sulfasalazine

sulfasalazine /sul·fa·sal·a·zine/ (-sal´ah-zēn) a sulfonamide used in the treatment and prophylaxis of inflammatory bowel disease and the treatment of rheumatoid arthritis.

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sulfasalazine

[sul′fəsəlaz′ēn]

a sulfonamide, and aminosalicylic acid derivative. Also called salicylazosulfapyridine.

indications It is prescribed in the treatment of mild to moderate ulcerative colitis and as adjunctive therapy in severe cases. It is also used to treat juvenile- and adult-onset forms of rheumatoid arthritis and has investigational uses for other autoimmune disease, such as ankylosing spondylitis and Crohn's disease.

contraindications Urinary obstruction, porphyria, or known hypersensitivity to this drug, to other sulfonamide medications, or to salicylates prohibits its use. It is not given during the last trimester of pregnancy.

adverse effects Among the more serious adverse effects are crystalluria, blood dyscrasias, and severe hypersensitivity reactions. GI symptoms and anorexia commonly occur.

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sulfasalazine (sul´fsal´zēn),

n brand name: Asulfi-dine-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.

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sulfasalazine

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

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sulfasalazine

APO Sulfasalazine (CA), Azulfidine, Azulfidine EN-tabs, PMS-Sulfasalazine (CA), PMS-Sulfasalazine-E.C. (CA), SAS Tab (CA), Salazopyrin (CA) (UK), Salazopyrin EN-Tabs (CA), Sulazine (UK), Sulfazine, Sulfazine EC

Pharmacologic class: Sulfonamide

Therapeutic class: Anti-infective, GI tract anti-inflammatory, antirheumatic

Pregnancy risk category B

Action

Unknown. Thought to inhibit prostaglandin synthesis by interfering with secretions in colon and causing local anti-inflammatory action.

Availability

Tablets: 500 mg

Tablets (Azulfidine EN-tabs - delayed-release, enteric-coated): 500 mg

⊘Indications and dosages

➣ Ulcerative colitis

Adults: Initially, 1 to 2 g P.O. daily in equally divided doses q 6 to 8 hours, then 3 to 4 g P.O. daily in equally divided doses q 6 to 8 hours. For maintenance, 500 mg q 6 hours.

Children ages 6 and older: 40 to 60 mg/kg P.O. daily in three to six divided doses. For maintenance, 30 mg/kg P.O. q 6 hours in four divided doses.

➣ Acute rheumatoid arthritis

Adults: Initially, 500 mg to 1 g (delayed-release) P.O. daily for 1 week; then increase by 500 mg/day P.O. q week up to 2 g/day in two divided doses. If no benefit after 12 weeks, increase to 3 g/day given in two divided doses.

➣ Polyarticular-course juvenile rheumatoid arthritis

Children ages 6 and older: 30 to 50 mg/kg P.O. daily in two evenly divided doses. Maximum dosage is 2 g daily.

Off-label uses

• Ankylosing spondylitis
• Crohn's disease
• Psoriatic arthritis

Contraindications

• Hypersensitivity to drug, other sulfonamides, sulfonylureas, thiazides, loop diuretics, or salicylates
• Porphyria
• Marked renal or hepatic impairment
• Urinary tract or intestinal obstruction
• Pregnancy at term or when premature birth is possible
• Children younger than age 2

Precautions

Use cautiously in:
• renal or hepatic disease, bronchial asthma, G6PD deficiency, group A beta-hemolytic streptococcal infections, blood dyscrasias
• history of multiple allergies
• pregnant (before term) or breastfeeding patients
• children (use in systemic-course rheumatoid arthritis not recommended).

Administration

• Give after meals and space doses evenly to reduce GI effects.
• Give with a full glass of water.
• Administer delayed-release tablets whole. Don't let patient crush or chew them.

