Anxiolytics

Question 1

Diazepam (Valium)

Answer 1

• Benzo: GABAa agonist: binds bw a1 and y2 subunits
• 43 hr t1/2
• Short-term depression treatment; maintenance of bipolar; severe bipolar; anticonvulsant; muscle relaxant
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, psychologic and physiologic dependence (chronic use)

Question 2

Chlordiazepoxide

Answer 2

• Benzo: GABAa agonist; binds bw a1 and y2 subunits
• 10 hr t1/2
• Short term depression tx, bipolar
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)

Question 3

Lorazepam

Answer 3

• Benzo: GABAa agonist: binds bw a1 and y2 subunits
• 14 hr t12/2
• Short term depression, bipolar,sedation, anticonvulsant, prevent withdrawl symptoms in alcoholics
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
• Directly conjugated into inactive metabolite (NO active metabolite)

Question 4

Flurazepam

Answer 4

• Benzo: GABAa agonist: binds bw a1 and y2 subunits
• 74 hr t1/2
• Short term depression, bipolar
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, psychologic and physiologic dependence (chronic use)

Question 5

Alprazolam (Xanax)

Answer 5

• Benzo: GABAa agonist: binds between a1 and y2 subunits
• 12 hr t1/2
• Short term depression, bipolar, anxiety, sedation
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, psychologic and physiologic dependence (chronic use)

Question 6

Midazolam

Answer 6

• Benzo: GABAa agonist, binds between a1 and y2 subunits
• 1.9 hr t1/2
• Anesthesia (colonoscopy)
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, psychologic and physiologic dependence (chronic use)

Question 7

Triazolam

Answer 7

• Benzo: GABAa agonist, binds between a1 and y2 subunits
• 2.9 hr t1/2
• Short term depression, bipolar, induce sleep
• Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, psychologic and physiologic dependence (chronic use)

Question 8

Zolpidem

Answer 8

• Non-benzo receptor agonist: BDZ-1 selective agonist
• Sedation, hypnosis w/o muscle relaxation or anticonvulsant activity
• Side effects: sleep walking, next morning impairment

Question 9

Flumazenil

Answer 9

• Benzo antagonist: competitive non-selective
• Benzo overdoses
• Side effects: withdrawal, seizures in mixed overdoses

Question 10

Thiopental

Answer 10

• Barbituate: GABAa agonist (binds a or b subunit) , highly lipid soluble
• Induce anesthesia
• Daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
• Abrupt withdrawal can be life threatening

Question 11

Phenobarbitol

Answer 11

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

Question 12

Buspirone

Answer 12

• No GABAa interaction, may be partial agonist at 5HT1A

- Anxiolytic without marked sedation