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Antimetabolites as Chemotherapy Agents

Antimetabolites are medications primarily used in the treatment of cancer. An “antimetabolite” is drug that is similar enough to a naturally occurring chemical in the body that it can participate in a biochemical reaction yet different enough to interfere with the normal division and functioning of cells. The presence of antimetabolites can have toxic effects, such as stopping cells from growing and dividing (apoptosis), so these compounds are most often used as chemotherapy for cancer, as they interfere with DNA creation and therefore the growth of tumors. Because cancer cells divide more quickly than other cells, inhibiting cell division impacts tumor cells more negatively than it dose other cells.

Serious Side Effects of Antimetabolites

Antimetabolites can seriously weaken the immune system. This can be life-threatening, particularly in patients who are already compromised. Serious side effects of antimetabolites, which warrant immediate medical attention, include:

  • Severe nausea, vomiting, or diarrhea
  • Hemorrhage
  • Liver damage
  • Kidney damage
  • Serious infection
  • Anemia
  • Neutropenia/Leukopenia (very low white cell count)
  • Wheezing or trouble breathing
  • Severe rash or hives
  • Acute pancreatitis
  • Summary of Common Antimetabolite Side Effects

    Because antimetabolites slow or halt cell replication, they can lead to a large number of side effects. Common side effects of antimetabolites include:

  • Unexplained fever, chills, or sore throat
  • Reduced appetite
  • Muscle pain
  • Rash
  • Diarrhea or constipation
  • Numbness, tingling in hands or feet (paresthesia)
  • Swelling of hands or feet
  • Hair loss
  • Fatigue
  • Understand Your Risks with the Rxight® Genetic Test

    Rxight® genetic testing from MD Labs is designed to help determine how well you metabolize medications based on the genetically encoded enzymes in your body. Hundreds of clinically relevant over-the-counter and prescription medications across over 50 pharmacological classes, including antimetabolites, are analyzed as part of the Rxight® panel. Rxight® is very simple test. All that is required is a cheek swab of your DNA at a participating pharmacy. After your sample is sent to our labs for analysis, the results will be reviewed with you in detail and will help guide your prescriber(s) in finding the best dose for you.

    Contributors to this Article:
    Michael Sapko, MD, PhD; Deborah Kallick, PhD, Medicinal Chemistry

    Antimetabolites Tested Include:

    • Capecitabine (Xeloda)
    • Fluorouracil (Adrucil, Carac, Efudex, Fluoroplex)
    • Methotrexate (Otrexup, Rasuvo, Trexall)
    • Thioguanine (Tabloid)

    Read more about Rxight® Genetic Testing For Drug Metabolism