Expiration date: 08/2025

Release form, composition and packaging

Tablets from light yellow to yellow color, valium forms, with facet, scored on one side, tolerance of marbling and small inclusions

1 tablet contains:

meloxicam 15 mg

Excipients: lactose, cellulose microcrystalline, sodium citrate dihydrate, povidone (polyvinylpyrrolidone), sodium carboximetilkrahmal (primogel), silicon dioxide colloidal (Aerosil), calcium stearate.

10 PCs. - packaging sells contoured (1) - packs of cardboard.

10 PCs. - packaging sells contoured (2) - packs of cardboard.

10 PCs banks polymer (1) - packs of cardboard.

20 PCs banks polymer (1) - packs of cardboard.

Pharmacological action

Meloxicam is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic activity. Anti-inflammatory effect due to inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2) involved in the biosynthesis of prostaglandins in inflammation. To a lesser extent meloxicam acts on cyclooxygenase-1 (COX-1) involved in the synthesis of prostaglandin, protects the mucous membranes of the gastrointestinal tract and is involved in the regulation of blood flow to the kidneys.

Pharmacokinetics

Well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Simultaneous eating does not change suction. When using the drug orally in doses of 7.5 and 15 mg concentrations proportional to the dose.

Equilibrium concentration achieved within 3-5 days. Long-term use of the drug (more than 1 year), concentrations similar to those observed after the first achievement of the equilibrium state. The plasma protein binding is 99%. The range of differences between the maximum and basal concentrations of the drug after taking it once a day and is relatively small when using a dose of 7.5 mg 0.4-1 mg/ml, and when using doses of 15 mg — 08-2 µg/ml. Meloxicam permeates through gistogematicalkie barriers, concentration in synovial fluid reaches the 50% of the Cmax of the drug in plasma.

Metaboliziruetsa almost completely in the liver with the formation of four inactive in the pharmacological relation to derivatives. The main metabolite, 5’-carboxy-meloxicam (60% of the dose), formed by oxidation of an intermediate metabolite 5’-hydroxymethyluracil, which is also excreted, but to a lesser extent (9% of the dose). In vitro studies showed that this metabolic transformation plays an important role of CYP 2C9, additional value is CYP 3A4 isoenzyme. The formation of two other metabolites (components, respectively, 16% and 4% of the dosage) participating peroxidase, activity which, probably, individually varies.

Excreted equally in feces and urine, primarily as metabolites. Faeces in unaltered form appears less 5% the magnitude of the daily dose, in the urine in an unmodified form the drug is detected only in trace amounts. T1/2 meloxicam is 15-20 hrs, Plasma clearance averages 8 ml/min in the elderly, clearance of the drug is reduced. Vd low and averages 11 l

Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.

Dosage

The drug is taken orally during meals 1 times/day.

The recommended dosing regimen:

Rheumatoid arthritis: 15 mg/day. After a therapeutic effect dose can be reduced to 7.5 mg/day.

Osteoarthritis: 7.5 mg/day. If necessary, the dose may be increased to 15 mg/day.

Ankylosing spondylitis: 15 mg/day. The maximum daily dose should not exceed 15 mg.

In patients with an increased risk of side effects and in patients with renal failure, on hemodialysis, dose should not exceed 7.5 mg/day.

Overdose

Symptoms: violation of consciousness, nausea, vomiting, pain in epigastrii, gastrointestinal bleeding, acute renal failure, hepatic failure, respiratory arrest, asystole.

Treatment: no specific antidote to overdose of the drug should be gastric lavage, reception activated carbon (within hours), symptomatic therapy. Cholestyramine accelerates the elimination of the drug from the body. Forced diuresis, alkalinisation of the urine, hemodialysis is ineffective because of the high regard of the drug with blood protein.

Drug interaction

With simultaneous use with other NSAIDs (as well as with acetylsalicylic acid) increases the risk of erosivno-yazvennah losses and bleeding of the gastrointestinal tract.

While the use of antihypertensive drugs may decrease the effectiveness of the latter.

With the simultaneous use of drugs lithium may develop accumulation of lithium and increase its toxicity (to control the concentration of lithium in the blood).

While the use of methotrexate increases the side effect on the hematopoietic system (the risk of anemia and leukopenia, shows periodic monitoring of complete blood count).

While the use of diuretics and cyclosporine increases the risk of renal failure.

While the use of intrauterine contraceptive devices may reduce the effectiveness of the latter.

At simultaneous application with anticoagulants (heparin, tiklopidin, warfarin), and thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (a periodic monitoring of indicators of blood coagulation).

While the use of kolestiraminom, as a result of binding of meloxicam, increasing its excretion through the gastrointestinal tract.

Pregnancy and lactation

The drug is not recommended during pregnancy and lactation.

