Anxiolytics / Sedative-Hypnotics

Question 1

What kind of drugs are diazepam, lorazepam,and flurazepam? What 3 disorders are they all used to treat?

Answer 1

Benzodiazepines; all treat anxiety disorders, short-term depression and bipolar disorder

Question 2

What kind of drugs are chlordiazepoxide, alprazolam, and triazolam? What 3 disorders are they all used to treat?

Answer 2

Benzodiazepines; all treat anxiety disorders, short-term depression and bipolar disorder

Question 3

Besides treating depression and bipolar disorder, what is a therapeutic use of alprazolam?

Answer 3

Sedation

Question 4

Which benzodiazepine is used only for its anesthesia (calming and anterograde amnesia) effects, not as a treatment for psychiatric disorders?

Answer 4

Midazolam

Question 5

What receptors do all the benzodiazepines bind to, are they agonists or antagonists, and where on the receptor do they bind?

Answer 5

GABA-A receptor agonists, bind between the α1 and γ2 subunits

Question 6

Which benzodiazepine is given as a muscle relaxant, anticonvulsant, and to prevent withdrawal symptoms in alcoholics?

Answer 6

Lorazepam

Question 7

Which benzodiazepine is used in sleeping pills because it causes hypnosis?

Answer 7

Triazolam

Question 8

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?

Answer 8

Lorazepam

Question 9

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?

Answer 9

Diazepam, chlordiazepoxide, and flurazepam; flurazepam itself has the longest half life of 74 hours

Question 10

Name the non-benzodiazepine, non-barbiturate GABA receptor agonist in the drug table. Which kind of GABA receptors does it selectively affect?

Answer 10

Zolpidem; agonist for BDZ-1 receptors only

Question 11

What are the 2 therapeutic uses for zolpidem? What are 2 important side effects?

Answer 11

Sedation and hypnosis; can cause sleep-walking and next-day impairment

Question 12

What kind of drugs are phenobarbital and thiopental? What receptors do they bind, where on the receptor, and are they agonists or antagonists?

Answer 12

Barbiturates; GABA-A receptor agonists, bind the α or β subunit

Question 13

Comparing phenobarbital to thiopental: which one is more lipid soluble? Which displays more fast-on, fast-off activity?

Answer 13

Thiopental is more lipid soluble and therefore displays more fast-on, the fast-off activity (due to rapid tissue redistribution)

Question 14

What are the main uses for phenobarbital and thiopental?

Answer 14

Phenobarbital is an anticonvulsant / anti-epileptic; thiopental is used to induce anesthesia

Question 15

What synthetic drug can be used to treat benzodiazepine overdose, although it is not uniform in reversing respiratory depression?

Answer 15

Flumazenil

Question 16

What receptors does flumazenil affect, is it an agonist or antagonist, and what are 2 possible side effects of its use?

Answer 16

GABA-A receptors (both BDZ-1 and BDZ-2) antagonist; may see life-threatening withdrawal or seizures

Question 17

What drug is best used to relieve anxiety without sedation, such as for generalized anxiety disorder?

Answer 17

Buspirone

Question 18

What receptor does buspirone affect, and is it an agonist or antagonist?

Answer 18

5HT-1a receptor partial agonist (note: only anxiolytic that doesn’t bind to GABA receptors)

Question 19

Which of the benzodiazepines and barbiturates can cause effects of daytime sedation and drowsiness, anterograde amnesia, and physiologic dependence?

Answer 19

All of them (note that zolpidem does not cause these effects and isn’t a benzo or barb anyways)

Question 20

Name 2 anxiolytics that are given as muscle relaxants and anticonvulsants, in addition to treatment for depression or bipolar.

Answer 20

Diazepam and lorazepam