SEDATIVE

- HYPNOTIC DRUGS LM

BENZODIAZEPINES BARBITURATES
[Binds GABA-A receptor subunits to increase FREQUENCY of Cl‫ ﹶ‬ OTHERS
[Binds GABA-A receptor sites; increases DURATION of Cl‫ ﹶ‬channel opening;
channel opening; membrane hyperpolarizaDon] blocks glutamic acid neurotransmission; at high doses blocks Na channels]

SHORT ACTING INTERMEDIATE ACTING LONG ACTING ULTRA SHORT SHORT-INTERMEDIATE LONG ACTING MELATONIN RECEPTOR
IMIDAZOPYRINE AGONIST ANXIOLYTIC
[T½: 1.5 - 2.5h ] [T½: 12h ] [T½: 100h ] [T½: 4-9m ] [T½: 15 - 50h ] [T½: 118h ]

MIDAZOLAM (Bro%zolam, THIOPENTAL PENTOBARBITAL (Secobarbital, PHENOBARBITAL ZOLPIDEM
Triazolam, Oxazepam, E%zolam) LORAZEPAM (Alprazolam, DIAZEPAM ( Chlorazepate, Amobarbital, Butalbital, RAMELTEON BUSPIRONE
Estazolam, Clonazepam, Chlordiazepoxide, Flurazepam, (Methohexital, Thiamylal) (Mephobarbital, Primidone) (Zaleplon, Eszopiclone)
Butabarbital, Talbutal,
Lormetazepam, Nitrazepam, Quazepam, Flunitrazepam)
Aprobarbital)
Uses: Anesthesia inducDon Temazepam) MOA: AcDvates Melatonin receptors MOA: ParDal agonist at 5HT1A
Uses: Anesthesia inducDon Uses: Status epilepDcus MOA: Binds selecDvely to a subroup
and possibly D2 receptors
Preop sedaDon Uses: Status EpilepDcus (MT1 and MT2) in the suprachiasma-
Increased ICP Uses: Insomnia Seizure d/o of GABA-A receptors to enhance
Acute Anxiety Uses: Status epilepDcus Dc nuclei thus decreasing latency of
Skeletal muscle relaxant Insomnia membrane hyperpolarizaDon
Preop sedaDon Uses: Generalized anxiety d/o
Panic aOacks Skeletal muscle relaxant Anesthesia sleep onset
SE: Acute intermiOent Hyperbilirubinemia
Insomnia [Triazolam] Tranquilizers
Anxiety/Seizure d/o porphyria; Extension of CNS (Gilbert Syndrome) Uses: Insomnia
SE: Acute intermiOent SE: Non-specific chast pain
Seizure d/o [Clonazepam] Alcohol withdrawal Uses: Insomnia
depressant acDons; dependence porphyria; Extension of CNS Delayed sleep onset
SE: Anterograde amnesia Bipolar d/o [Clonazepam] Tachycardia/palpitaDons
Insomnia [Flurazepam] liability greater than Benzos SE: Severe Cardio/respi
depressant acDons; dependence Dizziness/nervousness
Rebound insomnia/anxiety Anxiety d/o [Clonazepam] SE: Dizziness
liability greater than Benzos depression; Extension of CNS SE: Few amnesDc effects
Dec. psychomotor skills Panic d/o [Clonazepam] FaDgue Tinnitus/GI distress
SE: Anterograde amnesia Notes: AddiDve CNS depression depressant acDons; dependence Dependence liability (less)
Paresthesia
Dependence liability Insomnia [Estazolam] Dec. psychomotor skills Decreased testosterone
if taken with ethanol; CYP450 Notes: AddiDve CNS depression liability greater than Benzos
Unwanted dayDme Increased prolacDn Pupillary constricDon
Dependence liability inducer Notes: Lack anD-convulsant, anD-
if taken with ethanol; CYP450
sedaDon SE: Anterograde amnesia Respiratory depression anxiety and muscle relaxant
inducer Notes: May be excreted
Dec. psychomotor skills Notes: Minimal rebound insomnia Notes: No anDconvulsant effect
Unwanted dayDme unchanged effects; very rapid onset of acDon;
Notes: Decreased REM sleep Dependence liability Minimal abuse liability No muscle relaxant effect
sedaDon in the urine; AddiDve CNS effects reversed by FLUMAZENIL
Avoid during 1st trimester Respiratory depression Minimal withdrawal s/sx Minimal CNS depression
depression if taken with ethanol;
Floppy infant syndrome Unwanted dayDme
Notes: Flunitrazepam (Rohypnol) CYP450 inducer
Inceased oral cleX risk sedaDon used as a Date-rape drug (odorless
colorless, tasteless, anterograde
Notes: Lorazepam preferred over amnesia effect)
Diazepam in Status epilepDcus
due to its long distribuDon T½

FLUMAZENIL [T½: 30m] MNEMONICS:

BENZodiazepines = Mercedes Benz (Fast Frequency)
MOA: Antidote; antagonist at benzodiazepine sites on GABA-A receptor BARBiturates = Barbed wire (Duration)
Uses: Benzodiazepine overdose TAYOpental = TAYO agad (shortest acting)
SE: Agitation, Confusion, Precipitates benzodiazepine withdrawal syndrome
for those with benzodiazepine dependence
Chlordiazepoxide = longest spelling (longest T½: 36-200h)
Notes: Seizure and arrhythmias may occur for those who took TCAs and
benzodiazepines Most catastrophic symptom of sedative-hypnotic withdrawal?
- REBOUND SUICIDE