Benzo, Sedatives, Hypnotics
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| what type of effects do BDZs produce, and are these effects dose-dependent | BDZs fall into group known as sedative-hypnotics that produce dose-dependent CNS depressant effects
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| what term is recently replacing the term "sedative" in sedative-hypnotic drugs, and why | anxiolytic - more accurately describes the effects - reduced activity, excitement, and calming effect
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| what are hypnotics | drugs that produce drowsiness and facilitate sleep
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| at what concentration do anxiolytic effects occur compared to hypnotic effects, in sedative/anxiolytic benzodiazepenes | anxiolytic effects occur at much lower concentration
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| what is the difference with hypnotic benzodiazepenes | concentrations at which anxiolytic and hypnotic effects occur are much closer
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| what type of effects occur with BDZs at even higher doses than hypnotic effects | some anesthetic actions
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| what part of the CNS do BDZs cause little depression of | medullary centers controlling respiration
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| what is the implication of this | BDZs are safe when used alone
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| what can occur when they are combined with other sedative/hypnotic drugs (i.e. alcohol) | fatal overdose
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| what drugs were said to be general CNS depressants (no "flattening out" of curve representing CNS effects as dose gets to high levels) | barbiturates - BDZs level off
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| how many times greater is the lethal dose compared to the typical therapeutic dose for BDZs | 1000x
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| what is the chemical structure of BDZs like | three ring structure - "benzodiazepene" refers to a benzene ring fused to a diazepine ring - all clinically relevant BDZs also contain a 5-aryl ring
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| are these drugs lipophilic, and what variation exists | lipophilic, but lipophilicity can vary by 50 fold
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| what is determined by the level of lipophilicity | rate of onset of action
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| which BDZ is the most lipophilic | diazepam (Valium)
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| what are the targets of BDZs | GABA-A receptors in the CNS (gamma subunit)
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| what is the structore of GABA-A receptors like | they are chloride channels
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| when GABA binds to the receptor, what does it cause to happen to chloride flow, and what is the result | chloride influx into cell, resulting in hyperpolarization and inhibition of cell's activity
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| what does the GABA-A receptor mediate | most of rapid, inhibitory transmission in the CNS
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| what is the other GABA receptor in the brain, and what effect do BDZs have on this receptor | GABA-B receptor - BDZs have no actions, and this is not a chloride channel
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| what other substance do BDZs require to function, and why | require GABA, as they enhance GABA binding to the receptor - BDZs are unable to directly open the channel themselves
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| what do BDZs cause by increasing GABA affinity for the receptor | increase in opening frequency of GABA-A receptor/ion channels and increased chloride influx
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| what do barbiturates, such as phenobarbital, cause to happen at the GABA-A receptor | prolonged duration of opening, rather than increased frequency caused by BDZs
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| what are six classes of disease or purposes that BDZs can be used for | 1) anxiety disorders; 2) insomnia; 3) muscle spasms; 4) epilepsy/seizures; 5) sedation for medical/surgical procedures; 6) ethanol withdrawal
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| what group should be given a lower dose of BDZ, and how much lower | patients over 65 - give 1/2 to 1/3 as much
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| what is the most potent benzodiazepene | triazolam (halcion)
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| what fraction of patients with pathological anxiety seek treatment | one third
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| in what ways can pathological anxiety occur (4) | 1) primary anxiety disorder; 2) secondary anxiety disorder; 3) response to acute stress; 4) with other psychiatric illness
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| for what common and serious medical problem was treatment of anxiety said to reduce risk of recurrence | MI
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| what commonly used drug often causes anxiety | caffeine
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| for what primary anxiety disorders are benodiazepenes first line treatments of (2) | 1) GAD (generalized anxiety disorder); 2) panic disorder
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| what other primary anxiety disorders were mentioned (3) | 1) phobic disorders; 2) OCD; 3) PTSD
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| for generalized anxiety disorder, what BDZ is most effective | all are equally effective in preventing anxiety
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| what is the most frequently prescribed anxiolytic in the US | alprazolam (Xanax)
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| what are three other most frequently prescribed BDZs | 1) lorazepam (Ativan); 2) diazepam (Valium); 3) clonazepam (Klonopin)
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| what are the primary differences among BDZs | pharmacokinetic properties
