Hypnotics(Benzo&Barb)

Question 1

Name the 5 major classes of drugs used as hypnotics

Answer 1

Benzodiazepines
Barbiturates
NBBRAs - nonbenzo benzo receptor agonists
5-HT1A partial agonists
MT (melatonin) receptor agonists

Question 2

Which type of drug has more pronounced depression of the CNS? Sedative or hypnotic?

Answer 2

Hypnotic - can be achieved by increasing dose of sedative as well

Question 3

Which type of sedative hypnotic drug shows a nonlinear dose-response curve? Why is this important?

Answer 3

Benzos
Increasing dose eventually tapers off the sedation effects so they are safer drugs. Older drugs showing linear curve could produce anesthesia or even coma and death with increasing dose

Question 4

MOA of benzos

Answer 4

Bind GABAa receptors at BZ1 or BZ2 which functions as a chloride channel and increase its activity by causing more frequent channel openings.

They reduce the EC50 of the GABA induced Cl- influx

Question 5

Agonists at the benzo receptors produce what two important clinical effects?

Answer 5

Anxiolytic (anti-anxiety) and anticonvulsant

Question 6

What is the method of delivery for benzos? How do they distribute?

Answer 6

Oral - highly lipophilic and distribute throughout body

Question 7

Name the 2 short acting benzos

Answer 7

Oxazepam and triazolam

Question 8

Name the three intermediate acting benzos

Answer 8

Alprazolam
Lorazepam
Temazepam

Question 9

Name the two long acting benzos

Answer 9

Diazepam

Flurazepam

Question 10

What enzyme catalyzes phase I reactions of benzos? After this, how are they excreted?

Answer 10

CYP3A4

Conjugated and excreted in urine

Question 11

Name three benzos that are NOT metabolized by the P450 system

Answer 11

Oxazepam
Lorazepam
Temazepam
Skip phase I reactions and are conjugated directly

Question 12

Which benzo is metabolized in liver to active metabolites that can vary in half lives between 30 and 100 hours?

Answer 12

Flurazepam

Question 13

What is the role of benzos in treating anxiety?

Answer 13

They are only given short term, 4-6 weeks, while waiting for the SSRI to take effect

Question 14

Which benzo is useful in treating muscle spasms and can be used in MS and cerebral palsy?

Answer 14

Diazepam

Question 15

Which benzo is used to treat epileptic seizures?

Answer 15

Clonazepam

Question 16

Name the two benzos used to treat status epilepticus

Answer 16

Diazepam and lorazepam

State where brain is constantly having a seizure

Question 17

Which two benzos can be used in managing alcohol withdrawal?

Answer 17

Diazepam and oxazepam

Question 18

Name a benzo for each category used in sleep disorders: long, intermediate, and short acting

Answer 18

Long: Flurazepam
Intermed: Temazepam
Short: triazolam

Question 19

Patient taking a sleep aid presets with anxiety, irritability, rage, and hostility. What type of drug was she most likely taking?

Answer 19

Benzo - can cause paradoxical effects

Barbiturates also do this

Question 20

Name the only two class of drugs where abrupt withdrawal can kill you

Answer 20

Benzos and barbiturates

Question 21

What does flumazenil do? Two adverse effects?

Answer 21

It is the only benzo receptor antagonist - used in benzo overdose
Can cause withdrawal in the physiologically dependent
Can lead to seizures if the benzo was being used to treat them

Question 22

MOA of barbiturates?

Answer 22

Like benzos, act at GABAa receptors (but bind at a different site)
But they also bind less specifically than benzos so they also block glutamate receptors and sodium channels

Question 23

Explain how barbiturates can lead to death by respiratory failure

Answer 23

They suppress the hypoxic and chemoreceptor response to CO2. So impulse to breathe is blocked

Question 24

What actions do barbiturates have on CYP enzymes?

Answer 24

They are CYP inducers

Question 25

Which barbiturate is still used IV to induce anesthesia?

Answer 25

Ultra short acting thiopental

Question 26

Which barbiturate has anticonvulsant properties and is still used to treat tonic-clonic seizures, status epilepticus, and eclampsia?

Answer 26

Phenobarbital

Question 27

Which sedative drug can be used to treat hyperbillirubinemia and kernicterus in the neonate?

Answer 27

Phenobarbital

Question 28

Which sedative class of drug is contraindicated in patients with porphyria?

Answer 28

Barbiturates - increase porphyrin synthesis

Question 29

Which sedative class of drug can cause hangover effects?

Answer 29

Barbiturates

Question 30

Which sedative class of drug can cause hyperalgesia?

Answer 30

Barbiturates

Question 31

Which class of sedative drug, if given rapidly by IV can lead to cardiovascular collapse?

Answer 31

Barbiturates