DrugInfoSys

Diacerein

Also known as: Diacetylrhein

Drug #2218

Diacerein is a new anti-inflammatory analgesics and antipyretic drug, developed specially for the treatment of osteoarthritis. It may be able to modify the course of the disease condition. It directly inhibits IL-1 synthesis and release in vitro and down modulate IL-1 induced activities and have been shown to posses disease modifying effect in experimental models of osteoarthritis and in human subjects with finger joint and knee osteoarthritis. IL-1 plays a fundamental role in osteoarthritis pathophysiology and cartilage destruction and also promotes expression of inducible nitric oxide synthase , increase release of prostaglandin E2, IL-6,IL-8 in human osteoarthritis chondrocytes, which promote joint degradation. Hence, by inhibiting IL-1 diacerein retards all pathological prepossess initiated in osteoarthritir. Diacerein also inhibits IL-1 induced expression of cartilage degrading enzymes. It also enhances expression of TGF BETA-1 and TGF BETA 2 thus favoring matrix synthesis and turnover in articular chondrocytes, thereby accounting for disease modifying property of diacerein It is reported to be safe in comparison to NSAIDs with no documented upper gastrointestinal toxicity like gastric or duodenal ulcer.

Primary Characteristics

Diacerein is also known as Diacetylrhein.

It is of Semi Synthetic origin and belongs to Anthraquinone derivative.

It is also classified under Bone Metabolism .

Molecular Weight: 368.29 · Non-proprietary name: Diacerein.

Molecular structure of Diacerein

Pharmacokinetics

Distribution: Diacerein has a volume of distribution is 13.2 L for rhein. plasma protein binding is high for its active metabolite (rhein).

Elimination: it is metabolised via by deactylation to active metabolite rhein, plasma half-life is 4.3 hours for rhein, renal excretion is 20% and 80% conjugated in liver.

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Indications

Diacerein is primarily indicated in conditions like Osteoarthritis.

Contraindications

Diacerein is contraindicated in conditions like Pregnancy, Lactation, Hypersensitivity to anthraquinone derivatives.

Dosage

Diacerein's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
50 mg50 mgEvery 12hPOTake with food. If CrCl is less then 30ml/min then reduce the dose to 25mg per day.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

2 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

The signs and symptoms that are produced after acute overdosage of Diacerein are Diarrhea.

Diacerein is known to cause more or less tolerable side effects which are usually transient. These include Diarrhea, Discoloration of urine, Epigastric pain, Nausea, Pruritus , Rashes , Vomiting .

Warnings / Precautions

Dose modification is required in mild to sever renal insufficiency (50% dose reduction in sever renal failure). Monitor CBC, LFT and urinanalysis every 6 mth.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Caps

Storage Conditions

Diacerein should be stored tablet.

Drug Classification

  1. 1.18.14Drugs affecting bone metabolism

Manufacturers

Manufacturers of Diacerein in Pakistan: