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