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Antipsychotics Flashcards

antipsychotics - uses and side effects

1
Q

All antipsychotics have ________ affinity for _______

A

comparable, dopamine D2 receptors

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2
Q

D2 receptor affinity is ______ correlated with antipsychotic efficacy

A

highly

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3
Q

all antipsychotics require _______ of _______ for dopamine receptors for efficacy

A

blockade, ~65%

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4
Q

name three D2 partial agonists

A

aripiprazole, brexpiprazole, and caripraszine

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5
Q

what generation antipsychotics have higher risk of EPS?

A

first generation

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6
Q

first generation antipsychotics have _____ efficacy with atypical agents

A

equal

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7
Q

Name the six high-potency first generation antipsychotics

A 
Droperidol (Inapsine)
Fluphenazine (Prolixin)
Haloperidol (Haldol)
Perphenazine (Trilafon) 
Pimozide (Orap)
Thiothixene (Navane)
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8
Q

Name the three low-potency first generation antipsychotics

A

Chlorpromazine (Thorazine)
Loxapine (Loxitane)
Thioridazine (Mellaril)

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9
Q

First generation high vs low potency antipsychotics

A

High potency -
More EPS
Less sedating
Less anticholinergic

Low potency:
Fewer EPS
More sedating
More anticholinergic

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10
Q

First Generation Antipsychotics: Short-acting Injectable (IM or IV)

A

Haloperidol (Haldol)

Chlorpromazine (Thorazine)

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11
Q

First Generation Antipsychotics: Long-acting Injectable

A 
Haloperidol decanoate (Haldol-D)
Fluphenazine decanoate (Prolixin-D)
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12
Q

Second Generation (Atypical) Antipsychotics - list of eleven

A 
Olanzapine (Zyprexa)
Quetiapine (Seroquel)
Risperidone (Risperdal)
Ziprasidone (Geodon)
Clozapine (Clozaril) -- second-line use only
Aripiprazole (Abilify)
Asenapine (Saphris)
Brexpiprazole (Rexulti)
Iloperidone (Fanapt)
Lurasidone (Latuda)
Paliperidone (Invega)
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13
Q

Second Generation Antipsychotics are first-line agents for: (5 items)

A
  • Psychosis of any type
  • Schizophrenia or schizoaffective disorder
  • Acute mania
  • Depression with psychotic features
  • Behavioral dyscontrol
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14
Q

Second Generation Antipsychotics: Short-acting Injectable formulations (IM only)

A

Olanzapine (Zyprexa)

Ziprasidone (Geodon)

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15
Q

Second Generation Antipsychotics: Long-acting Injectable (LAI)

A 
Risperidone (Risperal Consta; Perseris)
Paliperidone palmitate (Invega Sustenna; Trinza)
Olanzapine pamoate (Relprevv)
Aripiprazole (Abilify Maintena; Aristada)
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16
Q

Antipsychotics: common side effects

A 
Sedation
Akathisia (restlessness)
Movement disorders
Weight gain and other metabolic problems
Sexual dysfunction
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17
Q

What does metabolic dysregulation resulting from antipsychotics look like?

A 
Weight gain
Type 2 diabetes
Elevated LDL cholesterol
Elevated triglycerides
Decreased HDL cholesterol
Diabetic ketoacidosis
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18
Q

Antipsychotics: Relative Risk of Metabolic Complications

A

High:
Clozapine/Olanzapine/Low Potency FGAs

Medium: Quetiapine/Risperidone/Paliperidone/Iloperidone/Asenapine/High Potency FGAs

Low:
Aripiprazole/Brxpiprazole/Lurasidone/Ziprasidone

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19
Q

Antipsychotics - Movement Disorders (3)

A 
Extrapyramidal symptoms (EPS)
- stiff, rigid muscles
- slow movements
- muscle cramps
Akathisia
Tardive Dyskinesia
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20
Q

Antipsychotics - Relative Risk of EPS

A

[Insert graph - High potency FGAs worst, Quetiapine/Iloperidone/Clozapine rare]

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21
Q

All antipsychotics carry ______ .

A

risk

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22
Q

Antipsychotics all-cause mortality relative risk for dementia patients is _____.

A

1.4 - 1.7

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23
Q

Antipsychotics cardiac mortality relative risk is _____ and ______.

A

1.3 - 2.5, dose-dependent

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24
Q

Relative risk of antipsychotics is ________ for younger patients

A

at least as high

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25
Q

tardive dyskinesia - define

A

“Late bad movements” - writhing movements of the face, limbs, or body

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26
Q

risk of tardive dyskinesia per year of exposure to SGAs, FGAs

A

0.5% risk per year exposure to SGAs

7% risk per year of exposure to FGAs

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27
Q

risk of tardive dyskinesia ________ with age

A

increases dramatically

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28
Q

Tardive dyskinesia: treatment

A
  • Reduce antipsychotic dose and duration of treatment
  • Clozapine
  • Medications: Valbenazine (Ingrezza) or Deutetrabenazine (Austedo) –> reduce dopamine uptake into presynaptic vesicles
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29
Q

Clozapine (Clozaril): Side effects (6)

A

Severe side effects:

  • sedation
  • weight gain
  • anticholinergic effects
  • Hypotension (limiting factor during titration)
  • severe neutropenia
  • increased seizure risk (2-6%)
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30
Q

Antipsychotics differ in ________ and _____________.

A

Side effects and routes of administration.

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31
Q

Summary of CATIE trial:

A

Schizophrenia patients stayed on olanzapine longer than other agents, but have more weight gain and metabolic problems.

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32
Q

List of Mood Stabilizers

A

Lithium

Vanticonvulsants:

  • Valproic acid (Depakote, Depakene)
  • Carbamazepine (Tegretol)
  • Lamotragine (Lamictal)
  • Oxcarbazepine (Trileptal)
  • Topiramate (Topamax)
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33
Q

Mood stabilizers are primarily effective at treating what?

A

Primarily effective in treating and preventing manic episodes.

Frequently used for impulsivity, agitation, and aggression in dementia and brain injury patients; augmentation of other agents.

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34
Q

Lithium - highly effective for __________, less effective for ________ and ________.

A

Preventing mania; depression and psychosis

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35
Q

Short-term side effects of lithium

A

Tremor, nausea, diarrhea, sedation, polydipsia/polyuria

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36
Q

Long-term side effects of lithium

A

Hypothyroidism and renal insufficiency

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37
Q

What is the range for lithium levels?

A

0.7-1.2 mEq/L

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38
Q

What does lithium reduce overall?

A

Reduces suicide risk overall (RR 0.26)

Reduces overall death rate (RR 0.42)

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39
Q

What is the preferred mood stabilizer for women of childbearing years?

A

Lithium.

1.65% adjusted risk ratio (2.4% risk) for Ebstein’s anomaly (a right ventricular outflow tract obstruction defect)

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40
Q

Anticonvulsants: highly effective for….?

A

Preventing mania, somewhat effective for treating mania, rapid cycling, agitation, aggression

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41
Q

Common side effects of anticonvulsants:

A 
Sedation
Ataxia
Blurred vision
Dyspepsia
Dizziness

Rare side effects:

  • bone marrow suppression and aplastic anemia (carbamazepine)
  • hepatotoxicity (especially valproic acid)
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42
Q

Agents for bipolar depression

A

Lurasidone
Olanzapine + fluoxetine
Quetiapine
Others possible effective:lithium, lamotrigine

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43
Q

Names of amphetamines

A

Adderal

Dexedrine

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44
Q

Brand name of methylphenidate?

A

Ritalin

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45
Q

Brand name of modafinil?

A

Provigil

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46
Q

Psychostimulants: name the types

A 
Amphetamines (Adderal, Dexedrine)
Methylphenidate (Ritalin)
Modafinil (Provigil)
Pemoline (Cylert)
Atomoxetine (Strattera) **nonstimulant attention enhancer
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47
Q

What do amphetamines, methylphenidate (MPH), and pemoline do?

A

Enhance dopamine release

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48
Q

What is modafinil’s mechanism of action?

A

May inhibit GABA-mediated neurotransmision

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49
Q

What does atomexetine do?

A

Blocks reputake of norepinephrine

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50
Q

Indications for psychostimulants

A

ADHD
Narcolepsy
Excessive daytime somnolence

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51
Q

Side effects of psychostimulants:

A 
Anxiety
Insomnia
Weight loss
Decreased growth rate
Abuse/dependency
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52
Q

Major Neurotransmitters in Psychiatry: Dopamine

A

Psychosis, muscle control

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53
Q

Major Neurotransmitters in Psychiatry: Serotonin

A

Depression, anxiety, sleep

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54
Q

Major Neurotransmitters in Psychiatry: Norepinephrine

A

Depression, anxiety

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55
Q

Major Neurotransmitters in Psychiatry: Acetylcholine (cholinergic)

A

Memory, movement

56
Q

Major Neurotransmitters in Psychiatry: GABA

57
Q

Major Neurotransmitters in Psychiatry: Histamine

A

Sleep, appetite

58
Q

All antidepressants are ________ effective against depression.

