Diacerein

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Diacerein.jpg

[edit] MECHANISM OF ACTION

Diacerein, an anti-osteoarthritis, analgesic and anti-inflammatory drug, has a unique mode of action through inhibition of the production and activity of interleukin-1, the key mediator in the progression of osteoarthritis.

Diacerein is effective in reducing pain and functional impairment, the major symptoms of OA, and has shown structure-modifying effects with good gastrointestinal tolerability.

[edit] INDICATIONS

Long-term oral treatment of degenerative joint diseases (osteoarthritis and related diseases).

[edit] DOSAGE

The usual dosage is 50 mg taken orally twice a day with the main meals for prolonged periods (not less than 6 months). However, as Diacerein may cause acceleration in intestinal transit time during the first 2 weeks of treatment, it is recommended that treatment be started with one 50 mg capsule per day taken orally with the evening meal for 4 weeks. Once the patient has become accustomed to the medication, the dose should be increased to 2 capsules per day, taken orally with meals. Due to its late onset of action (after 2-4 weeks of treatment), and its excellent gastroduodenal tolerability, Diacerein may be associated with a non-steroidal anti-inflammatory drug or analgesics for the first 2-4 weeks of treatment.

In clinical trials the product has been administered for up to 2 years with no safety problems. Once treatment is stopped, symptomatic benefits with persist for some time, demonstrating the carry-over effects of the drug

[edit] CONTRAINDICATIONS

  • known hypersensitivity to Diacerein.
  • Temporary treatment suspension must be considered in case of antibiotic therapy, which may affect intestinal flora and kinetics.
  • The benefit/risk ratio of administering Diacerein to patients with previous episodes of enterocolic disturbances, especially irritable colon, must be considered.

[edit] PRECAUTIONS

  • Renal insufficiency modifies the pharmacokinetics of Diacerein and therefore a dose reduction is recommended in such cases (creatinine clearance < 30 ml/min).

[edit] INTERACTIONS

  • Laxatives should not be taken concomitantly with Diacerein.
  • The concomitant administration of products containing aluminium hydroxide and/or magnesium hydroxide should be avoided in order to maximise the bioavailability of Diacerein.
  • Treatment with Diacerein may cause an increase in enterocolic events in patients undergoing antibiotic and/or chemotherapy which could affect the intestinal flora.

[edit] PREGNANCY AND LACTATION

  • Diacerein should not be administered during pregnancy.
  • Diacerein should not be prescribed to lactating women due to reports that small amounts of Diacerein derivatives pass into the maternal milk

[edit] SIDE EFFECTS

Accelerated intestinal transit is the most frequently reported side-effect (7%) associated with Diacerein treatment. The symptoms may appear within the first few days of treatment. In most cases these symptoms resolve spontaneously with continuing treatment. Diarrhea and epigastric pain and disturbances were reported in 3-5% of the treated patients, with nausea and vomiting reported in less than 1% of the patients.

The intake of Diacerein may sometimes result in a more intense yellow colouring of the urine. This is typical of the type of compound and is of no clinical significance.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib