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Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
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Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
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Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
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5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
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Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
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Antipsychotic drugs primarily block dopamine and serotonin receptors and cholinergic, adrenergic, and histaminergic receptors, thereby reducing hallucinations and delusions in conditions like schizophrenia. However, they can trigger unwanted extrapyramidal effects such as dystonias, Parkinson-like symptoms, and tardive dyskinesia.
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Related Experiment Video

Updated: Dec 19, 2025

Nerve Excitability Assessment in Chemotherapy-induced Neurotoxicity
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Anticancer Drugs and the Nervous System.

Bianca D Santomasso

    Continuum (Minneapolis, Minn.)
    |June 4, 2020
    PubMed
    Summary

    Neurotoxicity from anticancer drugs is common, affecting both central and peripheral nervous systems. Early recognition of these adverse effects from immunotherapies and other cancer treatments is crucial for patient outcomes.

    Area of Science:

    • Neuro-oncology
    • Cancer Therapeutics
    • Neurology

    Background:

    • Neurotoxicity is a significant concern in cancer therapy, impacting both traditional chemotherapy and newer agents.
    • Neurologic adverse effects are increasingly observed due to longer patient survival and complex treatment regimens.
    • Distinguishing treatment-related neurotoxicity from cancer progression or other neurologic disorders is critical.

    Purpose of the Study:

    • To review the clinical features, prognosis, and treatment of neurotoxicity associated with various anticancer drugs.
    • To highlight the unique neurologic complications of novel immunotherapies, including immune checkpoint inhibitors and CAR T-cell therapy.
    • To emphasize the importance of early recognition and management of treatment-related neurotoxicity.

    Main Methods:

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    • Review of clinical features, prognosis, and treatment strategies for anticancer drug-induced neurotoxicity.
    • Focus on emerging patterns of neurotoxicity from immunotherapies (immune checkpoint inhibitors, CAR T-cells).
    • Discussion of central and peripheral nervous system complications.

    Main Results:

    • Neurotoxicity from cancer therapy is common, affecting both central and peripheral nervous systems.
    • Newer immunotherapies present distinct patterns of neurologic adverse effects.
    • Prompt identification and management can prevent permanent neurologic injury.

    Conclusions:

    • Neurotoxicity is a frequent complication of cancer therapy, necessitating vigilance.
    • Immune checkpoint inhibitors and CAR T-cells have unique neurotoxic profiles.
    • Early detection and intervention are key to managing neurotoxicity and optimizing cancer care.