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15 Cards in this Set

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Flurazepam
BZD; T1/2 = 50-100 hr
Active metabolites (N-DAF)
No rebound insomnia
Quazepam
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
Lorazepam
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
Temazepam
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.
Triazolam
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
Estazolam
BZD; T1/2 = 12-15 hr
Inactive metabolites (ring opening)
Not much rebound insomnia
Diazepam
BZD; T1/2 = 50-100
Active metabolites (Nordiazepam)
No rebound insomnia
Zolpidem (Ambien)
Non-BZD
5-10 mg qd
Partial agonist of GABA-A receptor; may be selective for alpha1 subunit
Zaleplon (Sonata)
Non-BZD
5-10 mg qd
Partial agonist of GABA-A receptor; may be selective for alpha1 subunit
Flumazenil (Romazicon)
Non-BZD
GABA-A antagonist
Eszopidone (Lunesta)
Non-BZD
S-isomer of zopiclone which is not availabe in the US.
GABA-A agonist more selective for alpha1 subunit
Rozerem
Melatonin receptor agonist w/ high binding affinity for MT1 and MT2 receptors
Approved for insomnia.
What are FAM?
Full allosteric modulators -
act with high potency and efficacy at a great variety of subtypes of the GABA-A receptor.
i.e. triazolam, lorazepam
What are SAM?
Selective allosteric modulators -
act with high potency and efficacy at a small number of subtypes of the GABA-A receptor.
i.e. diazepam
What are PAM?
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