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Questions and Answers
What is the neurotransmitter released by enterochromaffin cells of the small intestine in response to blood-borne emetics and local irritants?
Which receptor is stimulated by serotonin to initiate the vomiting reflex?
What is the main neurotransmitter involved in mediating signaling in the emetic center?
Which neurotransmitter binds to 5HT3 receptors to initiate the vomiting reflex?
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Which neurotransmitter receptor may mediate signaling in the emetic center?
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Which neurotransmitter is released by the enterochromaffin cells of the small intestine?
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Which neurotransmitter stimulates vagal afferents by binding to 5HT3 receptors?
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Which neurotransmitter is responsible for initiating the vomiting reflex?
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Which receptor antagonist is most commonly used for preventing nausea and vomiting?
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What is the primary route of excretion for Dolasetron's active metabolite?
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Which medication should be given at a decreased dose when used with Aprepitant due to drug interactions?
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What is the mechanism of action of metoclopramide in preventing nausea and vomiting?
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Which medication has a black box warning for tardive dyskinesia with high doses or long-term use?
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What is the primary route of excretion for Aprepitant?
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Which combination was approved by the FDA for use around 2014?
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What is the most effective drug for the prophylaxis and treatment of motion sickness?
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What is the most frequent side effect of antihistamines?
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What is the primary use of Histamine (H1R) antagonists?
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What receptor would be directly affected by local irritants such as bacteria, radiation, and cytotoxic drugs?
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Where are the serotonin receptors localized and how do they influence the emetic center?
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What are the names of the 5-HT3 receptor antagonists?
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What are some side effects of antihistamines and anticholinergics?
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Why should metoclopramide not be given at high doses or used long-term?
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What are the stimuli that activate the Area postrema (chemo receptive area)?
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Which areas in the CNS would be most associated with motion sickness?
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Which pharmacologic agent is useful for nausea and vomiting associated with vertigo and motion sickness?
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What is the appropriate prophylactic regimen for moderate emetic risk chemotherapy-induced nausea and vomiting (CINV)?
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In the context of postoperative nausea and vomiting (PONV), which agent is considered the 'gold standard'?
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What is the primary use of Butyrophenones in the treatment of chemotherapy-induced nausea and vomiting (CINV)?
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Which type of nausea and vomiting is usually self-limiting and will often be treated with over-the-counter (OTC) options?
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What are the common types of antiemetic agents used as breakthrough therapy for chemotherapy-induced nausea and vomiting (CINV)?
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In the context of simple nausea and vomiting, which agent is useful in nausea and vomiting related to reflux?
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Which class of antiemetic agents is useful in refractory chemotherapy-induced nausea and vomiting (CINV)?
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What is the primary prophylactic agent for postoperative nausea and vomiting (PONV)?
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What is the preferred treatment for pregnancy-induced nausea and vomiting?
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What is the key consideration in choosing a pharmacologic agent for treating nausea and vomiting?
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What should be the approach to treatment when selecting a pharmacologic agent for simple nausea/vomiting?
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Study Notes
Neurotransmitters and Receptors in Vomiting Reflex
- Serotonin is released by enterochromaffin cells of the small intestine in response to blood-borne emetics and local irritants.
- Serotonin stimulates 5-HT3 receptors to initiate the vomiting reflex.
- Dopamine is the main neurotransmitter involved in mediating signaling in the emetic center.
- Serotonin binds to 5-HT3 receptors to initiate the vomiting reflex.
- 5-HT3 receptors may mediate signaling in the emetic center.
- Serotonin is released by enterochromaffin cells of the small intestine.
- Serotonin stimulates vagal afferents by binding to 5-HT3 receptors.
- Serotonin is responsible for initiating the vomiting reflex.
Antiemetic Agents
- 5-HT3 receptor antagonists, such as dolasetron, are used to prevent nausea and vomiting.
- Ondansetron is a 5-HT3 receptor antagonist commonly used to prevent nausea and vomiting.
- Aprepitant is a medication that may be used at a decreased dose when used with other medications due to drug interactions.
- The primary route of excretion for dolasetron's active metabolite is renal.
- Aprepitant's primary route of excretion is hepatic.
- The combination of netupitant and palonosetron was approved by the FDA for use in 2014.
Mechanism of Action and Side Effects
- Metoclopramide prevents nausea and vomiting by blocking dopamine receptors in the central nervous system.
- Metoclopramide has a black box warning for tardive dyskinesia with high doses or long-term use.
- The most effective drug for the prophylaxis and treatment of motion sickness is scopolamine.
- The most frequent side effect of antihistamines is drowsiness.
- Histamine (H1R) antagonists are primarily used for their anti-emetic properties.
- Local irritants such as bacteria, radiation, and cytotoxic drugs directly affect the 5-HT3 receptor.
Motion Sickness and Chemotherapy-Induced Nausea and Vomiting
- The areas in the CNS most associated with motion sickness are the Area postrema, vestibular apparatus, and cerebral cortex.
- Scopolamine is a pharmacologic agent useful for nausea and vomiting associated with vertigo and motion sickness.
- The appropriate prophylactic regimen for moderate emetic risk chemotherapy-induced nausea and vomiting (CINV) includes a 5-HT3 receptor antagonist, dexamethasone, and aprepitant.
- In the context of postoperative nausea and vomiting (PONV), ondansetron is considered the 'gold standard'.
- Butyrophenones, such as droperidol, are used in the treatment of chemotherapy-induced nausea and vomiting (CINV).
Treatment of Nausea and Vomiting
- Mild nausea and vomiting is usually self-limiting and will often be treated with over-the-counter (OTC) options.
- Common types of antiemetic agents used as breakthrough therapy for chemotherapy-induced nausea and vomiting (CINV) include phenothiazines, butyrophenones, and cannabinoids.
- In the context of simple nausea and vomiting, metoclopramide is useful in nausea and vomiting related to reflux.
- Corticosteroids are useful in refractory chemotherapy-induced nausea and vomiting (CINV).
- The primary prophylactic agent for postoperative nausea and vomiting (PONV) is ondansetron.
- The preferred treatment for pregnancy-induced nausea and vomiting is vitamin B6 with or without doxylamine.
- The key consideration in choosing a pharmacologic agent for treating nausea and vomiting is the underlying cause of nausea and vomiting.
- The approach to treatment when selecting a pharmacologic agent for simple nausea/vomiting should be to start with a low dose and gradually increase as needed.
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Description
Test your knowledge of the anatomical areas, neurotransmitters, receptors, mechanisms of action, pharmacokinetics, and adverse effects of drugs used to treat nausea, vomit, and motion sickness. Explore the tight junctions of endothelial cells and the blood-brain barrier (BBB) in pharmacology.
