The anti-inflammatory action due to inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2) involved in the biosynthesis of prostaglandins in inflammation. To a lesser extent meloxicam effect on cyclooxygenase-1 (COX-1) participating in the synthesis of prostaglandins which protect the mucosa of the gastrointestinal tract, and taking part in the regulation of renal blood flow. Suspension testosteronewell absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam – 89 %. Simultaneous food intake does not modify absorption. When using the drug orally in doses of 7.5 and 15 mg doses are proportional to its concentration. Equilibrium concentration is achieved in 3-5 days. With long-term use (more than 1 year), the concentrations are similar to those that have been observed after the first reach a steady state pharmacokinetics. Plasma protein binding is more than 99%. The range difference between the maximum and basal concentrations of the drug after administration once a day is relatively small and is at a dose of 7.5 mg 0.4-1.0 mg / ml, and at a dose of 15 mg – 0.8-2, 0 mg / mL (shown, respectively, the values Cmin and Cmax). Meloxicam penetrates the blood-tissue barriers in the synovial fluid concentration reaches 50% of the maximum drug concentration in plasma. Almost completely metabolized in the liver to form four pharmacologically inactive derivatives. The main metabolite, 5′-karboksimeloksikam (60% of the dose), formed by oxidation of an intermediate metabolite 5′-gidroksimetilmeloksikama which is also excreted, but to a lesser extent (9% of the dose). Studies in vitro have shown that the metabolic conversion plays an important role CYP 2C9, additional importance isoenzyme CYP 3A4.The formation of two other metabolites (components, respectively, 16% and 4% of the dose) participates peroxidase, which activity is likely to vary individually.Deduced equally with feces and urine, mainly as metabolites. Since feces in unchanged output of less than 5% of the daily dose in the urine as unchanged drug is found only in trace amounts. The half-life (T1 / 2) of meloxicam is 15-20 hours. Plasma clearance averages of 8 ml / min. Elderly persons drug clearance is reduced. The volume of distribution is low, with an average of 11 liters. Hepatic or renal insufficiency of moderate severity substantially significant effect on the pharmacokinetics of meloxicam has not.
Symptomatic treatment of osteoarthritis;
- Symptomatic treatment of rheumatoid arthritis;
- Symptomatic treatment of ankylosing spondylitis (ankylosing spondylitis).Contraindications
- hypersensitivity to any component of the drug; aspirin-induced asthma;
- aggravation of gastric ulcer and duodenal ulcer; severe renal failure (unless hemodialysis);
- severe hepatic impairment;
- Children under the age of 15 years; pregnancy;
The drug should be used with caution in elderly patients. Erosive and ulcerative lesions of the gastrointestinal tract in history.
Dosing and Administration
The drug is taken orally during a meal once a day.
The recommended dosing regimen:
- Rheumatoid Arthritis: 15 mg. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.
- Osteoarthritis: 7.5 mg. With the ineffectiveness of the dose may be increased to 15 mg per day.
Ankylosing spondylarthritis: 15 mg per day. The maximum daily dose should not exceed 15 mg.
In patients with an suspension testosterone increased risk of side effects, as well as in patients with severe renal impairment on hemodialysis, the dose should not exceed 7.5 mg per day.Pregnancy and lactation
The drug is not recommended for use during pregnancy and lactation.
Side effects Bodies of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions of the gastrointestinal tract, perforation of the stomach or intestines, gastrointestinal bleeding (implicit or explicit), increased activity of “liver” enzymes, hepatitis, colitis, stomatitis, dry mouth, esophagitis. Cardiovascular system: tachycardia, increased blood pressure, a sense of “tide”. Respiratory system: exacerbation of asthma, cough. Central nervous system: headache, dizziness, tinnitus, disorientation, confusion thoughts, sleep disturbance. Urogenital system: edema, interstitial nephritis, renal medullary necrosis, urinary infection, proteinuria, hematuria, renal failure. The bodies of: conjunctivitis, blurred vision. skin: itching, skin rash, urticaria, erythema multiforme exudative (in including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), increased photosensitivity. hemopoietic system: anemia, leukopenia, thrombocytopenia. Allergic reactions: anaphylactoid reactions (including anaphylaxis), swelling of the lips and tongue, allergic vasculitis. Other: fever.
Interaction with other drugs
- At simultaneous application with other nonsteroidal anti-inflammatory drugs (as well as acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and gastrointestinal bleeding;
- In an application with antihypertensive drugs may decrease the effectiveness of the latter;
- In an application with lithium therapy may develop lithium accumulation and increase its toxic effect (recommended monitoring of blood concentrations of lithium);
- In an application with methotrexate increases the side effects of the latter on the hematopoietic system (risk of anemia and leukopenia, shows periodic blood count control);
- While the use of diuretics and cyclosporine increases the risk of renal failure;
- While the use of intrauterine contraceptive devices may reduce the effectiveness of the latter;
- While the use of anticoagulants (heparin, ticlopidine warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolizin) increases the risk of bleeding (requires periodic monitoring of indicators of coagulation).
- In an application with kolestiraminom, as a result of binding of meloxicam, enhanced its excretion via the gastrointestinal tract.Management vehicles, maintenance vehicles and machinery
use of the drug can cause undesired effects in the form of headaches and dizziness, drowsiness. If you have the above phenomenon it is necessary to abandon the vehicle management and maintenance of machines and mechanisms.
. Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal-bleeding, acute renal failure, liver failure, respiratory arrest, asystole
Treatment: No specific antidote; . with an overdose of the drug should carry out gastric lavage, activated charcoal (within the next hours, symptomatic therapy Cholestyramine accelerates the elimination of the drug from the body Forced diuresis, alkalization of urine, hemodialysis, -. are ineffective because of the high regard of the drug to blood proteins.
- Caution should be exercised when using the drug in patients with a history in which the gastric ulcer and duodenal ulcers, as well as in patients on anticoagulant therapy. These patients are at increased risk of occurrence of erosive ulcerous diseases of the gastrointestinal tract.
- Use caution and monitor renal function when using the drug in elderly patients, patients with chronic suspension testosterone heart failure with signs of circulatory failure in patients with cirrhosis, and in patients with hypovolemia in surgical care.
- In patients with renal insufficiency, if creatinine clearance greater than 25 ml / min do not require a correction mode.
- In patients undergoing dialysis, medication dosage should not exceed 7.5 mg / day.
- Patients taking both diuretics and meloxicam, should take plenty of fluids.
- If you experience an allergic reaction (itching, skin rash, urticaria, fotosesibilizatsiya) during treatment should consult a doctor in order to address the issue of termination of dosing.Management vehicles, maintenance vehicles and machinery
use of the drug can cause undesired effects in the form of headaches and dizziness, drowsiness. It is necessary to abandon the vehicle management and maintenance of machines and mechanisms that require concentration.