Antipsychotic Drugs Classification Flashcards
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Questions and Answers

Which drugs are contained in phenothiazine?

  • Fluphenazine (correct)
  • Clozapine
  • Chlorpromazine (correct)
  • Haloperidol

    • What is the structure-activity relationship (SAR) of phenothiazines?

    Distance between two nitrogens should contain 3 carbons and the N-side chain needs a tertiary amine to be the most active.

    What group does chlorpromazine have?

    Aliphatic

    What is the generation, potency, and metabolic risk of chlorpromazine?

    <p>First Generation, Low potency, Medium metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of fluphenazine?

    <p>First Generation, High potency, Low metabolic risk</p> Signup and view all the answers

    What group does fluphenazine have?

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

    What drug is contained in butyrophenones?

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

    What is the structure-activity relationship (SAR) of butyrophenones?

    <p>Tertiary amino to 4-C skeleton is essential; modifying the propyl chain decreases potency; replacing keto-moiety decreases potency; most potent is fluorine in para of benzene.</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of haloperidol?

    <p>First Generation, High potency, Low metabolic risk</p> Signup and view all the answers

    Name the drugs classified as benzazepines.

    <p>Clozapine, Olanzapine, Quetiapine, Asenapine</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of clozapine?

    <p>Second Generation, Low potency, High metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of olanzapine?

    <p>Second Generation, Medium potency, High metabolic risk</p> Signup and view all the answers

    What drugs are classified as benzisoxazoles?

    <p>Risperidone, Paliperidone</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of risperidone?

    <p>Second Generation, High potency, Medium metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of quetiapine?

    <p>Second Generation, Low potency, High metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of paliperidone?

    <p>Second Generation, High potency, Medium metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of asenapine?

    <p>Second Generation, Medium potency, Medium metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of ziprasidone?

    <p>Second Generation, Medium potency, Low metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of lurasidone?

    <p>Second Generation, Medium potency, Low metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of lumateperone?

    <p>Second Generation, Medium potency, Low metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of aripiprazole?

    <p>Second Generation, Partial-Agonist, Low metabolic risk</p> Signup and view all the answers

    What is the mechanism of action (MOA) of aripiprazole?

    <p>D2 partial agonist, an agonist at 5HT2A and 5HT1A</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of brexpiprazole?

    <p>Second Generation, Partial-Agonist, Low metabolic risk</p> Signup and view all the answers

    What is the generation, potency, and metabolic risk of cariprazine?

    <p>Second Generation, Partial-Agonist, Low metabolic risk</p> Signup and view all the answers

    What receptors does cariprazine preferentially act upon?

    <p>D3/D2 receptor partial agonist, D3 receptor preferring</p> Signup and view all the answers

    What is the mechanism of action (MOA) of brexpiprazole?

    <p>Higher affinity for D2, 5-HT2A and 5HT1A receptors than aripiprazole, lower intrinsic activity at D2 than aripiprazole</p> Signup and view all the answers

    Which antipsychotics are the biggest offenders of causing QT prolongation? (Select all that apply)

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

    What issues are FGAs more likely to cause than SGAs?

    <p>Drug-induced movement disorders, prolactin issues, QTc prolongation, sedation</p> Signup and view all the answers

    What issues are high potency medications more likely to cause?

    <p>Drug-induced movement disorders, hyperprolactinemia</p> Signup and view all the answers

    What issues are low potency medications more likely to cause?

    <p>Anticholinergic side effects, sedation, hypotension</p> Signup and view all the answers

    Study Notes

    Antipsychotic Drugs Classification

    • Phenothiazines include chlorpromazine and fluphenazine, characterized by the -azine suffix.
    • Structure-Activity Relationships (SAR) for phenothiazines:
      • Distance between two nitrogen atoms should be three carbons.
      • A tertiary amine is essential in the N-side chain for maximum activity.
    • Chlorpromazine features an aliphatic group and belongs to first-generation antipsychotics with low potency and medium metabolic risk.
    • Fluphenazine, also a first-generation antipsychotic, has a piperazine group, high potency, and low metabolic risk.
    • Butyrophenones are represented by haloperidol, a first-generation antipsychotic known for its high potency and low metabolic risk.
    • SAR of butyrophenones:
      • A tertiary amino group is necessary for activity.
      • Modifications to the propyl chain or replacing the keto-moiety decrease potency.
      • The most potent variant contains fluorine in the para position of the benzene ring.
    • Benzazepines include clozapine, olanzapine, quetiapine, and asenapine.
    • Clozapine is a second-generation antipsychotic with low potency and high metabolic risk.
    • Olanzapine features medium potency and high metabolic risk but is notably sedating.
    • Risperidone belongs to the benzisoxazole class, categorized as second-generation, high potency, with medium metabolic risk.
    • Quetiapine, a second-generation drug, has low potency and high metabolic risk.
    • Paliperidone is also a second-generation antipsychotic with high potency and medium metabolic risk.
    • Asenapine is classified as second-generation with medium potency and medium metabolic risk.
    • Benzisothiazole consists of ziprasidone and lurasidone, both second-generation drugs with medium potency and low metabolic risk.
    • Lumateperone is a second-generation antipsychotic with medium potency and low metabolic risk as well.
    • Aripiprazole, a second-generation partial agonist, shows low metabolic risk, functioning primarily as a D2 partial agonist and agonist at 5HT2A and 5HT1A receptors.
    • Brexpiprazole has a similar profile to aripiprazole but features higher affinity for D2 and 5-HT2A and 5HT1A receptors with lower intrinsic activity at D2.
    • Cariprazine, another second-generation partial agonist, prefers the D3 receptor while being a D2 receptor partial agonist.
    • Antipsychotics causing significant QT prolongation: ziprasidone, iloperidone, thorazine, and thioridazine; generally, first-generation antipsychotics (FGAs) have a higher risk than second-generation antipsychotics (SGAs).
    • FGAs are more likely than SGAs to cause:
      • Drug-induced movement disorders
      • Prolactin elevation
      • QTc prolongation
      • Sedation
    • High-potency medications have increased chances of causing movement disorders and hyperprolactinemia.
    • Low-potency medications tend to lead to:
      • Anticholinergic side effects
      • Sedation
      • Hypotension

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    Description

    This quiz focuses on the classification and structure-activity relationships (SAR) of antipsychotic drugs, particularly phenothiazines. Test your knowledge on key drugs such as chlorpromazine and fluphenazine, their active groups, and related pharmacological concepts.

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