β οΈ Patient advice: Report immediately if rash, sore throat, purpura, bruising, bleeding, fever, or infection symptoms develop. These may signal blood dyscrasias or hypersensitivity.
- πΉ A combination drug of 5-aminosalicylate (5-ASA) linked to sulphapyridine via an azo bond.
- π§ͺ The 5-ASA component β local anti-inflammatory effect in the colon.
The sulphapyridine carrier β systemic effects, esp. useful in rheumatoid arthritis.
- π Poor bowel absorption keeps drug concentrated in the gut lumen.
βοΈ Mode of Action
- π§ͺ In the colon, gut bacteria split sulfasalazine into:
β 5-ASA β reduces prostaglandins & cytokines, β inflammation in IBD.
β Sulphapyridine β provides immunomodulatory activity in RA.
- π Dual activity makes it useful in both IBD and rheumatology.
π― Indications / Dose
- π€² Rheumatoid Arthritis: start 500 mg daily β titrate to 2 g/day PO in divided doses over weeks.
- π₯ Acute UC / Crohnβs colitis: 1β2 g PO 6-hourly in active disease β reduce to 500 mg QDS for maintenance.
- π Rectal formulations (distal UC):
β Suppositories: 0.5β1 g BD.
β Enemas: 3 g nocte.
π Interactions
- β οΈ Use cautiously with other bone marrow suppressants (risk of additive toxicity).
β Contraindications
- π« Severe renal or hepatic impairment.
- π« Acute porphyrias.
- β οΈ G6PD deficiency (risk of haemolysis).
- β οΈ Allergy, asthma (higher risk of hypersensitivity reactions).
- π€° Can be used in pregnancy, but supplement with folic acid (antifolate activity).
β οΈ Side Effects
- π½οΈ GI: nausea, vomiting, diarrhoea, gallstones.
- π§βπ§ Male infertility: reversible azoospermia.
- π€ Hypersensitivity: rash, StevensβJohnson syndrome, interstitial nephritis, lupus-like syndrome.
- π©Έ Haematological: agranulocytosis, aplastic anaemia, neutropenia, thrombocytopenia β urgent FBC if unexplained anaemia, infection, or bleeding.
- π« Pulmonary: fibrosing alveolitis, eosinophilia.
- π§ Neurological: depression, peripheral neuropathy.
- π Cosmetic: orange urine & tears (warn contact lens wearers).
π Cautions & Monitoring
- π FBC: every 2 weeks for first 12 weeks, then at least monthly until stable.
- π LFTs: monthly for 12 weeks, then periodically.
- β οΈ Monitor renal function periodically (U&E, creatinine).
- π Advise patients about early warning signs (rash, sore throat, bleeding, bruising).
π References