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27 Cards in this Set
- Front
- Back
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What drugs are the Benzodiazepines?
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"ACT OLD"
Alprazolam Clonazepam Triazolam Oxazepam Lorazepam Diazepam |
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What is the MOA of the Benzodiaepines?
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CNS depressants that enhance GABA transmission by potentiating the effect of GABA at its GABAa receptor (ligand gated Cl channel)
BZs bind at the junction of the alpha and gamma subunits and induce a conformational change that increases the likelihood of Cl- channel opening when GABA binds to its site |
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The GABA receptor has ____ subunits.
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5 (in a pentameric assembly) alpha, beta, gamma, delta
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What are alpha subunits are associated with the BZ I and BZ II receptors?
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BZ I -- alpha1 (sedative effects)
BZ II -- alpha 2,3, or 5 (anxiolytic effects) |
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Which BZs are clinically used as anxiolyics?
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Alprazolam
Clonazepam Oxazepam Lorazepam Diazepam |
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Which BZs are clinically used as hypnotics?
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Triazolam
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What is the MOA of Clomipramine?
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TCA that blocks NE & 5-HT reuptake
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Which SSRIs are used to treat anxiety disorders?
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Fluoxetine
Fluvoxamine Paroxetine Sertaline |
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What is the MOA of Buspirone?
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Direct activation of the 5-HT1a receptor (partial agonist)
*5-HT1a receptors are coupled to K channels, this drug enhances K+ conductance and hyperpolarizes neurons 4-8 wks to be effective in anxiety; no drug dependence or withdrawal rxn |
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What is the MOA of Zolpidem, Zaleplon, Eszopiclone?
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BZ1 receptor agonists; soporific (induce sleep)
Sedative-hypnotic and produce amnesia, but they DO NOT exert an anti-anxiety, anticonvulsant or skeletal muscle relaxant effect |
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How do the "Z drugs" differ from the BZs?
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Not addicting
No withdrawal syndrome Do not potentiate CNS depression caused by ethanol |
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What is the MOA of Flumazenil?
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BZ receptor antagonist
(prevents the binding of BZs to receptor) Clinical Uses: BZ overdose, rapidly reverse effects of BZ when they are used as adjunct with anesthesia in outpatient surgery |
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What is the MOA of Ramelteon?
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Melatonin receptor agonist
Acts on MT-1 & MT-2 receptors in the SCN of the hypothalamus which regulates the circadian rhythm that supports the normal sleep/wake cycle |
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What are the clinical uses of Ramelteon?
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Treat insomnia distinguished by difficulty falling asleep
*mild s/e (headache, drowsiness, dizziness) *no abuse potential |
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What are the five pharmacological actions of the BZs?
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Sedative-hypnotic properties
Anti-anxiety effects Anti-convulsant properties Muscle relaxant effects (@ spinal cord level) Anterograde amnesia |
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What are the adverse effects of the BZs?
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In general: modest, readily managed, little organ toxicity
Sedation, dizziness, uncoordination, paradoxical agitation, impairment of cognitive function Minimal suicidal potential by themselves; combo w/ EtOH is problematic |
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What is the BZ of choice for older patients? Why?
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Oxazepam
Metabolized via glucouronidation which doesn't decrease with age |
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What patients are at greatest risk for BZ withdrawal rxn?
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Patients taking high doses
Patients using BZs for more than 8 months |
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What are the symptoms of a BZ withdrawal rxn?
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Most often like the flu
muscle cramps, abdominal discomfort, diarrhea seizures--rarely encountered *most effectively prevented by slowly tapering the dose |
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What is responsible for the efficacy of Clomipramine in the treatment of OCD?
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Very potent inhibitor of 5-HT re-uptake
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With the exception of the BZs, all the other drugs used to treat the different anxiety disorders take _________ to be effective.
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4-8 weeks
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What drugs are used to treat GAD?
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BZs
SSRIs Venlafaxine Buspirone |
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What drugs are used to treat PD?
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SSRIs
BZs TCAs |
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What drugs are used to treat OCD?
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Clomipramine
SSRIs |
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What drugs are used to treat PTSD?
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SSRIs
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What drugs are used to treat SAD?
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SSRIs
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Patients with a newly-diagnosed anxiety disorder are started on a combination of? After several months of treatment, which drug is discontinued?
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BZ + Buspirone or BZ + SSRI
Discontinue the BZ after Buspirone/SSRI has had time to develop anxiolytic effects |
