Movasin – NSAID, has anti-inflammatory, antipyretic, analgesic action. It belongs to the class of oxycams; a derivative of enolic acid.
Meloxicam is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic effects.
The anti-inflammatory action is due to the inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the area of inflammation.
To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandin, which protects the mucosa of the gastrointestinal tract (GIT) and is involved in the regulation of blood flow in the kidneys.
The relative bioavailability is almost 100%. After intramuscular administration of the drug at a dose of 5 mg, the maximum concentration (Cmax) is 1.62 mcg/ml and is reached within approximately 60 min. Meloxicam binds well to plasma proteins, especially to albumin (99%). It penetrates the synovial fluid, the concentration in the synovial fluid is approximately 50% of the plasma concentration. The volume of distribution (Vd) is low, averaging 11 L. Interindividual variation is 30-40%.
Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive derivatives. The main metabolite, 5′-carboxymeloxicam (60% of the dose value), is formed by oxidation of the intermediate metabolite, 5′-hydroxy-methylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose value). In vitro studies have shown that CYP2C9 isoenzyme plays an important role in this metabolic transformation, isoenzyme CYP3A4 has additional importance. Peroxidase, the activity of which probably varies individually, is involved in the formation of the other two metabolites (which constitute, respectively, 16% and 4% of the drug dose).
Extracted equally in the feces and urine, mainly as metabolites. Less than 5% of daily dose is excreted unchanged in the feces, the drug is excreted unchanged in the urine only in trace amounts. Mean elimination half-life (T½) is 20 hours. Plasma clearance averages 8 ml/min.
Meloxicam exhibits linear pharmacokinetics at doses of 7.5-15 mg when administered intramuscularly.
Moderate hepatic or renal insufficiency has no significant effect on the pharmacokinetics of meloxicam.
- Symptomatic treatment of rheumatoid arthritis
- Symptomatic treatment of osteoarthritis;
- Symptomatic treatment of ankylosing spondylitis (Behterev disease).
1 ml contains meloxicam – 10 mg,
water for injection.
How to take, the dosage
Intramuscularly. Intramuscular administration of Movasin is indicated only during the first 2-3 days. Later the treatment is continued with the use of oral forms (tablets).
The recommended dose is 7.5 mg or 15 mg once a day, depending on the intensity of pain and severity of the inflammatory process.
The drug is administered deeply intramuscularly. Intravenous administration of the drug is prohibited!
In patients with an increased risk of adverse reactions, the daily dose should not exceed 7.5 mg.
In patients with end-stage renal failure who are on hemodialysis, the dose of the drug should not exceed 7.5 mg. In patients with mild to moderate renal impairment (CKD greater than 30 ml/min) the dose of the drug should not exceed 7.5 mg.
The dosage regimen of the drug for intramuscular injections in children and adolescents has not been defined; this dosage form can be used only in adult patients. The maximum recommended daily dose is 15 mg.
When different dosage forms of the drug are used in combination, the maximum daily dose of the drug in tablets, suppositories and solution for injection is 15 mg.
Simultaneous use with other NSAIDs (as well as with acetylsalicylic acid) increases the risk of erosive ulcerative lesions and bleeding from the gastrointestinal tract.
In concomitant use with hypotensive drugs, the effectiveness of the latter drugs may decrease.
Concomitant use with lithium preparations may lead to cumulation of lithium and increase its toxic effect (it is recommended to control the lithium concentration in the blood).
In concomitant use with methotrexate there is increased side effect of the latter on the hematopoietic system (risk of anemia and leukopenia, periodic control of total blood count is indicated).
Concomitant use with diuretics and with cyclosporine increases the risk of renal failure.
Concomitant use with intrauterine contraceptives may decrease the effectiveness of the latter.
In concomitant use with anticoagulants (heparin, ticlopidine, warfarin), antiaggregants (acetylsalicylic acid, clopidogrel), as well as with fibrinolytic drugs (streptokinase, fibrinolysin) the risk of bleeding increases (periodic monitoring of blood clotting is necessary).
