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Composition:


active ingredient: glucosamine sulfate sodium chloride


2 ml of the solution (ampoule A) contains glucosamine sulfate sodium chloride 502.5 mg, equivalent to: glucosamine sulfate 400 mg and sodium chloride 102.5 mg;


excipients: lidocaine hydrochloride, water for injection;


solvent (ampoule B) contains:


excipients: diethanolamine, water for injection.


Dosage form. Solution for injection.


Basic physical and chemical properties: ampoule a made of Brown transparent glass contains a colorless or light yellow transparent liquid;


ampoule B (solvent) of colorless transparent glass contains a colorless transparent liquid;


ampoule A + B (solution for injection) – a clear, colorless or light yellow solution.


Pharmacotherapeutic group. Nonsteroidal anti-inflammatory and anti-rheumatic drugs.


ATX code M01A X05.


Pharmacological properties.


Pharmacodynamics.


Active substance glucosamine sulfate is a salt of the aminomonosaccharide glucosamine, which under physiological conditions is present in the human body and is used together with sulfates for the biosynthesis of hyaluronic acid in synovial fluid and glycosaminoglycans of the main substance of articular cartilage.


Thus, the mechanism of action of glucosamine sulfate is to stimulate the synthesis of glycosaminoglycans and joint proteoglycans. In addition, glucosamine has an anti-inflammatory effect and suppresses the process of destruction of articular cartilage, mainly due to the manifestations of its own metabolic properties, the ability to inhibit the activity of interleukin 1 (IL-1), which on the one hand affects the symptoms of osteoarthritis, and on the other hand delays structural damage to joints, as evidenced by data from long-term clinical studies.


According to initial in vitro and in vivo studies, exogenous administration of glucosamine sulfate stimulates proteoglycan biosynthesis, which is insufficient in osteoarthritis, promotes the fixation of sulfur ions in the synthesis of glycosaminoglycans, and improves the trophism of articular cartilage.


Subsequent studies have shown that glucosamine sulfate inhibits the synthesis of tissue-destroying substances, such as superoxide radicals, as well as the activity of lysosomal enzymes in addition to enzymes that can destroy articular cartilage tissue, such as collagenases and phospholipases A2. This effect causes a moderate anti-inflammatory effect, which is observed in animal models in vivo, including in some cases in experimental osteoarthritis, even without inhibition of cyclooxygenases, in contrast to nonsteroidal anti-inflammatory drugs (NSAIDs).


More recent studies have shown that most of the above metabolic and anti-inflammatory effects may be associated with inhibition of intracellular signal transduction by stimulating IL-1, one of the cytokines involved in the pathogenesis of osteoarthritis, followed by inhibition of cytokine-induced gene transcription. Glucosamine sulfate, due to plasma and synovial fluid concentrations recorded in patients with osteoarthritis, can actually inhibit IL-1-induced gene expression of a number of pro-inflammatory enzymes in joint tissues, as well as prodegenerative enzymes in cartilage, such as certain metalloproteases, including aggrecanases. The possible effect of sulfur ions on the mentioned pharmacodynamic properties of glucosamine has not been definitively elucidated.


All of the above properties have a beneficial effect on the degenerative processes in the cartilage that underlie the pathogenesis of osteoarthritis, as well as on the clinical picture of the disease.


Short-term and medium-term studies have shown that the effectiveness of glucosamine sulfate in relation to the symptoms of osteoarthritis is manifested as early as 2-3 weeks after the start of its use.


On the other hand, the effectiveness of treatment with glucosamine sulfate, in comparison with conventional analgesics and nonsteroidal anti-inflammatory drugs, is optimal after a course of continuous use for 6 months or after a course of use for 3 months with an obvious effect after action for 2 months after withdrawal.


The results of clinical studies of daily continuous treatment for 3 years indicate a progressive increase in its effectiveness, taking into account the symptoms and slowing of structural damage to the joints, which is confirmed by X-rays.


Glucosamine sulfate has shown good tolerability. No significant effects of glucosamine sulfate on the cardiovascular, respiratory, autonomic, or central nervous systems were found.


Pharmacokinetics.


