Sulphasalazine

Sulphasalazine Brands

Brand Name	Manufacturer Name	Distributor	Drug Strength	Packaging	Formulation	Formulation Strength	Price
Salazopyrin EN	Pfizer Global Pharmaceuticals	Surgipharm Ltd	500mg	100	Tablet	per tablet	KES 2,614.00

Sulphasalazine More info
Mode Of Action	5-Aminosalicylic acid derivatives appear to diminish inflammation by inhibiting cyclo-oxygenase and lipoxygenase, hence decreasing the production of prostaglandins, leukotrienes and hydroxyeicosatetraenoic acids (HETEs). It also appears to act as a scavenger of oxygen-derived free radicals, produced in greater numbers in those with inflammatory bowel disease.
Drug Indication	Ulcerative colitis, Crohns disease, rheumatoid arthritis.
Precautions	Breastfeeding, pregnancy, elderly patients.
Side Effects	GI disturbances, headache, and exacerbation of colitis.
Dosage	Acute attack: Adult; 1000-2000mg QID, Children over 2 years; 40-60mg/kg daily- until remission occurs. Maintenance: Adult; 500mg QID, Children over 2 years; 20-30mg/kg daily.
Special Information	Its mode of action may be related to the anti-inflammatory and/or immunomodulatory properties that have been observed in animal and in vitro models.
Pregnancy Category	Category A1:
Pregnancy Category Description	Drugs which have been taken by a sizeable number of pregnant women and women of child-bearing age with no any established rise in the frequency of malformations or other direct or indirect detrimental effects on the foetus having been noted.

Initial: 3-4 g/day in evenly divided doses at ≤8-hour intervals. Note: American College of Gastroenterology guideline recommendations: Titrate to 4-6 g/day in 4 divided doses (Kornbluth, 2010).

Maintenance dose: 2 g/day in evenly divided doses at ≤8-hour intervals; may initiate therapy with 1-2 g/day to reduce GI intolerance

Rheumatoid arthritis: Oral (enteric coated tablet): Initial: 0.5-1 g/day; increase weekly to maintenance dose of 2 g/day in 2 divided doses; maximum: 3 g/day (if response to 2 g/day is inadequate after 12 weeks of treatment)

Ulcerative colitis: Oral: Children ≥6 years: Initial: 40-60 mg/kg/day in 3-6 divided doses; maintenance dose: 30 mg/kg/day in 4 divided doses

Juvenile idiopathic arthritis (JIA): Oral (enteric coated tablet): Children ≥6 years: 30-50 mg/kg/day in 2 divided doses; Initial: Begin with 1/4 to 1/3 of expected maintenance dose; increase weekly; maximum: 2 g/day typically

GI intolerance is common during the first few days of therapy (administer with meals). Do not crush enteric coated tablets.

Treatment of mild-to-moderate ulcerative colitis or as adjunctive therapy in severe ulcerative colitis; enteric coated tablets are also used for rheumatoid arthritis (including juvenile idiopathic arthritis [JIA]) in patients who inadequately respond to analgesics and NSAIDs

<1% (limited to important or life-threatening; includes reactions reported with mesalamine or other sulfonamides): Agranulocytosis, alopecia, anaphylaxis, aplastic anemia, arthralgia, ataxia, cholestatic jaundice, cirrhosis, crystalluria, depression, diarrhea, drowsiness, drug rash with eosinophilia and systemic symptoms (DRESS), eosinophilia, epidermal necrolysis, exfoliative dermatitis, fibrosing alveolitis, fulminant hepatitis, Guillain-Barré syndrome, hallucinations, hearing loss, hemolytic-uremic syndrome, hematuria, hepatic failure, hepatic necrosis, hepatitis, hypoglycemia, hypoprothrombinemia, insomnia, interstitial lung disease, interstitial nephritis, jaundice, Kawasaki-like syndrome (single case report), lupus-like syndrome, megaloblastic anemia, meningitis, methemoglobinemia, myelitis, myelodysplastic syndrome, myocarditis (allergic), nephropathy (acute), nephrotic syndrome, neutropenia (congenital), neutropenic enterocolitis, pancreatitis, pericarditis, periorbital edema, peripheral neuropathy, photosensitization, pleuritis, pneumonitis, polyarteritis nodosa, proteinuria, purpura, rhabdomyolysis, seizure, serum sickness-like reactions, skin discoloration, Stevens-Johnson syndrome, thyroid function disturbance, tinnitus, urine discoloration, vasculitis, vertigo

