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

    1 ampoule contains:

    Active ingredient: meloxicam - 15 mg;

    Auxiliary components: ethanol, poloxamer 188, sodium chloride, glycine, meglumine, sodium hydroxide, water for injection.

    Description:Transparent solution of yellow with a green tint of color.
    Pharmacotherapeutic group:Nonsteroidal anti-inflammatory drugs
    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 acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandin, which protects the mucous membrane of the gastrointestinal tract and takes part in the regulation of blood flow in the kidneys.
    Pharmacokinetics:

    The relative bioavailability is almost 100%. After the / m introduction of the drug in a dose of 5 mg Cmax is 1.62 μg / ml and is achieved within about 60 minutes. Meloksikam binds well to 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. Vd 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'-hydroxymethylmeloxicam, 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 found only in trace amounts. Average T1/2 is 20 hours. Plasma clearance is an average of 8 ml / min.

    Meloxicam demonstrates a linear pharmacokinetics in doses of 7.5-15 mg with an IM injection.

    Hepatic or renal failure of moderate severity does not have a significant effect on 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 aortocoronary bypass surgery;

    Decompensated heart failure;

    - complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance of acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (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 impairment or active liver disease;

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

    - pregnancy, the period of breastfeeding;

    - Children under 18 years.

    Carefully:

    Ischemic heart disease, cerebrovascular disease, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease, smoking, creatinine clearance from 30 to 60 ml / min. Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of non-steroidal anti-inflammatory drugs (NSAIDs), frequent alcohol use, severe physical illnesses, 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:Application in pregnancy and lactation is contraindicated.
    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 greater 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; <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% - hives; 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 side of the central 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% - increased blood pressure, 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 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, incl. 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.

    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 use with other NSAIDs (as well as acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract;

    - With simultaneous use with antihypertensive drugs, the effectiveness of the latter may be reduced;

    - With simultaneous use with lithium preparations, development of cumulation of lithium and increase of its toxic effect (it is recommended to control the concentration of lithium in the blood);

    - 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;

    - With simultaneous use with anticoagulants (heparin, ticlopidine, warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), as well as with fibrinolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (periodic monitoring of blood coagulability);

    - With simultaneous application with selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases.

    Special instructions:

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

    - Care should be taken to monitor kidney function in elderly patients, patients with chronic heart failure with circulatory failure, in patients with cirrhosis, as well as in patients with hypovolemia as a result of surgical interventions.

    - In patients with renal failure, if the creatinine clearance is more than 30 ml / min, dosage adjustment is not required.

    - In patients undergoing 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, photosensitization) occur during treatment, you should consult a doctor to decide whether to stop taking the drug.

    - Meloksikam, like other non-steroidal anti-inflammatory drugs, 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. It should abandon the management of vehicles and maintenance of machines and mechanisms that require concentration of attention.
    Form release / dosage:Solution for intramuscular injection 10 mg / ml (15 mg / 1.5 ml).
    Packaging:For 1.5 ml of the drug in a glass ampoule. 3 glass ampoules per tray plastic contour. For 1 pallet plastic contour along with instructions for medical use in a cardboard box.
    Storage conditions:

    Store in a dry, 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-000300/10
    Date of registration:25.01.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:Danson Trading Pharmaceutical Company LimitedDanson Trading Pharmaceutical Company Limited Vietnam
    Representation: & nbspDominanta-Service CJSCDominanta-Service CJSC
    Information update date: & nbsp22.04.2018
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