Movasin, 10 mg/ml 1.5 ml 3 pcs.

Pharmgroup:

NSAIDs.

Pharmic action:

Movasin – NSAID, has anti-inflammatory, antipyretic, analgesic action. It belongs to the class of oxycams; a derivative of enolic acid.

Meloxicam is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic effects.

The anti-inflammatory action is due to the inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the area of inflammation.

To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandin, which protects the mucosa 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 administration of the drug at a dose of 5 mg, the maximum concentration (Cmax) is 1.62 mcg/ml and is reached within approximately 60 min. Meloxicam binds well to plasma proteins, especially to albumin (99%). It 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 L. Interindividual variation is 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 value), is formed by oxidation of the intermediate metabolite, 5′-hydroxy-methylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose value). In vitro studies have shown that CYP2C9 isoenzyme plays an important role in this metabolic transformation, isoenzyme CYP3A4 has additional importance. Peroxidase, the activity of which probably varies individually, is involved in the formation of the other two metabolites (which constitute, respectively, 16% and 4% of the drug dose).

Extracted equally in the feces and urine, mainly as metabolites. Less than 5% of daily dose is excreted unchanged in the feces, the drug is excreted unchanged in the urine only in trace amounts. Mean elimination half-life (T½) is 20 hours. Plasma clearance averages 8 ml/min.

Meloxicam exhibits linear pharmacokinetics at doses of 7.5-15 mg when administered intramuscularly.
Moderate hepatic or renal insufficiency has no significant effect on the pharmacokinetics of meloxicam.

Indications

Symptomatic treatment of rheumatoid arthritis
Symptomatic treatment of osteoarthritis;
Symptomatic treatment of ankylosing spondylitis (Bechterew’s disease).

Pharmacological effect

Pharmgroup:

NSAIDs.

Pharmaceutical action:

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

Meloxicam is a non-steroidal 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), which is involved in the biosynthesis of prostaglandins in the area of ​​inflammation.

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 takes part in the regulation of blood flow in the kidneys.

Pharmacokinetics:

Relative bioavailability is almost 100%. After intramuscular administration of the drug at a dose of 5 mg, the maximum concentration (Cmax) is 1.62 μg/ml and is achieved within approximately 60 minutes. Meloxicam binds well to plasma proteins, especially albumin (99%). Penetrates into synovial fluid, the concentration in synovial fluid is approximately 50% of the concentration in plasma. 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 oxidation of the 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 CYP2C9 isoenzyme plays an important role in this metabolic transformation; the CYP3A4 isoenzyme is of additional importance. Peroxidase is involved in the formation of the other two metabolites (constituting, respectively, 16% and 4% of the drug dose), the activity of which probably varies individually.

It is excreted equally in feces and urine, mainly in the form of metabolites. In unchanged form, less than 5% of the daily dose is excreted in feces; in urine, unchanged, the drug is found only in trace amounts. The average half-life (T½) is 20 hours. Plasma clearance averages 8 ml/min.

Meloxicam exhibits linear pharmacokinetics in doses of 7.5-15 mg when administered intramuscularly.
Moderate hepatic or renal failure does not significantly affect the pharmacokinetics of meloxicam.

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 on anticoagulant therapy. Such patients have an increased risk of erosive and ulcerative diseases of the gastrointestinal tract.

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

In patients with renal failure, if CC is more than 30 ml/min, no dosage adjustment is required.
In patients on dialysis, the dosage of the drug should not exceed 7.5 mg/day.

Patients taking diuretics and meloxicam simultaneously should take sufficient fluids.

If allergic reactions occur during treatment (itching, skin rash, urticaria, photosensitivity), you must 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, like other drugs that block prostaglandin synthesis, can affect fertility and is therefore not recommended for women planning pregnancy.

Active ingredient

Meloxicam

Composition

1 ml contains meloxicam – 10 mg,

excipients:

sodium chloride,

glycine,

glycofurfural (tetraglycol),

poloxamer 188,

meglumine (meglumine),

sodium hydroxide,

water for injections.

Contraindications

hypersensitivity to the active substance or auxiliary components;
contraindicated in the period after 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 to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (NSAIDs) (including a history);
erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding;
exacerbation of inflammatory bowel diseases (nonspecific ulcerative colitis, Crohn’s disease);
cerebrovascular bleeding or other bleeding;
severe liver failure or active liver disease;
severe renal failure in patients not undergoing dialysis (creatinine clearance (CC) less than 30 ml/min), progressive kidney disease, incl. confirmed hyperkalemia;
pregnancy, breastfeeding period;
children under 18 years of age.

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, belching, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis.

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

From the skin: more than 1% – itching, skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitivity, bullous rashes, 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 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 urea in the blood serum; less than 0.1% – acute renal failure; no connection with meloxicam has been established – interstitial nephritis, albuminuria, hematuria.

From the senses: 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% – pain at the injection site

Interaction

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

When used simultaneously with antihypertensive drugs, the effectiveness of the latter may be reduced.
When used simultaneously with lithium preparations, the development of accumulation of lithium and an increase in its toxic effect are possible (monitoring the concentration of lithium in the blood is recommended).

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

When used simultaneously with diuretics and cyclosporine, the risk of developing renal failure increases.

When used simultaneously with intrauterine contraceptives, the effectiveness of the latter may decrease.

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 clotting parameters is necessary).

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

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, alkalization of urine, hemodialysis are ineffective due to the high binding of the drug to blood proteins.

Storage conditions

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

Shelf life

3 years.

Manufacturer

Sintez, Russia