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Meloxicam is a nonsteroidal anti-inflammatory agent. Selective inhibition of the isoenzyme cyclooxygenase-2 provides anti-inflammatory and analgesic effects of the drug. For Meloxicam selectivity coefficient IS is 2. Absorbed in the alimentary canal almost completely. Internally, the percent absolute bioavailability is approximately 89. After 5-6 hours after administration orally (once) reached the maximum concentration of the active substance blood plasma. After 3-5 days of regular re-administration of the drug is achieved the equilibrium state.
Equilibrium concentration of Meloxicam (Withmy–Cmax) is 0.4–1.0 mg/l while receiving 7.5 mg of the drug inside and 0.8–2.0 mg/l, with the admission of 15 mg orally. The maximum concentrations are not changed when using for a long time. Simultaneous intake of food does not affect extent of absorption of Meloxicam from the digestive system. After intramuscular injection parameter bioavailability is 89%, and after 60 minutes in the blood plasma maximum concentration of the active substance. Linear pharmacokinetics characterized by when taking Meloxicam in sredneterapevticheskih doses of 7.5 mg and 15 mg.
The affinity of Meloxicam with large plasma proteins, particularly albumin – to 99%. 50% from the plasma concentration of Meloxicam was observed in the synovial fluid. The volume of distribution averaged 11 l with the limits of individual variations between 30 and 40%. Metabolized by hepatic enzymes. Eliminated by the kidneys and the gut in equal measure, and urine in a single 4 pharmacologically inactive metabolite of the drug. 5’-carboxymethoxy is the main metabolite. It is up to 60% of the administered or the dose and is formed by the oxidation of intermediate metabolic forms (for example, 5’-hydroxymethyluracil). In unaltered 9% 5’-hydroxymethyluracil.
In vitro studies have shown that the first phase of metabolic transformation is carried out mainly by CYP 2C9 isoenzyme. However, to a small extent involved in the process and CYP 3A4. Other metabolites ranged from 4 to 16% of adopted or entered and Meloxicam are formed by exposure to peroxidase. Unmodified Meloxicam is found in urine in trace concentrations. The half-life is determined on average within 20 hours. Total plasma clearance of active substance is approximately 8 ml/min.
Indications for use.
Meloxicam is used as a symptomatic agent in the treatment of:
– Exacerbations of osteoarthritis (short-term);
– chronic polyarthritis (long time);
– rheumatoid arthritis (a long time);
– Bekhterev’s disease (ankylosing spondylitis).
Method of application:
Tablets Meloxicam take 1 time a day, during meals. Pill Meloxicam need to drink 250 ml of liquid. Solution for injection Meloxicam is intended solely for incorporation into the muscle. Contraindicated intravenous use solution. Intramuscular use in the first days of therapy. In a further move to the inside the use of the drug in tablet form.
During exacerbation of osteoarthritis administered 7.5 mg 1 time a day. You can increase the dosage to 15 mg if the therapeutic effect is insufficient.
With ankylosing spondylitis and rheumatoid arthritis – on 15 mg of 1 times a day. If there is a sufficient therapeutic effect, the daily dose reduced to 7.5 mg once a day. Do not exceed recommended dosage Meloxicam 15 mg per day.
Treatment special categories of patients.
For dialysis patients, a daily dose not higher than 7.5 mg. At insufficiency of renal function the daily dose of Meloxicam is 7.5 mg. Can reduce the dosage of the drug, if creatinine clearance is 25 ml/min and above (medium or mild renal function).
For elderly patients with Bechterew’s disease or rheumatoid arthritis need long-term treatment recommended daily dosage is 7.5 mg. If there is a need for higher doses, but there is a risk of undesirable side effects, limited to a daily dose of 7.5 mg.
You do not want to reduce the dosage, if a patient is diagnosed with secondary or slight decrease of liver function.