Antipsychotics Flashcards
1
Q
what are the criteria for schizophrenia
A
- 2 or more of the following symptoms present for 1 month:
- delusions
- hallucinations
- disorganized speech
- grossly disorganized or catatonic behavior
- negative symptoms (affective blunting, alogia or avolition)
- significant effect major areas of functioning
- continuous signs of disturbance persist for at least 6 months
- symptoms are not due to another psychiatric illness, medical disorder or substance induced
2
Q
what are the 3 categories of symptoms of schizophrenia
A
- psychotic or positive symptoms
- primary negative symptoms
- primary cognitive symptoms
3
Q
what are the positive symptoms of schizophrenia
A
- hallucinations
- illusions
- delusions
- bizarre behavior
- irritability
- aggression
- paranoia
4
Q
what are the negative symptoms of schizophrenia
A
- social isolation
- anhedonia
- affective impairment
- amotivation
- alogia
5
Q
what are the cognitive symptoms of schizophrenia
A
- poor concentration
- memory disturbances
- inability to plan
- difficulty executing tasks
- poor abstraction
- impaired decision making
6
Q
what is the proposed pathophysiologic of schizophrenia
A
dopamine theory
7
Q
what is the function and antipsychotic effect of nigrostriatal (A9) track for FGA
A
- function: EP system- movement
- antipsychotic effect- movement disorders
8
Q
what is the function and antipsychotic effect of mesolimbic (A10) track for FGA
A
- function: arousal, memory, motivation
- antipsychotic effect: relief of psychosis
9
Q
what is the function and antipsychotic effect of mesocortical (A10) track for FGA
A
function: cognition, communication, social function, response to stress
- antipsychotic effect: increase in negative symptoms
10
Q
what is the function and antipsychotic effect of tuberoinfundibular track for FGA
A
- function: regulates prolactin release
- antipsychotic effect: increase prolactin concentrations
11
Q
what are the FDA approved uses for antipsychotics
A
- schizophrenia
- bipolar disorder
- adjunctive therapy in major depressive disorder
- autism spectrum disorder
12
Q
what are the off-label uses for antipychotics
A
- anxiety disorders
- PTSD
- OCD
- psychosis (other than schizophreni)
- acute treatment of aggression and agitation
13
Q
what are the names for first generation antipsychotics (FGA)
A
- typical antipsychotics
- conventional antipsychotics
14
Q
what is the efficacy of FGA
A
limited spectrum of efficacy/activity
- only works for positive symptoms
15
Q
what are the high potencies FGA drugs
A
- fluphenazine
- haloperidol
16
Q
what are the CPZ equivalent and dosage range for fluphenazine
A
- 2mg
- 2-40 mg/day
17
Q
what are the CPZ equivalent and dosage range for haloperidol
A
- 2mg
- 1-100mg/day
18
Q
what are the mid potencies FGA drugs
A
- mesoridazine
- loxapine
- perphenazine
- molindone
- trifluoperazine
- thiothixene
19
Q
what are the CPZ equivalent and dosage range for mesoridazine
A
- 50mg
- 50-500mg/day
20
Q
what are the CPZ equivalent and dosage range for loxapine
A
- 10mg
- 20-250mg/day
21
Q
what are the CPZ equivalent and dosage range for perphenazine
A
-10mg
- 8-64mg/day
22
Q
what are the CPZ equivalent and dosage range for molindone
A
-10mg
- 15-225 mg/day
23
Q
what are the CPZ equivalent and dosage range for trifluoperazine
A
-5mg
- 2-80mg/day
24
Q
what are the CPZ equivalent and dosage range for thiothixene
A
-4mg
- 5-60mg/day
25
what are the low potency FGA drugs
- chlorpromazine
- thioridazine
26
what are the CPZ equivalent and dosage range for chlorpromazine
-100mg
- 60-2000mg/day
27
what are the CPZ equivalent and dosage range for thioridazine
- 100mg
- 50-800 mg/day
28
what are the adverse effects from H1 receptor blockade with FGA drugs
- weight gain
- drowsiness
- dry mouth
29
what are the adverse effects from M1 receptor blockade with FGA drugs
- constipation
- blurred vision
- dry mouth
- drowsiness
30
what are the adverse effects from alpha receptor blockade with FGA drugs
- dizziness
- decreased BP
31
what are the side effects of dopamine antagonism
- extrapyramidal side effects - "movement disorders"
- dystonic reaction
- pseudoparkinsonism
- akathisia
- tardive dyskinesia
- hyperprolactinemia- galactorrhea, menstrual irregularities, amenorrhea, gynecomastia, sexual dysfunction
