Anxiolytics / Sedative-Hypnotics Flashcards
What kind of drugs are diazepam, lorazepam,and flurazepam? What 3 disorders are they all used to treat?
Benzodiazepines; all treat anxiety disorders, short-term depression and bipolar disorder
What kind of drugs are chlordiazepoxide, alprazolam, and triazolam? What 3 disorders are they all used to treat?
Benzodiazepines; all treat anxiety disorders, short-term depression and bipolar disorder
Besides treating depression and bipolar disorder, what is a therapeutic use of alprazolam?
Sedation
Which benzodiazepine is used only for its anesthesia (calming and anterograde amnesia) effects, not as a treatment for psychiatric disorders?
Midazolam
What receptors do all the benzodiazepines bind to, are they agonists or antagonists, and where on the receptor do they bind?
GABA-A receptor agonists, bind between the α1 and γ2 subunits
Which benzodiazepine is given as a muscle relaxant, anticonvulsant, and to prevent withdrawal symptoms in alcoholics?
Lorazepam
Which benzodiazepine is used in sleeping pills because it causes hypnosis?
Triazolam
Many benzodiazepines are transformed in the body into active metabolites with long half-lives. Which benzo is notably NOT transformed (displays 1-pass metabolism), making its concentration in the body easier to control?
Lorazepam
Name the 3 benzodiazepams that have active metabolites with half-lives of 100+ hours. Which of the pre-metabolite drugs has the longest half-life?
Diazepam, chlordiazepoxide, and flurazepam; flurazepam itself has the longest half life of 74 hours
Name the non-benzodiazepine, non-barbiturate GABA receptor agonist in the drug table. Which kind of GABA receptors does it selectively affect?
Zolpidem; agonist for BDZ-1 receptors only
What are the 2 therapeutic uses for zolpidem? What are 2 important side effects?
Sedation and hypnosis; can cause sleep-walking and next-day impairment
What kind of drugs are phenobarbital and thiopental? What receptors do they bind, where on the receptor, and are they agonists or antagonists?
Barbiturates; GABA-A receptor agonists, bind the α or β subunit
Comparing phenobarbital to thiopental: which one is more lipid soluble? Which displays more fast-on, fast-off activity?
Thiopental is more lipid soluble and therefore displays more fast-on, the fast-off activity (due to rapid tissue redistribution)
What are the main uses for phenobarbital and thiopental?
Phenobarbital is an anticonvulsant / anti-epileptic; thiopental is used to induce anesthesia
What synthetic drug can be used to treat benzodiazepine overdose, although it is not uniform in reversing respiratory depression?
Flumazenil
What receptors does flumazenil affect, is it an agonist or antagonist, and what are 2 possible side effects of its use?
GABA-A receptors (both BDZ-1 and BDZ-2) antagonist; may see life-threatening withdrawal or seizures
What drug is best used to relieve anxiety without sedation, such as for generalized anxiety disorder?
Buspirone
What receptor does buspirone affect, and is it an agonist or antagonist?
5HT-1a receptor partial agonist (note: only anxiolytic that doesn’t bind to GABA receptors)
Which of the benzodiazepines and barbiturates can cause effects of daytime sedation and drowsiness, anterograde amnesia, and physiologic dependence?
All of them (note that zolpidem does not cause these effects and isn’t a benzo or barb anyways)
Name 2 anxiolytics that are given as muscle relaxants and anticonvulsants, in addition to treatment for depression or bipolar.
Diazepam and lorazepam
