Antipsychotics Flashcards
(171 cards)
1
Q
Define schizophrenia.
A
A mental disorder caused by an inherent dysfunction of the brain that manifests in:
- Delusions.
- Hallucinations (mostly auditory).
- Disturbed thinking and speech patterns.
2
Q
What percentage of the population has schizophrenia?
A
1%
3
Q
Which age group is most likely to develop schizophrenia?
A
Schizophrenia usually affects people during late adolesence or early adulthood.
4
Q
What is the prevalence of schizophrenia by gender?
A
Equal prevalence in men and women.
5
Q
Do genetics play a part in developing schizophrenia?
A
Yes.
6
Q
Which area of the brain is associated with schizophrenia?
A
Schizophrenia is thought to occur as a result of a dysfunction of the mesolimbic and mesocortical dopaminergic neuronal pathways.
7
Q
What are the positive symptoms of schizophrenia?
A
- Hallucinations.
- Bizarre delusions.
- Disorganized thought.
- Perception disturbances.
- Inappropriate emotions.
8
Q
What are the negative symptoms of schizophrenia?
A
- Blunted emotions.
- Anhedonia.
- Lack of feeling.
- Social withdrawal.
- Lacking insight.
- Suicidal ideations.
- Social withdrawal.
- Paucity of speech.
- Diminished affect.
- Loss of drive.
- Impaired personal hygiene.
9
Q
What are the cognitive manifestations of schizophrenia?
A
Disturbance in forming new memories and learning.
10
Q
Which aspect of schizophrenia does the dopamine hypothesis cover?
A
The positive symptoms of schizophrenia.
11
Q
What is the dopamine hypothesis?
A
Hyperactivity of dopamine D2 receptor neurotransmission in the mesocortical neuronal pathway contributes to the positive symptoms of schizophrenia, whereas negative and cognitive symptoms of the disorder can be attributed to the hypofunctionality of dopamine D1 receptor neurotransmission in the prefrontal cortex.
12
Q
How was the dopamine hypothesis created?
A
Repeated administration of stimulants like amphetamines and cocaine (which enhance central dopaminergic neurotransmission) can cause a psychosis that resembles the positive symptoms of schizophrenia.
Low doses of amphetamine can induce a psychotic reaction in schizophrenics in remission.
Stress, a major predisposing factor in schizophrenia, can produce a psychotic state in recovered amphetamine addicts.
13
Q
Is stress a major predisposing factor in schizophrenia?
A
Yes.
14
Q
Which neurotransmitter is thought to cause the negative symptoms of schizophrenia?
A
Serotonin hyperactivity.
15
Q
What other names are given to antipsychotics?
A
Neuroleptics.
Major tranquilizers.
16
Q
Do antipsychotics cure?
A
They do not cure the disease and don’t eliminate the chronic thinking patterns, they just eliminate the schizophrenic symptoms by decreasing dopaminergic and/or serotonergic neurotransmission, thereby decreasing the intensity of hallucinations and delusions.
17
Q
What is the general structure of antipsychotics?
A
Antipsychotics are present as several diverse heterocyclic structures with marked different potencies.
18
Q
How are antipsychotic drugs divided?
A
- First-generation agents.
- Second generation agents.
19
Q
How are first-generation antipsychotics further divided?
A
- Low potency first-generation antipsychotics.
- High potency first-generation antipsychotics.
20
Q
Does the classification of antipsychotics relate to their clinical efficacy?
A
No! Rather, it specifies the affinity for the dopamine D2 receptor, which in turn, may influence the adverse effect profile of antipsychotics.
21
Q
List first-generation antipsychotics (low potency).
A
- Chlorpromazine.
- Prochlorperazine.
- Thioridazine.
22
Q
List first-generation antipsychotics (high potency).
A
- Fluphenazine.
- Haloperidol.
- Pimozide.
- Thiothixene.
23
Q
List second-generation antipsychotics.
A
- Aripiprazole.
- Clozapine.
- Olanzapine.
- Quetiapine.
- Risperidone.
24
Q
What is the mechanism of action of first-generation antipsychotics?
A
Blocking D2 dopamine receptors competitively.
25
What side effect/disorder is most associated with first-generation antipsychotics?
Movement disorders.
26
Which drug is more likely to cause movement disorders, haloperidol or chlorpromazine?
Haloperidol, as it binds tightly to dopaminergic receptors.
27
Are any first-generation antipsychotics clinically more effective than others?
No.
28
What is another term for second-generation antipsychotics?
Atypical antipsychotics.
29
Second-generation antipsychotics have fewer of what kind of symptoms?
Extrapyramidal symptoms (EPS).
30
What type of side effects are higher with second-generation antipsychotics?
Metabolic side effects.
