9 - Sedative - Hypnotics

Question 1

MOA of barbiturates

Answer 1

• increase DURATION of opening of chloride channels
• blocks action of glutamic acid
• blocks Na channels

Question 2

MOA of benzodiazepines

Answer 2

• increase in FREQUENCY in opening of Chloride channels

Question 3

5 principle pharmacologic effects of benzodiazepine

Answer 3

1. Anxiolytic
2. Sedative and hypnosis
3. Anticonvulsant
4. Muscle relaxant
5. Anterograde amnesia (take note of this)

Question 4

Use of benzodiazepines short BEFORE delivery

Answer 4

Floppy baby syndrome

Question 5

Prenatal BZD exposure

Answer 5

Increase risk of oral cleft

Question 6

Abnornmal sleep pattern seen in BZD

Answer 6

Decreased REM sleep

Question 7

Long-acting BZD that is painful on injection

Answer 7

Diazepam

Question 8

Most effective drug for stopping Status Epilepticus

Answer 8

Diazepam

Question 9

Date-rape drugs

Answer 9

1. Alcohol - most common
2. Flunitrazepam (rohypnol) - BZD
3. Gamma hydroxybutyrate

Question 10

Anticonvulsant maintenance

Answer 10

Clonazepam

- intermediate-acting

Question 11

Status epilepticus

Answer 11

1. Lorazepam - intermediate

2. Diazepam- long

Question 12

Skeletal muscle relaxation (eg cerebral palsy)

Answer 12

Diazepam

Question 13

Panic disorder, phobia

Answer 13

Alprazolam - intermediate

Clonazepam

Question 14

Insomnia

Answer 14

1. Estazolam - intermediate
2. Flurazepam - long
3. Triazolam - short

Question 15

Anesthesia induction

Answer 15

1. Midazolam - short

2. Diazepam

Question 16

Bipolar disorder

Answer 16

Clonazepam

Question 17

Alcohol withdrawal

Answer 17

1. Chlordiazepoxide - long (longest half-life pf 36-200 hours)
2. Diazepam

Question 18

Antidote for BZD overdose

Answer 18

Flumazenil

• BZD antagonist
• competitive

Question 19

Parent compound of barbiturates

Answer 19

Barbituric acid

Question 20

Oxygen is found at the 2nd position

Answer 20

Oxybarbiturates

• pentobarbital
• secobarbital

Question 21

Replacement of oxygen with sulfur which makes it more lipid soluble

Answer 21

Thiobarbiturates

• thiopental
• thiamylal

Question 22

Phenyl group at 5th position which increases anticonvulsant effect

Answer 22

Phenobarbital

Question 23

Methyl group of nitrogen increases potency but lowers seizure threshold

Answer 23

Methohexital

Question 24

For seizure induction for epilepric patients undergoing temporal lobe resection

Answer 24

Methohexital

Question 25

Contraindication for barbiturate use

Answer 25

Porphyria
- side effect of barbs

Acute intermittent porphyria
- HMB synthase deficiency

Question 26

High dose BZD and barbs may suppress seizures but at the expense of marked sedation EXCEPT

Answer 26

• clonazepam

- phenobarbital

Question 27

Considered as DOC for seizures in infants

Answer 27

Phenobarbital

Question 28

Tx for seizures in pregnancy

Answer 28

Phenobarbital

Question 29

Intermediate-acting barb

Answer 29

• pentobarbital

- secobarbital

Question 30

Long-acting barb

Answer 30

• phenobarbital
• mephobarbital
• primidone

Question 31

BZ1 receptor agonist can will cause sedation ONLY

Answer 31

Zolpidem

BZ2 receptor
- cognition

Question 32

Used for insomnia and sleep disorders

Answer 32

Zolpidem

Zaleplon

Question 33

Partial agonist at 5HT1A and D2 agonist
For GAD (generalized anxiety disorder)

Answer 33

Buspirone

- safe for pregnant

Question 34

Anxiolytic:

Melatonin receptor agonist

Answer 34

Ramelteon

Question 35

Most catastrophic symptom of sedative-hypnotic withdrawal

Answer 35

Rebound suicide