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73 Cards in this Set

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Reason that Vd of BDZs is less than would be expected?
High degree of plasma protein binding (70 - 99%)
Where are BDZs metabolized?
Liver
BDZ that must be given I.M. or I.V.
Lorazepam
Mechanism of BDZs
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)
Tolerance develops to all BDZ effects except for which one?
Anxiolysis

Only low doses are required for this
What characteristics of a BDZ lead to increaesed withdrawal severity (2)?
Higher Dosage
Shorter half-life
What effect do BDZs have when administered w/ other depressants?
An ADDITIVE effect
What is the only BDZ that does NOT suppress REM sleep?
Zolpidem (Ambien)
Half-life category for flurazepam
Long half-life
Unpleasant side effect of flurazepam
"Drunk-like" driving the next morning
These two BDZs are know for affecting driving the morning after
Flurazepam
Temazepam
Two BDZs assoc. w/ earlier awakenings and heightened next day anxiety
Estrazolam
Triazolam
Half-life category for triazolam
Short half-life
Effect mediated by binding the alpha-1 subunit of the GABA receptor
Sedation
Effect mediated by binding the alpha-2 subunit of the GABA receptor
Anxiolysis
Zolpidem binds exclusively to what subunit of the GABA receptor?
alpha-1
Half-life category of alprazolam
Short half-life
Use of alprazolam
Treatment of severe anxiety
These BDZs can be used in treating absence seizures (2)
Clonazepam
Clorazepate

NOTE: both of these have LONG half-lives
NOTE: both of these can cause tolerance
This BDZ is the DOC for status epilepticus
Lorazepam
This is the most water soluble BDZ
Lorazepam
Half-life category for lorazepam
Intermediate
Half-life category for diazepam
Long
This BDZ is used against cocaine-induced convulsions
Diazepam
These BDZs are safe to use in pts. w/ hepatic disease (2)
Lorazepam
Oxazepam
Half-life category for midazolam
Short
These BDZs are the two main ones that can be given I.M.
Lorazepam
Midazolam
OD of this BDZ is known to cause respiratory arrest / death
Midazolam
This BDZ in particular is used to suppress symptoms of EtOH withdrawal
Chlordiazepoxide
How are BDZs administered so as to prevent peak-dose sedation?
Small, divided doses
This BDZ is known for having active metabolite accumulation
Flurazepam

NOTE: can pose a problem in hepatic disease, elderly, etc.
These BDZs can be used in pre-anesthesia
Midazolam
Clorazepate
Diazepam
Lorazepam
These BDZs are used in status epilepticus
Lorazepam
Diazepam
This BDZ is also used as an anti-emetic
Lorazepam
What type of drug is flumazenil?
BDZ antagonist

NOTE: binds same sites as BDZs
(But, produces no effect of its own)
Why may you need repeated administrations of flumazenil to counter a BDZ?
It has a SHORT half-life of < 1 hr.
What receptor activities does buspirone have?
PARTIAL AGONIST @ 5-HT1 receptors

NOTE: effects are NOT antagonized by flumazenil
Relatively, how does buspirone's efficacy compare to that of BDZs?
LESS efficacious than BDZs
What are some of the benefits of buspirone over BDZs (2)?
Very low abuse potential
Does NOT potentiate other CNS depressants
Why can't NON-BDZ sedative hypnotics usually be used for anesthesia?
There is no gap between anesthetic dose and CV collapse

NOTE: there are exceptions in circumscribed conditions
What characteristic of unconsciousness caused by NON-BDZ SHs is imporant?
NON-ANALGESIC
Tolerance develops rapidly to all effects of NON-BDZ SHs except what?
Lethal respiratory/CV depression

NOTE: chronic use increases lethal dose only very slightly
How does tolerance to NON-BDZ SHs affect that towards BDZs, etc.?
CROSS-TOLERANCE
(extends to alcohol, BDZs, most general anesthetics)
Which NON-BDZ SH has the least problem w/ dependence/withdrawal?
Phenobarbital
Generally, what is the range of half-lives of NON-BDZ SHs?
4 - 48 hrs

NOTE: exception is phenobarbital
(has a longer half-life)
This side effect of NON-BDZ SHs can interfere w/ hypnotic effect
Hyperalgesia
Mechanism of NON-BDZ SHs @ LOW doses
Potentiate GABAergic transmission
Mechanism of NON-BDZ SHs @ HIGH doses
GABA-INDEPENDENT Chloride influx
Mechanism of NON-BDZ SHs @ VERY HIGH doses
Non-specific depressant effects
Perturberance of membranes
Use of phenobarbital
Anti-convulsant
(3rd line against partial seizures)
Special characteristics of phenobarbital (3)
Longer lasting
LESS ability to induce GABA-independent activity
LESS serious withdrawal
Sudden withdrawal of this NON-BDZ SH can induce status epilepticus
Phenobarbital
Use of secobarbital
Pre-anesthetic
Use of thiopental
Anesthesia
Special characteristics of thiopental (2)
Very short DOA, 10 minutes
Very lipid soluble
This NON-BDZ SH is used to treat migraines
(often combined w/ analgesic & coffee)
Butalbital
This drug can be used as an antidote to EPS caused by neuroleptics
Diphenhydramine

NOTE: it is contained in OTC sleep-aid preparations
Uses of Hydroxyzine (2)
Pre-anesthetic

N&V due to motion sickness
(Remember, grouped w/ Meclizine, Dimenhydrinate)
These drugs are still prescribed for anxiety/insomnia
(BUT, THEY SHOULDN'T BE)
Meprobamate
Chloral Hydrate
What is the RLS of alcohol metabolism?
Ethanol --> Acetaldehyde
(catalyzed by alcohol dehydrogenase)
What negative effect does acetaldehyde have on liver enzymes?
Depletes hepatic glutathione
(sets stage for "bad things" (Tylenol toxicity, etc.))
What is the second step in alcohol metabolism?
Acetaldehyde --> Acetic acid
(catalyzed by acetaldehyde dehydrogenase)
What enzyme does Disulfiram inhibit?
Acetaldehyde dehydrogenase
What are the kinetics of alcohol in blood?
Zero-order kinetics

Blood concentration declines LINEARLY w/ time
(Alcohol dehyd. get saturated @ low BACs)
4 main effects of alcohol in body
Increased GABA receptor function
Disruption of normal sleep patterns
Overall vasoconstriction (Inc. BP)
Diuresis

NOTE: there is CUTANEOUS vasodilation
What two types of drugs are used in acute alcohol detoxification?
BDZs and anti-convulsants
Alcohol can be used to treat poisoning by what two substances?
Methanol
Ethylene glycol
Why is the therapeutic expectation of Disulfiram low?
Depends upon pt. cooperation

NOTE: disulfiram causes aversive effects after alcohol ingestion
What receptor activity does naltrexone have?
Opiate receptor antagonist
What pts. is disulfiram contraindicated in?
Those exposed to heavy metals
(Side effects include heavy metal chelation)
What effects does naltrexone have (2)?
Attenutates the reward effects of alcohol
Decreases relapse to heavy drinking
What effects does acamprosate A have (2)?
May attenuate alcohol craving
Reduces relapse rate after detox
What is the main side effect of acamprosate A?
Diarrhea