Diacerein; Uses, Dosage, Side Effects, Interactions, Pregnancy

Diacerein; Uses, Dosage, Side Effects, Interactions, Pregnancy

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

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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:

Dose Single Dose Frequency Route Instructions

Adult Dosage

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.

Observed in a small fraction of the population

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
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Pregnancy & Lactation of Diacerein 

FDA pregnancy Category B
Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
The use of Diacerein is not recommended in women attempting to conceive. No clinical data on exposed pregnancies are available for Diacerein. The potential for human risk in pregnancy is unknown.


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