Expiration date: 07/2026
The composition and form of issue:
Tablets. 1 tablet contains:
meloxicam 7.5 and 15 mg
other ingredients: microcrystalline cellulose PVP (povidone) milk sugar (lactose) starch potato kollidon CL-M (crospovidon) talc magnesium stearate
in packing contour cell 10 PCs the paper cartons 1 or 2 packages or in a polymeric 20 PCs the paper cartons 1 Bank.
Description pharmaceutical form:
Round valium tablets without the risks (7, 5 mg) or valium (15 mg), light yellow color. On the surface of the tablets, the slight marbling.
Pharmacokinetics:
Well absorbed from the gastrointestinal tract, absolute bioavailability of 89%. Simultaneous eating does not change suction. When applied orally in doses of 7, 5 and 15 mg of the drug concentration is proportional to dose. Equilibrium concentrations achieved within 3-5 days. Long-term use of the drug (more than 1 year) concentrations are similar to those observed after the first equilibrium. The plasma protein binding is more than 99%. The range of differences between the maximum and basal concentrations of the drug after taking it 1 time a day is relatively small and is 0, 4-1, 0 µg/ml when using doses of 7, 5 mg, and when using doses of 15 mg — 0, 8-2, 0 µg/ml (shown, respectively, values of Cmin and Cmax). Meloxicam permeates through gistogematicalkie barriers, concentration in synovial fluid is 50% Cmax in the plasma. Almost completely metabolized in the liver with the formation of four inactive in the pharmacological relation to derivatives. The main metabolite, 5'-carboxymethoxy (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 varies individually. Excreted equally in feces and urine, primarily as metabolites. Faeces in unaltered form appears less 5% the daily dose, in the urine in an unmodified form the drug is detected only in trace amounts. T1/2 — 15-20 h. Plasma clearance averages 8 ml/min in the elderly, clearance of the drug is reduced. The volume of distribution is low, and averages 11 l
Hepatic or renal insufficiency medium severity significant effect on the pharmacokinetics of meloxicam does not have.
Description of the pharmacological action:
Anti-inflammatory effect due to inhibition of the enzymatic activity of COX-2, involved in the biosynthesis of PG in the field of inflammation. To a lesser extent meloxicam acts on COX-1, involved in the synthesis of GHG to protect the gastrointestinal mucosa and involved in the regulation of blood flow to the kidneys.
Indications:
Symptomatic treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis (Bechterew's disease) and other rheumatic diseases, accompanied by pain syndrome.
Contraindications:
Hypersensitivity to any component of the drug, aspirin bronchial asthma, exacerbation of ulcers stomach and duodenal ulcers, gastrointestinal, cerebrovascular or other haemorrhage, severe renal failure (unless hemodialysis is performed), severe liver failure, severe heart failure, children under 15 years, pregnancy, lactation.
With caution: elderly patients with erosive-ulcerative lesions of gastrointestinal tract in anamnesis.
Application of pregnancy and breastfeeding:
The drug is not recommended during pregnancy and lactation.
Side effect:
From the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosivno-azwenne shock syndrome, perforation of the stomach or intestines, gastrointestinal bleeding, increased liver enzymes, hepatitis, colitis, stomatitis, dry mouth, esophagitis.
From the side of cardiovascular system: tachycardia, increased blood pressure, a feeling of "tides".
On the part of the respiratory system: exacerbation of asthma, cough.
From the nervous system and sensory organs: headache, dizziness, tinnitus, disorientation, confusion, sleep disturbances, conjunctivitis, blurred vision.
From the urogenital system: swelling, interstitial nephritis, renal medullary necrosis, a urinary-tract infection, proteinuria, hematuria, renal failure.
With the skin: itching, skin rash, urticaria, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity.
Organs of hematopoiesis: anemia, leukopenia, thrombocytopenia.
Allergic reactions: anaphylactoid reaction (including anaphylactic shock), swelling of the lips and tongue, allergic vasculitis.
Other: fever.
Drug interaction:
While the use of other NSAIDs (including with acetylsalicylic acid) increases the risk of erosivno-yazvennah losses and bleeding from the digestive tract hypotensive drugs may reduce the effectiveness of the latest drugs lithium is the development of accumulation of lithium and increase its toxicity (to control the concentration of lithium in the blood) with methotrexate — increases the side effect on the hematopoietic system (the risk of anemia and leukopenia, shows periodic monitoring of complete blood count) with diuretics and cyclosporine — increases the risk of renal insufficiency with intrauterine contraceptives — may reduce the effectiveness of the latter with anticoagulants (heparin, tiklopidin, warfarin), and thrombolytic drugs (streptokinase, fibrinolysin) — increases risk of bleeding (a periodic monitoring of indicators of blood coagulation) holestiraminom — increases the excretion of meloxicam through blood (as a result of binding).
Method of application and doses:
Inside, during a meal, 1 time a day.
The recommended dosing regimen:
- rheumatoid arthritis — on 15 mg/day, depending on the therapeutic effect dose can be reduced to 7, 5 mg/day
- osteoarthritis — 7, 5 mg/day, the ineffectiveness of 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, epigastric pain, bleeding in the digestive tract, acute renal failure, hepatic failure, respiratory arrest, asystole.
Treatment: no specific antidote if overdose should carry out gastric lavage, reception activated carbon (within hours), symptomatic therapy. Cholestyramine accelerates the elimination of the drug from the body. Forced diuresis, alkalinisation of urine, haemodialysis ineffective because of the high regard of the drug with blood protein.
