Neuropharm Anxiolytics And Hypnotics Flashcards
Barbiturates, phenobarbituates, benzodiazepines, benzodiazepine antidote,
Ok
Zolpidem (ambien)
Benzodiazepine like hypnotic drug intended for short term management of insomnia in patients who have difficulty staying asleep
Side effects zolpidem (ambien)
Daytime drowsiness, angioedema, strange sleep behaviors such as sleep eating and sleepwalking.
Why zolpidem taken right before bedtime
Rapid onset
MOA zolpidem (ambien
Hypnotic
Binds to the benzodiazepine-1 receptor site of the GABA receptor-chloride channel complex acting as an agonist
Purpose of zolpidem
Lengthen sleep time and minimize awakenings.
Unlike other benzodiazepines, zolpidem has no ____
Anti anxiety, muscle relaxing, or anticonvulsant properties
Indications for zolpidem
Insomnia
Side effects zolpidem
Daytime drowsiness, bizarre sleep behaviors (careful falling asleep while driving), angioedema
Considerations zolpidem
Short term administration
Take immediately before bed
Triazolan (hail on)
Rapid onset benzodiazepine that potentiating the inhibitory effects of GABA..causing CNS depression and is indicated for treatment of insomnia
Side effects triazolam (hail on)
Anterograde amnesia, paradoxical excitement, rebound insomnia, confusion, respiratory depression, and hypotension
Who is triazolam (hail on) contraindicated in
Pregnant women
Triazolam is recommended for short term. Why
Dependency risk
MOA triazolam
Rapid onset benzodiazepine binds to GABA receptor , increasing frequency of chloride channel opening. As chloride ions enter the channels spanning across the neuronal membrane, the neuron becomes highly negative and decreases its ability to fire electrical impulses. This action enhances the inhibitory effects of GABA and causes CNS depression
Indications for triazolam
Insomnia
Promotes sleep affecting through the cortical areas of the brain.short term acute insomnia like jet lag (not for maintain sleep it is short acting, starts sleep! Not maintain)
Side effects triazolam
Rebound insomnia, respiratory depression, hypotension, paradoxical excitement, amnesia, confusion
Contradcitions triazolam
Pregnant -teratogen lipid soluble and cross placenta
Causes congenital malformations in fetus and cns depression near term
Warn female patients of baby bearing age
Consideration triazolam
Short term administration
Hypnotic effects can develop quick
Faster than other benzodiazepines
Nonbenzodiazepine hypontics
Zolpidem (ambien), zaleplon and eszopiclone
Indication for nonbenzodiazepine hypnotics
Short term treatment of insomnia
Are nonbenzodiazepine hypnotics more or less selective than benzodiazepines
More as they are not indicated for chronic anziety , muscular relaxation, or seizure disorders
MOA nonbenzodiazepine hypnotics
Act on BZ1 GABA subtype receptors to increase chloride conductance. They are rapidly metabolized by the liver and have a short half like of roughly 2.5 hours
Side effects nonbenzodiazepine hypnotics
Ataxia, confusion
How treat overdose of nonbenzodiazepine hypnotics
Flumazenil
Indications for nonbenzodiazepine hypnotics
Insomnia
MOA nonbenzodiazepine hypnotics
Short half life
Acts on BZ1 GABA receptor
Less dependence
Zolpidem (ambien)
Commonly used drug of this class and is also known as ambien. Reduce sleep onset latency
Also zaleplon and eszopiclone
Side effects nonbenzodiazpipine hypnotics
Ataxia confusion
Buspirone
Generalized anxiety but often combined with SSRI to treat clinical depression
MOA buspirone
5-HT1A receptor partial agonist and increases the release of dopamine and norepinephrine
Helps mediate anxiety and depressive symptoms
Bind D2 also
Hallmark of buspirone
Low side effects does not cause addiction, sedation, or tolerance (unlike benzodiazepines) does not interact with alcohol to cause respiratoy depression
Indication buspirone
Generalized anxiety
Also combined with SSRI therapy to. Treat clinical depression
MOA buspirone
Releases dopamine and NE-blocks presynaptic mesolimbic D2 autoreceptors in lower doses and yields increased dopamine synthesis and release. Also increases firing in the locus ceruleus-an area of brain where NE cell bodies are found in high concentrations, increasing NE
Also stimulated 5-HT1A receptors -partial agonist mediates its anxiety and anti depressive effects and because this drug is partial agonist, it has a lower side effect profile
Side effect buspirone
Low side effect
No alcohol interaction
Trazodone
Atypical antidepressant primarily indicated for insomnia
At high doses, trazodone is a ___
Antidepressant
MOA trazodone
Inhibits serotonin reuptake, but also displays serotonergic receptor antagonism
Side effects trazodone
Sedation and orthostatic hypotension from blockade a1
Priapism-erection lasting long time (over 4 hours)
Indications for trazodone
Insomnia also depression
MOA trazodone
Inhibit serotonin reuptake
Alpha blocker
Side effects trazodone
Sedation, priapism (trazoBONE), orthostatic hypotension
