Description
Release form
Tablets.
Packing
20 pcs.
Pharmacological action
Pharmaceutical group: NSAIDs.
Pharmaceutical action: Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with the inhibition of prostaglandin synthesis as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in prostaglandin biosynthesis in the area of inflammation.
When prescribed in high doses, prolonged use and individual characteristics of the body, selectivity for COX-2 decreases. Suppresses the synthesis of prostaglandins in the area of inflammation to a greater extent, than in the mucous membrane of the stomach or kidneys, which is associated with a relatively selective inhibition of COX-2. Less commonly, it causes erosive and ulcerative diseases of the gastrointestinal tract (GIT). To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandins that protect the gastrointestinal mucosa and are involved in the regulation of blood flow in the kidneys.
Pharmacokinetics: Well absorbed from the digestive tract, the absolute bioavailability of meloxicam is 89%. Simultaneous eating does not alter absorption. When using the drug inside at doses of 7.5 and 15 mg, its concentration is proportional to the doses. Equilibrium concentrations are reached within 3 to 5 days. With prolonged use of the drug (more than 1 year), concentrations are similar to those that are observed after the first achievement of a steady state of pharmacokinetics.
Plasma protein binding is more than 99%. The range of differences between the maximum and basal concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-1.0 μg / ml when using a dose of 7.5 mg, and 0.8-2 when using a dose of 15 mg. 0 μg / ml (values of the minimum concentration (Cmin) and maximum concentration (Cmax), respectively, are given). Meloxicam crosses the histohematological barriers, the concentration in the synovial fluid reaches 50% of the maximum concentration of the drug in plasma. It is almost completely metabolized in the liver with the formation of four pharmacologically inactive derivatives.
The main metabolite of 5′-carboxymeloxicam (60% of the dose) is formed by oxidation of the intermediate metabolite of 5′-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose). In vitro studies have shown that the CYP 2C9 isoenzyme plays an important role in this metabolic transformation, and the CYP 3A4 isoenzyme plays an additional role. In the formation of two other metabolites (constituting, respectively, 16% and 4% of the dose of the drug), peroxidase is involved, the activity of which probably individually varies.
It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted through the intestine in an unchanged form, in the urine in an unchanged form, the drug is found only in trace amounts. The half-life (T1 / 2) of meloxicam is 15–20 hours. Plasma clearance is an average of 8 ml / min. In the elderly, the clearance of the drug is reduced. The volume of distribution is low and averages 11 liters.
Hepatic or renal failure of moderate severity does not significantly affect the pharmacokinetics of meloxicam.
Indications
– symptomatic treatment of osteoarthritis
– symptomatic treatment of rheumatoid arthritis
– symptomatic treatment of ankylosing spondylitis (ankylosing spondylitis).
Contraindications
– hypersensitivity to meloxicam or excipients of the drug contains lactose, therefore patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug srdlkort – uncompensated heart failure
– a complete and incomplete combination of bronchial asthma, polynosis of the nose and intolerance to acetyls itsilovoy acid and other NSAIDs
– erosive and ulcerative changes in the mucosa of the stomach or duodenum 12, active gastrointestinal bleeding
– inflammatory bowel disease (ulcerative colitis, Crohn’s disease)
– cerebrovascular bleeding or other bleeding
– severe liver failure or active liver disease
– chronic renal failure in patients not undergoing dialysis (creatinine clearance (CC) less than 30 ml / min), progressive kidney disease, in tons h confirmed hyperkalemia
– pregnancy, period of breastfeeding
– children under 12 years old.
Caution.
Coronary heart disease (CHD), cerebrovascular disease, compensated heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, CC 30-60 ml / min.
Anamnestic data on the development of gastrointestinal ulcer, the presence of Helicobacter pulori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs: – anticoagulants (e.g. warfarin)
– antiplatelet agents (e.g. acetylsalicylic acid, clopidogrel)
– oral glucocorticosteroids (GCS) (e.g. prednisolone selective inhibition
(e.g. citalopram, fluoxetine, paroxetine, sertraline).
To reduce the risk of adverse events from the gastrointestinal tract, the minimum effective dose should be used with the lowest possible short course.
