Tirase

Tirase

diacerein

Manufacturer:

Windlas Biotech

Distributor:

Maxxcare

Marketer:

Mega Lifesciences
Full Prescribing Info
Contents
Diacerein.
Description
Each hard gelatin capsule contains: Diacerein 50mg.
Diacerein is an anthracene derivative. It has shown to be as effective as NSAID in reducing pain and inflammation along with a positive effect on the growth of the cartilage, thus found to be effective in management of osteoarthritis.
Molecular formula: C19H12O8.
Molecular weight: 368.30.
Diacerein is available as a fine yellow powder.
Tirase is available as - Maroon coloured cap/Maroon coloured body size "2" hard gelation capsule containing yellow coloured granular powder.
Excipients/Inactive Ingredients: Maize starch BP, Microcrystalline cellulose BP, Purified Talc BP, Magnesium stearate BP.
Action
Pharmacology: Pharmacodynamics: Diacerein is a prodrug. After metabolism in the liver, the active metabolite rhein is formed. Rhein is a selective inhibitor of Interleukin - 1 (IL-1). This unique mode of action make diacerein superior to the conventionally used NSAIDs for the treatment of OA. Diacerein has beneficial effects on the anabolic processes that occur in the cartilage. It increases the production of transforming growth factor-β (TGF-β) that triggers chondrocyte proliferation and stimulates the production of collagen & proteoglycan.
Pharmacokinetics: Absorption: Diacerein is well absorbed following oral dosing. Diacerein is taken with food, there is an increase in the absorption by 24%.
Distribution: Total protein binding of rhein is about 99%. It achieves synovial fluid concentration of 0.3 to 3.0 milligrams/liter. Peak plasma concentration of rhein was reached 15-30 minutes after dosing.
Metabolism: Diacerein is metabolized extensively (100%) in liver following oral dosing, to the deacetylated active metabolite rhein, prior to entering systemic circulation. Major active metabolites include Rhein glucuronide and Rhein sulfate with half-life being 7 to 8 hours. In healthy adults, rhein has plasma half life of 4.2 hours after the first 50mg dose.
Excretion: Diacerein is eliminated mainly by the kidneys (20% unchanged form, 60% glucuronide and 20% sulphate derivatives).
Indications/Uses
Symptomatic relief in long-term treatment of osteoarthritis.
Dosage/Direction for Use
The usual dosage regimen is one capsule taken orally twice a day with the main meals for prolonged periods (not less than 6 months).
However, as Diacerein may cause acceleration intestinal transit time during the first 2 weeks of treatment, it is recommended that treatment be started with one capsule per day taken orally with 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.
The doctor should decide the duration of treatment as a function of the outcome. However this should not be less than 6 months.
As with prolonged treatment with any other medication, a complete blood test, including liver enzymes, and urine analysis should be conducted every 6 months.
Due to its late onset of action (after 2-4 weeks of treatment). Diacerein may be associated with a non-steroidal anti-inflammatory drug or analgesic for the first 2-4 weeks of treatment.
Children: No Clinical studies have been conducted in children. As the safety and efficacy on the product have not been established in this age group, its use is not recommended.
Elderly: No change in the usual recommended dose is necessary in elderly subjects.
Renal Insufficiency: In subjects with moderate renal insufficiency, the daily dose should be decreased by 50% of the recommended dose for adults.
Diacerein is contraindicated in subjects with severe renal insufficiency.
Hepatic insufficiency: No significant deviations were observed in any of the pharmacokinetic parameters in cirrhotic with mild or moderate hepatic insufficiency and therefore no dose adjustment is required in these patients.
However, the use of diacerein is contraindicated in patients with a severe deterioration of hepatic function.
Overdosage
The accidental or voluntary ingestion of high doses of Diacerein could produce diarrhoea. No specific antidotes exist. If diarrhea persists, please consult the doctor. Emergency treatment consist of restoring the hydroelectrolytic balance if necessary.
Contraindications
Diacerein is contraindicated in patients with known hypersensitivity to the drug or those with previous episodes of hypersensitivity to anthraquinone derivatives.
The benefit/risk ratio of administering Diacerein to patients with previous episode of enterocolic disturbances and IBS must be considered.
Combined use with laxatives is contraindicated.
Special Precautions
Severe renal insufficiency modifies the pharmacokinetics of Diacerein and therefore a dose reduction is recommended in such cases (creatinine clearance < 30 ml/min). When diacerein is taken with food, there is an increase (about 24%) in the absorption of Diacerein; on the other hand, severe nutritional deficiencies decrease the bioavailability of Diacerein. As the incidence of collateral effects, such as accelerated intestinal transit time, is directly proportional to the amount of unabsorbed Diacerein, the intake of the product in a fasting state or after very small amounts of food could cause an increased incidence of collateral effects.
Effect on ability to drive and use machines: No sedative effect, which may affect the ability to handle machines, is known for Diacerein. It should not be prescribed clinical studies have been undertaken in this age-group.
Use in Pregnancy: Safety during Pregnancy is not established hence not recommended in pregnancy.
Use in Lactation: Not recommended in lactating mother as safety in lactating mother is not established.
Use in Children: Safety and effectiveness in children have not been established.
Laxatives should not be taken concomitantly with Diacerein.
Use In Pregnancy & Lactation
Pregnancy: Safety during Pregnancy is not established hence not recommended in pregnancy.
Lactation: Not recommended in lactating mother as safety in lactating mother is not established.
Side Effects
Studies conducted have shown that Diacerein is well tolerated. Commonly seen adverse effects are diarrhoea, and abdominal pain, which are expected owing to the chemical nature of the drug. In small percentage of patient dark yellow coloured urine has been reported. This is due to excretion of diacerein metabolites via the urine and is of no clinical significance. There were no changes in any laboratory safety variables, especially those related to liver and kidney function.
Drug Interactions
Diacerein must not be administered as the same time as drugs that modify intestinal transit and/or the quality of the intestinal content (eg excess fibres or phytates).
The concomitant administration of products containing aluminium hydroxide and / or magnesium hydroxide should be avoided in order to maximize 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.
Caution For Usage
Incompatibilities: None.
Storage
Protect from light and moisture.
Store below 30°C in a dry place.
Shelf Life: 24 months from the date of manufacture.
MIMS Class
Other Drugs Acting on Musculo-Skeletal System
ATC Classification
M01AX21 - diacerein ; Belongs to the class of other non-steroidal antiinflammatory and antirheumatic products.
Presentation/Packing
Cap 50 mg x 3 x 10's.
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