Antiemetic medications for nausea
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Classes of Antiemetic Medications for Nausea
Antiemetic medications are used to prevent and treat nausea and vomiting caused by various triggers, including chemotherapy, surgery, pregnancy, and other medical conditions. There are several main classes of antiemetic drugs, each working through different mechanisms. These include serotonin (5-HT3) receptor antagonists, dopamine antagonists, neurokinin-1 (NK1) receptor antagonists, antihistamines, anticholinergics, corticosteroids, benzodiazepines, and some newer agents like atypical antipsychotics and cannabinoids 1310.
Serotonin (5-HT3) Receptor Antagonists: Ondansetron, Granisetron, Palonosetron
5-HT3 antagonists such as ondansetron, granisetron, and palonosetron are highly effective for chemotherapy-induced nausea and vomiting (CINV) and are also used in other settings like surgery and pregnancy. Palonosetron may be more effective than ondansetron for delayed nausea, and adding dexamethasone can further improve control of vomiting 34910. These drugs are generally safe, but can sometimes cause mild side effects like headache or constipation, and may prolong the QT interval on ECG 37.
Dopamine Antagonists: Metoclopramide and Others
Dopamine antagonists, such as metoclopramide, are commonly used for nausea and vomiting, especially in pregnancy and less severe cases. However, they can cause extrapyramidal side effects, particularly in children, and may also prolong the QT interval 310.
Neurokinin-1 (NK1) Receptor Antagonists: Aprepitant, Netupitant, Rolapitant
NK1 antagonists are especially effective for preventing both acute and delayed CINV, particularly when combined with 5-HT3 antagonists and dexamethasone. These combinations are recommended in guidelines for patients receiving highly emetogenic chemotherapy 47910.
Corticosteroids: Dexamethasone
Dexamethasone is often used in combination with other antiemetics to enhance their effectiveness, especially in CINV. It is particularly useful when added to 5-HT3 antagonists 349.
Atypical Antipsychotics: Olanzapine, Mirtazapine, Blonanserin
Newer antipsychotics like olanzapine and mirtazapine target multiple neurotransmitter receptors and have shown effectiveness in treating refractory nausea, including in palliative care and CINV. Olanzapine, in particular, can reduce the need for other antiemetic medications and improve appetite, though it may cause mild sedation and, less commonly, QTc prolongation 24578.
Cannabinoids and Other Innovative Therapies
Cannabinoids have shown some effectiveness in treating cancer-related nausea, but their use is limited by significant side effects. Other innovative therapies, such as Kampo medicines in Japan and isopropyl alcohol aromatherapy, are being explored for their antiemetic effects, especially in specific settings like advanced cancer or emergency care 25.
Antihistamines, Anticholinergics, Sedatives, and Opioid Antagonists
Antihistamines and anticholinergics are sometimes used for nausea, particularly in motion sickness or pregnancy, but are generally less effective for severe cases. Sedatives have ranked highly for preventing nausea and vomiting during and after cesarean section, while opioid antagonists have limited effectiveness in this context 3610.
Safety and Adverse Effects of Antiemetic Medications
Most guideline-recommended antiemetics are considered safe when used at recommended doses. Common side effects include mild headache, constipation, and sedation. Some agents, particularly dopamine antagonists and certain 5-HT3 antagonists, can cause more serious effects like QT prolongation or extrapyramidal symptoms 379.
Conclusion
There is no single ideal antiemetic for all causes of nausea and vomiting. The choice of medication depends on the underlying cause, patient characteristics, and potential side effects. 5-HT3 antagonists, NK1 antagonists, and dexamethasone are mainstays for CINV, while newer agents like olanzapine and mirtazapine offer options for refractory cases. Ongoing research aims to improve efficacy, reduce side effects, and expand options for patients with nausea from various causes 12457910.
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