Antipsychotics Overview

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Questions and Answers

What is the primary purpose of antipsychotic drugs?

To enhance cognitive function

To induce sleep

To reduce hallucinations and delusions⁸ (correct)

To treat depression

What D2-receptor occupancy range is typically associated with the antipsychotic effect?

60-70% (correct)

70-80%

40-50%

80-90%

Which of the following is a first-generation antipsychotic?

Quetiapine

Aripiprazole

Clozapine

Haloperidol (correct)

Which atypical antipsychotic is associated with a risk of agranulocytosis?

Clozapine Signup and view all the answers

Which antipsychotic is least likely to cause extrapyramidal side effects?

Clozapine Signup and view all the answers

What common adverse effect is linked to Olanzapine?

QT prolongation Signup and view all the answers

Which of the following characteristics is NOT typical of atypical antipsychotics?

Can cause tardive dyskinesia Signup and view all the answers

Which antipsychotic drug has the shortest half-life?

Quetiapine Signup and view all the answers

What is a common adverse effect associated with antipsychotic drugs?

Constipation Signup and view all the answers

Which drug is a 5-HT2-D2 receptor antagonist?

Risperidone Signup and view all the answers

What is a common adverse effect of Quetiapine?

Somnolence Signup and view all the answers

How long does it typically take to reach steady-state drug levels of most antipsychotic drugs?

Several weeks Signup and view all the answers

What type of side effects is Risperidone most likely to cause?

Extrapyramidal side effects Signup and view all the answers

What is the licensed dosing interval for Haloperidol decanoate?

4 weeks Signup and view all the answers

Which of the following side effects is categorized under antidopaminergic movement effects?

Acute dystonia Signup and view all the answers

What is the time to peak plasma level for Fluphenazine decanoate?

1-2 days Signup and view all the answers

Which of the following side effects is primarily associated with antihistaminic effects of antipsychotic drugs?

Sedation Signup and view all the answers

What is the typical clinical dose for Risperidone microspheres?

37.5 mg Signup and view all the answers

What is a prominent motor symptom observed in the clinical picture described?

Generalized muscular hypertonicity Signup and view all the answers

Which medication is used specifically to treat malignant hyperthermia?

Dantrolene Signup and view all the answers

Which of the following conditions is a contraindication for the use of Bromocriptine?

Myasthenia gravis Signup and view all the answers

What symptom is associated with autonomic disturbances in this condition?

Tachycardia Signup and view all the answers

Which medication should not be administered with parenteral benzodiazepines?

Olanzapine Signup and view all the answers

What is one of the side effects characterized by an expressionless face, lack of movement, and rigidity after months of antipsychotic treatment?

Parkinsonian syndrome Signup and view all the answers

Which drug is commonly used to control Parkinsonian syndrome resulting from antipsychotic medication?

Procyclidine Signup and view all the answers

Which statement about tardive dyskinesia is correct?

It can occur in patients taking metoclopramide. Signup and view all the answers

What are the specific movements associated with tardive dyskinesia?

Grimacing and choreoathetoid movements Signup and view all the answers

Which complication is associated with antihistaminic effects from antipsychotic medications?

Increased appetite and weight gain Signup and view all the answers

What is a consequence of excessive dopamine-receptor blockade in patients treated with antipsychotics?

Mood depression and anhedonia Signup and view all the answers

Which side effect is categorized as an anticholinergic effect of antipsychotics?

Dry mouth and constipation Signup and view all the answers

What is the recommended monitoring for potential cardiac issues arising from antipsychotic use?

ECG monitoring for arrhythmias Signup and view all the answers

What is the primary concern associated with obesity in patients taking certain antipsychotic medications?

Increased risk of developing type 2 diabetes Signup and view all the answers

Which specific antipsychotic medications are noted for significantly increasing lipid levels?

Olanzapine, clozapine, and quetiapine Signup and view all the answers

Which combination constitutes metabolic syndrome?

Central obesity, high fasting glucose, low HDL cholesterol, high triglycerides Signup and view all the answers

What is a recommended monitoring frequency for body mass index in patients on antipsychotic drugs?

Once every 4 weeks for 12 weeks, then at least biannually Signup and view all the answers

What is a side effect associated with clozapine that requires regular monitoring?

Leucopenia requiring blood count Signup and view all the answers

Which lifestyle intervention is recommended for patients on antipsychotic medication to mitigate weight gain?

