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Understanding Rheumatoid Arthritis Medications (cont.)

Leflunomide (Arava), Methotrexate (Rheumatrex, Trexall), Penicillamine (Cuprimine), and Sulfasalazine (Azulfidine)

Leflunomide (Arava)

  • Who should not use this medication: People with the following conditions should not use leflunomide:
    • People with allergy to leflunomide
    • Women who are pregnant or breastfeeding; or who plan to become pregnant soon
    • Sexually active men who are not using contraception
    • Alcoholism
    • Immune deficiency syndromes
    • Liver failure
  • Use: Leflunomide is taken as an oral tablet.
  • Drug or food interactions: Cholestyramine (Questran) reduces the amount of leflunomide in the blood, thereby decreasing effectiveness. This medication is used to more rapidly eliminate leflunomide from the body if serious side effects are experienced. Rifampin (Rifadin, Rimactane) may increase leflunomide's risk of toxicity. Leflunomide may increase the level of warfarin (Coumadin) in the blood and the risk for bleeding. Some vaccinations are not recommended while taking leflunomide.
  • Side effects: Effective birth control is essential while taking leflunomide. This drug may cause birth defects if it is taken by the mother during pregnancy or by the father during the time of conception. Individuals with kidney or liver disease may need lower doses. Leflunomide may cause high blood pressure or worsen preexisting high blood pressure. Common side effects include stomach pain and diarrhea.

Methotrexate (Rheumatrex, Trexall)

  • Who should not use this medication: People with the following conditions should not take methotrexate:
    • Allergy to methotrexate
    • Alcoholism
    • Liver or kidney failure
    • Immune deficiency syndromes
    • Low blood cell counts
    • Pregnancy
  • Use: Methotrexate is taken orally or as an injection once per week. It is the major DMARD to treat RA and the standard to which other treatments are compared.
  • Drug or food interactions: NSAIDs (Motrin, Advil, Aleve, aspirin) may increase toxicity. Folic acid deficiency may worsen side effects of methotrexate. To lessen GI toxicity, daily administration of low dose folic acid (1-2 mg) is recommended.
  • Side effects: To guard against problems, kidney and liver function are monitored on a regular basis, as are blood cell counts. Methotrexate may cause toxic effects on blood, kidneys, liver, lungs, and gastrointestinal and nervous systems.

Penicillamine (Cuprimine)

  • Who should not use this medication: People with the following conditions should not use penicillamine:
    • Allergy to penicillamine
    • Aplastic anemia or agranulocytosis
    • Pregnancy
  • Use: Penicillamine is taken orally at least one hour before or two hours after meals. Penicillamine may take many months before a benefit is seen. It is rarely used to treat RA today.
  • Drug or food interactions: Penicillamine may increase bone marrow toxicity when used with other drugs that depress bone marrow function. When used with gold salts (auranofin [Ridaura], aurothioglucose [Solganal]) or hydroxychloroquine (Plaquenil), penicillamine may increase the risk for skin rash, bone marrow toxicity, and decreased blood cell counts. Vitamins containing iron, sucralfate, or antacids should not be taken within two hours of taking penicillamine, since they decrease its absorption.
  • Side effects: Penicillamine must be used with caution in individuals who are allergic to penicillin or who have kidney impairment. Penicillamine may decrease blood cell counts. Common side effects include nausea, vomiting, stomach pain, and diarrhea. Sense of taste may be impaired. Contact a doctor if any of the following occur:
    • Wheezing or breathing troubles
    • Unexplained fever
    • Sore throat
    • Unusual bleeding or bruising
    • Vision changes
    • Rash
    • Itching

Sulfasalazine (Azulfidine)

  • Who should not use this medication: People with the following conditions should not use sulfasalazine:
    • Allergy to sulfa drugs, aspirin, or aspirin-like products (NSAIDs)
    • Active peptic ulcer disease
    • Severe kidney failure
  • Use: Sulfasalazine is taken orally in varying doses with food.
  • Drug or food interactions: Sulfasalazine may decrease warfarin (Coumadin) absorption, thereby decreasing warfarin effectiveness. Sulfasalazine may increase the risk of bleeding when administered with other drugs that alter blood coagulation (for example, heparin [Hep-Lock]).
  • Side effects: Sulfasalazine may cause the following:
    • Toxicity to blood cells
    • Nausea
    • Vomiting
    • Abdominal cramping
    • Constipation
Medically Reviewed by a Doctor on 7/14/2016

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