E1- Sedative-Hypnotics and Anxiolytics

Question 1

What is the major inhibitory neurotransmitter in the brain?

Answer 1

GABA

Question 2

What is the general MOA of sedative-hypnotics/anxiolytics?

Answer 2

Bind to GABA, to either intensify or prolong the actions of GABA

Question 3

What is an antihistamine used as an anti-anxiety medication that causes sedation that is a good option for recovering addicts and the elderly?

Answer 3

Hydroxyzine

Question 4

What is the MOA of barbiturates?

Answer 4

Bind to GABA receptor to stimulate Cl- influx and produce inhibition independent of GABA (prolongs channel opening time)

Question 5

What makes barbiturates a drug of abuse?

Answer 5

Causes euphorai

Question 6

What long-acting barbiturate is used as an anticonvulsant?

Answer 6

Phenobarbital

Question 7

Do barbiturates cross the BBB?

Answer 7

Yes, CNS depressant

Question 8

How are barbiturates metabolized?

Answer 8

By the liver

Induce CYP450s

Question 9

What are SE of barbiturates?

Answer 9

CNS depression
Paradoxical excitement
Severe physiological and psychological dependence

Question 10

What are contraindications of barbiturates?

Answer 10

Porphyria
Pulmonary insufficiency
Combination with alcohol (supra-additive effects)

Question 11

What is the safety margin of barbiturates?

Answer 11

Low margin of safety, no “ceiling effect”

Question 12

How is barbiturate OD treated?

What should not be given?

Answer 12

Diuresis and alkalization of the urine

Stimulants increase mortality rate

Question 13

What patient population should typically not be given benzodiazepines?

Answer 13

Elderly (do not metabolize BZs as quickly)

Question 14

What benzodiazepines have a long duration of action?

Answer 14

Diazepam

Flurazepam

Question 15

What benzodiazepines have an intermediate duration of action?

Answer 15

Alprazolam
Lorazepam
Oxazepam

Question 16

What benzodiazepine has a short duration of action?

Answer 16

Midazolam

Question 17

What is the MOA of benzodiazepines?

Answer 17

Bind to GABA receptor to increase the affinity of the receptor to GABA, prolonging its action; dependent on GABA

Question 18

What is the safety margin of benzodiazepines?

Answer 18

High margin of safety, “ceiling effect”

Question 19

What are the general uses of benzodiazepines?

Answer 19

Anxiety
Insomnia
Status epilepticus
Sedation, amnesia, anesthesia
Muscle relaxation

Question 20

In what anxiety disorders are benzodiazepines not used?

Answer 20

Panic disorder, phobias, obsessive compulsive

PTSD, anxiety in children and adolescents

Question 21

What benzodiazepines are used for insomnia?

Answer 21

Flurazepam

Temazepam

Question 22

What benzodiazepines are used for Status Epilepticus?

Answer 22

Diazepam

Lorazepam

Question 23

What benzodiazepines is used in preparation for anesthesia for short surgical procedures?
What is a SE?

Answer 23

Midazolam (IV)

Anterograde amnesia

Question 24

What benzodiazepines are used for muscle relaxation?

Answer 24

Diazepam

Question 25

What are SE of benzodiazepines?

Answer 25

CNS depression Paradoxical excitement Supra-additive with alcohol Sleep related behaviors Physical dependence may occur (high abuse potential)

Question 26

What are contraindications of benzodiazepines?

Answer 26

Pregnancy Sleep apnea Elderly

Question 27

Regarding BZs, what can cause rebound increases in insomnia and anxiety? How can this be avoided?

Answer 27

Abrupt discontinuation | Taper slowly

Question 28

What is the MOA of Fluemazenil?

Answer 28

Benzodiazepine antagonist; competes with BZs for GABA receptor

Question 29

What is the use of Fluemazenil? (2)

Answer 29

Hypoersomnia | Reverse the effects of BZs (Ex: Midazolam, which can sometimes cause respiratory depression)

Question 30

What are SE of Fluemazenil?

Answer 30

Triggers withdrawal and seizures in pts who are physically dependent upon BZs

Question 31

What is a contraindication of Fluemazenil?

Answer 31

Pts with hx of seizures

Question 32

What the the "z-drugs?"

Answer 32

Zolpidem, Zaleplon, Eszopiclone

Question 33

What is the MOA of the "z-drugs?"

Answer 33

Bind to the BZ1 subtype of the GABA receptor to increase GABA mediated inhibition

Question 34

What class of sedative-hypnotics have no anxiolytic, anticonvulsant, or muscle relaxant properties?

Answer 34

The "z-drugs?"

Question 35

What is the use of the "z-drugs?"

Answer 35

Insomnia

Question 36

Do most "z-drugs" have a short or long duration of action?

Answer 36

Short duration of action (morning drowsiness is unlikely )

Question 37

Which "z-drug" has a long half-life and can be used for long-term tx of insomnia?

Answer 37

Eszopiclone

Question 38

What is the margin of safety for the "z-drugs?"

Answer 38

High margin of safety

Question 39

What are SE of the "z-drugs?"

Answer 39

GI (diarrhea, nausea) Drowsiness Sleep related behaviors Confusion, memory loss, and psychosis in elderly

Question 40

Regarding the "z-drugs," what can use rebound insomnia?

Answer 40

Rapid discontinuation

Question 41

Abrupt cessation after long-term use of Eszopiclone can cause what?

Answer 41

Withdrawal sxs (CNS stimulation, anxiety, seizures)

Question 42

What is the MOA of Suvorexant?

Answer 42

Orexin receptor antagonist

Question 43

What is a possible drug interaction with Suvorexant?

Answer 43

Metabolized by CYP3A4 (Cimetidine inhibits CYP3A4)

Question 44

What are SE of Suvorexant?

Answer 44

``` HA Abnormal dreams Sleep paralysis Hallucinations Worsening depression ```

Question 45

What is a contraindication of Suvorexant?

Answer 45

Narcolepsy

Question 46

What is the MOA of Ramelteon?

Answer 46

Melatonin analogue; resets sleep-wake cycle; promotes sleepiness with no GABA effect

Question 47

What are SE of Ramelteon?

Answer 47

Drowsiness, dizziness, nausea

Question 48

What is the use of Suvorexant?

Answer 48

Insomnia

Question 49

What is the use of Ramelteon?

Answer 49

Insomnia

Question 50

What is an antihistamine that can be used for occasional insomnia? (good option for addicts)

Answer 50

Diphenhydramine

Question 51

What is the MOA of Chloral Hydrate?

Answer 51

Converted to trichloroethanol which causes sedation

Question 52

What is the margin of safety of Chloral Hydrate?

Answer 52

Low margin of safety (high doses induce respiratory and vasomotor depression)

Question 53

What can long-term use of Chloral Hydrate cause?

Answer 53

Liver damage and fatal intoxication

Question 54

What are uses of Chloral Hydrate?

Answer 54

Sedation during pediatric dental procedures | cheap

Question 55

What is the MOA of Buspirone?

Answer 55

Relieves anxiety without producing sedation; works independently of GABA at serotonin receptors

Question 56

What class of anxiolytic has no muscle relaxant or anticonvulsant properties?

Answer 56

Buspirone

Question 57

Why is Buspirone a good option for tx of anxiety in alcoholics/addicts?

Answer 57

Does not potentiate CNS depression with alcohol or BZs

Question 58

What are uses of Buspirone? (6)

Answer 58

``` Generalized anxiety Anxiety with depression ADHD Autistic pts with anxiety PMS Anxiety in recovering alcoholics/addicts ```