Artrollar^® (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Ellara, LLC (Russia)

ATC Code

M01AX25 (Chondroitin sulfate)

Active Substance

Chondroitin sulfate sodium (Ph.Eur. European Pharmacopoeia)

Dosage Form

Artrollar®

Lyophilizate for preparation of solution for intramuscular and intra-articular administration 100 mg: amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Lyophilizate for preparation of solution for intramuscular and intra-articular administration in the form of a white, porous, compacted into a tablet mass.

Excipients: sodium disulfite – 0.5 mg.

Solvent: water for injections, solvent for preparation of medicinal forms for injections (ampoules 1 ml or 2 ml).

Glass ampoules (5) – cardboard packs with an insert.
Glass ampoules (10) – cardboard packs with an insert.
Glass ampoules (5) – contour cell packs (1) – cardboard packs.
Glass ampoules (5) – contour cell packs (2) – cardboard packs.
Glass ampoules (5) – contour cell packs (1) in a set with a solvent (amp. 1 ml 5 pcs. in a contour cell pack (1 pc.)) – cardboard packs.
Glass ampoules (5) – contour cell packs (1) in a set with a solvent (amp. 2 ml 5 pcs. in a contour cell pack (1 pc.)) – cardboard packs.

Clinical-Pharmacological Group

Drug regulating metabolism in cartilage tissue

Pharmacotherapeutic Group

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

Pharmacological Action

The agent affecting phosphorus-calcium metabolism in cartilage tissue is a high-molecular-weight mucopolysaccharide. It has chondrostimulating, regenerating, anti-inflammatory, and analgesic effects.

Chondroitin sulfate is involved in the construction of the fundamental substance of cartilage and bone tissue. It has chondroprotective properties, enhances metabolic processes in hyaline and fibrous cartilage, and subchondral bone; inhibits enzymes causing degradation (destruction) of articular cartilage; stimulates the production of proteoglycans by chondrocytes.

It helps reduce the release of inflammatory mediators and pain factors into the synovial fluid, suppresses the secretion of leukotrienes and prostaglandins. It slows down bone tissue resorption and reduces calcium loss, accelerates bone tissue repair processes.

Chondroitin sulfate slows the progression of osteoarthritis and osteochondrosis. It promotes the restoration of the joint capsule and cartilaginous surfaces of the joints, prevents the collapse of connective tissue, and normalizes the production of synovial fluid.

Due to its structural similarity to heparin, it may potentially prevent the formation of fibrin thrombi in the synovial and subchondral microcirculatory bed.

Pharmacokinetics

After intramuscular administration, Chondroitin sulfate sodium is readily absorbed. It is detected in the blood in significant concentrations as early as 30 minutes after injection.

The C_max of Chondroitin sulfate sodium in plasma is reached after 1 hour, then gradually decreases over 2 days. Chondroitin sulfate sodium accumulates mainly in the cartilage tissue forming the joints.

The synovial membrane is not a barrier to the penetration of the agent into the joint cavity. Fifteen minutes after intramuscular injection, Chondroitin sulfate sodium is detected in the synovial fluid, then penetrates into the articular cartilage, where its C_max is reached after 48 hours.

With intra-articular administration, retention of chondroitin sulfate in the joint tissues and its gradual release into the bloodstream are observed. After a single intra-articular administration at a dose of 200 mg, C_max is reached after 1-2 hours and is 52.5-86.9 ng/ml, T_1/2 is 2.5 hours.

Indications

Degenerative-dystrophic diseases of the joints and spine (osteoarthritis of peripheral joints, intervertebral osteoarthritis and osteochondrosis), to accelerate the formation of callus in fractures.

ICD codes

Dosage Regimen

For intramuscular administration, it is prescribed at a dose of 100 mg every other day. With good tolerance, the dose is increased to 200 mg, starting from the fourth injection. The course of treatment is 25-30 injections. If necessary, repeated courses of treatment can be conducted after 6 months.

For intra-articular administration, a single dose is 200 mg. The frequency and duration of use are according to a special scheme.

Adverse Reactions

Allergic reactions infrequently – skin itching, erythema, urticaria, dermatitis, angioneurotic edema.

From the digestive system often – diarrhea, abdominal pain, nausea; frequency unknown – vomiting.

Local reactions pain and hemorrhages at the injection site.

Contraindications

Hypersensitivity to chondroitin sulfate, tendency to bleeding, thrombophlebitis; pregnancy, breastfeeding period; children and adolescents under 18 years of age; presence of active inflammatory and infectious processes in the joint, presence of active skin disease and skin infection in the area of the intended injection.

With caution

Concomitant use with direct-acting anticoagulants.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

There are no specific instructions for use in elderly patients.

Special Precautions

In case of allergic reactions or hemorrhages, treatment should be discontinued.

Drug Interactions

It is possible to enhance the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics, which requires more frequent monitoring of blood coagulation parameters when used concomitantly.

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.