Meloxicam DC solution 10mg/ml 1.5ml ampoules, 3pcs

Composition

1 ampoule contains:

Active ingredient:

meloxicam-15 mg;

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

Pharmacological action

Pharmacotherapeutic group: Nonsteroidal anti-inflammatory drugscode ATX: M01AC06 Pharmacodynamics : Meloxicam is a nonsteroidal anti-inflammatory drug with analgesic anti-inflammatory and antipyretic effects. The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2) involved in prostaglandin biosynthesis in the inflammatory region. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandin, which protects the gastrointestinal mucosa and is involved in the regulation of blood flow in the kidneys. Pharmacokinetics:

The relative bioavailability is almost 100%. After intravenous use of the drug at a dose of 5 mg, the Cmax is 1.62 mcg / ml and is reached within approximately 60 minutes. Meloxicam binds well to plasma proteins, especially albumin (99%). Penetrates synovial fluid The synovial fluid concentration is approximately 50% of the plasma concentration. VD is low averaging 11 liters. Interindividual differences are 30-40%.

Meloxicam is almost completely metabolized in the liver to form 4 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 to a lesser extent (9% of the dose). In vitro studies have shown that the CYP2C9 isoenzyme plays an important role in this metabolic transformation and the CYP3A4 isoenzyme is of additional importance. The formation of the other two metabolites (which make up 16% and 4% of the drug dose, respectively) involves peroxidase, the activity of which probably varies individually.

It is excreted equally in the feces and urine, mainly in the form of metabolites. In unchanged form, less than 5% of the daily dose is excreted in the feces in the urine. In unchanged form, the drug is detected only in trace amounts. The average T 1/2 is 20 hours. The average plasma clearance is 8 ml/min.

Meloxicam demonstrates linear pharmacokinetics at doses of 7.5-15 mg when administered intravenously.

Moderate hepatic or renal insufficiency 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).

Use during pregnancy and lactation

Use during pregnancy and lactation is contraindicated.

Contraindications

– hypersensitivity to the Active ingredient or auxiliary components;

– contraindicated in the period after the coronary artery 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 NSAIDs (including in the anamnesis);

– erosive and ulcerative changes in the mucous membrane of the stomach and 12 duodenal ulcer, active gastrointestinal bleeding;

– exacerbation of inflammatory bowel disease (ulcerative colitis, Crohn’s disease);

– cerebrovascular bleeding or other bleeding;

– severe hepatic impairment or active liver disease;

– severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 ml/min), progressive kidney diseases including confirmed hyperkalemia;

– pregnancy period of breastfeeding;

– children’s age till 18 years.

With caution:

Coronary heart disease cerebrovascular diseases chronic heart failure dyslipidemia / hyperlipidemia diabetes mellitus peripheral arterial diseases smoking creatinine clearance from 30 to 60 ml/min. Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract presence of Helicobacter pylori infection elderly age long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) frequent alcohol consumption severe somatic diseases concomitant therapy with the following drugs:

– Anticoagulants (e. g. warfarin);

– Antiplatelet agents (e. g. acetylsalicylic acid clopidogrel);

– oral glucocorticosteroids (e. g. prednisone);

– selective serotonin reuptake inhibitors (e. g. citalopram fluoxetine paroxetine sertraline);

To reduce the risk of gastrointestinal adverse events, the minimum effective dose should be used in the shortest possible course.

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 belching esophagitis gastroduodenal ulcer gastrointestinal bleeding (including hidden) stomatitis;

From the hematopoietic system: more than 1% – anemia; 0.1-1% – changes in the blood formula, including leukopenia and thrombocytopenia.

From the skin: more than 1% – pruritus skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitization bullous rashes erythema multiforme including Stevens-Johnson syndrome toxic epidermal necrolysis.

From the respiratory system: less than 0.1% – bronchospasm.

From 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 cardiovascular system: more than 1% – peripheral edema; 0.1-1% – increased blood pressure palpitations “flushes” of blood to the skin of the face.

From the urinary system: 0.1-1% – hypercreatininemia and / or increased serum urea; less than 0.1% – acute renal failure; no association with meloxicam has been established – interstitial nephritis albuminuria hematuria.

From the 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.

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;

– While the use of antihypertensive drugs may reduce the effectiveness of the latter;

– With simultaneous use with lithium preparations may develop accumulation of lithium and increase its toxic effect (it is recommended to monitor the concentration of lithium in the blood);

– While the use of methotrexate increases adverse effect on the hematopoietic system (the risk of anemia and leukopenia shows periodic monitoring of complete blood count);

– While the use of diuretics and cyclosporine increases the risk of renal failure;

– together with the use of intrauterine contraceptives may reduce the effectiveness of the latter;

– With the simultaneous use of anticoagulants (heparin, warfarin tiklopidin) antiplatelet agents (acetylsalicylic acid clopidogrel) as well as with fibrinolytic drugs (streptokinase fibrinolysin), the risk of bleeding increases (periodic monitoring of blood clotting parameters is necessary);

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

How to take, course of use and dosage

Intramuscularly. Intramuscular use of the drug is indicated only during the first 2-3 days. In the future, 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 deep intramuscularly. Intravenous use 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 or moderate renal impairment (creatinine clearance greater than 30 ml / min), the dose of the drug should not exceed 7.5 mg.

The dosage regimen of the drug for intramuscular injection in children and adolescents is not defined this dosage form can only be used 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 suppository tablets and in the form of a solution for injection is 15 mg.

Overdose

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

Treatment:  there is no specific antidote; symptomatic therapy. Forced diuresis alkalinization of urine hemodialysis – ineffective due to the high binding of the drug to blood proteins.

Special instructions

– Caution should be exercised when using the drug in patients with a history of peptic ulcer of the stomach or duodenum, as well as in patients undergoing anticoagulant therapy. Such patients have an increased risk of erosive and ulcerative diseases of th