Antifolates Drug Class

Also known as folate antagonists or antifols, antifolates are a class of drugs that is used to restrain the production of folic acid. In the body, folic acid works as a cofactor with several other chemicals for protein synthesis, DNA/RNA synthesis, and to aid cell division. Thus, antifolates inhibit all of those processes by limiting folic acid. Some antifolates are built to specifically target folic acid in microbial organisms. Most antifolates work by targeting dihydrofolate reductase.

Antifolates Drugs

There are several different antifolates commonly prescribed in the United States as part of different treatment programs:

Antifolates Uses

Antifolates are used primarily in cancer treatments as a way to suppress the growth of malignant tumors, usually as a part of chemotherapy. These drugs act either in conjunction with other drugs to make cancer-fighting characteristics stronger or to protect healthy cells while a patient is undergoing chemotherapy treatment. The types of cancer that antifolates are used to treat include: acute lymphocytic leukemia, non-Hodgkin’s lymphoma, head and neck cancer, osteogenic sarcoma, breast cancer, mesothelioma, choriocarcinoma, and bladder cancer. They’ve also been shown to be useful in treating other nonmalignant diseases such as arthritis, malaria, plasmodial infections, bacterial infections, and psoriasis.

Antifolates Side Effects

These drugs should never be taken during pregnancy. Many of the side effects are unavoidable, but if you are taking antifolates you should let your doctor know about any issues that you are having. Antifolates tend to come with serious side effects that particularly affect skin, hair, and bone marrow. Evidence has shown that supplemental doses of folic acid and/or a high folate diet may help alleviate some side effects. It’s also been shown that over time the body can build up a resistance to antifolates as part of a cancer treatment, but that can be mitigated using a combination of other medications. Possible side effects include:

  • Weight loss
  • Renal failure
  • Pharyngitis
  • Inflammation of the mouth
  • Chills
  • Vomiting
  • Fever
  • Rashes
  • Anemia
  • Dermatitis
  • Dehydration
  • Diarrhea
  • Numbness in hands or feet
  • Constipation
  • Chest Pain
  • Fatigue

Antifolates Interactions

Antifolates are commonly used in conjunction with other drugs, as well as with drugs to lessen side effects. However, there are a number of other steps that can be taken to make life better while on these drugs. Anyone planning on taking antifolates should consult with their doctor for a comprehensive list of do’s and don’ts.