Sedatives and Hypnotics

Question 1

Define sedatives

Answer 1

reduce anxiety, exert calming effect with minimal effects on motor or cognitive functions

Question 2

Define hypnotics

Answer 2

produce drowsiness and promote the onset and maintenance of sleep

Question 3

GABA is the main ____ neurotransmitter of the CNS and GABA-A receptors work by opening ____ pores in the receptor itself allowing for _____

Answer 3

inhibitory
Chloride
hyperpolarization

Question 4

Describe the mechanism of action of benzodiazepines

Answer 4

Positive modulators at GABA-A receptors; increase the affinity of the GABAA receptor for GABA and increase the frequency of Cl- channel openings but do not directly activate the GABAA receptor

Question 5

Describe the mechanism of action of barbiturates

Answer 5

increase the duration of GABA-induced channel openings and at high concentrations, directly activate the GABAA receptor

Question 6

List some similarities and differences between barbiturates and benzodiazapines

Answer 6

Barbiturates cause surgical anesthesia and coma with increasing doses

BZDs do not produce anesthesia, depress respiration, or induce CYPs

Both act to increase Cl flux and cause neuronal hyperpolarization

Question 7

List some adverse reactions to benzodiazepines

Answer 7

CNS effects: drowsiness, ataxia, slurred speech
Should be used for short term and dosage should be tapered before DC
Highly teratogenic

Question 8

Compar and contrast diazepam and lorazepam

Answer 8

Diazepam has active metabolites (longer acting). It is used to treat alcohol withdrawal, seizure disorders, cerebral plasy, stroke, MS in addition to anxiety

Lorazepam has no active metabolites but persists in the CSF longer so is used for status epilepticus

Both increase affinity of GABA-A for GABA

Question 9

List the indications of flumazenil use

Answer 9

BZD antagonist used to treat BZD overdose or reverse BZD sedation during anesthesia (no effect on barbiturate activity)

Question 10

Explain why patients should be closely monitored after giving flumazenil to reverse BZD effects

Answer 10

Flumazenil has a shorter half life than all BZDs so re-sedation is possible and repeat flumazenil doses may be needed

Question 11

Desribe the mechanism of action of buspirone

Answer 11

Partial agonist at 5-HT IA receptors with moderate affinity and partial agonist effets at D2 receptors

Question 12

Describe the use of buspirone

Answer 12

Anxiolytic with no sedation, anticonvulsant effects, or psychomotor impairment

Question 13

_____ is a drug used to treat insomnia that works at the GABA-A receptor, is used in lower doses for women, and can cause somnambulism

Answer 13

Zolpidem

Question 14

List some adverse reactions and precautions for zolpidem

Answer 14

Can cause rebound insomnia, somnambulism
Avoid alcohol and abrupt DC
Elderly are more sensitive

Question 15

Describe the mechanism of action and clinical use of eszopiclon

Answer 15

Non-BZD drug used for insomnia, first drug approved for long term use.
Works at GABA-A receptor complex

Question 16

List some adverse reactions and precautions for eszopiclon

Answer 16

Rebound insomnia, anxiety, unpleasant taste in mouth
Avoid alcohol
Elderly are more sensitive

Question 17

List four other indications for sedatives and hypnotics

Answer 17

Adjucts to anesthesia
Treatment for seizure disorders
Muscle relaxation
Alcohol withdrawal