Sedatives-Hypnotics/Anxiolytics
Terms
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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