Description
Release form
Tablets
Packing
20 pcs.
Pharmacological 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 inhibition of prostaglandin synthesis as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the area of inflammation.
When prescribed in high doses, prolonged use and individual characteristics of the body, selectivity for COX-2 decreases. It inhibits 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 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 orally in doses of 7, 5 and 15 mg of its concentration are 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 insufficiency
complete and incomplete combination of bronchial asthma, polynosis of the nose and intolerance to acetylsalicylic acid and other NSAIDs
erosive-ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding
inflammatory bowel disease (ulcerative colitis, Crohn’s disease)
cerebral hemorrhage or active liver disease
chronic renal failure in patients not undergoing dialysis (creatinine clearance (CC) less than 30 ml / min), progressive bolevaniya kidney, including confirmed hyperkalemia
pregnancy, 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 ulceration, 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, for example, acetyl acetic acid,
oral glucocorticosteroids (GCS) (e.g., prednisone)
selective serotonin reuptake inhibitors (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.
Composition of
1 tablet contains:
Active substance: meloxicam (in terms of 100% substance) 7.5 mg
Excipients: 12 thousand. low molecular weight polyvinylpyrrolidone medical 12600 В± 2700), lactose monohydrate (milk 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.
osteoarthrosis: 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
with simultaneous use with other NSAIDs (as well as with acetylsalicylic acid) increases the risk of erosive-ulcerative lesions and bleeding of the gastrointestinal tract
while the use of Movasin with antihypertensive drugs may decrease the effectiveness of the last
with simultaneous use lithium and increase its toxic effect (it is recommended to control the concentration of lithium in the blood)
with simultaneous use ovasina with methotrexate increases the side effects of the latter on the hematopoietic system (risk of anemia and leukopenia, periodic monitoring of a general blood test is indicated)
with simultaneous use with diuretics and with cyclosporine increases the risk of renal failure
with simultaneous use of Movasin with intrauterine contraceptives, the effectiveness of the latter
may be reduced while it is used with anticoagulants (heparin, ticlopidine, warfarin, also with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring is necessary the coagulation index)
with the simultaneous use of Movasin with colestyramine accelerates the excretion of the drug from the body
while the use of selective serotonin reuptake inhibitors increases the risk of bleeding from the gastrointestinal tract.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, respiratory arrest, asystole.
Treatment: there is no specific antidote in case of an overdose of the drug, gastric lavage should be performed, activated charcoal intake (within the next hour), symptomatic therapy. Forced diuresis, alkalization of urine, hemodialysis are ineffective due to the high connection of the drug with blood proteins.
Deystvuyuschee substances
meloxicam
dosage form
tablets
Synthesis, Russian
