Diacerein is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including severe diarrhea. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.
Diacerein also is known as diacetylrhein, is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis (swelling and pain in the joints). It works by inhibiting interleukin-1 beta. An updated 2014 Cochrane review found diacerein had a small beneficial effect on pain. It is used to relieve pain and swelling associated with Osteoarthritis. This medicine is slow acting and is used as a long-term treatment option for osteoarthritis.
Mechanism of action of Diacerein
Diacerein’s active metabolite rhein reduces cartilage destruction by decreasing expression of matrix metalloproteinase (MMP)-1 and -3 as well as upregulating tissue inhibitor of matrix metalloproteinases which serve to reduce the activity of several MMPs.This compound belongs to the class of organic compounds known as anthracene carboxylic acids. These are organic compounds containing a carboxylic acid group attached to an anthracene ring system. The anti-inflammatory action of rhein reduces the level of interleukin-1beta activity which plays a large role in the reduction of extracellular matrix production, MMP activity, and continued inflammation. Rhein reduces abnormal osteoblast synthetic activity through an unknown mechanism
Indications of Diacerein
For the treatment of osteoarthritis affecting the hip or knee .
- Cervical spondylosis
- Weight loss
- Degeneration of cartigage
- Road Traffic accident,
- Post oparetive joint injury
- Interstitial cystitis, a bladder condition
- Joint pain, such as knee pain
- Multiple sclerosis (MS)
Contra-Indications of Diacerein
The patient should not take this medicine if he has hypersensitivity of Diacerein or any other active ingredient in the medicine
Dosage of Diacerein
The recommended starting dose is 50 mg once daily with the evening meal for the first 2 to 4 weeks of treatment, after which the recommended daily dose is 50mg twice daily. The treatment should be taken with food, one with breakfast and the other with the evening meal. The capsules must be swallowed intact, without opening them, together with a glass of water.
Diacerein’s dosage details are as follows:
|50 to 50 mg||50 (50)||12 hourly||PO||Take with food. If CrCl is less then 30ml/min then reduce the dose to 25mg per day.|
Paedriatic Dosage (20kg)
|No data regarding the Paedriatic dosage details of Diacerein is available.|
Neonatal Dosage (3kg)
|No data regarding the neonatal dosage details of Diacerein is available.|
Side Effects of Diacerein
Diacerein may cause some unwanted effects too. In such cases, you must seek medical attention immediately.
- Yellow colouration of urine
Yellowing of skin and eyes
Intense yellow urine
Increase in liver enzyme levelsE
Drug Interactions of Diacerein
Ask your doctor about whether diacerein is safe for you if you’re taking any of the following
- Non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naproxen
- Drugs that stop platelets from sticking together, such as clopidogrel and prasugrel
- Blood thinners, such as warfarin, heparin,
- Medications for depression like citalopram and venlafaxine
- Cancer chemotherapy drugs, such as etoposide and doxorubicin
- Diabetes medications, such as pioglitazone , rosiglitazone , and insulin
Pregnancy & Lactation of Diacerein
Pharmacokinetics of Diacerein has not been studied in lactating women and its administration is not recommended.