Sulfasalazine

trade name: Asulfidine-EN-Tabs, Azulfidine; drug class: sulfonamide derivative with antiinflammatory action; action: acts as a prodrug to deliver sulfapyridine and mesalamine (5-aminosalicylic acid) to the colon; uses: treatment of ulcerative colitis, Crohn’s disease.

Brand names: Azulfidine®Azulfidine® En-Tabs®Sulfazine®Sulfazine® EC

Chemical formula:

Drug Forms:
• Sulfasalazine Gastro-resistant tablet (below)
• Sulfasalazine tablets or enteric-coated tablets
• Sulfasalazine Oral tablet

Español:
• Sulfasalazina, Tabletas gastrorresistentes
• Tabletas de sulfasalazina o tabletas de sulfasalazina con recubrimiento entérico
• Sulfasalazina, Tableta oral

Sulfasalazine Gastro-resistant tablet

What is this medicine?

SULFASALAZINE (sul fa SAL a zeen) is for ulcerative colitis and certain types of rheumatoid arthritis.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•asthma
•blood disorders or anemia
•glucose-6-phosphate dehydrogenase (G6PD) deficiency
•intestinal obstruction
•kidney disease
•liver disease
•porphyria
•urinary tract obstruction
•an unusual reaction to sulfasalazine, sulfa drugs, salicylates, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a full glass of water. Follow the directions on the prescription label. If the medicine upsets your stomach, take it with food or milk. Do not crush or chew the tablets. Swallow the tablets whole. Take your medicine at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your doctor's advice.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed. While this drug may be prescribed for children as young as 6 years for selected conditions, precautions do apply.

Patients over 65 years old may have a stronger reaction and need a smaller dose.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

•digoxin
•folic acid

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. You will need frequent blood and urine checks.

This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.

Drink plenty of water while taking this medicine.

Tell your doctor if you see the tablet in your stools. Your body may not be absorbing the medicine.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•fever, chills, or any other sign of infection
•painful, difficult, or reduced urination
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•severe stomach pain
•unusual bleeding or bruising
•unusually weak or tired
•yellowing of the skin or eyes

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•headache
•loss of appetite
•nausea, vomiting
•orange color to the urine
•reduced sperm count

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A combination of sulfapyridine and salicylic acid, used in the treatment and prophylaxis of ulcerative colitis. Previously called salicylazosulfapyridine.

Sulfasalazine

Systematic (IUPAC) name
6-oxo-3-(2-[4-(N-pyridin-2-ylsulfamoyl)phenyl]hydrazono)cyclohexa-1,4-dienecarboxylic acid
Identifiers
CAS number	599-79-1
ATC code	A07EC01
PubChem	5384001
DrugBank	APRD00152
Chemical data
Formula	C18H14N4O5S
Mol. mass	398.394 g/mol
Pharmacokinetic data
Bioavailability	<15%
Metabolism	?
Half life	5-10 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	oral
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Sulfasalazine (brand name Azulfidine in the U.S., Salazopyrin in Europe) is a sulfa drug, a derivative of Mesalazine (5-aminosalicylic acid abbreviated as 5-ASA), used primarily as an anti-inflammatory agent in the treatment of inflammatory bowel disease as well as for rheumatoid arthritis. It may be abbreviated SSZ. It is not a pain killer.

Contents 1 Indications 2 Mode of action 2.1 Bowel disease 2.2 Arthritis 3 Side effects 4 References 5 External links

Indications

See also Disease-modifying antirheumatic drugs for its role in rheumatoid arthritis

Sulfasalazine is mainly used for treatment of inflammatory bowel disease, including ulcerative colitis and Crohn's disease. It is also effective in several types of arthritis, particularly rheumatoid arthritis.

According to the findings of a case series published in BMC Musculoskeletal Disorders, the use of sulfasalazine in the treatment of inflammatory arthritis can result in serious hepatotoxicity - an adverse effect which appears to be ‘under-appreciated’ in practice.

