sedatives/hypnotics/anxiolytics Flashcards

1
Q

sedative def.

A

calms anxiety, decreases excitement and activity, does not produce drowsiness or impair performance

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2
Q

hypnotic

A

induces sleep, implies restful, refreshing sleep, not “hypnotized”, natural sleep

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3
Q

anxiolytic

A

antianxiety, relieves anxiety without sleep or sedation (not all are sedative)

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4
Q

narcotic

A

actually means “sleep producing”, refers to opiods or illegal drugs

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5
Q

the reticular formation

A

contains dopamine, adrenergic, serotonergic and cholinergic neurons; regulates the sleep-wake cycle

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6
Q

factors that regulate sleep

A

age, sleep history, drug ingestion, circadian rhythms

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7
Q

benzodiazepine chemistry

A

annealating the 1-2 bond with an electron rich ring (triazole or imidazole) yields high affinity and decreased t1/2
no ring = antagonist

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8
Q

long acting benzos

A

accumulation, active metabolites

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9
Q

short acting benzos

A

midazolam, anasthetic

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10
Q

bezodiazepine antagonist

A

flumazenil
no phenyl ring
used to treat benzo overdose
SE: induce convulsions and panic attacks in those that are benzo dependent

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11
Q

Z-hypnotics

A
zolpidem, zaleplon, eszopiclone (long term use)
3A4 to some extent
oversode treatment (flumazenil)
SE: daytime drowsniness, dizziness, ataxia, NV, doing activities in sleep
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12
Q

illicit use of sedative-hypnotics

A

benzos:
flunitrazepam (“roofies”), clonazepam
nonbenzos: zolpidem

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13
Q

barbituates compared to benzos

A

“worse at everything”

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14
Q

benzo and barbituate binding

A

benzos are only allosteric

barbituates are allosteric and orthosteric

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15
Q

GHB

A

not common, used to next day wakefulness

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16
Q

melatonin agonists

A

ramelteon, tasimelteon

preferred over melatonin because FDA approved

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17
Q

buspirone

A

anxiety tx
longer onset of action ~ weeks (dont use for an acute situation)
used for: GAD, social anxiety, comorbid depression, adjunct in OCD, PTSD; not good for panic disorders

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18
Q

propranolol

A

uses: social anxiety, PTSD

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19
Q

tolerance and withdrawl from benzos

A

normal: Cl- moves through
add benzo acutely: more Cl- moves through: hyperpolarized
chronic: downregulation of receptors, return to baseline
withdrawl: not enough Cl- is coming in, neurons being firing

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20
Q

DSM 5 for generalized anxiety

A

Excessive worry around a number of life events that is difficult to control, present for at least 6 months

21
Q

generalized anxiety disorder treatment

A

SSRI (first line) x 2-4 weeks for initial onset of symptom relief, take 6-8 weeks to see full impact (paroxetine and escitalopram are FDA approved; any can be used - lower doses and slower titrations that depression)
SNRIs can be helpful: duloxetine and venlafaxine are FDA approved (useful for concomitant pain syndrome)
Benzodiazepines are used for bridge therapy until other meds kick in; if used longer than 30-60 days, must be tapered to avoid withdrawal (seizures)
Buspirone: dosed high enough (15 TID) and patient is aware of how long it takes to work

22
Q

social anxiety disorder epidemiology

A

Persistent fear about social and/or performance situations in which the patient fears embarrassment or humiliation that is unreasonable; duration at least 6 months

23
Q

Social Anxiety Disorder Treatment

A

SSRI are first line: paroxetine and sertraline are FDA-approved (any can be used)
SNRI: may be useful for failure of SSRI: Venlafaxine is FDA-approved (any can be used)
Beta-blockers: may be useful for non-generalized, performance-related SAD

24
Q

Panic Disorder etiology

A

Recurrent, unexpected panic attacks
Panic Attack: abrupt surge of intense fear or discomfort that reaches a peak in minutes and is accompanied by at least 4 physical and psychological symptoms
May lead to agoraphobia: isolating themselves in a safe place

25
Q

panic disorder treatments

A

SSRIs are first-line maintenance therapy: most are FDA approved
SNRIs: Venlafaxine approved, Duloxetine has good clinical data
TCAs, mirtazapine, MAO-inhibitors: show efficacy similar to SSRIs but have worse side effects
Benzodiazepines should NOT be considered for maintenance therapy unless after several treatment failures (clonazepam and alprazolam FDA approved)

26
Q

OCD

A

Obsessions: recurrent thoughts or images that are intrusive and cause anxiety
Compulsions: repetitive behavior or mental acts performed in response to obsession
Must cause marked distress and take more than 1 hours per day or interfere significantly with functioning

27
Q

OCD treatment

A

SSRIs are first-line treatment for OCD; most are FDA approved
Failure of a few trials of SSRIs, can try clomipramine (TCA)
Venlafaxine XR has been studied with effectiveness
Antipsychotics can be considered for augmentation therapy with antidepressants

28
Q

PTSD

A

Exposure to real or threatened death, serious injury, or sexual violence leading to distressing memories, avoidance of associated stimuli, negative alterations in mood, or marked alterations in reactivity or arousal