Studies conducted in humans and animals have shown that after oral administration of 14C-glucosamine, radioactively labeled elements are rapidly and almost completely absorbed at the systemic level. In humans, about 90% of the radioactively labeled dose of the drug is absorbed. The absolute bioavailability of glucosamine in rats after oral administration of glucosamine sulfate was 26% due to the first-pass effect through the liver. Absolute bioavailability in humans is unknown, but according to allometric calculations, it is similar to that observed in rats, that is, from 20% to 30 %.


In healthy volunteers,after repeated oral administration of glucosamine sulfate at a dose of 1500 mg per day, the maximum steady-state plasma concentration (Cmax, ss) was 1602 ± 425 ng/mL (8.9 µM). This concentration was reached 1.5–4 hours (median: 3 hours) after administration (tmax). At steady state, the AUC of plasma concentrations relative to time was 14564 ± 4138 nghh/ML. These parameters were obtained when using the drug on an empty stomach, so it is not known whether food intake can significantly affect the absorption of the drug.


When administered orally after absorption, glucosamine is mainly distributed in the extravascular environment (including synovial fluid), the volume of distribution is approximately 37 times higher than the total amount of water in the human body. Binding of glucosamine to proteins was not detected.


The metabolic profile of glucosamine has not been studied, since this drug, being a natural substance present in the human body, is used for the biosynthesis of certain components of articular cartilage.


Only the final elimination Half-Life of glucosamine from human blood plasma was established, based on the results of the study of plasma glucosamine levels, which were measured within 48 hours after oral administration of the drug. The calculated value was about 15 hours.


After oral administration of 14C-glucosamine, urinary excretion of radioactively labeled elements in humans was 10 ± 9% of the administered dose ,while fecal excretion was 11.3 ± 0.1 %. The level of excretion of unchanged glucosamine in human urine after oral administration was, on average, low (approximately 1% of the administered dose). These results indicate that the kidneys do not play a significant role in the elimination of glucosamine and/or its metabolites and/or its breakdown products.


With repeated administration at a dose of 750-1500 mg once a day, the pharmacokinetics of glucosamine were linear, while with a dose of 3000 mg, plasma glucosamine levels were lower than expected in accordance with the dose increase. The pharmacokinetics of glucosamine at steady state were time-independent, with no accumulation or decrease in bioavailability compared to the pharmacokinetic profile observed after a single injection.


The pharmacokinetics of glucosamine in men and women are similar, and there are no differences in pharmacokinetics in healthy volunteers and in patients with knee osteoarthritis. In the latter, the average concentration in blood plasma 3 hours after taking the last dose of 1500 mg, with repeated use once a day, was 7.2 µM and was similar to that found in healthy volunteers, while the average concentration in synovial fluid was only 25% lower and, therefore, was also in the range of 10 µM. In patients with renal or hepatic insufficiency, the pharmacokinetics of glucosamine have not been studied, since, given the safety profile of the drug and the insignificant involvement of the kidneys in the elimination of glucosamine, no dose reduction is provided in these groups of patients.


Steady-state concentrations of glucosamine in plasma and synovial fluid after repeated administration once a day at a dose of 1500 mg are in the range of 10 mM and, therefore, correspond to those for which pharmacological activity was shown in studies in experimental models in vitro, which confirms the mechanism of action and clinical effect of the drug.


Clinical characteristics.


Indications. Treatment of osteoarthritis symptoms: pain and functional limitations.

Contraindications. Individual hypersensitivity to the active substance or to any of the excipients, tendency to bleeding.


The drug Glucosate should not be used in patients with allergies to shellfish because the active substance is obtained from the shells of shellfish: such patients are more likely to develop allergic reactions to glucosamine with a possible exacerbation of the symptoms of their disease.


The composition of the injectable form of the drug includes the auxiliary substance lidocaine, which has the following contraindications: cardiogenic shock, severe hypotension, severe forms of chronic heart failure, reduced left ventricular function, atrioventricular block II–III degree, severe bradycardia, blood clotting disorders, Wolf–Parkinson–White syndrome, Adams–Stokes syndrome, a history of convulsions caused by the use of lidocaine, sinus node weakness syndrome, severe liver function disorders, hypovolemia, myasthenia gravis, infections at the injection site, hypersensitivity to other amide-type anesthetics (since there is an increased risk of cross-hypersensitivity reactions).


Interactions with other drugs and other types of interactions. Avoid using mixtures of the contents of ampoules of the drug with other injectable drugs.


