Antipsychotic Drugs: Second Generation

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Questions and Answers

What is a common characteristic of second-generation antipsychotics, except for aripiprazole?

  • They have higher rates of metabolic adverse effects and weight gain
  • They are associated with lower rates of extrapyramidal adverse effects and TD (correct)
  • They are anticholinergic antagonists
  • They are dopamine D2 agonists

What is the primary mechanism of action of clozapine?

  • Dopamine D1 receptor agonist
  • Weak D2-receptor antagonist (correct)
  • Selective serotonin reuptake inhibitor
  • Strong D2-receptor antagonist

What is a specific use of clozapine in the treatment of schizophrenia?

  • Reducing the risk of recurrent suicidal behavior (correct)
  • Managing acute psychotic episodes
  • Treating EPS in patients with schizophrenia
  • Improving cognitive function in patients with schizophrenia

What is a common adverse effect of risperidone?

<p>Hypotension (C)</p> Signup and view all the answers

What type of receptors does risperidone have high affinity for?

<p>Serotonin type 2 (5-HT2) receptors (A)</p> Signup and view all the answers

What is a benefit of risperidone in the treatment of psychoses?

<p>Improving negative symptoms (A)</p> Signup and view all the answers

What is a common adverse effect of clozapine?

<p>Sedation (B)</p> Signup and view all the answers

What is a unique characteristic of clozapine compared to other antipsychotics?

<p>It has anticholinergic and antihistaminic effects (D)</p> Signup and view all the answers

What is the mechanism of action of asenapine?

<p>Acts as an antagonist at dopamine D2 and serotonin 5-HT2 receptors (A)</p> Signup and view all the answers

Which of the following is a side effect of olanzapine?

<p>Dry mouth (B)</p> Signup and view all the answers

What is the indication of asenapine?

<p>Acute and maintenance treatment of schizophrenia (D)</p> Signup and view all the answers

What is the mechanism of action of serotonin-dopamine activity modulators (SDAMs)?

<p>Acts as a partial agonist at 5-HT1A and dopamine D2 receptors at similar potency (A)</p> Signup and view all the answers

What is the use of aripiprazole?

<p>Acute and maintenance treatment of schizophrenia and adjunctive therapy for major depressive disorder (D)</p> Signup and view all the answers

What is the side effect of asenapine?

<p>Sedation (B)</p> Signup and view all the answers

What is the mechanism of action of aripiprazole?

<p>Acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and an antagonist at serotonin 5-HT2A receptors (A)</p> Signup and view all the answers

What is the advantage of asenapine compared to typical antipsychotics?

<p>It has less extrapyramidal adverse effects (D)</p> Signup and view all the answers

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Study Notes

Second-Generation Antipsychotics (Atypical)

  • Characterized as dopamine D2 antagonists, except for aripiprazole, with lower rates of extrapyramidal adverse effects and tardive dyskinesia (TD) compared to first-generation antipsychotics.
  • However, they are associated with higher rates of metabolic adverse effects and weight gain.

Clozapine

  • Weak D2-receptor antagonist with significant anticholinergic, antihistaminic, and antiserotoninergic (5-HT1C, 5-HT2, 5-HT3) properties.
  • Used to treat refractory schizophrenia, especially atypical type with negative manifestations, and to reduce the risk of recurrent suicidal behavior in schizophrenia or schizoaffective disorder.
  • Adverse effects include:
    • Neurological: sedation, drooling, dizziness
    • Cardiovascular: tachycardia, cardiomyopathy, myocarditis
    • Hematological: agranulocytosis (frequent CBC required)
    • GIT: constipation
    • Metabolic: weight gain

Risperidone

  • Has high affinity for serotonin type 2 (5-HT2) receptors and binds to dopamine D2 receptors, antagonizing alpha1-adrenergic, alpha2-adrenergic, and histaminergic receptors.
  • Improves negative symptoms of psychoses and reduces incidence of extrapyramidal symptoms (EPS).
  • Adverse effects include:
    • Mild sedation
    • Hypotension
    • Akathisia
    • Increase in prolactin
    • Weight gain

Other Atypical Antipsychotic Drugs

Asenapine

  • Acts as an antagonist at dopamine D2 and serotonin 5-HT2 receptors, improving negative symptoms of psychoses and reducing incidence of EPS.
  • Indicated for acute and maintenance treatment of schizophrenia.
  • Adverse effects include:
    • Sedation
    • Weight gain
    • Dizziness
    • Extrapyramidal symptoms

Olanzapine

  • Acts through combination of dopamine and serotonin type 2 receptor site antagonism.
  • Side effects include:
    • Weight gain
    • Sedation
    • Akathisia
    • Hypotension
    • Dry mouth
    • Constipation

Aripiprazole (Serotonin-Dopamine Activity Modulator (SDAM))

  • Acts as a partial agonist at 5-HT1A and dopamine D2 receptors, and as an antagonist at 5-HT2A and noradrenaline alpha1/2 receptors.
  • Used for acute and maintenance treatment of schizophrenia, acute and maintenance treatment of bipolar I disorder, and adjunctive therapy for major depressive disorder.
  • Adverse effects include:
    • Headache
    • Nausea
    • Vomiting
    • Insomnia
    • Tremor
    • Constipation

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