40 Questions
What is the primary category of mental illness that includes schizophrenia?
Psychoses
What is the minimum number of symptoms required for a diagnosis of schizophrenia?
Two
What is the name of the hypothesis that suggests that schizophrenia results from increased dopaminergic neurotransmission?
Dopamine hypothesis
What is the duration of time that symptoms must persist for a diagnosis of schizophrenia?
6 months
What is the term for the ability to comprehend reality, which is retained in anxiety disorders?
Reality testing
What is the category of mental illness that includes anxiety disorders?
Neuroses
What is the term for the symptoms of delusions and sensory hallucinations?
Psychosis
Before a diagnosis of schizophrenia can be made, what must be ruled out?
Affective disorders
Serotonergic modulation is associated with a beneficial increase in which neurotransmitter release?
Dopamine release
What type of receptors can be located postsynaptically as well as presynaptically on dopamine neurons?
D2-type receptors
What are dopamine receptors located presynaptically on dopamine cell bodies and nerve terminals called?
Autoreceptors
What is the effect of autoreceptors on neuronal firing and dopamine synthesis and release?
They negatively modulate neuronal firing and dopamine synthesis and release
What is the cause of the parkinsonian-like movement side effects of neuroleptics?
Antagonism of dopamine D2 receptors
What percentage of patients experience extrapyramidal side effects from neuroleptics?
30-50%
What is a common metabolic side effect of neuroleptics?
Weight gain
What type of antipsychotics act as D2 receptor partial agonists?
Atypical antipsychotics
What is the beneficial effect of neuroleptics?
Antiemetic effects
What is the prototype of the phenothiazine-thioxanthene group of antipsychotic agents?
Chlorpromazine
What is the structural difference between phenothiazines and thioxanthenes?
Thioxanthenes have a carbon at position 10
What increases the antipsychotic efficacy of phenothiazines?
Substitution of an electron-withdrawing group at position 2
What is the effect of N-dealkylation of the side chain of phenothiazines?
Decreases antipsychotic activity
How can phenothiazines and thioxanthenes be divided based on substitution at position N10?
Into 3 groups: aliphatic, piperidine, and piperazine
What is the characteristic of phenothiazines with an aliphatic side chain?
They have a low potency
What is the characteristic of phenothiazines with a piperidine ring in the side chain?
They have a low incidence of extrapyramidal effects
What is the effect of haloperidol on hypotension?
It causes mild hypotension
What is the effect of replacing the keto moiety with other groups in butyrophenones?
It decreases neuroleptic potency
What is the characteristic of the most potent butyrophenone compounds?
They have a fluorine substituent in the para position
What is the use of haloperidol decanoate in noncompliant people?
It is used for its long duration of action
What is the effect of lengthening or shortening the three-carbon propyl chain in butyrophenones?
It decreases neuroleptic potency
What is the characteristic of the tertiary amino group in butyrophenones?
It is essential for neuroleptic activity
What is the use of droperidol in anesthesia?
It is used for its sedative and antiemetic effects
What is the result of replacing the keto function in butyrophenones with 4-flurophenylmethane?
It results in diphenylbutylpiperidine neuroleptics
What is the main mechanism by which atypical neuroleptics improve on the efficacy of antipsychotics?
By complementing or replacing D2 dopaminergic antagonism with an action on serotonergic transmission
Which of the following is a benzazepine derivative?
Clozapine
What is a serious drawback to the use of clozapine?
Agranulocytosis
Which enzyme is mainly involved in the metabolism of clozapine?
CYP3A4
What is risperidone's activity compared to clozapine?
More potent antidopaminergic and less potent antimuscarinic activity
What is the main difference between risperidone and clozapine in terms of extrapyramidal effects?
Risperidone can induce extrapyramidal symptoms at low daily doses
How is risperidone metabolized?
CYP2D6-catalyzed 9-hydroxylation
What is a characteristic of atypical neuroleptics such as clozapine and risperidone?
Limited adverse extrapyramidal effects at low daily doses
This quiz covers the medicinal chemistry of antipsychotics, including typical and atypical neuroleptics, and their use in treating schizophrenia. It also touches on the portrayal of schizophrenia in the movie A Beautiful Mind.
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