Sedative Hypnotic Drugs

Question 1

CNS depressant effects of Benzodiazepines

Answer 1

Anxiolysis
Sedation
Hypnosis
Anesthesia

Question 2

Which GABA receptor do Benzo’s act on?

Answer 2

Benzos act on GABAa receptors as agonists that increase the frequency of Cl- channel opening which leads to Hyperpolarization of the cell

Question 3

Can Benzo’s and Barbiturates effects be reversed?

Answer 3

Benzo’s can be reversed with flumazenil

Barbiturates cannot be reversed which is why they are more dangerous and not really prescribed anymore.

Question 4

What class schedule are Benzos?

Answer 4

Class IV

Barbiturates are Class II

Question 5

What is the most prescribed Benzo

Answer 5

Alprazolam (Xanax)

Question 6

Which Benzo is used for insomnia

Answer 6

Temazepam (Restoril)

Question 7

What is the date rape drug?

Answer 7

Flunitrazepam (Rohypnol)

Question 8

Clinical uses of Benzo’s

Answer 8

Anxiolytic
Sedative
Anticonvulsant
EtOH withdrawal

Question 9

How are Benzos eliminated?

Answer 9

Phase I- CYP3A4

Phase II- Glucuronidation

Question 10

Most common side effect with benzo’s

Answer 10

Drowsiness

Other: confusion, muscle weakness, slurred speech, dizziness

Question 11

Diazepam (Valium)

Answer 11

GABAa receptor agonist used for EtOH withdrawal, anxiety, Status Epilepticus

Off-label use: Sympathomimetic intoxication (cocaine, Meth)
Serotonin Syndrome

Question 12

Alprazolam (Xanax)

Answer 12

GABAa agonist used for generalized anxiety DO, Depression-induced anxiety, Panic DO

Question 13

Temazepam (Restoril)

Answer 13

GABAa agonist used to treat insomnia

“TAZmanian devil never sleeps, so he takes TemAZepam”

Question 14

Midazolam

Answer 14

Benzo used for pre-op sedation, induction of anesthesia.

Can be IV or IM** (if someone is already seizing and no IV has been inserted)

Question 15

Non-Benzo BZ Agonists

Answer 15

Zolpidem (Ambien)
Eszopiclone (Lunesta)- approved for long-term use
Zaleplon

Question 16

Zolpidem (Ambien)

Answer 16

BZ1 receptor used for insomnia. Safe for pregnancy.

SE- Complex sleep behaviors that can be dangerous such as sleep-walking, driving, sex, eating food

Question 17

Flumazenil

Answer 17

Benzo antagonist that blocks Benzo binding to GABAa receptor.
Can cause seizures

Question 18

Barbiturate examples

Answer 18

Phenobarbital- Tonic clonic seizures
Pentobarbital
Thiopental- sedative/anesthetic; replaced by propofol

Question 19

Barbiturate MOA

Answer 19

GABA independent increase in duration of Cl- channel opening to hyperpolarize cell

Question 20

You have a patient that is taking Warfarin and was given a barbiturate for a seizure. What is the effect on his Warfarin?

Answer 20

Barbiturates are CYP inducers, so his Warfarin dose will need to be increased to maintain an adequate level

Question 21

Buspirone

Answer 21

Nonbenzo anxiolytic; partial 5HT agonist for anxiety

Question 22

Ramelteon

Answer 22

MT1/MT2 agonist in suprachiasmatic nuclei to enhance release of Melatonin in insomniacs

Question 23

Suvorexant

Answer 23

Blocks orexins from binding and promoting wakefulness.
Helps patients FALL asleep

“Soothing Suvorexant helps you go to sleep”

Question 24

Doxepin

Answer 24

H1 antagonist and 5HT/NE reuptake inhibitor.

Helps patients STAY asleep

Question 25

What is the general current first line treatments for Anxiety/Panic DO’s

Answer 25

1. CBT
2. SSRI
3. Benzo only if no hx of SUD