Meloxicam tablets 7.5mg №10×2

Name Meloxicam tabl. Tablets with a dosage of 15 mg are at risk on the one hand. The main active ingredient Meloxicam Release form Tablets Dosage 7.5 mg Pharmacological properties Pharmacodynamics Meloxicam is a non-steroidal anti-inflammatory drug (NSAID), belongs to enolic acid derivatives and has anti-inflammatory, analgesic and antipyretic properties. The pronounced anti-inflammatory effect of meloxicam has been established in all standard models of inflammation. As with other NSAIDs, the exact mechanism of action remains unknown. However, there is at least one common mechanism of action common to all NSAIDs (including meloxicam): inhibition of the biosynthesis of prostaglandins known as inflammatory mediators. PharmacokineticsAbsorption. Meloxicam is well absorbed from the gastrointestinal tract, which is reflected in its high absolute bioavailability (about 90% after oral administration). After a single application of meloxicam, the average maximum plasma concentrations are reached within 5-6 hours after taking solid oral dosage forms (capsules and tablets). With repeated use, the equilibrium state of pharmacokinetics was achieved within 3-5 days. The administration of a single daily dose provides plasma concentrations of the drug with a relatively small peak fluctuation in the range of 0.4-1.0 μg / ml for a dosage of 7.5 mg and 0.8-2.0 μg / ml for a dosage of 15 mg ( Cmin and Cmax, respectively, in the equilibrium state). The average maximum concentrations of meloxicam in blood plasma in an equilibrium state were reached within 5-6 hours. The degree of absorption of meloxicam after oral administration did not depend on food intake or the use of inorganic antacids. Distribution. Meloxicam binds well to plasma proteins, mainly to albumin (99%). Penetrates into the synovial fluid, the concentration in the synovial fluid is approximately 50% of the plasma concentration. The volume of distribution after taking several oral doses of meloxicam (from 7.5 mg to 15 mg) is about 16 liters with an interindividual variation coefficient of about 11-32%. Biotransformation. Meloxicam is extensively metabolized in the liver. Four pharmacologically inactive derivatives were found in urine. 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 administered dose). In vitro studies have shown that CYP2C9 plays an important role in this metabolic transformation, and the CYP3A4 isoenzyme is of additional importance. Peroxidase takes part in the formation of two other metabolites (constituting, respectively, 16% and 4% of the dose of the drug). Withdrawal. It is excreted equally in the form of metabolites with feces and urine. Less than 5% of the daily dose is excreted unchanged in the feces, in the urine in unchanged form the drug is found only in trace amounts. The mean half-life of meloxicam varies from 13 hours to 25 hours after oral, intramuscular and intravenous administration. The total plasma clearance averages 7-12 ml / min after a single oral administration. Linearity/Nonlinearity. The linearity of the pharmacokinetics of meloxicam has been demonstrated with the introduction of therapeutic doses orally or intramuscularly in the range from 7.5 mg to 15 mg. Patients with renal / hepatic insufficiency. Insufficiency of liver function, as well as moderately severe renal failure, does not significantly affect the pharmacokinetics of meloxicam. In patients with moderate renal insufficiency, a higher clearance of the drug was observed. In patients with end-stage renal disease, a decrease in plasma protein binding was observed. In end-stage renal disease, an increase in the volume of distribution may lead to higher concentrations of free meloxicam, so in these patients the daily dose should not exceed 7.5 mg. Elderly patients. Pharmacokinetic parameters for elderly male patients were similar to pharmacokinetic parameters for young male patients. In elderly female patients, a higher AUC value and a longer half-life were observed compared with young patients of both sexes. In elderly patients, the mean plasma clearance during steady state pharmacokinetics is slightly lower than in younger patients. Indications for use Short-term symptomatic therapy of exacerbation of osteoarthritis. Long-term symptomatic therapy of rheumatoid arthritis or ankylosing spondylitis. Dosage and administration Meloxicam is administered orally. The daily dose of the drug is taken once with a meal, washed down with water or other liquid. The likelihood of adverse effects can be minimized by using the lowest effective dose of the drug for the shortest period of time necessary to control symptoms. The need for therapy and the patient’s response to therapy should be periodically assessed, especially in patients with osteoarthritis. Exacerbations of osteoarthritis: 7.5 mg / day (one 7.5 mg tablet or half a 15 mg tablet). If necessary, in the absence of improvement, the dose may be increased to 15 mg / day (two 7.5 mg tablets or 1 tablet 15 mg). Rheumatoid arthritis, ankylosing spondylitis: 15 mg / day (two 7.5 mg tablets or 1 tablet 15 mg). Depending on the severity of the response to therapy, the dosage may be reduced to 7.5 mg / day (one 7.5 mg tablet or half a 15 mg tablet). Do not exceed the maximum daily dose of meloxicam 15 mg. Special patient populations Elderly patients and patients at increased risk of adverse reactions. The recommended dose for long-term treatment of elderly patients with rheumatoid arthritis or ankylosing spondylitis is 7.5 mg per day. Patients with an increased risk of developing adverse reactions should begin treatment with a dosage of 7.5 mg per day. Impaired renal function In patients with severe renal insufficiency on dialysis, the dose should not exceed 7.5 mg per day. Dose reduction is not required in patients with mild to moderate renal impairment (i.e. patients with creatinine clearance greater than 25 ml/min.). Impaired liver function Patients with mild to moderate hepatic impairment do not require dose reduction. Children and adolescents Meloxicam is contraindicated in children and adolescents under 16 years of age. Use during pregnancy and lactation Suppression of prostaglandin synthesis may have an undesirable effect on pregnancy and fetal development. Data from epidemiological studies