Sedatives-Hypnotics
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A patient develops respiratory depression after sedative overdose. Which class has the highest safety margin?
Benzodiazepines
Which sedative-hypnotic class produces a linear dose-response leading to coma?
Barbiturates
Which receptor subunit is primarily targeted by Z-drugs?
Alpha1 subunit of GABA-A receptor
Why do benzodiazepines have a ceiling effect on CNS depression?
They require endogenous GABA to act
Which drug class can directly activate GABA receptors at high doses?
Barbiturates
Which receptor is inhibited by barbiturates contributing to CNS depression?
AMPA receptor
Which drug reverses benzodiazepine overdose?
Flumazenil
Why is flumazenil risky in chronic benzodiazepine users?
It can precipitate seizures
Which pharmacokinetic property explains rapid onset of triazolam?
High lipid solubility
Which benzodiazepines avoid Phase I metabolism?
Lorazepam, oxazepam
Which enzyme metabolizes most sedative-hypnotics?
CYP3A4
Which drug interaction increases zolpidem levels?
CYP3A4 inhibitors
Which sedative-hypnotic is metabolized by aldehyde oxidase?
Zaleplon
Which barbiturate has the longest half-life?
Phenobarbital
How does urine alkalinization affect phenobarbital?
Increases excretion
Which effect is caused by benzodiazepines on sleep?
Increase stage 2 NREM
Which sleep stage is reduced by sedative-hypnotics?
REM sleep
What is REM rebound?
Increased REM after withdrawal
Which drug is best for sleep-onset insomnia?
Zaleplon
Which drug is best for sleep maintenance?
Zolpidem extended-release
Which drug causes next-day sedation most commonly?
Suvorexant
Which receptor does ramelteon activate?
Melatonin receptors MT1 and MT2
Which neurotransmitter system is enhanced by benzodiazepines?
GABA
What channel is opened by GABA-A receptor activation?
Chloride channel
What is the effect of chloride influx in neurons?
Hyperpolarization
Which sedative causes anterograde amnesia?
Benzodiazepines
Which clinical use benefits from amnesia?
Procedural sedation
Which class is contraindicated in porphyria?
Barbiturates
Which condition increases sedative sensitivity?
Elderly age
What is the major cause of death in overdose?
Respiratory depression
Which factor increases overdose risk significantly?
Polypharmacy
Which drug combination is most dangerous?
Sedatives + alcohol
Which sedatives induce hepatic enzymes?
Barbiturates
What is cross-tolerance commonly seen with sedatives?
Ethanol
Which drugs cause minimal tolerance?
Z-drugs
What type of dependence develops with long-term use?
Physical dependence
Which withdrawal symptom is life-threatening?
Seizures
Which drugs treat sedative withdrawal?
Long-acting benzodiazepines
Which drug is first-line for acute anxiety?
Benzodiazepines
Which drugs are first-line for chronic anxiety?
SSRIs and SNRIs
Which sedative has slow onset and no sedation?
Buspirone
Which receptor does buspirone act on?
5-HT1A receptor
Which sedative-hypnotics cross placenta?
All
What neonatal effect can occur?
Respiratory depression
Which sedative causes paradoxical disinhibition?
Benzodiazepines
Which CNS effect impairs driving ability?
Psychomotor impairment
Which condition worsens with sedatives?
Sleep apnea
Which route avoids first-pass metabolism?
Intranasal or IV
Which drug is used preoperatively for sedation?
Midazolam
Which class is used as anticonvulsant?
Benzodiazepines
Which barbiturate treats seizures?
Phenobarbital
Which sedatives lack anticonvulsant activity?
Z-drugs
Which drug increases duration of Cl channel opening?
Barbiturates
Which drug increases frequency of Cl channel opening?
Benzodiazepines
Which antagonist does NOT reverse barbiturates?
Flumazenil
Which receptor subtype is NOT affected by benzodiazepines?
GABA-B
Which drug causes rebound insomnia?
Zolpidem
Which sedative has minimal effect on sleep architecture?
Zaleplon
Which effect occurs with high-dose sedatives?
Coma
Which drug causes hangover effect?
Long-acting benzodiazepines
Which sedative has biphasic release formulation?
Zolpidem
Which factor prolongs half-life of sedatives?
Hepatic impairment
Which sedative has active metabolites causing accumulation?
Diazepam
Which sedative is safest in liver disease?
Lorazepam
Which sedative is used for panic disorder?
Alprazolam
Which sedative causes minimal cardiovascular effects?
Benzodiazepines
Which sedative affects orexin system?
Suvorexant
What is orexin’s role?
Promotes wakefulness
Which sedative blocks wakefulness signaling?
Orexin antagonists
Which adverse effect occurs with orexin blockers?
Daytime somnolence
A patient develops respiratory depression after sedative overdose. Which class has the highest safety margin?
Benzodiazepines
Which sedative-hypnotic class produces a linear dose-response leading to coma?
Barbiturates
Which receptor subunit is primarily targeted by Z-drugs?
Alpha1 subunit of GABA-A receptor
Why do benzodiazepines have a ceiling effect on CNS depression?
They require endogenous GABA to act
Which drug class can directly activate GABA receptors at high doses?
Barbiturates
Which receptor is inhibited by barbiturates contributing to CNS depression?
AMPA receptor
Which drug reverses benzodiazepine overdose?
Flumazenil
Why is flumazenil risky in chronic benzodiazepine users?
It can precipitate seizures
Which pharmacokinetic property explains rapid onset of triazolam?
High lipid solubility
Which benzodiazepines avoid Phase I metabolism?
Lorazepam, oxazepam
Which enzyme metabolizes most sedative-hypnotics?
CYP3A4
Which drug interaction increases zolpidem levels?
CYP3A4 inhibitors
Which sedative-hypnotic is metabolized by aldehyde oxidase?
Zaleplon
Which barbiturate has the longest half-life?
Phenobarbital
How does urine alkalinization affect phenobarbital?
Increases excretion
Which effect is caused by benzodiazepines on sleep?
Increase stage 2 NREM
Which sleep stage is reduced by sedative-hypnotics?
REM sleep
What is REM rebound?
Increased REM after withdrawal
Which drug is best for sleep-onset insomnia?
Zaleplon
Which drug is best for sleep maintenance?
Zolpidem extended-release
Which drug causes next-day sedation most commonly?
Suvorexant
Which receptor does ramelteon activate?
Melatonin receptors MT1 and MT2
Which neurotransmitter system is enhanced by benzodiazepines?
GABA
What channel is opened by GABA-A receptor activation?
Chloride channel
What is the effect of chloride influx in neurons?
Hyperpolarization
Which sedative causes anterograde amnesia?
Benzodiazepines
Which clinical use benefits from amnesia?
Procedural sedation
Which class is contraindicated in porphyria?
Barbiturates
Which condition increases sedative sensitivity?
Elderly age
What is the major cause of death in overdose?
Respiratory depression