How Does Methotrexate Work?

Methotrexate works by inhibiting an enzyme known as dihydrofolic acid reductase (also known as dihydrofolate reductase). This enzyme is important for transforming an inactive form of folic acid into the active form, which is necessary to make some of the building blocks needed for DNA production. By inhibiting this enzyme, methotrexate interferes with a cell's ability to repair and replicate (copy) itself.
Although this drug can damage healthy cells as well as unhealthy cells, it tends to target rapidly replicating cells, such as cancer cells and bone marrow cells.
It is not entirely clear how methotrexate works to treat rheumatoid arthritis, although it is thought to work by affecting the immune system.

When and How Do I Take It?

Considerations to keep in mind during treatment with methotrexate include the following:
  • The medication comes in the form of a tablet and an injection. The tablet form is taken by mouth, and the injectable form can be injected into a muscle, artery, vein, or the space around the spinal cord -- or injected just under the skin.
  • Methotrexate can be taken with or without food.
  • It does not matter what time(s) of day you take this medication. However, it should be taken at the same time each day or each week.
  • For methotrexate to work properly, you have to take it as prescribed.

Dosing Information for Methotrexate

The dose of this medication that your healthcare provider recommends will vary, depending on several factors, such as:
  • The medical condition being treated
  • Your age and weight
  • How you tolerate this medication.
(Click Methotrexate Dosage to learn more.)
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Methotrexate Drug Information

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