Sulfasalazine

Aka: Sulfasalazine, Azulfidine

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II. Indications

  1. Inflammatory Bowel Disease (e.g. Ulcerative Colitis)
  2. Rheumatoid Arthritis (especially seronegative)
    1. Second-line agent in combination with Methotrexate and Hydroxychloroquine
  3. Psoriatic Arthritis
  4. Arthritis in Reiter's Syndrome

III. Contraindications

  1. Significant renal dysfunction
  2. Significant hepatic dysfunction
  3. Bowel Obstruction
  4. Porphyria
  5. G6PD Deficiency
    1. Risk of Hemolysis
    2. Screen for G6PD Deficiency before dosing
  6. Sulfa Allergy
    1. Consider Mesalamine (Asacol, Pentasa) as alternative
    2. Consider slowly tapering to dose if unclear allergy
      1. Start: 250 grams per day
      2. Increase: 250 grams per week

IV. Mechanism

  1. Derivative of 5-Aminosalicylic Acid (synthetic salicylic acid)
  2. Prodrug, metabolized into sulfapyridine and Mesalamine by colonic Bacteria
    1. Ideal location for activation in Inflammatory Bowel Disease (esp. Ulcerative Colitis)
  3. Active at connective tissues containing elastin (including those affected by Rheumatoid Arthritis)
    1. Metabolites have antiinflammatory activity via inhibition of cyclooxygenase and Prostaglandin production

V. Medications

  1. Sulfasalazine (Azulfidine)
    1. Available as 500 mg oral tablets
    2. Total 4 grams is equivalent to 1.6 grams 5-ASA
  2. Enteric-coated Sulfasalazine (Azulfidine EN Tabs)
    1. Available as 500 mg delayed release tablets
    2. Total 4 grams is equivalent to 1.6 grams 5-ASA
    3. Better tolerated than standard Sulfasalazine

VI. Dosing: Rheumatoid Arthritis

  1. Start 500 mg orally once to twice daily
  2. May titrate to 500 mg three times daily OR 1000 mg twice daily

VII. Dosing: Ulcerative Colitis in Adults

  1. General
    1. Increase slowly to lowest effective dose
    2. Co-administer Folic Acid 1 mg/day
    3. Starting Protocol (example in adults)
      1. Start: 500 mg per day
      2. Increase: 500 mg per week up to 2 grams per day
      3. Increase: 3 grams per day after 3 months
      4. Maximum: 4 grams per day (2 grams twice daily) after 6 months
  2. Active Disease (Induction)
    1. Take 500 to 1000 mg orally four times daily (max: 4 to 6 g/day)
  3. Maintenance
    1. Take 500 orally four times daily (max: 2 to 4 g/day)

VIII. Dosing: Ulcerative Colitis in Children

  1. Avoid in age <2 years
  2. Supplement Folic Acid
  3. Active Disease (Induction) for age 6 years and older
    1. Give 40 to 60 mg/kg/day orally divided 3 to 6 times daily (max: 75 mg/kg/day)
  4. Maintenance for age 6 years and older
    1. Give 30 mg/kg/day orally divided 4 times daily with food

IX. Adverse Effects

  1. General
    1. Take Folic Acid 1-2 mg/day
  2. Nausea and other Gastrointestinal Intolerance (30%)
    1. Decreased appetite
    2. Dyspepsia
    3. Nausea or Vomiting
    4. Consider enteric coated Azulfidine EN-tablets (better tolerated)
  3. Neurologic adverse effects
    1. Headache (20%)
    2. Dizziness or Lightheaded (<20%)
  4. Hematologic adverse effects (marrow suppression)
    1. Folate-inhibition Anemia
    2. Hemolytic Anemia
    3. Granulocytopenia and Leukopenia
    4. Thrombocytopenia
  5. Pulmonary
    1. Fibrosing Alveolitis
  6. Skin rash associated with Sulfa Allergy
    1. Requires discontinuing medication immediately
  7. Sexual Function
    1. Oligospermia (Infertility risk)
  8. Renal adverse effects
    1. Urine Discoloration (orange)
      1. May also discolor other body fluids (e.g. tears and Contact Lenses)
    2. Micro-Crystalluria
      1. Risk of Interstitial Nephritis
      2. Avoid Dehydration
      3. Avoid high doses

X. Drug Interactions

  1. Decreases other drug levels
    1. Folic Acid
    2. Digoxin
    3. Cyclosporine
    4. Serum Iron

XI. Safety

  1. Pregnancy Category B
    1. However, Folate supplementation is critical
  2. Unknown safety in Lactation
    1. Case reports of nursing infants with Diarrhea and bloody stools
  3. Monitoring
    1. Complete Blood Count (CBC) every 2 to 4 weeks for 3 months, then every 3 to 6 months
    2. Aspartate Aminotransferase (AST, SGOT) at 2 months
    3. Serum Creatinine

