Anxiolytics and Hypnotics

Question 1

Benzodiazepine Sedative-Hypnotics (4)

Answer 1

Flurazepam
Tempazepam
Triazolam
Midazolam

Question 2

Benzodiazepine Anxiolytics (5)

Answer 2

Alprazolam
Clorazepate
Diazepam
Lorazepam
Oxazepam

Question 3

Benzodiazepine-like (Z drugs) (3)

Answer 3

Zolpidem
Zaleplon
Eszopiclone

Question 4

Serotonin Agonists (1)

Answer 4

Busprione

Question 5

Barbituates

Answer 5

Pentobarbital*
Phenobarbital*
Thiopental*

Question 6

Melatonin agonist

Answer 6

Ramelteon

Question 7

Antihistamines

Answer 7

Hydroxyzine

Diphenhydramine

Question 8

Alcohols

Answer 8

Ethanol

Chloral hydrate

Question 9

Type of drugs that progress on linear slope. High doses may lead to state of general anethesia

Answer 9

Barbituates

Alcohols

Question 10

Non-Linear Slope drugs that reach a plateau in CNS depression

Answer 10

Benzodiazepines and newer hypnotics

Question 11

Absorption of benzos

Best and poor routes

Answer 11

best absorption by oral route

Poor absorption and compatibility problems via parenteral route

Question 12

Metabolism of benzos:
Organ
Main enzyme
Primary biotransformation method

Answer 12

Liver
CYP3A4
Glucuronidation

Question 13

Influence of age on metabolism of benzos (3)

Answer 13

1. > 65 shows slowing of hepatic processing
2. Increased Vd due to decreased lean body mass
3. Decreased rate of elimination

Question 14

Primary MOA for benzos

Answer 14

Potentiate effects of GABA at the GABAa receptors which are chloride channels

Question 15

How do benzos work on GABAa receptors

Answer 15

Increase the frequency of opening and conductance of the chloride channels.
Increased chloride ion concentration within the cell causes a hyperpolarization and overal neuronal inhibition

Question 16

Which GABAa subunits cause sedation, anticonvulsant action, and anterograde amnesia?

Answer 16

GABAa1

Question 17

Which GABAa subunit causes anxiolysis?

Answer 17

GABAa2

Question 18

Which benzo is used at a date rape drug?

Answer 18

Flunitrazepam

Question 19

Additive CNS depression is caused by mixing benzos with which other drugs? (6)

Answer 19

Ethanol
Opiods
Anticonvulsants
Phenothiazide
Antihistamines
TCAs

Question 20

Purpose of flumazenil?

Answer 20

Benzo antagonist

Question 21

MOA of flumazenil?

Answer 21

Competitive inhibitor of BZ receptor.

Can reverse the effects of BZ

Question 22

Uses (2) for flumazenil

Answer 22

1. Terminate BZ-induces sedation

2. Diagnosis and treatment of BZ toxicity

Question 23

MOA of barbs

Answer 23

Increase the duration of the GABA-gated chloride channel opening

Question 24

Cellular effects of barbs (2)

Answer 24

1. Membrane hyperpolarization

2. Neuronal inhibition

Question 25

How does Buspirone work?

Answer 25

Non-sedating anxiolytic

Partial agonist at 5HT1a receptor

Question 26

Effects of 5HT1a receptor activation?

Answer 26

Reduces neuronal excitability, firing frequency, and 5-HT release