FAMELLO [Meloxicam] 15 mg Solution for intramuscular injection

FAMELLO

instructions for medical use of the medicinal product

Tradename

Famello, Фамелло

International non-proprietary name

Meloxicam , Мелоксикам

Composition

Each ampoule (1.5 ml solution) contains:

active substance: meloxicam BP 15 mg

excipients: glucoamine, propylene glycol, anhydrous sodium sulfite, activated charcoal, water for injection.

Dosage form

Solution for injection .

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drugs ( NSAIDs) . Oxycams.

Pharmacological properties

Famello is a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. Active ingredient - meloxicam

Pharmacodynamics

Meloxicam belongs to the class of oxicams, derivatives of enolic acid. The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2, which is involved in the biosynthesis of prostaglandins in the area of inflammation. To a lesser extent, meloxicam acts on cyclooxygenase-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

Meloxicam is completely absorbed after intramuscular administration. The relative bioavailability compared to the oral route of administration is almost 100%. In this regard, there is no need to adjust the dose of the drug when switching from intramuscular to oral administration. Peak plasma concentrations after intramuscular injection of 15 mg of the drug were reached after 1-6 hours and were about 1.6-1.8 μg / ml.

Meloxicam binds well to plasma proteins, mainly to albumin (99%). Meloxicam penetrates into the synovial fluid, reaching a concentration corresponding to approximately 50% of the plasma concentration.

The volume of distribution is low, approximately 11 liters after intramuscular administration, with an interindividual variation coefficient of about 7-20%.

Meloxicam is extensively metabolized in the liver. Four different pharmacodynamically inactive metabolites of meloxicam have been identified in urine. The main metabolite, 5-carboxymeloxicam (60% of the administered dose), is formed by oxidation of the intermediate metabolite 5-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the administered dose). In vitro studies have shown that CYP 2C9 plays an important role in this metabolic transformation, and the CYP 3A4 isoenzyme is of additional importance. The activity of peroxidase in the patient's body probably causes the appearance of two other metabolites, which account for 16% and 4%, respectively, of the administered dose.

It is excreted equally with feces and urine, mainly in the form of metabolites. Less than 5% of the daily dose is excreted unchanged in the feces; in the urine, unchanged, the drug is found only in trace amounts. The mean elimination half-life of meloxicam is 20 hours. Plasma clearance averages 8 ml/min.

Indications for use

Symptomatic treatment of osteoarthritis (arthrosis, degenerative joint diseases), rheumatoid arthritis, ankylosing spondylitis, other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathy, dorsopathy (for example, sciatica, lower back pain, shoulder periarthritis, and others), accompanied by pain .

Contraindications

·          hypersensitivity to meloxicam;

·          complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs due to the existing likelihood of cross-sensitivity (including history);

·          erosive and ulcerative changes in the mucous membrane of the stomach and duodenum in the acute stage or recently transferred;

·          inflammatory bowel disease - Crohn's disease or ulcerative colitis in the acute stage;

·          active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of diseases of the blood coagulation system;

·          severe liver failure;

·          severe renal failure;

·          severe uncontrolled heart failure;

·          concomitant therapy with anticoagulants, as there is a risk of intramuscular hematomas;

·          pregnancy;

·          breastfeeding period;

·          age up to 18 years.

Dosage and administration

The drug is administered by deep intramuscular injection.

Depending on the degree of pain and inflammation, the recommended dose is 7.5 mg or 15 mg 1 time per day.

General recommendations

Since the potential risk of adverse reactions depends on the dose and duration of treatment, the lowest possible dose and duration of use should be used.

The maximum recommended daily dose is 15 mg.

The drug should not be administered intravenously.

Combined application

Do not use the drug simultaneously with other NSAIDs.

The total daily dose of the drug Famello, used in the form of different dosage forms, should not exceed 15 mg.

Intramuscular administration of the drug is indicated only during the first few days of therapy. In the future, treatment is continued with the use of oral dosage forms. The recommended dose is 7.5 mg or 15 mg 1 time per day, depending on the intensity of pain and the severity of the inflammatory process.

Given the possible incompatibility, the drug should not be mixed in the same syringe with other drugs.

Special instructions and precautions

Use with caution in diseases of the upper gastrointestinal tract in history, in combination with anticoagulants, myelotoxic drugs, incl. methotrexate (possible cytopenia). The occurrence of gastroduodenal ulcers, gastrointestinal bleeding, side effects from the skin and mucous membranes serve as the basis for discontinuing the drug. If allergic reactions occur during treatment (itching, skin rash, urticaria, photosensitivity), you should consult a doctor to decide whether to stop taking the drug.

risk of gastrointestinal complications. Serious gastrointestinal side effects, including inflammation, bleeding, ulceration, and perforation of the stomach or intestines, may occur at any time during the use of NSAIDs without warning symptoms. Elderly patients have a higher risk of serious complications from the gastrointestinal tract , the likelihood of these complications also increases with prolonged use.

Meloxicam, like other NSAIDs , may mask the symptoms of infectious diseases.

The appointment of NSAIDs to patients with reduced renal blood flow and BCC can accelerate kidney decompensation (after discontinuation of NSAID therapy, kidney function is usually restored to its previous level). The risk of developing such reactions is especially high in patients with symptoms of dehydration, congestive heart failure, cirrhosis of the liver, nephrotic syndrome and severe kidney disease, in patients receiving diuretics, as well as in those who have undergone significant surgery that led to hypovolemia (careful monitoring is necessary from the start of treatment). diuresis and kidney function). In rare cases, NSAIDs can cause interstitial nephritis, glomerulonephritis, renal medulla necrosis, or nephrotic syndrome. With a significant deviation from the norm of the level of serum transaminases and other indicators characterizing liver function, you should stop taking it and conduct control laboratory tests. Be wary appoint elderly, debilitated and malnourished patients.

Influence on the ability to drive vehicles and mechanisms

The use of Famello may cause such undesirable effects as headache and dizziness, drowsiness. In this regard, it is necessary to abandon the management of vehicles, maintenance of machines and mechanisms and other activities that require increased concentration of attention.

Use during pregnancy and during breastfeeding

Use during pregnancy and during breastfeeding is contraindicated.

Interaction with other drugs

With simultaneous use:

with other non-steroidal anti-inflammatory drugs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding of the gastrointestinal tract increases,

with antihypertensive drugs, it is possible to reduce the effectiveness of the latter,

with lithium preparations, lithium accumulation and an increase in its toxic effect are possible (it is recommended to control the concentration of lithium in the blood),

with methotrexate, the side effect of the latter on the hematopoietic system increases (the risk of anemia and leukopenia, periodic monitoring of a complete blood count is indicated),

with diuretics and with cyclosporine, the risk of developing renal failure increases,

with intrauterine contraceptives, it is possible to reduce the effectiveness of the latter,

with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring of blood clotting is necessary),

with cholestyramine, as a result of the binding of meloxicam, its excretion through the gastrointestinal tract is enhanced,

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

Side effect

From the digestive system: more than 1% - dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea. 0. 1-1% - a transient increase in the activity of "liver" transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including latent), stomatitis. less than 0. 1% - perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.

On the part of the hematopoietic organs: more than 1% - anemia. 0. 1-1% - a change in the blood count, including leukopenia, thrombocytopenia.

For the skin: more than 1% - itching, skin rash. 0. 1-1% - urticaria. less than 0. 1% - photosensitivity, bullous rashes, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

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

From the 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, palpitations, "flushing" 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. connection with taking meloxicam has not been established - interstitial nephritis, albuminuria, hematuria.

From the sensory organs: less than 0.1% - conjunctivitis, visual impairment, including blurred vision.