Route	Onset	Peak	Duration
P.O.	1.5 hr	10 hr	Unknown

Adverse reactions

CNS: headache, depression, hallucinations, insomnia, drowsiness, vertigo, fatigue, apathy, anxiety, ataxia, polyneuritis, peripheral neuropathy, seizures

CV: allergic myocarditis or pericarditis

EENT: periorbital edema, optic neuritis, transient myopia, tinnitus

GI: nausea, vomiting, abdominal pain, stomatitis, glossitis, pancreatitis, dry mouth, anorexia, pseudomembranous colitis

GU: hematuria, proteinuria, orange-yellow urine, reversible oligospermia, crystalluria, toxic nephrosis with oliguria and anuria, renal failure

Hematologic: megaloblastic anemia, agranulocytosis, aplastic anemia, thrombocytopenia, leukopenia, hemolytic anemia

Hepatic: jaundice, hepatitis, hepatocellular necrosis

Respiratory: shortness of breath, pleuritis, cyanosis, allergic pneumonitis, pulmonary infiltrates, fibrosing alveolitis

Skin: generalized skin eruption, urticaria, pruritus, alopecia, local irritation, orange-yellow skin discoloration, exfoliative dermatitis, photosensitivity reaction, erythema multiforme, epidermal necrolysis, Stevens-Johnson syndrome

Other: reversible immunoglobulin suppression, chills, drug fever, hypersensitivity reactions including anaphylaxis, serum sickness, lupus-like syndrome

Interactions

Drug-drug. Cyclosporine: increased nephrotoxicity

Folic acid: decreased folic acid absorption

Hydantoins: increased hydantoin blood level

Indomethacin, probenecid: increased sulfasalazine blood level

Iron: decreased sulfasalazine absorption

Methenamine: increased risk of crystalluria, causing serious adverse reactions

Methotrexate: increased risk of bone marrow depression

Oral anticoagulants: increased anticoagulant effect

Other anti-infectives: altered sulfasalazine metabolism

Para-aminobenzoic acid (PABA), PABA-derived local anesthetics: inhibited sulfasalazine action

Sulfonylureas: increased risk of hypoglycemia

Thiazide diuretics: increased thrombocytopenic effects

Uricosuric drugs: increased effects of these drugs

Drug-diagnostic tests. Bilirubin, blood urea nitrogen, creatinine, eosinophils, transaminases: increased levels

Granulocytes, hemoglobin, platelets, white blood cells: decreased levels

Urine glucose test: false-positive result

Drug-food. Folic acid, iron: decreased folic acid or iron absorption

Drug-herbs. Dong quai, St. John's wort: increased risk of photosensitivity

Drug-behaviors. Sun exposure: increased risk of photosensitivity

Patient monitoring

☞ Monitor CBC with white cell differential. Watch for evidence of blood dyscrasias.
☞ Stay alert for signs of erythema multiforme. Report early signs before condition can progress to Stevens-Johnson syndrome.
• Monitor patient for signs and symptoms of superinfection, including fever, tachycardia, and chills.
☞ Monitor liver function tests; watch for signs and symptoms of hepatitis.
☞ Check kidney function tests weekly. Evaluate patient's fluid intake, urine output, and urine pH. Report hematuria, oliguria, or anuria right away.
• Monitor neurologic status. Report seizures, hallucinations, or depression.
• If patient takes drug for rheumatoid arthritis, monitor therapeutic response 4 to 12 weeks after therapy begins.

Patient teaching

• Tell patient to take on regular schedule as prescribed, along with a full glass of water. Instruct him to drink plenty of fluids to minimize crystal formation in urine.
• Urge patient to complete full course of treatment, even if he feels better after a few days.
☞ Instruct patient to watch for and immediately report signs and symptoms of hypersensitivity reaction, especially rash.
☞ Tell patient drug can cause blood disorders, GI and liver problems, serious skin reactions, and other infections. Describe key warning signs and symptoms (easy bruising or bleeding, severe diarrhea, unusual tiredness, yellowing of skin or eyes, sore throat, rash, cough, mouth sores, fever). Instruct him to report these right away.
☞ Advise patient to promptly report scant or bloody urine or inability to urinate.
• Instruct patient to contact prescriber if he develops depression.
• Teach patient effective ways to counteract photosensitivity effect. Tell him that dong quai and St. John's wort increase phototoxicity risk and should be avoided during therapy.
• Inform patient that drug may discolor skin and body fluids orange-yellow and may permanently stain contact lenses.
• Advise female patient to inform prescriber if she is pregnant. Caution her not to take drug near term or when breastfeeding.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

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sulfasalazine

Therapeutics An agent used for inflammatory conditions such as ulcerative colitis and arthritis Adverse effects Headaches, N&V, abdominal pain. See AIDS.