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89 Cards in this Set
- Front
- Back
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What is alprazolam?
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benzodiazepine
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what is chloradiazepoxide?
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benzodiazepine
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What is clonazepam?
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benzodiazepine
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What is Clorazepate?
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benzodiazepine
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What is diazepam?
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benzodiazepine
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What is flurazepam?
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benzodiazepine
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What is lorazepam?
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benzodiazepine
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What is marzipam?
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benzodiazepine
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What is midazolam?
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benzodiazepine
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What is oxazepam?
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benzodiazepine
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What is temazepam?
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benzodiazepine
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What is Triazolam?
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benzodiazepine
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What is flumazenil?
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benzodiazepine antagonist
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What is phenobarbital?
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barbituate
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What is thiopental?
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barbituate
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What is secobarbital?
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barbituate
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What is buspirone?
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non-benzodiazepine sedative hypnotic
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What is zolpidem?
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sedative hypnotic - imidazopyridine derivative
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What is Zaleplon?
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sedative hypnotic
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What is eszopiclone?
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sedative hypnotic
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What is Ramelteon?
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sedative hypnotic
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What is the action of benzodiazepines?
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increases the frequency of GABA mediated chloride channel opening
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Which receptor do benzodiazepines bind to?
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GABAa receptor
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Which 3 benzodiazepines can be given by IV?
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Diazepam, midazolam and Lorazepam
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How are benzodiazepines absorbed?
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given orally - well absorbed by the GI
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How are benzodiazepines metabolized?
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hepatic metabolism and secretion
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Which 6 benzodiazepines are metabolized to their active state?
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flurazepam, diazepam, chlordiazepam, chlorazepate, alprazolam, triazolam
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Which 5 benzodiazepines are not metabolized to their active state?
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lorazepam, oxazepam, midolazam, temazepam, clonazepam
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What is the action of barbiturates?
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depress the midbrain reticular foramtion and facilitate and prolong the inhibitor effects of GABA and glycine
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Where do barbiturates bind?
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interacts with a site on the chloride channel that is neither the GABA receptor nor benzodiazepine receptor site
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What is the effect of barbiturates on the GABA chloride channel?
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increases the duration of GABA mediated chloride ion channel opening
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How are barbiturates absorbed?
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given orally - well absorbed by the GI
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How are barbiturates metabolized?
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hepatically except for phenobarbital - excreted unchanged in the urine
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Can sedative hypnotics cross the placenta?
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Yes, they can also be detected in breast milk
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What other types of drugs have additive effects when taken with sedative hypnotics?
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opioids, analgesics, alcohol, anticonvulsants, phenothiazines
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What 3 types of drugs have enhanced CNS depression when taken with sedative hypnotics?
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antihistamines, anti-hypertensives and tricyclic anti-depressants
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What are the 5 therapeutic effects of sedative hypnotics?
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1. sedation with relief of anxiety, 2. hypnosis, 3. anesthesia with loss of consciousness, amnesia and suppression of relfexes, anticonvulsant, muscle relaxation
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What happens to REM sleep with high doses of sedative/hypnotics?
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REM sleep is decreased, REM rebound can occur following termination
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Which benzodiazepine is a muscle relaxant at non-sedative doses?
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diazepam
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What are the side effects of sedative hypnotics?
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ataxia, nystagmus, confusion, slurred speech, coma
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Does psychological or physiolgical dependence occur with sedative hypnotics?
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BOTH!
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What drug is used to treat anxiety states?
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intermediate to long duration drugs - diazepam, chlordiazepoxide, chlorazepate, flurazepam, clonazepam, alprazolam
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What drug is used to treat sleep disorders?
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short duration drugs - lorazepam, oxazepam, temazepam
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What drugs is used to treat grand mal seizures?
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diazepam or phenobarbital
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What is used to treat muscle spasticity?
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diazepam
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What is used to treat phobic anxiety states?
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alprazolam
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What is used to induce anesthesia?
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midazolam or thiopental
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What is used for general anesthesia?
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midazolam
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What is used for detoxification?
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longer acting drugs - clonazepam, flurazepam, diazepam, chlordiazepam, chlorazepate
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What benzodiazepine has ultra short duration?
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midazolam and Triazolam (not on the market due to weird side effects)
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What is midazolam used for?
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induction of anesthesia and to produce amnesia for short procedures
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What are lorazepam, oxazepam and temazepam used for?
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sleep inducers and anxiolytics
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What is the duration of lorazepam, oxazepam and temazepam?
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short to intermediate duration
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What is the duration of alprazolam?
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medium duration
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What is alprazolam used for?
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anxiolytic and may have antidepressant effects
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When is alprazolam commonly prescribed?
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to cancer patients
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What is the duration of diazepam, chlordiazepoxide and chlorazepate?
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long duration
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What is the active metabolite alprazolam?
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alpha-hydroxy-alprazolam
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What is the active metabolite of chlordiazepoxide and chlorazepate?
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nor-diazepam
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What is unique about diazepam?
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it has potency in the spinal cord to relieve muscle spasms
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What are diazepam, chlordiazepoxide and chlorazepate used for?
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anziolytic
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What duration does flurazepam have?
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long duration
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What is flurazepam used for?
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anxiolytic
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What is the major side effect of flurazepam?
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extreme day time sedation
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What is the active metabolite of flurazepam?
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desmethyl-furazepam
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What duration does clonazepam have?
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long
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What is clonazepam used for?
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chronic treatment of epilepsy
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What is the action of flumazenil?
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competitive antagonist, reverses CNS depressant effects
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How is flumazenil administered?
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IV
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How is flumazenil metabolized?
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rapidly metabolized by the liver - has short half life
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What may occur with fluemazenil in patients who have a physical dependence of benzodiazepines?
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it may precipitate withdrawal symptoms
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What is buspirone used for?
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to treat anxiety - does so without excessive sedation or euphoria
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How long does buspirone take to be clinically significant?
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more than a weak
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What is the mechanism of action of buspirone?
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it is a partial agonists for brain serotonin receptors
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Is there rebound anxiety or withdrawal symptoms?
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No, thus it is not a controlled substance
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How is buspirone absorbed?
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through the GI, given orally
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How is buspirone metabolized?
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hepatic metabolism - significant first pass effect
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What is zolpidem used for?
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to induce sleep
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What is the mechanism of action of zolpidem?
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binds selectively to a subtype of benzodiazepine recetpors and facilitates GABA mediated induction of neural suppression
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What antagonizes zolpidem?
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flumazenil
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How is zolpidem absorbed and metabolized?
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Absorbed through the GI - given orally; metabolized by the liver via oxidation and hydroxylation
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What is zaleplon used for?
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sleep induciton
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Where does zaleplon act?
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on the benzodiazepine receptor site
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What is unique about zaleplon in relation to sleep cycles?
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It produces little interruption of basic sleep patterns
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What is eszopiclone used for?
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falling asleep and staying asleep - has longer half life
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What can occur with eszopliclone use?
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drug accumulation
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What is ramelteon used for?
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to treat insomnia characterized by difficulty with sleep onset
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What is the mechanism of action of ramelteon?
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melatonin receptor agonist on the MT1 and MT2 receptors
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What is thiopental used for?
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given IV to induce anesthesia - it is rapidly acting
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