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36 Cards in this Set
- Front
- Back
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How are sedative drugs used as anxiolytics? What makes an ideal anxiolytic?
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produce a calming effect through CNS depression and this by a wide range of chemical structures and receptor systems. Ideal sedatives do not produce drowsiness or memory impairment.
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What kind of receptors are GABA-A receptors?
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heteropentameric ligand gated Chloride channels.
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What are positive modulators of the GABA-A receptor? How do they work?
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barbiturates, benzodiazepines, zolpidem, zaleplon, eszopiclone
allosterically bind to the receptor to potentiate the response to endogenous GABA. Zolpidem, zaleplon, eszopiclone have more selective hypnotic effects because they bind to a subset of GABA-A receptors containing the α1 subunit. |
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What are the three hypnotics/anxiolytics in the barbiturate class? What are their durations of action?
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Pentobarbital - intermediate to short acting - P450 Enzyme Induction, excreted unchanged in urine
Phenobarbital - Long-acting Thiopental - ultra-short acting whose action is terminated by tissue redistribution (from brain to fat) |
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What is the mechanism of action of Pentobarbital?
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Depression of synaptic sx in ascending reticular activating sx
increase GABA binding duration at high concentrations also directly open Cl channel |
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What are the side-effects and/or complications of using Pentobarbital?
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acute toxicity, tolerance, dependance
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What are the contraindications when using Pentobarbital?
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antihistamines, neuroleptics, narcotics, alcohol, acute intermittent porphyria
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What class of hypnotics/anxiolytics is alprazolam in? What it its use? What is its benefits?
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benzodiazepine
anxiety, panic shorter half life - less 'hangover' intermediate onset |
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What class of hypnotics/anxiolytics is chlorazepate in? What it its use? What is its benefits?
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benzodiazepine
anxiety, panic longer half life - hangover fast onset prodrug: needs bioconversion to desmethyldiaz before active |
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What class of hypnotics/anxiolytics is chlordiazepoxide in? What it its use? What is its benefits?
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benzodiazepine
anxiety, panic, muscle spasticity, alcohol withdrawal, seizures, adjunct to anesthesia, social anxiety |
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What class of hypnotics/anxiolytics is clonazepam in? What it its use? What is its benefits?
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benzodiazepine
anxiety/panic intermediate onset and intermediate half life |
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What class of hypnotics/anxiolytics is diazepam in? What it its use? What is its benefits?
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benzodiazepine
anxiety/panic longer half life - hangover and fast onset |
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What class of hypnotics/anxiolytics is flumazenil in? What it its use? What is its benefits?
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benzodiazepine antagonist
treat benzodiazepine overdose displaces benzodiazepine, blocks binding of b-carbolin to receptor |
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What class of hypnotics/anxiolytics is lorazepam in? What it its use? What is its benefits?
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benzodiazepine
anxiety, panic shorter half life - less hangover intermediate onset no active metabolites |
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What class of hypnotics/anxiolytics is midazolam in? What it its use? What is its benefits?
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benzodiazepine
anxiety, panic similar to clorazepate longer half life - hangover fast onset prodrug |
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What class of hypnotics/anxiolytics is oxazepam in? What it its use? What is its benefits?
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benzodiazepine
anxiety, panic shorter half life - less hangover sow onset active metabolite of desmethyldiazepam but does not itself have an active metabolite |
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What class of hypnotics/anxiolytics is temazepam in? What it its use? What is its benefits?
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benzodiazepine
insomnia minor metabolite of diazepam short half life - less hangover less respiratory depression/abuse potential than barbiturate |
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What class of hypnotics/anxiolytics is triazolam in? What it its use? What is its benefits?
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benzodiazepine
insomnia rapid, short half life high potency may induce 'rebound insomnia' upon withdrawal, rare anterograde amnesia chronic use may possibly induce psychosis |
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What are the general properties of benzodiazepines wrt mechanism and side effects?
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Mechanism: binds to high affinity recognition site on CNS GABA-A receptor and increases effects of GABA on Cl- conductance
Side effects: sedation, psychomotor impairment (driving) anterograde amnesia, tolerance (rare without SA history), withdrawal (must taper), falls in elderly |
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What is the mechanism of action of β carbolines? What are they used for?
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produces anxiety and convulsions
binds to benzodiazepine receptor induces conformational change in receptor produces opposite effect as benzodiazepine (decreased binding of GABA to receptor and closing of Cl- channel) |
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What are some drugs used to treat insomnia in the non-benzodiazepine categories? What are their mechanism of action? Benefits/risks?
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zolpidem, zaleplon, and eszopiclone
acts on subtype of BZD1 receptor largely devoid of anxiolytic, spasmolytic, and anti-convulsive activities no dependence of withdrawal, few side effects short half life reduce doses in elderly |
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How does Buspirone work? What are its benefits?
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results in cessation or attentuation of serotonergic neuron firing - partial agonist of 5HT1A-R w/no direct effect on GABA-A/CL system
no dependence/abuse potential evident no sedating slow onset - requires 2 weeks |
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Diphenhydramine to treat insomnia?
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not proven more effective than placebo
can produce tolerance and rebound insomnia |
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What is GBH?
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structural resemblance to GABA
used recreationally to produce sedation and euphoria |
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What is Meprobamate?
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approved anxiety agent but has been replaced by safer drugs
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What is Chloral hydrate?
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rapidly reduced to active compound trichloroethanol by alcohol dehydrogenase in liver
barbiturate-like effects historically for children rarely used now |
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Where is Melatonin produced? What is it used to treat?
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neurohoromone produced by pineal gland
initial insomnia jet lag or shift work |
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Where is Ramelteon produced? What is it used to treat?
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oral formulation
initial insomnia jet lag or shift work |
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In general what are selective serotonin reuptake inhibitors good for?
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panic disorder
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In general, what is the mechanism of action of barbiturates?
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act on part of β-subunit
increases duration of Cl- channel opening |
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In general, what is the mechanism of action of benzodiazepines? What are they used for?
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binds at the interface between α-β subunits - increases frequency of channel opening
anxiolytic, skeletal muscle, anticonvulsant sedation |
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A patient comes in reporting sudden, unexpected episodes of fear. What do they have and what are your treatment options?
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panic disorder
ADs—SSRI or venlafaxine, nefazodone (not buproprion or trazodone) BZD Other (valproate, gabapentin) CBT, avoid caffeine, stimulants, alcohol |
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A patient comes in reporting excessive anxiety for 6 months or more. What do they have and what are your treatment options?
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Generalized Anxiety Disorder
BZD (1 week) Buspirone (2-3 weeks) Sedating ADs—imipramine, trazodone, (SSRIs, venlafaxine)—need 12 weeks (Hydroxyzine) (B-blockers) |
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Your patient comes in with recurrent, intrusive thoughts and repetitive behaviors. What do they have and what are the treatment options?
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OCD
SSRI & Behavior therapy |
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A patient comes in reporting an unreasonable fear and avoidance of social situations, as well as a fear of public humiliation and being judged. What do they have and what are your treatment options?
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social anxiety disorder
SSRI (MAOI also effective, TCAs not effective) BZD effective—but high comorbidity w/alcohol abuse Gabapentin (1 clinical trial) |
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Your patient has had previous exposure to a traumatic event and is overwhelmed by a sense of fear, helplessness, and horror. They report re-experiencing the event and avoiding anything reminding them of it. What do they have and what are your treatment options?
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PTSD
Psychotherapy + med ADs—decrease intrusive thoug hts, flashbacks, anxiety SSRIs—for avoidance and emotional numbing Prazosin for nightmares |
