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Neorologia > Anxiolytic and Hypnotic Drugs > Flashcards

Anxiolytic and Hypnotic Drugs Flashcards

1
Q

Fluoxetine (Proxac)

MOA

A

SSRI

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2
Q

Duloxetine (Cymbalta)

MOA

A

SERT & NET

Blocker

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3
Q

How long does it take to see response in SSRI/SERT&NET blockers?

A

2-4 week delay

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4
Q

Barbiturate Uses

A

Induction of anestesia
Epilepsy
Tension/Migraine HA

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5
Q

Barbiturate synergism with which Drugs?

A

EtOH,
BZD’s,
Z drugs
opioids

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6
Q

Barbiturates

MOA

A

APLs of all GABAa receptors

Increase DURATION of GABAa channel opening

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7
Q

Barbiturates and tolerance

A

Rapid PK tolerance due to induction of CYP

Slow PD tolerance:change in receptor number and composition

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8
Q

Ultrashort acting barbiturate use

A

Induction of anesthesia

Terminal anesthesia

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9
Q

Intermediate acting barbiturate use

A

Single drug lethal injection

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10
Q

Long acting barbiturate use

A

Anti-convulsant

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11
Q

Long acting barbiturate example

A

Phenobarbital

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12
Q

Phenobarbital

MOA

A

Barbiturate:

APL of GABAa

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13
Q

ADRs for Barb»BZD»Zdrug

A 
Sedation
Decreased cognition
Decreased REM sleep 
Hangover
-Anterograde Amnesia
-Tolerance
-Dependence
-Ataxia
-Withdrawal
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14
Q

How are BZDs similar?

A

Therapeutic use
pharmaco action
ADRs

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15
Q

How do BZDs differ?

A
  • Onset of action
  • Maximal efficacy
  • Lipid solubility
  • Drug interactions
  • Duration of action
  • Metabolic pathways
  • Active Metabolites
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16
Q

BZD MOA

A
  • APL of GABAa receptor

- Binding increases affinity for endogenous GABA increasing FREQUENCY of channel opening

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17
Q

Barbiturates vs BZDs which increases duration vs frequency of channel opening

A

Barbiturates: Duration
BZDs: Frequency

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18
Q

Do BZDs directly open the chloride channel?

What is the effect of this?

A

No.

Difficult to produce fatal respiratory depression in normal pt

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19
Q

Which GABAa subunits do BZDs interact with?

A

Alpha: 1,2,3, or 5

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20
Q

Which GABAa alpha subunit is most widely distributed, most sedating

A

Alpha 1

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21
Q

Where is alpha 2 subtype localized?

What is the effect?

A 
Limbic system (Hippocampus and Striatum)
Anxiolytic
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22
Q

Where are alpha 3 and 5 subtypes located?

What is the effect?

A

Spinal chord

Muscle relaxant

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23
Q

Which subtype are Z drugs more selective for?

What is the effect?

A

Alpha 1
Good hypnotic
Poor muscle relaxant

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24
Q

BZD metabolism

A

CYP3A4 and CYP2C19

-Do not induce CYP

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25
Q

Do BZDs induce PK tolerance?

A

No. No CYP induction

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26
Q

BZD Withdrawal

A 
Anxiety
Psychosis
ANS (N&V, CV, Sweating)
Panic, 
Convulsions
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27
Q

Diazepam (Valium)

Uses

A

Anxiolytic,
Anticonvulsant,
Muscle Relaxant
Preanesthetic med

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28
Q

What is a major source in variability for BZDs with regards to half life and potency?

A

Metabolites.

All have different half lives and potency

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29
Q

Flumazenil (Romazicon)

MOA

A

GABAa (BZD site) direct antagonist

30
Q

Flumazenil (Romazicon)

Use and administration

A

IV administration for BZD overdose

31
Q

Is Flumazenil Used for Barbiturate overdose?

A

No. It has a different binding site

32
Q

What is a non-barbiturate, non-BZD drug used for anxiolytic/sedation

A

Buspirone (Buspar)

33
Q

Buspirone (Buspar)

MOA

A

5-HT-1a partial agonist (Gi)

34
Q

Whereis g-HT-1a highly concentrated?

A

amygdala and limbic regions of the cortex

35
Q

Bupsirone (Buspar) primary use

36
Q

Buspirone (Buspar) compared to BZDs

A

-Less sedation and other ADRs

37
Q

Buspirone (Buspar)

Onset

A

-Onset delayed for 2-4 weeks

38
Q

Buspirone (Buspar) ADRs

A

N&V, dizziness, HA

39
Q

Buspirone (Buspar)

Metabolism

40
Q

Why is Buspirone favored over BZDs for pt with a history of drug abuse?

