Movasin solution 10mg/ml 1.5ml ampoules, 5pcs

Composition

Active ingredient:

meloxicam – 10 mg,

Auxiliary substances:

sodium chloride,

glycine,

glycofurfural (tetraglycol),

poloxamer 188,

meglumine (meglumine),

sodium hydroxide,

water for injection.

Pharmacological action

of NSAIDs. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in prostaglandin biosynthesis in the inflammatory region. When prescribed in high doses, long-term use and individual characteristics of the body, selectivity for COX-2 decreases.

Inhibits prostaglandin synthesis in the area of inflammation to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2. Less often causes erosive and ulcerative diseases of the gastrointestinal tract. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandins that protect the gastrointestinal mucosa and take part in the regulation of blood flow in the kidneys.

Pharmacokinetics

Suction

After oral use, meloxicam is well absorbed from the gastrointestinal tract, with an absolute bioavailability of 89%. Simultaneous intake with food does not change the absorption. The concentration of meloxicam when taking the drug orally at doses of 7.5 and 15 mg is proportional to the dose.

After intravenous use, 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 demonstrates linear pharmacokinetics at doses of 7.5-15 mg when administered intravenously.

Css distribution is achieved within 3-5 days of regular admission. With prolonged use of the drug (more than 1 year), the concentrations are similar to those observed after the first achievement of a stable state of pharmacokinetics. Binding to plasma proteins (especially albumin) is more than 99%.

The range of differences between the maximum and basal concentrations of the drug after taking it 1 time/day is relatively small and amounts to 0.4-1 mcg / ml when using a dose of 7.5 mg, and 0.8-2 mcg/ml when using a dose of 15 mg (Cmin and Cmax values are shown, respectively).

Meloxicam penetrates through histohematic barriers, the concentration in synovial fluid reaches 50% of the maximum concentration of the drug in plasma.

The Vd is low and is 11 liters. Interindividual differences are 30-40%.

Metabolism

Meloxicam is almost completely metabolized in the liver to form four pharmacologically inactive metabolites. The main metabolite of 5 ‘- carboxymeloxicam (60% of the dose) is formed by oxidation of the intermediate metabolite 5’ – hydroxymethylmeloxicam, which is also excreted, but 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 plays an additional role. 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.

Deduction

It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted unchanged through the intestines, and only trace amounts of the drug are detected unchanged in the urine. T1 / 2 of meloxicam after oral use is 15-20 hours, with intramuscular use-20 hours. Plasma clearance averages 8 ml / min

. Pharmacokinetics in special clinical cases

In the elderly, the clearance of the drug decreases.

Moderate hepatic or renal insufficiency does not significantly affect the pharmacokinetics of meloxicam.

Indications

Symptomatic therapy:

— osteoarthritis

— – rheumatoid arthritis;

– ankylosing spondylitis (Ankylosing spondylitis).

Contraindications

— status after conducting 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 of acetylsalicylic acid and other NSAIDs (including in the anamnesis);

— erosive and ulcerative changes in the mucous membrane of the stomach or duodenal ulcers, active gastrointestinal bleeding;

— inflammatory bowel disease (ulcerative colitis, Crohn’s disease);

— cerebrovascular bleeding or other bleeding;

— severe hepatic impairment or active liver disease;

— chronic renal failure in patients not undergoing dialysis (KK less than 30 ml/min), progressive kidney disease (including confirmed hyperkalemia);

— children’s age up to 12 years (for tablets);

— children’s age up to 18 years (for a solution for the/m introduction);

— pregnancy;

— lactation (breastfeeding);

— hypersensitivity to meloxicam and other components of the drug.

The drug contains lactose in tablet form, so patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug.

With carefully

— CHD;

— cerebrovascular disease;

— compensated heart failure;

— dyslipidemia/hyperlipidemia;

diabetes mellitus;

diseases of peripheral arteries;

— Smoking;

— KK 30-60 ml/min;

anamnestic information about the development of ulcerative lesions of the gastrointestinal tract;

— the presence of infection Helicobacter pylori;

old age;

— prolonged use of NSAIDs;

— frequent use of alcohol;

— severe somatic diseases;

— concomitant therapy with the following drugs:  anticoagulants (e. g., warfarin); antiplatelet agents (e. g., acetylsalicylic acid, clopidogrel); oral corticosteroids (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” hepatic ” transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, gastrointestinal bleeding (including hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis. From the hematopoietic system:  more than 1% – anemia; 0.1-1% – changes in the blood formula, including leukopenia, thrombocytopenia. From the side of 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. Respiratory system disorders:  less than 0.1% – bronchospasm. Central nervous system (CNS)disorders:  more than 1% – dizziness, headache; 0.1-1% – vertigo, tinnitus, drowsiness; less than 0.1% – confusion, disorientation, emotional lability. From the cardiovascular system (CVS):  more than 1% – peripheral edema; 0.1-1% – increased blood pressure( BP), 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 side of the senses:  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

When taken concomitantly with other NSAIDs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

When used concomitantly with antihypertensive drugs, the effectiveness of the latter may decrease. When used concomitantly with lithium preparations, it is possible to develop lithium accumulation and increase its toxic effect (monitoring of lithium concentration in the blood is recommended).

When used concomitantly with methotrexate, the side effect of the latter on the hematopoietic system increases (the risk of anemia and leukopenia, periodic monitoring of the general blood test is indicated).

Concomitant use with diuretics and cyclosporine increases the risk of developing renal failure. When used simultaneously with intrauterine contraceptives, the effectiveness of the latter may decrease.

When used concomitantly 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 clotting parameters is necessary).

Concomitant use with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

How to take it, course of use and dosage

Intramuscularly.Intramuscular use of Movasin is indicated only for 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 injections 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 tablets, suppositories 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: no specific antidote; symptomatic therapy. Forced diuresis, urine alkalinization, and hemodialysis are 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 gastric and duodenal ulcers, as well as in patients undergoing anticoagulant therapy. Such patients have an increased risk of erosive and ulcerative diseases of the gastrointestinal tract.

Caution should be exercised and renal function parameters monitored when using the drug 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 creatinine clearance exceeds 30 ml/min, no dosage adjustment is required. In patients undergoing 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 (pruritus, skin rash, urticaria, photosensitization) occur during treatment, you should consult a doctor to decide whether to stop taking 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, can affect fertility, so it is not recommended for women planning pregnancy.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 30 ° C.

Shelf life

3 years

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection