Anxiolytics Flashcards
Name three benzodiazepines with active metabolites up to 100 hours after dosing.
Diazepam, Chlordiazepoxide, Flurazepam
What is Midazolam (Versed) used for?
Anesthesia
What is it about Benzos vs. Barbs that causes significant reduction in overdose deaths?
Benzos have a ceiling effect. They do not directly open Cl- channels like Barbs due at high doses. Benzos can only augment binding of GABA to GABA receptors.
Name 6 benzodiazepines used as a short term depression, maintenance bipolar, and severe bipolar treatments
Diazepam, Lorazepam, Chlordiazepoxide, Flurazepam, Alprazolam, and Triazolam
Name two of the benzodiazepines used to cause sedation?
Lorazepam (Ativan) and Alprazolam (Xanax)
In addition to the treatment of bipolar and depression, what can Diazepam by used as?
Anticonvulsant and muscle relaxant
Which sedative-hypnotics can be used to induce sleep?
Triazolam and zolpidem
Lorazepam can limit withdrawal from what?
Alcohol
MOA of benzos?
GABAa agonist, bind between alpha 1 and gamma 2 subunits
SE of benzos and barbs?
Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS w/ other drugs, pyschologic and physiologic dependence.
What is the difference between a sedative and hypnotic?
sedative= calming Hypnotic= induce sleep, more pronounced CNS depression than sedation
Name the six overall uses of sedative-hypnotics.
Anxiety disorder, induce sleep, anesthesia, anticonvulsants, muscle relaxation, recreation
What GABAa receptor subtypes do benzos bind to?
BOTH BDZ1 (omega1) and BDZ2 (omega 2)
What are BDZ1 selective agonists?
sleeping pills
Name a BDZ-1 selective agonist.
Zolpidem
SE of Zolpidem?
sleeping walking; next morning impairment
From low dose to high dose what effects do benzos have?
Sedation, hypnosis, muscle relaxation, anticonvulsant activity
What can be used to treat benzo overdose?
Flumazenil
MOA of flumazenil?
competitive non-selective antagonist
SE of flumazenil?
withdrawal (potentially life threatening)
Seizures in mixed overdoses
MOA of thiopental?
GABAa agonist (binds a or B subunit) highly lipid soluble, fast on, fast off
Thiopental use?
Induce anesthesia
Phenobarbitol use?
anti-epileptic, anti-convulsant
What class of drugs do Phenobarbitol and thiopental belong to?
Barbiturates
MOA of phenobarbital?
GABAa agonist (binds a or b subunit)
What is the risk of stopping barbiturates/ alcohol immediately?
abrupt withdrawal is life threatening
What is buspirone used as?
anxiolytic w/o sedation
MOA of buspirone?
No GABAa interaction, may be 5HT1A agonist
What sedative hypnotics are used for anesthesia?
Thiopental- induction
Midazolam- calming and produce anterograde amnesia
Name three sedative hypnotics used as anticonvulsants?
lorazepam, diazepam, phenobarbital
