Sedative-Hypnotic Drugs

Question 1

GABA receptor effects

benzodiazepine vs. barbiturate

Answer 1

FREnzodiazepine - FREQuency

barbiDURATes - DURATion

Question 2

major inhibitory NT

Answer 2

GABA

Glycine

Question 3

major excitatory NT

Answer 3

glutamic acid

aspartic acid

Question 4

short-acting benzodiazepine
binds GABA-A receptor TO INCREASE FREQUENCY of Cl- channel opening –> membrane hyperpolarization
for ANESTHESIA INDUCTION, PRE-OPERATIVE SEDATION
SE: anterograde amnesia, unwanted daytime sedation, insomnia

Answer 4

midazolam
brotizolam, triazolam, oxazepam, etizolam

additive CNS depression with ethanol
half life dictated by metabolite

Question 5

intermediate-acting benzodiazepine
binds GABA-A receptor TO INCREASE FREQUENCY of Cl- channel opening –> membrane hyperpolarization
for SEIZURE DISORDER, TRANQUILIZER
SE: anterograde amnesia, unwanted daytime sedation

Answer 5

lorazepam
alprazolam, estazolam, clonazepam, lormetazepam, nitrazepam, temazepam

additive CNS depression with ethanol

Question 6

what abnormal sleep pattern results from benzodiazepine use?

Answer 6

decreased REM sleep

Question 7

long-acting benzodiazepine
binds GABA-A receptor TO INCREASE FREQUENCY of Cl- channel opening –> membrane hyperpolarization
for SEIZURE DISORDER, TRANQUILIZER, ALCOHOL WITHDRAWAL
SE: ANTEROGRADE AMNESIA, unwanted daytime sedation

Answer 7

diazepam

chlorazepate, chlordiazepoxide, flurazepam, quazepam, flunitrazepam

Question 8

date rape drugs

Answer 8

alcohol (most common)
Flunitrazepam (rohypnol)
gamma-hydroxybutyrate

Question 9

benzodiazepine with longest half life

Answer 9

chlordiazepoxide

half life of 36-200 hours

Question 10

antidote; benzodiazepine antagonist
for benzodiazepine overdose
precipitates benzodiazepine withdrawal syndrome
seizures and arrhythmias may occur when administered in patient who took both TCAs and benzodiazepines

Answer 10

flumazenil

via IV

Question 11

ultra-short acting barbiturate
bind to GABA-A receptor allosteric site –> increases DURATION of Cl- channel opening
for anesthesia induction, increased ICP
SE: dependence liability greater than benzodiazepines, acute intermittent porphyria
additive CNS depression with ethanol
POTENT INDUCER OF CYP450 ENZYMES

Answer 11

thiopental (shortest acting)

methohexital, thiamylal

Question 12

short- and intermediate-acting barbiturate
bind to GABA-A receptor allosteric site –> increases DURATION of Cl- channel opening
for insomnia, pre-operative sedation
SE: dependence liability greater than benzodiazepines, acute intermittent porphyria

Answer 12

pentobarbital

secobarbital, amobarbital, butalbital, butabarbital, talbutal, aprobarbital

Question 13

long-acting barbiturate
bind to GABA-A receptor allosteric site –> increases DURATION of Cl- channel opening
for seizure disorders, status epilepticus, Gilbert’s Syndrome (hyperbilirubinemias)
SE: dependence liability greater than benzodiazepines, acute intermittent porphyria
additive CNS depression with ethanol
POTENT INDUCER OF CYP450 ENZYMES

Answer 13

phenobarbital
mephobarbital, primidone

off label use against ketamines

Question 14

what enzyme is deficient in acute intermittent dysphoria?

Answer 14

HMB Synthase

Question 15

most catastrophic symptom of sedative-hypnotic withdrawal?

Answer 15

rebound suicide

Question 16

Newer hypnotic
imidazopyridine
for INSOMNIA ONLY (sleep initiation NOT maintenance)
SE: dependence liability less than benzodiazepines
effects REVERSED BY FLUMAZENIL
lacks anti-convulsant, anti-anxiety, and muscle relaxant effects

Answer 16

zolpidem

zaleplon, eszopiclone

Question 17

anxiolytic
partial agonist at 5-HT1A receptors and possibly D2 receptors
for acute GAD
NOT anti-convulsant, muscle relaxant
minimal CNS depressant effects
minimal abuse liability
minimal tolerance and withdrawal

Answer 17

buspirone