Active substanceMeloksikamMeloksikam
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  • Dosage form: & nbspsolution for intramuscular injection
    Composition:

    1 ml of the solution contains:

    active substances: meloxicam 10.00 mg / ml;

    Excipients: glycine (aminoacetic acid), macrogol (polyethylene glycol 400), meglumine (N-methyl-D-glucamine), povidone-K 17 (plastidone C-15 or collidon 17 F), 1,2-propylene glycol, sodium hydroxide, water for injection .

    Description:Transparent liquid from yellow to yellow with a greenish shade of color.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug
    ATX: & nbsp

    M.01.A.C.06   Meloksikam

    M.01.A.C   Oksikamy

    Pharmacodynamics:Non-steroidal anti-inflammatory drug (NSAID), has anti-inflammatory, antipyretic, analgesic effect. Refers to the class of oxycomams; a derivative of enolic acid. The mechanism of action is the inhibition of the synthesis of prostaglandins (Pg) as a result of selective suppression of the enzymatic activity of cyclooxygenase 2 (COX2). With the appointment in high doses, long-term use and individual features of the organism, COX2, the selectivity decreases. Suppresses the synthesis of Pg in the inflammatory region to a greater extent than in the gastric mucosa or kidneys, which is due to the relatively selective inhibition of COX2. Less often causes erosive and ulcerative diseases of the gastrointestinal tract (GIT).
    Pharmacokinetics:

    Meloksikam is completely absorbed after intramuscular injection. The relative bioavailability compared with the bioavailability with oral administration is almost 100%.After intramuscular injection of the drug at a dose of 5 mg, the maximum concentration in the blood is 1.62-μg / ml and is reached-for about 60 minutes.

    Meloxicam binds well to plasma proteins, especially albumin (99%). Penetrates into the synovial fluid. The concentration in the synovial fluid is approximately 50% of the concentration in the plasma. The volume of distribution - an average of 11 liters. Interindividual deviations are 30-40%.

    Meloksikam is almost completely metabolized to 4 pharmacological inert metabolites. The main metabolite, 5-carboxymeloxicam (60% dose), is formed by oxidation of the intermediate metabolite of 5-hydroxymethylmeloxicam. In vitro studies have shown that the isozyme CYP2C9 plays an important role in this metabolic transformation, the CYP3.A4 isoenzyme plays an additional role. In the formation of two other metabolites (which make up 16 and 4% of the dose, respectively), peroxidase takes part, the activity of which can individually vary.

    Excretion of meloxicam, mainly in the form of metabolites, is carried out in the same amount with urine and feces.In unchanged form with feces less than 5% of the daily dose is output. In urine, in an unchanged form, the drug is found only in trace amounts. The average half-life is about 20 hours. Plasma clearance is an average of 8 ml / min.

    Meloxicam demonstrates linear pharmacokinetics in doses of 7.5-15 mg with intramuscular injection.

    Indications:

    Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis (Bechterew's disease) and other inflammatory and degenerative joint diseases accompanied by pain syndrome. Designed for symptomatic therapy, reducing pain and inflammation at the time of use; on the progression of the disease has no effect.

    Contraindications:Hypersensitivity (including NSAIDs of other groups), a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA), and drugs of the pirablock range; stomach ulcer and duodenal ulcer (in the phase of exacerbation), severe hepatic insufficiency, chronic renal failure (CRF) in patients not undergoing dialysis (creatinine clearance less than 30 ml / min),active gastrointestinal bleeding; progressive renal disease, severe liver failure or active liver disease, condition after coronary bypass surgery, confirmed by hyperkalemia, inflammatory bowel disease, children's age (15 years), pregnancy, lactation.
    Carefully:Elder, age, coronary artery disease (CAD), chronic heart failure (CHF) cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral vascular disease, smoking, CC less than 60 ml / min, ulcerative lesions of the gastrointestinal tract in the history, the presence of H infection . pylori, long-term use of NSAIDs, alcoholism, severe somatic diseases, simultaneous reception of oral glucocorticoid means (GCS) (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including klopido relational), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).
    Pregnancy and lactation:Contraindicated in pregnancy and lactation.
    Dosing and Administration:

    Intramuscular administration of meloxicam is advisable during the first 2-3 days of treatment. In the future, you should switch to taking the drug inside.