59
Q

Antidepressants differ in:

A
  • side effects
  • efficacy against anxiety
  • efficacy against obsessive compulsive disorders
60
Q

SSRIs (8)

A 
Fluoxetine (Prozac)
Sertraline (Zoloft)
Paroxetine (Paxil)
Fluvoxamine (LuVox)
Citalopram (Celexa)
Escitalopram (Lexapro)
Vilazodon (Viibryd) **
Vortioxetine (Trintellix; formerly ‘Brintellix’)**

**5HT1A partial antagonist

61
Q

SSRIs are the most common first-line agents for:

A
  • Major depression, dysthymia
  • Panic disorder, generalized anxiety, social phobia
  • OCD
  • eating disorders
62
Q

SSRI side effects

A
  • dizziness, hypotension
  • nausea, diarrhea
  • Serotonin syndrome — agitation, aka this is, insomnia, anxiety (esp. in the first few days of treatment)
  • weight gain
  • sexual dysfunction
63
Q

SNRIs - list of names (5)

A 
Venlafaxine (Effexor)
Desvenlafaxine (Pristiq)
Duloxetine (Cymbalta)
Trazodone (Desiree)
Tricyclics antidepressants (TCA)
64
Q

Venlafaxine, Desvenlafaxine and Duloxetine - efficacy and side effects

A
  • excellent efficacy for depression, panic, generalized anxiety
  • may cause insomnia, agitation, or hypertension
65
Q

Trazodone - use and side effects

A
  • highly sedating —> widely used for sleep and agitation in elderly and brain-injured patients
  • major side effect is hypotension
66
Q

TCAs: Name the four Tertiary Amines

A

Amitriptyline (Elavil)
Clomipramine (Anafranil)
Imipramine (Tofranil)
Doxepin (Sinequan)

67
Q

TCAs: Name the four Secondary Amines

A

Amoxapine* (Asendin)
Despiramine (Norpramine)
Nortriptyline (Pamelor)
Protriptyline (Vivactil)

*Tetracyclic

68
Q

Which TCA is effective for OCD?

A

Clomipramine (Anafranil)

69
Q

What do TCAs have excellent efficacy for?

A

Major depression, generalized anxiety, and panic disorder

70
Q

Side effects of TCAs

A 
Hypotension
Cardiac effects (qT prolongation)
Sexual dysfunction
Anticholinergic effects
-dry mouth
-constipation
-urinary hesitancy
-blurred vision
71
Q

Differences in side effects between secondary and tertiary amines

A 
Tertiary amines:
More anticholinergic
More sedation
More hypotension 
(Secondary amines are fewer/less of these SEs)
72
Q

How lethal are TCAs?

A

Highly lethal in overdose; 1000mg may be <1 wk supply

73
Q

What is Bupropion’s mechanism of action?

74
Q

What is Bupropion used for?

A

Depression (not anxiety, panic, or OCD)

75
Q

What are Bupropion side effects?

A
  • Mildly activating; may interfere w sleep

- lowers seizure threshold

76
Q

What is Bupropion appropriate for?

A

1st-line use for depression

No sexual dysfunction or cardiac complications

77
Q

Mirtazapine brand name?

78
Q

Mirtazapine mechanism of action

A

Blocks presynaptic alpha2 receptors, causing disinhibition of norepinephrine release

79
Q

What is mirtazapine used for?

A

Depression, anxiety, and panic disorder

80
Q

Major side effects of mirtazapine

A

Sedation and weight gain

81
Q

Is mirtazapine safe in overdose?

82
Q

Is bupropion safe in overdose?

83
Q

MAOIs mechanism of action

A

Block metabolism of norepinephrine, serotonin, dopamine, and tyramine

84
Q

What are MAOIs used for?

A

Major depression
panic disorder (especially with agoraphobia)
generalized anxiety
social phobia

85
Q

MAOIs: side effects?

A 
Sedation
Hypotension
Hypertensive crisis
Anticholinergic effects
Sexual dysfunction
86
Q

MAOIs may be more effective than other agents for what?

A

Atypical depression
Panic with agoraphobia
Social phobia

87
Q

What do MAOIs require?

A

Require a low-tyramine diet

88
Q

What does the Selegeline transdermal patch (Ensam) do?

A

Preferentially inhibits MOA-B, but at antidepressant doses is nonspecific

89
Q

What receptors do MAOI oral agents inhibit?

A

MAO-A and MAO-B; MAO-A responsible for most side effects

90
Q

Benzodiazepines to know (8)

A 
Alprazolam (Xanax)
Chlordiazepoxide (Librium)
Clonazepam (Klonopin)
Diazepam (Valium, Dizac)
Flurazepam (Dalmane)
Lorazepam (Ativan)
Midazolam (Versed)
Temazepam (Restoril)
91
Q

Alprazolam: class and generic name

A

Benzodiazepine, Xanax

92
Q

Chlordiazepoxide: brand name and class

A

Librium, benzodiazepine

93
Q

Diazepam: brand name and class

A

Valium,Dizac; benzodiazepine

94
Q

Flurazepam: brand name and class

A

Dalmane; benzodiazpine

95
Q

Lorazepam: brand name and class

A

Ativan; benzodiazepine

96
Q

Midazolam: brand name and class

A

Versed; benzodiazepine

97
Q

Temazepam: brand name and class

A

Restoril; benzodiazepine

98
Q

What is benzodiazepine’s mechanism of action?

