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Selective serotonin receptor (5-HT3) antagonists block serotonin, specifically targeting gastrointestinal (GI) vagal nerve terminals and the chemoreceptor trigger zone within the central nervous system. This blockade leads to antiemetic effects, making them invaluable in managing nausea and vomiting induced by chemotherapy, radiation therapy, and postoperative procedures. Understanding the indications, dosing, administration, and potential adverse events associated with 5-HT3 receptor antagonists is crucial for healthcare professionals across disciplines. This activity provides comprehensive insights into the pharmacological mechanism, pharmacokinetics, contraindications, precautions, monitoring strategies, and toxicity profiles of these agents, emphasizing the collaborative efforts of interdisciplinary healthcare teams in effectively preventing and treating nausea and vomiting. Objectives: Identify the mechanism of action of 5-HT3 receptor antagonists. Identify the approved indications for 5-HT3 receptor blockers. Determine the potential adverse events associated with 5-HT3 receptor antagonists. Develop strategies for the interprofessional healthcare team to improve care coordination and communication to improve patient outcomes when using 5-HT3 receptor antagonists. Access free multiple choice questions on this topic.

Overdose is rare, and there is no fatal dose yet established. 5-HT3 receptor antagonists have a broad therapeutic index with mild side effects that occur infrequently. There is no antidote for 5-HT3 receptor antagonists.[50] Therefore, the healthcare team treats patients with supportive therapy, such as IV fluid resuscitation and norepinephrine infusions. In a case report of intentional granisetron overdose, the patient presented with significant hemodynamic instability, characterized by hypotension and ECG changes.[50]

Nausea and vomiting can negatively impact a patient's health and quality of life, especially when induced by cancer treatment. CINV is associated with increased healthcare costs.[51] An interdisciplinary team can ensure that antiemetic guidelines are appropriately followed. Physicians, physician assistants, and nurse practitioners can identify patient-specific factors that increase the risk of CINV, such as female gender, age less than 50 years, and anxiety.[52] Nurses can assess patient history to anticipate nausea and vomiting and advocate to premedicate patients. Pharmacists can identify the emetogenic risk of cancer medications, identify drug interactions and adverse effects, and recommend the appropriate monitoring parameters.[53] An interdisciplinary team can work together to ensure patients understand the antiemetic role of 5-HT3 receptor antagonists in preventing CINV. This will help increase adherence when the healthcare team prescribes additional doses of 5-HT3 receptor antagonists for the patient to take at home.[54]