Nonsteroidal anti-inflammatory drug (NSAID) that has anti-inflammatory, analgesic and antipyretic activity. Mechanism pronounced anti-inflammatory action of meloxicam is associated with inhibition of the enzyme cyclooxygenase, which is involved in the synthesis of prostaglandins (PGs) are almost exclusively in the field of inflammation. Due to the relatively selective inhibition of inhibits the synthesis of prostaglandins (PGs) in the area of inflammation to a greater extent than in the gastric mucosa and kidney. Demonstrated that meloxicam at recommended doses has no effect on platelet aggregation, and bleeding time, unlike non-selective inhibitors (indomethacin, diclofenac, ibuprofen and naproxen), which is significantly inhibited platelet aggregation and increased bleeding time.
These effects depend on the dose. The selectivity of action of meloxicam is reduced by assigning it in high doses, long-term use and individual characteristics of equipoise vs deca.
Meloxicam is well absorbed from the gastrointestinal tract, by ingestion bioavailability is 89%, food intake does not affect absorption of the drug. Equilibrium concentration buy equipoise in the blood plasma is reached after 3-5 days after starting the drug. If ingestion maximum concentration (the C max ) in plasma is achieved in 5-6 hours.
Meloxicam penetrates the blood-tissue barriers in the synovial fluid concentration reaches 50% of the C max in the blood plasma. Meloxicam almost completely metabolized in the liver to form four pharmacologically active metabolites. The main metabolite, 5′-karboksimeloksikam (60% of the dose), formed by oxidation of an intermediate metabolite 5′-gidroksikarboksimeloksikama 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 CYP2C9 isozyme, somewhat smaller value is CYP3A4 isozyme. The formation of two other metabolites (components, respectively, 16% and 4% of the dose) participates peroxidase activity, which is likely to have a high individual variability. Excreted mainly as metabolites through the intestine and kidney in equal proportions. 5% of the daily the dose is equipoise vs deca excreted unchanged through the intestines, in urine unchanged drug is found only in trace amounts. The half-life (T 1/2 ) of meloxicam is 15-20 hours. Plasma clearance is on average 8 mL / min, but may be reduced in the elderly. The amount of the average distribution of approximately 11 liters. Hepatic and renal insufficiency of mild to moderate severity did not significantly affect the pharmacokinetics of meloxicam. In severe renal insufficiency due to lower excretion of the drug daily dose should not exceed 7.5 mg.
Symptomatic therapy of the following diseases: • osteoarthritis; • rheumatoid arthritis; • ankylosing spondylitis; • gout; . • other inflammatory and degenerative diseases of the joints accompanied by pain drug is intended for symptomatic therapy reduce pain and inflammation at the time of use, the progression of the disease does not affect .
• Hypersensitivity to meloxicam or any other component of the product, other NSAIDs; • lactose intolerance, lactase deficiency or syndrome of glucose-galactose malabsorption; • complete or incomplete combination of bronchial asthma with recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid (ASA) or NSAIDs (including history); • erosive and ulcerative lesions of the mucous membrane of the stomach or duodenum 12 in the acute stage; • gastrointestinal, cerebrovascular bleeding, bleeding at other sites, including a history of (or suspicion of bleeding); • inflammatory bowel disease (ulcerative colitis, Crohn’s disease) in the acute stage; • severe liver failure or liver disease in the active stage; • chronic renal failure patients who are not undergoing hemodialysis (creatinine clearance (CC) of less than 30 ml / min); • progressive kidney disease, including those confirmed by hyperkalemia; • condition after coronary artery bypass surgery; • decompensated heart failure; • pregnancy; • breastfeeding; • children’s age (15 years).
You should use the lowest effective dose for the shortest possible course to reduce the risk of dose-related adverse effects. • Coronary heart disease; • cerebrovascular disease; • compensated heart failure; • dyslipidemia / hyperlipidemia, diabetes mellitus; • peripheral arterial disease; • bronchial asthma; • smoking , frequent use of alcohol; • chronic renal insufficiency with CC 30-60 ml / min; • a history of the development of ulcerative lesions gastrointestinal tract, an infection of Helicobacter pylori; • advanced age; • long-term use of NSAIDs; • severe somatic diseases; • concomitant therapy following drugs: anticoagulants (e.g. warfarin), antiplatelet agents (aspirin, clopidogrel), oral corticosteroids (e.g., prednisone), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).
