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69 Cards in this Set
- Front
- Back
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Is chlorpromazine a typical (first generation) or an atypical (second generation) antipsychotic?
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Typical antipsychotic
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Chlorpromazine blocks which receptor? (Be specific!)
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Blocks D2 receptors!
Drug most likely blocks mesocortical D2 receptors |
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Do typical antipsychotics work better for the positive or negative symptoms of schizophrenia?
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They work much better and blocking the positive symptoms of schizophrenia
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What are extrapyramidal effects?
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Adverse effects that result from DA receptor blockade in the basal ganglia.
They cause parkinsonian symptoms of slowness, stiffness, and tremors |
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Which group of antipsychotics tends to have more extrapyramidal effects?
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Antipsychotics with higher affinity for D2 receptors.
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The positive symptoms of schizophrenia are associated with ________ (excessive / diminished) dopamine in the ______ (mesolimbic / mesocortical) system, while the negative symptoms are a result of ______ (excessive / diminished) dopamine in the _________ (mesolimbic / mesocortical) system.
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The positive symptoms of schizophrenia are associated with EXCESSIVE dopamine in the MESOLIMBIC system while the negative symptoms are a result of DIMINISHED dopamine in the MESOCORTICAL system.
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The typical antipsychotics fall into several structural classes. Name the two most prominent classes:
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Butyrophenones and Phenothiazines.
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Chlorpromazine is the prototypical drug in which structural class of antipsychotics?
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Chlorpromazine is a prototypical PHENOTHIAZINE (typical antipsychotic)
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What is the most widely used butyrophenone?
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Haloperidol
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What is meant by on-target and off-target effects of typical antipsychotics?
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On-target refers to antagonist action of D2 dopamine receptors outside the mesolimbic system.
Off-target refers to nonspecific antagonist action at other receptor types. |
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Are extrapyramidal effects considered 'on-target' or 'off-target'?
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On-target since it's a side effect involving D2 receptors
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Which type of drugs could you prescribe to a patient having extrapyramidal side effects?
Which type should you avoid? |
You could use non-dopamine Parkinson's treatments (amantadine / anticholinergic drugs).
You should avoid dopamine and D2 agonists because they can cause schizophrenia. |
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What is the most severe side effect when using typical antipsychotics (according to the text)?
Describe it. |
Neuroleptic malignant syndrome.
This is a rare life-threatening syndrome characterized by catatonia, stupor, fever, and autonomic instability. Leads to death in 10% of cases |
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How long does it take for tardive dysknesia to develop in someone taking typical antipsychotic drugs?
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Takes months to years.
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This side effect is characterized by repetitive, involuntary, stereotyped movements of the face, arms, and trunk.
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Tardive Dyskinesia
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Some adverse effects of typical antipsychotics are thought to be caused by inhibited prolactin secretion. This can lead to several symptoms. Name them:
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In women: amenorrhea, galactorrhea, and false-positive pregnancy.
In men: gyecomastia (large breasts) and decreased libido |
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The typical antipsychotics can cause dry mouth, constipation, difficulty urinating, and loss of accommodation. What do these symptoms have in common?.
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These are all 'off-target' effects caused by antipsychotics antagonizing muscarinic pathways in the periphery.
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The typical antipsychotics can cause orthostatic hypertension, sedation, and failure to ejaculate. What do these symptoms have in common?
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These are all 'off-target' effects caused by antipsychotics antagonizing alpha-adrenergic pathways.
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Name a drug that is a typical antipsychotic available in intramuscular injection and is especially useful for non-compliant patients:
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Haloperidol
Fluphenazine would also work, but we didn't really talk about it. |
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In which disease are dopamine antagonists contra-indicated?
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Parkinson's
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Name five principal atypical antipsychotics:
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Clozapine, olanzapine, quetapine, ziprasidone, and risperidone
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(T/F) Unlike typical antipsychotics, the affinity of atypical antipsychotics does not correlate to their effective dose.
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True
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What is the 5-HT2 hypothesis?
