Well absorbed from deca durabolin injection 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 of C min and C max ). 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 with equally through the intestine and the kidney, mainly in the form of metabolites. Through the intestines 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).
– hypersensitivity to the active substance or auxiliary components;
– contraindicated in the post-coronary artery bypass surgery;
– uncompensated heart failure;
– complete or incomplete combination of bronchial asthma, recurrent nasal polyposis, and paranasal sinuses and intolerance of aspirin and other NSAIDs (including.. h in history);.
– erosive and ulcerative changes in gastric mucosa and 12 duodenal ulcer, active gastrointestinal bleeding,
– inflammatory bowel disease (ulcerative colitis, Crohn’s disease)
– cerebrovascular bleeding or other bleeding
– severe hepatic impairment or active liver disease;
– severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 mL / min), progressive renal disease including . confirmed hyperkalemia
– pregnancy, breast-feeding;
– Children up to age 15 years;
Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 mL / min. A history of the development of ulcerative lesions gastrointestinal tract, the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy following medications:
– Anticoagulants (eg, warfarin)
– antiplatelet agents (eg, aspirin, clopidogrel)
– oral corticosteroids (such as prednisone)
– selective serotonin reuptake inhibitors (such as citalopram, fluoxetine, paroxetine, sertraline)
To reduce the risk of adverse effects on the gastrointestinal tract to use the minimum effective dose as deca durabolin injection low as possible short course.
Dosing and Administration
The drug is taken orally during a meal once a day.
The recommended dosing regimen:
– Rheumatoid arthritis: 15 mg per day. 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 spondylitis: 15 mg per day. The maximum daily dose should not exceed 15 mg.
In patients with an 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.
Side effect From the digestive system: more than 1% – indigestion, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1% – 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 side of hematopoiesis: more than 1% – anemia; 0.1-1% – changes in blood counts, including leukopenia, tromotsitopeniya. For the skin: more than 1% – itching, skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitivity, bullous rash, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis. The respiratory system: less than 0.1% – bronchospasm.From the nervous system: more than 1% – dizziness, headache; 0.1-1% – vertigo, tinnitus, drowsiness; less than 0.1% – confusion, disorientation, emotional lability. On the part of the cardiovascular system:more than 1% – peripheral edema; 0.1-1% – increase in blood pressure, palpitations, “tides” of blood to the skin. From the urinary system: 0.1-1% – 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. From the senses: less than 0.1% – conjunctivitis, visual disturbances, including blurred vision. Allergic reaction: less than 0.1% – angioedema, anaphylactoid / anaphylactic reactions.
Overdose Symptoms: . Impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal-bleeding, acute renal failure, liver failure, respiratory arrest, asystole Treatment: No specific antidote; 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.
Interaction with other drugs
– the simultaneous use of other NSAIDs (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 drugs lithium may develop cumulation of lithium and increase its toxic action (control of blood lithium concentration is recommended)
– When 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);
– simultaneous use of diuretics and cyclosporine increases the risk of renal failure;
– the simultaneous use of intrauterine contraceptive devices may reduce the effectiveness of the latter;
– the simultaneous use of anticoagulants (heparin, ticlopidine warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolizin) It increases the risk of bleeding (requires periodic monitoring of indicators of clotting).
– in an application with kolestiraminom, as a result of binding of meloxicam, enhanced its excretion via the gastrointestinal tract.
– while the use of selective serotonin reuptake inhibitors increase the risk of gastrointestinal bleeding.
– Use caution 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. In these patients increased the risk of ulcerative-erosive gastro-intestinal tract.
– Use caution and monitor renal function when using the drug in elderly patients, patients with chronic heart failure with signs of circulatory failure in patients with cirrhosis of the liver, as well as 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 on dialysis, the dosage of the drug should not exceed 7.5 mg / day.
– patients taking both diuretics and meloxicam, should take plenty of fluids.
– If during treatment any allergic reaction (itching, skin rash, urticaria, fotosesibilizatsiya) should consult a doctor in order to address the issue of termination of dosing.
– meloxicam, as well as deca durabolin injection and other NSAIDs, may mask the symptoms of infectious diseases.
– The use of meloxicam, as with other drugs that block the synthesis of prostaglandins could affect fertility, so is not recommended for women wishing to become pregnant.
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.