What are antifolate drugs used for?

A type of drug that stops cells from using folic acid to make DNA and may kill cancer cells. Certain antifolates are used to treat some types of cancer and inflammatory conditions, such as rheumatoid arthritis. Also called folate antagonist and folic acid antagonist.

What does antifolate mean?

Antifolates are a class of antimetabolite medications that antagonise (that is, block) the actions of folic acid (vitamin B9). Folic acid’s primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis.

What are antimetabolite drugs?

Antimetabolites are a form of chemotherapy drug. They’re one of the most commonly used therapies to treat cancer. And they’re one of the oldest, dating back to the 1940s, when doctors used a medication that’s now considered an antimetabolite to treat children with leukemia.

Is Methotrexate an antifolate?

Methotrexate is an antifolate and antimetabolite originally developed to treat malignancy. In the setting of RA, it is given at much lower doses than when given as an anticancer agent. The usual dose is 7.5 to 25 mg per week given as a single dose orally.

Is atovaquone an antifolate?

The proguanil-atovaquone combination has a synergistic effect, although atovaquone, acting on mitochondrial electron transport system, is not an antifolate drug and the mechanism of synergism is still poorly understood.

Is methotrexate an antifolate?

Methotrexate is an antimetabolite of the antifolate type. It is thought to affect cancer and rheumatoid arthritis by two different pathways. For cancer, methotrexate competitively inhibits dihydrofolate reductase (DHFR), an enzyme that participates in the tetrahydrofolate synthesis.

Is doxorubicin an antimetabolite?

Anthracyclines are anti-tumor antibiotics that interfere with enzymes involved in copying DNA during the cell cycle. Examples of anthracyclines include: Daunorubicin. Doxorubicin (Adriamycin®)

Is hydroxychloroquine an antimetabolite?

Plaquenil is an antimalarial medication and Rheumatrex and Trexall are antimetabolite drugs.

What are the most common side effects of methotrexate?

GI problems such as nausea and vomiting are the most common side effects associated with methotrexate, affecting between 20% and 65% of rheumatoid arthritis (RA) patients who take the drug. Up to one-third develop mouth ulcers or sores. Many also complain of headaches, fatigue and an overall “blah” feeling.

What are the side effects of methotrexate?

Methotrexate may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • dizziness.
  • drowsiness.
  • headache.
  • swollen, tender gums.
  • decreased appetite.
  • reddened eyes.
  • hair loss.

Why is methotrexate an antifolate?

The antifolate, methotrexate, tightly binds dihydrofolate reductase (DHFR) thereby inhibiting folate metabolism. Through this inhibition, thymidylate synthesis is blocked, and thus, purine biosynthesis. In addition, some amino acid synthesis is impaired through blockade of this enzyme resulting in cytotoxicity.