Diaflex rompharm capsules 50mg, No. 30

Symptomatic treatment of osteoarthritis of the hip and knee joints.

The drug is taken orally during meals. The capsule must be swallowed whole without chewing, drinking plenty of water.

The drug should be prescribed by a specialist with experience in the treatment of osteoarthritis.

It is recommended to start treatment by taking 1 capsule (50 mg) / day with a meal (for example, dinner) for 4 weeks, because during the first 2 weeks of use, the drug can cause an acceleration of the transit of intestinal contents.

Then the dose is increased to 100 mg / day - 1 capsule (50 mg) 2 times / day (morning and evening).

Treatment is carried out continuously for a long time or in courses lasting at least 4 months.

In patients with moderate renal insufficiency (CC 30-60 ml / min), the dose of the drug should be reduced to 50 mg / day.

Hard gelatin capsules, size 1, yellow with a slight brownish tint; the contents of the capsules are yellow powder.

1 caps. diacerein 50 mg

Excipients: magnesium stearate - 12.5 mg, lactose monohydrate (capsule 60) - up to 250 mg.

• Hypersensitivity to diacerein, other components of the drug or anthraquinone derivatives (for example, laxatives);

• lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

• pregnancy;

• lactation period (breastfeeding);

• liver diseases, incl. history;

• severe renal failure (CC less than 30 ml / min);

• inflammatory bowel disease (ulcerative colitis, Crohn's disease);

• intestinal obstruction;

• abdominal pain of unknown origin;

• age up to 18 years.

With care: renal failure of moderate severity (CC 30-60 ml / min), irritable bowel syndrome; age over 65.

pharmachologic effect

Diacerein is an anthraquinoline derivative, a diacetylated rhein derivative. Metabolized to the active metabolite - rhein, inhibits the activity of interleukin-1, which plays an important role in the development of inflammation and cartilage degradation in osteoarthritis.

Diacerein inhibits the action of other cytokines that cause inflammation, incl. interleukin-6, TNF- ?. Slows down the synthesis of metalloproteinases (collagenase, elastase), which contribute to damage to cartilage tissue. With prolonged use, diacerein stimulates the synthesis of proteoglycans, does not affect the synthesis of prostaglandins.

The drug has analgesic and anti-inflammatory activity when taken orally. The action develops in 2-4 weeks.

Pharmacokinetics

Suction

After oral administration, diacerein is rapidly absorbed from the gastrointestinal tract. With a single dose of 50 mg, Cmax in plasma is 3.15 mg / l. Tmax - 144 min. Bioavailability is 50-65% and increases by 25% when taken simultaneously with food.

Distribution

With repeated administration in connection with the cumulation of the drug, Cmax in plasma increases.

The binding of rhein to plasma proteins (albumin) is almost 100%. Rein accumulates in organs and tissues for up to 168 hours after ingestion. The highest concentration of rhein is observed in the kidneys and spleen. It accumulates in small amounts in the brain tissue, bone marrow, bone tissue and the eyeball.

Rein crosses the BBB and the placental barrier. Transplacental transfer is about 3% of rhein concentration in blood plasma 45 minutes after ingestion.

Metabolism

Diacerein is completely deacetylated to rhein, an active metabolite.

Withdrawal

T1 / 2 - 255 min. It is excreted by the kidneys unchanged (20%), in the form of glucuronide (60%), in the form of sulfate - 20%.

Side effect

From the immune system: infrequently - allergic reactions, urticaria, bronchospasm, angioedema, anaphylactic shock.

From the gastrointestinal tract: rarely - diarrhea, nausea, vomiting, abdominal pain.

From the liver and biliary tract: infrequently - an increase in the activity of hepatic enzymes.

On the part of the skin and subcutaneous tissues: infrequently - itching, rash.

General disorders: rarely - malaise; frequency unknown - intense staining of urine (depending on pH) from yellow to brown (has no clinical significance and does not require drug withdrawal or dose reduction).

If any adverse reactions not described in these instructions occur, the patient should stop taking the drug and inform the attending physician about it.

Application during pregnancy and lactation

Studies confirming the safety of using diacerein during pregnancy and breastfeeding have not been conducted. There are no data on the effect of diacerein on the fetus.

The drug is contraindicated during pregnancy and during breastfeeding. When taking the drug, breastfeeding should be canceled.

Application for violations of liver function

The use of the drug is contraindicated for liver diseases, incl. history.

Application for impaired renal function

The use of the drug is contraindicated in severe renal failure (CC less than 30 ml / min).

The drug should be prescribed with caution in case of moderate renal failure (CC 30-60 ml / min).

Application in children

The use of the drug under the age of 18 is contraindicated.

Use in elderly patients

The drug should be prescribed with caution to patients over the age of 65 years.

special instructions

Treatment can be lengthy.

Before the onset of the therapeutic effect, diacerein can be taken simultaneously with analgesic drugs (including NSAIDs).

Periodic monitoring of blood counts, liver function tests (hepatic transaminase activity), determination of the concentration of creatinine and CK are required.

In case of deterioration of renal function, it is necessary to reduce the dose of the drug.

Staining urine can make it difficult to interpret urinalysis results (such as glucose).

Taking diacerein can lead to the development of diarrhea, which can lead to dehydration and hypokalemia. If diarrhea develops, the use of diacerein should be discontinued.

Influence on the ability to drive vehicles and use mechanisms

The effect of diacerein on the ability to drive vehicles and mechanisms has not been studied.

Overdose

Symptoms: diarrhea, weakness.

Treatment: carrying out symptomatic therapy. With severe diarrhea, it is necessary to replenish the water and electrolyte balance.

Drug interactions

Medicines containing aluminum hydroxide and / or magnesium hydroxide (antacids) reduce the bioavailability of diacerein.

When taken simultaneously with antibiotics or chemotherapeutic drugs that affect the intestinal microflora, as well as substances that increase the volume of intestinal contents and the rate of emptying (for example, a large amount of fiber), the frequency of adverse events from the intestine may increase.

Simultaneous use with laxatives is not recommended.