Anxiolytics, Sedatives, and Hypnotics

Question 1

Dose Dependent GABA receptor agonist

Answer 1

Barbituates (phenobarbitol)

Question 2

Benzodiazepines drug list

Answer 2

Diazapam
Triazapam
Alprazolam
Clonazapam
Midazolam

Question 3

Benzodiazepines Receptor Agonists

Answer 3

“Z drugs”

Zolpidem (Ambien)
Eszopiclone

Question 4

Benzodiazapene Receptor Antagonists

Answer 4

Flumazenil

Question 5

Melatonin Congener

Answer 5

Ramelteon

Question 6

5-HT receptor agonist (non-sedative anxiolytic)

Answer 6

Buspirone

Question 7

Sedative vs Hypnotic

Answer 7

Sedative - calming

Hypnotic - Sleep inducing.

Question 8

Graded Dose-Response - Pentobarbitol vs Benzodiazepines

Answer 8

Pentobarbitol has a linear relationship - keeps on going from sedation to hypnosis to anesthesia to coma. Benzos have a proportionately higher dose required to cause coma, making them safer.

Question 9

Non-antidepressant medication for Panic disorders, Agoraphobia

Answer 9

Alprazolam - can cause dependence and rebound anxiety when discontinued.

Question 10

Non-antidepressant treatment for Social Phobia

Answer 10

Clonazapam

Question 11

Medications for Generalized Anxiety Disorder

Answer 11

Benzodiazepines , Buspirone

Question 12

Phenobarbitol mechanism

Answer 12

Direct, dose-dependent inhibition of neurons via binding to GABA receptors. Neurons become hyperpolarized due to chlorine influx and stop firing.

CYP Enzyme inducer - significant DDI’s.

Question 13

Benzodiazapenes mechanism

Answer 13

GABA-dependent GABA receptor binding (no direct effect without GABA), increases chloride influx and membrane polarization.

Question 14

Benzodiazepine receptor sensitivity

Answer 14

BZ binding sites are found on different subunits of GABA receptors.

alpha1 - sedation, amnesia, ataxia
alpha2,3 anxiolysis, muscle relaxation
alpha5 - cognitive impairment

Question 15

Full agonist Benzodiazepines

Answer 15

Diazapam
Alprazolam
Zolpidem (hypnotic)

Question 16

What is flumezenil used for? Why?

Answer 16

Benzodiazapene overdose - it binds competitively to the GABA receptor without altering its function.

Question 17

Adverse effects of Benzodiazepines

Answer 17

Dependence, tolerance.

Respiratory depression (usually in children, pulmonary disease, or with other CNS depressants -Etoh)

CI in sleep apnea
Decreases BP, increases HR

Question 18

Benzodiazepines for generalized anxiety disorder

Answer 18

alprazolam, diazapam

Question 19

Benzodiazepines for epilepsy and muscle relaxation

Answer 19

clonazapam, diazapam.

Question 20

Benzodiazepine that is best for anethesia - and why

Answer 20

midazolam - lipophilic, crosses BBB easily.

Also alprazolam, diazapam

Question 21

Benzodiazepines ADME

Answer 21

PO (Diazapam - also IV, IM, rectal), variable duration - active metabolites produced by CYP3A4. Must be converted to glucoronides for excretion.

Question 22

Does flumazenil help with etoh or barbituate overdose?

Answer 22

No - only Benzodiazepines

Question 23

Buspirone - what makes it different from other anxiolytics?

Answer 23

No sedative, hypnotic, euphoric, or muscle relaxant effects. No issues with tolerance, dependence, or abuse.

Question 24

Disadvantages of buspirone

Answer 24

Slow-acting, unpredictable response. CI with MAOI’s. Also causes chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, GI upset.

Question 25

Melatonin receptor agent - name and use.

Answer 25

Ramelteon - long term insomnia only.

Question 26

Benzodiazapine Receptor Agonists - usefulness

Answer 26

"Z drugs" - sedation only - no anxiolytic, anticonvulsant, or muscle relaxation.

Question 27

Benzodiazapine Receptor Agonists - advantages over Benzos for treating insomnia

Answer 27

Rapid acting, short duration, Less REM suppression, less tolerance,

Question 28

Benzodiazapine Receptor Agonists - disadvantages

Answer 28

Reduced clearance in the elderly. Respiratory depression at high dose, or w/other depression. Hepatic dysfunction with cimetidine.