Meloxicam-Teva pills 7.5 mg 20 pcs
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Active ingredients
Meloxicam
Release form
Pills
Composition
Active ingredient: Meloxicam - 7.5 mg; Excipients: lactose monohydrate 77.2 mg, microcrystalline cellulose 56.0 mg, sodium citrate dihydrate 18.0 mg, povidone-KZO 6.0 mg, crospovidone 12.0 mg, colloidal silicon dioxide 1.5 mg, magnesium stearate 1, 8 mg.
Pharmacological effect
Meloxicam is a non-steroidal anti-inflammatory drug with anti-inflammatory and antipyretic effects. The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in the biosynthesis of prostaglandin in the area of inflammation. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandin that protects the mucous membrane of the gastrointestinal tract (GIT) and is involved in the regulation of blood flow in the kidneys.
Pharmacokinetics
Well absorbed from the gastrointestinal tract, the absolute bioavailability when administered orally - 89%. Simultaneous ingestion of food does not change the absorption. The maximum concentration (Сmax) is reached within 5-6 hours after a single dose of the drug. When administered in doses of 7.5 and 15 mg, the concentration is proportional to the dose. Equilibrium concentrations are reached within 3-5 days. With prolonged use (more than 1 year), concentrations are similar to concentrations that are noted after the first achievement of equilibrium concentrations. Plasma protein binding is more than 99%. The range of differences between the maximum and basal concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-2.0 mcg / ml when using a dose of 7.5 mg, and when using a dose of 15 mg - 0.8-2.0 mcg / ml (respectively, the values of Cmin to Сmах are given). Gets through histohematogenous barriers, the concentration in the synovial fluid reaches 50% of the maximum concentration of the drug in the plasma .; Almost completely metabolized in the liver to form 4 pharmacologically inactive metabolites. The main metabolite, 5-carboxymeloxicam (60% of the dose), is formed by oxidation of the intermediate metabolite, 5'-hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (9% of the dose). An important role in the metabolism of meloxicam is played by CYP2C9 isoenzyme, and to a lesser extent CYP3A4 isoenzyme.The formation of two other metabolites (constituting 16% and 4%, respectively, of the dose of the drug) involves peroxidase, the activity of which varies individually .; It is derived equally through the intestines and kidneys, mainly in the form of metabolites. At least 5% of the daily dose is excreted unchanged through the intestine, in the urine in unchanged form is found in trace amounts. The average half-life of T1 / 2 is 15-20 hours. The plasma clearance averages 8 ml / min; Pharmacokinetics in special clinical situations; Hepatic and mild or moderate renal insufficiency do not have a significant effect on the meloxicam pharmacokinetics. In terminal renal failure, an increase in the volume of distribution (Vd) can lead to higher concentrations of unbound meloxicam, in these patients the daily dose should not exceed 7.5 mg. In elderly patients, the average plasma clearance is reduced. Vd average of 11 liters.
Indications
Symptomatic treatment of osteoarthritis; symptomatic treatment of rheumatoid arthritis; symptomatic treatment of ankylosing spondylitis (ankylosing spondylitis).
Contraindications
Hypersensitivity to meloxicam or auxiliary components of the drug; intolerance to acetylsalicylic acid and pyrazolone drugs; the period after coronary artery bypass surgery; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history of); erosive and ulcerative changes of the mucous membrane of the stomach or duodenum, gastrointestinal bleeding; inflammatory bowel disease (ulcerative colitis, Crohn's disease); rare hereditary diseases (lactose intolerance, lactase deficiency or glucose-galactose malabsorption); cerebrovascular or other bleeding / hemorrhage; decompensated heart failure; severe liver failure; severe renal failure (creatinine clearance less than 30 ml / min), if hemodialysis is not performed; pregnancy, breastfeeding, children under 15 years.
