Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
NSAIDs, selective inhibitor of COX-2. It belongs to the class of oxyocams, it is a derivative of enolic acid. Has anti-inflammatory, analgesic and antipyretic effect. The mechanism of action is associated with a decrease in the biosynthesis of prostaglandins as a result of inhibition of the enzymatic activity of COX. In this case, meloxicam more actively affects COX-2, which is involved in the synthesis of prostaglandins in the inflammation focus, which reduces the risk of side effects on the upper GI tracts and slightly affects COX-1.
At the same time, meloxicam does not affect the synthesis of proteoglycan by the chondrocytes of articular cartilage, it does not affect the development of spontaneous arthrosis in rats and mice, which indicates its chondrojetrality.
PHARMACOKINETICS
After oral administration or rectal administration, the absorption of meloxicam from the digestive tract is 89%. Eating does not affect the absorption of meloxicam.
The concentration in the plasma depends on the dose. Plateau concentration in plasma is achieved by 3-5 days. With prolonged use (more than 1 year), there is no increase in plasma concentration in comparison with the level reached when reaching the plateau. In plasma 99% of meloxicam is in protein conjugated form.Fluctuations in meloxicam concentration when taken 1 time / day are small and are within 0.4-1 Ојg / ml for a dose of 7.5 mg and 0.8-2 Ојg / ml for a dose of 15 mg.
The concentration of meloxicam in the synovial fluid is 50% of the concentration in the blood plasma.
Meloksikam is almost completely metabolized to inactive metabolites.
T 1/2 meloxicam is 20 hours. The plasma clearance is an average of 8 ml / min. Meloksikam is excreted by the kidneys and through the intestine in approximately equal proportions.
Hepatic and renal failure of mild to moderate severity does not significantly affect the pharmacokinetic parameters of meloxicam.
INDICATIONS
Inflammatory and degenerative joint diseases (arthrosis, osteoarthritis), rheumatoid arthritis, Bechterew's disease (ankylosing spondylitis).
DOSING MODE
Inside for 7.5-15 mg 1 time / day. The maximum daily dose is 15 mg.
External apply 2 times / day. Apply a thin layer on a clean dry skin over the lesion and lightly rub for 2-3 minutes.
SIDE EFFECT
From the digestive system: dyspepsia, nausea, vomiting, abdominal pain, constipation, intestinal colic, diarrhea, esophagitis, stomatitis; rarely - erosive-ulcerative lesions of the gastrointestinal tract.
From the side of the central nervous system: dizziness, headache, tinnitus.
From the side of the cardiovascular system: increased blood pressure, palpitations, swelling, hot flashes.
From the side of the urinary system: changes in laboratory parameters of kidney function.
On the part of the hematopoiesis system: anemia, leukopenia, thrombocytopenia.
Allergic reactions: bronchospasm, photosensitivity, itching, rash, urticaria.
CONTRAINDICATIONS
Peptic ulcer disease in the stomach and duodenal ulcers in the exacerbation phase, expressed violations of the liver, renal failure (without hemodialysis), pregnancy, children and adolescents under 15 years, hypersensitivity to meloxicam and other NSAIDs (including salicylates).
PREGNANCY AND LACTATION
Contraindicated in pregnancy.
If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.
In experimental studies, there was no teratogenic effect of meloxicam.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in renal failure (without hemodialysis).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 15 years.
SPECIAL INSTRUCTIONS
Use with caution in patients with a history of gastrointestinal disease.
DRUG INTERACTION
With simultaneous use, it is possible to reduce the effectiveness of antihypertensive drugs (beta-adrenoblockers, ACE inhibitors, vasodilators).
With simultaneous use with anticoagulants, the risk of bleeding increases.
With simultaneous use with diuretics, the risk of developing kidney failure in patients in a state of dehydration increases.
With simultaneous use with NSAIDs, the risk of ulcerative gastrointestinal lesions and gastrointestinal bleeding increases.
With simultaneous use with lithium preparations, the concentration of lithium in the blood plasma increases.
With the simultaneous application of colestramine, accelerates the excretion of meloxicam.
With simultaneous use with methotrexate, it is possible to enhance myelodepressive action; with cyclosporine - it is possible to enhance the nephrotoxic effect of cyclosporine.
