Artrox

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ARTROX (ARTROX)

Composition:

Active substance: sodium chondroitin sulfate;

1 vial (2 ml of medicinal product) contains 200 mg of sodium chondroitin sulfate;

Excipients: benzyl alcohol, water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless or slightly yellowish solution.

Pharmacotherapeutic group. Drugs affecting the musculoskeletal system. Chondroitin sulfate. ATC code M01AX25.

Pharmacological Properties

Pharmacodynamics

The active ingredients of the medicinal product are sodium salts of chondroitin sulfate A and C (average molecular weight 11,000 daltons). Chondroitin sulfate is a high-molecular-weight mucopolysaccharide and is a key component of proteoglycans, which together with collagen fibers form the cartilage matrix.

The medicinal product inhibits the degenerative process and stimulates regeneration of cartilage tissue, exerting chondroprotective, anti-inflammatory, and analgesic effects. It replaces chondroitin sulfate in articular cartilage that has been catabolized by the pathological process. It inhibits the activity of enzymes responsible for degradation of articular cartilage: specifically, it inhibits metalloproteinases, including leukocyte elastase. It reduces hyaluronidase activity. It partially blocks the release of reactive oxygen species and promotes inhibition of chemotaxis and antigenic determinants. It stimulates chondrocytes to produce proteoglycans and influences calcium-phosphate metabolism in cartilage tissue. It helps restore the mechanical and elastic integrity of the cartilage matrix. The anti-inflammatory and analgesic effects are achieved by reducing the release of inflammatory mediators and pain-inducing factors into the synovial fluid by synoviocytes and macrophages of the synovial membrane, as well as by inhibiting the secretion of leukotriene B and prostaglandin E.

The use of the medicinal product promotes restoration of the joint capsule and articular cartilage surfaces, prevents compression of connective tissue, acts as a lubricant for joint surfaces, normalizes the production of synovial fluid, improves joint mobility, and contributes to a reduction in pain intensity.

Chondroitin sulfate slows down bone resorption and reduces calcium loss, while accelerating bone tissue regeneration processes.

Pharmacokinetics

After intramuscular administration, chondroitin sulfate penetrates into the synovial fluid. Maximum concentration in synovial fluid is reached 4–5 hours after injection. It is eliminated from the body within 24 hours. Excretion occurs predominantly via the kidneys.

Clinical characteristics.

Indications.

Degenerative-dystrophic joint and spinal diseases (primary osteoarthritis, intervertebral osteochondrosis, osteoarthritis), osteoporosis, periodontal diseases, fractures (to accelerate formation of bone callus), as well as for treatment of consequences of joint surgeries.

Contraindications.

Hypersensitivity to any component of the drug, predisposition to bleeding, thrombophlebitis, renal failure, hepatic insufficiency in decompensated stage, pregnancy, lactation, pediatric age (under 18 years).

With caution: in patients with coagulation disorders; in diabetes mellitus; in patients with increased body weight; in patients on low-salt diet; in renal function impairment; in women planning pregnancy.

Interaction with other medicinal products and other types of interactions.

When used concomitantly, chondroitin sulfate may reduce the need for glucocorticoids, non-steroidal anti-inflammatory drugs, and analgesics. It exhibits synergistic effects when used simultaneously with glucosamine and other chondroprotective agents. Treatment efficacy increases when diet is enriched with vitamins A and C, and salts of manganese, magnesium, copper, zinc, and selenium.

When used concomitantly with acetylsalicylic acid or other anticoagulants or antiplatelet agents, monitoring of blood coagulation is recommended. Chondroitin may affect serum concentration of tetracycline when used concomitantly with tetracyclines.

Special precautions for use.

To achieve a stable clinical effect, at least 25 injections of the medicinal product are required. The effect persists for many months after completion of treatment. To prevent exacerbations, repeated treatment courses should be administered. Dose escalation under physician supervision is recommended for patients with excess body weight, gastric peptic ulcer, those receiving concomitant diuretic therapy, and at the beginning of treatment when a faster clinical response is needed.

Treatment should be discontinued in case of allergic reactions or hemorrhages.

1 ml of the medicinal product contains 9 mg of benzyl alcohol; therefore, it should not be used in premature infants and newborns. Benzyl alcohol may cause toxic and allergic reactions in infants and children under 3 years of age.

Use during pregnancy or breastfeeding.

Contraindicated during pregnancy and breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

There are no restrictions regarding driving or operating complex machinery during use of this medicinal product.

Dosage and Administration

Administer the medicinal product intramuscularly to adults at a dose of 1 ml every other day. If well tolerated, increase the dose to 2 ml starting from the fourth injection. Treatment course: 25–35 injections. Repeat courses: every 6 months.

Children. There is no experience with the use of the medicinal product in children.

Overdose.

To date, there have been no reports of overdose symptoms associated with the use of chondroitin sulfate. Nevertheless, exceeding the recommended daily dose may enhance the drug's adverse effects. Treatment is symptomatic.

Adverse Reactions

Frequency of adverse reactions according to the MedDRA classification: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10000 to < 1/1000), very rare (< 1/10000), frequency not known (cannot be estimated based on available data).

The frequency of adverse reactions with this medicinal product is unknown.

When using the medicinal product in individuals with hypersensitivity to it, the following disorders may occur:

Immune system disorders: allergic reactions, anaphylactic shock, angioneurotic edema;

Skin and subcutaneous tissue disorders: skin rashes, pruritus, erythema, urticaria, dermatitis, alopecia; at the injection site, redness, pruritus, and swelling may occur;

Gastrointestinal disorders: nausea, vomiting, abdominal pain, flatulence, dyspeptic symptoms, diarrhea;

Other: disorders of the visual organs, keratopathy, dizziness, peripheral edema.

Reporting of suspected adverse reactions

Reporting of suspected adverse reactions after registration of the medicinal product is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions.

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children. Do not use any leftover medicinal product.

Incompatibility. No incompatibility cases have been documented since the beginning of chondroitin sulfate use (1960); however, mixing solutions of high-molecular-weight polysaccharides (including chondroitin sulfate) with solutions of other medicinal products should be avoided.

Packaging. 2 mL in a vial; 5 vials in a blister pack; 2 blister packs in a cardboard box.

Prescription status. Prescription only.

Manufacturer. Limited liability company "Novofarm-Biosyntez".

Manufacturer's address and place of business.

38, Zhytomyrska Street, city of Zviahel, Zviahel district, Zhytomyr region, 11700, Ukraine.