Cautions
– Caution should be exercised when using Movasin drug in patients with a history of gastric ulcer and duodenal ulcer, as well as in patients undergoing anticoagulant therapy. In such patients, the risk of erosive and ulcerative diseases of the gastrointestinal tract
is increased – care should be taken and the renal function indicators should be monitored when using Movasin in elderly patients, patients with chronic heart failure (CHF) with circulatory failure, in patients with cirrhosis, and also in patients with hypovolemia as a result of
surgical interventions – in patients with a slight or moderate decrease in renal function (CC more than 30 ml / min) no correlation is required
dosage regimen – patients taking diuretics and meloxicam at the same time should take a sufficient amount of
liquid – if allergic reactions occur during treatment (itching, skin rash, urticaria, photosensitization) it is necessary to consult a doctor to decide whether to stop taking Movasin
– meloxicam, like other NSAIDs, can mask the symptoms of
infectious diseases – the use of meloxicam, like other drugs that block prostaglandin synthesis, can affect fertility, therefore not recommended for women who wish to become pregnant.
Driving a vehicle, servicing machines and mechanisms
Using the drug Movasin may cause unwanted effects in the form of headaches and dizziness, drowsiness, therefore, while taking the drug, you should refuse to drive vehicles and maintain machines and mechanisms that require concentration.
Composition
1 tab.: – meloxicam (in terms of 100% substance) 7.5 mg or 15 mg
Excipients: povidone-12.6 thousand (polyvinylpyrrolidone medical low molecular weight 12600 В± 2700), lactose monohydrate (sugar ), crospovidone (collidone CL, collidone CL-M), potato starch, talc, magnesium stearate, microcrystalline cellulose.
Dosage and administration
The drug Movasin is taken orally during meals in a daily dose of 7.5-15 mg.
Recommended dosage: – rheumatoid arthritis: 15 mg movasin per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.
– osteoarthritis: 7.5 mg Movasin per day. With inefficiency, the dose can be increased to 15 mg per day.
– ankylosing spondylitis: 15 mg Movasin per day.
The maximum daily dose is 15 mg.
In patients with an increased risk of side effects, as well as in patients with severe renal failure undergoing hemodialysis, the dose should not exceed 7.5 mg Movasin per day.
Side effects of
From the digestive system: more than 1% – dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea 0.1-1% – a transient increase in hepatic transaminase activity, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, gastrointestinal bleeding (including hidden), stomatitis less than 0, 1% – gastrointestinal perforation, colitis, hepatitis, gastritis.
From the side of hematopoietic organs: more than 1% – anemia 0.1-1% – change in blood count, incl. leukopenia, thrombocytopenia.
From the skin: more than 1% – itching, skin rash 0.1-1% – urticaria less than 0.1% – photosensitivity, bullous rashes, erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the respiratory system: less than 0.1% – bronchospasm.
From the nervous system: more than 1% – dizziness, headache 0.1-1% – vertigo, tinnitus, drowsiness less than 0.1% – confusion, disorientation, emotional lability.
From the cardiovascular system (CCC): more than 1% – peripheral edema 0.1-1% – increased blood pressure (BP), palpitations, flushing of the face.
From the urinary system: 0.1-1% – hypercreatininemia and / or increased urea in the blood serum of less than 0.1% – acute renal failure, no connection with meloxicam has been established – interstitial nephritis, albuminuria, hematuria.
On the part of the sensory organs: less than 0.1% – conjunctivitis, visual impairment, including blurred vision.
Allergic reactions: less than 0.1% – angioedema, anaphylactoid / anaphylactic reactions.
Drug interaction
– when used simultaneously with other NSAIDs (as well as with acetylsalicylic acid), the risk of erosive-ulcerative lesions and bleeding of the gastrointestinal tract
increases – while the use of Movasin with antihypertensive drugs may decrease the effectiveness of the last
drugs – with development of cumulation of lithium and increase in its toxic effect is possible (it is recommended to control the concentration of lithium in the blood)
– with simultaneous use Research of Movasin with methotrexate increases the side effect of the latter on the hematopoietic system (the risk of anemia and leukopenia, periodic monitoring of a general blood test is indicated)
– with simultaneous use with diuretics and with cyclosporine, the risk of developing renal failure
increases – with simultaneous use of Movasin with intrauterine contraceptives, the effectiveness of the latter
may decrease – with simultaneous use with anticoagulants (heparin, ticlopidine, warfarin ), as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring blood coagulation parameters)
– with the simultaneous use of Movasin with colestiramine, the drug is excreted from the body
– with simultaneous use with selective serotonin reuptake inhibitors, the risk of bleeding from the gastrointestinal tract increases.
Deystvuyuschee substances
meloxicam
Terms of dispatch from
pharmacies Prescription
dosage form
tablets
Synthesis, Russian