A

Bind a unique site on GABAA receptors (major inhibitory neurotransmitter in CNS; ``bind multiple GABAA receptor subtypes) —> Enhance GABAA inhibitory activity

99
Q

What are benzodiazepines good for?

A 
Excellent for:
Anxiety
Panic attacks
Acute agitation
Alcohol withdrawal
Insomnia
100
Q

Side effects of benzodiazepines?

A

Sedation
Dependency
Delirium
Disinhibition

101
Q

What are benzodiazepines cross-reactive with?

A 
Alcohol
Choral hydrate
Barbiturates
Zolpidem
Zaleplon
102
Q

Advantages of benzodiazepines:

A

Immediately effective

Safe in overdose (except with alcohol)

103
Q

Disadvantages of benzodiazepines

A

High abuse potential

Sleep benefit is of limited duration (4-6 weeks)

104
Q

Lorazepam: uptake and clearance time

A

Intermediate uptake and clearance time (16 hours)

105
Q

Is lorazepam available for IM administration?

106
Q

Clonazepam: uptake and clearance time

A

Intermediate uptake and long clearance time (30 hr)

107
Q

What are the benzodiazepine-like agents? (3)

A

Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)

108
Q

How are benzodiazepine-like agents different from benzodiazepines?

A

Different chemistry but similar pharmacology

  • bind only 1 GABAA subtype
  • poor efficacy for anxiety
  • low dependency risk because of short half-life
109
Q

Ramelteon: brand name, mechanism of action

A

Rozerem; Melatonin MT1 & MT2 agonist

110
Q

What is ramelteon’s clearance half-time?

111
Q

Is ramelteon addictive?

112
Q

What is buspirone’s mechanism of action?

A

5-HT1A partial agonist

113
Q

Buspirone: generic name

114
Q

What is buspirone used for?

A

Generalized anxiety

Agitation in elderly and brain-injured patients

115
Q

Advantages of buspirone

A

Favorable side effect profile
Not sedating
Safe, even in overdose
No abuse potential

116
Q

Disadvantages of buspirone

A

Questionable effectiveness for anxiety (esp for former benzodiazepine users)

Not effective for panic attacks

117
Q

Droperidol: generic name and class

A

Inapsine; high-potency first-gen antipsychotic

118
Q

Fluphenazine: generic name and class

A

Prolixin; high-potency first gen antipsychotic

119
Q

Haloperidol: generic name and class

A

Haldol: high-potency first-gen antipsychotic

120
Q

Perphenazine: generic name and class

A

Trilafon; high potency first-gen antipsychotic

121
Q

Pimozide: generic name and class

A

Orap; high potency first-gen antipsychotic

122
Q

Thiothixene

A

Navane; high potency first-generation antipsychotic

123
Q

Chlorpromazine: generic name and class

A

Thorazine; low potency first-gen antipsychotic

124
Q

Loxapine: generic name and class

A

Loxitane; low potency first generation antipsychotic

125
Q

Thioridazine: generic name and class

A

Mellaril; low potency first-generation antipsychotic

126
Q

Olanzapine: generic name, class

A

Zyprexa; 2nd gen antipsychotic

127
Q

Quetiapine: generic name, class

A

Seroquel; second gen antipsychotic

128
Q

Risperidone: generic name and class

A

Risperdal; second gen antipsychotic

129
Q

Ziprasidone: generic name and class

A

Geodon; second gen antipsychotic

130
Q

Clozapine: generic name and class

A

Clozaril; second gen antipsychotic

131
Q

Aripiprazole: generic name and class

A

Abilify; second gen antipsychotic

132
Q

Asenapine: generic name and class

A

Saphris; second gen antipsychotic

133
Q

Brexpiprazole: generic name and class

A

Rexulti; second gen antipsychotic

134
Q

Iloperidone: generic name and class

A

Fanapt; second gen antipsychotic

135
Q

Lurasidone: generic name and class

A

Latuda; second gen antipsychotic

136
Q

Paliperidone: generic name and class

A

Invega; second gen antipsychotic

137
Q

Mental status exam: order

A 
Appearance
Behavior
Speech
Mood
Affect
Thought process
Thought content
Cognition
Insight/judgement

Jibson Psychopharm (1 decks)

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