Instructions for Movex Active film-coated tablets No. 60
Composition
active ingredients: glucosamine sulfate, chondroitin sulfate sodium, diclofenac potassium;
1 film-coated tablet contains glucosamine sulfate 500 mg, chondroitin sulfate sodium 400 mg, diclofenac potassium 50 mg;
Excipients: povidone, microcrystalline cellulose, colloidal anhydrous silica, talc, croscarmellose sodium, magnesium stearate, sodium starch glycolate (type A), hypromellose, polyethylene glycol 6000, titanium dioxide (E 171), sunset yellow FCF dye (E 110).
Dosage form
Film-coated tablets.
Main physicochemical properties: film-coated tablets, orange in color, oval in shape, biconvex, with a score on one side.
Pharmacotherapeutic group
Drugs affecting the musculoskeletal system. Combined anti-inflammatory and antirheumatic drugs. Other anti-inflammatory/antirheumatic drugs in combination with other drugs.
ATX code M01B X.
Pharmacological properties
Pharmacodynamics
The drug has anti-inflammatory, analgesic, chondroprotective and regenerative effects. It slows down the processes of cartilage damage and bone resorption, restores cartilage, accelerates the formation of bone callus in injuries, and helps restore joint function.
Glucosamine is a substrate for the construction of articular cartilage and stimulates the regeneration of cartilage tissue. Any adverse effect (disease, age-related metabolic disorders, trauma) reduces its synthesis and concentration in connective tissue, which leads to a violation of the structure, function of the joints and the appearance of pain. Glycosaminoglycans and proteoglycans are part of the complex matrix that makes up cartilage.
Glucosamine is a component of endogenous glycosaminoglycans of cartilage tissue. Glucosamine sulfate has chondroprotective properties, reduces the deficiency of glycosaminoglycans in the body and participates in the synthesis of proteoglycans and hyaluronic acid. Due to its ability to selectively affect cartilage tissue, glucosamine initiates the process of sulfur fixation during the synthesis of chondroitin sulfate, normalizes calcium deposition in bone tissue, promotes the restoration of joint functions and the disappearance of pain syndrome. Glucosamine sulfate selectively acts on articular cartilage, is a specific substrate and stimulator of the synthesis of hyaluronic acid and proteoglycans, inhibits the formation of superoxide radicals and enzymes that cause damage to cartilage tissue (collagenase and phospholipase), prevents the destructive effect of glucocorticoids on chondrocytes and disruption of glycosaminoglycan biosynthesis caused by nonsteroidal anti-inflammatory drugs.
Chondroitin sulfate is a high-molecular polysaccharide that participates in the construction of cartilage tissue, reduces the activity of enzymes (elastase, hyaluronidase) that destroy articular cartilage, maintains the viscosity of synovial fluid and stimulates the regeneration of articular cartilage. It affects the phosphorus-calcium metabolism of cartilage tissue, slows down the resorption of bone tissue. Slows down the progression of osteoporosis. In the early stages of the inflammatory process, chondroitin sodium sulfate inhibits its activity and, thus, slows down the degeneration of cartilage tissue. Helps reduce pain, improves joint function and reduces the need for non-steroidal anti-inflammatory drugs. Prevents compression of connective tissue, "lubricates" joint surfaces and normalizes the production of joint fluid.
Diclofenac potassium is a nonsteroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic activity, has a rapid onset of action, which is especially important for the treatment of acute pain in inflammatory conditions. The mechanism of action is associated with non-selective blocking of the synthesis of the enzyme cyclooxygenase, which leads to inhibition of the synthesis of prostaglandins, which play a major role in the development of inflammation, pain and fever.
Diclofenac potassium inhibits mainly the exudation phase, to a lesser extent proliferation, reducing collagen synthesis and the associated tissue sclerosis.
Reduces pain at rest and during movement, reduces morning stiffness in joints, swelling of soft tissues, and improves the functional state of the musculoskeletal system.
Pharmacokinetics
Glucosamine sulfate. The bioavailability of glucosamine when administered orally is 25–26%. After distribution in tissues, the highest concentrations are determined in the liver, kidneys and cartilage. Approximately 90% of glucosamine, which entered the body orally, is absorbed from the small intestine in the form of glucosamine salt and from there through the portal circulation enters the liver. A significant part of the absorbed glucosamine is metabolized in the liver, disintegrating into urea, water and carbon dioxide. About 30% of the dose taken persists in the connective tissue for a long time. It is excreted mainly by the kidneys and in a very small amount - with feces.
