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Active ingredients
Diacerein
Release form
Capsules
Composition
Active ingredient: Diacerein Auxiliary substances: magnesium stearate - 12, 5 mg, lactose monohydrate (Capsulac 60) - up to 250 mg; Active substance concentration (mg): 50 mg
Pharmacological effect
NSAID, anthraquinoline derivative, diacetylated rhein derivative. Metabolizing to the active metabolite, Rein, inhibits the activity of interleukin-1, which plays an important role in the development of inflammation and degradation of cartilage in osteoarthrosis. Inhibits the action of other cytokines (including interleukin-6, TNFα). The action develops in 2-4 weeks. Diacerein has analgesic and anti-inflammatory activity when taken orally.
Pharmacokinetics
AbsorptionAfter ingestion is rapidly absorbed from the gastrointestinal tract. With a single dose of 50 mg Cmax in plasma - 3.15 mg / l. Tmax - 144 min. Bioavailability is increased by 25% when taken with food. Distribution When repeated intake due to cumulation of the drug Cmax in the plasma increases. Rein binding to plasma proteins (albumin) is almost 100%. Derivation T1 / 2 - 255 min. Excreted by the kidneys in unchanged form (20%), as glucuronide (60%), as sulfate - 20%.
Indications
Primary and secondary osteoarthritis.
Contraindications
Hypersensitivity to diacerein, other components (including anthraquinone drugs (laxatives), age under 18. Lactose intolerance, lactase deficiency, glucose galactose malabsorption
Precautionary measures
Do not exceed the recommended dose. With caution: severe hepatic or renal failure, intestinal obstruction, inflammatory bowel disease.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation. When taking the drug, you must cancel breastfeeding.
Dosage and administration
Inside, after eating, it is necessary to swallow whole, without chewing, drinking water, 50 mg 2 times a day (in the morning and in the evening). Continuously long or in courses (at least 4 months). Diaflex Rompharm during the first 2 weeks may cause an acceleration of transit in the intestine, therefore it is recommended to begin treatment with one capsule per day in the evening with food for 4 weeks. Then the dose is increased to 100 mg / day.
Side effects
On the part of the digestive system: diarrhea, nausea, vomiting, abdominal pain, hepatitis.Allergic reactions: urticaria, fever, bronchospasm, angioedema, anaphylactic shock. Other: malaise, intense urine staining (depending on pH) from yellow to brown (no clinical significance).
Overdose
Symptoms: diarrhea, weakness. Treatment: symptomatic therapy. In severe diarrhea, plasma electrolyte control is necessary.
Interaction with other drugs
Diaflex Rompharm is not recommended to be taken together with drugs that increase the volume of intestinal contents (for example, a large amount of fiber). Medicines containing aluminum hydroxide and / or magnesium hydroxide, reduce the bioavailability of diacerein. Antacids reduce the absorption of the drug. When taken simultaneously with antibiotics or chemotherapeutic drugs , affecting the intestinal microflora, may increase the frequency of adverse events on the part of the intestine. Simultaneous use with laxatives you are not recommended.
special instructions
Treatment can be long. Before the onset of the therapeutic effect, diacerein can be taken simultaneously with analgesics (including COX inhibitors). Periodic monitoring of blood parameters, functional liver tests (determination of hepatic transaminase levels), urine (determination of creatinine and CC) is necessary. ). In case of deterioration of renal function, it is necessary to reduce the dose of the drug. In patients with chronic renal failure, with CC less than 30 ml / min, the dose of diacerein should be reduced to 50 mg / day and then titrated according to tolerability and clinical efficacy. Urine staining can make it difficult to interpret the results of urinalysis (for example, glucose content). Effect on the ability to drive vehicles and control mechanismsNo data.