Application of pregnancy and during breastfeeding
Meloxicam is contraindicated during pregnancy. Synthesis Reduction of GHG may have an adverse effect on pregnancy and fetal development. Data from epidemiological studies suggest an increased risk of spontaneous abortion, development of heart disease and defekta anterior abdominal wall of the fetus after applying PG synthesis inhibitors during pregnancy. The absolute risk of developing heart disease increased from less than 1% to 1.5%. This risk increases with the dose and duration of therapy. In the III trimester of pregnancy, the use of PG synthesis inhibitors can cause the following violations of the fetus: • premature closure of the ductus arteriosus and the development of pulmonary hypertension; • renal dysfunction with the further development of renal failure with a decrease equipoise vs deca in the amount of amniotic fluid. The mother during birth may increase the bleeding duration and decrease the contractile ability of the uterus, and as a consequence, increase the time of delivery. Antiplatelet effect may occur even when taking low doses. Meloxicam is released in breast milk, therefore the use of the drug during breast-feeding is contraindicated. If necessary, use during breast-feeding, you must resolve the issue of termination of breastfeeding.
Dosing and Administration
The drug is taken orally with meals at a daily dose of 7.5-15 mg. The drug should be taken during or after a meal, drinking water or milk (liquid volume of at least 100 ml). The maximum daily dose – 15 mg. In osteoarthritis, and other inflammatory and degenerative diseases of the joints accompanied by pain, the average daily dose is 7.5 mg. In some cases to achieve a better effect, dose increased to 15 mg per day. In rheumatoid arthritis, gout, and the average daily dose is 15 mg. If necessary, the dose may be reduced to 7.5 mg per day. In ankylosing spondylitis the average daily dose is 15 mg. If necessary, the dose may be reduced to 7.5 mg per day. In elderly patients and in patients with severe renal impairment (creatinine clearance less than 30 mL / min), hemodialysis, dose should not exceed 7.5 mg per day. In renal moderate insufficiency (CC 30-60 ml / min) and in hepatic failure moderate dose adjustment is required.
On the part of the gastrointestinal tract are very common: dyspepsia, nausea, vomiting, abdominal pain, constipation equipoise vs deca or diarrhea, flatulence; rare: gastrointestinal bleeding (including hidden ), stomatitis, transient increase in activity of “liver” transaminases, hyperbilirubinemia, belching; rarely ulcerative lesion of the mucous membrane of the stomach or duodenal ulcers, esophagitis, colitis, hepatitis, very rarely . perforation of the digestive tract wall Part of the central nervous system common: headache; uncommon: dizziness, drowsiness; rarely: “nightmarish” dream, disorientation, insomnia, emotional lability; the frequency is unknown: confusion. From the side of hematopoiesis rare: anemia rare: changes in blood counts (leykotsitopeniya, thrombocytopenia); very rare: agranulocytosis. allergic reactions: uncommon:other allergic reactions rare: angioedema, the frequency is not known: anaphylactoid / anaphylactic reactions. On the part of the cardiovascular system often: peripheral edema uncommon: increase in blood pressure (BP), “tides” of blood to the skin of the face; rare: palpitations. respiratory system rare: bronchospasm. For the skin rarely: itching, skin rash, angioedema, rare: urticaria, Lyell’s syndrome (toxic epidermal necrolysis), erythema multiforme (including malignant exudative erythema – Stevens syndrome Johnson); very rare: bullous dermatosis, the frequency is not known: photosensitivity. From the senses rare: conjunctivitis, visual disturbances, including . blurred vision, tinnitus Urinary system Uncommon: hypercreatininemia and / or increasing the concentration of serum urea, sodium and water retention, hyperkalemia, lower limb edema, rare: acute renal failure in patients with initially increased risk; connection with the intake of meloxicam is not installed – interstitial nephritis, nephrotic syndrome (albuminuria), hematuria. If any of these instructions side effects are compounded, or if you notice any other side effects not mentioned in the instructions, inform your doctor. buy legal anabolic steroids online
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