Hypersensitivity to sulfasalazine, sulfa drugs, salicylates, or any component of the formulation; porphyria; GI or GU obstruction

• Blood dyscrasias: Fatalities associated with severe reactions including agranulocytosis, aplastic anemia, and other blood dyscrasias have occurred; discontinue use at first sign of rash or signs of serious adverse reactions. Use with extreme caution in patients with blood dyscrasias.

• CNS effects: Deaths from irreversible neuromuscular and central nervous system changes have been reported.

• Dermatologic reactions: Fatalities associated with severe reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis have occurred with sulfonamides; discontinue use at first sign of rash.

• Folate deficiency: May cause folate deficiency; consider providing 1 mg/day folate supplement.

• GI effects: Nausea, vomiting, and abdominal discomfort commonly occur; titration of dose and/or using the enteric coated formulation may decrease GI adverse effects.

• Hepatic necrosis: Fatalities associated with hepatic damage have occurred; discontinue use at first sign of jaundice or hepatotoxicity.

• Oligospermia: In males, oligospermia (rare) has been reported; usually reverses upon discontinuation.

• Sulfonamide allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonamide allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe.

• Allergies/asthma: Use with caution in patients with severe allergies or asthma.

• G6PD deficiency: Use with caution in patients with G6PD deficiency; hemolytic anemia may occur.

• Hepatic impairment: Use with extreme caution in patients with impaired hepatic function.

• Renal impairment: Use with extreme caution in patients with renal impairment. Maintain adequate hydration to prevent crystalluria.

• Slow acetylators: Patients classified as slow acetylators may be at increased risk for adverse reactions due to a prolonged half-life of sulfapyrazine (metabolite of sulfasalazine).

(For additional information: Launch Lexi-Interact™ Drug Interactions Program )

Cardiac Glycosides: 5-ASA Derivatives may decrease the serum concentration of Cardiac Glycosides. Risk C: Monitor therapy

Heparin: 5-ASA Derivatives may enhance the adverse/toxic effect of Heparin. Specifically, the risk for bleeding/bruising may be increased. Risk C: Monitor therapy

Heparin (Low Molecular Weight): 5-ASA Derivatives may enhance the adverse/toxic effect of Heparin (Low Molecular Weight). Specifically, the risk for bleeding/bruising may be increased. Risk C: Monitor therapy

Methylfolate: SulfaSALAzine may decrease the serum concentration of Methylfolate. Risk C: Monitor therapy

Thiopurine Analogs: 5-ASA Derivatives may decrease the metabolism of Thiopurine Analogs. Risk C: Monitor therapy

Varicella Virus-Containing Vaccines: 5-ASA Derivatives may enhance the adverse/toxic effect of Varicella Virus-Containing Vaccines. The primary concern is the potential development of Reye's Syndrome, a condition that has been associated with the use of salicylates in children with varicella infections. Risk D: Consider therapy modification

Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization)

Adverse events have not been observed in animal reproduction studies. Sulfasalazine and sulfapyridine cross the placenta; a potential for kernicterus in the newborn exists. Agranulocytosis was noted in an infant following maternal use of sulfasalazine during pregnancy. Based on available data, an increase in fetal malformations has not been observed following maternal use of sulfasalazine for the treatment of inflammatory bowel disease or ulcerative colitis.

Enters breast milk/use caution (AAP recommends use “with caution”; AAP 2001 update pending)

Sulfonamides are excreted in human breast milk and may cause kernicterus in the newborn. Although sulfapyridine has poor bilirubin-displacing ability, use with caution in women who are breast-feeding.

Since sulfasalazine impairs folate absorption, consider providing 1 mg/day folate supplement