Adult: Usual dose: 50 mg bid. Alternatively, 50 mg once daily with evening meal for 2-4 weeks. Dose may be increased to 100 mg daily in divided doses according to patient tolerability. Treatment duration may vary according to patient response and expected clinical outcome.
Decrease to half of the recommended dose.
Should be taken with food. Take w/ or immediately after meals.
Hypersensitivity to anthraquinone derivatives. Inflammatory intestinal disease (e.g. ulcerative colitis, Crohn’s disease), intestinal obstruction, painful abdominal syndromes of undetermined cause. Severe renal and hepatic impairment. Concomitant use with laxatives.
Patient with previous episode of enterocolic disturbances (e.g. irritable bowel syndrome). Elderly. Moderate renal and mild to moderate hepatic impairment. Pregnancy and lactation.
Significant: Diarrhoea. Gastrointestinal disorders: Abdominal pain, flatulence. Hepatobiliary disorders: Hepatitis. Investigations: Elevated liver enzymes. Renal and urinary disorders: Dark yellow coloured urine. Skin and subcutaneous tissue disorders: Pruritus, rash, eczema.
Symptoms: Diarrhoea. Management: Restore hydroelectrolytic balance if necessary.
Reduced bioavailability with aluminium hydroxide, magnesium hydroxide or calcium-based antacids. Increased risk of enterocolic events with antibiotics (e.g. amoxicillin/clavulanic acid) and/or chemotherapy. Increased risk of dehydration and hypokalaemia with diuretics. Increased risk of arrhythmia with cardiac glycosides (e.g. digitoxin, digoxin).
Increased absorption with food.
Description: Diacerein is an anthraquinone derivative and a prodrug that is metabolised to rhein, a selective inhibitor of interleukin-1 (IL-1). It increases the production of transforming growth factor-β (TGF-β) which triggers chondrocyte proliferation and stimulates the production of collagen and proteoglycan. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Food, increases absorption. Time to peak plasma concentration: 15-30 minutes (rhein). Distribution: Plasma protein binding: Approx 99% (rhein). Metabolism: Extensively metabolised in the liver to active metabolite, rhein. Excretion: Mainly via urine (20% [as unchanged drug], 60% [as glucuronide], 20% [as sulfate derivatives]). Elimination half-life: 7-8 hours.
Store below 30°C. Protect from light and moisture.