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?

Clozapine Signup and view all the answers

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

They are approved for the treatment of acute mania Signup and view all the answers

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

They are more effective in the treatment of negative symptoms Signup and view all the answers

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

It is not associated with tardive dyskinesia Signup and view all the answers

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

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

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

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

Which of the following is a contraindication for clozapine?

Hematologic disorder Signup and view all the answers

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

Atypical antipsychotics with low EPS Signup and view all the answers

What is the recommendation for patients with a seizure history?

Use atypical antipsychotics with a low risk of seizures Signup and view all the answers

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

A slight increase in the risk of anomalies Signup and view all the answers

What is the recommendation for patients with prostatic hypertrophy?

Avoid using antipsychotics with high anticholinergic activity Signup and view all the answers

What are antipsychotic agents primarily used for?

Treating mood disorders with psychotic symptoms Signup and view all the answers

What is the primary difference between typical and atypical antipsychotics?

Their receptor-binding profiles with dopamine and serotonin receptors Signup and view all the answers

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

D2 receptor Signup and view all the answers

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

High, moderate, and low potency Signup and view all the answers

What is the role of dopamine receptors in the brain?

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

What is the characteristic of high-potency antipsychotic agents?

They are effective at relatively lower doses Signup and view all the answers

What is the characteristic of low-potency antipsychotic agents?

They require larger doses to elicit an antipsychotic effect Signup and view all the answers

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

5 Signup and view all the answers

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

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

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

Mesolimbic dopamine pathway Signup and view all the answers

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

50% hepatic, 50% renal Signup and view all the answers

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

Greater selectivity for the mesolimbic dopamine pathway Signup and view all the answers

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

Taper the typical agent while introducing the atypical agent Signup and view all the answers

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

2-4 hours Signup and view all the answers

Which of the following is a characteristic of antipsychotic agents?

Highly lipophilic Signup and view all the answers

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

Past history of neuroleptic response and side effects Signup and view all the answers

What is the primary characteristic of Tardive Dyskinesia?

Involuntary, irregular movements Signup and view all the answers

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

1% per year Signup and view all the answers

What is the recommended treatment for Tardive Dyskinesia?

Reduce or stop antipsychotic if possible Signup and view all the answers

What is Neuroleptic Malignant Syndrome (NMS) characterized by?

Elevated temperature, autonomic instability, and delirium Signup and view all the answers

What is a risk factor for Neuroleptic Malignant Syndrome?

Dehydration Signup and view all the answers

What is a metabolic side effect of atypical antipsychotics?

Type II diabetes and hyperlipidemia Signup and view all the answers

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

Weight, waist circumference, blood pressure, and fasting glucose and lipids Signup and view all the answers

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

Switch to an atypical agent associated with less weight gain and diabetes 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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Description

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