Drugs for insomnia (no dreams of lions and tigers and bears... oh whatever)

Question 1

Types of sleep Apnea

Answer 1

Transient less than 3 days, acute stress
Short term- < 3 weeks acute stressor of ongoing nature
Chronic- > 3 weeks, psychiatric, beh, medical, or primary issue

Question 2

Barbiturates- MOA

Answer 2

prolong Cl channel opening

act independent of GABA @ high doses

Question 3

Barbiturate actions

Answer 3

sedation, hypnosis, anticonvulsant, muscle relaxant, medullary suppression

Question 4

Barbiturate- Clinical use

Answer 4

Not used anymore due to risk of tolerance, dependence, AE and withdrawal

Question 5

Barbiturate- AE

Answer 5

Respiratory depression, coma, and death

Question 6

Benzodiazepine- Drug names

Answer 6

Triazolam
Temazepam, Estazolam
Flurazepam, Quazepam
(there are more but these are the only ones used for this)
Classified based on spd of onset & T1/2

Question 7

BZD- MOA

Answer 7

GABA depenent
changes allosteric conformation of GABA to inc frequency of opening.
Enhance response to GABA

Question 8

BZD- receptors

Answer 8

omega 1- sedative effects, most common receptor in CNS
Omega 2- anterograde amnesia, anxiolysis- hippocampus, striatum, spinal cord
omega 3- process sensory and motor info- cerebellum

Question 9

BZD- actions

Answer 9

sedation, anxiolytic, muscle relaxation

Question 10

BZD- effects on sleep

Answer 10

decrease time to tall asleep
increases total duration of sleep
Doesn’t effect REM as much as barbiturates unless there is repeated dosing

Question 11

Triazolam- kinetics, use

Answer 11

rapid onset and short acting

best for problems initiating sleep

Question 12

Temazepem and Estazolam- kinetics, use

Answer 12

delayed onset

intermediate length of axn

Question 13

Flurazepam and Quazepam- kinetics, use

Answer 13

rapid onset and long acting

best for problems maintaining sleep

Question 14

BZD- problems and AE

Answer 14

Tolerance
Dependence
Residual daytime sedation
rebound insomnia
anterograde amnesia
reduced REM with repeated dosing
OD

Question 15

BZD- tolerance

Answer 15

Tolerance develops to the hypnotic effects in 2–4 weeks, not to the anxiolytic effects.
to avoid this use intermittent pattern of use or gradual escalation of dose

Question 16

BZD- dependance

Answer 16

physical- withdrawal= worse insomnia, tinnitus, photophobia, fatal seizures
psychological crazing is NBD

Question 17

BZD- residual sedation

Answer 17

common with agents with long T 1/2 @ high doses

Question 18

BZD- rebound insomnia

Answer 18

common with short acting agents when the drug is stopped

this is worse than the original insomnia

Question 19

BZD- anterograde amnesia

who is this a problem for

Answer 19

seen in all agents
impairs acquisition and encoding of new info
b/c of which receptor
PROBLEM IN THE ELDERLY

Question 20

BZD- OD

Answer 20

CNS and respiratory depression

this is rare to happen alone but can happen concomitant alcohol, barbituate, or narcotic use

Question 21

BZD- OD antidote

Answer 21

Flumazenil- competitive antagonist with BZDs for GABA-A binding complex.
only works on BZDs doesnt work on other agents
has a short duration of 30-60 min so may need to dose repeatedly.
Can induce withdrawal seizures in BZD dependent person

Question 22

BZD- clinical use

Answer 22

low dose= anxiolytics, skeletal muscle relaxation

higher dose= sleep aid

Question 23

Non BZDs= Imidazopyridines- drug names

Answer 23

Zaleplon
Zolpidem
Zopiclone/ Eszopiclone

Question 24

Zaleplon- duration, advantages, use

Answer 24

shortest T1/2, fewest morning problems, use during night time awakenings

Question 25

Zolpidem- use

Answer 25

has CR formulation, used for long term therapy

Question 26

Zopiclone- duration, use, AE

Answer 26

longest T 1/2, used for sleep maintenance or chronic insomnia.
AE= daytime sleepiness

Question 27

Imidazopyridines- MOA

Answer 27

bind Omega 1- less cognitive, memory, and motor effects

Question 28

Imidizopyridines- difference with BZD

Answer 28

No anticonvulsant axn and muscle relaxation
better AE profile- no tolerance or withdrawal, no respiratory depression, minimal rebound insomnia and morning sedation.
No effect on REM

Question 29

Imidizopyridines- clinical use

Answer 29

Good choice when avoiding BZDs

cannot be used in obstructive sleep apnea

Question 30

Melatonin receptor agonists

Answer 30

Rameltreon

Question 31

Ramelteon- MOA

Answer 31

activates suprachiasmatic nucleus (in hypothalamus) melatonin receptors- which are circadian rhythm regulators

Question 32

Ramelteon- clinical use

Answer 32

no indication of dependence/ tolerance

can be used for chronic insomnia and safely used in OSA

Question 33

OTC medication for insomnia

Answer 33

Antihistamines- Diphenhydramine

Question 34

Antihistamines- effect

Answer 34

sedating and anti cholinergic

Question 35

Antihistamine- popular use, CI what population… why?

Should it be used, why or why not?

Answer 35

Diphenhydramine is popularly used with BZD
CI in elderly b/c anticholinergics can worse dementia
regular use is not recommended b/c not very efficacious and causes daytime sedation

Question 36

Sedating Antidepressants

Answer 36

TCAs and Trazodone

Question 37

Trazodone in insomnia

Answer 37

Use alone for insomnia or to combat SSRI induced insomnia

no dependence

Question 38

Tarzodone- dosing and AE

Answer 38

lower dose than depression but significant AE and not a lot of data on long term use.

Question 39

Drugs not to use with OSA

Answer 39

Barbituates
BZDs
Imidazopyridines