Sedative Hypnotic Drugs Flashcards
What is a sedative?
Reduces anxiety
Calming effect
Minimum CNS depression consistent with its therapeutic efficacy
What is a hypnotic?
Drowsiness
Onset and maintenance of sleep
More pronounced CNS depression
What are the GABA receptor effects of Benzodiazepines and Barbiturates?
Benzodiazepine: Frequence
Barbiturates: Duration
Major inhibitory and excitatory NT?
Inbihitory: GABA(in), GLYC(in)E
Excitatory: ex-GLUTAMIC ACID, ex-ASPARTIC ACID (ACIDex)
What are the available short-acting benzodiazepines?
MOB-ET Midazolam Oxazepam Brotizolam Etizolam Triazolam
What is the MOA of benzodiazepines?
it binds to GABA-A receptor subunits to increase frequency of chloride channel opening -> membrane hyperpolarization
What are the common SE of short-term BZD?
Rebound insomnia/anxiety
What are the available intermediate-acting BZD?
CALL-NET Clonazepam Alprazolam Lorazepam Lormetazepam Nitrazepam Estazolam Temazepam
Which drugs suppress seizures with no associated marked sedation?
Clonazepam
Phenobarbital
What is the preferred drug for status epilepticus?
Lorazepam, long distribution halflife
What abnormal sleep pattern results from the use of benzodiazepines?
Decreased REM sleep
Which BZD are used for status epilepticus?
Lora-Diaz
Lorazepam
Diazepam
Which BZD is used for anesthetic induction?
Mida-Diaz
Midazolam
Diazepam
Which BZD has the longest half-life?
Chlorodiazepoxide (36-200 hours)
What are the date-rape drugs?
FAG
Flunitrazepam
Alcohol
Gamma-hydroxybutyrate
What is the toxic does of BZD?
Treatment?
1000x the therapeutic dose
Antidote: flumazenil (receptor antagonist)
What is the MOA of barbiturates?
Bind to GABA-A receptors -> inc duration of Cl channel opening -> block glutamic acid NT
What are the available ultra-short acting barbiturates?
Thiopental
Methohexital
Thiamylal
Which drug has the highest lipid solubility, entering the CNS in less than 1 minute?
Thiopental
What are the available long-acting barbiturates?
Primidone
Phenobarbital
Mephobarbital
What is the enzyme deficient in acute intermittent porphyria?
HMB synthase
What is the most catastrophic symptom of sedative-hypnotic withdrawal?
Rebound suicide
What are the drugs belonging to Imidazopyridine class?
Zolpidem
Zaleplon
Eszopiclone
What is the MOA of Buspirone?
Partial agonist at 5HT1A and D2 receptors
