Sedative-Hypnotic Drugs Flashcards
Identify drug class:
Pampatulog
Hypnotics
Identify drug class:
Pampakalma
Sedatives
Better safety profile:
Barbiturates or Benzodiazepines?
Benzodiazepines
MOA of Benzodiazepines
Increased FREQUENCY of Cl channel opening
FREnzodiazepine
MOA of Barbiturates
Increased DURATION of Cl channel opening
BarbiDURATes
CNS inhibitory NT
GABA
PNS inhibitory NT
Glycine
Excitatory NT
Glutamate (CNS)
Aspartate
Increases frequency of chloride channel opening
Intermediate-acting drug for seizure disorders, tranquilizer
SE: anterograde amnesia, unwanted daytime sedation
Additive CNS depression with alcohol
Drug?
Lorazepam
(Alprazolam, Clonazepam)
LAHAT NG -ZEPAM
Increases frequency of chloride channel opening
Short-acting drug for acute anxiety, anesthesia induction, preop sedation
SE: anterograde amnesia, unwanted daytime sedation, rebound insomnia/anxiety
Additive CNS depression with alcohol
Drug?
Midazolam
LAHAT NG -ZOLAM
How can benzodiazepine use affect sleep?
Decreases REM sleep
Increases frequency of chloride channel opening
Long-acting drug for seizure disorders, tranquilizer, alcohol withdrawal
SE: anterograde amnesia, unwanted daytime sedation
Additive CNS depression with alcohol
Drug?
Diazepam
Flunitrazepam
This long acting benzodiazepine is used as a date-rape drug
Flunitrazepam (Roofies/Rohypnol)
Other date rape drugs: alcohol, gamma-hydroxybutyrate
Benzodiazepine with the longest half life
Dhlordiazepoxide
36-200h
The toxic dose of benzodiazepines is how many times more than its therapeutic dose?
1000x
Antidote for Benzodiazepine Toxicity
SE: dizziness, nausea, withdrawal in those with dependence
Seizure and arrhythmia can occur when taken with TCAs
Drug, Class
Flumenazil, Benzodiazepine receptor antagonist
Role of activated charcoal im benzodiazepine toxicity
NONE. It’s useless
Increases duration of chloride channel opening
Short and intermediate acting drug for insomnia, preop sedation
SE: higher likelihood of dependence than benzodiazepines, acute intermittent porphyria
Additive CNS depression with alcohol
Potent inducer of CYP450
Drug, Class
Pentobarbital, Barbiturate
LAHAT NG -BARBITAL
Ultrashort acting
Increases duration of Chloride channel opening
Drug for anesthesia induction, increased ICP
SE: higher likelihood of dependence than benzodiazepines
Contraindicated in Acute Intermittent Porphyria
Additive CNS effects with ethanol
Potent indicer of CYP450
Drug, Class
Thiopental, Barbiturate
TAYO agad THIOpental
Increases duration of chloride channel opening
Long acting drug for seizure disorders, status epilepticus, hyperbilirubinemias (Gilbert’s Syndrome)
SE: higher likelihood of dependence than benzodiazepines, acute intermittent porphyria
Additive CNS depression with alcohol
Potent inducer of CYP450
Safe for pregnant*
Phenobarbital*, barbiturate
Mephobarbital, Primidone*
Enzyme deficient in Porphyria
HMB Synthase
Selectively binds to GABA-A
Drug for insomnia
SE: less likelihood of dependence than benzodiazepines
Effects reversed with Flumezanil
No anti-convulsant, anti-anxiety, and muscle relaxant effects
Zolpidem, Newer hypnotic
(Zaleplon, Ezopiclone)
Zolpidem, Zaleplon for Zleeeep
Partial agonist at 5HT1A and possibly D2 receptors Drug for Generalized Anxiety Disorder Good safety profile Minimal CNS depressant effects Minimal abuse liability Minimal tolerance and withdrawal
Buspirone
BUSpirone for BUSy people (anxious)
Barbiturates
Thiopental
Pentobarbital
Phenobarbital
Benzodiazepines
Midazolam
Lorazepam
Clonazepam