Sulfasalazine

Registered South African indications:

• Ulcerative colitis
• Crohn's disease
• Rheumatoid arthritis

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to sulfonamides or salicylates
• Infants (<2 years)
• Porphyria

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Blood dyscrasia
• Severe allergy
• Bronchial asthma
• Children with systemic onset juvenile rheumatoid arthritis
• Glucose-6 phosphatase dehydrogenase deficiency

Forms avail. in SA and covered in this monograph: tab

Ulcerative colitis - Acute attack
Crohn's disease - Acute attack

• Oral (tab): 1-2g, 6hrly; Max: 12g/24hrs

Ulcerative colitis - Maintenance of remission

• Oral (tab): 2g/day, in 3-4 divided doses

Rheumatoid arthritis

• Oral (tab): Initial: 500mg, dly at night for 1 week; Titrate by 500mg/day at intervals of 1 week; Maintenance: 1g, 12hrly; Max: 3g/24hrs

	Week 1	Week 2	Week 3	Week 4 onwards
Morning		500mg	500mg	1000mg
Evening	500mg	500mg	1000mg	1000mg

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In rheumatoid arthritis, if no response is obtained after two months of treatment, the total daily dose may be increased to 3g/day

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Intervals between doses should not exceed 8hrs even at night

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Enteric coated tablets: Do not cut/crush/chew/dissolve

Paed. forms avail. in SA and covered in this monograph: tab

Ulcerative colitis - Acute attack
Crohn's disease - Acute attack

Younger than 6 years

• Not established for use

Older than 6 years

• Oral (tab): 40-60mg/kg/day in 3-6 divided doses; Max: 4g/24hrs

Ulcerative colitis - Remission

Younger than 6 years

• Not established for use

Older than 6 years

• Oral (tab): 20-30mg/kg/day in 4 divided doses; Max: 2g/24hrs

Juvenile rheumatoid arthritis

Younger than 6 years

• Not established for use

Older than 6 years

• Oral (tab): Week 1: 5mg/kg, 12hrly; Week 2: 10mg/kg, 12hrly; Week 3 onwards: 15mg/kg, 12hrly

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Do not crush or break

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Take tablets at regular intervals

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Night time intervals between doses should not exceed 8 hours

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Must maintain adequate fluid intake

Pregnancy

• Caution
• Reproduction studies in rats and rabbits have revealed no evidence of harm to the fetus. Published data regarding use of sulfasalazine in pregnant women have revealed no evidence of teratogenic hazards. If sulfasalazine is used during pregnancy, the possibility of fetal harm appears remote. Oral sulfasalazine inhibits the absorption and metabolism of folic acid and may cause folic acid deficiency. Because the possibility of harm cannot be completely ruled out, sulfasalazine should be used during pregnancy only if clearly needed

Breastfeeding

• Caution; not recommended
• Sulfasalazine and sulfapyridine are found in low levels in breast milk. Patients should avoid breastfeeding while taking this medicine. There have been reports of bloody stools or diarrhoea in infants who were breastfeeding from mothers on sulfasalazine. In cases where the outcome was reported, bloody stools or diarrhoea resolved in the infant after discontinuation of sulfasalazine in the mother

Fertility

• Oligospermia and infertility may occur in men treated with sulfasalazine. Discontinuation of the drug appears to reverse these effects within 2 to 3 months

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Caution, no dose adjustment recommended

Elderly

• No dose adjustment recommended

Porphyria Information

•  Porphyrinogenic (P)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Depression
• Hallucinations
• Dizziness
• Headache
• Seizures
• Aseptic meningitis
• Ataxia
• Encephalopathy
• Peripheral neuropathy

Cardiovascular Disorders

• Allergic myocarditis
• Cyanosis
• Pericarditis
• Vasculitis

Respiratory Disorders

• Cough
• Dyspnoea
• Fibrosing alveolitis
• Eosinophilic infiltration
• Interstitial lung disease

Gastrointestinal Disorders

• Gastric distress
• Nausea and vomiting 
• Abdominal pain
• Diarrhoea
• Stomatitis
• Aggravation of ulcerative colitis
• Pancreatitis
• Parotitis

Hepatobiliary Disorders

• Hepatic failure
• Fulminant hepatitis
• Hepatitis

Genitourinary Disorders

• Proteinuria
• Nephrotic syndrome
• Interstitial nephritis
• Crystalluria
• Haematuria
• Reversible oligospermia

Endocrine and Metabolic Disorders

• Loss of appetite

Musculoskeletal Disorders

• Arthralgia

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Alopecia
• Urticaria
• Epidermal necrolysis (Lyell's syndrome)
• Stevens-Johnson syndrome
• Drug rash with eosinophilia and systemic symptoms
• Toxic pustuloderma
• Erythema
• Exanthema
• Exfoliative dermatitis
• Periorbital oedema
• Lichen planus
• Photosensitivity
• Yellow discoloration of skin and body fluids
• Facial oedema 

Immune, Blood and Lymphatic System Disorders

• Leukopenia
• Thrombocytopenia
• Agranulocytosis
• Aplastic anemia
• Haemolytic anemia
• Heinz body anaemia
• Hypoprothrombinaemia
• Lymphadenopathy
• Macrocytosis
• Megaloblastic anemia
• Methaemoglobinaemia
• Neutropenia
• Pancytopenia
• Anaphylaxis
• Polyarteritis nodosa
• Serum sickness
• Pseudomembranous colitis
• Systemic lupus erythematosus
• Fever

Sensory Disorders

• Tinnitus
• Vertigo
• Conjuctivial and scleral injection
• Taste disorders
• Smell disorders

• Digoxin
• Sulphonylureas
• Thiopurine 6-mercaptopurine
• Azathioprine
• Methotrexate

• Full blood count

Specific cases may require

• Renal function
• Hepatic function 

Sulfasalazine is broken down by intestinal bacteria in the colonic lumen into active sulfapyridine and mesalazine. Overall the drug and its metabolites exert immunomodulatory effects, antibacterial effects, effects on the arachidonic acid cascade and alteration of activity of certain enzymes. The net result clinically is a reduction in activity of the inflammatory bowel disease. Enteric coated sulfasalazine is registered for the treatment of rheumatoid arthritis, where the effect resembles penicillamine or gold.

Tablet 500mg

• Salazopyrin (Pfizer) originator

Tablet ECT 500mg

• Salazopyrin EN (Pfizer) originator