
Active metabolites (N-DAF) No rebound insomnia |
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Quazepam
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BZD; T1/2 = 40 h
Selective for BZ-1, but metabolites (N-DAF) are not selective so chronic users will experience no selectivity. No rebound insomnia |
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Lorazepam
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BZD; T1/2 short
C3 conjugated to produce inactive metabolites May be safer in the elderly or those with hepatic impairment. No longer labeled for insomnia b/c of rebound insomnia |
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Temazepam
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BZD; T1/2 = ?
C3 conjugated to produce inactive metabolites. May be safer in the elderly or those with hepatic impairment. Rebound insomnia may or may not occur depending on speed of metabolism. Fast metabolism means no rebound insomnia. |
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Triazolam
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BZD; T1/2 = 1.5 - 5 hr
Inactive metabolites (ring opening) Metabolism is so fast that REM sleep can be made up later in the night and therefore no rebound insomnia. Dose > 0.5 mg = MEMORY IMPAIRMENT |
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Estazolam
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BZD; T1/2 = 12-15 hr
Inactive metabolites (ring opening) Not much rebound insomnia |
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Diazepam
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BZD; T1/2 = 50-100
Active metabolites (Nordiazepam) No rebound insomnia |
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Zolpidem (Ambien)
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Non-BZD
5-10 mg qd Partial agonist of GABA-A receptor; may be selective for alpha1 subunit |
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Zaleplon (Sonata)
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Non-BZD
5-10 mg qd Partial agonist of GABA-A receptor; may be selective for alpha1 subunit |
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Flumazenil (Romazicon)
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Non-BZD
GABA-A antagonist |
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Eszopidone (Lunesta)
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Non-BZD
S-isomer of zopiclone which is not availabe in the US. GABA-A agonist more selective for alpha1 subunit |
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Rozerem
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Melatonin receptor agonist w/ high binding affinity for MT1 and MT2 receptors
Approved for insomnia. |
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What are FAM?
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Full allosteric modulators -
act with high potency and efficacy at a great variety of subtypes of the GABA-A receptor. i.e. triazolam, lorazepam |
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What are SAM?
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Selective allosteric modulators -
act with high potency and efficacy at a small number of subtypes of the GABA-A receptor. i.e. diazepam |
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What are PAM?
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Partial allosteric modulators -
Act with high potency but low efficacy (intrinsic activity) at a great variety of subtypes of the GABA-A receptor. i.e. experimental compounds such as imidazenil and bretazenil |
