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Look Up > Drugs > Sulfasalazine
Sulfasalazine
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(sul fa SAL a zeen)

U.S. Brand Names
Azulfidine® EN-tabs®; Azulfidine® Tablets

Generic Available

Yes


Canadian Brand Names
Apo®-Sulfasalazine; PMS-Sulfasalazine; Salazopyrin®; Salazopyrin EN-Tabs®; S.A.S™

Synonyms
Salicylazosulfapyridine

Pharmacological Index

5-Aminosalicylic Acid Derivative


Use

Management of ulcerative colitis; enteric coated tablets are used for for rheumatoid arthritis in patients who inadequately respond to analgesics and NSAIDs


Pregnancy Risk Factor

B/D (at term)


Contraindications

Hypersensitivity to sulfasalazine, sulfa drugs, or any component; porphyria, GI or GU obstruction; hypersensitivity to salicylates; children <2 years of age


Warnings/Precautions

Use with caution in patients with renal impairment; impaired hepatic function or urinary obstruction, blood dyscrasia, severe allergies or asthma, or G-6-PD deficiency; may cause folate deficiency (consider providing 1 mg/day folate supplement)


Adverse Reactions

>10%:

Central nervous system: Dizziness, headache (33%)

Dermatologic: Photosensitivity

Gastrointestinal: Anorexia, nausea, vomiting, diarrhea (33%)

Genitourinary: Reversible oligospermia (33%)

<3%:

Dermatologic: Urticaria/pruritus (<3%)

Hematologic: Hemolytic anemia (<3%), Heinz body anemia (<3%)

<0.1%: Lyell's syndrome, Stevens-Johnson syndrome, thyroid function disturbance, crystalluria, granulocytopenia, leukopenia, thrombocytopenia, aplastic anemia, jaundice, interstitial nephritis, acute nephropathy, hematuria, serum sickness-like reactions


Overdosage/Toxicology

Symptoms of overdose include drowsiness, dizziness, anorexia, abdominal pain, nausea, vomiting, hemolytic anemia, acidosis, jaundice, fever, agranulocytosis; the aniline radical is responsible for hematologic toxicity

High volume diuresis may aid in elimination and prevention of renal failure


Drug Interactions

Decreased effect of iron, digoxin, folic acid, and, as with other sulfa drugs, PABA or PABA metabolites of drugs (ie, procaine, proparacaine, tetracaine)

Increased effect of oral anticoagulants, methotrexate, and oral hypoglycemic agents as with other sulfa drugs


Stability

Protect from light; shake suspension well


Mechanism of Action

Acts locally in the colon to decrease the inflammatory response and systemically interferes with secretion by inhibiting prostaglandin synthesis


Pharmacodynamics/Kinetics

Absorption: 10% to 15% of dose is absorbed as unchanged drug from the small intestine

Distribution: Small amounts appear in feces and breast milk

Metabolism: Following absorption, both components are metabolized in the liver; split into sulfapyridine and 5-aminosalicylic acid (5-ASA) in the colon

Half-life: 5.7-10 hours

Elimination: Primary excretion in urine (as unchanged drug, components, and acetylated metabolites)


Usual Dosage

Oral:

Adults: Initial: 1 g 3-4 times/day, 2 g/day maintenance in divided doses; may initiate therapy with 0.5-1 g/day enteric-coated tablets

Dosing interval in renal impairment:

Clcr 10-30 mL/minute: Administer twice daily

Clcr <10 mL/minute: Administer once daily

Dosing adjustment in hepatic impairment: Avoid use


Dietary Considerations

Since sulfasalazine impairs folate absorption, consider providing 1 mg/day folate supplement.


Mental Health: Effects on Mental Status

Dizziness is common; sulfonamides reported to cause restlessness, irritability, depression, euphoria, disorientation, panic, hallucinations, and delusions


Mental Health: Effects on Psychiatric Treatment

Photosensitivity is common; use caution with concurrent psychotropics; may cause leukopenia; caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Do not crush, chew, or dissolve coated tablets. Shake suspension well before use. Do not take on an empty stomach or with antacids. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake) to prevent kidney damage. Increased dietary iron may be recommended. You may experience nervousness or dizziness (use caution when driving or engaging in hazardous activities until response to drug is known). You may experience photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). Orange-yellow color of urine, sweat, tears is normal and will stain contact lenses and clothing. Report rash, persistent nausea or anorexia, or lack of improvement in symptoms (after 1-2 months). Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Drug commonly imparts an orange-yellow discoloration to urine and skin


Dosage Forms

Tablet: 500 mg

Tablet, enteric coated: 500 mg


References

American College of Rheumatology Ad Hoc Committee on Clinical Guidelines, "Guidelines for the Management of Rheumatoid Arthritis," Arthritis Rheum, 1996, 39(5):713-22.

Ardizzone S and Porro GB, "A Practical Guide to the Management of Distal Ulcerative Colitis," Drugs, 1998, 55(4):519-42.

Gabay C, DeBandt M, and Palazzo E, "Sulfasalazine-Related Life-threatening Side Effects: Is N-acetylcysteine of Therapeutic Value?" Clin Exp Rheumatol, 1993, 11(4):417-20.

Giannini EH and Cawkwell GD, "Drug Treatment in Children With Juvenile Rheumatoid Arthritis," Pediatr Clin North Am, 1995, 42(5):1099-125.

Haines JD, Jr, "Hepatotoxicity After Treatment With Sulfasalazine," Postgrad Med, 1986, 79(6):193-4, 197-8.

Jick H, Myers MW, and Dean AD, "The Risk of Sulfasalazine- and Mesalazine-Associated Blood Disorders," Pharmacotherapy, 1995, 15(2):176-81.

Jullien D, Wokenstein P, Roupie E, et al, "Toxic Epidermal Necrolysis After Sulfasalazine Treatment of Mild Psoriatic Arthritis: Warning on the Use of Sulfasalazine for a New Indication," Arthritis Rheum, 1995, 38(4):573.

Kirschner BS, "Inflammatory Bowel Disease in Children," Pediatr Clin North Am, 1988, 35(1):189-208.

O'Dell JR, "Triple Therapy With Methotrexate, Sulfasalazine, and Hydroxychloroquine in Patients With Rheumatoid Arthritis," Rheum Dis Clin North Am, 1998, 24(3):465-77.

Peppercorn MA, "Sulfasalazine: Pharmacology, Clinical Use, Toxicity, and Related New Drug Development," Ann Intern Med, 1984, 101(3):377-86.

van Rossum MA, Fiselier TJ, Franssen MJ, et al, "Sulfasalazine in the Treatment of Juvenile Chronic Arthritis: A Randomized, Double-Blind, Placebo-Controlled, Multicenter Study. Dutch Juvenile Chronic Arthritis Study Group," Arthritis Rheum, 1998, 41(5):808-16.

Veale DJ, Ho M, and Morley KD, "Sulfasalazine-Induced Lupus in Psoriatic Arthritis," Br J Rheumatol, 1995, 34(4):383-4.


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