Azulfidine Sulfasalazine

Sulfasalazine is a compound of sulfapyridine and 5-aminosalicylic acid (5-ASA) that exerts anti-inflammatory activity in the bowel and is useful in ulcerative colitis.

Its actual mechanism of action is not determined. Sulfasalazine may have direct anti-inflammatory action in the colon. It also systemically interferes with secretion by prostaglandin synthesis inhibition.

In addition, it suppresses the disease in a significant number of Rheumatoid Arthritis (RA) patients.

Sulfapyridine split off in the colon by bacterial action and absorbed systemically appears to be the active moiety (contrast ulcerative colitis, in which 5-ASA acting locally in the colon is the active component).

Generation of superoxide radicals and cytokine elaboration by inflammatory cells may be suppressed.

Efficacy of sulfasalazine in RA is modest and side effects may be unpleasant, neutropenia/thrombocytopenia occurs in about 10% patients and hepatitis is possible. 

If you are about to start a drug therapy, the risks, and benefits ratio of taking the medicine should be considered. This is a decision that your doctor will make with your active participation.

For this medicine, certain factors that may alter the drug action should be considered.

Present and past illness, drug interactions, hypersensitivity reactions, pregnancy, lactation and metabolic impairments should be considered cautiously.

Always try to answer each question appropriately asked by your physician. If you have had any allergic reaction to such medications or any other medicines, tell your doctor about that.

This is the medicine which is used irrespective of age and sex. Animal studies have shown an adverse effect but there are no adequate studies in pregnancy and lactation.

Hence, potential benefits may warrant use of the drug in pregnant women despite potential risks.

Salfasalazine has a specific therapeutic effect in inflammatory bowel disease (IBD). Having low solubility, it is poorly absorbed from the ileum.

Given during active phase of the disease, it reduces the number of stools, abdominal cramps, and fever, but is less effective than corticosteroids; may be employed for mild to moderate exacerbation.

A dose of 3-4 g/day induces remission over a few weeks in many patients, but relapses are common after the stoppage.

Maintenance therapy with 1.5-2 g/day has been found to postpone relapse in the majority, but not all cases.

In order to treat rheumatoid arthritis effectively, an enteric-coated tablet of 500 mg is given to adults at initial stage once in a day for the 1st week increased by 500 mg every week.

3 g daily in 2-4 divided doses is the maximum therapeutic dose.

For polyarticular juvenile rheumatoid arthritis, children of above 6 years are given 30-50 mg/kg/day in 2 divided doses.

Begin treatment with ¼ to 2/3 of expected maintenance dose and increase weekly to reach maintenance dose in 1 month. Here, the maximum therapeutic dose is 2 g daily.

You should avoid the use of such medication in hepatic impairment.

Some important measures should be taken if you feel any discomfort following any drug therapy.

In case of such drug therapy, you may not need to discontinue the therapy as there are least chances of drug toxicity.

But you should not delay consulting with your physician in case of extreme unwanted effects such as a headache, anorexia, nausea, vomiting, diarrhea, abdominal discomfort, photosensitivity, crystalluria, reversible oligospermia, alopecia etc.

Moreover, yellow-orange staining of contact lens, skin, urine and other body fluids may occur affecting about 1/3rd patients.

Certain drugs should not be used concurrently with such medications. It is always recommended to consult with your doctor if you are in need of some drugs for another health problem.

Sometimes it is must to avoid the particular medicines during a drug therapy in order to remain out of danger of serious drug reactions.

Rifampicin and ethambutol reduce the efficacy of sulfasalazine by decreasing its plasma concentration. This drug also interferes with absorption of folic acid.

Increased haematological toxicity has been noticed with azathioprine.

Discuss with your doctor elaborately if the drugs may show any reaction with some foods, tobacco or alcohol. Try not to fail to take the drug according to the doctor’s directions.

On the contrary, the presence of some medical problems may affect the desired plasma concentration as well as the duration of action of the drug.

Make sure you tell your doctor if you have any other medical problems. You should also know in which conditions the use of sulfasalazine is contraindicated.

Hypersensitivity to sulphonamides or salicylates, porphyria, below 2 years of age, intestinal or urinary obstruction, blood dyscrasia, history of leucopenia with gold therapy, hepatic/renal impairment and G6PD deficiency are the alarming conditions which become worse if sulfasalazine is used.

There are some unwanted side-effects associated with each drug that usually do not need medical attention.

These side-effects usually go away during the treatment episode as your body adjusts to the medicine.

Additionally, your health care professional may advise you about the ways how to prevent or reduce those unwanted side-effects.

Sometimes you may need to consult with the doctor if you feel any serious discomfort. The sulfapyridine moiety only serves to carry 5-ASA to the colon without being absorbed proximally.

However, most of the released sulfapyridine is absorbed in the colon and is responsible for adverse effects like rashes, fever, joint pain, haemolysis and blood dyscrasias.

Nausea, vomiting, headache. Malaise and anaemia are other frequent dose-related side effects. Oligozoospermia and male infertility have been reported.

Sulfasalazine interferes with folate absorption. That’s why folic acid supplementation should always be given during its use.

Potentially fatal conditions such as severe hypersensitivity reactions, blood dyscrasias, renal and hepatic toxicity, fibrosing alveolitis etc. may occur which warrant emergency medical care immediately.