However, in recent British research involving animal studies, and more recently, human trials for the treatment of chronic alcoholics, sulfasalazine has been found to reverse the scarring associated with cirrhosis of the liver. Apparently, cells called myofibroblasts, that cause scar tissue to form in a diseased liver, also give off proteins that prevent the breakdown of the scar tissue. Sulfasalazine appears to retard the secretion of these proteins.

A study at University of Newcastle found that the drug may also act to aid the healing of cirrhosis of the liver.^[1]

It is usually not given to children under 2 years of age.

The use of sulfasalazine has declined due mainly to the fact that it yields the metabolite sulfapyridine which gives rise to side-effects such as agranulocytosis and hypospermia. However, the other metabolite of sulfasalazine, 5-aminosalicylic acid (5-ASA) is attributed to the drug's therapeutic effect. Therefore, 5-ASA and other derivatives of 5-ASA, are now usually preferred and given alone (as mesalazine), despite their increased cost, due to their more favourable side-effect profile.

Sulfasalazine has also been used successfully to treat cases of idiopathic urticaria that do not respond to antihistamines. (McGirt et al, 2006)

Mode of action

Sulfasalazine, and its metabolite 5-ASA, are poorly absorbed from the gut. Its main mode of action is therefore believed to be inside the intestine.

Bowel disease

In Crohn's disease and ulcerative colitis, it is thought to be an antinflammatory drug that is essentially providing topical relief inside the intestine. It does this via a number of mechanisms such as reducing the synthesis of inflammatory mediators known as eicosanoids and inflammatory cytokines. However, unlike glucocorticoids (another class of drug used in the treatment in inflammatory bowel disease), sulfasalazine has no immunosuppressant action.

Arthritis

When treatment for arthritis is successful, pain, joint swelling and stiffness will be reduced and this may slow down or stop the development of joint damage. The precise reasons why sulfasalazine is effective in various forms of arthritis is not clearly understood.

Because sulfasalazine and its metabolite 5-ASA are poorly absorbed into the bloodstream, it is surprising that the drug is effective against symptoms outside of the intestine. One possible explanation is that, given that ulcerative colitis produces arthritic symptoms, the arthritic symptoms are actually a product of unrecognized ulcerative colitis, which is effectively treated with sulfazalazine.

The other metabolite, sulfapyridine, is absorbed into the blood, and is believed to be the source of the side-effects discussed below. It is possible that the sulfapyridine is responsible for some of the anti-arthritic effects of sulfasalazine.

Side effects

Refer to external links for a full listing of known side effects.

Sulfasalazine in rare cases can cause severe depression in young males.^{[citation needed]}

Sulfsalazine metabolizes to sulfapyridine. Serum levels should monitored every three months, and more frequently at the outset. Serum levels above 50 micrograms/L are associated with side effects.

Immune thrombocytopenia has been reported.^[2]

References

1. ^ "BBC NEWS". http://news.bbc.co.uk/1/hi/health/5382172.stm. 
2. ^ Cantarini L, Tinazzi I, Biasi D, Fioravanti A, Galeazzi M (June 2007). "Sulfasalazine-induced immune thrombocytopenia". Postgraduate medical journal 83 (980): e1. doi:10.1136/pgmj.2006.055194. PMID 17551063. 

3. McGirt, L.Y., Vasagar, K., Gober, L.M., Saini, S.S., Beck, L.A. (2006) Successful treatment of recalcitrant chronic idiopathic urticaria with sulfasalazine. Arch Dermatol, 142:1337-1342.

External links

• National Rheumatoid Arthritis Society (NRAS) Information on Disease Modifying drugs such as Sulphasalazine
• New Zealand Rheumatology Assoc., Sulphasalazine (Salazopyrin)
• Web MD
• Upjohn FDA Label
• Optimal Dosing of 5-Aminosalicylic Acid: 5 Decades of Choosing Between Politicians

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