ORCERIN Capsule

For the treatment of osteoarthritis.

Dosage and administration

Diacerein 50mg is to be administered orally, twice daily.

Initiate the treatment with 1 capsule nighttime for 2-4 weeks, gradually adjust the dose to 2 capsules twice daily. Oral absorption is greatest when administered with food.

Hypersensitivity to Diacerein or any of the components.

Combined use with laxatives is contraindicated.

The commonest reported adverse reaction was acceleration of the time of intestinal transit (diarrhoea 37% of patients). Few cases of abdominal pains have been described. The modification of the dose in the initial periods of the treatment (2-4 weeks) has allowed to surpass or to diminish these adverse events.

Other adverse events reported are urine discoloration in 14.4% cases and single cases of hypokalemia, hepatotoxicity resulting into acute hepatitis and fatal toxic epidermal necrolysis (Lyell’s syndrome).

The clinical studies have demonstrated the absence of interaction with the drugs such as; warfarin, tolbutamide, aspirin (acetylsalicylic acid), chlorpromazine, indomethacin.

Pregnancy

Use of Diacerein is not recommended in women attempting to conceive. No clinical data on exposed human risk in pregnancy is unknown.

Lactation

Pharmacokinetics of Diacerein has not been studied in lactating women and its administration is not recommended.

General

- It is recommended to initiate therapy with 1 capsule at night for the first 2-4 weeks as use of the drug can produce an acceleration of the intestinal transit time initially.

- It is recommended to continue treatment for at least 6 months; the clinical studies have demonstrated that the drug can be used for 2 years without serious adverse effects.

- As with any other long-term therapy, it is recommended to monitor laboratory parameters, including hepatic enzymes, every 6 months.

See the package insert about the details below:

Renal impairment

Hepatic impairment

Pediatric use

Geriatric use

Interleukin-1 inhibitor.

The mechanism of the synthesis of the NSAIDs since it is not related to the inhibition of the synthesis of the prostaglandins. Antiosteoarthritic and cartilage-stimulating properties have been demonstrated in vitro and in animal models. Diacerein and rhein have been shown to inhibit the production of interleukin-1 beta by human monocytes and the effect of the cytokine on chondrocytes in vivo. They exert chondroprotective effects in cultured articular cartilage and reduce severity of cartilage, bone, and synovial membrane damage in osteoarthritis. There appear to be some inhibitory effects on leucocyte migration and activation, contributing to the weak anti-inflammatory activity of the drug. Studies indicate that Diacerein does not block the synthesis of prostaglandins, thromboxanes, or leukotrienes but may actually stimulate prostaglandin synthesis, especially PGF-2, with potential cartilage repairing properties. Diacerein does not alter renal or platelet cyclo-oxygenase activity and may therefore be tolerated by patients with prostaglandin-dependent renal function.