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73 Cards in this Set
- Front
- Back
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Reason that Vd of BDZs is less than would be expected?
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High degree of plasma protein binding (70 - 99%)
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Where are BDZs metabolized?
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Liver
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BDZ that must be given I.M. or I.V.
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Lorazepam
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Mechanism of BDZs
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Positive allosteric modulators of GABA receptors
NOTE: have NO effect in absence of GABA NOTE: NOT all GABA receptors are affected by BDZs (ones in the brainstem are NOT) |
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Tolerance develops to all BDZ effects except for which one?
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Anxiolysis
Only low doses are required for this |
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What characteristics of a BDZ lead to increaesed withdrawal severity (2)?
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Higher Dosage
Shorter half-life |
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What effect do BDZs have when administered w/ other depressants?
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An ADDITIVE effect
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What is the only BDZ that does NOT suppress REM sleep?
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Zolpidem (Ambien)
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Half-life category for flurazepam
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Long half-life
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Unpleasant side effect of flurazepam
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"Drunk-like" driving the next morning
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These two BDZs are know for affecting driving the morning after
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Flurazepam
Temazepam |
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Two BDZs assoc. w/ earlier awakenings and heightened next day anxiety
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Estrazolam
Triazolam |
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Half-life category for triazolam
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Short half-life
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Effect mediated by binding the alpha-1 subunit of the GABA receptor
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Sedation
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Effect mediated by binding the alpha-2 subunit of the GABA receptor
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Anxiolysis
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Zolpidem binds exclusively to what subunit of the GABA receptor?
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alpha-1
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Half-life category of alprazolam
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Short half-life
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Use of alprazolam
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Treatment of severe anxiety
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These BDZs can be used in treating absence seizures (2)
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Clonazepam
Clorazepate NOTE: both of these have LONG half-lives NOTE: both of these can cause tolerance |
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This BDZ is the DOC for status epilepticus
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Lorazepam
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This is the most water soluble BDZ
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Lorazepam
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Half-life category for lorazepam
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Intermediate
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Half-life category for diazepam
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Long
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This BDZ is used against cocaine-induced convulsions
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Diazepam
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These BDZs are safe to use in pts. w/ hepatic disease (2)
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Lorazepam
Oxazepam |
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Half-life category for midazolam
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Short
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These BDZs are the two main ones that can be given I.M.
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Lorazepam
Midazolam |
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OD of this BDZ is known to cause respiratory arrest / death
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Midazolam
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This BDZ in particular is used to suppress symptoms of EtOH withdrawal
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Chlordiazepoxide
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How are BDZs administered so as to prevent peak-dose sedation?
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Small, divided doses
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This BDZ is known for having active metabolite accumulation
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Flurazepam
NOTE: can pose a problem in hepatic disease, elderly, etc. |
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These BDZs can be used in pre-anesthesia
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Midazolam
Clorazepate Diazepam Lorazepam |
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These BDZs are used in status epilepticus
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Lorazepam
Diazepam |
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This BDZ is also used as an anti-emetic
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Lorazepam
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What type of drug is flumazenil?
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BDZ antagonist
NOTE: binds same sites as BDZs (But, produces no effect of its own) |
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Why may you need repeated administrations of flumazenil to counter a BDZ?
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It has a SHORT half-life of < 1 hr.
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What receptor activities does buspirone have?
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PARTIAL AGONIST @ 5-HT1 receptors
NOTE: effects are NOT antagonized by flumazenil |
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Relatively, how does buspirone's efficacy compare to that of BDZs?
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LESS efficacious than BDZs
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What are some of the benefits of buspirone over BDZs (2)?
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Very low abuse potential
Does NOT potentiate other CNS depressants |
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Why can't NON-BDZ sedative hypnotics usually be used for anesthesia?
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There is no gap between anesthetic dose and CV collapse
NOTE: there are exceptions in circumscribed conditions |
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What characteristic of unconsciousness caused by NON-BDZ SHs is imporant?
