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Indications and Dosage
Oral
Osteoarthritis 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.
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Renal Impairment
Severe: Contraindicated.
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Hepatic Impairment
Severe: Contraindicated.
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Administration
Should be taken with food. Take w/ or immediately after meals.
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Contraindications
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.
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Special Precautions
Patient with previous episode of enterocolic disturbances (e.g. irritable bowel syndrome). Elderly. Moderate renal and mild to moderate hepatic impairment. Pregnancy and lactation.
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Adverse Reactions
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. |
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Overdosage
Symptoms: Diarrhoea. Management: Restore hydroelectrolytic balance if necessary.
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Drug Interactions
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).
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Food Interaction
Increased absorption with food.
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Action
Description:
Mechanism of Action: 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. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 26248, Diacerein. https://pubchem.ncbi.nlm.nih.gov/compound/Diacerein. Accessed Aug. 25, 2020. |
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Storage
Store below 30°C. Protect from light and moisture.
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ATC Classification
M01AX21 - diacerein ; Belongs to the class of other non-steroidal antiinflammatory and antirheumatic products.
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References
Anon. Diacerein. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/08/2020. Artrodar 50 mg (TRB Pharma S.A.). MIMS Thailand. http://www.mims.com/thailand. Accessed 07/08/2020. Buckingham R (ed). Diacerein. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/08/2020. Tirase Capsules 50 mg (Elder Pharmaceuticals Ltd). MIMS Myanmar. http://www.mims.com/myanmar. Accessed 07/08/2020.
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