Composition
Active ingredient: Â meloxicam;
Excipients:
Pregelatinized starch (starch 1500);
MCC;
Sodium Citrate dihydra;
Colloidal silicon dioxide (aerosil 380);
Magnesium stearate
Pharmacological action
Pharmaceutical Group:
NSAIDs.
Pharmaceutical action: Â
NSAIDs have anti-inflammatory, antipyretic, and analgesic effects. Belongs to the class of oxycams; a derivative of enolic acid.
The mechanism of action is inhibition of Pg synthesis as a result of selective suppression of COX-2 enzymatic activity. When prescribed in high doses, long-term use and individual characteristics of the body, COX 2 selectivity decreases. Inhibits Pg synthesis in the inflammatory region to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2. It is less likely to cause erosive and ulcerative diseases
of the gastrointestinal tract. :
Absorption from the gastrointestinal tract after oral or rectal use is 89%; tablets and suppositories are bioequivalent. Food intake does not affect absorption. The plasma concentration is dose-dependent. TCmax – 5-6 hours. Css is created in 3-5 days. Binding to plasma proteins is 99%. Passes through histohematic barriers, penetrates synovial fluid. The synovial fluid concentration is 50% of the plasma concentration. Metabolism in the liver – to inactive metabolites.
It is excreted through the intestines and kidneys (in approximately equal proportions), unchanged – 5% of the daily dose (through the intestines). T1 / 2-20 hours Plasma clearance is on average 8 ml / min (decreases in the elderly).
Indications
Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis (Ankylosing spondylitis) and other inflammatory and degenerative joint diseases accompanied by pain syndrome.
It is intended for symptomatic therapy, reducing pain and inflammation at the time of use; it does not affect the progression of the disease.
Use during pregnancy and lactation
The drug is not recommended for use during pregnancy and lactation.
Contraindications
Hypersensitivity (including to other NSAIDs), the “aspirin” triad (a combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, and intolerance to acetylsalicylic acid and pyrazolone-type drugs), acute gastric and duodenal ulcers; gastrointestinal, cerebrovascular or other bleeding; severe heart failure, severe hepatic insufficiency, severe renal failure (if hemodialysis is not performed), pregnancy, breast-feeding, age up to 15 years.
Side effects
From the digestive tract: Â dyspepsia, nausea, vomiting, abdominal pain, constipation/diarrhea, flatulence; stomatitis, transient changes in liver function indicators (increased transaminases or bilirubin), belching, esophagitis, stomach and duodenal ulcers, hidden or macroscopically visible gastrointestinal bleeding;
Nervous system and sensory disorders: Â headache, dizziness; vertigo, drowsiness, tinnitus;
Cardiovascular and blood disorders (hematopoiesis, hemostasis): Â edema, anemia; increased blood pressure, palpitations, flushes of blood to the face, changes in the hemogram, including changes in the number of individual types of white blood cells, leukopenia, thrombocytopenia.
Respiratory system disorders: Â exacerbation of bronchial asthma, cough.
From the genitourinary system: Â changes in renal function indicators (increased blood creatinine and/or urea levels);
From the side of the skin: Â skin rash, pruritus; urticaria;
Interaction
When used concomitantly with acetylsalicylic acid and other NSAIDs, the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. When used concomitantly with antihypertensive agents, the effectiveness of the latter may decrease.
When used concomitantly with lithium preparations, lithium can accumulate and increase its toxic effect (monitoring of lithium concentration in the blood is recommended).
Simultaneous use with methotrexate increases the side effect of the latter on the hematopoietic system (there is a risk of anemia and leukopenia. Periodic monitoring of a general blood test is required). 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), as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (blood clotting parameters should be periodically monitored).
Simultaneous use with colestyramine increases the elimination of meloxicam through the gastrointestinal tract (as a result of meloxicam binding). No pharmacokinetic interaction was observed when meloxicam was co-administered with antacids.
How to take, course of use and dosage
Meloxicam is taken orally, with meals, without chewing, at a dose of 7.5-15 mg 1 time a day.
The dose is selected individually, and the lowest effective dose should be used for a minimum period of time.
Overdose
Symptoms:
Increased side effects.
Treatment:
Gastric lavage, taking activated charcoal (within the next hour), symptomatic therapy. Colestyramine accelerates the elimination of the drug from the body. Forced diuresis, urine alkalinization, and hemodialysis are ineffective due to the high binding of meloxicam to blood proteins. No specific antidotes or antagonists were found.
Special instructions
If an ulcer or gastrointestinal bleeding occurs, Meloxicam should be discontinued.
Caution should be exercised when prescribing Meloxicam to elderly patients who are more likely to have impaired renal, liver, and heart function.
The drug in the form of candles should not be used for hemorrhoids.
With the development of side effects such as dizziness and drowsiness, it is recommended to refrain from driving a car and other potentially dangerous activities that require an increased speed of mental and motor reactions.
Composition
Tablet Form of production
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C
Shelf life
2 years
Active ingredient
Meloxicam
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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