32
what are the side effects for high potency drugs with each receptor: H1, M1, alpha 1, EPS (D2)
- H1: low
- M1: low
- alpha1: low
- EPS (D2): high
33
what are the side effects for mid potency drugs with each receptor: H1, M1, alpha 1, EPS (D2)
- H1: mid
- M1: mid
- alpha1: mid
- EPS (D2): mid
34
what are the side effects for low potency drugs with each receptor: H1, M1, alpha 1, EPS (D2)
- H1: high
- M1: high
- alpha1: high
- EPS (D2): low
35
what is an acute dystonic reaction
- severe muscle spasm
- eye- oculogyric crisis
- back-retrocollis
- pharyngeal-laryngeal dystonia
- neck- torticollis
- tongue-glossospasms
36
what is the treatment for acute dystonia
acute tx: AC agent (benztropine, diphenhydramine, or benzo)
- chronic treatment: decrease dose, change AP agent, AC agent
37
what are the anticholinergic drugs to treat dystonia
- benztropine (cogentin)
- trihexyphenidyl (artane)
- diphenhydramine (benadryl)
38
what are the 4 cardinal symptoms of EPS- pseudoparkinsonism
- akinesia, bradykinesia or decreased motor activity
- tremor
- cogwheel rigidity
- postural abnormalities
39
what is the treatment for EPS- pseudoparkinsonism
- decrease dose, change AP agent, AC agnets ( cogentin), DA agonist (amantadine)
40
what are the anticholinergic drugs to treat psuedoparkinsonism
- benzotropine (cogentin)
- trihexyphenidyl (artane)
41
what is EPS- akathisia
extreme motor restlessness/inability to sit still
- pt can not typically control akathisia for even a short time period
42
what is the treatment for EPS- akathisia
- decrease dose, change AP agent, beta blocker (propranolol, or a benzodiazepine
43
what is the MOA for propranolol
nonselective beta adrenergic receptor blocking agent
44
what are the side effects for propranolol
- common: dizziness, weakness and fatigue
- no life threatening side effects
- no oral side effects
- overdose- hypotension and bradycardia
- high risk for drug interactions
45
what is EPS- tardive dyskinesia
syndrome characterized by involuntary movements
- buccal-lingual masticatory syndrome
- orofacial movements
- writhing movements of face, neck, back, trunk and extremities
46
what are the drugs approved for tardive dyskinesia and what is MOA
- MOA: vesicular monoamine transporter 2 inhibitor (VMAT2)
- Valbenzine (Ingrezza): oral side effect- dry mouth
- deutetrabenazine (Austedo): oral side effect- dry mouth
47
what are the oral side effects of chlorpromazine (thorazine)
- dry mouth
- hypersalivation (EPS)
- sialorrhea (EPS)
48
what are the oral side effects of haloperidol
- hypersalivatino (EPS)
- sialorrhea (EPS)
49
what are the medications that cause dry mouth of FGA
- benztropine (Cogentin)
- trihexyphenidyl (Artane)
- diphenhydramine (benadryl)
- valbenazine (ingrezza)
- deutetrabenazine (austedo)
50
what are the CV side effects of chlorpromazine and haloperidol and which one is worse
prolonged QTc
- chlorpromazine
51
which drug is worse for weight gain and FGA: chlorpromazine and haloperidol
chlorpromazine
52
what are the advantages and disadvantges of first generation antipsychotics
- advantages: effective for positive symptoms, multiple dosage formulations available, decreased cost
- disadvantages: not effective in 30% of patients, minimal efficacy for negative symptoms, minimal efficacy for cognitive symptoms, high side effect burden (EPS), risk of tardive dyskinesia, nonadherence
53
what is another name of second generation antipsychotics
atypical antipsychotics
54
what is the function and antispychotic effect of the nigrostriatal track with SGA
- function: EP system- movement
- antipsychotic effect: no effect
55
what is the function and antispychotic effect of the mesolimbic track with SGA
- function: arousal, memory, motivation
- antipsychotic effect: relief of psychosis
56
what is the function and antispychotic effect of the mesocortical track with SGA
- function: cognition, communication, social function, response to stress
- antipsychotic effect: relief of negative symptoms
57
what is the function and antispychotic effect of the tuberoinfundibular track with SGA
- function: regulates prolactin release
- antipsychotic effect: no effect
58
what is the brand name and available formulations for clozapine