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A theory that the true effect of atypical antipsychotics comes from 5-HT2 receptor antagonist (either instead of, or in addition to D2 antagonist)
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In addition to D2 receptors, what other dopamine receptors are atypical antipsychotics hypothesized to block?
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D4 receptors
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For older typical antipsychotics and most newer atypical antipsychotics, describe the margin between therapeutic levels and where you start seeing side effects?
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Very small margin
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What is the benefit of 5-HT2a antagonism?
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This actually leads to an increase in dopamine release.
Results in mitigation of the adverse D2 affects seen in the nigrostriatal and tuberoinfundibular pathways. It may even help alleviate some of the negative symptoms of schizophrenia |
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What are the most concerning side effects of clozapine?
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Agranulocytosis as well as lowering seizure threshold.
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What is unique about aripiprazole?
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It is a partial D2 agonist. It is proposed that the drug is an antagonist at high dopamine levels, and an agonist at low levels.
Thus it works to alleviate both positive and negative symptoms of schizophrenia |
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(T/F) While aripiprazole has a use in treating schizophrenia, it is of limited use in other psychotic disorders.
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False False False!
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FrontOfCard
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BackOfCard
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Is chlorpromazine a typical or atypical antipsychotic?
|
Typical antipsychotic
|
|
|
Chlorpromazine blocks which receptor? (Be specific!)
|
Blocks D2 receptors!
Drug most likely blocks mesocortical D2 receptors |
|
|
Do typical antipsychotics work better for the positive or negative symptoms of schizophrenia?
|
They work much better and blocking the positive symptoms of schizophrenia
|
|
|
What are extrapyramidal effects?
|
Adverse effects that result from DA receptor blockade in the basal ganglia.
They cause parkinsonian symptoms of slowness, stiffness, and tremors |
|
|
Which group of antipsychotics tends to have more extrapyramidal effects?
|
Antipsychotics with higher affinity for D2 receptors.
|
|
|
The positive symptoms of schizophrenia are associated with ________ (excessive / diminished) dopamine in the ______ (mesolimbic / mesocortical) system, while the negative symptoms are a result of ______ (excessive / diminished) dopamine in the _________ (mesolimbic / mesocortical) system.
|
The positive symptoms of schizophrenia are associated with EXCESSIVE dopamine in the MESOLIMBIC system while the negative symptoms are a result of DIMINISHED dopamine in the MESOCORTICAL system.
|
|
|
The typical antipsychotics fall into several structural classes. Name the two most prominent classes:
|
Butyrophenones and Phenothiazines.
|
|
|
Chlorpromazine is the prototypical drug in which structural class of antipsychotics?
|
Chlorpromazine is a prototypical PHENOTHIAZINE (typical antipsychotic)
|
|
|
What is the most widely used butyrophenone?
|
Haloperidol
|
|
|
What is meant by on-target and off-target effects of typical antipsychotics?
|
On-target refers to antagonist action of D2 dopamine receptors outside the mesolimbic system.
Off-target refers to nonspecific antagonist action at other receptor types. |
|
|
Are extrapyramidal effects considered 'on-target' or 'off-target'?
|
On-target since it's a side effect involving D2 receptors
|
|
|
Which type of drugs could you prescribe to a patient having extrapyramidal side effects?
Which type should you avoid? |
You could use non-dopamine Parkinson's treatments (amantadine / anticholinergic drugs).
You should avoid dopamine and D2 agonists because they can cause schizophrenia. |
|
|
What is the most severe side effect when using typical antipsychotics (according to the text)?
Describe it. |
Neuroleptic malignant syndrome.
This is a rare life-threatening syndrome characterized by catatonia, stupor, fever, and autonomic instability. Leads to death in 10% of cases |
|
|
How long does it take for tardive dysknesia to develop in someone taking typical antipsychotic drugs?
|
Takes months to years.
|
|
|
This side effect is characterized by repetitive, involuntary, stereotyped movements of the face, arms, and trunk.
|
Tardive Dyskinesia
|
|
|
Some adverse effects of typical antipsychotics are thought to be caused by inhibited prolactin secretion. This can lead to several symptoms. Name them:
|
In women: amenorrhea, galactorrhea, and false-positive pregnancy.
