Unit 3-Anxiolytics Flashcards by Akil Miah

Diazepam

Class

Benzodiazepine

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Diazepam

Mechanism

GABAa agonist; binds between a1 and y2 subunits; half-life of 43 hours (active metabolites up to 100 hours)

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Diazepam

Uses

Short-term depression treatment; maintenance of bipolar; severe bipolar; anticonvulsant; muscle relaxant

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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

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Chlordiazepoxide

Class

Benzodiazepine

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Chlordiazepoxide

Mechanism

GABAa agonist; binds between a1 and y2 subunits; half-life of 10 hours (active metabolites up to 100 hours)

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Chlordiazepoxide

Uses

Short-term depression treatment; maintenance of bipolar; severe bipolar

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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

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Lorazepam

Class

Benzodiazepine

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Lorazepam

Mechanism

GABAa agonist; binds between a1 and y2 subunits; half-life of 14 hours

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Lorazepam

Uses

Short-term depression treatment; maintenance of bipolar; severe bipolar; sedation; anticonvulsant; prevent withdrawal symptoms in alcoholics

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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

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Flurazepam

Class

Benzodiazepine

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Flurazepam

Mechanism

GABAa agonist; binds between a1 and y2 subunits; half-life of 74 hours (active metabolites up to 100 hours)

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Flurazepam

Uses

Short-term depression treatment; maintenance of bipolar; severe bipolar

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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

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Alprozolam

Class

Benzodiazepine

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Alprozolam

Mechanism

GABAa agonist; binds between a1 and y2 subunits; half-life of 12 hours

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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