- brand name: clozaril, fazaclo
- available formulations: tablet, ODT
59
what is the brand name and available formulations for risperidone
- brand name: risperdal; risperdal M tabs; risperdal Consta, Perseris
- available formulations: tablet, ODT, liquid, long-acting injectable
60
what is the brand name and available formulations for olanzapine
- brand name: zyprexa
- available formulations: tablet, ODT, short-acting injectable, long acting injectable
61
what is the brand name and available formulations for quetiapine
- brand name: seroquel
- available formulations: tablet- IR and XR
62
what is the brand name and available formulations for aripiprazole
- brand name: abilify
- available formulations: tablet, ODT, liquid, long acting injectable
63
what is the brand name and available formulations for lurasidone
- brand name: Latuda
- available formulations: tablet
64
clozapine is "yes" for:
- little or no EPS
- efficacy for negative symptoms
- absence of TD
- lack of effect on prolactin levels
- DA/5HT mechanism
- superior efficacy
65
second generation antipsychotics significantly reduced side effect burden (EPS and TD) for:
positive symptoms only
66
what are the indications for clozapine
- treatment of refractory schizophrenia
- lack of efficacy
- intolerable side effects
- decreased risk of recurrent suicidal behavior in schizophrenia and schizoaffective disorder
67
what are the additional considerations for clozapine
- agranulocytosis
- dose related seizure risk
- myocarditis
- oral side effects: dry mouth, sialorrhea, hypersalivation
68
what are the receptor binding affinities for clozapine with H1, alpha 1, and M1
++++
++++
++++
for all
69
what are the metabolic side effects of clozapine
- weight gain: ++++
- risk for diabetes: ++++
- worsening of lipid profiles: ++++
70
what are the indications for risperidone
- schizophrenia: acute treatment adults and adolescents 13-17 years. maintenance treatment
- bipolar disorder: acute manic or mixed episodes- monotherapy or in combination with lithium or VPA. adults and children and adolescents 10-17 years
- autism: treatment of irritability associated with autistic disorder in children and adolescents (ages 5-16 years). symproms of aggression towards others, deliberate self- injuriousness, temper tantrums, and quickly changing moods
71
what are the additional considerations of risperidone
- dose: more than 6mg day- increase of EPS
- increased prolactin- not dose related
- no oral side effects
72
what are the receptor binding affinities for risperidone with H1, alpha 1, and M1
- H1: -
- alpha1: +++
- M1: -
73
what are the metabolic side effects of risperidone
- weight gain: ++
- risk for diabetes: ++
- worsening of lipid profiles: ++
74
what are the indications for olanzapine (zyprexa)
- schizophrenia: acute treatment of adults and adolescents 13-17 years. maintenance and treatment
- bipolar I disorder
- acute manic or mixed episode- monotherapy or combination with lithium or VPA. adults and adolescents 13-17 years. maintenance treatment- monotherapy. depressed episodes - combination product only (symbyax- olanzapine + fluoxetine)
- treatment resistant major depressive disorder- combination product only (symbyaz - olanzapine + fluoxetine)
- defined as nonresponse to 2 separate trials of different antidepressants of adequate dose and duration in the current episode. acute agitation with schizophrenia or bipolar I mania (IM formulation only)
75
what is the oral side effect of olanzapine
dry mouth
76
what are the receptor binding affinities for olanzapine
- H1: ++++
- alpha1: +++
- M1: +++
77
what are the metabolic side effects of olanzapine
- weight gain: +++
- risk for diabetes: +++
- worsening of lipid profiles: +++
78
what are the indications for quetipaine (seroquel and seroquel XR)
- schizophrenia: acute treatment, maintenance treatment
- bipolar I disorder: acute manic of mixed episodes- monotherapy or in combination with lithium or VPA, depression (bipolar I and II disorder) , maintenance. adjunctive treatment of major depressive disorder (inadequate response to antidepressant monotherapy)
79
what is the oral side effect for quetiapine
dry mouth
80
quetiapine is commonly used off label as:
a sedative hypnotic and anxiolytic
81
what are the receptor binding affinities for quetiapine
- H1: +++
- alpha 1: ++
- M1: -
82
what are the metabolic side effects of quetiapine
- weight gain: ++
- risk for diabetes: ++
- worsening of lipid profiles: ++
83
what is the MOA for aripiprazole
- D2 partial agonist
- 5HT2a antagonist
84
what are the indications for aripiprazole
- schizophrenia (adults and adolescents 13-17 years: acute treatment and maintenance treatment
- bipolar disorder I (adults and childre/adolescents 10-17 years): acute manic or mixed episodes- monotherapy or in combination with VPA or lithium. maintenance treatment
- adjuntcive treatment of major depressive disorder (inadequate response to antidepressant monotherapy)
- autism: treatment of irritability associated with autistic disorder in children and adolescents (ages 5-16 years)
- symptoms of aggression towards others, deliberate self-injuriousness, temper tantrums, and quickly changing moods
85
what are the additional considerations with aripiprazole
- akathisia is more common with DA partial agonists
- no oral side effects
86
what are the receptor binding affinities for arirpirazole
- H1: -
- alpha1: -
- M1: -
87
what are the metabolic side effects of aripiprazole
- weight gain: +/-
- risk for diabetes: +/-
- worsening of lipid profiles: +/-
88
what are the indications for lurasidone (Latuda)
- schizophrenia: acute treatment
- depressive episodes associated with bipolar I disorder
89
what are the additional considerations with lurasidone
- must be taken with food (at least 350 kcal)
- no oral side effects
90
what are the receptor binding affinities for lurasidone
- H1: -
- alpha1: -
- M1: -
91
what are the metabolic side effects for lurasidone
- weight gainL +/-
- risk for diabetes: +/-
- worsening of lipid profiles: +/-
92
what drugs cause sialorrhea, hypersalivation
- clozapine (clozaril)
93
what drugs cause dry mouth
- clozapine (clozaril)
- olanzapine (zyprexa)
- quetiapine (seroquel)
94
what drug has the highest risk for CV side effects (SGA)
clozapine
95
what are the advantages and disadvantages of SGAs
- advantages:
- effective for positive symptoms
- may be effective for negative symptoms
- clozapine effective in treatment refractory schizophrenia
- improved side effect profile as compared with FGA
- decreased risk of TD
- decreased incidence of EPS
- minimal o no prolactin elevation (except RIS)
- disadvantages: risk of metabolic side effects
96
second generation antipsychotics with the exception of _________ have become the agents of first choice for the treatment of:
clozapine, olanzapine, and iloperidone
- schizophrenia
97
what is the suggested schizophrenia pharmacotherapy treatment for stage 1A
- treatment naive individual with 1st break schizophrenia
- any antipyschotic monotherapy except clozapine, olanzapine and iloperidone
98
what is the suggested schizophrenia pharmacotherapy treatment for stage 1B
- previously treated with an antipsychotic for schizophrenia, and treatment is being restarted
- any antipsychotic monotherapy except clozapine. an antipsychotic that previously produced poor efficacy or intolerance should not be used
99
what is the suggested schizophrenia pharmacotherapy treatment for stage 2
- patient had inadequate clinical response with antipsychotic used in stage 1A or 1B
- any antipsychotic monotherapy, except clozapine, not used in stage 1A or 1B. may consider clozapine in severely suicidal patient
100
what are the responses to antipsychotic therapy in chronological order
- decreased: agitation, hostility, aggression, combativeness, anxiety. Normalization of sleep and eating patterns
- improvement in socialization/self care habits and mood
- improvement in thought disorder and mood. decrease in delusions, hallucinations. appropriate conversation
- impaired insight and judgement. inappropriate affect. fixed delusions/hallcuinations
101
what are the potentially persistent symptoms
- impaired insight and judgement. inappropriate affect. fixed delusions/hallcuinations
102
expect to see initial improvement in symptoms with treatment within ______ of starting antipsychotic therapy
2 weeks
103
maximum response to starting antipsychotic therapy may take up to:
6-8 weeks
104