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| what can BDZs be classified according to | half life
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| do any have very long half lives | yes, many
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| what factors should be considered when prescribing a BDZ (4 - unrelated to illness BDZ is being prescribed for) | 1) half-life; 2) age of patient; 3) presence of liver disease; 4) presence of other drugs which compete for metabolism
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| what are criteria for diagnosis of panic disorder (2) | 1) at least two unexpected attacks; 2) persistent worry about having another panic attack
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| what is the term for panic attacks that are more likely to occur, but not always, in response to a certain situation | situationally predisposed
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| what else can panic attacks occur with or without | agoraphobia (fear of places from which escape may be difficult)
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| what are the FDA approved BDZs for treatment of panic disorder | 1) alprazolam; 2) clonazepam
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| what are times until onset like for these drugs | quick
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| what should be remembered about dosing for panic disorder, compared to GAD | higher doses of alprazolam are required for treatment of panic disorder compared to GAD
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| what is often msitaken for panic attack | PSVT (paroxysmal supraventricular tachycardia)
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| what classes of phobic disorders are there (2) | 1) simple phobia; 2) social phobia
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| what drug is used for simple phobia | drugs contraindicated
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| how is social phobia differentiated from agoraphobia | social phobia involves fear of humiliation, rather than fear of being unable to escape
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| what is the first line treatment for social phobia | SSRIs
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| what BDZs are used (2) but are second line treatments | 1) alprazolam; 2) clonazepam
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| what secondary problem has increased incidence in social phobics | alcoholism (25% increase)
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| what is contraindicated in these cases | BDZs
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| what type of benzodiazepene treatment course should be used for insomnia | between one to four weeks
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| what two undesirable problems develop | 1) tolerance to hypnotic effects; 2) physial dependence
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| what are desirable characteristics for hypnotic agents (3) | 1) rapid onset; 2) sustained action to facilitate sleep; 3) no residual action by morning
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| of the BDZs, which fits these criteria the best | triazolam (halcion)
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| what are the advantages of triazolam (2) | 1) short duration of action; 2) effective for people who have difficulty going to sleep
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| what are disadvantages of triazolam (4) | 1) tolerance develops within a few days; 2) early morning insomnia; 3) rebound insomnia upon discontinuation; 4) REM sleep rebound (blocks REM)
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| what problem arises from blocked REM | underlying anger gets expressed (violence)
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| what BDZ is useful for people with frequent wakening, and why | temazepam - peak effect is 2-3 hours after oral dose - intermediate rate of onset
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| what other advantage does temazepam have | no hepatic metabolism
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| what is a very long acting BDZ hypnotic that is used primarily for inpatients (half life is over 100 hours) | flurazepam
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| how long can it be effective | up to four weeks
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| what is one disadvantage | causes daytime sedation
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| how does it affect sleep (3) | 1) shortens time to onset; 2) decreases number of wakenings; 3) increases duration
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| what is another fast acting BDZ with a considerably long half life (39 hours) | quazepam
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| how potent are quazepam and flurazepam | low potency compared to other BDZ
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| what should be noted about quazepam and flurazepam's effects on sleep | these less potent and more slowly eliminated drugs continue to improve sleep even after discontinuation
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| what is an intermediate onset BDZ with a half life ranging from 8-31 hours | estazolam
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| who are BDZs contraindicated in for insomnia, and why | patients with obstructive sleep apnea - they decrease muscular tone in upper airway and exaggerate the impact of episodes of apnea
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| what are the muscle relaxant actions of BDZs due to, and where does this action take place | increase in presynaptic inhibition in the spinal cord
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| what BDZs are indicated for muscle spasms/spasticity (2) | 1) diazepam; 2) clonazepam
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| in what situations are these drugs used for spasms/spasticity (2) | 1) muscle injuries; 2) degenerative disorders
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| what degenerative disorders were mentioned (2) | 1) cerebral palsy; 2) MS
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| which of these drugs has an advantage, and what is that advantage | clonazepam has the advantage that it can be used to reduce spasticity at non-sedative doses
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| what BDZs are used for epilepsy (2) | 1) clonazepam; 2) clorazepate
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| what type of seizures is clonazepam used for | absence seizures
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| what problem can occur, and when does it | tolerance within 1-6 months
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| what type of seizures is clorazepate used for | partial seizures
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| in what strategy is clorazepate used | used with other anticonvulsants
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| what BDZs are used for acute seizures / status epilepticus (2) | 1) lorazepam; 2) diazepam
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| what line of treatment are these drugs | DOCs for status epilepticus
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| which stops seizures in the shortest time, how long does it take, and why | diazepam (IV) stops seizures in one minute (reaches brain in 10 seconds) because it is the most lipophilic
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| what is the half life of diazepam (IV) | 15 minutes
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| what should diazepam be followed by | phenytoin
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| how long does lorazepam (IV) take to stop seizures, and what is its half life | stops seizures in about five minutes, half life 12-15 hours
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| what BDZ is used for sedation prior to invasive procedures | midazolam
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| what effects does it produce that are useful for this purpose (3) | 1) conscious sedation; 2) muscle relaxation; 3) anterograde amnesia
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| what doses are required for anterograde amnesia | preanesthetic doses
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| what doses are required to cause general anesthesia | does not cause general anesthesia by itself
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| what serious problem has midazolam caused during use for conscious sedation, and in what patient groups (2) | death due to respiratory arrest in: 1) patients premedicated with narcotics; 2) patients with COPD
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| what problem occurs frequently upon withdrawal of chronic alcohol that can be treated with BDZs | seizures
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| what BDZs are used for the management of acute effects of alcohol withdrawal (4) | 1) chlordiazepoxide; 2) diazepam; 3) clorazepate; 4) oxazepam
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| how is dosing determined | doses are titrated so that only a tremor is present during withdrawal
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| what dose usually needs to be given, and why | because of cross-tolerance at GABA-A receptor, you need to give max therapeutic dose of BDZ
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| how well are almost all BDZs absorbed, and from where | quickly, from the gut
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| what is the exception, and what is different about its absorption | clorazepate - it is decarboxylated in gastric juice to an active metabolite which is completely absorbed
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| what is the implication of the high lipid solubility of BDZs | taken up rapidly into brain (and other highly perfused organs) then redistributed to tissues less well perfused
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| what BDZs have fastest redistribution | highest lipid solubility
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| how important is redistribution from brain to other tissues in terminating CNS effects | can be as important as metabolism in terminating CNS effects
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| do BDZs cross the placenta, and are they secreted into breast milk | yes, yes
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| what transformation, and where, is necessary for elimination of BDZs | hepatic metabolism to water-soluble compounds
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| what important compounds are many BDZs metabolized to | active metabolites
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| what is the half time of the active metabolite like, compared to parent compound | longer
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| what is the implication of the longer half life of active metabolite | long half-lives can cause cumulative effects with multiple doses
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| what was said to be true about metabolism of those with short half lives (one of two things) | 1) don't have active metabolites; 2) active metabolites are quickly eliminated
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| what class of BDZs usually don't have active metabolites | hypnotic BDZs
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| what exception must we know | flurazepam is a hypnotic with active metabolites and a long half life
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| what is an ultra-short acting BDZ | midazolam (half life 1-2 hours)
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| what is a short acting BDZ | halcion
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| what are four long-acting BDZs mentioned | 1) chlordiazepoxide; 2) diazepam; 3) flurazepam; 4) quazepam
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| how many phases does hepatic metabolism of most BDZs occur in | three
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| what is phase one, and what does it result in | initial oxidation step results in N-desalkylated active metabolites
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| what is phase two, and what does it result in | hydroxylation at R3 yields another active metabolite
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| what is phase three, and what does it result in | conjugation of hydroxyl compounds with glucuronic acid yeilding inactive metabolites which are excreted in the urine
