Diagistan (Capsules) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

M01AX21 (Diacerein)

Active Substance

Diacerein (Rec.INN registered by WHO)

Dosage Form

Diagistan

Capsules 50 mg: 20, 30 or 40 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 1, yellow or yellow with a slight brownish tint; the capsule contents are a yellow or almost yellow powder.

Excipients: lactose monohydrate, povidone, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate.

Composition of the hard gelatin capsule: titanium dioxide, yellow iron oxide, gelatin.

10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.

Clinical-Pharmacological Group

Drug used for inflammatory and inflammatory-dystrophic diseases of the musculoskeletal system

Pharmacotherapeutic Group

Anti-inflammatory agent with delayed symptom-modifying action

Pharmacological Action

An anthraquinoline derivative, a deacetylated derivative of rhein. Metabolizing to the active metabolite rhein, it inhibits the activity of interleukin-1, which plays an important role in the development of inflammation and cartilage degradation in osteoarthritis.

It inhibits the action of other cytokines (including interleukin-6, TNFα). The effect develops after 2-4 weeks.

Diacerein has analgesic and anti-inflammatory activity when taken orally.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. After a single dose of 50 mg, the C_max in plasma is 3.15 mg/L. T_max is 144 min. Bioavailability increases by 25% when taken with food. With repeated administration, due to drug accumulation, the C_max in plasma increases.

Diacerein is completely deacetylated to rhein. The binding of rhein to plasma proteins (albumin) is almost 100%. Rhein penetrates the blood-brain barrier and the placental barrier. T_1/2 is 255 min.

It is excreted by the kidneys unchanged (20%), as a glucuronide (60%), and as a sulfate – 20%.

Indications

Primary and secondary osteoarthritis.

ICD codes

Dosage Regimen

Take orally, with food to increase bioavailability.

Initiate therapy at 50 mg once daily.

After two to four weeks, assess tolerance and clinical response.

If well-tolerated, increase the dose to 50 mg twice daily.

Administer the maintenance dose as one capsule in the morning and one in the evening.

Continue treatment continuously for a long term; the therapeutic effect develops gradually.

For course therapy, the minimum treatment duration is four months.

In patients with chronic renal failure and creatinine clearance below 30 ml/min, reduce the dose to 50 mg once daily.

Titrate the dose for renally impaired patients based on individual tolerance and clinical effectiveness.

Do not exceed the maximum recommended daily dose of 100 mg (two capsules).

Adverse Reactions

From the digestive system: diarrhea, nausea, vomiting, abdominal pain, hepatitis.

Allergic reactions: urticaria, fever, bronchospasm, angioedema, anaphylactic shock.

Other: malaise, intense coloration of urine (depending on pH) from yellow to brown (has no clinical significance).

Contraindications

Children and adolescents under 18 years of age; hypersensitivity to diacerein; hypersensitivity to anthraquinone laxative drugs.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Special Precautions

Use with caution in severe hepatic or renal failure, intestinal obstruction, inflammatory bowel diseases.

During treatment, periodic monitoring of blood counts, liver function tests (determination of liver transaminase levels), and urine (determination of creatinine and CC levels) is necessary.

If renal function deteriorates, the dose must be reduced. 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 tolerance and clinical effectiveness.

Drug Interactions

Diacerein is not recommended to be taken together with drugs that increase the volume of intestinal contents (for example, a large amount of fiber).

Antacids reduce the absorption of diacerein.

When taken concomitantly with antibiotics or chemotherapeutic drugs that affect the intestinal microflora, the frequency of intestinal adverse reactions may increase.

Medicinal products containing aluminum hydroxide and/or magnesium hydroxide reduce the bioavailability of diacerein.

Concomitant use with laxatives is not recommended.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.