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32 Cards in this Set
- Front
- Back
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What is an example of a long-acting barbituates?
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Phenobarbital
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What are some examples of intermediate-acting barbituates?
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-Pentobarbital
-Secobarbital |
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What are some examples of short-acting barbituates?
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-Thiopental
-Methohexical |
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What are barbituates used for clinically?
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-Induction in general anesthesia
-Seizure disorder |
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Which alpha subunit of the GABAa receptor is only found in the hippocampus?
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-Alpha 5
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What are the adverse drug reactions associated with barbituates?
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Symptoms of overdose include: comatose state, marked respiratory depression, shortened REM sleep, hypotension, weak rapid pulses.
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What is the treatment for barbituate overdose?
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-Maintain respiration
-Rule out narcotics -Gastric Lavage -Bicarbonate |
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When is giving barbituate contraindicated?
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Family or personal hx of acute intermittent porphyria
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What is the mechanism of action of benzodiazepines?
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Benzodiazepines bind between the gamma and alpha subunits of the GABAa receptor, increasing the influx of chloride, hyperpolarizing the cell and increasing the inhibitory effect of GABA.
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What are advantages do benzodiazepines have over barbituates?
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-Do not induce liver enzymes
-Very little effect on REM sleep -Much wider margin of safety -Withdrawal is mild |
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What activities are seen with the use of benzodiazepines?
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-Sedative/Hypnotic
-Anxiolytic -Anticonvulsant (not used prophylactically) -Muscle Relaxant -Amnestic |
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Besides treating anxiety, what other uses do benzodiazepines have?
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-Sleeping Disorders
-Convulsive Disorders -Neuromuscular Disorders -Preoperative medication -Treatment of withdrawal from CNS depressants |
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What characterizes the absorption of benzodiazepines?
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Oral absorption (1-3 hrs)
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What is the only benzodiazepine that is administered via IM injection?
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Lorazepam
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What benzodiazepines are not metabolized to active metabolites (HINT LOTT)?
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-Lorazepam
-Oxazepam -Temazepam -Triazolam |
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What is the best way to avoid side effects when withdrawing benzodiazepines?
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Gradually taper the dose
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What is Flumazenil?
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Benzodiazepine antagonist: used for overdose to reverse respiratory depression; it will precipitant withdrawal so do not give to pts. with a hx of seizures or pts with barbituate/TCA overdose, have a rapid onset and short duration.
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What benzodiazepines are used as sedative/hypnotics (HINT FLTT)?
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-Flurazepam
-Lorazepam -Temazepam -Triazolam |
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What characterizes Flurazepam?
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Metabolized to active metabolites (desakylflurazepam& desmethyldiazepam); peak concentration of active metabolites reached 1-3 hrs after oral intake, good BA, proper dose can give 8 hrs of sleep with minimal residual effects the next day.
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What characterizes Lorazepam?
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Absorbed slowly orally; Well absorbed following IM administration; not metabolized to active metabolites, proper dose adjustment can give a good night's sleep with minimal residual effects.
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Which benzodiazepine used as a sedative/hypnotic possess the longest half-life?
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Flurazepam (24-100hrs)
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Which benzodiazepine used as a sedative/hypnotic has the shortest half-life?
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Triazolam (2-5hrs)
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What characterizes Temazepam?
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Oral absorption slow and erratic; No active metabolites
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What characterizes Triazolam?
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Well absorbed orally, peak plasma levels 1 hr after oral administration; no active metabolites, higher abuse potential and more withdrawal with chronic use; higher incidence of adverse behavioral reactions.
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Which benzodiazepines are used as anxiolytics (HINT DOCA)?
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-Diazepam
-Oxazepam -Chlordiazeperoxide -Alprazolam |
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What characterizes Diazepam?
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Well absorbed orally, elimination is biphasic and variable; metabolized to desmethyldiazepam which is further metabolized to oxazepam (both metabolites are active).
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What characterizes Oxazepam?
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Slow oral absorption; half-life 5-10 hrs; No active metabolites.
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What characterized Chlordiazeperoxide?
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Slower oral absorption than diazepam; Half-life 7-13 hrs; Metabolized to desmethyldiazepam and oxazepam.
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What characterizes Alprazolam?
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Oral absorption slower than diazepam; Half-life 10-14 hrs; metabolized to active metabolites.
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What are the advantages of treatment with benzodiazepines in sleep disorders?
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-Safety
-Do not disrupt REM -Do not induce P450 -Milder withdrawal syndrome |
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What type of drug class are the azaspirodecanediones?
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Non-benzodiazepine anxiolytic; prototypical drug is buspirone
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What are the GABAa-alpha1 agonists?
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Zolpidem, Eszopiclone, Zaleplon
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