FAMELLO [Meloxicam] 15 mg Film-coated tablets
FAMELLO
instructions for medical use of the medicinal product
Tradename
Famello, Фамелло
International non-proprietary name
Meloxicam , Мелоксикам
Composition
Each film-coated tablet contains:
active ingredient: meloxicam USP 15 mg
excipients: mannitol, granulated mannitol, sorbitol, povidone, anhydrous citric acid, aspartame, talc, magnesium stearate, povidone K30, sodium lauryl sulfate.
Dosage form
Tablets.
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
Well absorbed from the gastrointestinal tract (GIT), the absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not change absorption. When using the drug inside in doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Equilibrium concentration is reached within 3-5 days. With prolonged use of the drug (more than 1 year), the concentrations are similar to those observed after the first achievement of a steady state of pharmacokinetics. Plasma protein binding is over 99%. The range of differences between the maximum and basal concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-1.0 mcg / ml when using a dose of 7.5 mg, and 0.8-2.0 mcg / ml when using a dose of 15 mg, (given, respectively, C min and C max values). Meloxicam penetrates through histohematic barriers, the concentration in the synovial fluid reaches 50% Cmax of the drug in plasma. Almost completely metabolized in the liver with the formation of four pharmacologically inactive derivatives. The main metabolite, 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 CYP2C9 plays an important role in this metabolic transformation, and the CYP3A4 isoenzyme is of additional importance. In the formation of two other metabolites (constituting, respectively, 16% and 4% of the dose of the drug), peroxidase takes part, the activity of which, probably, varies individually. Excreted equally through the intestines and kidneys, mainly in the form of metabolites. Less than 5% of the daily dose is excreted through the intestine unchanged; in the urine, unchanged, the drug is found only in trace amounts. T 1/2 meloxicam is 15-20 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
inside. Tablets should be swallowed whole, without chewing, with a sufficient amount of liquid during meals in a daily dose of 7.5-15 mg.
Recommended dosing regimen:
Rheumatoid arthritis: 15 mg per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.
Osteoarthritis: 7.5 mg per day. With inefficiency, the dose can be increased to 15 mg per day.
Ankylosing spondylitis: 15 mg per day.
The maximum daily dose should not exceed 15 mg.
In patients with an increased risk of side effects, as well as in patients with severe renal insufficiency on hemodialysis, the dose should not exceed 7.5 mg per day.
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
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.
Allergic reactions: less than 0.1% - angioedema, anaphylactoid / anaphylactic reactions.
Overdose
Symptoms: nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, drowsiness, changes in blood pressure, convulsions, cardiovascular collapse, cardiac arrest, anaphylactoid reactions.
Treatment: There is no specific antidote. In case of an overdose of the drug, symptomatic therapy should be carried out.
Storage conditions
Store in a cool and dry place, at a temperature not exceeding 30º C.
Store in