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NON-ANALGESIC
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Tolerance develops rapidly to all effects of NON-BDZ SHs except what?
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Lethal respiratory/CV depression
NOTE: chronic use increases lethal dose only very slightly |
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How does tolerance to NON-BDZ SHs affect that towards BDZs, etc.?
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CROSS-TOLERANCE
(extends to alcohol, BDZs, most general anesthetics) |
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Which NON-BDZ SH has the least problem w/ dependence/withdrawal?
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Phenobarbital
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Generally, what is the range of half-lives of NON-BDZ SHs?
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4 - 48 hrs
NOTE: exception is phenobarbital (has a longer half-life) |
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This side effect of NON-BDZ SHs can interfere w/ hypnotic effect
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Hyperalgesia
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Mechanism of NON-BDZ SHs @ LOW doses
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Potentiate GABAergic transmission
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Mechanism of NON-BDZ SHs @ HIGH doses
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GABA-INDEPENDENT Chloride influx
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Mechanism of NON-BDZ SHs @ VERY HIGH doses
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Non-specific depressant effects
Perturberance of membranes |
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Use of phenobarbital
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Anti-convulsant
(3rd line against partial seizures) |
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Special characteristics of phenobarbital (3)
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Longer lasting
LESS ability to induce GABA-independent activity LESS serious withdrawal |
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Sudden withdrawal of this NON-BDZ SH can induce status epilepticus
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Phenobarbital
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Use of secobarbital
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Pre-anesthetic
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Use of thiopental
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Anesthesia
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Special characteristics of thiopental (2)
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Very short DOA, 10 minutes
Very lipid soluble |
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This NON-BDZ SH is used to treat migraines
(often combined w/ analgesic & coffee) |
Butalbital
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This drug can be used as an antidote to EPS caused by neuroleptics
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Diphenhydramine
NOTE: it is contained in OTC sleep-aid preparations |
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Uses of Hydroxyzine (2)
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Pre-anesthetic
N&V due to motion sickness (Remember, grouped w/ Meclizine, Dimenhydrinate) |
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These drugs are still prescribed for anxiety/insomnia
(BUT, THEY SHOULDN'T BE) |
Meprobamate
Chloral Hydrate |
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What is the RLS of alcohol metabolism?
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Ethanol --> Acetaldehyde
(catalyzed by alcohol dehydrogenase) |
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What negative effect does acetaldehyde have on liver enzymes?
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Depletes hepatic glutathione
(sets stage for "bad things" (Tylenol toxicity, etc.)) |
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What is the second step in alcohol metabolism?
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Acetaldehyde --> Acetic acid
(catalyzed by acetaldehyde dehydrogenase) |
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What enzyme does Disulfiram inhibit?
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Acetaldehyde dehydrogenase
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What are the kinetics of alcohol in blood?
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Zero-order kinetics
Blood concentration declines LINEARLY w/ time (Alcohol dehyd. get saturated @ low BACs) |
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4 main effects of alcohol in body
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Increased GABA receptor function
Disruption of normal sleep patterns Overall vasoconstriction (Inc. BP) Diuresis NOTE: there is CUTANEOUS vasodilation |
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What two types of drugs are used in acute alcohol detoxification?
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BDZs and anti-convulsants
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Alcohol can be used to treat poisoning by what two substances?
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Methanol
Ethylene glycol |
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Why is the therapeutic expectation of Disulfiram low?
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Depends upon pt. cooperation
NOTE: disulfiram causes aversive effects after alcohol ingestion |
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What receptor activity does naltrexone have?
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Opiate receptor antagonist
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What pts. is disulfiram contraindicated in?
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Those exposed to heavy metals
(Side effects include heavy metal chelation) |
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What effects does naltrexone have (2)?
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Attenutates the reward effects of alcohol
Decreases relapse to heavy drinking |
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What effects does acamprosate A have (2)?
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May attenuate alcohol craving
Reduces relapse rate after detox |
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What is the main side effect of acamprosate A?
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Diarrhea
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