Sustalong^® (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Ellara, LLC (Russia)

ATC Code

M09AX (Other drugs for the treatment of musculoskeletal system diseases)

Active Substances

Chondroitin sulfate sodium (Ph.Eur.)

Glucosamine (Rec.INN)

Dosage Form

Sustalong®

Lyophilizate for the preparation of a solution for intramuscular administration 200 mg+50 mg/ 1 ml: 250 mg amp.

Dosage Form, Packaging, and Composition

Lyophilizate for the preparation of a solution for intramuscular administration is a white with a yellowish tint amorphous powder or a porous mass compacted into a tablet; the reconstituted solution is transparent with a yellowish tint.

Excipients: trometamol – to pH 3.0-5.0.

Solvent composition (per 1 ml)*: active substance – lidocaine hydrochloride monohydrate (calculated as lidocaine hydrochloride) – 20 ml, excipients – Sodium chloride – 6 mg, sodium hydroxide – to pH 5.0-7.0, water for injection – up to 1 ml.

* in case the drug is packaged in a kit with a solvent.

250 mg – ampoules made of light-protective glass (6) – contour cell packaging (1) – cardboard packs.
250 mg – ampoules made of light-protective glass (6) – contour cell packaging (2) – cardboard packs.
250 mg – ampoules made of light-protective glass (6) – contour cell packaging (3) – cardboard packs.
250 mg – ampoules made of light-protective glass (6) – contour cell packaging (4) – cardboard packs.
250 mg – ampoules made of light-protective glass (6) – contour cell packaging (5) – cardboard packs.
250 mg – ampoules made of light-protective glass (6) – contour cell packaging (1) (in a kit with a solvent) – cardboard packs.
250 mg – ampoules made of light-protective glass (6) – contour cell packaging (2) (in a kit with a solvent) – cardboard packs.

Clinical-Pharmacological Group

Drug stimulating the process of regeneration of cartilage tissue

Pharmacotherapeutic Group

Drugs for the treatment of musculoskeletal system diseases; other drugs for the treatment of musculoskeletal system diseases

Pharmacological Action

A combined agent that stimulates the regeneration of cartilage tissue.

Glucosamine sulfate is one of the components of hyaluronic acid synthesis, which is necessary for the formation of proteoglycans of the structural matrix of joints.

It has also been established that glucosamine sulfate protects articular cartilage from the damaging effects of some NSAIDs. The sulfate ion is necessary for the synthesis of glycosaminoglycans, which are esters of sulfuric acid. Oral intake of exogenous glucosamine stimulates the production of cartilage matrix and provides its non-specific protection. It has a certain anti-inflammatory effect.

Chondroitin sulfate, regardless of whether it is absorbed in its intact form or as individual fragments, serves as an additional substrate for the formation of a healthy cartilage matrix. It stimulates the formation of hyaluronan, the synthesis of proteoglycans and type II collagen, and also protects the cartilage tissue matrix from enzymatic cleavage (by suppressing hyaluronidase activity) and from the damaging effects of free radicals. It maintains the viscosity of synovial fluid, stimulates the mechanisms of cartilage repair and suppresses the activity of those enzymes (elastases, hyaluronidases) that break down cartilage. In the treatment of osteoarthritis, it alleviates the symptoms of this disease and reduces the need for NSAIDs.

Pharmacokinetics

Glucosamine and chondroitin sulfate are easily absorbed upon intramuscular administration and distributed in tissues.

Glucosamine

After administration, glucosamine is first detected in plasma components and later penetrates into tissues. C_max is found in the liver, kidneys, and articular cartilage. About 30% persists for a long time in bone and muscle tissues. The fraction of glucosamine that is not metabolized or bound to plasma proteins is excreted primarily by the kidneys. The final T_1/2 of the active substance bound to plasma proteins is 70 hours.

Chondroitin sulfate

Significant concentrations are detected in the blood 30 minutes after intramuscular administration; after 15 minutes – in the synovial fluid. C_max in blood plasma is reached 1 hour after administration, then the concentration gradually decreases over 2 days. It accumulates mainly in cartilage tissue (C_max in articular cartilage is reached after 48 hours); the synovial membrane is not an obstacle to the penetration of the active substance into the joint cavity. Chondroitin sulfate is metabolized by desulfation (after administration of low molecular weight chondroitin sulfate). Chondroitin sulfate is eliminated from the body mainly by the kidneys within 24 hours.

Indications

Osteoarthritis of peripheral joints and spine.

ICD codes

Dosage Regimen

Administer intramuscularly three times per week.

Reconstitute the lyophilizate in one ampoule with 1 ml of the supplied solvent (lidocaine hydrochloride solution) prior to administration.

Inject the entire volume of the prepared solution.

The standard treatment course is 4 to 6 weeks.

Administer repeated courses as indicated for the prevention of disease exacerbations.

Do not exceed the recommended frequency of administration.

Discontinue treatment immediately if allergic reactions or hemorrhages occur.

Monitor blood coagulation parameters more frequently if used concomitantly with anticoagulants, antiplatelet agents, or fibrinolytics.

Adverse Reactions

Blood and lymphatic system disorders methemoglobinemia.

Immune system disorders skin rash, urticaria (on the skin and mucous membranes), skin itching, angioedema, anaphylactic shock, exacerbation of bronchial asthma.

Nervous system disorders dizziness, headache, drowsiness, insomnia; weakness, motor restlessness, nystagmus, loss of consciousness, visual and auditory disturbances, tremor, trismus, convulsions (the risk of their development increases against the background of hypercapnia and acidosis), paralysis of the respiratory muscles, respiratory arrest, motor and sensory block, paralysis of the respiratory center.

Cardiac disorders bradycardia, arrhythmia, tachycardia, chest pain, increase or decrease in blood pressure, peripheral vasodilation, collapse.

Gastrointestinal disorders abdominal pain, flatulence, constipation or diarrhea, nausea, vomiting, involuntary defecation.

Renal and urinary disorders involuntary urination.

General disorders leg pain and peripheral edema.

Other respiratory depression, up to arrest, hypothermia.

Contraindications

Hypersensitivity to glucosamine, chondroitin sulfate; thrombophlebitis; phenylketonuria; cardiac conduction disorders; acute heart failure; history of epileptiform seizures; severe liver and/or kidney dysfunction; pregnancy, breastfeeding period; children and adolescents under 18 years of age.

With caution

Chronic heart failure; arterial hypotension; bronchial asthma; diabetes mellitus; tendency to bleeding; hypersensitivity to seafood (shrimp, shellfish).

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and during breastfeeding.

Use in Hepatic Impairment

Severe liver dysfunction.

Use in Renal Impairment

Severe kidney dysfunction.

Pediatric Use

Contraindicated in children under 18 years of age (efficacy and safety have not been established).

Geriatric Use

Approved for use in elderly patients.

Special Precautions

Use with caution in patients with impaired glucose tolerance.

When used concomitantly with indirect anticoagulants, antiplatelet agents, fibrinolytics, more frequent monitoring of blood coagulation parameters is required.

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

Repeated courses of treatment are indicated to prevent exacerbations.

Influence on the ability to drive vehicles and mechanisms

During the treatment period, it is necessary to refrain from driving vehicles and other moving mechanisms, and also to exercise caution when performing potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Increases the absorption of tetracyclines, reduces the effect of semi-synthetic penicillins.

This combination is compatible with NSAIDs and corticosteroids.

Use with caution simultaneously with direct-acting anticoagulants. It is also possible to enhance the effect of indirect anticoagulants, antiplatelet agents and fibrinolytics.

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.