TERAFLEX ADVANCED CAPSULE

Tradename

TeraflexAdvans.

International non-proprietary or grouping name

Glucosamine + Ibuprofen + Chondroitin Sulfate.

Dosage Form

Capsules

Composition

1 capsule contains:

Active ingredients: Glucosamine sulfate in the form of D-glucosamine potassium chloride sulfate 250 mg, chondroitin sodium sulfate1 200 mg ibuprofen2 100 mg.

Excipients: microcrystalline cellulose 17.4 mg, corn starch (pregelatinized starch) 4.1 mg, stearic acid 10.2 mg, carboxymethyl starch sodium 10 mg, crospovidone 10 mg, Magnesium stearate 3 mg, silicon dioxide 2 mg, povidone 0, 3 mg.

Gelatin capsule: gelatin 97.07 mg, titanium dioxide 2.83 mg, dye diamond blue aluminum varnish 0.09 mg.

1Chondroitin sodium sulfate is contained in the form of a 90% substance, taking into account the 10% loss in mass during drying and the excess - 241 mg;

2 ibuprofen is contained in the form of granules of direct compression 66%, containing: ibuprofen 66%, pregelatinized starch 8%, croscarmellose sodium 2%, microcrystalline cellulose 14%, colloidal silicon dioxide 1%, stearic acid 1.5%, corn starch 6%, povidone 1.5% - 152 mg.

Ink composition: shellac NF, dehydrated ethyl alcohol USP, isopropyl alcohol USP, butyl alcohol NF, propylene glycol USP, ammonia NF solution, indigo carmine aluminum varnish, titanium dioxide USP.

Description

Opaque hard gelatin capsules of size 0, consisting of two parts: a blue cap and a white casing with the inscription in blue “THERAFLEX ADVANCE”, filled with a white or almost white powder with a faint odor.

Pharmacotherapeutic group

Reparation tissue stimulator + non-steroidal anti-inflammatory drug.

Pharmacological properties

Teraflex®Advance is a combined preparation containing chondroitin sulfate, glucosamine sulfate and ibuprofen as active ingredients.

Chondroitin sulfate is involved in the construction and restoration of cartilage, protects it from destruction and improves joint mobility.

Glucosamine sulfate activates the synthesis of proteoglycans, hyaluronic, chondroitin sulfuric acids and other substances that make up the articular membranes, intra-articular fluid and cartilage tissue.

Ibuprofen is a derivative of propionic acid and has analgesic, antipyretic and anti-inflammatory effects due to the non-selective blockade of cyclooxygenase 1 and 2. The glucosamine sulfate and chondroitin sulfate preparations potentiate the analgesic effect of ibuprofen.

Pharmacokinetics

The oral bioavailability of glucosamine is 25% (the effect of “first passage” through the liver), the highest concentrations are found in the liver, kidneys and articular cartilage. About 30% of the accepted dose persists for a long time in bone and muscle tissue.Excreted predominantly with urine unchanged, partially with feces. The half-life is 68 hours.

More than 70% of chondroitin sulfate is absorbed in the digestive tract. Bioavailability is about 13%. With a single ingestion of the average therapeutic dose, the maximum concentration in plasma is noted after 3-4 hours, in synovial fluid after 4-5 hours. Absorbed in the gastrointestinal tract drug accumulates in the synovial fluid. Excreted by the kidneys.

Ibuprofen is well absorbed from the stomach. Тmax - about 1 hour. Ibuprofen is approximately 99% bound to plasma proteins. It is slowly distributed in the synovial fluid and is removed from it more slowly than from plasma. Ibuprofen is metabolized in the liver mainly by hydroxylation and carboxylation of the isobutyl group. CYP2C9 isoenzyme is involved in the metabolism of the drug. After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen slowly transforms into the active S-form. Ibuprofen has a biphasic elimination kinetics. The half-life (T1 / 2) of plasma is 2-3 hours. Up to 90% of the dose can be detected in the urine as metabolites and their conjugates. Less than 1% is excreted unchanged in the urine and, to a lesser extent, in the bile. Ibuprofen is completely excreted in 24 hours.

Indications for use

Osteoarthritis of large joints, osteochondrosis of the spine, accompanied by moderate pain syndrome.

Contraindications

Hypersensitivity to any of the ingredients that make up the drug. Hypersensitivity to Acetylsalicylic acid or other NSAIDs in history.

Erosive and ulcerative diseases of the organs of the gastrointestinal tract (including peptic ulcer of the stomach and duodenum in the acute stage, Crohn's disease, ulcerative colitis).

A complete or incomplete combination of asthma, recurrent nasal polyposis and paranasal sinuses.

Confirmed hyperkalemia.

Hemophilia and other bleeding disorders (including hypocoagulation), hemorrhagic diathesis.

Gastrointestinal bleeding and intracranial hemorrhage.

Severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease.

Severe liver failure or active liver disease.

Period after coronary artery bypass surgery.

Pregnancy, lactation.

Children's age up to 18 years.

Carefully

Old age, heart failure, arterial hypertension, cirrhosis of the liver with portal hypertension, hepatic and / or renal insufficiency, nephrotic syndrome, hyperbilirubinemia, gastric ulcer and duodenal ulcer (history), gastritis, enteritis, colitis, diseases of the duodenum, etiology, gastritis, enteritis, colitis, obstructive diseases, etiology, gastritis, enteritis, colitis; and anemia), bronchial asthma, diabetes mellitus, concomitant therapy with anticoagulants, antiplatelet agents, glucocorticosteroids,selective serotonin reuptake inhibitors, peripheral arterial disease, mild renal impairment (creatinine clearance of 30-60 ml / min), smoking, alcoholism, dyslipidemia / hyperlipidemia, coronary heart disease, cerebrovascular disease, the presence Helicobacterpilori infection, prolonged use of NSAIDs, tuberculosis, severe somatic diseases. If you are intolerant to seafood (shrimp, shellfish), the likelihood of an allergic reaction to the drug increases.

Use during pregnancy and lactation

Not recommended for use during pregnancy and during breastfeeding.

Dosage and administration

Inside Adults use 2 capsules 3 times a day after meals. Capsules are taken orally with a small amount of water. The duration of admission without consulting a doctor should not exceed 3 weeks. Further use of the drug should be agreed with the doctor.

Side effects

When using the drug Teraflex ®Advance possible: nausea, abdominal pain, flatulence, diarrhea, constipation, allergic reactions; these reactions disappear after drug withdrawal.

Consideration should be given to the possibility of adverse reactions associated with ibuprofen present in the preparation.

Gastrointestinal tract (GIT): NSAID gastropathy (abdominal pain, nausea, vomiting, heartburn, loss of appetite, diarrhea, flatulence, constipation; rarely, ulceration of the gastrointestinal mucosa, which in some cases is complicated by perforation and bleeding); irritation or dryness of the oral mucosa, pain in the mouth, ulceration of the mucous membrane of the gums,aphthous stomatitis, pancreatitis.

Hepatobiliary system: hepatitis.

Respiratory system: shortness of breath, bronchospasm.

Sense organs: hearing impairment (hearing loss, ringing or tinnitus); visual impairment (toxic damage to the optic nerve, blurred vision or double vision, scotoma, dryness and irritation of the eyes, conjunctival edema, and age of allergic genesis).

Central and peripheral nervous system: headache, dizziness, insomnia, anxiety, nervousness and irritability, psychomotor agitation, drowsiness, depression, confusion, hallucinations, rarely - aseptic meningitis (more often in patients with autoimmune diseases).

Cardiovascular system: the development or aggravation of heart failure, tachycardia, increased blood pressure.

Urinary system: acute renal failure, allergic nephritis, nephrotic syndrome (edema), polyuria, cystitis.