Diclofenac potassium does not accumulate. The maximum concentration in the blood plasma is reached 2 hours after administration. Binding to plasma proteins is 99.7%. Penetrates into the synovial fluid. Systemic clearance of the active substance is 263 ml/min. Plasma half-life is 1–2 hours. 60% is excreted in the urine as metabolites, less than 1% is excreted by the kidneys in unchanged form, the rest is excreted in the form of metabolites with bile.
Indication
Treatment of diseases of the musculoskeletal system, accompanied by signs of inflammation, pain, degenerative-dystrophic changes in the cartilage tissue of the joints and spine, decreased joint mobility. Osteoarthritis, periarthritis (including knee, hip joints, intervertebral osteochondrosis, spondyloarthrosis), rheumatoid arthritis. Fractures and injuries (to accelerate the formation of bone callus), post-traumatic inflammation of soft tissues and the musculoskeletal system (due to sprains, blows).
Contraindication
Hypersensitivity to the active substances or to any of the other ingredients of the drug; allergy to shellfish; history of allergic reactions in the form of asthma attacks, bronchospasm, urticaria, acute rhinitis, nasal polyps or allergy-like symptoms after using acetylsalicylic acid or other non-steroidal anti-inflammatory drugs; acute ulcer, bleeding or perforation of the stomach or intestines; history of acute or recurrent ulcer/bleeding of the stomach or intestines (two or more separate episodes of established ulceration or bleeding); history of gastrointestinal bleeding or perforation associated with previous treatment with non-steroidal anti-inflammatory drugs (NSAIDs); inflammatory bowel disease (Crohn's disease or ulcerative colitis); severe hepatic impairment (Child-Pugh class C); severe renal impairment (creatinine clearance < 30 ml/min); bleeding tendency, thrombophlebitis, phenylketonuria; treatment of perioperative pain in coronary artery bypass grafting (or use of an artificial circulatory device); congestive heart failure (NYHA II–IV); uncontrolled arterial hypertension; ischemic heart disease in patients with angina; history of myocardial infarction; cerebrovascular disease in patients who have had a stroke or have episodes of transient ischemic attacks; peripheral arterial disease.
Interaction with other medicinal products and other types of interactions
Lithium: Diclofenac may increase plasma lithium concentrations when used concomitantly. Monitoring of serum lithium levels is recommended.
Digoxin: Diclofenac may increase the plasma concentration of digoxin when used concomitantly. Monitoring of serum digoxin levels is recommended.
Diuretics and antihypertensives. As with other NSAIDs, concomitant use of diclofenac may reduce the antihypertensive effect of diuretics or antihypertensive drugs (e.g. beta-blockers, angiotensin-converting enzyme (ACE) inhibitors) by inhibiting the synthesis of vasodilator prostaglandins. Therefore, this combination should be used with caution; patients, especially the elderly, should have their blood pressure checked regularly. Patients should be adequately hydrated and renal function should be monitored at the start of combination therapy and regularly thereafter, particularly because of the increased risk of nephrotoxicity with diuretics and ACE inhibitors.
Agents that may cause hyperkalemia: Concomitant treatment with potassium-sparing diuretics, cyclosporine, tacrolimus or trimethoprim may be associated with increases in serum potassium levels, which should be monitored.
Other NSAIDs, including selective cyclooxygenase-2 inhibitors, and corticosteroids. Concomitant use of diclofenac with other systemic NSAIDs or corticosteroids may increase the incidence of gastrointestinal adverse reactions. The simultaneous use of two or more NSAIDs should be avoided.
Anticoagulants and antithrombotic agents: Caution is recommended as concomitant use with diclofenac may increase the risk of bleeding.
Although clinical studies do not indicate that diclofenac affects the action of anticoagulants, there are isolated reports of an increased risk of bleeding in patients taking diclofenac and anticoagulants concomitantly. Close monitoring of patients taking diclofenac and anticoagulants concomitantly is recommended, and if necessary, adjustment of the anticoagulant dosage. Like other nonsteroidal anti-inflammatory drugs, diclofenac in high doses can reversibly inhibit platelet aggregation.
Antidiabetic agents. Clinical studies have shown that diclofenac can be administered concomitantly with oral antidiabetic agents without affecting their clinical effect. However, there have been isolated reports of hyperglycemia and hypoglycemia requiring dose adjustment of antidiabetic agents during treatment with diclofenac. Monitoring of blood glucose levels is recommended as a precautionary measure during combination therapy. Possible changes in the interaction process caused by metformin/metabolic acidosis.
