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Antipsychotics Flashcards

antipsychotics - uses and side effects (137 cards)

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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
tardive dyskinesia - define
"Late bad movements" - writhing movements of the face, limbs, or body
26
risk of tardive dyskinesia per year of exposure to SGAs, FGAs
0.5% risk per year exposure to SGAs | 7% risk per year of exposure to FGAs
27
risk of tardive dyskinesia ________ with age
increases dramatically
28
Tardive dyskinesia: treatment
- Reduce antipsychotic dose and duration of treatment - Clozapine - Medications: Valbenazine (Ingrezza) or Deutetrabenazine (Austedo) --> reduce dopamine uptake into presynaptic vesicles
29
Clozapine (Clozaril): Side effects (6)
Severe side effects: - sedation - weight gain - anticholinergic effects - Hypotension (limiting factor during titration) - severe neutropenia - increased seizure risk (2-6%)
30
Antipsychotics differ in ________ and _____________.
Side effects and routes of administration.
31
Summary of CATIE trial:
Schizophrenia patients stayed on olanzapine longer than other agents, but have more weight gain and metabolic problems.
32
List of Mood Stabilizers
Lithium Vanticonvulsants: - Valproic acid (Depakote, Depakene) - Carbamazepine (Tegretol) - Lamotragine (Lamictal) - Oxcarbazepine (Trileptal) - Topiramate (Topamax)
33
Mood stabilizers are primarily effective at treating what?
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.
34
Lithium - highly effective for __________, less effective for ________ and ________.
Preventing mania; depression and psychosis
35
Short-term side effects of lithium
Tremor, nausea, diarrhea, sedation, polydipsia/polyuria
36
Long-term side effects of lithium
Hypothyroidism and renal insufficiency
37
What is the range for lithium levels?
0.7-1.2 mEq/L
38
What does lithium reduce overall?
Reduces suicide risk overall (RR 0.26) | Reduces overall death rate (RR 0.42)
39
What is the preferred mood stabilizer for women of childbearing years?
Lithium. 1.65% adjusted risk ratio (2.4% risk) for Ebstein’s anomaly (a right ventricular outflow tract obstruction defect)
40
Anticonvulsants: highly effective for....?
Preventing mania, somewhat effective for treating mania, rapid cycling, agitation, aggression
41
Common side effects of anticonvulsants:
``` Sedation Ataxia Blurred vision Dyspepsia Dizziness ``` Rare side effects: - bone marrow suppression and aplastic anemia (carbamazepine) - hepatotoxicity (especially valproic acid)
42
Agents for bipolar depression
Lurasidone Olanzapine + fluoxetine Quetiapine Others possible effective:lithium, lamotrigine
43
Names of amphetamines
Adderal | Dexedrine
44
Brand name of methylphenidate?
Ritalin
45
Brand name of modafinil?
Provigil
46
Psychostimulants: name the types
``` Amphetamines (Adderal, Dexedrine) Methylphenidate (Ritalin) Modafinil (Provigil) Pemoline (Cylert) Atomoxetine (Strattera) **nonstimulant attention enhancer ```
47
What do amphetamines, methylphenidate (MPH), and pemoline do?
Enhance dopamine release
48
What is modafinil’s mechanism of action?
May inhibit GABA-mediated neurotransmision
49
What does atomexetine do?
Blocks reputake of norepinephrine
50
Indications for psychostimulants
ADHD Narcolepsy Excessive daytime somnolence
51
Side effects of psychostimulants:
``` Anxiety Insomnia Weight loss Decreased growth rate Abuse/dependency ```
52
Major Neurotransmitters in Psychiatry: Dopamine
Psychosis, muscle control
53
Major Neurotransmitters in Psychiatry: Serotonin
Depression, anxiety, sleep
54
Major Neurotransmitters in Psychiatry: Norepinephrine
Depression, anxiety
55
Major Neurotransmitters in Psychiatry: Acetylcholine (cholinergic)
Memory, movement
56
Major Neurotransmitters in Psychiatry: GABA
Anxiety
57
Major Neurotransmitters in Psychiatry: Histamine
Sleep, appetite
58
All antidepressants are ________ effective against depression.