Allergic reactions: skin rash (usually erythematous or urticaria), pruritus, angioedema, anaphylactoid reactions, anaphylactic shock, dyspnea, fever, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal erythema (including edematous erythema), toxic toxicosis, toxic tract erythema, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal erythema, including toxic erythema, including toxic erythema allergic rhinitis.

Organs of hematopoiesis: anemia (including hemolytic, aplastic), thrombocytopenia and thrombocytopenic purpura, agranulocytosis, leukopenia.

Other: increased sweating.

Laboratory indicators: bleeding time (may increase), serum glucose concentration (may decrease), creatinine clearance (may decrease), hematocrit or hemoglobin (may decrease), serum creatinine concentration (may increase), liver transaminase activity (may increase ).

Overdose

Symptoms (associated with ibuprofen): abdominal pain, nausea, vomiting, lethargy, drowsiness, depression, headache, tinnitus, metabolic acidosis, coma, acute renal failure, blood pressure reduction, hyperkalemia, bradycardia, tachycardia, atrial fibrillation, symptoms breathing.

Treatment: gastric lavage (effective only for 1 hour after ingestion), Activated carbon, alkaline drinking, forced diuresis, symptomatic therapy (correction of the acid-base state, blood pressure).

Interaction with other drugs

Inductors of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites of ibuprofen, increasing the risk of severe hepatotoxic reactions.

Inhibitors of microsomal oxidation reduce the risk of hepatotoxic action.

Reduces the hypotensive activity of vasodilators (including slow Calcium channel blockers and ACE inhibitors), natriuretic and diuretic - Furosemide and hydrochlorothiazide.

Reduces the effectiveness of uricosuric drugs, enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics (increased risk of hemorrhagic complications), ulcerogenic effects with bleeding glucocorticosteroids, NSAIDs, colchicine, estrogen, ethanol; enhances the effect of oral hypoglycemic drugs and insulin.

Antacids and colestyramine reduce the absorption of ibuprofen.

Increases blood concentration of Digoxin, lithium preparations and Methotrexate.

Caffeine enhances the analgesic effect.

With the simultaneous appointment of ibuprofen reduces the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (it is possible to increase the incidence of acute coronary insufficiency in patients receiving small doses of acetylsalicylic acid as an antiplatelet agent after starting ibuprofen).

When administered with anticoagulant and thrombolytic drugs (alteplazy, streptokinase, urokinase), the risk of bleeding increases at the same time.

Cefamundol, cefoperazone, cefotetan, valproic acid, plykamycin increase the incidence of hypoprothrombinemia.

Myelotoxic drugs enhance hematotoxicity.

Cyclosporine and gold preparations enhance the effect of ibuprofen on the synthesis of prostaglandins in the kidneys, which is manifested by an increase in nephrotoxicity.Ibuprofen increases the plasma concentration of cyclosporine and the likelihood of its hepatotoxic effects.

Drugs that block tubular secretion, reduce excretion and increase the plasma concentration of ibuprofen.

In connection with the content of glucosamine in the preparation, it is possible to reduce the effectiveness of hypoglycemic drugs, doxorubicin, teniposide, etoposide. Glucosamine increases the absorption of tetracyclines, reduces the effect of semi-synthetic penicillins, chloramphenicol.

special instructions

During long-term treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys.

When symptoms of gastropathy appear, close monitoring is shown, including esophagogastroduodenoscopy, blood analysis with hemoglobin, hematocrit, and fecal occult blood analysis.

If necessary, the simultaneous reception of additional NSAIDs and analgesic drugs, the doctor should consider the presence in the drug ibuprofen. If long-term use of additional NSAIDs is necessary, Teraflex should be used.®ibuprofen free.

If necessary, determine the 17-ketosteroids drug should be canceled 48 hours before the study.

During treatment, alcohol is not recommended.

Influence on ability to drive machinery and other vehicles