Questions and Answers
Which drugs are contained in phenothiazine?
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?
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What is the generation, potency, and metabolic risk of fluphenazine?
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What group does fluphenazine have?
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What drug is contained in butyrophenones?
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What is the structure-activity relationship (SAR) of butyrophenones?
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What is the generation, potency, and metabolic risk of haloperidol?
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Name the drugs classified as benzazepines.
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What is the generation, potency, and metabolic risk of clozapine?
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What is the generation, potency, and metabolic risk of olanzapine?
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What drugs are classified as benzisoxazoles?
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What is the generation, potency, and metabolic risk of risperidone?
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What is the generation, potency, and metabolic risk of quetiapine?
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What is the generation, potency, and metabolic risk of paliperidone?
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What is the generation, potency, and metabolic risk of asenapine?
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What is the generation, potency, and metabolic risk of ziprasidone?
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What is the generation, potency, and metabolic risk of lurasidone?
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What is the generation, potency, and metabolic risk of lumateperone?
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What is the generation, potency, and metabolic risk of aripiprazole?
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What is the mechanism of action (MOA) of aripiprazole?
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What is the generation, potency, and metabolic risk of brexpiprazole?
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What is the generation, potency, and metabolic risk of cariprazine?
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What receptors does cariprazine preferentially act upon?
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What is the mechanism of action (MOA) of brexpiprazole?
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Which antipsychotics are the biggest offenders of causing QT prolongation? (Select all that apply)
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What issues are FGAs more likely to cause than SGAs?
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What issues are high potency medications more likely to cause?
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What issues are low potency medications more likely to cause?
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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.
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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.