Pharm
Sulfasalazine
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Sulfasalazine
, Azulfidine
See Also
5-Aminosalicylic Acid Derivative
Mesalamine
Balsalazide
Olsalazine
Indications
Inflammatory Bowel Disease
(e.g.
Ulcerative Colitis
)
Early
Rheumatoid Arthritis
(especially seronegative)
Psoriatic Arthritis
Arthritis
in
Reiter's Syndrome
Contraindications
Significant renal dysfunction
Significant hepatic dysfunction
Bowel Obstruction
Porphyria
Sulfa Allergy
Consider
Mesalamine
(
Asacol
,
Pentasa
) as alternative
Consider slowly tapering to dose if unclear allergy
Start: 250 grams per day
Increase: 250 grams per week
Mechanism
5-Aminosalicylic Acid Derivative
which is metabolized into sulfapyridine and
Mesalamine
by colonic
Bacteria
Medications
Sulfasalazine (Azulfidine)
Available as 500 mg oral tablets
Total 4 grams is equivalent to 1.6 grams
5-ASA
Enteric-coated Sulfasalazine (Azulfidine EN Tabs)
Available as 500 mg delayed release tablets
Total 4 grams is equivalent to 1.6 grams
5-ASA
Better tolerated than standard Sulfasalazine
Dosing
Adult (
Ulcerative Colitis
)
Gene
ral
Increase slowly to lowest effective dose
Co-administer
Folic Acid
1 mg/day
Starting Protocol (example in adults)
Start: 500 mg per day
Increase: 500 mg per week up to 2 grams per day
Increase: 3 grams per day after 3 months
Maximum: 4 grams per day (2 grams twice daily) after 6 months
Active Disease (Induction)
Take 500 to 1000 mg orally four times daily (max: 4 to 6 g/day)
Maintenance
Take 500 orally four times daily (max: 2 to 4 g/day)
Dosing
Child (
Ulcerative Colitis
)
Avoid in age <2 years
Supplement
Folic Acid
Active Disease (Induction) for age 6 years and older
Give 40 to 60 mg/kg/day orally divided 3 to 6 times daily (max: 75 mg/kg/day)
Maintenance for age 6 years and older
Give 30 mg/kg/day orally divided 4 times daily with food
Adverse Effects
Gene
ral
Take
Folic Acid
1-2 mg/day
Nausea
and other Gastrointestinal Intolerance (30%)
Decreased appetite
Dyspepsia
Nausea
or
Vomiting
Consider enteric coated Azulfidine EN-tablets (better tolerated)
Neurologic adverse effects
Headache
(20%)
Dizziness
or
Lightheaded
(<20%)
Hematologic adverse effects (marrow suppression)
Folate
-inhibition
Anemia
Hemolytic Anemia
Granulocytopenia
and
Leukopenia
Thrombocytopenia
Pulmonary
Fibrosing Alveolitis
Skin rash associated with
Sulfa Allergy
Requires discontinuing medication immediately
Sexual Function
Oligospermia
(
Infertility
risk)
Renal adverse effects
Urine Discoloration
(orange)
May also discolor other body fluids (e.g. tears and
Contact Lens
es)
Micro-
Crystalluria
Risk of
Interstitial Nephritis
Avoid
Dehydration
Avoid high doses
Monitoring
Complete Blood Count
(CBC) every 2 to 4 weeks for 3 months, then every 3 to 6 months
Aspartate Aminotransferase
(AST,
SGOT
) at 2 months
Drug Interactions
Decreases other drug levels
Folic Acid
Digoxin
Cyclosporine
Serum Iron
Safety
Pregnancy Category B
However,
Folate
supplementation is critical
Unknown safety in
Lactation
Case reports of nursing infants with
Diarrhea
and bloody stools
References
Hamilton (2020) Tarascon Pocket Pharmacopoeia
(2022) Treatment of Mild to Moderate
Ulcerative Colitis
, Presc Lett, #350406
(2023) Drugs for
Inflammatory Bowel Disease
, Med Lett Drug Ther 65: 105-12
Adams (2013) Am Fam Physician 87(10): 699-705 [PubMed]
Adams (2022) Am Fam Physician 105(4): 406-11 [PubMed]
Kornbluth (2010) Am J Gastroenterol 105(3): 501-23 [PubMed]
Matteson (2000) Mayo Clin Proc 75:669-74 [PubMed]
Pincus (1999) Clin Rheumatol 17(6 Suppl 18):S2-S124 [PubMed]
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