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pharmacology > anxiety/insomnia drugs > Flashcards

anxiety/insomnia drugs Flashcards

1
Q

Generalized Anxiety Disorder:

A

6 months or more of excessive worry or anxiety, generally with an unidentified cause.

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2
Q

panic disorder

A

periods of sudden, intense fear or terror and feelings of impending doom.

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3
Q

social anxiety disorder

A

persistent fear and anxiety in social or performance situations that are recognized as excessive or unreasonable. These situations are either avoided or endured with intense anxiety.

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4
Q

agoraphobia

A

intense fear in at least 2 settings (public transportation, open spaces, closed spaces, standing in line, being in a crowd, being outside the home alone)

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5
Q

PTSD

A

follows a traumatic event, characterized by increased arousal and avoidance of stimuli that approximate the original traumatic event

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6
Q

OCD

A

Obsessive or intrusive thoughts that cannot be controlled and are repetitive. (e.g., washing hands, combing hair, cleaning house)

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7
Q

3 groups of Pharmacotherapeutic Options for 
Anxiety & Related Disorders

A
  1. benzodiazepines
  2. non-benzos: anti-depressants, buspirone
  3. MISC: BBs, MAOIs, antihistamines, barbituates, antipyschotics
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8
Q

sedative vs hypnotic drugs

A

sedative: anxiolytic (calming) effect but ideally don’t produce sleep (no CNS depression)
hypnotic: low doses = encourage drowsiness- onset and maintenance of sleep. CNS depression

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9
Q

Most sedatives will first cause _____

Then, at higher doses, produce ______

A

sedation

hypnosis

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10
Q

what are the benzodiazepine drugs?

A

all end in “pam” or “lam”

include xanax, versed, valium, klonopin, etc.

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11
Q

benzos are schedule __ substances

A

schedule IV- hold potential for addiction and OD (MUST give naloxone when prescribing this)

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12
Q

5 properties shared by benzos (to varying degrees)

A 
Anxiolytic
Hypnotic
Muscle relaxation
Anticonvulsant
Amnesic actions ( agent: versed)
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13
Q

what does binding of GABA to GABAa receptor cause?

A

increase CL- through the channel = hyperpolarization =makes it harder to cell to depolarize = reduces neuronal excitability (calming effect)
(inhibitory in action)

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14
Q

what is the MOA of benzos ?

A

increase Cl- flow through channel by binding alpha and gamma GABA subunits = reduce neuronal excitability

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15
Q

what is the distribution of benzo drugs?

A

large distribution b/c they are lipophilic

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16
Q

effect of individual benzo agents depends on what 4 factors?

A
  1. receptor affinity
  2. lipid solubility
  3. metabolism
  4. half-life
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17
Q

what is the significance of receptor affinity for benzo agents?

A

high potency = higher GABAa affinity = more intense withdrawal symptoms
(alprazolam, lorazepam)

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18
Q

what is the significance of lipid solubility for benzo agents?

A

higher lipophilic = more rapid onset and may wear off quicker
(midazolam)
lower lipophilic = more sustained effect
(clonazepam)

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19
Q

what is the significance of metabolism for benzo agents? what are the three types ?

A
  1. oxidative metabolism (majority)
  2. have active metabolites that extend DOA
  3. glucoronidation (LOT: lorazepam, oxazepam, temazepam)
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20
Q

why are the LOT agents safer benzos for elderly to use?

A

they undergo glucoronidation (not converted to active metabolites- excreted unchanged in urine) = less likely to accumulate to toxic levels

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21
Q

what is the significance of half life for benzo agents?

A

Extended in hepatic and renal dysfunction and the elderly

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22
Q

two agents with low potency and short half life (<12 hrs) ?

A

xanax (alprazolam) and versed (midazolam)

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23
Q

two agents with intermediate halfe like and potency?

A

klonapin (clonazepam) and ativan (lorazepam)

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24
Q

what agent has long half life (>40hrs ) and high potency?

A

valium (diazepam )

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25
Q

short half life/ low potency vs long half life/high potency (kinda weeds)

A

Short half-life/high potency (for acute management)

  • Rapid acting agents for quick relief of symptoms
  • Tolerance develops quickly
  • Withdrawal problems common
  • Interdose breakthrough symptoms occur

Long half-life/low potency: “hangover” effect in morning
Accumulate in older adults

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26
Q

what are the short acting benzos? (4)

A 
Short Acting:  “ATOM”
Alprazolam
Triazolam
Oxazepam
Midazolam
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27
Q

what are the intermediate acting benzos (3) ?

