Sedative Hypnotic Agents

Question 1

A drug that induces sleep =

Answer 1

hypnotic

Question 2

A drug that produces sedation =

Answer 2

sedative

See… easy, peasy! ;-)

Also:
Calming of mental excitement
Reduction of agitation or irritability
Reduction of anxiety and apprehension (anxiolytic)

Question 3

T/F: Barbiturates are safer than Benzodiazepines b/c they don’t induce coma.

Answer 3

False. The reverse is true. Benzodiazepines are safer.

Question 4

Which of the following is NOT a benzodiazepine?
A.Diazepam
B. Clonazepam
C. Chlordiazepoxide
D. Eszopiclone

Answer 4

D. This is a non-benzodiazepine

Question 5

Name 3 Non-benzodiazepines

Answer 5

Zolpidem
Zaleplon
Eszopiclone

Question 6

What is required on the benzodiazepine structure for sedative-hypnotic activity?

Answer 6

Halogen or nitro group

Question 7

Name 2 barbiturates

Answer 7

Phenobarbital

Primidone

Question 8

Buspirone and doxepin are ___

Answer 8

anxiolytics

Question 9

Ramelteon, diphenhydramine, doxylamine are ___

Answer 9

hypnotics

Question 10

Name the GABAA receptor subunits

Answer 10

2 alpha, 2 beta, gamma

Question 11

Benzodiazepine or barbiturates, both or neither?

GABAa receptor agonist

Answer 11

Neither b/c they do NOT activate GABA-A receptors in the absence of GABA.

Both are GABA-A receptor modulators

Question 12

Benzodiazepine or barbiturates, both or neither?

Increase frequency of Cl- channel opening, even without GABA present

Answer 12

Neither

Question 13

Benzodiazepine or barbiturates, both or neither?

Increase frequency of Cl- channel opening with GABA present

Answer 13

Benzodiazepine

Question 14

Benzodiazepine or barbiturates, both or neither?

Enhance GABA’s inhibitor effect by increasing Cl- influx (hyperpolarization)

Answer 14

Both

Question 15

Benzodiazepine or barbiturates, both or neither?

At high concentration, it directly activates Cl- channel, even without GABA

Answer 15

Barbiturates

Question 16

Benzodiazepine or barbiturates, both or neither?

Increase the duration of GABA-gated Cl- channel opening

Answer 16

Barbiturates

Question 17

What happens at high concentrations of barbiturates?

Answer 17

They bind to other receptors –> less selective for GABA-A receptor

Interact w/ glutamate receptors as antagonists –> greater CNS effects –> coma

Question 18

Name the drug:

Used as reversal agent for BZD overdose

Answer 18

Flumazenil

Question 19

Which of the following TRUE about Flumazenil?
A. Noncompetitive antagonist of BZD receptor
B. Antagonizes the effects of alcohol, barbiturates and anesthetics
C. Duration of action is shorter than BZD and nBZDs
D. Used for barbituate overdose

Answer 19

C. Need to dose repeatedly b/c of this.

A. Competitive antagonist of BZD receptor
B. Does not antagonize any of those
D. Used for BZD overdose and speed recovery from BZD administered for surgical or diagnostic procedures.

Question 20

Which receptor does Buspirone act on?

Answer 20

Partial agonist at 5HT1A receptor

Question 21

T/F: Buspirone is mainly an anxiolytic but also has sedative-hypnotic effects.

T/F: Buspirone has little risk of tolerance or dependence.

Answer 21

False. Does NOT have sedative-hypnotic effects

True.

Question 22

Buspirone half life:

Onset of effect:

Answer 22

~2 hours

~ 1 week

Question 23

Doxepin is a _____

Type of effect:

Answer 23

Antidepressant

Anxiolytic

Question 24

Which receptor does Ramelteon act on?

Uses?

Answer 24

Melatonin receptors: MT1 and MT2 melatonin receptors in suprachiasmatic nucleus
NO affinity for GABA-A - BDZ receptor complex

Reduce latency to sleep in pts w insomnia

Question 25

What receptors do diphenhydramine and doxylamine act on?

Use?

Answer 25

Antagonist at H1 histamine and muscarinic ACh receptor

Hypnotic

Question 26

Which of the following is TRUE about benzodiazepines?
A. SubQ for anxiety and sleep disorders
B. Can cross the placenta and secreted to breast milk.
C. Triazolam and lorazepam are fast onset since they are more lipid soluable.
D. Oxazepam and diazepam are slow onset

Answer 26

B

A. Oral
C. Triazolam and diazepam are fast onset
D. Oxazepam and lorazepam are slow onset

Question 27

Benzodiazepine mostly metabolized by ___

Answer 27

liver

CYP3A4, CYP2C19

Question 28

2 benzodiazepines that are directly metabolized by glucuronide conjugation (phase 2)

Answer 28

Lorazepam

Oxazepam

Question 29

Name the BZD and nBZD used for insomnia (3)

Answer 29

Lorazepam
Alprazolam
Zolpidem

Question 30

Name the BZDs used for anxiety (3)

Answer 30

Didazepam
Lorazepam
Alprazolam

Question 31

Name the BZD used for pre-anesthetic medication

Answer 31

Midazolam
Ultra short elimination half-life
Fast peak plasma concentration: 0.2-1 hr

Question 32

Name the barbiturates used for preoperative sedation (2)

Answer 32

Pentobartital

Amobarbital

Question 33

Name the barbiturate used for anesthesia induction

Answer 33

Thiopental

Question 34

Name the barbiturate used for anticonvulsant

Answer 34

Phenobarbital

Question 35

T/F: Benzodiazepines can be used as general anesthetic drugs and analgesic drugs.

Answer 35

False. Even though increasing doses produce sedation, hypnosis, stupor, unconsciousness, it is NOT a general anesthetic drug.
Reported analgesia may be due to anterograde amnesia BZD produces. NOT an analgesic drug.

Question 36

Put in order of the onset of tolerance to BZD affects from 1st to last:
Sedation, antianxiety, anticonvulsant, muscle relaxant

Answer 36

Anticonvulsant > sedation&raquo_space; muscle relaxant > anti-anxiety

Question 37

Zolpidem, Zaleplon, Eszopiclone are used to ___

Answer 37

induce sleep

Decrease REM sleep, increase non REM-sleep but hey! At least you’re asleep!

Question 38

T/F: Hypnotic doses of Zolpidem, Zaleplon, Eszopiclone will cause respiratory & cardiovascular effects.

Answer 38

False. IV administration will cause this.