Equally
59
Antidepressants differ in:
- side effects - efficacy against anxiety - efficacy against obsessive compulsive disorders
60
SSRIs (8)
``` Fluoxetine (Prozac) Sertraline (Zoloft) Paroxetine (Paxil) Fluvoxamine (LuVox) Citalopram (Celexa) Escitalopram (Lexapro) Vilazodon (Viibryd) ** Vortioxetine (Trintellix; formerly ‘Brintellix’)** ``` **5HT1A partial antagonist
61
SSRIs are the most common first-line agents for:
- Major depression, dysthymia - Panic disorder, generalized anxiety, social phobia - OCD - eating disorders
62
SSRI side effects
- 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
SNRIs - list of names (5)
``` Venlafaxine (Effexor) Desvenlafaxine (Pristiq) Duloxetine (Cymbalta) Trazodone (Desiree) Tricyclics antidepressants (TCA) ```
64
Venlafaxine, Desvenlafaxine and Duloxetine - efficacy and side effects
- excellent efficacy for depression, panic, generalized anxiety - may cause insomnia, agitation, or hypertension
65
Trazodone - use and side effects
- highly sedating —> widely used for sleep and agitation in elderly and brain-injured patients - major side effect is hypotension
66
TCAs: Name the four Tertiary Amines
Amitriptyline (Elavil) Clomipramine (Anafranil) Imipramine (Tofranil) Doxepin (Sinequan)
67
TCAs: Name the four Secondary Amines
Amoxapine* (Asendin) Despiramine (Norpramine) Nortriptyline (Pamelor) Protriptyline (Vivactil) *Tetracyclic
68
Which TCA is effective for OCD?
Clomipramine (Anafranil)
69
What do TCAs have excellent efficacy for?
Major depression, generalized anxiety, and panic disorder
70
Side effects of TCAs
``` Hypotension Cardiac effects (qT prolongation) Sexual dysfunction Anticholinergic effects -dry mouth -constipation -urinary hesitancy -blurred vision ```
71
Differences in side effects between secondary and tertiary amines
``` Tertiary amines: More anticholinergic More sedation More hypotension (Secondary amines are fewer/less of these SEs) ```
72
How lethal are TCAs?
Highly lethal in overdose; 1000mg may be <1 wk supply
73
What is Bupropion’s mechanism of action?
Unknown
74
What is Bupropion used for?
Depression (not anxiety, panic, or OCD)
75
What are Bupropion side effects?
- Mildly activating; may interfere w sleep | - lowers seizure threshold
76
What is Bupropion appropriate for?
1st-line use for depression | No sexual dysfunction or cardiac complications
77
Mirtazapine brand name?
Remeron
78
Mirtazapine mechanism of action
Blocks presynaptic alpha2 receptors, causing disinhibition of norepinephrine release
79
What is mirtazapine used for?
Depression, anxiety, and panic disorder
80
Major side effects of mirtazapine
Sedation and weight gain
81
Is mirtazapine safe in overdose?
Yes.
82
Is bupropion safe in overdose?
Yes.
83
MAOIs mechanism of action
Block metabolism of norepinephrine, serotonin, dopamine, and tyramine
84
What are MAOIs used for?
Major depression panic disorder (especially with agoraphobia) generalized anxiety social phobia
85
MAOIs: side effects?
``` Sedation Hypotension Hypertensive crisis Anticholinergic effects Sexual dysfunction ```
86
MAOIs may be more effective than other agents for what?
Atypical depression Panic with agoraphobia Social phobia
87
What do MAOIs require?
Require a low-tyramine diet
88
What does the Selegeline transdermal patch (Ensam) do?
Preferentially inhibits MOA-B, but at antidepressant doses is nonspecific
89
What receptors do MAOI oral agents inhibit?
MAO-A and MAO-B; MAO-A responsible for most side effects
90
Benzodiazepines to know (8)
``` Alprazolam (Xanax) Chlordiazepoxide (Librium) Clonazepam (Klonopin) Diazepam (Valium, Dizac) Flurazepam (Dalmane) Lorazepam (Ativan) Midazolam (Versed) Temazepam (Restoril) ```
91
Alprazolam: class and generic name
Benzodiazepine, Xanax
92
Chlordiazepoxide: brand name and class
Librium, benzodiazepine
93
Diazepam: brand name and class
Valium,Dizac; benzodiazepine
94
Flurazepam: brand name and class
Dalmane; benzodiazpine
95
Lorazepam: brand name and class
Ativan; benzodiazepine
96
Midazolam: brand name and class
Versed; benzodiazepine
97
Temazepam: brand name and class
Restoril; benzodiazepine
98
What is benzodiazepine’s mechanism of action?
