Sulfasalazine (salicylazosulfapyridine)

What is Sulfasalazine

Sulfasalazine (salicylazosulfapyridine) is a prodrug that is metabolized by intestinal bacteria to sulfapyridine and 5-aminosalicylate (5-ASA) (mesalamine). Sulfasalazine is used in the treatment of ulcerative colitis (UC), rheumatoid arthritis (RA), and juvenille idiopathic arthritis (JIA).

Guidelines include the use of sulfasalazine as a conventional DMARD in selected adult patients with RA and pediatric patients with JIA.

The local actions of 5-ASA in the colon from sulfasalazine are believed to be responsible for the effectiveness of sulfasalazine in the treatment of inflammatory bowel disease, particularly ulcerative colitis (UC).

Guidelines for UC support the use of standard-dose mesalamine (2 to 3 grams/day) or diazo-bonded 5-ASAs (balsalazide or olsalazine) for induction and maintenance of remission rather than sulfasalazine in patients with extensive mild to moderate UC.

Indications

  • Crohn’s disease
  • juvenile rheumatoid arthritis (JRA)/juvenile idiopathic arthritis (JIA)
  • rheumatoid arthritis
  • ulcerative colitis

Side Effects

  1. abdominal pain
  2. acute generalized exanthematous pustulosis (AGEP)
  3. agranulocytosis
  4. alopecia
  5. anaphylactoid reactions
  6. angioedema
  7. anorexia
  8. anuria
  9. aplastic anemia
  10. arthralgia
  11. ataxia
  12. cholestasis
  13. colitis
  14. crystalluria
  15. cyanosis
  16. cystitis
  17. depression
  18. diarrhea
  19. diuresis
  20. dizziness
  21. drowsiness
  22. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  23. dyspepsia
  24. elevated hepatic enzymes
  25. enterocolitis
  26. eosinophilia
  27. erythema multiforme
  28. exfoliative dermatitis
  29. fever
  30. folate deficiency
  31. goiter
  32. Guillain-Barre syndrome
  33. hallucinations
  34. headache
  35. hearing loss
  36. hematuria
  37. hemolytic anemia
  38. hemolytic-uremic syndrome
  39. hepatic failure
  40. hepatic necrosis
  41. hepatitis
  42. hypoglycemia
  43. hypoprothrombinemia
  44. infection
  45. infertility
  46. insomnia
  47. interstitial nephritis
  48. jaundice
  49. leukopenia
  50. lupus-like symptoms
  51. megaloblastic anemia
  52. meningitis
  53. methemoglobinemia
  54. myelitis
  55. myocarditis
  56. nausea
  57. nephrolithiasis
  58. nephrotic syndrome
  59. neutropenia
  60. oligospermia
  61. oliguria
  62. pancreatitis
  63. pericarditis
  64. peripheral neuropathy
  65. photosensitivity
  66. pneumonitis
  67. proteinuria
  68. pruritus
  69. purpura
  70. rash
  71. rhabdomyolysis
  72. seizures
  73. serum sickness
  74. skin discoloration
  75. Stevens-Johnson syndrome
  76. stomatitis
  77. thrombocytopenia
  78. tinnitus
  79. toxic epidermal necrolysis
  80. urine discoloration
  81. urticaria
  82. vertigo
  83. vomiting

Monitoring Parameters

  • CBC with differential
  • glucose-6-phosphate dehydrogenase (G6PD) activity
  • LFTs
  • serum creatinine/BUN
  • urinalysis

Contraindications

  • 5-aminosalicylates hypersensitivity
  • agranulocytosis
  • aplastic anemia
  • asthma
  • bone marrow suppression
  • breast-feeding
  • children
  • dehydration
  • folate deficiency
  • G6PD deficiency
  • GI obstruction
  • hematological disease
  • hepatic disease
  • hepatotoxicity
  • hypovolemia
  • infants
  • infection
  • infertility
  • jaundice
  • laboratory test interference
  • nephrolithiasis
  • neutropenia
  • porphyria
  • pregnancy
  • premature neonates
  • renal failure
  • renal impairment
  • salicylate hypersensitivity
  • serious rash
  • slow acetylation
  • sulfonamide hypersensitivity
  • sunlight (UV) exposure
  • urinary tract obstruction

