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

    Per 1 ml:

    Active substance: meloxicam - 10 mg,

    Excipients: sodium chloride, glycine, glycofurfural (tetraglycol), poloxamer 188, meglumine (meglumine), sodium hydroxide, water for injection.

    Description:Transparent or slightly opalescent solution of yellow with a greenish tinge.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)
    ATX: & nbsp

    M.01.A.C.06   Meloksikam

    M.01.A.C   Oksikamy

    Pharmacodynamics:Meloksikam - a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. Anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the inflammatory region. Less meloxicam It acts on cyclooxygenase-1 (COX-1) involved in prostaglandin synthesis, protecting the mucosa of the gastrointestinal tract (GIT) and participate in the regulation of blood flow in the kidney.
    Pharmacokinetics:

    The relative bioavailability is almost 100%. After intramuscular injection of the drug at a dose of 5 mg, the maximum concentration (Cmax) is 1.62 μg / ml and is achieved within about 60 minutes. Meloksikam is well bound by plasma proteins, especially albumin (99%). It penetrates into the synovial fluid, the concentration in the synovial fluid is approximately 50% of the concentration in the plasma. The volume of distribution (Vd) is low, an average of 11 liters.Interindividual differences account for 30-40%.

    Meloksikam is almost completely metabolized in the liver with the formation of 4 pharmacologically inactive derivatives. The main metabolite, 5-carboxymeloxicam (60% of the dose value), is formed by oxidation of the intermediate metabolite, 5-hydroxymethyl methyloxicam, which is also excreted, but to a lesser degree (9% of the dose value). In vitro studies have shown that the isoenzyme CYP2C9 plays an important role in this metabolic transformation, the isoenzyme CYP3A4 has an additional significance. In the formation of the other two metabolites (which constitute, respectively, 16% and 4% of the dose), peroxidase takes part, the activity of which probably varies individually.

    It is excreted equally with feces and urine, mainly in the form of metabolites. In unchanged form with feces less than 5% of the daily dose is excreted, in the urine in unchanged form the drug is detected only in trace amounts. The mean half-life (T1/2) is 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.

    Liver 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 (Bekhterev's disease).

    Contraindications:

    - Hypersensitivity to the active substance or ancillary components;

    - contraindicated in the period after aorto-coronary bypass surgery;

    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 nonsteroidal anti-inflammatory drugs (NSAIDs) (including in the anamnesis);

    - erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal hemorrhage;

    - exacerbation of inflammatory bowel diseases (ulcerative colitis, Crohn's disease);

    - cerebrovascular bleeding or other bleeding;

    - severe hepatic failure or active liver disease;

    - marked renal failure in patients not undergoing dialysis (creatinine clearance (CK) is less than 30 ml / min), progressive kidney diseases including. confirmed hyperkalemia;

    - pregnancy, the period of breastfeeding;

    - Children under 18 years.

    Carefully:

    Ischemic heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease, smoking, KC from 30 to 60 ml / min.

    Anamnestic data on the development of gastrointestinal ulcer (GI), presence of Helicobacter pylori infection, advanced age, prolonged use of NSAIDs, frequent alcohol use, severe physical illness, concomitant therapy with the following drugs:

    - anticoagulants (for example, warfarin);

    - antiaggregants (for example, acetylsalicylic acid, clopidogrel);

    - oral glucocorticosteroids (for example, prednisolone);

    - selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

    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.

    Pregnancy and lactation:Contraindicated in pregnancy and lactation.
    Dosing and Administration:

    Intramuscularly. Intramuscular injection of the drug is indicated only during the first 2-3 days. Further treatment is continued with the use of oral forms (tablets).

    The recommended dose is 7.5 mg or 15 mg 1 time / day, depending on the intensity of pain and the severity of the inflammatory process.

    The drug is administered intramuscularly. Intravenous injection 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 terminal stage of renal failure who are on hemodialysis, the dose of the drug should not exceed 7.5 mg. In patients with small or moderate renal impairment (QC more than 30 ml / min), the dose of the drug should not exceed 7.5 mg.