Side effect

From the digestive system: more 1% - neuralgia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhoea, 0.1-1% - transient increase in liver transaminases, hyperbilirubinemia, eructation, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including hidden), stomatitis, less than 0.1% perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.

Organs of hematopoiesis: more than 1% - anemia, 0.1-1% - changes in blood counts, including leukopenia, thrombocytopenia.

With the skin: more 1% - itching, rash, 0.1-1% urticaria, less than 0.1% - photosensitivity, bullous eruptions, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

The respiratory system: less than 0.1% bronchospasm.

From the nervous system: more 1% - dizziness, headache, 0.1-1% - vertigo, tinnitus, drowsiness, less than 0.1% - confusion, disorientation, emotional lability.

From the cardiovascular system with more than 1% and peripheral edema, 0.1-1% - increased blood pressure, palpitations, rush of blood to the skin.

From the urinary system: 0.1-1% gipercreatininemia and/or increase of urea in blood serum, less than 0.1% - acute renal failure, the connection with the reception of meloxicam is not set — interstitial nephritis, albuminuria, hematuria.

From the sensory organs: less than 0.1% - conjunctivitis, visual disturbances including blurred vision.

Allergic reactions: less than 0.1% - angioneurotic edema, anaphylactoid/ anaphylactic reactions.

Terms and conditions storage

List B. In a dry, dark, inaccessible to children place at temperature not exceeding 25°C. shelf Life - 2 years. Do not use after expiration date.

Indications

• symptomatic treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis (Bechterew's disease) and other inflammatory and degenerative diseases, accompanied by pain syndrome.
  

Contraindications

• anamnestic data about attack of bronchial mast, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or partial syndrome of intolerances acetylsalicylic acid — rhinosinusitis, urticaria, polyps are nasal mucosa, asthma (bronchial)),
  
• erosive-ulcerative changes of the mucous membrane of the stomach or duodenal ulcers, active gastrointestinal bleeding,
  
• inflammatory bowel disease (ulcerative colitis, Crohn's disease),
  
• cerebrovascular bleeding or other bleeding,
  
• since the coronary artery bypass surgery,
  
• decompensated heart failure,
  
• severe hepatic impairment or active liver disease,
  
• severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 ml/min), progressive kidney diseases including confirmed hyperkalemia,
  
• pregnancy,
  
• breastfeeding,
  
• children up to age 15 years,
  
• hypersensitivity to any component of the drug.
  

With caution:

Coronary artery disease, cerebrovascular disease, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral artery disease, Smoking, creatinine clearance less than 60 ml/min.

Anamnestic data about the development of ulcerative lesions of the gastrointestinal tract, infections of Helicobacter pylori, older age, prolonged use of NSAIDs, frequent use of alcohol, serious somatic diseases, concomitant therapy the following medications:

• anticoagulants (eg, warfarin),
  
• antiplatelet agents (e.g. acetylsalicylic acid, clopidogrel),
  
• oral corticosteroids (e.g., prednisone),
  
• selective inhibitors of reverse takeover serotonin (e.g., citalopram, fluoxetine, paroxetine, sertraline).
  

To reduce the risk of adverse effects from the blood should use the minimum effective dose minimum possible short course

Special instruction

Caution must be exercised in applying the drug in patients with a history who have peptic ulcer or duodenal ulcer and in patients on anticoagulant therapy. These patients are at increased risk of erosive-ulcerative diseases of the gastrointestinal tract.

Use caution and monitor indicators of kidney function if use of the drug in elderly patients, patients with congestive heart failure with symptoms of insufficient blood circulation in patients with cirrhosis of the liver, as well as in patients with gipovolemiei as a result of surgical interventions.

In patients with renal impairment if creatinine clearance over 25 ml/min does not require correction of dosing regimen. In patients on dialysis, the dosage should not exceed 7.5 mg/day.

Patients simultaneously receiving diuretics and meloxicam, should take plenty of fluids.

If the treatment process had an allergic reaction (itching, skin rash, urticaria, photosensitization), you need to stop taking the drug and consult a doctor.

Effects on ability to drive vehicles and management mechanisms

The use of the drug may cause unwanted effects such as headaches and dizziness, drowsiness. Should abandon the management of vehicles and maintenance of machines and mechanisms requiring concentration of attention.

If impaired renal function

In patients with renal impairment if creatinine clearance over 25 ml/min does not require correction of dosing regimen. In patients on dialysis, the dosage should not exceed 7.5 mg/day.

Contraindicated:

• severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 ml/min), progressive kidney diseases including confirmed hyperkalemia.
  

When disorders of liver function

Contraindicated:

• severe hepatic impairment or active liver disease.
  

The use in children

Contraindicated in children up to 15 years.

Conditions of supply of pharmacies

A drug dispensed by prescription.