Sedatives & Hypnotics Flashcards
NE levels in anxiety and depression
Increased in anxiety
Decreased in depression
Dopamine levels in schizophrenia, Parkinson’s and depression
Increased in schizophrenia
Decreased in Parkinson’s
Decreased in depression
Serotonin levels in anxiety and depression
Decreased in anxiety
Decreased in depression
Classic triad of serotonin syndrome with examples
Mental status changes
Autonomic hyperactivity
Neuromuscular abnormalities
Treatment of serotonin syndrome
Cyproheptadine (serotonin antagonist)
ACh level in REM sleep, Alzheimers and Huntington’s disease
Increased in REM sleep
Decreased in Alzheimers
Decreased in Huntington’s disease
Major excitatory neurotransmitter
Glutamate
Receptor for glutamate
NMDA receptor
Phenycyclidine
Antagonist to NMDA receptor
Causes stimulatory side effects
What is a sedative?
AKA anxiolytics
Reduces anxiety and exerts a calming effect
What is a hypnotic?
Produces drowsiness
Encourage onset and maintenance of a state of sleep
Simpler examples in the sedative-hypnotic class?
Ethanol
Chloral hydrate
Something that differentiates benzodiazepines from barbiturates and alcohol?
Benzodiazepines will not progress past CNS depression into coma
Drugs that are GABAa agonists
Benzodiazepines
Barbiturates
Zolpidem, zaleplon, eszopiclon
Action of buspiron?
Serotonin receptor agonist
Action of Ramelteon
Melatonin agonist
Action of Suvorexant
Orexin antagonist that improves sleep duration
What is unique about buspirone’s anxiolytic effect?
It has a pure anxiolytic affect with no other effects
Clinical use of Buspirone
GAD
Begins to take effect after 1-2 weeks
GABA levels in anxiety and Huntington’s disease
Decreased in anxiety
Decreased in Huntington’s disease
GABA receptor anaesthetics
Etomidate
Propofol
Difference between mechanism of benzodiazepines and mechanism of barbiturates?
Benzodiazepines potentiate GABA thereby increasing the frequency of Cl- channels opening
Barbiturates prolong GABA activity and thereby prolong the duration of Cl- channels opening
What receptors do benzodiazepines and Barbiturates act on and where are they?
Benzodiazepines bind to specific benzodiazepine binding sites that are part of the GABAa complex
Barbiturates bind to other binding sites on the GABAa complex
How do the drugs with ‘z’ selectively cause sedation?
They agonise Benzodiazepine-1 receptors but select against binding to benzodiazepine-2 receptors
How does buspirone eeduce anxiety without sedation?
Does not affect GABA
Partial agonist at serotonin receptors
What is the antidote for sedative-hypnotic drugs?
Flumezanil
Which sedative-hypnotics can flumezanil not antagonise?
Barbiturates and alcohol as they bind to sites other than benzodiazepine receptors
Effects of sedation?
Decreases psychomotor and cognitive functions
Disinhibition
Anterograde amnesia
How does hypnosis affect sleep?
Sleep latency decreased
Duration of stage 2 NREM sleep is increased (deep sleep)
Duration of REM sleep is Decreased
Duration of stage 3 NREM slow wave sleep is decreased
Barbiturates used for anaesthesia?
Thiopental
Methohexital
Management of generalised convulsive status epilepticus?
IV lorazepam, diazepam or midazolam
Drug used in sedative-hypnotic withdrawal states
Diazepam
Even in bezodiaepine withdrawal
What does orexin do and therefore what does suvorexant do?
Orexin causes wakefulness and therefore suvorexant enables sleep but antagonising orexin
Earliest features of alcohol withdrawal within hours to a day?
Mainly tremor
When do seizures, occur in alcohol withdrawal?
6 to 48 hours
When do hallucinations occur in alcohol withdrawal?
12 to 48 hours
When does delirium tremendous occur in alcohol withdrawal?
72 to 96 hours
What is delirium tremens?
Markedly altered mental status
Autonomic hyperactivity
FDA approved drugs for alcoholism therapy?
Disulfiram
Naltrexone
Acamprosate
Why does naltrexone help alcoholics?
Endogenous opioids reinforce alcohol effects
When given there is no buzz
How does acamprosate work for alcoholics?
Modulates NMDA receptors
What is Wernicke-Korsakoff syndrome?
Wernicke: acute encephalopathy
Korsakoff: permanent neurological condition usually due to Wernicke
Causes of Wernicke-Korsakoff syndrome?
Thiamine (B1) deficiency
Alcoholism
Brain finding in Wernicke-Korsakoff syndrome?
Atrophy of mammilary bodies
Features of Korsakoff syndrome?
Confabulation - can’t remember so make things up
Apathy
Personality changes
Amnesia, more likely anterograde
Features of foetal alcohol syndrome?
Growth restriction
Midfacial hypoplasia
Microcephaly
Marked CNS dysfunction
Diagnosis of recurrent episodes of chest pain, tachycardia, SOB, sweating and tremulousness in a young, otherwise healthy patient?
Panic disorder
Best hypnotics for elderly patients?
Melatonin agonists like ramelteon
How are benzodiazepines administered in status epilepticus?
IV
What drugs should benzodiazepines not be used with?
Any drug that causes sedation
How do GABA agonists help in cerebral palsy?
Improve the spasticity that results from a decrease in descending inhibitory control
