Movasin solution 10mg/ml 1.5ml ampoules, 3pcs

Composition

1 ml contains meloxicam-10 mg,

excipients:

sodium chloride,

glycine,

glycofurfural (tetraglycol),

poloxamer 188,

meglumine (meglumine),

sodium hydroxide,

water for injection.

Pharmacological action

Pharmaceutical Group:

NSAIDs.

Pharmaceutical action:  

Movasin is an NSAID that has anti-inflammatory, antipyretic, and analgesic effects. Belongs to the class of oxycams; a derivative of enolic acid.

Meloxicam is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects.

The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in the biosynthesis of prostaglandins 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 mucous membrane of the gastrointestinal tract (GIT) and is involved in the regulation of blood flow in the kidneys.

Pharmacokinetics:  

The relative bioavailability is almost 100%. After intramuscular use of the drug at a dose of 5 mg, the maximum concentration (Cmax) is 1.62 mcg / ml and is reached within approximately 60 minutes. Meloxicam binds well to plasma proteins, especially albumin (99%). Penetrates the synovial fluid, the concentration in the synovial fluid is approximately 50% of the plasma concentration. The volume of distribution (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,5′ – carboxymeloxicam (60% of the dose), is formed by the oxidation of an intermediate metabolite,5′ – hydroxy-methylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose). In vitro studies have shown that the SUR2C9 isoenzyme plays an important role in this metabolic transformation, while the SUR3A4 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.

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

Meloxicam demonstrates linear pharmacokinetics at doses of 7.5-15 mg when administered intramuscularly. Moderate hepatic or renal insufficiency does not significantly affect the pharmacokinetics of meloxicam.

Indications

• Symptomatic treatment of rheumatoid arthritis
• Symptomatic treatment of osteoarthritis; 
• Symptomatic treatment of ankylosing spondylitis (ankylosing spondylitis).

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 kitty-and lots of other nonsteroidal anti-inflammatory drugs (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 insufficiency in patients not undergoing dialysis (creatinine clearance (CC) of less than 30 ml/min), progressive kidney diseases including confirmed hyperkalemia;
• pregnancy, lactation;
• children up to age 18 years.

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, 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.

Form of production

Solution for intramuscular use.

Storage conditions

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

Shelf

life is 3 years.

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection