When It Comes to Methotrexate Toxicity, Give Patients a Superior Folate

Rheumatoid arthritis (RA) is a chronic disease where the body’s immune system mistakenly attacks the joints. This causes inflammation of the joint lining. This inflammation can cause pain, stiffness, swelling and redness in and around the joints, especially in the hands and feet. People living with RA have periods of increased disease activity, called “flare-ups,” and periods of activity where symptoms fade or disappear, called “remission.” Without treatment, RA causes loss of normal movement and joint deformity. RA should be treated as early as possible to maintain joint function, help relieve symptoms, and improve quality of life. Because RA occurs throughout the body, the skin, heart, lungs, and eyes may also be affected. There are more than 200,000 new cases of RA in the US every year.

Methotrexate (MTX), a Disease-Modifying Anti-Rheumatic Drug (DMARD), is the most common treatment for people with RA. Methotrexate is one of the most commonly prescribed DMARDs because it has been proven to work well. MTX decreases the body’s autoimmune response, which means less inflammation and pain.
Although MTX is effective, it can also decrease the body’s much-needed supply of folate. Folate helps the body produce red blood cells, supports adrenal function and maintains a healthy nervous system. When the body is low in folate, the patient may experience nausea, fatigue, flu-like symptoms, stomach pain, mouth sores, hair loss, elevated liver enzyme levels, and a low number of blood cells (leukopenia and anemia).

Rheumate is a prescription medical food for the clinical dietary management of metabolic effects of methotrexate therapy.

Rheumate is a prescription medical food. The U.S. Food and Drug Administration (FDA) regulates medical foods in a separate category than drugs and supplements. Similar to drugs, medical foods help manage diseases and require physician supervision. Sound laboratory and clinical science must prove the effectiveness of a medical food. Dietary supplements are meant for healthy people and do not require a prescription. The term “food” speaks to the safety of these products because they must contain only ingredients that have been designated as GRAS (Generally Recognized as Safe), a strict food-safety standard set by the FDA.

For patients taking methotrexate, Rheumate replenishes folate by delivering a bioavailable form (L-5-methyltetrahydrofolate) that doesn’t need to be converted by the body. This is different from folic acid, which has to be converted to active folate before the body can use it. The folate in Rheumate is superior because MTX can decrease the conversion of folic acid into folate. Also, nearly half of the US population has a genetic defect (MTHFR polymorphism) that blocks the conversion of folic acid into the active form, folate.

Rheumate is a mixture of active folate (L-5-methyltetrahydrofolate), curcumin and vitamin B-12. Curcumin is a powerful antioxidant and addresses methotrexate induced oxidative stress (too many free radicals in the body). Vitamin B- 12 is added to avoid masking borderline deficiency of B-12 from taking folate supplements.
Rheumate also contains the following: microcrystalline cellulose, magnesium stearate, and silicone dioxide. The capsule contains bovine gelatin, titaniumdioxide (color), FD&C yellow 5, and FD&C green 3. The product does not contain fructose, glucose, sucrose, lactose, gluten, maltodextrin, tree nuts, peanuts, soy, or flavors.

The most common side effects are mild diarrhea, nausea and upset stomach. These are often mild and do not usually mean a patient needs to stop use.

Rheumate is not for people with allergies or hypersensitivity to any of its ingredients. Folate may interfere with absorption of tetracycline.

Prescribe one capsule by mouth once or twice daily.

Rheumate is safe to take with or without food. If patients experience indigestion, recommend that they take it with food.

If the patient misses a dose, instruct them to take it when they remember. If it is almost time for the next dose, wait and take the next dose on schedule.

If the patient is on both Rheumate and tetracycline, recommend that each is taken at least one hour apart. Sulfasalazine, phenytoin, statins and some birth control medications may lower levels of serum folate and impair utilization of folate.

Rheumate is prescription-only. The FDA regulates Rheumate as a medical food product, which must be used under physician supervision according to federal laws.