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61 Cards in this Set
- Front
- Back
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What are the top 3 prescribed benzos?
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1. Alprazolam
2. Lorazepam 3. Diazepam |
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What does an effective Sedative (anxiolytic) agent do?
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Reduces anxiety.
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What does a hypnotic drug do?
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Produces drowsiness, onset and maintenance of sleep.
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What effect does a Sedative-Hypnotic drug have?
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Induces sleep in high doses.
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What kind of response is anxiety and define it?
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Adaptive - prepares a person to react to a threatening event.
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What kind of response is maladaptive and define it.
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Maladaptive - response to psychological stress - may impair normal daily activities
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Define acute anxiety disorder
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Result of recent adverse event: illness, death ....
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Define panic disorder
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acute episode of severe anxiety leading to symptoms of impending doom
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Define OCD
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obsessions and compulsions w/recurring or persistent throughts
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Define GAD
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persistent state of fear/apprehension
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Benzos end in?
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lam/pam
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Barbs end in?
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tal
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name 2 sedative-hypnotic/anxiolytic drugs classified as antihistamines
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diphenhydramine, hydoxyzine
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name the sedative hypnotic drugs classified as others...
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chloral hydrate, melatonin, zolpidem, zaliplone, esZopiclone
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nonsedating anxiolytic drugs
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buspirone, propranolol
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Benzos are better than barbs because....
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doubling the dose of benzos doesnt double the effect
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How does propranolol work?
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non-selective beta blocker; it blocks the action of epinephrine on both β1- and β2-adrenergic receptors
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How does Buspirone work?
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serotonin receptor agonist. similar to diazepam and can be used to treat GAD
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What are the top 3 "other" prescribed anxiolytics?
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1. Zolpidem
2. Buspirone 3. Phenobarbital |
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Name a short acting benzo and its use
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Midazolam (2-6 hrs) - colonoscopy
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Name an intermed acting benzo and its use
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Alprazolam (12-15 hrs) - panic disorder
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Name a long acting benzo and its use
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Diazepam (20-80 hrs) - grand mal seizures
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Where are benzos most effectively absorbed?
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at high pH in the duodenum - hence slower onset of action
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Where are barbs absorbed?
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low pH of stomach - rapid absorption
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How do acidic drugs act in the stomach?
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acidic drugs are neutral in the stomach so they get into the blood faster
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What is the MOA of anxiolytics
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1. bind GABAa
2. Cl- channel 3. inhibitory NT in CNS |
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What does GABA do in the CNS?
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it is the major inhibitory NT
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What are the binding sites of GABA receptors?
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alpha 1,2,3,5
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what does binding of a benzo agonist do?
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1. inc affinity of GABA to GABAa rec
2. inc freq of Cl channel opening 3. GABA-ergic inhibition at all levels |
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What is the MOA of Diazepam?
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full agonist at all subtypes of GABAaR
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What are the side effects of Diazepam?
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ataxia
amnesia (anterograde)/cognition impairment sedation tolerance/abuse |
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What are the therapeutic properties of Diazepam?
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anxiolytic
anticonvulsant |
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What are the behavioral effects at alpha 1 w/benzo?
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selective ligands (Zolpidem) - sedative
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What are the effects of alpha2/alpha3 with benzo?
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anxiolysis
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what are the effects of alpha5 with benzo?
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cognition - hippocampal receptors
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What are the 3 nonbenzos
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Zolpidem, esZopiclone, Flumazenil
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what is esZopiclone used for?
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chronic insomnia - approved for long term use
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Where do barbs bind?
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a site on GABAa chloride ionophore-distinct from sites to which benzos bind
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How do barbs affect the chloride channel opening?
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increase the duration of GABA mediated chloride channel opening leading to increased membrane polarization
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How do barbs act with AMPA glutamate receptors?
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block the AMPA glutamate receptor leading to decreased membrane depolarizaiton
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What is the MOA of Buspirone?
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interacts with 5HT1A subclass of serotonin receptors as a partial agonist
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What are the pharmacological effects of barbs?
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depressant effects additive when mixed, particularly toxic w/alcohol.
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How is REM sleep affected w/barbs?
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usually decreased at high dose, on withdrawal rebound increase in REM may occur
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How are barbs used in anesthesia?
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depresses CNS to stage III - general anesthesia w/loss of consciousness- depending on lipidity solubility
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what are the 2 most lipid soluble barbs?
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thiopental and methohexital - penetrating brain tissue rapidly
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what are 2 benzos used w/other anesthetic agents?
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midzaolam and diazepam- diazepam cannot produce anesthesia by itself and can cause persistent post anesthetic depression
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What are 3 barbs/benzos used in Status Epilepticus
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Diazepam, Lorazepam, Phenobarbital
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Which benzo is used for cerebral palsy?
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diazepam
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high doses of benzos can cause?
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medullary depression - respiratory arrest, hypotension - causes of death in OD
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sedative hypnotics can cause
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respiratory depression in patients with OPD
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what is tolerance?
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decrease in responsiveness - occurs with continuous use, requires higher dose to get same response
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withdrawal signs are more common with?
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shorter acting drugs (barbs) b/c they disappear from your system faster
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physical dependence is unlikely to occur with?
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buspirone
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benzos are commonly used for?
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anxiety
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what drug is used for panic disorders and agoraphobia
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alprozolam
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define excess CNS depression
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decreased psychomotor functioning and unwanted daytime sedation
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symptoms of CNS depression
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drowsiness, dizziness, motor incoordination
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interaction with what? is the most common type of drug interaction involving sedative hypnotics?
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ethanol
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ethanol is less likely to cause additive CNS depression with what? than other sedative hypnotics
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Buspirone
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what may reverse CNS depressant effects of benzos?
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Flumazenil
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what has no specific antidote for its OD?
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barbs
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