Diacerein (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

), also known as diacetylrhein, is a slow-acting medicine of the class

anthraquinone Anthraquinone, also called anthracenedione or dioxoanthracene, is an aromatic organic compound with formula . Isomers include various quinone derivatives. The term anthraquinone however refers to the isomer, 9,10-anthraquinone (IUPAC: 9,10-dioxo ...

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 Cochrane may refer to: Places Australia *Cochrane railway station, Sydney, a railway station on the closed Ropes Creek railway line Canada * Cochrane, Alberta * Cochrane Lake, Alberta * Cochrane District, Ontario ** Cochrane, Ontario, a town wit ...

review A review is an evaluation of a publication, product, service, or company or a critical take on current affairs in literature, politics or culture. In addition to a critical evaluation, the review's author may assign the work a content rating, ...

found diacerein had a small beneficial effect on pain. Diacerein-containing medications are registered in some European Union and Asian countries and included as a treatment option on several international therapeutic guidelines.

Pharmacology

Diacerein works by blocking the actions of interleukin-1 beta, a protein involved in the inflammation and destruction of

cartilage Cartilage is a resilient and smooth type of connective tissue. In tetrapods, it covers and protects the ends of long bones at the joints as articular cartilage, and is a structural component of many body parts including the rib cage, the neck an ...

that plays a role in the development of symptoms of degenerative joint diseases such as

osteoarthritis Osteoarthritis (OA) is a type of degenerative joint disease that results from breakdown of joint cartilage and underlying bone which affects 1 in 7 adults in the United States. It is believed to be the fourth leading cause of disability in the w ...

. Due to its specific mode of action, which does not involve the inhibition of

prostaglandin The prostaglandins (PG) are a group of physiologically active lipid compounds called eicosanoids having diverse hormone-like effects in animals. Prostaglandins have been found in almost every tissue in humans and other animals. They are derive ...

synthesis, diacerein has been shown to have anti-osteoarthritis and cartilage stimulating properties in vitro and animal models.

Side effects

The most common

side effects In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...

of diacerein treatment are

gastrointestinal The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The GI tract contains all the major organs of the digestive system, in humans and ...

symptoms including soft stools and

diarrhea Diarrhea, also spelled diarrhoea, is the condition of having at least three loose, liquid, or watery bowel movements each day. It often lasts for a few days and can result in dehydration due to fluid loss. Signs of dehydration often begin wi ...

. These are generally mild to moderate and occur more frequently in the first 2 weeks, and lessen with continued treatment. Based on review by European Medicines Agency (EMA), diacerein-containing medicines use is restricted due to severe diarrhoea and liver disorders in patients. An uncommon side effect is hepatic adverse events (most frequently reported as liver function test abnormalities). These have been described as mild/moderate cases of elevated liver enzymes in the blood. Mild skin reactions (rash, pruritus and eczema) have also been reported with diacerein treatment. Discoloration of urine (yellow or pink) is another side effect of diacerein. This effect is due to the elimination of rhein metabolites via the urine and no clinical significance has been found; it may also be dependent on general fluid intake.

Special warning

In 2014 the European Medicines Agency (EMA’s) Pharmacovigilance and Risk Assessment Committee (PRAC) performed a review of diacerein-containing medicines over concerns about its gastrointestinal and liver effects. As a result, the PRAC has introduced additional proposals to manage diacerein’s risks and was satisfied that with new restrictions diacerein’s benefit on pain outweighs the side effects for osteoarthritis treatment. The following recommendations have been made around the use of diacerein: * Due to the potential complications that can occur as a result of

in older adults, diacerein is no longer recommended in patients aged 65 years and above. * It is also advised that patients start treatment on half the normal dose (i.e. 50 mg daily instead of 100 mg daily), and should stop taking diacerein if

occurs. * It should not be used in any patient with liver disease or a history of liver disease, and doctors should be monitoring their patients for early signs of liver problems. * The use of diacerein is to be limited to treating symptoms of osteoarthritis affecting the hip or knee. * Diacerein should not be administered during pregnancy and lactation. The PRAC concluded that the benefit-risk balance of diacerein-containing medicinal products remained favourable in the symptomatic treatment osteoarthritis, subject to the agreed changes to the product information and conditions.

Dosage and administration

The recommended starting dose is 50 mg once daily with evening meal for the first 2 to 4 weeks of treatment, after which the recommended daily dose is 50 mg twice daily. The treatment should be taken with food, one with breakfast and the other with evening meal. The capsules must be swallowed intact, without opening them, together with a glass of water.

References

{{Anti-inflammatory and antirheumatic products Anti-inflammatory agents Anthraquinones Carboxylic acids Acetate esters

Pharmacology

Side effects

Special warning

Dosage and administration

See also

References