29
Q

PTSD treatment

A

SSRIs/SNRIs are first-line treatment - With multiple failed trials, can consider mirtazapine
Prazosin may be helpful for sleep or nightmares (10mg/day)
Benzodiazepines are NOT recommended for PTSD
Substance abuse disorders should be treated simultaneously

30
Q

PTSD prevention

A

Beta-blockers and opioids have been studied in civilian and combat trauma surviviors (give everyone in an IED attack morphine)
Varying degrees of success

31
Q

Selected Drug Therapy Issues in Anxiety Disorders

A

Jitteriness: results from the use SSRIs and SNRIs - Lower doses than depression doses and slower dose titration
Onset of action for SSRIs/SNRIs is 2-4 weeks with maximal response at 6-8 weeks and withdrawl symptoms (flu like symptoms)
Abrupt discontinuation of benzodiazepines can be life-threatening

32
Q

nonpharm anxiety counseling

A

Psychotherapy and cognitive behavioral therapy are mainstays of treatment
Drug therapy often helps the effectiveness of these modalities

33
Q

insomnia

A

Difficulty with sleep initiation, sleep maintenance, and/or early-morning awakening
Takes place at least 3 weeks per night and present for at least 3 months

34
Q

insomnia treatment

A

First line is non-pharmacological! - Behavior therapy: stimulus control, sleep restriction, relaxation, Sleep hygiene principles are necessary
The Z-hypnotics: Zolpidem has several dosage forms, including a sublingual form (Intermezzo), Eszopiclone: FDA-approved for long-term use (6 months)
Benzodiazepines: temazepam is most common, Longer-acting agents (diazepam, chlordiazepoxide) cause significant daytime hangover, Any benzodiazepine can be used for insomnia, Must consider taper to discontinue to avoid life-threatening withdrawal
Melatonin agonists are useful for sleep latency (staying asleep)
Doxepin: lower, branded dose of doxepin = same side effects, suicidality warning, and sleep behavior warning
All medications FDA-approved for sleep have sleep behavior warning

35
Q

Suvorexant (Belsomra)

A

Selective dual orexin receptor antagonist = blocking the wake promoting neuropeptides orexin to suppress “wake drive”
Daytime somnolence risk: 10mg dose carries risk for impaired driving; patients taking 20mg should be warned against daytime driving
Should NOT be used in patients with narcolepsy (absolutely CI, patients already don’t have enough orexin)
3A4 inhibitor

36
Q

sleep apnea

A

Breathing related sleep disorders are divided into obstructive sleep apnea, central sleep apnea, and sleep-related hypoventilation
Patients must have evidence of at least 5 obstructive apneas per hour of sleep confirmed by polysomnography

37
Q

sleep apnea treatment

A

Weight loss
Initially CPAP: continuous positive airway pressure
Excessive daytime sleepiness: modafinil or armodafinil
Surgery is an option
Ensure that obstructive apnea is addressed before recommending sedative/hypnotic drug therapy

38
Q

narcolepsy

A

Cataplexy: emotional response (tearfulness, laughter), losing muscle tone - Sodium oxybate (Xyrem) = Gamma-hydroxy butyrate: Dosed twice nightly, must set alarm to take 2nd dose, Black Box Warning: respiratory depression and misuse risk
Excessive daytime sleepiness: Methylphenidate, dextroamphetamine, mixed amphetamine salts, Modafinil/ amodafinil, Sodium oxybate, Selegiline

39
Q

Shift Work Sleep Disorder

A

Problem for those working night shifts or those with changing shifts throughout the week
Sleep hygiene may be helpful: black-out curtains, noise markers
Drug Therapy: focuses on improving wakefulness during wake time
Modafinil and armodafinil are drugs of choice

40
Q

Restless Leg Syndrome

A

Urge to move the legs in response to an uncomfortable or unpleasant sensation that begins/worsens during periods of rest, partially or completely relieved by movement, worse in the evening/night
Dopamine agonists are first line: pramipexole and ropinirole
Levodopa/carbidopa can be considered
Gabapentin encarbil: unclear benefit/risk
Others: opioids not recommended, iron supplementation has little evidence, and clonazepam may be considered

41
Q

GAD treatment overview

A

SSRI
SNRI
buspirone/benzos

42
Q

SAD treatment overview

A

SSRI
SNRI
BB
phenelzine

43
Q

panic disorder treatment overview

A

SSRI
SNRI
TCAs, MAOIs, Mirtazapine

44
Q

OCD treatment overview

A

SSRI
clomipramine
venlafaxine XR
augment: antipsychotics

45
Q

PTSD treatment overview

A

SSRI/SNRI
mirtazapine
nightmares: prazosin

46
Q

sleep apnea treatment overview

A

weight loss/CPAP

modafinil/armodafinil (daytime sleepiness

47
Q

insomnia treatment overview

A
nonpharm
Z-hypnotics
benzos
melatonin agonists
doxepin
48
Q

narcolepsy treatment ovreview

A

cataplexy: Xyrem

daytime sleepiness: stimulants, modafinil/armodafinil, Xyrem