Medications and Drugs
Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD
GENERIC NAME: sulfasalazine
BRAND NAME: Azulfidine
DRUG CLASS AND MECHANISM: Sulfasalazine is a drug that is used primarily for
treating ulcerative colitis. It is a prodrug, that is, it is not active in its
ingested form. It is broken down by bacteria in the colon into 5-aminosalicylic
acid (5-ASA), and sulfapyridine. (5-ASA is also marketed as mesalamine
(Lialda,
Rowasa, Pentasa, Canasa Apriso, and Asacol.) The 5-ASA has therapeutic benefit,
but it is not clear if sulfapyridine adds any additional therapeutic benefit.
The inflammation of ulcerative colitis and other inflammatory diseases is
caused, in part, by excessive production of chemicals (for example, prostaglandins)
that produce inflammation. Prostaglandins are produced by two enzymes,
cyclooxygenase and lipoxygenase, and these enzymes are over-active in
individuals with ulcerative colitis. 5-ASA may reduce inflammation by blocking
the activity of cyclooxygenase and lipoxygenase thereby reducing the production
of prostaglandins. Sulfasalazine was approved by the FDA in 1950.
PRESCRIPTION: Yes
GENERIC AVAILABLE: Yes
PREPARATIONS: Tablets: 500 mg.
STORAGE: The tablets should be kept at room temperature, 15-30 C (59-86 F).
PRESCRIBED FOR: Sulfasalazine is used for the treatment of mild to severe
ulcerative colitis, and treatment of rheumatoid arthritis. It has also been used
"off label" (unapproved by the FDA) for Crohn's disease and ankylosing
spondylitis.
DOSING: Adult doses range from 1000 mg to 4000 mg daily. Sulfasalazine is
administered 2 to 4 times daily depending on the disease for which it is used.
Sulfasalazine should be taken with a full glass of water after meals or with
food to minimize upset stomach. Patients with kidney diseases may need to use
lower doses of sulfasalazine.
DRUG INTERACTIONS: Sulfasalazine may cause reduced absorption of folic acid
and digoxin (Lanoxin). Reduced folic acid absorption may cause folic acid deficiency and
result in anemia. Reduced digoxin absorption may reduce the effectiveness of
digoxin. Sulfapyridine (a byproduct of sulfasalazine) is a sulfonamide, and
sulfonamides increase blood levels of methotrexate
(Rheumatrex, Trexall), resulting in increased
methotrexate toxicity. Conversely, methotrexate can increase the occurrence of
the anemia caused by sulfonamides because methotrexate also causes folic acid
deficiency. Sulfonamides can increase the risk of kidney damage from
cyclosporine by an unknown mechanism. They also may increase the blood glucose
lowering effect of oral anti-diabetic drugs and potentially cause excessive
reductions in blood sugar (hypoglycemia) by decreasing elimination of
anti-diabetic drugs by the liver and elevating the levels of the anti-diabetic
drugs in the blood.
Combining 5-ASA with drugs that affect kidney function such as nonsteroidal
antiinflammatory drugs, for example, ibuprofen (Advil), may increase the likelihood of
kidney dysfunction. Concurrent use of 5-ASA and 6-mercaptopurine or azathioprine
(Imuran) may increase the likelihood of blood disorders. 5-ASA may increase the
blood thinning effect of warfarin (Coumadin).
PREGNANCY: In hundreds of pregnant women with ulcerative colitis or Crohn's
disease treated with sulfasalazine, there has been no increase in the risk of
fetal malformations relative to other women with these illnesses who have not
been treated with sulfasalazine. Additionally, there have not been ill effects
on pregnant animals given high doses of sulfasalazine. Thus, sulfasalazine may
be used during pregnancy if the physician feels the benefit outweighs the
possible risk.
It should also be noted, however, that sulfasalazine may reduce sperm count
and sperm function in men. These effects are reversible upon stopping the drug.
NURSING MOTHERS: Caution should be exercised by women who are nursing their
infants. Sulfasalazine and its constituents are secreted into
breast milk. There
is a small risk that sulfapyridine (a byproduct of sulfasalazine) may displace
bilirubin from albumen in the blood of infants and cause jaundice.
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
- Drug Interactions - Learn about potential drug interactions you may be exposed to. Drug interactions can occur with prescription drugs, OTC medication, vitamins, herbs, and supplements.
- Rheumatoid Arthritis - Learn more about rheumatoid arthritis, an autoimmune disease that causes chronic joint inflammation, which has symptoms that include stiffness, fever, muscle and joint aches, loss of appetite, and fatigue. Treatment of rheumatoid arthritis incorporates the use of first-line drugs (aspirin and corticosteroids for pain and inflammation) and second-line drugs (methotrexate and hydroxychloroquine to prevent joint destruction and promote remission).
- mesalamine, Pentasa, Rowasa, Asacol, Lialda, Canasa - Information about mesalamine - 5-aminosalicylic acid (Pentasa, Rowasa, Asacol, Lialda, Canasa), a drug used for the treatment of mild to moderately severe ulcerative colitis.
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