Antipsychotic Drugs - Classification and Structure Activity Relationships 2
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Questions and Answers

What structural feature allows antipsychotic agents to form highly hydrophobic esters?

  • Variety of oils
  • Long-chain aliphatic esters
  • Free hydroxyl (OH) moiety
  • Terminal alcohol group (correct)
  • Which type of antipsychotic drugs have longer duration of action when prepared as long-chain fatty acid esters?

  • Neuroleptics with a free hydroxyl (OH) moiety (correct)
  • Antipsychotic agents with a terminal alcohol group
  • Long-chain aliphatic esters
  • Typical antipsychotics – Phenothiazen SAR
  • What distinguishes fluphenazine enanthate and fluphenazine decanoate from their unesterified precursors in clinical use?

  • Low hydrophobicity
  • Longer acting with fewer side effects (correct)
  • Less patient compliance needed
  • Shorter acting with more side effects
  • Why are patients treated with fluphenazine enanthate and fluphenazine decanoate less frequently than with their unesterified precursors?

    <p>Longer duration of action</p> Signup and view all the answers

    What is the main advantage of treating patients with long-acting antipsychotics like fluphenazine enanthate and fluphenazine decanoate?

    <p>Reduced need for frequent doses</p> Signup and view all the answers

    What is dissolved in a variety of oils to enhance the characteristics of typical antipsychotics like decanoate and palmitate?

    <p>Long-chain aliphatic esters</p> Signup and view all the answers

    Which antipsychotic agent has a longer duration of action than butyrophenone analogues?

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

    Which typical antipsychotic agent is specifically noted for its usefulness in treating acute exacerbation of schizophrenia and reducing the rate of relapse in chronic schizophrenia patients?

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

    Which benzamide derivative displays relatively low incidence of extrapyramidal side effects (EPS)?

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

    Which second-generation antipsychotic has a more typical neuroleptic biochemical profile with mainly antidopaminergic activity at D2-type receptors?

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

    Which antipsychotic has a relatively low affinity for brain dopamine D1 and D2 receptors but moderate affinity for D4 receptors?

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

    Which butyrophenone derivative is 50 times more potent than chlorpromazine but also produces a higher incidence of extrapyramidal reactions?

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

    Which benzamide derivative has poor oral absorption due to hydrophilicity and limited penetration into the central nervous system?

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

    Which second-generation antipsychotic agent has a variable half-life ranging from 20 to 50 hours?

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

    Which typical antipsychotic agent is known for its propensity to induce weight gain compared to most atypical antipsychotics?

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

    What is the role of endogenous plasma esterases in the action of butyrophenone based antipsychotic drugs?

    <p>They hydrolyse the esterified compound and liberate the parent drug</p> Signup and view all the answers

    What was the primary goal of research aimed at improving the analgesic activity of pethidine?

    <p>To develop a drug with only analgesic activity</p> Signup and view all the answers

    What effect does variation of the X and R groups on the general structure of butyrophenone have on its activity?

    <p>It eliminates the analgesic activity and enhances the antipsychotic activity</p> Signup and view all the answers

    What is the effect of altering the tertiary amino group on the fourth carbon of the butyrophenone skeleton?

    <p>It decreases the antipsychotic activity</p> Signup and view all the answers

    What is the result of replacing the ketone with thioketone, olefinic, or phenoxy groups in the butyrophenone structure?

    <p>It decreases the neuroleptic activity</p> Signup and view all the answers

    Which structural feature around the tertiary amine in the butyrophenone structure can be varied?

    <p>The tertiary amino group on the fourth carbon of the butyrophenone skeleton</p> Signup and view all the answers

    Which of the following antipsychotics is a benzisothiazole containing agent?

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

    Which of the following antipsychotics is an active metabolite of risperidone and has a short time to steady state due to rapid release from nanocrystals?

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

    Which of the following antipsychotics has a half-life of 22 hours and is metabolized by hepatic CYP2D6?

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

    Which of the following antipsychotics has a half-life of 6 hours and is metabolized to an active metabolite with 9-hydroxy?

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

    Which of the following antipsychotics is not insoluble in water and does not need co-administration with the oral formulation due to its rapid release from nanocrystals?

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

    Which of the following antipsychotics is a 5-HT2A/C/D2 antagonist with relatively high affinity at histamine H1 and adrenergic a1 and a2 receptors?

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

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