Sustagard Artro solution for injection 200mg / ml, No. 5

Primary and secondary osteoarthritis;

osteochondrosis;

spondyloarthrosis.

V / m (only). The drug is not intended for intravenous administration.

Immediately before administration, mix the contents of ampoule A with ampoule B (solvent) in one syringe. The prepared solution (3 ml) is injected intramuscularly 3 times a week for 4-6 weeks.

Injections of the drug can be combined with oral glucosamine.

Concentrate for the preparation of a solution for intramuscular injection (ampoule A) in the form of a clear liquid, colorless or light yellow, or greenish-yellow, or brownish-yellow; solvent (ampoule B) - colorless transparent liquid; the prepared solution (ampoule A + ampoule B) is a colorless or light yellow, or greenish-yellow, or brownish-yellow transparent liquid without suspended particles.

Ampoule A:

1 amp. (2 ml)

glucosamine sulfate sodium chloride 502.5 mg

contains glucosamine sulfate 400 mg

sodium chloride 102.5 mg

* in terms of dry matter.

Excipients: lidocaine hydrochloride, sodium metabisulfite, concentrated hydrochloric acid, water d / i.

Solvent (ampoule B): diethanolamine, water d / i.

• Hypersensitivity

Due to the content of lidocaine hydrochloride:

• cardiac conduction disorders;

• acute heart failure;

• history of epileptiform seizures;

• severe impairment of liver and kidney function;

• the period of pregnancy and breastfeeding;

• children and adolescents up to 18 years old.

With caution: patients with chronic heart failure and arterial hypotension.

With intolerance to seafood (shrimp, shellfish), the likelihood of developing allergic reactions to the drug increases.

The safety of using anesthetics of the lidocaine hydrochloride group is questionable in patients prone to malignant hyperthermia, therefore, in such cases, their use should be avoided. Special care must be taken when using the drug in patients with circulatory insufficiency, impaired liver and / or kidney function. Care should be taken when prescribing lidocaine hydrochloride to elderly patients, patients with epilepsy, cardiac conduction disorders, and respiratory failure.

pharmachologic effect

Stimulator of tissue regeneration. The drug has a stimulating regeneration of cartilage tissue, anabolic, anti-catabolic, chondroprotective, anti-inflammatory, analgesic effects.

Glucosamine sulfate, the active component of SustagardЃ Artro, is a salt of natural amino-monosaccharide glucosamine, which is physiologically contained in the body. Glucosamine stimulates the synthesis of proteoglycans (glucosaminoglycans and hyaluronic acid) of the synovial fluid by chondrocytes; inhibits enzymes (including collagenase, phospholipase A2) that cause the destruction of cartilage tissue; prevents the formation of superoxide radicals, inhibits the activity of lysosomal enzymes; initiates the process of fixing sulfur in the synthesis of chondroitinsulfuric acid and promotes the normal deposition of calcium in bone tissue; prevents the damaging effect of corticosteroids on chondrocytes and disruption of glycosaminoglycan synthesis induced by non-steroidal anti-inflammatory drugs.

Sulfo groups are also involved in the synthesis of glycosaminoglycans and the metabolism of cartilage tissue, and side chain sulfoesters in proteoglycans, contributing to water retention, in maintaining the elasticity of the cartilage matrix.

Glucosamine sulfate stops cartilage destruction and reduces symptoms of osteoarthritis. Reduction of clinical symptoms usually manifests itself after 2 weeks from the start of treatment with the preservation of clinical improvement for 8 weeks after discontinuation of the drug.

Pharmacokinetics

Absorption and distribution

After i / m administration of glucosamine, sulfate quickly passes through biological barriers and penetrates into tissues, mainly articular cartilage.

Withdrawal

T1 / 2 - about 60 hours. It is excreted mainly by the kidneys.

Side effect

From the digestive system: flatulence, diarrhea, constipation.

Allergic reactions: urticaria, itching.

Local reactions: a slight burning sensation (disappears with the development of the anesthetic effect within 1 min), thrombophlebitis.

Adverse reactions due to lidocaine, which is part of the drug

From the digestive system: nausea, vomiting.

From the nervous system: numbness of the tongue and oral mucosa, drowsiness, diplopia, headache, dizziness, tremors, euphoria, disorientation.

From the side of the cardiovascular system: impaired cardiac conduction.

Allergic reactions: edema, anaphylactic shock.

Disulfite, which is part of the solution for intramuscular sodium administration, can in rare cases cause severe hypersensitivity reactions and bronchospasm.

special instructions

SustagardЃ Artro should be prescribed with caution to patients with impaired glucose tolerance, patients with bronchial asthma.

One dose of the drug in the form of a solution for intramuscular administration contains 40.8 mg of sodium. This should be taken into account when prescribing to patients who are shown a strict salt-free diet.

Due to the fact that the injectable form of the drug includes the auxiliary substance lidocaine, before using it, it is necessary to conduct a skin test for individual sensitivity to the drug, which may be indicated by edema and redness of the injection site.

Influence on the ability to drive vehicles and mechanisms

The effect of glucosamine on the ability to drive vehicles and mechanisms has not been considered. It should be borne in mind that the drug contains lidocaine, which can have a temporary effect on motor ability and coordination. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities.

Overdose

No cases of overdose have been identified.

Symptoms: the drug contains the excipient lidocaine hydrochloride. The first symptoms of an overdose of lidocaine hydrochloride from the central nervous system may be numbness of the tongue and lips, agitation, anxiety, tinnitus, dizziness, blurred vision, tremor, depression, drowsiness.

Treatment: it is necessary to monitor the functions of the cardiovascular and respiratory system. A change in the relevant parameters may indicate an overdose of the drug, therefore, the patient should be provided with oxygen immediately. With the development of any complications, symptomatic therapy is carried out.

Drug interactions

Glucosamine sulfate is compatible with NSAIDs, paracetamol and GCS.

Drug interaction due to the presence of lidocaine in the composition of the drug

Cimetidine, peptidine, bupivacaine, propranolol, quinidine, disopyramide, amitriptyline, nortriptyline, chlorpromazine, imipramine increase the concentration of lidocaine in the blood plasma, reducing its hepatic metabolism.

With simultaneous use with class IA antiarrhythmic drugs (including quinidine, procainamide, disopyramide), the QT interval is lengthened, in very rare cases, the development of AV blockade or ventricular fibrillation is possible.

When used simultaneously with sedatives, the sedative effect is enhanced.

Phenytoin enhances the cardiodepressant effect of lidocaine.

With simultaneous use with procainamide, delirium, hallucinations are possible.

Lidocaine can enhance the effect of drugs that predetermine the blockade of neuromuscular transmission, since the latter reduce the conduction of nerve impulses.

Ethanol enhances the inhibitory effect of lidocaine on respiration.