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| what is the fastest, second-fastest, and slowest reaction | phase 1 (fastest), phase 3, phase 2 (slowest)
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| what phase(s) are often bypassed in drugs with shorter half lives | phase 1, 2
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| in what patients are phase 1 and 2 reactions often reduced in (2) | 1) elderly; 2) liver disease
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| what related drugs were said to be able to increase their own metabolism, and how | barbiturates increase their own metabolism by inducing the hepatic microsomal enzymes
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| what three substances were mentioned to reduce or slow down phase 1 and 2 reactions (3) | 1) cimetidine; 2) oral contraceptives; 3) grapefruit juice
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| what BDZs have no active metabolites (3) | 1) lorazepam; 2) oxazepam; 3) temazepam
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| who would these be good options for (2) | 1) elderly; 2) liver disease
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| what effects of BDZ effects does tolerance develop more for (3) | 1) hypnotic; 2) muscle relaxant; 3) anti-convulsant (not anxiolytic effects)
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| when does physical dependence occur with BDZ treatment | if BDZs are given for long periods
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| which BDZs are physical dependence more likely with (what characteristics - 2) | 1) shorter acting; 2) more potent
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| what four were mentioned to be shorter acting and more potent | 1) alprazolam; 2) klonazepam; 3) lorazepam; 4) triazolam
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| what are symptoms of withdrawal from BDZs like | similar to those for which the BDZ was originally prescribed
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| what group of BDZs do not produce as severe withdrawal symptoms | those with longer half lives
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| what is indicated for people on BDZs for prolonged periods who are to stop taking them | gradual withdrawal
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| what are the two most common adverse effects | 1) drowsiness; 2) confusion
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| what are three other adverse effects | 1) motor incoordination; 2) cognitive impairment; 3) anterograde amnesia
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| when is anterograde particularly common | when BDZs are used with alcohol
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| how should doses for elderly be adjusted, and what BDZs are more appropriate | doses should be one third to a half of those typically prescribed, and BDZs with a shorter half life are more appropriate
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| what other problems can BDZs cause in the elderly | increased risk of falling (even with those drugs that have shorter half lives)
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| what are BDZs used during pregnancy linked to | cleft palate
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| besides pregnancy, when should women always avoid BDZs | when nursing
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| what drugs have an additive effect with BDZs (2) | 1) alcohol; 2) other sedative hypnotics
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| what can these cause when combined | respiratory depression
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| in what diseases are BDZs contraindicated (3) | 1) liver disease; 2) COPD; 3) obstructive sleep apnea
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| what is the problem in liver disease | effects are potentiated because of decreased metabolism
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| what BDZs are more appropriate for patients with liver disease | those without active metabolites
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| what drug was said to cause problems in patients with COPD (asthma, chronic bronchitis, and emphysema) and what problem does it casue | effects of midazolam on respiration are exaggerated in these patients
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| why are BDZs bad in sleep apnea | muscle relaxant effects aggravates disroders - use with caution in people who snore a lot, too
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| what non-benzodiazepene is useful for anxiety | buspirone (Buspar)
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| what is the MOA of buspirone | partial agonist at 5HT1A receptors (also has affinity for DA receptors, possibly a mixed agonist/antagonist)
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| what undesirable properties of BDZs is it missing (4) | 1) physical dependence; 2) withdrawal; 3) no cross-tolerance; 4) no interaction with alcohol
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| what else is a major difference between buspirone and BDZs | buspirone has a slow onset of action (2-4 weeks)
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| who is buspirone good for (2) | 1) elderly; 2) patients with substance abuse problems
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| what main non-benzodiazepene is good for insomnia | zolpidem (Ambien)
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| what is onset and half life like | quick onset (within 1-2 hours), half life of 2.5 hours
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| how do the effects of zolpidem compare to BDZs (what effects of BDZs does and doesn't it have) | it has selective hypnotic effect, but minimal anxiolytic, anticonvulsant, and muscle relaxant effects
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| who should doses be adjusted for, and how | should be adjusted down for elderly
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| what are side effects (4) | 1) dizziness; 2) headache; 3) confusion; 4) sleepiness
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| what drug can zolpidem interact with | alcohol
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| what is a similar option to zolpidem | zaleplon (Sonata)
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