Dosage and administration
Since the risk of adverse events (includingon the part of the gastrointestinal tract) may increase with increasing dose and duration of treatment; to reduce the risk of adverse effects, use the minimum effective dose as short as possible .; The drug is taken orally once a day with meals, drinking plenty of liquids .; Recommended dosing regimen: In case of rheumatoid arthritis and ankylosing spondylitis: 15 mg once a day, depending on the therapeutic effect, the dose can be reduced to 7.5 mg / day; In osteoarthritis: 7.5 mg1 once a day, if necessary, increase the dose to 15 mg / day. The maximum daily dose is 15 mg. In children older than 15 years, the maximum dose is 0.25 mg / kg body weight .; In elderly patients with an increased risk of adverse reactions, the initial daily dose is 7.5 mg. In patients with severe renal insufficiency who are on hemodialysis, the dose of the drug Meloxicam -Teva should not exceed 7.5 mg / day; In patients with renal insufficiency (creatinine clearance more than 30 ml / min) dose reduction is not required .; In patients with minor or moderate hepatic impairment, no dose reduction is required.
Side effects
Side effects are classified according to the following frequency: very often - at least 10%; often not less than 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including isolated cases .; On the part of the digestive system: often - dyspepsia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequently - esophagitis, stomatitis, belching, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including latent), transient changes in liver function (increased activity of liver transaminases or increased bilirubin concentration); rarely - gastrointestinal perforation, colitis; hepatitis, gastritis .; From the hemopoietic system: often - anemia; infrequently - leukopenia, change in leukocyte formula, thrombocytopenia, agranulocytosis .; On the part of the skin: often - itching, skin rash; infrequently - urticaria; rarely, Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous rash, erythema multiforme, photosensitization .; On the part of the respiratory system: rarely - bronchospasm, asthma attack in predisposed patients with hypersensitivity to acetylsalicylic acid or other NSAIDs .; The nervous system: often - dizziness, headache; infrequently - tinnitus, drowsiness; rarely - confusion, disorientation,emotional lability .; Since the cardiovascular system: often - peripheral edema; infrequently, increased blood pressure, palpitations, "flush" of blood to the skin of the face .; From the urinary system: infrequently - changes in laboratory parameters of renal function (increased concentration of creatinine and / or urea in the blood); rarely, acute renal failure; interstitial nephritis, albuminuria and hematuria, however, the relationship of these changes with the use of meloxicam has not been established .; On the part of the organ of vision: rarely - conjunctivitis, visual impairment, incl. blurred vision .; Allergic reactions: rarely - angioedema, anaphylactic / anaphylactoid reactions.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain are usually reversible. GI bleeding is possible. Severe poisoning can lead to acute renal failure, liver failure, respiratory arrest, asystole .; Treatment: there is no specific antidote; in the case of an overdose of the drug should be a gastric lavage, taking activated charcoal (within the next hour) and symptomatic therapy. In clinical studies it has been shown that colestyramine, binding meloxicam in the gastrointestinal tract, leads to its more rapid elimination. Forced diuresis, alkalization of urine, hemodialysis are ineffective due to the high association with blood proteins.