31
Name three metabolic side effects associated with second-generation antipsychotics.
- Diabetes.
- Hypocholesteremia.
- Weight gain.
32
Why are second-generation agents commonly selected over first-generation antipsychotics?
To minimize movement disorders associated with first-generation antipsychotics.
33
What guides drug selection for antipsychotic patients besides minimizing side effects?
- Patient response.
- Comorbid conditions.
34
Should second-generation drugs be considered interchangeable?
No.
35
Why should second-generation drugs not be considered interchangeable?
Different patient responses.
36
How many types of dopamine receptors are there?
Five.
37
Which dopamine receptors excite neurons?
D1, D5.
38
Which dopamine receptors inhibit neurons?
D2, D3, D4.
39
Which type of receptor do neuroleptic drugs bind to in the brain?
Dopamine receptors.
40
What do all 1st generation and most 2nd generation antipsychotics block?
Dopamine receptors.
41
Blocking which dopamine receptors in the mesolimbic system leads to clinical efficacy with antipsychotic drugs usage?
D2 receptors.
42
Which drug is 100 times more potent towards the D2 receptor than chlorpromazine?
Haloperidol.
43
Which atypical antipsychotic has a higher affinity for D4 and lower for D2?
Clozapine.
44
What drugs antagonize the actions of antipsychotic drugs?
- Levodopa.
- Bromocriptine.
- Amphetamines.
45
What type of receptor-blocking activity other than dopamine receptors is involved in the mechanism of action for most 2nd generation antipsychotics?
Serotonin receptors.
46
Which specific serotonin receptors are particularly inhibited by most 2nd generation antipsychotics?
5-HT2A receptors.
47
Which receptors does Clozapine have a high affinity for?
D1, D4, 5-HT2, muscarinic, α-adrenergic.
48
Is Clozapine a strong or weak dopamine D2-receptor antagonist?
Weak.
49
Which receptors does Risperidone primarily block?
5-HT2A > D2.
50
Aripiprazole is a partial agonist at which receptors?
D2, 5-HT1A.
51
Aripiprazole is a blocker of which receptor?
5-HT2A.
52
Which receptors does Quetiapine block?
D2, 5-HT2A.
53
What is the mechanism of action for antipsychotic drugs?
Blockade at dopamine and/or serotonin receptors.
54
What symptoms do antipsychotic drugs reduce?
Hallucinations, delusions.
55
To a lesser extent, what negative symptoms do antipsychotic drugs reduce?
Blunted affect, anhedonia, apathy, impaired attention, cognitive impairment.
56
How long do antipsychotic effects usually take to occur?
Several days to weeks.
57
What are the therapeutic effects of antipsychotic drugs related to?
Secondary changes in the corticostriatal pathway.
58
Which second-generation agent ameliorates negative symptoms of schizophrenia to some extent?
Clozapine.
59
What effect do all antipsychotic drugs have on physical movement and anxiety?
- Calming effect.
- Reduce spontaneous movement.
60
How do antipsychotics compare to CNS depressants like barbiturates in terms of intellectual functioning?
Do not depress as much.
61
What is minimal with antipsychotic use compared to CNS depressants?
Motor coordination difficulties.
62
What are extrapyramidal effects caused by antipsychotics?
Dystonias, Parkinson-like symptoms, akathisia, tardive dyskinesia.
63
What is tardive dyskinesia?
Involuntary movements of the tongue, lips, neck, trunk, and limbs.
64
What probably causes unwanted movement symptoms in antipsychotic use?
Blocking dopamine receptors in the nigrostriatal pathway.
65
Which generation of antipsychotics exhibits a lower incidence of these symptoms?
Second-generation.
66
Which antipsychotic drugs do NOT have antiemetic effects?
Aripiprazole, thioridazine.
67
How do antipsychotics exert antiemetic effects?
Blocking D2 receptors in the chemoreceptor trigger zone.
68
What are common anticholinergic effects of antipsychotics?
Blurred vision, dry mouth, confusion.
69
Which antipsychotic increases salivation instead of causing dry mouth?
Clozapine.
70
What effect do antipsychotics have on gastrointestinal and urinary tract smooth muscle?
Inhibition.
71
What can inhibition of gastrointestinal and urinary tract smooth muscle lead to?
Constipation, urinary retention.
72
Name four antipsychotics with notable anticholinergic effects.
Thioridazine, chlorpromazine, clozapine, olanzapine.
73
What causes orthostatic hypotension and light-headedness in antipsychotic use?
Blockade of alpha receptor.
74
What condition is produced by altering temperature-regulating mechanisms?
Poikilothermia.
75
What causes an increase in prolactin release in antipsychotic use?
Blockade of D2 receptor in the pituitary gland.
