Flashcards in Sedatives & hypnotics Deck (49):
An effective sedative agent should reduce _____ & exert a _______
a calming effect
Hypnotic drugs should produce _______ & encourage the onset & maintenance of a ______
state of sleep
Describe the absorption & distribution of sedative-hypnotic drugs
Good distribution to the brain
Describe the metabolism & excretion of sedative-hypnotic drugs
Metabolized by hepatic enzymes
Active & inactive metabolites
What is the MOA of benzos?
Facilitates the inhibitory actions of GABA
Receptors for benzodiazepines are located in what 3 brain regions?
What are benzos used for?
Skeletal muscle relaxation
Toxicity of sedative-hypnotics (benzos, newer hypnotic drugs, barbiturates) can lead to what?
Extension of CNS depressant actions
Dependence (barbiturates > benzos)
What should you remember about diazepam?
Erratic bioavailability from IM injection
Which drug has active metabolites w/ long half-lives?
Which drugs have no active metabolites? (3)
High doses of benzos w/ long or intermediate half-lives have a greater potential to produce...
What are ADEs of benzos?
*Start at lowest effective dose to avoid these
The FDA requires labeling for benzos & barbiturates to include a caution regarding... (3)
complex sleep behaviors (sleep driving or eating, phone calls)
What is the MC type of drug interaction w/ sedative-hypnotics?
Additive CNS depression effects
What are examples of substances that interact w/ sedative-hypnotics?
Overdosage of sedative-hypnotics can result in...
respiratory & CV depression
What drug may reverse CNS depressant effects?
What is the MOA of flumazenil?
Antagonist at benzo sites on GABA receptor
Antagonist to benzos & the newer hyponotic drugs only
What are ADEs of flumazenil?
What are 3 newer hypnotic drugs (not among the benzo class)?
What is the MOA of the newer hypnotics?
Bind to GABA receptor sites
Facilitate Cl channel opening
What is the MOA of barbiturates ("tal") ?
Prolongs the inhibitory effects of GABA & glycine
What are barbiturates ("tal") used for?
insomnia & sedation
Which 2 drug classes induce liver enzymes?
What does this cause?
Barbiturates & carbamates
Which 2 antihistamines are more sedating than pyrilamine?
Diphenhydramine & doxylamine
Which antidepressant has FDA approval for the tx of sleep maintenance insomnia?
Which antidepressant may promote sleep?
Which antidepressant can be given at bedtime to improve sleep continuity?
What are ADEs of trazadone?
Alpha-adrenergic blockade - orthostasis
What are 2 ADEs of mirtazapine?
Which melatonin-receptor agonist is approved for the tx of sleep-onset insomnia?
Ramelteon forms active metabolite via...
What are the MC ADEs of ramelteon?
HA, dizziness, somnolence
Ramelton is helpful for sleep- onset difficulties in what 2 conditions?
COPD & sleep apnea
What is the main complaint regarding valerian (an herbal sleep remedy)?
Smells like old gym socks
What is the MOA of buspirone?
Partial agonist at 5-HT receptors & D2 receptors
Interacts w/ 5-HT1A subclass of serotonin receptors
What effects does buspirone express?
Minimal CNS depressant effects
Describe the onset of action of buspirone
Slow (> 1 week)
Does buspirone form active metabolite?
What does buspirone interact w/?
CYP3A4 inducers & inhibitors
What are the ADEs of buspirone?
GI distress, tachy
Tolerance is minimal w/ chronic use
Little rebound anxiety or withdrawal sx upon discontinuance
Is buspirone safe in pregnancy?
yes appears to be
Which classes of drugs are used for tx of panic d/o?
Which SSRI can cause QT prolongation?
What classes of drugs are used for tx of social anxiety d/o?
What are examples of stimulus control procedures used for sleep hygiene?
Avoid blue spectrum light from TV, phones, tablets
Schedule worry time during the day; do not take troubles to bed
What is another sleep hygiene recommendation?
Avoid illuminated clocks the bedroom
What are some of the clinical uses of sedative-hypnotics?
Relief of anxiety
Control of withdrawal states