No specific drug interaction studies have been conducted. However, given the physico-chemical and pharmacokinetic properties of glucosamine sulfate, a low interaction potential can be assumed. In addition, it was found that glucosamine sulfate does not lead to either inhibition or increase in the activity of the main human CYP450 enzymes.


The drug does not compete for the mechanisms of absorption, after absorption it does not bind to plasma proteins, but is metabolized by inclusion as an endogenous substance in proteoglycans or is broken down without the participation of cytochrome enzymes, as a result of which it is unlikely to interact with other drugs.


However, an increased effect of coumarin anticoagulants has been reported in patients with concomitant treatment with glucosamine. In this regard, it is advisable for such patients to monitor the parameters of coagulation.


The drug is compatible with nonsteroidal anti-inflammatory drugs and glucocorticosteroids.


It is possible to increase the gastrointestinal absorption of tetracycline.


The composition of the injectable form of the drug includes the auxiliary substance lidocaine. Cimetidine, peptidine, bupivacaine, propranolol, quinidine, disopyramide, amitriptyline, nortriptyline, chlorpromazine, imipramine increase the level of lidocaine in the blood serum, reducing its hepatic metabolism. Norepinephrine has a synergistic effect when interacting with lidocaine.


MAO inhibitors should be used with caution, as the risk of hypotension increases and their local anesthetic effect is prolonged.


When used concomitantly with class IA antiarrhythmic drugs (including quinidine, procainamide, disopyramide), the QT interval is prolonged, and in isolated cases AV block or ventricular fibrillation may develop. 


The cardiotonic effect of using cardiac glycosides is weakened.


When used concomitantly with sedatives, the calming effects are enhanced.


Phenytoin enhances the cardiodepressive effect of lidocaine.


When used concomitantly with procainamide, delusions and hallucinations are possible.


Lidocaine can enhance the effect of drugs that block neuromuscular transmission, since the latter reduce the conduction of nerve impulses. Ethanol enhances the inhibitory effect of lidocaine on respiration.


Application features. The drug can only be administered by medical professionals.


Caution should be exercised when prescribing to patients with glucose intolerance. At the beginning of treatment, it is advisable for patients with diabetes mellitus to monitor their blood sugar levels.


Use the drug with caution in the treatment of patients suffering from bronchial asthma, since such patients are more likely to develop allergic reactions to glucosamine with a possible exacerbation of their symptoms.


One dose of the drug contains 40.3 mg of sodium. This should be taken into account when prescribing to patients who are shown a strict salt-free diet.


Since the injectable form of the drug contains the auxiliary substance lidocaine, before using it, it is necessary to conduct a skin test for individual sensitivity to the drug, which is indicated by swelling and redness of the injection site. To avoid accidental intravasal administration of the drug, it is recommended to conduct an aspiration test.


The safety of using lidocaine group anesthetics is questionable in patients prone to malignant hyperthermia, so their use in such cases should be avoided.


Before using lidocaine for heart diseases (hypokalemia reduces the effectiveness of lidocaine), it is necessary to normalize the level of potassium in the blood and monitor the heart condition using an ECG.


Serum creatine phosphokinase activity may increase after intramuscular injection of the drug, which may lead to an error in the diagnosis of acute myocardial infarction.


In case of sinus node disorders, prolongation of the P–Q interval, expansion of QRS, or in case of occurrence or exacerbation of arrhythmia, the dose should be reduced or discontinued.


Special care should be taken when using the drug in patients with circulatory insufficiency, hypotension, a history of arrhythmias, moderate liver and/or kidney disorders. Due to the presence of lidocaine in the composition, caution should also be exercised when prescribing to elderly patients with epilepsy, impaired heart conduction, and respiratory failure.


Use during pregnancy or lactation. There are no data on the use of the drug during pregnancy or lactation, so the use of the drug is contraindicated in this category of patients.


Ability to influence the reaction rate when driving vehicles or other mechanisms. Studies on the effect of the drug on the ability to drive a car and use other mechanisms have not been conducted. You should be careful when driving vehicles and performing work that requires attention. In case of drowsiness, fatigue, dizziness or visual disturbances, driving vehicles and working with other mechanisms are prohibited.


Dosage and administration.


For intramuscular use! The drug is not intended for intravenous administration.