Interactions

  • Abacavir; Lamivudine, 3TC; Zidovudine, ZDV
  • Acalabrutinib
  • Acarbose
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetohexamide
  • Albiglutide
  • Alogliptin; Metformin
  • Alpelisib
  • Alpha-glucosidase Inhibitors
  • Aminosalicylate sodium, Aminosalicylic acid
  • Amlodipine; Celecoxib
  • Amoxicillin
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amoxicillin; Clavulanic Acid
  • Ampicillin
  • Ampicillin; Sulbactam
  • Articaine; Epinephrine
  • Aspirin, ASA
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Dipyridamole
  • Aspirin, ASA; Omeprazole
  • Aspirin, ASA; Oxycodone
  • Aspirin, ASA; Pravastatin
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Azathioprine
  • Benzocaine
  • Benzocaine; Butamben; Tetracaine
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Bismuth Subsalicylate
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bortezomib
  • Bromocriptine
  • Bupivacaine
  • Bupivacaine Liposomal
  • Bupivacaine; Lidocaine
  • Canagliflozin
  • Canagliflozin; Metformin
  • Capmatinib
  • Cardiac glycosides
  • Celecoxib
  • Chloroprocaine
  • Chlorpropamide
  • Choline Salicylate; Magnesium Salicylate
  • Colchicine; Probenecid
  • Cyclosporine
  • Daclatasvir
  • Dapagliflozin
  • Dapagliflozin; Metformin
  • Dapagliflozin; Saxagliptin
  • Dapsone
  • Darolutamide
  • Dicloxacillin
  • Dienogest; Estradiol valerate
  • Digitoxin
  • Digoxin
  • Dipeptidyl Peptidase-4 Inhibitors
  • Diphenhydramine; Naproxen
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Dulaglutide
  • Elbasvir; Grazoprevir
  • Eltrombopag
  • Empagliflozin
  • Empagliflozin; Linagliptin
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Ertugliflozin
  • Ertugliflozin; Metformin
  • Ertugliflozin; Sitagliptin
  • Esomeprazole; Naproxen
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Etanercept
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Exenatide
  • Fenoprofen
  • Fluvastatin
  • Folic Acid, Vitamin B9
  • Fostamatinib
  • Glecaprevir; Pibrentasvir
  • Glimepiride
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • Glipizide
  • Glipizide; Metformin
  • Glyburide
  • Glyburide; Metformin
  • Hydrochlorothiazide, HCTZ; Losartan
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Incretin Mimetics
  • Insulin Degludec; Liraglutide
  • Insulin Glargine; Lixisenatide
  • Insulins
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Lamivudine, 3TC; Zidovudine, ZDV
  • Lansoprazole; Naproxen
  • Leflunomide
  • Levomefolate
  • Lidocaine
  • Linagliptin; Metformin
  • Liraglutide
  • Lixisenatide
  • Losartan
  • Magnesium Salicylate
  • Meglitinides
  • Mepivacaine
  • Mepivacaine; Levonordefrin
  • Mercaptopurine, 6-MP
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methenamine
  • Methenamine; Sodium Acid Phosphate
  • Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
  • Methotrexate
  • Methoxsalen
  • Miglitol
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Omeprazole; Amoxicillin; Rifabutin
  • Oral Contraceptives
  • Osimertinib
  • Oxacillin
  • Ozanimod
  • Penicillin G
  • Penicillin G Benzathine
  • Penicillin G Benzathine; Penicillin G Procaine
  • Penicillin G Procaine
  • Penicillin V
  • Pexidartinib
  • Photosensitizing agents (topical)
  • Piperacillin
  • Piperacillin; Tazobactam
  • Ponatinib
  • Porfimer
  • Pramlintide
  • Prilocaine
  • Prilocaine; Epinephrine
  • Probenecid
  • Pyrimethamine
  • Pyrimethamine; Sulfadoxine
  • Regorafenib
  • Rifampin
  • Riluzole
  • Rimegepant
  • Rituximab
  • Rituximab; Hyaluronidase
  • Rolapitant
  • Ropivacaine
  • Safinamide
  • Salicylates
  • Salsalate
  • Semaglutide
  • SGLT2 Inhibitors
  • Simeprevir
  • Sodium Iodide
  • Sodium picosulfate; Magnesium oxide; Anhydrous citric acid
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Sulfonylureas
  • Tafamidis
  • Talazoparib
  • Tedizolid
  • Tetracaine
  • Thiazolidinediones
  • Thioguanine, 6-TG
  • Tolazamide
  • Tolbutamide
  • Topotecan
  • Typhoid Vaccine
  • Ubrogepant
  • Verteporfin
  • Voriconazole
  • Warfarin
  • Zidovudine, ZDV