    Dosage regimen for intramuscular injections in children and adolescents is not defined, this dosage form can be used only in adult patients. The maximum recommended daily dose is 15 mg.

    With the combined use of various dosage forms of the drug, its maximum daily dose in tablets, suppositories and as a solution for injection is 15 mg.

    Side effects:

    From the digestive system: more than 1% - dyspepsia, incl. 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 hematopoiesis system: more than 1% - anemia; 0.1-1% change in the blood formula, incl. leukopenia, thrombocytopenia.

    From the skin: more than 1% - itching, skin rash; 0,1-1% - urticaria; less than 0.1% - photosensitivity, bullous eruptions, erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis.

    From 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.

    From the side of the cardiovascular system (SSS): more than 1% - peripheral edema; 0.1-1% - increase in blood pressure (BP), palpitation, "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 renalfailure; communication with the reception of Myloxicam is not established - interstitial nephritis, albuminuria, hematuria.

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

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

    Local Reactions: more than 1% - puffiness at the injection site; less than 1% - painful sensations at the injection site.

    Overdose:

    Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, hepatic insufficiency, respiratory arrest, asystole.

    Treatment: there is no specific antidote; symptomatic therapy. Forced diuresis, alkalinization of urine, hemodialysis - ineffective because of the high connection of the drug with blood proteins.

    Interaction:

    With simultaneous administration with other NSAIDs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

    With simultaneous use with antihypertensive drugs, it is possible to reduce the effectiveness of the latter.

    With simultaneous use with lithium preparations, lithium cumulation and its toxic effect can be developed (control of lithium concentration in the blood is recommended).

    With simultaneous use with methotrexate, the side effect of the latter on the hematopoietic system is increased (the risk of anemia and leukopenia, periodic monitoring of the general blood test is shown).

    With simultaneous use with diuretics and with cyclosporine, the risk of developing kidney failure increases.

    With simultaneous use with intrauterine contraceptives, the effectiveness of the latter may be reduced.

    When used simultaneously with anticoagulants (heparin, ticlopidine, warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), as well as with fibrinolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring of blood coagulability indices is necessary).

    When used simultaneously with selective serotonin reuptake inhibitors, the risk of developing gastrointestinal bleeding increases.

    Special instructions:

    Care should be taken when using the drug in patients who have a history of peptic ulcer and duodenal ulcer, as well as in patients who are on anticoagulant therapy. In such patients, the risk of erosive and ulcerative gastrointestinal diseases is increased.

    Caution should be exercised and the kidney function should be monitored when the drug is used in elderly patients, in patients with chronic heart failure with clinical manifestations, in patients with cirrhosis of the liver, as well as in patients with hypovolemia as a result of surgical interventions.

    In patients with renal insufficiency, if the QC is more than 30 ml / min, dosage adjustment is not required.

    In patients on dialysis, the dosage of the drug should not exceed 7.5 mg / day.

    Patients taking both diuretics and meloxicam, should take a sufficient amount of fluid.

    If allergic reactions (itching, skin rash, urticaria, photosensibilization) occur during treatment, it is necessary to consult a doctor with a view to resolving the issue of stopping the drug.

    Meloksikam, 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, can affect fertility, so it is not recommended for women planning a pregnancy.

    Effect on the ability to drive transp. cf. and fur:The use of the drug may cause undesirable effects in the form of headaches and dizziness, drowsiness. During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Solution for intramuscular injection 10 mg / ml in ampoules of neutral glass grade HC-3, 1.5 ml.
    Packaging:

    3, 5 ampoules are placed in boxes of cardboard.

    3, 5 ampoules are placed in contoured cell packs from a polyvinyl chloride film and aluminum foil or into contoured cell packs from a polyvinyl chloride film.

    1 contour mesh package is placed in packs of cardboard.

    In each box, a pack of instructions for use and the ampoule scaler.Ampoule scapper does not invest when using ampoules with a kink ring or with an incision and a break point.

    Storage conditions:

    In a dry, protected from light place, at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-003632/10
    Date of registration:30.04.2010 / 06.12.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOKOM, CJSC BIOKOM, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspBIOKOM, CJSCBIOKOM, CJSC
    Information update date: & nbsp16.05.2018
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