Bind a unique site on GABAA receptors (major inhibitory neurotransmitter in CNS; ``bind multiple GABAA receptor subtypes) —> Enhance GABAA inhibitory activity
99
What are benzodiazepines good for?
``` Excellent for: Anxiety Panic attacks Acute agitation Alcohol withdrawal Insomnia ```
100
Side effects of benzodiazepines?
Sedation Dependency Delirium Disinhibition
101
What are benzodiazepines cross-reactive with?
``` Alcohol Choral hydrate Barbiturates Zolpidem Zaleplon ```
102
Advantages of benzodiazepines:
Immediately effective | Safe in overdose (except with alcohol)
103
Disadvantages of benzodiazepines
High abuse potential | Sleep benefit is of limited duration (4-6 weeks)
104
Lorazepam: uptake and clearance time
Intermediate uptake and clearance time (16 hours)
105
Is lorazepam available for IM administration?
Yes.
106
Clonazepam: uptake and clearance time
Intermediate uptake and long clearance time (30 hr)
107
What are the benzodiazepine-like agents? (3)
Zolpidem (Ambien) Zaleplon (Sonata) Eszopiclone (Lunesta)
108
How are benzodiazepine-like agents different from benzodiazepines?
Different chemistry but similar pharmacology - bind only 1 GABAA subtype - poor efficacy for anxiety - low dependency risk because of short half-life
109
Ramelteon: brand name, mechanism of action
Rozerem; Melatonin MT1 & MT2 agonist
110
What is ramelteon’s clearance half-time?
2-5 hours
111
Is ramelteon addictive?
No.
112
What is buspirone’s mechanism of action?
5-HT1A partial agonist
113
Buspirone: generic name
BuSpar
114
What is buspirone used for?
Generalized anxiety | Agitation in elderly and brain-injured patients
115
Advantages of buspirone
Favorable side effect profile Not sedating Safe, even in overdose No abuse potential
116
Disadvantages of buspirone
Questionable effectiveness for anxiety (esp for former benzodiazepine users) Not effective for panic attacks
117
Droperidol: generic name and class
Inapsine; high-potency first-gen antipsychotic
118
Fluphenazine: generic name and class
Prolixin; high-potency first gen antipsychotic
119
Haloperidol: generic name and class
Haldol: high-potency first-gen antipsychotic
120
Perphenazine: generic name and class
Trilafon; high potency first-gen antipsychotic
121
Pimozide: generic name and class
Orap; high potency first-gen antipsychotic
122
Thiothixene
Navane; high potency first-generation antipsychotic
123
Chlorpromazine: generic name and class
Thorazine; low potency first-gen antipsychotic
124
Loxapine: generic name and class
Loxitane; low potency first generation antipsychotic
125
Thioridazine: generic name and class
Mellaril; low potency first-generation antipsychotic
126
Olanzapine: generic name, class
Zyprexa; 2nd gen antipsychotic
127
Quetiapine: generic name, class
Seroquel; second gen antipsychotic
128
Risperidone: generic name and class
Risperdal; second gen antipsychotic
129
Ziprasidone: generic name and class
Geodon; second gen antipsychotic
130
Clozapine: generic name and class
Clozaril; second gen antipsychotic
131
Aripiprazole: generic name and class
Abilify; second gen antipsychotic
132
Asenapine: generic name and class
Saphris; second gen antipsychotic
133
Brexpiprazole: generic name and class
Rexulti; second gen antipsychotic
134
Iloperidone: generic name and class
Fanapt; second gen antipsychotic
135
Lurasidone: generic name and class
Latuda; second gen antipsychotic
136
Paliperidone: generic name and class
Invega; second gen antipsychotic
137
Mental status exam: order
``` Appearance Behavior Speech Mood Affect Thought process Thought content Cognition Insight/judgement ```

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