A 55-year-old female is receiving chemotherapy for metastatic carcinoma. She threatens to stop her treatment because of severe nausea and vomiting. The oncologist plans to use prochlorperazine to reduce the nausea and vomiting associated with chemotherapeutic agents.
What is the mechanism of action of prochlorperazine?
A . Serotonin 5-HT3 antagonist
B . Blocking dopamine receptors
C . Cannabinoids related
D . Blockage of prostaglandins
E . H2 receptor antagonist
Answer: B
Explanation:
B: A variety of drugs have been found to be of some value in the prevention and treatment of vomiting, especially cancer chemotherapy-induced vomiting. With the exception of thioridazine, most of the neuroleptic drugs have antiemetic effects that are mediated by blocking D2 dopaminergic receptors of the chemoreceptor trigger zone of the medulla. Phenothiazines, such as prochlorperazine, were the first drugs shown to be effective antiemetic agents and act by blocking dopamine receptors. They are effective against low to moderately emetogenic chemotherapeutic agents (for example, fluorouracil and doxorubicin). Although increasing the dose improves antiemetic activity, side effects, including hypotension and restlessness, are dose limiting. Other adverse reactions include extrapyramidal symptom and sedation. A: Serotonin 5-HT3 antagonist is incorrect. The specific antagonists of the 5-HT3 receptor, ondansetron and granisetron, selectively block 5-HT3 receptors in the periphery and in the brain (chemoreceptor trigger zone). C: Cannabinoids related is incorrect. Cannabinoids are marijuana derivatives including dronabinol and nabilone and are effective against moderately emetogenic chemotherapy.
However, they are seldom first-line antiemetics because of serious side effects. D: Blockage of prostaglandins is incorrect. Dexamethasone and methylprednisolone used alone are effective against mildly to moderately emetogenic chemotherapy. Their antiemetic mechanism is not known, but it may involve blockade of prostaglandins. E: H2 receptor antagonist is incorrect. Antagonists of histamine H2 receptor block the action of histamine at all H2 receptors; their chief clinical use is as inhibitors of gastric acid secretion.
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