Antipsychotics Indications and Uses
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Questions and Answers

What is the typical time frame required to achieve a significant antipsychotic effect of atypical antipsychotics?

  • At least four weeks
  • At least one week
  • At least two weeks (correct)
  • At least three weeks
  • What is a characteristic of clozapine in terms of treatment-resistant psychosis?

  • It is not approved for treatment-resistant psychosis
  • It is the only atypical agent with proven efficacy in treatment-resistant psychosis (correct)
  • It is less effective than typical antipsychotics in treatment-resistant psychosis
  • It is the only atypical agent not effective in treatment-resistant psychosis
  • Which of the following symptoms is an indication for a trial of an atypical antipsychotic agent?

  • Anhedonia
  • Tardive dyskinesia
  • Negative symptoms such as affective flattening (correct)
  • Positive symptoms such as hallucinations
  • Which atypical antipsychotic agent is associated with agranulocytosis?

    <p>Clozapine</p> Signup and view all the answers

    What is a characteristic of atypical antipsychotic agents in terms of bipolar disorder?

    <p>They are approved for the treatment of acute mania</p> Signup and view all the answers

    What is the advantage of atypical antipsychotic agents over typical antipsychotics in terms of negative symptoms?

    <p>They are more effective in the treatment of negative symptoms</p> Signup and view all the answers

    What is a characteristic of clozapine in terms of tardive dyskinesia?

    <p>It is not associated with tardive dyskinesia</p> Signup and view all the answers

    What is the advantage of atypical antipsychotic agents over typical antipsychotics in terms of long-term outcome?

    <p>They have a superior long-term outcome to typical antipsychotics</p> Signup and view all the answers

    What is recommended in patients with a cardiac history when using antipsychotics?

    <p>Use high-potency agents or atypicals to avoid conduction abnormalities</p> Signup and view all the answers

    Which of the following is a contraindication for clozapine?

    <p>Hematologic disorder</p> Signup and view all the answers

    In patients with Parkinson's disease, which type of antipsychotics is preferred?

    <p>Atypical antipsychotics with low EPS</p> Signup and view all the answers

    What is the recommendation for patients with a seizure history?

    <p>Use atypical antipsychotics with a low risk of seizures</p> Signup and view all the answers

    What is the risk associated with the use of typical antipsychotics in pregnancy?

    <p>A slight increase in the risk of anomalies</p> Signup and view all the answers

    What is the recommendation for patients with prostatic hypertrophy?

    <p>Avoid using antipsychotics with high anticholinergic activity</p> Signup and view all the answers

    What are antipsychotic agents primarily used for?

    <p>Treating mood disorders with psychotic symptoms</p> Signup and view all the answers

    What is the primary difference between typical and atypical antipsychotics?

    <p>Their receptor-binding profiles with dopamine and serotonin receptors</p> Signup and view all the answers

    Which of the following dopamine receptors is most closely related to the efficacy of typical antipsychotic agents?

    <p>D2 receptor</p> Signup and view all the answers

    What is the classification of antipsychotic agents based on their level of dopamine receptor antagonism?

    <p>High, moderate, and low potency</p> Signup and view all the answers

    What is the role of dopamine receptors in the brain?

    <p>Modulating motor functions, motivation, sensation, and drive, as well as cognition</p> Signup and view all the answers

    What is the characteristic of high-potency antipsychotic agents?

    <p>They are effective at relatively lower doses</p> Signup and view all the answers

    What is the characteristic of low-potency antipsychotic agents?

    <p>They require larger doses to elicit an antipsychotic effect</p> Signup and view all the answers

    What is the number of genes coding for different dopamine receptor subtypes?

    <p>5</p> Signup and view all the answers

    What is the primary characteristic that distinguishes atypical antipsychotic agents from typical agents?

    <p>Prominent antagonism at the serotonin receptor in addition to D2 blockade</p> Signup and view all the answers

    Which of the following is thought to be a site of antipsychotic action?

    <p>Mesolimbic dopamine pathway</p> Signup and view all the answers

    What is the typical ratio of antipsychotic excretion via the hepatic circulation and kidneys?

    <p>50% hepatic, 50% renal</p> Signup and view all the answers

    What is the reason for the reduced incidence of extrapyramidal side effects with atypical antipsychotic agents?

    <p>Greater selectivity for the mesolimbic dopamine pathway</p> Signup and view all the answers

    When switching from a typical to an atypical antipsychotic agent, what is the recommended approach?

    <p>Taper the typical agent while introducing the atypical agent</p> Signup and view all the answers

    What is the typical time frame for establishing plasma levels of antipsychotic agents after oral administration?

    <p>2-4 hours</p> Signup and view all the answers

    Which of the following is a characteristic of antipsychotic agents?

    <p>Highly lipophilic</p> Signup and view all the answers

    What is the primary consideration when choosing an antipsychotic agent for a patient?