Methotrexate. NSAIDs, including diclofenac, should be used with caution when administered less than 24 hours before or after treatment with methotrexate, as the blood concentration of methotrexate may increase and increase the toxicity of methotrexate. Cases of serious toxicity have been observed when methotrexate and NSAIDs, including diclofenac, were administered less than 24 hours apart. This interaction is mediated by accumulation of methotrexate as a result of impaired renal excretion in the presence of NSAIDs.
Cyclosporine: Diclofenac, like other NSAIDs, may potentiate the nephrotoxicity of cyclosporine through its effects on renal prostaglandins. Therefore, diclofenac should be used at lower doses than in patients not taking cyclosporine.
Tacrolimus: The use of NSAIDs with tacrolimus increases the risk of nephrotoxicity, which may be mediated by the inhibition of renal prostaglandins by the NSAID and the calcineurin inhibitor.
Quinolone antibiotics. There have been isolated reports of seizures, which may be associated with the concomitant use of quinolones and NSAIDs. Such cases may occur in patients with or without a history of epilepsy or seizures. Therefore, quinolone antibiotics should be used with caution in patients already receiving NSAIDs.
Colestipol and cholestyramine. These drugs may delay or reduce the absorption of diclofenac. Therefore, it is recommended to take diclofenac at least 1 hour before or 4-6 hours after taking colestipol/cholestyramine.
Cardiac glycosides. Concomitant use of cardiac glycosides and NSAIDs may exacerbate heart failure, reduce glomerular filtration rate, and increase plasma glycoside concentrations.
Mifepristone: NSAIDs should not be used for 8-12 days after taking mifepristone, as NSAIDs may reduce the effect of mifepristone.
Potent CYP2C9 inhibitors: Use caution when co-administering diclofenac with potent CYP2C9 inhibitors (e.g. sulfinpyrazone and voriconazole), which may lead to a significant increase in maximum plasma concentrations and exposure to diclofenac due to inhibition of diclofenac metabolism.
Phenytoin: When phenytoin and diclofenac are used concomitantly, phenytoin plasma concentrations should be monitored due to the expected increase in phenytoin exposure.
Increases the absorption of tetracyclines from the gastrointestinal tract, reduces the absorption of penicillins and chloramphenicol.
Application features
General.
To minimize risks, the lowest effective dose should be used for the shortest treatment period necessary to control symptoms.
The use of NSAIDs increases the risk of ulceration, perforation or bleeding, especially in elderly patients.
The risk of thrombotic cardiovascular and cerebrovascular complications is increased in connection with the use of selective COX-1/COX-2 inhibitors and certain NSAIDs.
Since the cardiovascular risks of diclofenac may increase with increasing dose and duration of treatment, it should be used for the shortest possible period and at the lowest effective dose.
Renal effects of NSAIDs include fluid retention with edema and/or hypertension, for this reason diclofenac should be used with caution in patients with impaired cardiac function and in the presence of other factors that lead to fluid retention.
Caution is also advised in patients taking diuretics or concomitant ACE inhibitors or who are at increased risk of hypovolemia.
Cardiovascular and cerebrovascular manifestations.
Appropriate medical supervision and advice is required in patients with a history of hypertension and/or mild to moderate congestive heart failure, as fluid retention and oedema have been reported with the use of NSAIDs, including diclofenac.
A small increased risk of arterial thrombotic events (e.g. myocardial infarction or stroke) may be associated with the use of diclofenac, especially at high doses and with long-term treatment.
Patients with cardiovascular risk factors (e.g. hypertension, hyperlipidemia, diabetes mellitus, smoking) should only be prescribed diclofenac after careful clinical evaluation and only at a dose ≤ 100 mg daily, if treatment does not exceed four weeks. The patient's need for diclofenac to relieve symptoms and the response to therapy should be reviewed periodically. Patients should be alert for the appearance of serious symptoms of atherothrombosis (e.g. chest pain, shortness of breath, weakness, speech disorders), which may occur without warning. Patients should be informed that in such cases they should immediately consult a doctor.
Effect on the kidneys.
Since fluid retention and edema have been reported with NSAIDs, including diclofenac, special caution should be exercised in patients with impaired cardiac or renal function, a history of hypertension, the elderly, patients receiving concomitant treatment with diuretics or drugs that may significantly affect renal function, and patients with a significant decrease in extracellular fluid volume for any reason, such as before or after surgery. In such cases, monitoring of renal function is recommended when using diclofenac. After discontinuation of therapy, the patient's condition usually returns to the state that existed before treatment.
Effect on the gastrointestinal tract.
Gastrointestinal bleeding (haematemesis, melena), ulceration or perforation, which can be fatal, have been reported with the use of NSAIDs, including diclofenac. These events can occur at any time during treatment, with or without warning symptoms or a previous history of serious gastrointestinal events.
In elderly patients, such complications are usually more serious. If gastrointestinal bleeding or ulceration occurs in patients receiving diclofenac, the drug should be discontinued. As with all NSAIDs, close medical supervision and special caution are required when prescribing diclofenac to patients with symptoms suggestive of gastrointestinal disorders, with suspected ulceration, bleeding, perforation or a history of such conditions.
The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing dose of NSAIDs, including diclofenac, and in patients with a history of ulcer, particularly complicated by bleeding or perforation, and in elderly patients.
To reduce the risk of gastrointestinal toxicity, treatment is initiated and maintained at the lowest effective dose.
Combination therapy with protective agents (e.g. misoprostol or proton pump inhibitors) should be considered for such patients, as well as for patients requiring concomitant use of low-dose acetylsalicylic acid (aspirin) or other drugs that increase the risk of gastrointestinal disorders.
Patients with a history of gastrointestinal toxicity, especially the elderly, should be monitored for unusual abdominal symptoms (especially gastrointestinal bleeding).
Caution should be exercised in patients receiving concomitant treatment with drugs that increase the risk of ulceration or bleeding, such as systemic corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors (SSRIs), or antiplatelet agents such as acetylsalicylic acid.
Patients with ulcerative colitis or Crohn's disease require close medical supervision and caution when using the drug, as these conditions may be exacerbated.
Effect on the skin.
Serious skin reactions, some of which have been fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported very rarely in association with the use of NSAIDs, including diclofenac. The risk of these reactions is highest at the beginning of therapy, in most cases within the first month of treatment. The drug should be discontinued at the first appearance of skin rash, mucosal ulceration or any other sign of hypersensitivity.
Effect on the liver.
It is recommended to monitor liver function tests during treatment. If the deviation from normal liver function tests persists or worsens, clinical symptoms of liver disease appear or other manifestations are observed (eosinophilia, rash), the drug should be discontinued. Hepatitis can develop during the use of diclofenac without prodromal symptoms. In addition to increased liver enzyme levels, severe liver reactions have been reported rarely, including jaundice and fulminant hepatitis, hepatic necrosis and hepatic failure, which have sometimes been fatal. Diclofenac should be used with caution in patients with hepatic porphyria, as it may provoke an attack.
Use in the presence of asthma.
In patients with asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (e.g. nasal polyps), chronic obstructive pulmonary disease or chronic respiratory tract infections (especially if associated with symptoms similar to allergic rhinitis), reactions to NSAIDs such as asthma exacerbations (so-called aspirin-induced asthma with intolerance to analgesics), angioedema and urticaria occur more frequently than in other patients. In this regard, special precautions (emergency medical attention) are recommended for such patients. This also applies to patients who have had allergic reactions, such as rash, itching or urticaria, to other substances.
Hematological manifestations.
The drug is used for short-term treatment to relieve symptoms in the acute period of the disease. In case of prescribing this drug for a longer period, it is recommended (as for other NSAIDs) to regularly monitor the blood count.
Like other NSAIDs, diclofenac may temporarily inhibit platelet aggregation, therefore patients with impaired hemostasis, hemorrhagic diathesis or hematological abnormalities should be carefully monitored.
Masking signs of infection.
Like other NSAIDs, diclofenac, due to its pharmacodynamic properties, may mask the symptoms of infection.
SLE and mixed connective tissue diseases.
Patients with systemic lupus erythematosus (SLE) and mixed connective tissue diseases may be at increased risk of aseptic meningitis.
Precautions.
Concomitant use of the drug and systemic non-steroidal anti-inflammatory drugs, such as selective cyclooxygenase-2 inhibitors, should be avoided due to the lack of any evidence of a synergistic effect and due to potential additive side effects.
In rare cases, as with other NSAIDs, allergic reactions, including anaphylactic/anaphylactoid reactions, may occur, even without prior exposure to diclofenac.
The drug should be used with caution in patients over 65 years of age, especially those who are physically weak or if the patient's body weight is below normal.
The dye sunset yellow FCF (E 110) may cause allergic reactions.
