Sedative/Hypnotics & Barbituates

Question 0

Class of Flurazepam

Answer 0

Benzodiazepine Receptor Agonist

Question 1

Class of Triazolam

Answer 1

Benzodiazepine Receptor Agonist

Question 2

Class of Secobarbital

Answer 2

Barbiturate

Question 3

Class of Zolpidem

Answer 3

Non-Benzodiazepine Benzodiazepine Receptor Agonist (Allosteric GABA-A agonist). GABAa receptor containing a1 subunit.

Question 5

Class of Ramelteon

Answer 5

Melatonin Receptor Agonist

Question 6

Halflife of Triazolam and what does this mean?

Answer 6

Ultrashort: 1.5 to 5 hours = Incidence of daytime drowsiness is low.

Question 7

T/F: Triazolam has a residual anti-anxiety effect?

Answer 7

False

Question 8

What can occur in a single night with Triazolam?

Answer 8

Rebound insomnia and REM rebound

Question 9

Is incidence of of anterograde amnesia higher or lower with triazolam than with other hypnotics?

Answer 9

HIGHER

Question 10

What are two major SE of triazolam?

Answer 10

Somnolence (14%) and Headache (10%)

Question 11

Duration of action for flurazepam?

Answer 11

6-8 hr : Long acting

Question 12

T/F: Flurazepam has a residual anti-anxiety effect

Answer 12

True

Question 13

T/F: The tolerance to flurazepam is SLOW to develop?

Answer 13

True: (2 weeks)- but not recommended for daily long term usage

Question 14

Because of the long duration of flurazepam, what side effect may it have?

Answer 14

Interfere with daytime wakefullness

Question 15

Most common side effects of Zolpidem?

Answer 15

Drowsiness, drugged feeling, dizziness. Increasing reports of somnambulism, sleep eating, sleep driving, etc.

Question 16

Why might you use ramelteon?

Answer 16

Quick acting, No rebound insomnia, with withdrawal, may work for circadian rhythm problems.

Question 17

SE of Ramelteon:

Answer 17

Dizziness, somnolence, fatigue. Metabolized by CYP 1A2 (not with fluvoxamine).

Question 18

MOA for Phenobarbital, secobarbital, and thiopental?

Answer 18

1) Bind to barbiturate binding site on GABA-A receptor.
2) Potentiate action of GABA (positive allosteric modulator) at normal doses.
3) At high concentrations barbiturates are direct GABA-A receptor agonists.

Question 19

T/F: It is difficult to separate the sedative and hypnotic properties of barbiturates?

Answer 19

True- so they usually occur together.

Question 20

Barbiturates strongly induce which enzymes?

Answer 20

Cytochrome P450: Leads to multiple drug reactions.

Question 21

The therapeutic window for barbiturates is narrow/wide?

Answer 21

NARROW: 10x the normal therapeutic dose- overdose can be fatal.

Question 22

What is a serious problem with barbiturates?

Answer 22

Physical dependence