What You Need to Know About Methotrexate

by Lene Andersen, MSW Patient Advocate

When you first get diagnosed with rheumatoid arthritis (RA) there is a very good chance that you will leave your doctor’s office with a prescription for methotrexate to treat your condition. This medication is a disease modifying antirheumatic drugs (DMARDs) and considered the gold standard for treating RA as well as other types of autoimmune arthritis. It may be prescribed on its own or in combination with other drugs.

Cancer cell and DNA strand.

From cancer treatment to RA

Methotrexate was developed in the 1940s to treat childhood leukemia. In the mid-1980s, several studies using placebo controls demonstrated that methotrexate could also be an effective treatment for RA. Methotrexate quickly received U.S. Food and Drug Administration (FDA) approval to treat RA and came to be considered the standard of care by the early 1990s. Up to 90 percent of people with RA have taken methotrexate at some point in their treatment career.

Worried woman.

Methotrexate is a chemotherapy drug?

You might feel anxious when you hear that methotrexate a chemotherapy drug. Many drugs work for more than one condition and in different doses. When used to treat RA, methotrexate is given in doses that are 100 times less than what is used to treat cancer. This medication has been used for autoimmune arthritis for three decades and is considered one of the safest medications, with a few caveats which will be discussed later in this slideshow.

Prescription pills and pill bottle.

How to take methotrexate

Rheumatologists will usually start you on oral methotrexate and the beginning dose tends to be between 7.52 to 10 mg once a week. That’s three or four small tablets. It can take up to three months for methotrexate to really start working. If it is not controlling your symptoms as well as you and your doctor had hoped, it’s common to increase the oral dose up to 25 mg. Your doctor may also choose to switch you to a subcutaneous injection, which they will teach you how to do yourself.

Prescription medications.

Use care when taking methotrexate

Methotrexate works for RA because it suppresses your immune system and therefore also the autoimmune response that causes RA inflammation. Make sure you are careful around infection and during flu season — as much as possible, stay away from sick people and wash your hands frequently. You should also be careful when taking methotrexate tablets and it’s important that you only take them once a week. The pills look quite similar to a number of other tablets, which can cause an accidental overdose.

Blood test vials.

Why blood tests are important

When you take methotrexate, your doctor will order blood tests every six weeks to check your liver function. The drug works by triggering your body’s cells to release a substance called adenosine, which blocks inflammation. However, it can also lead to scar tissue in the liver, which may, rarely, develop into liver disease. Your doctor will likely prescribe folic acid, which can prevent scar tissue and other side effects. Still, keeping an eye on your liver function is essential.

Young woman with headache drinking a glass of water.

Common side effects

Although methotrexate is considered safe and usually is well tolerated, it is common to have some side effects after taking the medication, called the “methotrexate hangover” in the RA community. For a day or two after taking your dose, you may be nauseated, dizzy, and have headaches. Eating bland foods and taking it easy is usually enough to cope.

Woman with upset stomach making a face.

Dealing with gastrointestinal side effects

If you have a hard time with GI side effects, there are steps you can take to help reduce the symptoms. One is to split your dose, taking half of your methotrexate tablets in the morning and the other half in the evening. As well, taking them with food will make it easier on your stomach. Anti-nausea drugs, either over-the-counter or prescription, may also help. You can also talk to your doctor about switching to injectable methotrexate, which often reduces extra intestinal side effects.

Mouthwash on bathroom shelf.

Mouth ulcers

Some people develop mouth ulcers when taking methotrexate, especially if they are on higher doses. This is caused by mucositis, an inflammation of the mucous membrane that can cause sores in your mouth. These can be prevented by taking folic acid, but if they do develop, rinsing with a salt water solution or a special mouthwash containing lidocaine can ease symptoms.

Hair loss, hair in hairbrush.

Hair Loss

Although quite rare, methotrexate may cause hair loss. This medication works by stopping cells from growing, which includes the cells that cause inflammation. Unfortunately, it can also affect the hair follicles in about one to three percent of people taking the medication. The effect may be more of a thinning rather than your hair falling out in chunks. As with all side effects, you have to weigh the pros and cons and make the decision about treatment that is right for you.

Green folic acid capsule.

The role of folic acid

As you have seen, folic acid is an important companion when taking methotrexate. Folic acid is a synthetic form of vitamin B9 and may be prescribed as 1 mg a day or 5 mg once a week. Some rheumatologists don’t prescribe folic acid until the person experiences certain side effects. One study showed that taking folic acid reduced the experience of side effects by up to 26 percent. It’s important to not take too much folic acid, as it can mask a B12 deficiency.

Alcohol free zone sign on pavement.

Alcohol and methotrexate

Because of the potential impact of methotrexate on the liver, many rheumatologists advise against drinking alcohol while taking this medication. This can vary from not at all (primarily in the United States), to only once in a blue moon (in Europe). The American College of Rheumatology recommends against drinking alcohol on this medication, but some doctors allow it very occasionally. If you have a history of alcohol abuse or have liver disease, methotrexate is generally not recommended.

Birth control methods.

Don’t get pregnant

Although methotrexate tends to be well tolerated by the person taking it, it is not tolerated at all by a developing fetus. This medication can cause severe birth defects and it is essential that you not get pregnant while taking it. Doctors usually recommend double methods of birth control (for instance, the pill and a condom). You should be off methotrexate for three months before trying to conceive. If you do want to start a family, talk to your rheumatologist.

Woman standing on rock with outreached arms near beautiful mountain lake.

So, why take methotrexate?

With all this potential for side effects and having to be careful when taking methotrexate, you may very well ask yourself why you should take it at all. RA is a serious illness that, untreated, has very real potential to cause damage to joints, internal organs, and other systems in your body. Methotrexate is one of the medications that suppresses RA and therefore protects your ability to live your life to the fullest.

Lene  Andersen, MSW
Meet Our Writer
Lene Andersen, MSW

Lene Andersen is an author, health and disability advocate, and photographer living in Toronto. Lene (pronounced Lena) has lived with rheumatoid arthritis since she was four years old and uses her experience to help others with chronic illness. She has written several books, including Your Life with Rheumatoid Arthritis: Tools for Managing Treatment, Side Effects and Pain, and 7 Facets: A Meditation on Pain, as well as the award-winning blog, The Seated View. Lene serves on HealthCentral's Health Advocates Advisory Board, and is a Social Ambassador for the RAHealthCentral on Facebook page, facebook.com/rahealthcentral. She is also one of HealthCentral's Live Bold, Live Now heroes — watch her incredible journey of living with RA.