XII. Resources

  1. Sulfasalazine Tablets (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ddbe69f3-bd55-45f3-a64f-f60226c744c4

XIII. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2022) Treatment of Mild to Moderate Ulcerative Colitis, Presc Lett, #350406
  3. (2023) Drugs for Inflammatory Bowel Disease, Med Lett Drug Ther 65: 105-12
  4. Adams (2013) Am Fam Physician 87(10): 699-705 [PubMed]
  5. Adams (2022) Am Fam Physician 105(4): 406-11 [PubMed]
  6. Kornbluth (2010) Am J Gastroenterol 105(3): 501-23 [PubMed]
  7. Matteson (2000) Mayo Clin Proc 75:669-74 [PubMed]
  8. Pincus (1999) Clin Rheumatol 17(6 Suppl 18):S2-S124 [PubMed]

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Related Studies

Cost: Medications

sulfasalazine (on 1/18/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
SULFASALAZINE 500 MG TABLET Generic $0.16 each
SULFASALAZINE DR 500 MG TAB Generic $0.24 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Ontology: Sulfasalazine (C0036078)

Definition (NCI) A synthetic salicylic acid derivative with affinity for connective tissues containing elastin and formulated as a prodrug, antiinflammatory Sulfasalazine acts locally in the intestine through its active metabolites, sulfamide 5-aminosalicylic acid and salicylic acid, by a mechanism that is not clear. It appears inhibit cyclooxygenase and prostaglandin production and is used in the management of inflammatory bowel diseases. (NCI04)
Definition (MSH) A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D012460
SnomedCT 387248006, 45844004, 363635007, 317422008, 330038003
LNC LP18088-2, MTHU006799, MTHU003000
English Salazosulfapyridine, Salicylazosulfapyridine, Sulfasalazine, Sulphasalazine, Benzoic acid, 2-hydroxy-5-((4-((2-pyridinylamino)sulfonyl)phenyl)azo)-, Sulfasalazine [gastro-intest], Sulfasalazine [musc-skel], Sulphasalazine [gastro-intest], Sulphasalazine [musc-skel], 2-Hydroxy-5-[[4-[(2-pyridinylamino)sulfonyl]phenyl]azo]benzoic Acid, salazosulfapyridine, Sulfasalazine [gastro-intestinal use], Sulphasalazine [gastro-intestinal use], Sulfasalazine [musculoskeletal use], Sulphasalazine [musculoskeletal use], sulfasalazine (medication), SULFASALAZINE, Sulfasalazine [Chemical/Ingredient], sulphasalazine, salicylazosulfapyridine, sulfaSALAzine, SulfaSALAzine, sulfasalazine, Sulphasalazine product, Sulfasalazine [musculoskeletal use] (product), Sulfasalazine product, Sulfasalazine [gastro-intestinal use] (product), Sulfasalazine product (substance), Salazosulphapyridine, Salicylazosulphapyridine, Sulfasalazine (product), Sulfasalazine (substance), Sulfasalazine [gastro-intestinal use] (substance), Sulfasalazine [musculoskeletal use] (substance)
Swedish Sulfasalazin
Czech sulfasalazin
Finnish Salatsosulfapyridiini
Russian SALITSILAZOSUL'FAPIRIDIN, SUL'FASALAZIN, SALAZOSUL'FAPIRIDIN, САЛАЗОСУЛЬФАПИРИДИН, САЛИЦИЛАЗОСУЛЬФАПИРИДИН, СУЛЬФАСАЛАЗИН
Japanese エミナピリン, スルファサラジン, ラノフェン, アザルフィジンEN, サリチルアゾサルファピリジン, サラゾピリン, スラマ錠, スラマ, サフィルジンEN, Slama錠, サラゾスルファピリジン
French Sulfasalazine, Salicylazosulfapyridine
Croatian SULFASALAZIN
Polish Salazosulfapirydyna, Sulfasalazyna
Spanish sulfasalazina [uso gastrointestinal] (producto), sulfasalazina [uso musculoesquelético], sulfasalazina [uso musculoesquelético] (producto), sulfasalazina [uso gastrointestinal], salazosulfapiridina, salicilazosulfapiridina, sulfasalazina (producto), sulfasalazina (sustancia), sulfasalazina, Salicilazosulfapiridina, Sulfasalazina
German Salicylazosulfapyridin, Sulfasalazin
Italian Sulfasalazina
Portuguese Salicilazossulfapiridina, Sulfassalazina
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Azulfidine (C0699547)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D012460
English Azulfidine EN-tabs, Pyralin EN, Salazopyrin, EN, Azulfidine, Azulfidine EN, Sulfasalazine Pfizer Brand, Pfizer Brand of Sulfasalazine, salazopyrin, azulfidine, azulfadine, Azulfidine, Asulfidine, Azulfadine
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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