Diacerein

Diacerein, an active ingredient from the rhubarb root(Rhei radix), belongs to the group of anthraquinone derivatives. Diacerein is a diacetylated rhein, a prodrug that is converted in the body to its active metabolite rhein. Diacerein is also known as diacetyl rhein.

Diacerein and its metabolite rhein have anti-inflammatory, analgesic, antiarthrotic, antioedematous and laxative effects. The effects are based, among other things, on the inhibition of cytokines (e.g. IL-1beta), proteolytic enzymes and oxygen radicals (effects with topical application of a 1% cream in epidermolysis bullosa simplex). Rhine also appears to promote the synthesis of cartilage components.

Diacerein is used for the treatment of degenerative joint diseases(arthrosis). The drug was successfully tested as a 1% application form in a small clinical study in epidermolysis bullosa simplex (Dowling-Meara type). Effects were reported in psoriasis, which require further clinical confirmation.

Diacerein is a well-known laxative and can therefore trigger diarrhoea and digestive problems other than ADRs, especially at the beginning of treatment. The anthraquinone derivative discolours the urine brownish to reddish.

Diacerein is contraindicated in hypersensitivity, severe liver failure, inflammatory bowel disease, intestinal obstruction, painful lower abdominal pain of unknown cause. Furthermore, it must not be prescribed to children and adolescents under the age of 18 and during pregnancy and lactation.

Diacerein is available in Austria in the form of capsules (Verboril®, Artrolyt®).

1. Falgarone G et al (2001) Diacerein as a disease-modulating agent in osteoarthritis. Curr Rheumatol Rep 3: 479-483
2. Moghddam SR et al (2016) Formulation and optimization of niosomes for topical diacerein delivery using 3-factor, 3-level Box-Behnken design for the management of psoriasis. Mater Sci Eng C Mater Biol Appl 69:789-797.
3. Pelletier JP et al (2000) Efficacy and safety of diacerein in osteoarthritis of the knee: a double-blind, placebo-controlled trial. The Diacerein Study Group. Arthritis rheum 43: 2339-2348.
4. Spencer CM et al (1997) Diacerein. Drugs 53: 98-106
5. Wally V et al (2013) Topical diacerein for epidermolysis bullosa: a randomized controlled pilot study. Orphanet J Rare Dis 8:69.