A

Non-hypnotic

Non-addictive

41
Q

When to use caution with buspirone

A

Think Serotonin
MAOIs or SSRIs
-Better to use BZDs

42
Q

Buspirone is used for GAD, what about acute panic attacks? Why or why not?

A

Nope.

Onset 2-4 weeks

43
Q

Treatment of other anxiety disorders

A

Anti-depressant(s), buspirone, BZDs (for exacerbations)

-Or cominations

44
Q

Treatment of anxiety related disorders:

Acute panic attacks

A

Beta-blockers

45
Q

What regions regulate non-rem sleep?

A

The Raphe (5HT) and the nucleus of the solitary tract (NTS) [NE; autonomic control]

46
Q

Which brain region thought to control REM sleep

A

Cholinergic regions in the forbrain and midbrain

47
Q

Effect of BZDs on sleep

A

Decreased: latency to sleep, time until first REM cycle, number of awakenings
Increased time in stage 2 non-rem sleep

48
Q

BZDs and REM sleep

A

Decreased total REM, but increased total sleep. REM rebounds in withdrawal

49
Q

BZDs and sleep ADRs

A

Long acting - risk for hangover

Rapid onset have increased abuse potential and rebound insomnia

50
Q

Zdrug MOA

A

Interact selectively with Alpha 1 GABAa receptors in “sleep centers”

51
Q

Zdrugs as anxiolytics, anti-convulsants, or muscle relaxants

A

Don’t do it!

Wrong GABAa subtype

52
Q

Zdrugs and abuse

A

Have abuse potential
Tolerance an occur
Not as bad as barbiturates or BZDs

53
Q

Difference between Zopiclone (Imovane) and Eszopiclone (Lunesta)?

A

Eszopiclone (Lunesta) is chiral

54
Q

Zolpidem (Ambien)

t1/2 and use

A

~2 h

Use only if full night of sleep is possible

55
Q

Zalepon (Sonata)

t1/2 and use

A

~1h

Can take later at night or in the middle of the night

56
Q

Z drug Use

A

Approved for short-term (2 weeks at a time)

Less tolerance/dependence/withdrawal, but still not perfect

57
Q

Melatonin

A

Circadian synthesis, pineal gland
Facilitates sleep induction and maintenance
Ant-oxidant
output decreases with age

58
Q

Ramelteon (Rozerem)

MOA

A

MT1/MT2 receptor agonist

59
Q

Ramelteon (Rozerem)

Indication

A

Sleep induction

60
Q

Ramelteon (Rozerem)

REM

A

No decrease in time spent in REM

61
Q

MT1/MT2 Receptor description and location

A

Gi coupled GPCRs. Hi concentrations in pacemaker regions of hypothalamus

62
Q

Ramelteon (Rozerem)

ADRs

A

HA, Sedation, fategue, N/V

63
Q

Ramelteon (Rozerem)

Onset and Metabolism

A

30 min

Metabolized by CYP1A2 (No induction)

64
Q

Tasimelteon (Hetlioz)

Use

A

Non-24 Sleep-Wake Disorder

70% of Blind Pt

65
Q

Tasimelteon (Hetlioz) Vs Ramelteon (Rozerem)

A

Tasimelteon has higher affinity for M2 subtype, thought to be more important for sleep: but is 30 times more expensive

66
Q

Tasimelteon (Hetlioz)

Metabolism

A

CYP1A2 and CYP3A4

67
Q

Where are orexin synthesizing neurons located?

A

Lateral and posterior hypothalamus

68
Q

What are orexins?

A

Wake promoting peptides which bind to OX1 and OX to receptors (Gs) in the CNS

69
Q

Describe the awake state

A

Limbic/SCN/Energy balance act on orexin neurons which activate wake-active neurons which inhibit Sleep-active neurons/preoptic area (POA).
POA would otherwise be inhibiting wake active and orexin neurons

70
Q

Describe the sleep state

A

No Limbic/SCN/Energy balance to activate orexin neurons:

Pre optic area (POA) inhibits orexin neurons and wake-active neurons

71
Q

Suvorexant (Belsomra)

MOA

A

OX1 and OX2 Receptor antagonist in hypothalamus: Sleep induction

Neorologia (12 decks)

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