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Pharmacology 200 > 2-sleep aids > Flashcards

2-sleep aids Flashcards

1
Q

what is a hyptonic

A

a drug that is used to treat insomnia

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2
Q

what was dangerous about old hypnotic agents

A

narrow therapeutic windows

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3
Q

what 5 signals are involved in the sleep wake cycle

A 
histamine
GABA
Adenosine
Melatonin
Orexin
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4
Q

how do drugs affect histamine in the sleep wake cycle

A

block histamine to make you drowzy

but not a great quality sleep

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5
Q

how do drugs affect GABA in the sleep wake cycle

A

boost GABA to decrease neuronal excitability

most common

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6
Q

how do drugs affect adenosine in the sleep wake cycle

A

neuromodulator, caffeine blocks the effect of adenosine

lots of side effects, cardiac

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7
Q

what is adenosine in the sleep wake cycle

A

neuromodulator (changes how other neurotransmitters work)

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8
Q

how do drugs affect melatonin in the sleep wake cycle

A

they do more stuff for circadian rhythm

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9
Q

how do drugs affect orexin in the sleep wake cycle

A

drug blocks the peptide orexin which is made in the hypothalamus and is involved in sleep wake cycling

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10
Q

which stages of sleep do benzodiazepines affect

A

REM sleep suppressants

increase stage 2

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11
Q

what happens to REM sleep as the night progresses

A

REM sleep increases

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12
Q

where are sleep spindles and K complexes found

A

stage 2

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13
Q

which stages are the deep sleep

A

3 and 4

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14
Q

how well do hypnotics replicate normal sleep cycles

A

not perfectly

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15
Q

what did chloral hydrate (chlorinated ethanol) do and why was it dangerous

A

“knock-our drops” but very dangerous

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16
Q

why is alcohol bad as a sleep aid

A

it doesn’t get you into deep sleep, its just bad for you okay

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17
Q

how do barbiturates and benzodiazepines work (What is the target)

A

positive allosteric modulators of GABA-A receptors

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18
Q

what happens when you potentiate the agonist effects of GABA

A

more Cl- ions go through, it decreases neuronal excitability

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19
Q

what is pentobarbital

A

a barbiturate

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20
Q

how did pentobarbital work

A

allosteric modulator that increases the length of time the channel stays open in the presence of GABA

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21
Q

what happens with pentobarbital at high concentrations

A

it directly opens the channel even when GABA isnt there!

22
Q

why is pentobarbital lethal when combined with alcohol

A

both of them increase Cl- to pass through, often death by asphyxiation

23
Q

what is triazolam (halcion)

A

benzodiazepine

24
Q

why is triazolam safer than pentobarbital

A

at high doses, it does not directly activate . the channel

25
Q

what does triazolam do

A

allosteric modulator that increases the frequency of channel openings in the presence of GABA

26
Q

so why are benzodiazepines and barbiturates different if they bind at the same site

A

they dont bind at the same site. barbs bind lower

benzos bind closer to the top and closer to where gaba binds

27
Q

why are benzos good for anxiety

A

because it can decrease neuronal firing

28
Q

what receptors are bezos selective for

A

GABA-A

highly selective

29
Q

which receptors are benzos not selective for

A

no affinity for glycine (even tho its super similar) and none of glutamate LGICs

30
Q

why are benzos only used in acute emergency situations IV for seizures

A

rapid development of tolerance

31
Q

what is the ceiling effect

A

BZs do not directly effect the channel at high doses, so they is a plateau before there are severe dangerous side effects
(barbs have direct effects on the channel, creating severe effects,even death)

32
Q

what is the diazepam half life

A

long, 30-56 hours

33
Q

what is nordazepam half life

A

7 days

34
Q

why are benzos not great for sleep

A

super long half life, it gives daytime impairment

35
Q

what is triazolam (Halcion)

what half life

A

hypnotic, 2 hours

36
Q

what is the active metabolite of triazolam

A

none

37
Q

what are the side effects of traizolam

A

high doses cause daytime memory impairment and some violence

38
Q

why isnt triazolam good for time time or early waking

A

because short half life, only helps with falling asleep

39
Q

why are BZ bad for memory

A

they are not selective within GABA-A, so they affect hippocampal receptors in memory formation and storage, and also it decreases REM

40
Q

what happens once you stop using benzos to sleep

A

you get a really bad rebound insomnia

addiction and dependence

41
Q

why are Benzos good for surgeries

A

cause it reduces memory and helps you forget what happened

42
Q

whats so special about Z-drugs

A

they have short half lives and bind at the GABA-A

43
Q

why are there different side effects to benzos

A

may have different selectivity towards specific GABA-A receptors so diff symptoms and less REM suppression so less REM rebound

44
Q

what does suvorexant (belsomra) do

A

antagonises orexin receptor to promote sleep onset and maintenance

45
Q

what do orexins do

A

peptides that are important for signal control of the sleep/wake cycle

46
Q

what does high orexins cause

A

wake

47
Q

what does low orexins cause

A

seep

48
Q

what happens when you block orexin receptors

A

promotes sleep

49
Q

where are orexins made and what types

A

A and B are made in hypothalamus, secreted in the neurons there

50
Q

how powerful is suvorexant

A

not very, studies show it may help you sleep 6mins more at night

Pharmacology 200 (29 decks)

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