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Neuro Quiz 2 > Anxiolytic and Hypnotics > Flashcards

Anxiolytic and Hypnotics Flashcards

1
Q

Define sedative

A 
Decreases activity
Moderates 
Excitement
Calms
-Doesn't put you to sleep though
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2
Q

Define hypnotic

A

Produces drowsiness
Facilitates onset and maintenance of sleep that resembles natural sleep
Easily aroused sleep

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3
Q

GABA is

A

Major inhibitory NT

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4
Q

GABA(A)

A

Ligand operated

Permeable for Cl- which leads to hyperpolarization

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5
Q

GABA(B)

A

Metabotropic receptor
Inhibits adenylate cyclase, reduces NT release
Mostly in SPINE
Not helpful for anxiety

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6
Q

More Cl =

A

More inhibition = less anxiety

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7
Q

**Benzodiazepines MOA

A

Potentiate the action of GABA which increases the flux of chloride which makes more pronounced hyperpolarization and less excitable neurons
DOES NOT DIRECTLY ACTIVATE GABA(A) RECEPTOR

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8
Q

Flunitrazepam (BZ), pentobarbital and ethanol all

A

Cause sedation, CNS depression, anxiolysis and euphoria

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9
Q

GABA(A) has

A

different subunits

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10
Q

BZ are activators of which receptors

A

alpha 1/2/3/5 (not 4/6

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11
Q

Alpha 6 involved in

A

motor and balance coordination

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12
Q

Alpha 1 responsible for

A

Hypnotic/sedative
Anticonvulsant
Antergrade Amnesia

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13
Q

Alpha 2 responsible for

A

Anxiolysis

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14
Q

Pi pi stacking

A

Week form of bonding between groups when aligned parallel

Weak but multiple can be strong

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15
Q

Benzodiazepines are strictly :

A

allosteric modulators of the GABA(A) receptor

DO NOT directly open the receptor

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16
Q

What combination can be lethal?

A

Benzo and Alcohol

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17
Q

Antidote of Benzodiazepines

A

Flumazenil

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18
Q

Flumazenil MOA

A

Binds to GABA(A) receptor and competitively antagonizes BDZ

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19
Q

Overall Effects of BDZ

A 
Reduction of anxiety and aggression
Sedation (little suppression of REM)
Anti-convulsant effect
Anterograde amnesia
Paradoxical effect (excitation)
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20
Q

PK of BDZ

A

Lipophilic
Liver
Active metabolites
No enzymes

21
Q

Dizepam –>

A

Temazepam –> Oxazepam

22
Q

Dexomoxepam –>

A

Diazepam

23
Q

Prazepam –>

A

Diazepam

24
Q

Short half life BZs

A

Triazolam

Oxazepam

25
Q

Intermediate half life of BZ

A

Estazolam
Temazepam
Lorazepam
Alprazolam

26
Q

Long half life of BZ

A 
Flurazepam
Diazepam
Quazepam
Nitrazepam
Clonazepam
27
Q

Rapid onset BZ

A 
Triazolam
Estazolam
Flurazepam
Diazepam
Quazepam
Nitrazepam
Clonazepam
28
Q

Slow onset BZ

A

Oxazepam

Temazepam

29
Q

Intermediate onset of BZ

A

Lorazepam

Alprazolam

30
Q

Overall side effects BZ

A 
Daytime sedation
Reduction of reaction time
Ataxia, falls
COGNITIVE DEFICITS
Addictive!!!
31
Q

BZ Approved for Insomnia

A

Flurazepam and Quazepam (long half life)
Triazolam (short)
Estazolam and temazepam (int)

32
Q

Problem with ultra-long half-life

A

Sleep through the night and then sleep through the day

Then you take another and it keeps increasing until its toxic

33
Q

Problem with ultra-short half-life

A

Fall off around 3-4 hours so then you wake up

34
Q

Problem with moderate half-life

A

Stay during the day and you have a hangover effect

35
Q

Zolpidem is what?

A

Non-BZ hypnotic (Z drugs)

Selective for alpha 1 subunit (which is great)

36
Q

Zolpidem effects

A

Pronounced sedative

Onset: 15 minutes and last for 2-3 ours

37
Q

Other Z drugs

A

Zaleplon (1 hr) and Eszopiclone (6 hr)

38
Q

Thiopental

A

Pentothal

Induction of anesthesia

39
Q

Pentobarbital

A

Nembutal

40
Q

Secobarbital

A

Seconal
Pre-OP sedation
Insomnia

41
Q

Phenobarbital (luminal)

A

Anti-consulvant

42
Q

Barbiturates PD PK

A

High doses: open the channel directly (overdose)

Strong induction of P450s so drugdrug interactions

43
Q

Acute effects of barbiturates

A 
Strong sedation
Some anticonvulsants
No anxiety
Suppresses REM
Repiratory and CV depression at high doses
Paradoxical excitement
44
Q

BZ as drug of choice… But why?

A 
High therapeutic index
Few peripheral effects
Low tolerance
Low dependence
Few drug interaction
No respiratory depression (death)
45
Q

Ramelteon is a

A

Melatonin MT1/2 receptor agonist
Extensive first pass
Cyp1A2 which is induced in smokers
MEEEEHHHH

46
Q

Belsomra

A 
Suvorexant
Orexin antagonist (NT protein that regulate arousal and wakefulness)
47
Q

Belsomra AE

A

Daytime somnolence
Suicidal thinking
COPD
Sleep paralysis, hallucinations

48
Q

Belsomra Interactions

A

Digoxin

CYP3A

Neuro Quiz 2 (4 decks)

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