sedative and hypnotics

Question 0

Goal of Hypnotics

Answer 0

produce drowsiness, encourage onset and maintenance of sleep

Question 1

Goal of sedative

Answer 1

reduce anxiety & provide calming effect

Question 2

types of sedative-hypnotics

Answer 2

1. Benzodiazepines
2. Barbiturates
3. Newer hypnotics
4. other classes that have sedative effects: alcohol, antipsychotics, antidepressants, antihistamines

Question 3

Barbiturates
uses?
mechanism?
problems?

Answer 3

uses: promote sleep, more often used as general anesthetics
mechanism: increases duration of GABAa receptor Cl- channel opening and affects glutamate receptor (AMPA)

Problems: low therapeutic index, dependence, fatal overdose

Question 4

Benzodiazepines
uses?
mechanism?
benefits?
problems?

Answer 4

uses: promote sleep, especially acute situations
mechanism: increases frequency of GABAa receptor Cl- channel opening
benefits: less chance of lethal overdose than barbiturates
problems: residual effects, dependence

Question 5

Where in CNS does Benzodiazepines promote GABA inhibition?

Answer 5

spinal cord, hypothalamus, hippocampus, substantia nigra, cerebellar cortex, cerebral cortex

Question 6

Newer hypnotics
example?
use?
mechanism?
benefits?

Answer 6

example: Zolpidem (ambien)

Use: promote sleep

Mechanism: specific for alpha subunit for sedation effects

benefits: as effective as benzodiazepines with fewer side effects and less risk of dependence

Question 7

Active metabolite of Benzodiazepine?

Answer 7

Desmethyldiazepam

Question 8

organ level effects of sedative-hypnotics

Answer 8

sedation
hypnosis
anesthesia
antiseizure

Depress respiratory drive and cardiac muscle

Question 9

Pharmacokinetics of sedative hypnotics

Answer 9

Oral absorption varies
Rates at which drug enters CNS depends on its lipid solubility
Metabolism varies by chemical structure
Excretion primarily via kidney
All cross placental barrier and in breast milk

Question 10

Other uses of sedative hypnotics

Answer 10

Antiseizure
Anesthesia
Ethanol or other withdrawal management
Psychiatric uses
Skeletal muscle relaxation