Diaflex Rompharm (Capsules) Instructions for Use

Marketing Authorization Holder

S.C. Rompharm Company S.R.L. (Romania)

ATC Code

M01AX21 (Diacerein)

Active Substance

Diacerein (Rec.INN registered by WHO)

Dosage Form

Diaflex Rompharm

Capsules 50 mg: 30, 60 or 100 pcs.

Dosage Form, Packaging, and Composition

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

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

Capsule shell composition titanium dioxide – 0.75 mg, yellow iron oxide dye – 2.2125 mg, gelatin – up to 75 mg.

10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.
10 pcs. – blister packs (10) – cardboard packs.

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

Anti-inflammatory and antirheumatic drugs; non-steroidal anti-inflammatory and antirheumatic drugs; other non-steroidal anti-inflammatory and antirheumatic drugs

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, 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, 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

Administer orally. Swallow the capsule whole with a sufficient amount of water.

Initiate therapy with a dose of 50 mg once daily. Take the capsule with a meal to improve gastrointestinal tolerance and increase bioavailability.

After a minimum of two weeks, evaluate patient tolerance and clinical response. If well-tolerated and symptoms persist, increase the dosage to 50 mg twice daily.

Continue treatment for a minimum of four months to achieve full therapeutic effect. The treatment course can be extended for long-term, continuous management of osteoarthritis.

In patients with chronic renal failure and a creatinine clearance below 30 ml/min, reduce the dose to 50 mg once daily. Titrate the dose carefully based on individual tolerance and clinical efficacy.

Do not exceed the maximum recommended daily dose of 100 mg. Monitor liver function and renal parameters periodically during long-term therapy.

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

Childhood and adolescence 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 efficacy.

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 side reactions may increase.

Medicines 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.