27 Questions
What structural feature allows antipsychotic agents to form highly hydrophobic esters?
Terminal alcohol group
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
What distinguishes fluphenazine enanthate and fluphenazine decanoate from their unesterified precursors in clinical use?
Longer acting with fewer side effects
Why are patients treated with fluphenazine enanthate and fluphenazine decanoate less frequently than with their unesterified precursors?
Longer duration of action
What is the main advantage of treating patients with long-acting antipsychotics like fluphenazine enanthate and fluphenazine decanoate?
Reduced need for frequent doses
What is dissolved in a variety of oils to enhance the characteristics of typical antipsychotics like decanoate and palmitate?
Long-chain aliphatic esters
Which antipsychotic agent has a longer duration of action than butyrophenone analogues?
Pimozide
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?
Pimozide
Which benzamide derivative displays relatively low incidence of extrapyramidal side effects (EPS)?
Sulpiride
Which second-generation antipsychotic has a more typical neuroleptic biochemical profile with mainly antidopaminergic activity at D2-type receptors?
Loxapine
Which antipsychotic has a relatively low affinity for brain dopamine D1 and D2 receptors but moderate affinity for D4 receptors?
Clozapine
Which butyrophenone derivative is 50 times more potent than chlorpromazine but also produces a higher incidence of extrapyramidal reactions?
Haloperidol
Which benzamide derivative has poor oral absorption due to hydrophilicity and limited penetration into the central nervous system?
Sulpiride
Which second-generation antipsychotic agent has a variable half-life ranging from 20 to 50 hours?
Olanzapine
Which typical antipsychotic agent is known for its propensity to induce weight gain compared to most atypical antipsychotics?
Chlorpromazine
What is the role of endogenous plasma esterases in the action of butyrophenone based antipsychotic drugs?
They hydrolyse the esterified compound and liberate the parent drug
What was the primary goal of research aimed at improving the analgesic activity of pethidine?
To develop a drug with only analgesic activity
What effect does variation of the X and R groups on the general structure of butyrophenone have on its activity?
It eliminates the analgesic activity and enhances the antipsychotic activity
What is the effect of altering the tertiary amino group on the fourth carbon of the butyrophenone skeleton?
It decreases the antipsychotic activity
What is the result of replacing the ketone with thioketone, olefinic, or phenoxy groups in the butyrophenone structure?
It decreases the neuroleptic activity
Which structural feature around the tertiary amine in the butyrophenone structure can be varied?
The tertiary amino group on the fourth carbon of the butyrophenone skeleton
Which of the following antipsychotics is a benzisothiazole containing agent?
Ziprasidone
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?
Paliperidone
Which of the following antipsychotics has a half-life of 22 hours and is metabolized by hepatic CYP2D6?
Risperidone
Which of the following antipsychotics has a half-life of 6 hours and is metabolized to an active metabolite with 9-hydroxy?
Ziprasidone
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?
Paliperidone
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?
Ziprasidone
Learn about the classification and structural activity relationships of antipsychotic drugs, with a focus on drugs used to treat schizophrenia. Explore the different types of antipsychotic agents, including long-acting ones, and understand how they work.
Make Your Own Quizzes and Flashcards
Convert your notes into interactive study material.
Get started for free