Interaction with other drugs
With the simultaneous use of meloxicam with other NSAIDs, including salicylates (acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and gastrointestinal bleeding due to synergistic action .; The use of meloxicam increases the risk of acute renal failure in patients with dehydration. In patients receiving meloxicam and diuretics, adequate hydration should be maintained. A study of renal function is needed before treatment begins; Anticoagulants (heparin, ticlopidine, warfarin), as well as thrombolytic agents (streptokinase, fibrinolysin), while used with meloxicam, increase the risk of bleeding. If it is impossible to avoid the simultaneous use of these drugs, careful monitoring of blood clotting indicators is necessary .; Meloxicam reduces the effect of antihypertensive agents (for example, beta-blockers, angiotensin-converting enzyme inhibitors (ACE), vasodilators, diuretics), due to inhibition of prostaglandins,having vasodilating properties .; The combined use of NSAIDs and angiotensin II receptor antagonists, as well as ACE inhibitors, enhances the effect of reducing glomerular filtration. In patients with impaired renal function, this can lead to the development of acute renal failure .; Meloxicam, having an effect on renal prostaglandins, may enhance cyclosporine nephrotoxicity. In the case of combination therapy, renal function should be monitored .; Earlier it was reported that the effectiveness of intrauterine contraceptives decreased with the use of NSAIDs. This observation requires further confirmation. Meloxicam can increase the concentration of lithium in plasma by reducing renal excretion of lithium. The concentration of lithium in the plasma can reach toxic values. The combined use of lithium and meloxicam is not recommended. If necessary, such a combination therapy should control the concentration of lithium in the plasma at the beginning of treatment, in the selection of the dose and the abolition of meloxicam .; Meloxicam can reduce the tubular secretion of methotrexate and, thus, increase the concentration of methotrexate in plasma. In this regard, patients receiving high doses of methotrexate (more than 15 mg per week), the simultaneous use of meloxicam is not recommended. The risk of interaction with the simultaneous use of methotrexate and meloxicam is also possible in patients receiving low doses of methotrexate, especially in patients with impaired renal function. If necessary, combination therapy should monitor blood count and renal function. Care must be taken if meloxicam and methotrexate are used simultaneously for 3 days, because plasma plasma methotrexate concentration may increase and, as a result, toxic effects may occur. The simultaneous use of meloxicam did not affect the pharmacokinetics of methotrexate at a dose of 15 mg per week, however, it should be taken into account that the hematological toxicity of methotrexate is enhanced while taking NSAIDs. Kolestyramine, binding meloxicam in the digestive tract, leads to its more rapid elimination. With the simultaneous use of meloxicam, antacids, cimetidine, digoxin or furosemide, no significant pharmacokinetic interactions have been identified.
special instructions
Caution must be exercised in treating patients with gastrointestinal diseases in history and in patients receiving anticoagulants.These patients have an increased risk of erosive and ulcerative lesions of the gastrointestinal tract .; As with the use of other NSAIDs, gastrointestinal bleeding, ulcers and perforations that are potentially life-threatening to the patient can occur during treatment with meloxicam at any time, as if there are symptoms or information about serious gastrointestinal complications in history, the absence of these signs. The consequences of these complications are generally more severe in the elderly. If an erosive and ulcerative lesion of the gastrointestinal tract or gastrointestinal bleeding occurs, meloxicam must be canceled .; With the development of adverse events on the part of the skin and mucous membranes, the patient should consult a doctor to consider the issue of discontinuing meloxicam .; When using meloxicam, an episodic increase in the activity of “liver” transaminases or other indicators of liver function in the blood serum was reported. In most cases, this increase was small and transient. If the identified changes are significant or do not decrease with time, meloxicam should be canceled, and monitor the identified laboratory changes. NSAIDs inhibit kidney synthesis of prostaglandins, which are involved in maintaining renal perfusion. The use of meloxicam in patients with reduced renal blood flow or a reduced volume of circulating blood can lead to decompensation of latent renal failure. After the withdrawal of meloxicam, the kidney function is usually restored to its original level. Elderly patients, patients with dehydration, congestive heart failure, cirrhosis of the liver, nephrotic syndrome or kidney disease, patients receiving diuretics, ACE inhibitors, angiotensin II receptor antagonists, as well as patients undergone serious surgery, leading to hypovolemia. In these patients, diuresis and renal function should be carefully monitored at the start of therapy. The use of meloxicam in conjunction with diuretics can lead to a delay of sodium, potassium and water, and affect the natriuretic effect of diuretics.As a result, in predisposed patients may increase the signs of heart failure or hypertension .; Meloxicam, like other NSAIDs, can mask the symptoms of an infectious disease .; The use of meloxicam can lead to a decrease in fertility. Therefore, the drug is not recommended for women planning pregnancy. The drug contains lactose. It should not be taken in patients with hereditary intolerance to galactose, lactase deficiency or impaired glucose / galactose absorption.