Unit 3-Anxiolytics Flashcards
Diazepam
Class
Benzodiazepine
Diazepam
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 43 hours (active metabolites up to 100 hours)
Diazepam
Uses
Short-term depression treatment; maintenance of bipolar; severe bipolar; anticonvulsant; muscle relaxant
Diazepam
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA
Chlordiazepoxide
Class
Benzodiazepine
Chlordiazepoxide
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 10 hours (active metabolites up to 100 hours)
Chlordiazepoxide
Uses
Short-term depression treatment; maintenance of bipolar; severe bipolar
Chlordiazepoxide
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA
Lorazepam
Class
Benzodiazepine
Lorazepam
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 14 hours
Lorazepam
Uses
Short-term depression treatment; maintenance of bipolar; severe bipolar; sedation; anticonvulsant; prevent withdrawal symptoms in alcoholics
Lorazepam
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA; directly conjugated into inactive metabolite
Flurazepam
Class
Benzodiazepine
Flurazepam
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 74 hours (active metabolites up to 100 hours)
Flurazepam
Uses
Short-term depression treatment; maintenance of bipolar; severe bipolar
Flurazepam
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA
Alprozolam
Class
Benzodiazepine
Alprozolam
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 12 hours
Alprozolam
Uses
Short-term depression treatment; maintenance of bipolar; severe bipolar; sedation
Alprazolam
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA
Midazolam
Class
Benzodiazepine
Midazolam
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 1.9 hours
Midazolam
Uses
Anesthesia (calming effects, production of anterograde amnesia)
Midazolam
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA
Triazolam
Class
Benzodiazepine
Triazolam
Mechanism
GABAa agonist; binds between a1 and y2 subunits; half-life of 2.9 hours
Triazolam
Uses
Short-term depression treatment; maintenance of bipolar; severe bipolar; induce sleep
Triazolam
Side effects
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)
“Ceiling effect” due to augmenting action of GABA
Zolpidem
Class
Non-benzodiazepine receptor agonist
Zolpidem
Mechanism
BDZ-1 selective agonist
Zolpidem
Uses
Sedation and hypnosis without muscle relaxation or anticonvulsant activity
Zolpidem
Side effects
Sleep-walking; next morning impairment
Flumazenil
Class
Benzodiazepine antagonist
Flumazenil
Mechanism
Competitive non-selective antagonist
Flumazenil
Uses
Benzodiazapine overdose
Flumazenil
Side effects
Withdrawal (may be life-threatening); seizures in mixed overdoses
Non uniform in reversal of respiratory depression
Thiopental
Class
Barbiturate
Thiopental
Mechanism
GABAa agonist (binds a or b subunit); highly lipid soluble, fast-on, fast-off
Thiopental
Uses
Induce anesthesia
Thiopental
Side effects
Daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
Abrupt withdrawal life-threatening; redistribute from brain to muscle and fat, metabolized by liver; dosed based on lean body mass
Phenobarbital
Class
Barbiturate
Phenobarbital
Mechanism
GABAa agonist (binds a or b subunit)
Phenobarbital
Uses
Antiepileptic, anticonvulsant
Phenobarbital
Side effects
Daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
Abrupt withdrawal life-threatening
Buspirone
Mechanism
No GABAa interaction; may be partial agonist at 5HT1A
Buspirone
Uses
Anxiolytic without marked sedation