After oral administration of meloxicam is well absorbed from the gastrointestinal tract. The bioavailability of approximately 90%. Simultaneous food intake does not modify absorption. When deca durabolin reviews using the drug orally in doses of 7.5 and 15 mg doses are proportional to its concentration. The maximum plasma concentration (about 1000 mg / L for doses of 7.5 mg) after a single dose is reached about 4-6 hours. The equilibrium concentrations are reached within 3-5 days. Chronic administration of the drug (over 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 g / ml (Cmin values respectively and Sshah). Meloxicam penetrates the blood-tissue barriers.
The concentration of drug in the synovial fluid of 40-50% of the maximum concentration of drug in blood plasma.
Almost completely metabolized in the liver to form four pharmacologically inactive derivatives. The major metabolite, 5′-carboxy-meloxicam (60% of the dose), is formed by oxidation of an intermediate metabolite 5-gidroksimetilmeloksikama, which is also excreted to a lesser extent (9% of the dose). Studies in vitro have shown that the metabolic conversion plays an important role ZA4 CYP. The formation of two other metabolites (components, respectively 16% and 4% of the dose) participates peroxidase, which activity is likely varies individually.
Deduced equally drug in the feces and urine, mainly as metabolites. In unaltered output of less than 5% of the daily dose, and in urine unchanged meloxicam detected only in trace amounts. The half-life of meloxicam is 15-20 hours. Average plasma clearance of 8 ml / min. Elderly persons drug clearance is reduced. The volume of distribution is low and amounts to an average of 11 l. The drug does not rely on dialysis.
Moderate hepatic dysfunction and / or kidney does not have a significant effect on the pharmacokinetics of meloxicam.
- Symptomatic treatment of rheumatoid arthritis;
- Symptomatic treatment of osteoarthritis;
- Symptomatic treatment of ankylosing spondylitis (Ankylosing spondylitis).Contraindications
- hypersensitivity to meloxicam or other component of the formulation;
- Hypersensitivity to aspirin and other NSAIDs;
- asthma in combination with nasal polyposis mucosa;
- gastric ulcer or duodenal ulcer in the acute phase;
- gastrointestinal, or any other cerebrovascular bleeding;
- severe uncontrolled heart failure;
- severe hepatic impairment;
- severe renal failure deca durabolin reviews (without dialysis);
- Children under the age of 15 years;
- lactation.With caution
used in patients of advanced age who have a history of erosive and ulcerative lesions of the gastrointestinal tract, coronary heart disease.
Dosage and administration:
1 The drug is taken once a day, during meals. Rheumatoid arthritis: 15 mg / day. With sufficient severity therapeutic effect, the dose can be reduced to 7.5 mg / day. Osteoarthritis: 7.5 mg / day. . If necessary, the dose may be increased to 15 mg / day Ankylosing spondylitis: 15 mg / day. The maximum daily dose – 15 mg. In patients with an increased risk of adverse effects, as well as in patients with severe renal impairment on hemodialysis, the daily dose should not exceed 7.5 mg.
Melox generally well tolerated. However, you may experience the following side effects: From the digestive system: more than 1.0% – indigestion, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1.0% – transient increase in activity of “liver” transaminases, hyperbilirubinemia, eructation, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis. From the hematopoietic system: more than 1.0% – anemia; 0.1-1.0% – changes in blood counts, includingleukopenia, thrombocytopenia. With the skin side and mucous membranes: more than 1.0% – itching, skin rash, 0.1-1.0% – urticaria, less than 0.1% – photosensitivity, bullous rash, erythema multiforme, in Vol. h. . Stevens-Johnson syndrome, toxic epidermal necrolysis From the respiratory system: less than 0.1% – bronchospasm. On the part of the cardiovascular system: more than 1.0% – peripheral edema;0.1-1.0% – increase in blood pressure, palpitations, “tides” of blood to the skin. CNS: more than 1.0% – dizziness, headache; 0.1-1.0% – vertigo, tinnitus, drowsiness; less than 0.1% – confusion, disorientation, emotional lability. From the urinary system: 0.1-1.0% – hypercreatininemia and / or an increase in urea in blood serum; less than 0.1% – acute renal failure; connection with the intake of meloxicam is not installed – interstitial nephritis, albuminuria, hematuria. Allergic reaction: less than 0.1% – angioedema, anaphylactoid / anaphylactic reaction, the part of the organs of vision: less than 0.1% – conjunctivitis, visual disturbances, including blurred vision. Other: fever.
Interaction with other drugs:
The combined use of Melox with: – other NSAIDs, including salicylates in high doses: co-administration of a single drug from the group of NSAIDs may increase the risk of erosive and ulcerative lesions and gastrointestinal bleeding;
- anticoagulants (ticlopidine, heparin, warfarin, and with thrombolytic drugs (streptokinase, fibrinolizinom): increased risk of bleeding is necessary to periodically monitor the performance of blood clotting, -.
- Lithium drugs: possible development of lithium accumulation and increase its toxic effect (recommended for control of the plasma concentration of lithium);
- MTX: may potentiate the side effects of methotrexate on the hematopoietic system (risk of anemia and leukopenia). In such cases, a periodic monitoring of blood count;
- contraceptives: may decrease the effectiveness of intrauterine contraceptive devices;
- diuretics and cyclosporine: there is a potential for the development of renal failure.
- antihypertensive agents (eg beta-blockers, ACE inhibitors, vasodilators, diuretics): possible reduction in the effectiveness of antihypertensive drugs;
- kolestiraminom: as a result binding of meloxicam, increased excretion of the drug through the gastrointestinal tract;Driving, operating machinery and mechanisms:
The drug can cause undesired side effects such as headache, dizziness and drowsiness. Therefore, when taking meloxicam, it is desirable to give up driving 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. In case of overdose should be carried out gastric lavage, administration of activated charcoal to appoint (within the hour) and symptomatic therapy. To accelerate the elimination of meloxicam can be applied cholestyramine. Hemodialysis, forced diuresis and urine alkalization is not effective because of the high regard of the drug to blood proteins.
Like other NSAIDs, Melox should be used with caution in patients with a history of marked gastric and duodenal ulcers, as well as in patients on anticoagulant therapy. In these patients increased the risk of ulcerative erosive gastrointestinal diseases.
Use caution and monitor renal function in elderly patients, in patients with chronic heart failure with signs of circulatory failure in patients with cirrhosis, in patients with hypovolemia deca durabolin reviews 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 per day.
at the same time taking meloxicam and diuretics should be a sufficient number of fluid.
In the case of allergic reactions (itching, skin rash, urticaria, photosensitivity), please consult your doctor to decide on termination of the administration of the drug.
The use of meloxicam, as with other NSAIDs, may mask the symptoms of infectious diseases.
The use of meloxicam, as with other drugs blocking the synthesis of prostaglandins, may affect fertility, what should warn women planning a pregnancy (reduced chance of pregnancy).
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