    The recommended dose of Meloxicam for injection is 7.5 mg or 15 mg / day. depending on the intensity of the pain syndrome and the severity of the inflammatory process. The maximum recommended daily dose should not exceed 15 mg.

    In patients with chronic renal failure of severe degree, on hemodialysis, the dose of Meloxicam should not exceed 7.5 mg / day.

    Given that the dose regimen for children and adolescents under the age of 15 years is not established, Meloksikam is assigned only to adults and adolescents over 15 years of age.

    Meloksikam should be administered by deep intramuscular injection. Do not use intravenously.

    Side effects:

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

    On the part of the organs of hematopoiesis: more than 1% - anemia; 0.1-1% - change in the blood formula, including leukopenia, thrombocytopenia.

    From the skin: more than 1% - itching, skin rash; 0.1-1% - hives; less than 0.1% - photosensitivity, bullous eruptions, erythema multiforme, including 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 side of the cardiovascular system: more than 1% - peripheral edema; 0.1-1% - increase in blood pressure (BP), palpitations, "tides" of blood to the skin of the face.

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

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

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

    Overdose:

    Symptoms: impaired consciousness, bleeding from the gastrointestinal tract, acute renal failure.

    Treatment: there are no specific antidotes; Symptomatic therapy is indicated.

    Interaction:

    With simultaneous admission with other NSAIDs, the risk of ulcerative gastrointestinal lesions and gastrointestinal bleeding increases.

    With the simultaneous use of NSAIDs with lithium preparations, the concentration of lithium ions in the blood plasma increases due to a reduction in renal excretion of lithium. If such a combination therapy is required, it is recommended to monitor the level of lithium ions in the blood plasma at the beginning of treatment, when choosing a dose and canceling meloxicam.

    Meloksikam reduces the effectiveness of intrauterine contraceptives (IUDs), hypotensive drugs. Indirect anticoagulants, ticlopidine, heparin, thrombolytics increase the risk of bleeding. Methotrexate enhances myelodepressant effect; diuretics increase the risk of kidney dysfunction; ciclosporin strengthens nephrotoxic action; colestramine accelerates excretion. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    In the event of peptic ulcers or gastrointestinal bleeding, the development of side effects from the skin and mucous membranes, the drug should be discarded.

    In patients with reduced circulating blood volume (BCC) and reduced glomerular filtration (dehydration, CHF, liver cirrhosis, nephrotic syndrome, clinically pronounced kidney disease, diuretics, dehydration after major surgery), there may be a clinically pronounced CRF that is completely reversible after withdrawal drug (in such patients at the beginning of treatment should monitor daily diuresis and kidney function). With persistent and significant increase in transaminases and changes in other indicators of liver function, the drug should be discontinued and control tests should be carried out. In patients with an increased risk of side effects, treatment starts with a dose of 7.5 mg. In the terminal stage of CRF in patients on dialysis, the dose should not exceed 7.5 mg / day. During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions (with dizziness and drowsiness).To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions (with dizziness and drowsiness).
    Form release / dosage:Solution for intramuscular injection 10 mg / ml.
    Packaging:For 1.5 ml in ampoules from the glass of the first hydrolytic class of brown color, having a system of fracture. By 3, 5 or 10 ampoules are placed in a contour mesh package made of a polyvinyl chloride film. For 1 or 2 contour mesh packages along with the instruction for use are placed in a pack of cardboard.
    Storage conditions:

    List B. In a dry, the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007393/09
    Date of registration:18.09.2009 / 16.02.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia
    Information update date: & nbsp22.04.2018
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