Diet and exercise adjustments Signup and view all the answers

What is the rare serious condition that can occur in a small minority of patients treated with high potency antipsychotics?

Neuroleptic malignant syndrome Signup and view all the answers

What type of change can high prolactin levels cause in patients?

Galactorrhoea and amenorrhoea Signup and view all the answers

Study Notes

Antipsychotic Drug Overview

Antipsychotics reduce hallucinations, delusions, agitation, and psychomotor excitement in conditions like schizophrenia and mania.
Effective treatment occurs when D2-receptor occupancy is between 60-70%.

Types of Antipsychotics

Conventional Antipsychotics (First Generation)
- Examples: chlorpromazine, haloperidol.
- Function primarily as dopamine-receptor antagonists.
Atypical Antipsychotics (Second Generation)
- Produce effects with fewer extrapyramidal side effects.
- Higher risk of tardive dyskinesia is not common except with risperidone.

Common Antipsychotic Agents

Phenothiazines:
- Chlorpromazine, Triﬂuoperazine.
Thioxanthenes:
- Flupenthixol, Clopenthixol.
Butyrophenones:
- Haloperidol.
Dibenzodiazepines:
- Clozapine, Olanzapine.
Dibenzothiazepine:
- Quetiapine.
Substituted Benzamides:
- Sulpiride, Amisulpride.
Benzisoxazole:
- Risperidone.
Quinolinone:
- Aripiprazole.

Side Effects of Atypical Antipsychotics

Amisulpride: EPS, prolactin elevation, weight gain. Side effects include insomnia and QT prolongation.
Sulpiride: Similar profile to amisulpride.
Clozapine: Zero EPS or prolactin elevation, significant weight gain potential, and associated with agranulocytosis.
Olanzapine: Variable EPS, high weight gain. Side effects include somnolence and diabetes.
Quetiapine: No EPS or prolactin elevation. Monitor for somnolence and metabolic effects.
Risperidone: Higher risk of EPS and prolactin elevation. Side effects include insomnia and anxiety.

Pharmacology Highlights

Atypical antipsychotics act as 5-HT2-D2-receptor antagonists.
Most are metabolized by the liver; exceptions include sulpiride and amisulpride excreted unchanged by the kidneys.
Typical half-life of antipsychotics is around 20 hours; quetiapine requires twice-daily dosing.
Steady-state drug levels achieved after several weeks.

Common Side Effects

Antidopaminergic Effects: Acute dystonia, akathisia, parkinsonism, tardive dyskinesia.
Other Effects: Weight gain, sedation, cardiac arrhythmias, metabolic syndrome, endocrine changes (e.g., galactorrhea).
Serious Risks: Neuroleptic malignant syndrome (NMS), especially with high-potency compounds.

Tardive Dyskinesia

Characterized by involuntary movements primarily of the face, increased susceptibility in women and elderly.
Lower occurrence in atypical agents like clozapine and olanzapine compared to haloperidol.
Possible treatment includes clozapine or clonazepam.

Depot Antipsychotic Administration

Infrequently used antipsychotics available in depot forms for long-term treatment.
Includes agents like flupenthixol decanoate, haloperidol decanoate, and risperidone microspheres.
Various dosing intervals and clinical dosages, emphasizing monitoring.

Clinical Monitoring and Intervention

Regular monitoring of body mass index, blood glucose, lipid profile, and blood pressure.
Recommend lifestyle interventions and potential switching to drugs with a better side effect profile.
Metformin may assist with weight management.

Clozapine Monitoring

Requires weekly blood counts at initiation due to risk of leukopenia, transitioning to bi-weekly then monthly.
Potential side effects include drowsiness, weight gain, and seizures at higher doses.

Contraindications

Avoid in conditions like myasthenia gravis, Addison’s disease, and glaucoma.
Increased risk of severe movement disorders in dementia patients.
Caution with liver diseases and potential cardiac risks associated with certain medications.

Treatment of Acute Behavioral Disturbances

Medications like lorazepam, olanzapine, or haloperidol are commonly used for rapid tranquillization.
ECG monitoring is advised prior to administration of parenteral antipsychotics.

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Description

This quiz covers the fundamental aspects of antipsychotic drugs, including their purpose in treating conditions like schizophrenia and the different types of antipsychotics. Understand the mechanisms of action and the therapeutic effects associated with both conventional and atypical agents. Test your knowledge on the pharmacology of these important medications.