18 Questions
What is the main advantage of aripiprazole as a partial agonist antipsychotic?
No EPS even at 80% occupancy of D2 receptors
What are the common cardiovascular side effects of blocking a1-receptors?
Orthostatic hypotension, drowsiness, and dizziness
What is the typical proportion by which receptor blockade is reduced for a partial agonist like aripiprazole?
Approximately 25%
What are the side effects associated with H1 histamine receptor blockade?
Weight gain and drowsiness
What are some of the obesity-associated disorders that excessive weight gain induced by antipsychotic drugs can lead to?
Diabetes, hypertension, cardiovascular disease
What criteria characterize atypical antipsychotic drugs?
Low propensity for EPS or tardive dyskinesia, broad antipsychotic efficacy, minimal prolactin elevation, low catalepsy potential, and specific receptor affinities
Which antipsychotic drugs have severe effects on weight gain, with mean increases potentially exceeding 5kg?
Clozapine, olanzapine
What is the basis for the difference between atypical and typical antipsychotic agents?
Relatively high 5HT2A receptor affinity compared to D2 receptor affinity
Name a few antipsychotic drugs that have negligible effects on weight gain.
Ziprasidone
How do atypical antipsychotics differ from classical antipsychotics in terms of binding to the D2 receptor?
Atypical antipsychotics show rapid dissociation from the D2 receptor, while classical antipsychotics bind tightly to it
What is the main difference in mechanism of action between conventional antipsychotic drugs and atypical antipsychotic drugs?
Conventional drugs block dopamine D2 receptors, while atypical drugs have serotonin-dopamine antagonism
What is the role of 5-HT1A receptor partial agonism in some antipsychotic drugs like ziprasidone and aripiprazole?
Protection from weight gain
What are the side effects of conventional antipsychotics due to D2 receptor blockade in the nigrostriatal pathway?
Extrapyramidal symptoms (EPS) which include akathisia, Parkinsonian symptoms, and tardive dyskinesia.
What condition is produced by an increase in prolactin levels due to dopamine receptor blockade in the tuberoinfundibular pathway?
Galactorrhea.
What is the syndrome of abnormal, involuntary, repetitive movements that may result from continued use of conventional antipsychotics?
Tardive dyskinesia.
What pathway is responsible for the worsening of negative symptoms and potential cognitive dysfunction due to D2 receptor blockade by conventional antipsychotics?
Mesocortical pathway.
What are the side effects not related to D2 receptor blockade caused by the blockade of muscarinic receptors by antipsychotics?
Dry mouth, blurred vision, constipation, and cognitive impairment.
What is the condition characterized by restlessness and often alleviated by antimuscarinic drugs due to D2 receptor blockade in the nigrostriatal pathway?
Akathisia.
Test your knowledge on the pharmacological properties of aripiprazole, including its unique mechanism of action as a partial agonist, influence on dopamine system stabilization, and impact on weight gain in antipsychotic drug therapy.
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