Diacerein


Concise Prescribing Info
Indications/Uses
Osteoarthritis.
Dosage/Direction for Use
Adult : PO Usual dose: 50 mg bid. Alternatively, 50 mg once daily with evening meal for 2-4 weeks. Dose may be increased to 100 mg/day in divided doses according to patient tolerability. Treatment duration may vary according to patient response and expected clinical outcome.
Dosage Details
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.
Renal Impairment
Severe: Contraindicated.
CrCl (mL/min) Dosage
<30 Decrease to half of the recommended dose.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food. Take w/ or immediately after meals.
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.
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.
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.
Overdosage
Symptoms: Diarrhoea. Management: Restore hydroelectrolytic balance if necessary.
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).
Food Interaction
Increased absorption with food.
Action
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.
Chemical Structure

Chemical Structure Image
Diacerein

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.

Storage
Store below 30°C. Protect from light and moisture.
ATC Classification
M01AX21 - diacerein ; Belongs to the class of other non-steroidal antiinflammatory and antirheumatic products.
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.

Disclaimer: This information is independently developed by MIMS based on Diacerein from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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