Concomitant use with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.
Caution should be exercised when using the drug in patients with a history of peptic ulcer disease and duodenal ulcer, as well as in patients on anticoagulant therapy. These patients have an increased risk of gastrointestinal erosive-ulcer disease.
We should use the drug with caution and monitor renal function parameters when using in elderly patients, in patients with chronic heart failure with clinical manifestations, in patients with cirrhosis of liver as well as in patients with hypovolemia as a result of surgical interventions.
In patients with renal insufficiency, if the CKR is greater than 30 mL/min, no dosing adjustment is required.
In patients on dialysis, the dosage of the drug should not exceed 7.5 mg/day.
Patients taking diuretics and meloxicam at the same time should take sufficient fluids.
If allergic reactions occurred during treatment (itching, skin rash, urticaria, photosensitization) it is necessary to consult a physician to decide on stopping the drug.
Meloxicam, like other NSAIDs, can mask the symptoms of infectious diseases.
The use of meloxicam, as well as other drugs that block the synthesis of prostaglandins, may affect fertility, so it is not recommended for women who plan to become pregnant.
- hypersensitivity to the active substance or excipients;
- contraindicated in the period after coronary artery bypass grafting;
- decompensated heart failure;
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses, and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (NSAIDs) (incl.ч.
- erosive-ulcerative changes of mucous coat of stomach and duodenum, active gastrointestinal bleeding;
- acute inflammatory bowel disease (nonspecific ulcerative colitis, Crohn’s disease);
- cerebrovascular bleedingCerebrovascular bleeding or other bleeding;
- explicit hepatic insufficiency or active liver disease;
- explicit renal insufficiency in patients not on dialysis (creatinine clearance (CK) less than 30 ml/min), advanced renal disease including
- pregnancy, breastfeeding
- children under 18 years of age
Gastrointestinal system: more than 1 % – dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1 % – transient increase of “liver” transaminases activity, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, GI bleeding (including hidden bleeding), stomatitis; less than 0.1less than 0.1 % – gastrointestinal perforation, colitis, hepatitis, gastritis.
Blood system: over 1% – anemia; 0.1-1% – changes of the blood count, including leukopenia, thrombocytopenia.
Skin: more than 1% – itching, skin rash, 0.1-1% – urticaria, less than 0.1% – photosensitization, bullous rash, erythema multiforme, including Stevens-Johnson syndrome.
Respiratory system: less than 0.1 % – bronchospasm.
Central nervous system (CNS): over 1% – dizziness, headache; 0,1-1% – vertigo, tinnitus, somnolence; less than 0,1% – confusion, disorientation, emotional lability.
Cardiovascular system (CVS): over 1% – peripheral edema; 0,1-1% – increase of blood pressure (BP), palpitation, “rushes” of blood to the skin.
Urinary system: 0.1-1 % – hypercreatininemia and/or increased serum urea, less than 0.1% – acute renal failure, the relationship with meloxicam intake is not determined – interstitial nephritis, albuminuria, hematuria.
Sensory organs: less than 0.1% – conjunctivitis, visual disturbances, including blurred vision.
Allergic reactions: less than 0.1% – angioedema, anaphylactic/anaphylactoid reactions.
Local reactions: more than 1% – swelling at the injection site; less than 1% – painful sensations at the injection site.
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, respiratory arrest, asystole.
Treatment: no specific antidote; symptomatic therapy. Forced diuresis, urine alkalinization, hemodialysis are ineffective due to high binding of the drug to blood proteins.
Movalis, Meloxicam, Amelotex, Movasin, Arthrosan, Meloxicam-Teva, Meloxicam DS, Meloxicam Stada, Petcam Tabs, Meloxidil, Elox-SOLofar
|Conditions of storage|
In a dry, light-protected place at a temperature not exceeding 30 ° C.
Sintez OAO, Russia
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