In men: gyecomastia (large breasts) and decreased libido |
|
|
The typical antipsychotics can cause dry mouth, constipation, difficulty urinating, and loss of accommodation. What do these symptoms have in common?.
|
These are all 'off-target' effects caused by antipsychotics antagonizing muscarinic pathways in the periphery.
|
|
|
The typical antipsychotics can cause orthostatic hypertension, sedation, and failure to ejaculate. What do these symptoms have in common?
|
These are all 'off-target' effects caused by antipsychotics antagonizing alpha-adrenergic pathways.
|
|
|
Name a drug that is a typical antipsychotic available in intramuscular injection and is especially useful for non-compliant patients:
|
Haloperidol
Fluphenazine would also work, but we didn't really talk about it. |
|
|
In which disease are dopamine antagonists contra-indicated?
|
Parkinson's
|
|
|
Name five principal atypical antipsychotics:
|
Clozapine, olanzapine, quetapine, ziprasidone, and risperidone
|
|
|
(T/F) Unlike typical antipsychotics, the affinity of atypical antipsychotics does not correlate to their effective dose.
|
True
|
|
|
What is the 5-HT2 hypothesis?
|
A theory that the true effect of atypical antipsychotics comes from 5-HT2 receptor antagonist (either instead of, or in addition to D2 antagonist)
|
|
|
In addition to D2 receptors, what other dopamine receptors are atypical antipsychotics hypothesized to block?
|
D4 receptors
|
|
|
For older typical antipsychotics and most newer atypical antipsychotics, describe the margin between therapeutic levels and where you start seeing side effects?
|
Very small margin
|
|
|
What is the benefit of 5-HT2a antagonism?
|
This actually leads to an increase in dopamine release.
Results in mitigation of the adverse D2 affects seen in the nigrostriatal and tuberoinfundibular pathways. It may even help alleviate some of the negative symptoms of schizophrenia |
|
|
What are the most concerning side effects of clozapine?
|
Agranulocytosis as well as lowering seizure threshold.
|
|
|
What is unique about aripiprazole?
|
It is a partial D2 agonist. It is proposed that the drug is an antagonist at high dopamine levels, and an agonist at low levels.
Thus it works to alleviate both positive and negative symptoms of schizophrenia |
|
|
(T/F) While aripiprazole has a use in treating schizophrenia, it is of limited use in other psychotic disorders.
|
False False False!
|
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What are the side effects that we should know from the antipsychotics in general? (8)
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EPS
Tardive dyskenesia NMS Prolactin elevation Weight gain Anticholinergic symptoms Sedation agranulocytosis / seizures (clozapine only) |
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Do first generation (typical) or second generation antipsychotics cause more EPS?
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First generation
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What does akathisia mean?
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Feeling unable to relax, impulsive feelings and behaviors, fidgety
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How does the risk of tardive dyskinesia compare between typical and atypical antipsychotics?
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Atypical antipsychotics carry a much lower risk
This is a good reason to use them! |
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How does the risk of weight gain compare between first generation and second generation antipsychotics?
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First generation < Second generation
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What causes the endocrine problems seen in second generation antipsychotics?
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D2 blockade related hyperprolactinemia
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Which drug requires regular CBC monitoring, and why?
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Clozapine
The drug is notorious for hematologic toxicity (leukopenia, leukocytosis, thrombocytopenia, neutropenia, agranulocytosis) |
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The increased risk of death in elderly patients receiving treatment for dementia related psychosis caused which drug class to be black-boxed? What did these drugs cause specifically?
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Atypical (second generation) antipsychotics
These drugs caused respiratory depression (clozapine) and problems with thermoregulation Note - Patients on these drugs should be warned to stay out of the heat. |
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Which enzyme (or class of enzymes) are responsible for the drug interactions seen in antipsychotics?
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P450 isozymes
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Concerning pregnancy, which class do most antipsychotics fall into?
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Category C
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