Anxiolytics

Question 1

Diazepam (Valium)

Answer 1

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 43 hours (active metabolites up to 100 hours)
T: Short-term depression treatment; maintenance of bipolar; severe bipolar; anticonvulsant; muscle relaxant
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA

Question 2

Chlordiazepoxide (Librium)

Answer 2

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 10 hours (active metabolites up to 100 hours)
T: Short-term depression treatment; maintenance of bipolar; severe bipolar
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA

Question 3

Lorazepam (Ativan)

Answer 3

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 14 hours
T: Short-term depression treatment; maintenance of bipolar; severe bipolar; sedation; anticonvulsant; prevent withdrawal symptoms in alcoholics
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA; directly conjugated into inactive metabolite

Question 4

Flurazepam (Dalmane)

Answer 4

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 74 hours (active metabolites up to 100 hours)
T: Short-term depression treatment; maintenance of bipolar; severe bipolar
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA

Question 5

Alprazolam (Xanax)

Answer 5

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 12 hours
T: Short-term depression treatment; maintenance of bipolar; severe bipolar; sedation
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA

Question 6

Midazolam (Versed)

Answer 6

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 1.9 hours
T: Anesthesia (calming effects, production of anterograde amnesia)
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA

Question 7

Triazolam (Halcion)

Answer 7

C: Benzodiazepine
M: GABAa agonist; binds between a1 and y2 subunits; half-life of 2.9 hours
T: Short-term depression treatment; maintenance of bipolar; severe bipolar; induce sleep
SE: Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
MISC: “Ceiling effect” due to augmenting action of GABA

Question 8

Zolpidem (Ambien)

Answer 8

C: Non-benzodiazepine receptor agonist
M: BDZ-1 selective agonist Omega 1
T: Sedation and hypnosis without muscle relaxation or anticonvulsant activity
SE: Sleep-walking; next morning impairment
MISC:–

Question 9

Flumazenil (Romazicon)

Answer 9

C: Benzodiazepine antagonist
M: Competitive non-selective antagonist
T: Benzodiazapine overdose
SE: Withdrawal (may be life-threatening); seizures in mixed overdoses
MISC: Non uniform in reversal of respiratory depression

Question 10

Thiopental (Pentothal)

Answer 10

C: Barbiturate
M: GABAa agonist (binds a or b subunit); highly lipid soluble, fast-on, fast-off
T: Induce anesthesia
SE: Daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
MISC: Abrupt withdrawal life-threatening; redistribute from brain to muscle and fat, metabolized by liver; dosed based on lean body mass

Question 11

Phenobarbitol

Answer 11

C: Barbiturate
M: GABAa agonist (binds a or b subunit)
T: Antiepileptic, anticonvulsant
SE: Daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
MISC: Abrupt withdrawal life-threatening

Question 12

Buspirone (Buspar)

Answer 12

C: --
M: No GABAa interaction; may be partial agonist at 5HT1A
T: Anxiolytic without marked sedation
SE: --
MISC: --