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72 Cards in this Set

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Drugs that end in -____ are benzos? Other benzos?
-olam
-epam
Clorazepate
Drugs that end in -____ are barbiturates? Others?
-barbital
Thiopental
Meprobamate
Chloral hydrate
Non-benzo/barbiturates anti-anxiety agents
Buspirone
Zolpidem
Zaleplon
Zopiclone
Gaboxadol
Which benzos have the shortest half life? Why?
Lorazepam
Oxazepam

They start as hydroxylated compounds --> glucoronidate compounds (the form they are excreted in)
They have less drowsy effects
Onset is slower, though, b/c t is absorbed from gut
Which benzo has the highest lipid solubility? What effect does this have?
Diazepam
Quick onset
Which classes of anxiolytics cross the placenta?
Benzos and barbiturates
How are barbiturates metabolized? Exceptions?
All are metabolized in liver, except fro phenobarbital
What role do norE and 5HT play in anxiety?
Incresaed levels improve mood and can treat anxiety and depression
Features of primary insomnia?
Resembles normal sleep pattern, but increased sleep latency, multiple awakenings, or decreased total sleep time
How long does it take for buspirone to relieve anxiety sx?
A week or more, so not ideal for treating anxiety from a phobia or panic d/o
What is used for emergency tx of seizures?
barbiturates (also useful for pre-surgical sedation)
What do BZ do to the sleep cycle?
Decrease time spent in slow wavev sleep (deepest stage of sleep) and decresae the time in REM
# of REM episodes decreased
Sleep latency decreased
Onset to REM decreased
What type of BZ should be used in ppl with sleep-onset insomnia and no daytime anxiety?
What abt for those with daytime anxiety?
Compounds with short t1/2
BZ with longer t1/2
What would happen to a pt with sleep apnea who took BZ?
Decreases upper airway muscle tone and decreased arousal response to hypoxia
Would be BAD
Do barbiturates or BZ have a better safety profile? Why?
BZ are safer
Higher therapeutic:lethal ratio
Which anxiolytics are useful for sedation?
Alprozolam
Buspirone
Chlordiazepoxide
Diazepam
Halazepam
Lorazepam (low dose)
Oxazepam
Phenobarbital
Prazepam
Which anxiolytics are useful for hypnosis?
Chloral hydrate
Estazolam
Flurazepam
Lorazepam (high dose)
Quazepam
Secobarbital
Temazepam
Triazolam
Zaleptlon
Zolpidem
All barbiturates are derived from _____?
Barituric acid
What confers the sedative-hypnotic effects of barbiturates?
alkyl or aryl group at position 5
What are thiobarbiturates? Example?
Contain S group, more lipid soluble and have mroe rapid onset of effects
Thiopental
What role does lipid solubility play in pharmacokinetics?
Incresaed lipid solubility --> acts quicker and longer
Where is the GABA binding site?
btwn the alpha and beta subunits
Where is the BZ binding pocket?
btwn the alpha and gamma subunits
What subunits do barbiturates require?
alpha and beta subunits (gamma not needed)
What do BZ do to GABAergic transmission?
increases the frequency of channel opening and increases receptor affinity for GABA
What is the alpha1 subunit associated with in BZ?
sedative and amnestic effects
What is the alpha2 subunit associated with in BZ?
anxiolytic effects
What is the alpha3 subunit associated with in BZ?
noradrenergic, serotonergic, and cholinergic neurons
What do barbiturates do to GABAergic transmission?
increse the duration of channel opening
What do barbiturates do to AMPA receptors?
reduce the glutamate mediated neuronal excitation
Which drugs are least likely to alter sleep patterns?
Zolpidem
Zaleplon
Phases of BZ/barbiturate biotransformation?
Removal of substituent at position 1 or 2 of diazepam ring --> N-desalkylated compound
Hydroxylation --> oxazepam or nordazepam
Conjugation of 3-OH compound with glucaronic acid
Which is the slowest part of the biotransformation process?
forming 3-OH from desalkylated compounds
How are BZ/barbs excreted?
in urine
What drug interacts with warfarin? Why?