Precautionary measures:
Caution must be exercised in applying the drug in patients with a history of gastric ulcer or duodenal ulcer and in patients on anticoagulation therapy. These patients are at increased risk of ulcerative and erosive diseases of the gastrointestinal tract.
Use caution and monitor indicators of kidney function if use of the drug in elderly patients with chronic heart failure with symptoms of circulatory failure in patients with cirrhosis of the liver, as well as in patients with gipovolemiei as a result of surgical interventions.
In patients with renal insufficiency, if Cl creatinine more than 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 consume plenty of fluids.
If the treatment process had an allergic reaction (itching, skin rash, urticaria, photosensitivity), it is necessary to consult a doctor to address the issue of termination of treatment.
Meloxicam, like other NSAIDs, may mask symptoms of infectious diseases.
Application of meloxicam, like other drugs that block PG synthesis, may impair fertility and is not recommended for women who want to get pregnant.
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.
Dosage form
the solution for intramuscular introduction
Composition
meloxicam 10 mg,
Auxiliary substances: sodium chloride, glycine, plicopurpura (tetraglycol), poloxamer 188, meglumine (meglumine), sodium hydroxide, water for injections.
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 (GIT) and participate in the regulation of blood flow to the kidneys.
Pharmacokinetics
The relative bioavailability of almost 100 %. After intramuscular administration at a dose of 5 mg, the maximum concentration (Cmax) is 1, 62 µg/ml and is achieved within about 60 min. Meloxicam is well bound to plasma proteins, especially albumin (99 %). Penetrates into synovial fluid, the concentration in synovial fluid is approximately 50% of plasma concentration. The volume of distribution ( Vd) is low, on average 11 L. Interindividual differences amount to 30-40 %.
Meloxicam is almost completely metabolized in the liver with the formation of 4 pharmacologically inactive derivatives. The main metabolite, 5'-carboxymethoxy (60% of the dose), formed by oxidation of an intermediate metabolite, 5'-hydroxy-metallocycle, 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 isoenzyme CYP2C9, additional important isoenzyme CYP3A4. 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. In unaltered with faeces output of less than 5% of the magnitude of the daily dose, in the urine in an unmodified form the drug is detected only in trace amounts. The average half-life (T?) is 20 h. Plasma clearance averages 8 ml/min.
Meloxicam demonstrates linear pharmacokinetics in doses of 7, 5 to 15 mg when administered intramuscularly.
Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.
Side effect
From the digestive system: more 1 % - neuralgia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhoea, 0, 1-1 % - transient increase in activity of "liver" transaminases, hyperbilirubinemia, eructation, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including hidden), stomatitis, less than 0, 1 % - perforation of the digestive tract, colitis, hepatitis, gastritis.
With the hematopoietic system: more 1 % - anemia, 0, 1-1 % - changes in blood counts, including leukopenia, thrombocytopenia.
With the skin: more 1 % - itching, skin rash, 0, 1-1 % - hives, at least 0, 1 % - photosensitivity, bullous eruptions, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.
The respiratory system: less than 0, 1 % - bronchospasm.
From the Central nervous system (CNS): more than 1 % - dizziness, headache, 0, 1-1 % - vertigo, tinnitus, drowsiness, less than 0, 1 % - confusion, disorientation, emotional lability.
Of the cardiovascular system (CVS): more than 1% and peripheral edema, 0, 1-1 % - increase in blood pressure (BP), heart palpitations, "tides" 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.
Special conditions
Caution must be exercised in applying the drug in patients with a history who have peptic ulcer of stomach and duodenum, 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, in patients with chronic heart failure with clinical manifestations, in patients with liver cirrhosis, and in patients with gipovolemiei as a result of surgical interventions.
In patients with renal insufficiency, if QC more 30 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, photosensitivity), it is necessary to consult a doctor to address the issue of termination of treatment.
Meloxicam, like other NSAIDs, may mask symptoms of infectious diseases.
Application of meloxicam, like other drugs that block prostaglandin synthesis, may impair fertility and is not recommended to women planning pregnancy.
Indications
- Symptomatic treatment of osteoarthritis,
- Symptomatic treatment of rheumatoid arthritis,
- Symptomatic treatment of ankylosing spondylitis (Bechterew's disease).
Contraindications
- hypersensitivity to the active substance or auxiliary components,
- contraindicated in the period following the CABG,
- decompensated heart failure,
- full or partial combination of bronchial asthma, recurrent polyposis of the mucous membrane of the nose and paranasal sinuses and intolerance of acetylsalicylic KIS-lots and other non-steroidal anti-inflammatory drugs (NSAIDs) (including in the anamnesis),
- erosive-ulcerative changes of the gastric mucosa and 12 duodenal ulcer, active gastrointestinal bleeding,
- exacerbation of inflammatory bowel disease (ulcerative colitis, Crohn's disease),
- cerebrovascular bleeding or other bleeding,
- severe hepatic impairment or active liver disease,
- severe renal failure in patients not undergoing dialysis (creatinine clearance (CC) less than 30 ml/min), progressive kidney diseases including confirmed hyperkalemia,
Drug interaction
At simultaneous reception with other NSAIDs (as well as with acetylsalicylic acid) increases the risk of erosivno-yazvennah losses and bleeding from 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), antiplatelet agents