76
What effect do antagonists of the histamine receptor have?
Sedation.
77
Name three antipsychotics that act as histamine receptor antagonists causing sedation.
Chlorpromazine, olanzapine, clozapine.
78
What is a common sexual side effect of antipsychotic drugs?
Sexual dysfunction.
79
Do all patients respond to antipsychotic treatment for schizophrenia?
No.
80
Is complete normalization of behavior commonly achieved with antipsychotics?
No.
81
What symptoms do first-generation antipsychotics more effectively alleviate?
Positive symptoms.
82
What symptoms do second-generation antipsychotics more effectively alleviate, although not consistently?
Negative symptoms.
83
For which patients are second-generation antipsychotics particularly useful?
Patients resistant to first-generation.
84
Which antipsychotic is reserved for patients who do not respond to other neuroleptics?
Clozapine.
85
Why is clozapine reserved for certain patients?
Associated with blood dyscrasia.
86
Which antipsychotic is most commonly used for severe drug-induced nausea?
Prochlorperazine.
87
What should be used to treat nausea arising from motion?
Sedatives, antihistamines, anticholinergics.
88
Name an anticholinergic used to treat motion-induced nausea.
Scopolamine.
89
In what combination are antipsychotics used for chronic pain with severe anxiety?
Alongside narcotic analgesics.
90
Which antipsychotic is used to treat intractable hiccups?
Chlorpromazine.
91
What is promethazine used to treat, and why?
Pruritis, antihistamine effect.
92
Which two antipsychotics are used for motor and phonic tics of Tourette disorder?
Pimozide, haloperidol.
93
Which antipsychotics are used for disruptive behavior and irritability secondary to autism?
Risperidone, aripiprazole.
94
How is the absorption of antipsychotics described?
Variable absorption.
95
Can antipsychotics readily pass into the brain?
Yes.
96
What is the volume of distribution for antipsychotics?
Large.
97
What is the duration of action for long-acting injectable (LAI) formulations of antipsychotics?
2 to 4 weeks.
98
For what type of patients are LAI formulations often used?
Noncompliant patients.
99
What are the benefits of LAI formulations of antipsychotics?
Lower extrapyramidal symptoms, little physical dependence.
100
Do adverse effects of antipsychotics occur in all patients?
Yes.
101
In what percentage of patients are adverse effects of antipsychotics significant?
80%.
102
Despite the array of side effects, what is high in antipsychotics?
Therapeutic index.
103
What normally balances the inhibitory effects of dopaminergic neurons?
Excitatory actions of cholinergic neurons.
104
What happens when dopamine receptors are blocked?
Relative excess of cholinergic influence.
105
What results from a relative excess of cholinergic influence?
Extrapyramidal motor effects.
106
What determines the risk of appearance of movement disorders in antipsychotic use?
Time and dose dependency.
107
What is dystonia and how soon can it appear?
Movement disorder with repetitive muscle movements; few hours to days.
108
What is akathisia and how soon can it appear?
Inability to remain seated due to motor restlessness; days to weeks.
109
What are Parkinson-like symptoms and how soon can they appear?
Bradykinesia, rigidity, tremor; weeks to months.
110
What is tardive dyskinesia and how soon can it appear?
Involuntary uncontrolled movements, especially of the mouth, tongue, and trunk; months to years.
111
What is the effect of blocking cholinergic activity on extrapyramidal effects?
Minimizing effect.
112
Which anticholinergic drug can minimize extrapyramidal effects?
Benztropine.
113
Why do clozapine and risperidone have a lower potential for causing extrapyramidal symptoms?
5-HT2A antagonizing effect.
114
Which atypical antipsychotic is used as a first-line treatment?
Risperidone.
115
For which patients is clozapine reserved?
Patients refractory/unresponsive to traditional therapy.
116
What serious side effect is associated with clozapine?
Bone marrow suppression.
117
Why should white blood cell count be monitored in patients taking clozapine?
Risk of agranulocytosis.
118
When does tardive dyskinesia typically occur with neuroleptic drugs?
After long-time treatment.
119
What are the involuntary movements associated with tardive dyskinesia?
Bilateral and facial jaw movements, "fly-catching" motions of the tongue.
120
What effect can a prolonged drug holiday have on tardive dyskinesia symptoms?
Symptoms may diminish in months (reversible toxicity).
121
Is tardive dyskinesia always reversible?
No, it can be irreversible.
122
What is tardive dyskinesia a response to?
Compensatory response to long neuroleptic treatment.
123
What increases in the brain as a compensatory response leading to tardive dyskinesia?
Number of dopamine receptors.
124
What becomes supersensitive in tardive dyskinesia?
Neurons.
125
What results from the overpowered cholinergic input in tardive dyskinesia?