    <p>Past history of neuroleptic response and side effects</p> Signup and view all the answers

    What is the primary characteristic of Tardive Dyskinesia?

    <p>Involuntary, irregular movements</p> Signup and view all the answers

    What is the risk of developing Tardive Dyskinesia for each year of typical antipsychotic treatment?

    <p>1% per year</p> Signup and view all the answers

    What is the recommended treatment for Tardive Dyskinesia?

    <p>Reduce or stop antipsychotic if possible</p> Signup and view all the answers

    What is Neuroleptic Malignant Syndrome (NMS) characterized by?

    <p>Elevated temperature, autonomic instability, and delirium</p> Signup and view all the answers

    What is a risk factor for Neuroleptic Malignant Syndrome?

    <p>Dehydration</p> Signup and view all the answers

    What is a metabolic side effect of atypical antipsychotics?

    <p>Type II diabetes and hyperlipidemia</p> Signup and view all the answers

    What should be measured and monitored periodically in patients taking atypical antipsychotics?

    <p>Weight, waist circumference, blood pressure, and fasting glucose and lipids</p> Signup and view all the answers

    What should be done if diabetes or hyperlipidemia develop in patients taking atypical antipsychotics?

    <p>Switch to an atypical agent associated with less weight gain and diabetes</p> Signup and view all the answers

    Study Notes

    Indications for Antipsychotics

    • Schizophrenia and bipolar disorder
    • Schizoaffective disorder, mood disorders with psychotic symptoms, and brief psychotic disorder
    • Dementia or delirium when psychotic symptoms are present
    • Substance-induced psychotic disorders and in psychotic symptoms associated with certain personality disorders (borderline)

    Pharmacology

    • Typical and atypical antipsychotics are distinguished by their unique receptor-binding profiles
    • Dopamine receptors are widely distributed within the brain and play critical modulator roles on motor functions, motivation, sensation, drive, and cognition
    • Five genes code for different dopamine receptor subtypes (D1-D5)

    Typical Antipsychotics

    • Efficacy is primarily related to their binding to dopamine D2 receptors
    • Divided into high, moderate, and low potency categories based on their level of dopamine receptor antagonism
    • High-potency agents have the highest affinity for D2 receptors and are effective at relatively lower doses
    • Low-potency agents have lower D2 affinity and require larger doses to elicit an antipsychotic effect

    Atypical Antipsychotics

    • Distinguished by their prominent antagonism at the serotonin receptor in addition to D2 blockade
    • Ratio of serotonin to dopamine blockade is generally high for these agents
    • More selectivity for the mesolimbic dopamine pathway, which is thought to be a site of antipsychotic action
    • Relatively less action on the nigrostriatal pathway where extrapyramidal side effects are thought to originate
    • Associated with lesser extrapyramidal side effects in comparison with typical antipsychotics

    Examples of Antipsychotics

    • Typical: Chlorpromazine, Haloperidol, Trifluoperazine, Fluphenazine
    • Atypical: Risperidone, Olanzapine, Quetiapine

    Pharmacokinetics

    • Peak plasma levels of antipsychotics usually occur within 2-4 hours after oral absorption
    • IM injections reach peak levels in 30-60 minutes
    • Undergo extensive hepatic metabolism
    • Typically 50% of the antipsychotic is excreted via the hepatic circulation and 50% is excreted through the kidneys
    • 85-90% protein bound and highly lipophilic
    • Half-lives generally range from 5-50 hours

    Clinical Guidelines

    • Choice of neuroleptic should be based on past history of neuroleptic response and side effects
    • Atypical antipsychotics have gained acceptance as first-line drugs for the treatment of psychosis
    • At least two weeks of treatment is required before a significant antipsychotic effect is achieved
    • Poor response of negative symptoms is an indication for a trial of an atypical agent
    • Patients with tardive dyskinesia should be considered for treatment with an atypical agent to avoid progression of neurological impairment

    Adverse Drug Reactions

    • Tardive dyskinesia (TD) is a long-term, often permanent, neurological impairment resulting from extensive use of typical antipsychotics
    • Atypical agents have minimal risk of TD
    • Neuroleptic malignant syndrome is an uncommon, yet potentially fatal, adverse reaction to typical antipsychotics
    • Metabolic side effects: type II diabetes and hyperlipidemia may occur, especially with atypical antipsychotics

    Pre-Existing Medical Conditions

    • Cardiac History: use high-potency agents or atypicals to avoid conduction abnormalities
    • Elderly patients are more sensitive to side effects; atypical drugs should be utilized initially
    • Hematologic Disorder: clozapine is contraindicated
    • Hepatic, Renal, Cardiac, Respiratory Disease: use antipsychotics with caution; monitor renal, cardiac, and liver function
    • Parkinson's Disease: atypical agents with lower incidence of EPS (quetiapine) preferred due to selectivity for mesolimbic dopamine tract

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    Learn about the indications and uses of antipsychotic agents, including treatment of schizophrenia, bipolar disorder, and other mental health conditions.

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