Ability to influence reaction speed when driving vehicles or other mechanisms
Usually, when taking the drug in the recommended dose and with a short course of treatment, there is no effect on the speed of reactions. However, patients who experience central nervous system dysfunction when using the drug Movex®Active should not drive or operate complex mechanisms.
Use during pregnancy or breastfeeding
Female fertility: Like other NSAIDs, diclofenac may affect female fertility and is therefore not recommended in women attempting to conceive. Discontinuation of diclofenac should be considered in women who are unable to conceive or in women undergoing investigation of infertility.
Do not use the drug during pregnancy or breastfeeding.
Method of administration and doses
Adults should take 1 tablet up to 3 times a day. The tablets are taken orally after meals, with water.
The total duration of treatment at the recommended dose should not exceed 10 days.
The treatment regimen should be selected individually. Treatment may be longer if prescribed by a doctor.
The drug should be used in the lowest effective doses for the shortest period of time, taking into account the treatment objectives of each individual patient.
After relieving the pain syndrome and consulting a doctor, treatment can be continued with Movex® Comfort.
Children
The drug should not be used in children.
Overdose
Possible increased side effects.
Treatment of acute poisoning with nonsteroidal anti-inflammatory drugs, including diclofenac, usually consists of supportive measures and symptomatic treatment of complications such as hypotension, renal failure, convulsions, gastrointestinal disorders, respiratory depression. Special measures such as phosphate diuresis, dialysis or hemoperfusion do not contribute to the accelerated elimination of NSAIDs from the body due to the high degree of protein binding and extensive metabolism. In case of potentially toxic overdose, activated charcoal should be used; in case of potentially life-threatening overdose, gastric evacuation (induce vomiting, gastric lavage) should be performed.
Adverse reactions
The drug is usually well tolerated.
Most side effects after using Movex® Active are due to the diclofenac content and are dose-dependent.
Immune system: hypersensitivity reactions, including itching, rash (including erythematous, bullous), urticaria, eczema, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis, erythroderma (exfoliative dermatitis), anaphylactic and anaphylactoid reactions (including hypotension and shock), angioedema, bronchial asthma (including shortness of breath), pneumonitis, vasculitis.
Gastrointestinal: abdominal pain, nausea, vomiting, diarrhea, feeling of cramps, dyspepsia, bloating, anorexia, stomatitis, aphthous stomatitis, glossitis, changes in the esophagus, gastritis, gastric and intestinal ulcers, including with bleeding or perforation (sometimes fatal, especially in elderly patients), gastrointestinal bleeding (vomiting with blood, melena, diarrhea with blood), the occurrence of diaphragmatic strictures in the intestine, disorders of the lower intestinal tract, such as colitis, nonspecific hemorrhagic colitis, exacerbation of nonspecific ulcerative colitis or Crohn's disease, constipation, pancreatitis.
Liver disorders: liver dysfunction, increased serum aminotransferase levels, hepatitis, jaundice, fulminant hepatitis, liver necrosis, liver failure.
Changes in the course of stenosis of the gastrointestinal tract, peritonitis and ischemic colitis as more specific/severe forms of the already mentioned gastrointestinal side effects.
Nervous system: headache, dizziness, drowsiness, insomnia, sensory disturbances, including paresthesia, memory impairment, disorientation, vertigo, irritability, fatigue, confusion, hallucinations, cerebrovascular disorders, convulsions, depression, anxiety, general weakness, night terrors, tremor, psychotic disorders, aseptic meningitis, optic neuritis.
From the sensory organs: visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disturbance.
Dermatological reactions: hair loss, photosensitivity, purpura, including allergic purpura, dermatitis.
From the genitourinary system: edema, acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis, medullary necrosis of the kidney, impotence.
From the side of the hematopoietic system: anemia (including hemolytic, aplastic), thrombocytopenia, leukopenia, agranulocytosis.
Cardiovascular: palpitations, chest pain, hypertension, heart failure, myocardial infarction, hypotension, vasculitis. Clinical trial data and epidemiological data suggest an increased risk of thrombotic complications (e.g. myocardial infarction or stroke) associated with the use of diclofenac, particularly at high therapeutic doses (150 mg per day) and with prolonged use.
Expiration date
3 years.
Storage conditions
Store out of the reach of children in the original packaging at a temperature not exceeding 25 °C.
Packaging
30 or 60 tablets in a bottle; 1 bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
Meditop Pharmaceutical Ltd.
Location of the manufacturer and its business address
Hungary, Edi Endre y. 1., Pilisboroszeno, 2097.