Excess movement.
126
What is the potential severity of antipsychotic malignant syndrome?
Potentially fatal.
127
Name three symptoms of antipsychotic malignant syndrome.
Muscle rigidity, fever, altered mental status.
128
What happens to blood pressure in antipsychotic malignant syndrome?
Unstable blood pressure.
129
What is myoglobinemia and what causes it in antipsychotic malignant syndrome?
Muscle damage releasing myoglobin into the blood.
130
What must be done with the drug in the case of antipsychotic malignant syndrome?
Drug must be discontinued.
131
Name two treatments that may be helpful for antipsychotic malignant syndrome.
Dantrolene, bromocriptine.
132
What effect causes drowsiness with antipsychotic drugs?
Antihistamine effect.
133
Name a cognitive side effect of antipsychotic drugs.
Confusion.
134
What causes dry mouth, urinary retention, constipation, and loss of accommodation with antipsychotic drugs?
Antimuscarinic activity.
135
What causes lowered blood pressure and orthostatic hypotension with antipsychotic drugs?
Alpha adrenergic blockade.
136
Name five reproductive or hormonal side effects of antipsychotic drugs.
Amenorrhea, galactorrhea, gynecomastia, infertility, impotence.
137
What is a common side effect of antipsychotic drugs that can result in noncompliance?
Weight gain.
138
hat metabolic effects can antipsychotic drugs have?
Increased blood glucose (DM) and triglyceride levels.
139
What can acute agitation accompanying withdrawal from alcohol or other drugs be aggravated by?
Antipsychotics.
140
How do antipsychotics affect the seizure threshold?
Lower it.
141
In which patients should antipsychotics be used cautiously?
Patients with seizure disorders.
142
What serious condition is associated with clozapine?
Agranulocytosis.
143
What is recommended for patients with two or more psychotic episodes?
Maintenance therapy for at least 5 years.
144
How do higher doses of antipsychotics affect relapse rates?
Lower relapse.
145
Which generation of antipsychotics is associated with lower relapse rates?
Second-generation.
146
What potential side effects are associated with chlorpromazine?
EPS, weight gain, orthostasis, sedation, anti-muscarinic effects.
147
What is the potential for EPS in oral formulation of fluphenazine?
High potential.
148
What side effects have low potential in fluphenazine's oral formulation?
Weight gain, sedation, orthostasis, anti-muscarinic effects.
149
How often is LAI formulation of fluphenazine administered?
Every 2-3 weeks.
150
What are the side effect potentials for haloperidol?
High potential for EPS; low potential for weight gain, sedation, orthostasis, anti-muscarinic effects.
151
How often is LAI formulation of haloperidol administered?
Every 4 weeks.
152
What potential side effects are associated with aripiprazole?
Low potential for EPS, weight gain, sedation, anti-muscarinic effects.
153
What disorders is aripiprazole approved to treat?
Bipolar disorder, autistic disorder in children, major depression (adjunctive).
154
What potential side effects are associated with asenapine?
Low potential for EPS, weight gain, sedation, orthostasis.
155
What disorder is asenapine approved to treat?
Bipolar disorder.
156
What are the risks associated with clozapine?
Very low potential for EPS, high risk for blood dyscrasias, seizures, myocarditis, sialorrhea, weight gain, anti-muscarinic effects, orthostasis, sedation.
157
What potential side effects are associated with olanzapine?
Low potential for EPS, weight gain, sedation, orthostasis.
158
What disorders is olanzapine approved to treat?
Bipolar disorder.
159
How often is the LAI formulation of olanzapine administered?
Every 2-4 weeks.
160
What potential side effects are associated with paliperidone?
Low to moderate potential for EPS, weight gain, sedation.
161
What disorders is paliperidone approved to treat?
Schizo-affective disorder.
162
How often is the LAI formulation of paliperidone administered?
Every 4 weeks.
163
What potential side effects are associated with quetiapine?
Low potential for EPS, moderate potential for weight gain, orthostasis, sedation.
164
What disorders is quetiapine approved to treat?
Bipolar disorder, major depression (adjunctive).
165
What potential side effects are associated with risperidone?
Low to moderate potential for EPS, weight gain, orthostasis, sedation.
166
What disorders is risperidone approved to treat?
Bipolar disorder, autistic disorder in children.
167
How often is the LAI formulation of risperidone administered?
Every 2 weeks.
168
What potential side effects are associated with ziprasidone?
Low potential for extrapyramidal effects, minimal weight gain.
169
What condition contraindicates the use of ziprasidone?
Cardiac arrhythmias.
170
What is dystonia?
Sustained muscle contractions.
171
What are Parkinson-like symptoms?
Motor restlessness.