Adult patients and elderly patients.


Before use, mix the solvent (1 ml ampoule) with the drug (2 ml ampoule) in one syringe.


The prepared solution of the drug should be administered intramuscularly at 3 mL or 6 ML (solution A + B) 3 times a week, for 4-6 weeks.


The presence of a yellowish color of the solution in ampoule A does not affect the effectiveness and tolerability of the drug.


Injections of the drug can be combined with oral administration of the drug in powder form to prepare a solution.


Glucosamine is not indicated for the treatment of acute pain.


Relief of symptoms (especially reduction of pain) can occur only after several weeks of treatment, and in some cases even after a longer time. No dose adjustment recommendations are provided for patients with impaired renal and/or hepatic function, as no relevant studies have been conducted.


Children. Do not use in children and adolescents, as the safety and efficacy of the drug for such patients have not been established.


Overdose. No cases of overdose were reported. In cases of overdose, symptomatic treatment should be carried out aimed at restoring the water-electrolyte balance.


The composition of the injectable form of the drug includes the auxiliary substance lidocaine. The first symptoms of lidocaine hydrochloride overdose from the central nervous system may be numbness of the tongue and lips, agitation, euphoria, anxiety, tinnitus, dizziness, blurred vision, nystagmus, tremor, depression, drowsiness, loss of consciousness, up to coma, tonic-clonic convulsions. Symptoms of lidocaine hydrochloride overdose from the cardiovascular system and respiratory function may include decreased blood pressure, collapse, AV block, and respiratory depression. It is necessary to monitor the patient's cardiovascular and respiratory functions. A change in these parameters may indicate an overdose of the drug, so the patient should immediately provide oxygen access. All complications require symptomatic treatment.


Adverse reactions.


Criteria for assessing the frequency of adverse drug reactions: very often – > 1/10, often – from > 1/100 to 1/10, infrequently – from > 1/1000 to 1/1000, rarely – from > 1/10000 to 1/1000, very rarely – 1/10000, unknown – the frequency cannot be estimated from available data.


From the digestive system: often – abdominal pain, flatulence, dyspepsia, diarrhea, constipation, nausea, vomiting; unknown – hyperglycemia in patients with impaired glucose tolerance;


from the nervous system: often-headache – drowsiness, increased fatigue, dizziness;


immune system disorders: unknown-hypersensitivity reactions – including allergic reactions, exacerbation of bronchial asthma;


from the side of the visual organs: unknown-visual disorders;


from the skin and its structures: infrequently-erythema, pruritus, rash; unknown – angioedema, urticaria, hair loss, abscess;


local reactions: unknown - reactions at the injection site.


The injectable form of the drug contains lidocaine. In exceptional cases, adverse reactions characteristic of this component are possible:

from the digestive system: nausea – very rarely-vomiting;


from the nervous system: numbness of the tongue and lips, photophobia, diplopia, headache, confusion, muscle twitching, when used in high doses – tinnitus, agitation, anxiety, paresthesia, convulsions, loss of consciousness, coma, hyperacusia;


from the side of the visual organs: visual impairment, conjunctivitis; when used in high doses – nystagmus;


mental disorders: unknown-sleep disorders;


from the cardiovascular system: arterial hypotension, transverse heart block; unknown – increased blood pressure; when used in high doses – arrhythmia, bradycardia, slowing of heart conduction, cardiac arrest, peripheral vasodilation, collapse, tachycardia, pain in the heart area;


immune system disorders: immune system depression, allergic reactions, including edema, skin reactions, pruritus; very rarely – urticaria, hypersensitivity reactions, including anaphylactoid reactions (including anaphylactic shock), generalized exfoliative dermatitis;


from the respiratory system: respiratory depression or respiratory arrest, shortness of breath;


others: a feeling of heat, cold or numbness of the extremities, malignant hyperthermia; when used in high doses – rhinitis;


local reactions: tingling of the skin at the injection site, abscess, slight burning sensation (disappears with the development of the anesthetic effect within 1 minute), thrombophlebitis.


Expiration date. 2 years.


Do not use after the expiration date.


Storage conditions. Store in the original packaging to protect from light at a temperature of 2 to 8 °C. keep out of reach of children. 

Tags: Glucosate® [Glucosamine, Sodium Chloride]