Chloral hydrate
Displaces warfarin from its plasma proteins
Adverse side effects of BZ?
Euphoria
Impaired judgement
Loss of self-control
Hostility and violence at high doses
Anterograde amnesia
Tolerance/dependence
How does pharmacodynamic tolerance of BZ occur?
Down-regulation of BZ receptors
How is the t1/2 associated with w/d sxs?
longer t1/2 less likely to produce w/d
What can be used to alleviate w/d sx from short acting drugs?
longer acting ones (diazepam)
Contraindications for BZ?
other CNS depressants
Anti-convulsants
TCAs
OTC histamines
What can cross react with BZ?
Barbiturates and EtOh
How can BZ OD be treated?
Flumazenil (BZ antagonist) and conservative tx (mechanical ventilation, maintenance of plasma volume, etc)
What is flumzenil?
BZ receptor antagonist
Blocks actions of BZ, zolpidem, zaleplon
NOT effective against barbiturates, opioids, EtOH, or anesthetics
What aspect of BZ OD does flumezenil reverse?
sedative effect
reversal of respiratory distress less predictable
How is flumazenil administered?
IV
Has short t/12 (1hr), so must be given repeatedly
What is contraindication for flumazenil?
Seizures that are controlled with BZ
BZ dependent ptts
Co-ingestion of drugs that are epileptogenic in OD
Pts with head trauma or increased intracranial P
How does flumazenil work?
Binds GABA receptor and competitively inhibits BZ binding
Adverse side effects of barbiturates?
HA
Retrograde amnesia
Delirium
Prolonged somnolence
Paradoxical excitement myocardial, resp, circ depression
N/V
Nightmares, hallucinations
Tolerance
Minor w/d sx from barbiturates? Major w/d x?
anxiety, muscle twitching, tremor, etc
Convulsions, delirium, death
How do barbiturates and digitalis interact?
Increases the rate of its metabolism, decreasing effectiveness
What is the absolute contraindication of barbiturates in pts?
Pts with porphyria (deficiency in heme pathway, depositing porphyrin in the tissue)
Barbiturates increase porphyrin synthesis
Barbiturate OD features?
NOT reversed by flumazenil
Most common cause of death is from resp failure
What is buspirone used to treat?
GAD
NOT for acute anxiety or panic attacks
What are the cross tolerances of buspirone?
NONE!
MOA of buspirone?
interacts w DA and 5HT receptors
Contraindications for buspirone?
MAOIs
Features of zolpindem and zaleplon?
Have hypnotic but not anxiolytic actions
What antagonizes zolpidem and zaleplon?
Flumazenil
Adverse effects of zolpidem and zaleplon?
Zolpidem --> day after mental and motor depression and daytime sedation
Zaleplon has no more side effects than placebo
Contraindications for Zolpidem and Zaleplon?
Cimetidine
Elderly
Hepatic impairment
Compromised respiratory status
Zopiclone?
GABAA agonist
Longer lasting than Zolpidem and zaleplon
Reduces sleep latency, nighttime awakenings and increases total sleep time
What effect does Zopiclone have on sleep architecture at low doses?
None
What effect does Zopiclone have on sleep architecture at hiihg doses?
suppresses REM
Which of the Z drugs can be used long term?
Zopiclone
Contraindication for zopiclone?
Ingestion with large doses of other CNS depressents (ex: EtOH) = LETHAL!
Gaboxadol?
has lower affinity for gamma subunits, but also binds alpha, beta, delta receptors which are extrasynaptic
Benefits of gaboxadol?
Does not interact with BZ or EtOH (affects different receptors)
What role does gaboxadol play in sleep?
Decreases sleep latency and duration
Adverse side effects of gaboxadol?
NONE!
Which BZ are long acting?
Diazepam
Chlorazepate
Halazepam
Flurazepam
Which BZ are short or intermediate acting?
Triazolam
Midazolam
Alprazolam
What is the difference between how long and medium acting BZ are metabolized?
Long acting have 2 intermediate compounds before they get glucoronidated, short/medium acting have only 1 intermediate before they get glucoronidated