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36 Cards in this Set

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Barbituates?
-have a linear progression to hypnosis, coma, and death and that makes them unsutiable for outpatient use
Benzodiazapenes?
-require a proportionatley greater dose to achieve higher levels of CNS depression, giving them a greater margin of safety.
Ideally a anxiolytic should?
-decrease anxiety with little or no decrease in mental or motor fxn.
-Depress CNS to point of drowsiness allowing onset and maintenance of sleep
-Should have little or no effect on normal stages of sleep
Benzo's are used for?
GAD
Examples of older Benzo's?
-Diazepam
-Chlordiazepoxide

Newer:
-Lorazepam
-Alprazolam
-Clonazepam
Diazapam=?
Clonazepam=?
Diazepam = muscle relaxer
Clonazepam= mania and panic attacks
What two drugs can be combined for the tx of the agitation in a psychotic pt?
Clonazepam and Lorazepam
Where do all Benzo's metabolize?
In the liver
Oxidation and conjugation of Benzo metablites?
Oxidation = most benzo's
Conjugation = generally follows oxidation
Consequences of some extremely long half life benzo's?
-liver dsfxyn in elderly
-multiple acrive metabolites, esp. with long t1/2 may lead to cummulative CNS effects with multiple dosing
Avoid Benzo's with?
Avoid Benzo's with the ELDERLY!
MOA of Benzo's?
-Bind to GABA receptor within the CNS
-GABA receptor is the major inhibitory NT in the CNS
-GABA controlled chloride channel
Benzo's act to INCREASE FREQUENCY of channel opening*
Benzo's potentiate the effects of GABA by adding to the hyperpolarization of the membrane:
-Not GABA agonists
-result in a decrease firing of stimulatory neurons
Pharm effects of Benzo's?
-Sedation
-Hypnosis
-Anesthesia
-Anticonvulsant effects
-Resp and CV effects
Sedation effect with Benzo's?
-DIfficult to seperate sedation from anxiolytic effects with Benzo's
-Trycyclic antidepressants have sedation effects but DO NOT WORK in anxiety disorders
-Amnerograde amnesia*
Which two benzo's are used in Status Epilepticus?
-Lorazepam
-Diazepam
Respiration and CV effects with Benzo's?
-at theraputic doses=risk only with pts with Resp dz and CV disease (CHF)
- Cause of death with OD is generally due to depression fo the Medullary Response Center
Tolerance with Benzo's?
-Chronic use may result in tolerance, physical, and psychological dependance
-Withdrawl symptoms are varied between individuals and the dose used.
-Sxms of withdrawl may last few days to weeks
Somatic Sxms of withdrawl of Benzo's
-insomnia
-tremor
-nasuea
etc...
Psychological sxms?
-anxiety
-poor concentration
-irritability
etc...
perceptual sxms?
-poor coordination
-mild paranoia
-mild confusion
Withdrawl may be minimized by?
TAPERING THE DOSE
If long term use: decrease by 10% per week
Indications for Bezo use?
-Anxiety
-Insomnia
-Sedation and amnesia before proceedures
-tx of seizure disorder
-acute alcohol withdrawl syndrome
-Panic Attacks
Dont use Benzo's with?
-Signif liver DZ
-Lactation (valium)
-Preg Cat D (Benzo's pass freely through placenta
-Other CNS depressant drugs, alcohol.
**DO not use with the ELDERLY!
The most common reversible cause of confusional states in the elderly is?
-The overuse of sed/hypnotics
Zolpidem Tartrate (Ambien)?
-Non benzo hyptnotics
-classified as a hypnotic
-very little muscle relaxant effects
MOA of Zolpidem (Ambien)?
-Similar to Benzo's-attaches to alpha-subunit of the GABA-benzodiazepine
- more specific than bensos in the drug recepter interaction
-Preserves (stage 3 and 4) of deep sleep
Pharmicokinetics of Zolpidem?
-Rapid onset, short half life
-food will reduce and delay peak concentrations
-Metablolized in the liver and elim in urine
Zolpidem indications?
-Insomnia short term
-does not cause rebound insomnia at rec. dosages
-mild next day residual effects
-effec in short term and chronic insomnia
-Min or no changes in REM at rec. doses.
ADVSE RXNS with Zolpidem?
-daytime hdche and drowsiness
-pretty safe
-may be fatal with other drugs
-Preg cat C
-Lactation-DO NOT USE
Eszopiclone (Lunesta)
-Non-benzodiazapine
-hypnotic
-unrelated to benzo or barbs
Lunesta MOA?
-Similar to benzo:
binds GABA receptor complezeas located close to or coupled to benzodiazepine receptors
Lunesta Pharmokinetics?
-Rapidly absorbed
-no active metabolites
Inidcatins:
-Insomnia, *only agent not restricted to short term tx
ADVSE RXN Lunesta
-Same as Ambien but with dysgeusia
Buspirone (BusPar)?
-Used for GAD
-No anticonvulsant activity like Benzo have
-no muscle relaxant like some benzo
-No sedative, hypnotic, motor impairment or dependance...NO WITHDRAWL SXMS!
MOA unknown
-Rapidly absorbed with first pass elim, 95% protein bound.
-Excretion = renal
Barbs?
-not as safe and benzo's
-not used for anxiety or hypnosis in outpatients
-DOC for Oregon Death with Dignity Act
-MOA GABA channels