A

Intermediate Acting: “TLC”
Temazepam
Lorazepam
Clonazepam

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28
Q

what are the long acting benzos (4)?

A 
Long Acting: “CDeF”
Clorazepate
Chlordiazepoxide
Diazepam
Flurazepam
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29
Q

with increased doses, benzos can cause what ADRs?

A
  • drowsy/lethargy
  • Impaired motor coordination, dizziness, vertigo, slurred speech, blurry vision, mood swings, euphoria, hostile or erratic behavior
  • respiratory depression
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30
Q

Benzos with longer 1/2 life have what major concern?

A

accumulation =delayed symptoms of over-medication.

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31
Q

respiratory depression from Benzos are ____-dependent, exacerbated when administered with ____, _____ or _____?

A

Dose dependent, exacerbated when administered with opioids, alcohol or given to patients with COPD

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32
Q

how can you avoid residual daytime sedation with benzos? how to avoid rebound insomnia?

A

daytime sedation- use lowest effective dose

rebound insomnia- when discontinuing, taper

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33
Q

what is anterograde amnesia? what can cause it?

A

benzos: impaired memory and recall

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34
Q

3 cautions for using benzos in elderly

A

Memory problems
Increase the risk of falls
Drug accumulation (particularly those with long ½ lives)

35
Q

what drugs have tolerance and dependence cautions?

A

benzos

36
Q

abuse potential of benzos is low in patients using it for what? why?

A

Abuse potential is low in patients with true generalized anxiety disorder
Patients usually do not escalate dose because tolerance to the anxiolytic action is not prominent

37
Q

what is the OD antidote for Benzos?

A

Flumazenil : Competitively inhibits the activity at the benzodiazepine receptor site on the GABAA receptor complex.

38
Q

onset and DOA of flumazenil

A

Onset: 1-2 minutes, DOA: 60 minutes ( may have to repeat dose. shorter 1/2 like than benzo (benzo can outlast the antidote)

39
Q

what drug class is effective for several anxiety disorders & agents of choice for long-term treatment of anxiety?

A

SSRIs

40
Q

what drug class have preventive efficacy for panic disorder and anxiolytic activity?

A

TCAs

41
Q

what must you look out for when starting someone on an anti-depressant? (SSRI, TCA, effexor, cymbalta)?

A

may initially cause worsening anxiety - full benefit takes weeks (just like when txting depression)

42
Q

anti-depressants for anxiety use:
_______ approved for the treatment of generalized anxiety and social anxiety disorder
______approved for generalized anxiety disorder

A

effexor

cymbalta

43
Q

MOA of buspirone

A

MOA: 5-HT1A (serotonin) & dopamine receptors agonist

Upon activation, 5-HT1A receptors inhibit firing of 5-HT neurons

44
Q

what is the main drawback of buspirone (buspar)?

A

long onset of axn (3-4weeks): don’t use for acute anxiety!

45
Q

what can you as “bridge-therapy” when putting someone on buspirone (buspar) ?

A

short-term benzos

46
Q

how can beta-blockers be used for anxiety?

A

-block the peripheral symptoms of panic disorder or performance anxiety (e.g., propranolol for public speaking)

47
Q

how can MAOIs be used for anxiety?

A
  • panic disorder when the patient also has atypical depression.
  • *not commonly used because of serious ADRs
48
Q

how can anti-histamines be used for anxiety? what are the two agents?

A

Those with sedating properties can reduce anxiety and often tried in patients with substance abuse issues
Hydroxyzine (Atarax & Vistaril)
Diphenhydramine (Benadryl)

49
Q

what is a narrow-therapeutic drug with no ceiling that is RARELY used for anxiety?

A

barbituates

50
Q

generalized anxiety disorder: what are your 3 drug txt options ?

A
  1. 1st line: antidepressants: SSRIs, SNRIs
  2. acute episode or bridge therapy: benzos
  3. when you can’t use benzos: buspirone
    * USE ALL THREE with cognitive behavior therapy
51
Q

panic disorder: what are your 2 drug txt options

A
  1. 1st line: anti-depressants: SSRI
  2. high-potency Benzos (alprazolam, lorazepam)
    * BOTH with cognitive behavior therapy
52
Q

OCD: drug txt options

A

SSRIs and clomipramine (Anafranil)

*BOTH in high doses with cognitive behavioral therapy

53
Q

PTSD: drug txt options

A

1st line: SSRI

- then txt specific symptoms:

54
Q

txting specific symptoms of PTSD: explosive behavior, nightmares, aggression/anger/depression, pyschotic

A

explosive: BBs
nightmares: prazosin
aggression/anger/depression: valproic acid, carbamazepine, lamotrigine, topiramate
Psychotic symptoms – olanzapine, quetiapine, risperidone

55
Q

txting social anxiety disorder: 2 drugs, how long do you wait for full effect?

A

SSRI &SNRI

- takes 12 weeks for response

56
Q

how do you treat specific phobias?

A

Not treated with medications

- Systematic desensitization and other behavioral approaches often effective

57
Q

serotonin is converted into _______ in the _________ ______during sleep

A

melatonin in pineal gland

58
Q

The _______ ________ _______ maintains wakefulness, and when activity declines, sleep occurs.

A

reticular activating system

59
Q

what are the 5 NTs involved in sleep? which for dreaming? which for non-dreaming sleep?

A

NE, 5-HT, acetylcholine, histamine, and neuropeptides

NE is involved in dreaming, and 5-HT is active during non-dreaming sleep

60
Q

do you want to impact the sleep cycle with meds?

A

NO!- just want to induce or keep them asleep

61
Q

what are the stages in the sleep cycle?

A 
Wakefulness
Non-REM sleep
Stage 1
Stage 2
Stages 3 &amp; 4 (delta sleep)
REM sleep
62
Q

what are the 3 types of insomnia?

A

Transient
Short term
Chronic

63
Q

transient insomnia : define and txt

A

most associated with acute stressors, resolves when stressors removed.
Pharmacotherapy may be used for a few days until situations resolves

64
Q

short term insomnia : define and txt

A

associated with acute stressor, but it is of an ongoing nature.
Recommend avoiding stimulants (caffeine), pharmacotherapy for 7-10 days

65
Q

chronic insomnia

A

cause can be underlying medical or psychiatric cause, or behavioral problem

66
Q

what kind of agents do you want if you have problems initiating sleep? what about maintaining sleep?

A

PROBLEMS STARTING SLEEP- AGENT WITH QUICK ONSET AND SHORT DOA
PROBLEMS MAINTAINING SLEEP - LONGER DOA ( onset doesn’t matter as much)

67
Q

insomnia: which benzo agent is short acting?

A

triazolam

68
Q

insomnia: which benzo is long-acting?

A

flurazepam and quazepam

69
Q

what are the 3 non-benzos for insomnia? which can be used for sleep onset, maintenance and chronic therapy?

A

Zolpidem (Ambien)- onset and maintenance
Zaleplon (Sonata)- onset
Eszopiclone (Lunesta)- onset, maintanance and chronic therapy

70
Q

what is the melatonin receptor 1&2 agonist for insomnia?

A

Ramelteon (Rozerem)- for chronic

71
Q

tricyclic antidepressant for insomnia

A

Doxepin (Silenor)- for maintenance

*“hangover” effect next morning

72
Q

orexin receptor antagonist for insomnia

A

Suvorexant (Belsomra)- for maintenance

block orexin that normally promotes wakefulness

73
Q

non-benzo MOA for insomnia? which receptor does it bind to? which does it NOT bind to?

A

Selectively bind to benzodiazepine receptor 1 (BZ1) enhancing the activity of GABA = decr. neuron excitability = sedation
* NO BZ2 receptor activity
Minimal anxiolytic, muscle relaxation and anticonvulsant properties

74
Q

why are non-benzo agents replacing Benzos for insomnia txt?

A

Preferred because they don’t affect sleep architecture, just decrease sleep latency
Have less adverse effects compared to older agents
- HA, dizziness, daytime somnolence, GI complaints

75
Q

what drug Can be effective, helpful in managing insomnia associated with SSRI?

A

trazodone

76
Q

what 4 drugs may CAUSE insomnia?

A

SSRIs / SNRIs
stimulants (methylphenidate)
glucocorticoids
opiods (w. chronic use)

77
Q

what delays abs. of non-benzo sleep aids?

A

food

78
Q

for what patients is the 1/2 life extended for non-benzo sleep aids ?

A

renal and liver disease

79
Q

which non-benzo may have a hangover effect?

A

lunesta b/c of the very long DOA

80
Q

what is the boxed warning for non-benzo sleep aids?

A

increase risky behavior that can lead to death. patients may not remember driving, eating, sex, etc.

81
Q

what is the difference for men and women in terms of taking non-benzo sleep aids?

A

women have a lower max dose allowed

82
Q

what patient population must you warn about OTC diphenhydramine for sleep? why?

A

Use caution in elderly patients because anticholinergic action can worsen dementia or other medical conditions

83
Q

Which adverse effect of zolpidem carries the greatest potential for harm?

A

Abnormal behaviors while asleep

pharmacology (24 decks)

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