indicate an increased risk of spontaneous abortions, heart defects and gastroschisis in the fetus after the use of prostaglandin synthesis inhibitors in early pregnancy. The absolute risk of developing malformations of the cardiovascular system increased from less than 1% to 1.5%. This risk increases with increasing dose and duration of therapy. In animal studies, it has been shown that the administration of a prostaglandin synthesis inhibitor leads to an increase in pre- and post-implantation losses and feto-embryonic mortality. In addition, in animals treated with a prostaglandin synthesis inhibitor during organogenesis, an increase in the number of cases of various malformations, including those of the cardiovascular system, was registered. The use of meloxicam during the 1st and 2nd trimesters of pregnancy is not recommended unless absolutely necessary. When meloxicam is used by a woman planning a pregnancy, or during the first and second trimester of pregnancy, the dose of the drug should be the lowest and the duration of treatment as short as possible. In the III trimester of pregnancy, the use of any prostaglandin synthesis inhibitors can lead to the following disorders: in the fetus: due to toxic effects on the cardiopulmonary system: premature closure of the arterial duct and the development of pulmonary hypertension; kidney dysfunction, with the further development of renal failure with oligohydroamniosis. in the mother and newborn when used at the end of pregnancy: an increase in the duration of bleeding is possible, and the antiaggregatory effect can develop even at a low dosage; decrease in uterine contractility, and, as a result, an increase in the duration of labor. Therefore, meloxicam is contraindicated in the third trimester of pregnancy. Breastfeeding period Despite the lack of data on the experience with the use of meloxicam, it is known that NSAIDs pass into breast milk. Therefore, these drugs are not recommended during breastfeeding. Fertility The use of meloxicam, as well as other drugs that block cyclooxygenase/prostaglandin synthesis, can affect fertility, so this drug is not recommended for women planning pregnancy. In case of violation of the ability to conceive in women or an examination for infertility, it is necessary to consider the abolition of meloxicam. Precautions Undesirable effects can be minimized by administering the lowest effective dose necessary to control symptoms for the shortest period of time. In case of insufficient therapeutic effect, the recommended maximum daily dose should not be exceeded or an additional NSAID should be prescribed, because. this can lead to increased toxicity in the absence of therapeutic benefits. The simultaneous administration of meloxicam with other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided. Meloxicam is not suitable for the relief of acute pain. If there is no clinical improvement after a few days of taking the drug, it is recommended to re-evaluate the prescribed treatment. Patients with a history of esophagitis, gastritis and/or peptic ulcer should be ascertained to be cured. Careful monitoring of these patients receiving meloxicam is necessary in order to timely detect a relapse of the disease. Effects on the gastrointestinal tract As with other NSAIDs, potentially fatal gastrointestinal bleeding, ulceration or perforation may occur at any time during treatment with or without prior symptoms or a history of serious gastrointestinal disease. The risk of gastrointestinal bleeding, ulceration or perforation is higher with increasing dose of NSAIDs in patients with a history of ulcer, especially complicated by bleeding or perforation, and in elderly patients. In such patients, treatment should be initiated at the lowest effective dose. For these patients, consideration should be given to combination therapy with protective medicinal products (such as misoprostol or proton pump inhibitors), and for patients who need concomitant low-dose aspirin or other medicinal products that increase the risk of gastrointestinal injury. Patients with a history of gastrointestinal toxicity, especially elderly patients, should report all unusual abdominal symptoms (especially gastrointestinal bleeding), especially during the initial stages of treatment. Caution should be exercised in patients taking concomitant drugs that may increase the risk of ulcer or bleeding, such as heparin, prescribed both for radical treatment and in geriatric practice, anticoagulants such as warfarin, or other NSAIDs, including acetylsalicylic acid in anti-inflammatory doses (? 500 mg single dose or ? 3 g total daily dose). If gastrointestinal bleeding or ulcers occur in patients treated with meloxicam, treatment should be discontinued. NSAIDs should be used with caution in patients with a history of gastrointestinal disease (ulcerative colitis, Crohn’s disease), as these conditions may worsen. Influence on the cardiovascular system In patients with arterial hypertension and / or with a history of mild to moderate congestive heart failure, careful monitoring is recommended, since fluid retention and edema have been observed during NSAID therapy. Patients with risk factors are recommended clinical monitoring of blood pressure at the beginning of therapy, especially at the beginning of the course of treatment with meloxicam. Research and epidemiological data suggest that the use of some NSAIDs (especially at high doses and in long-term treatment) may be associated with a slight increase in the risk of vascular thrombotic events (such as myocardial infarction or stroke). There are insufficient data to rule out such a risk for meloxicam. Patients with uncontrolled arterial hypertension, congestive heart failure, established ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should be treated with meloxicam only after careful assessment of the patient’s condition. Such an assessment is necessary before initiating long-term treatment in patients with risk factors for cardiovascular disease (eg, hypertension, hyperlipidemia, diabetes mellitus, smokers). Skin reactions Severe skin reactions, including life-threatening ones, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported with the use of meloxicam. Patients should be aware of symptoms and signs and carefully monitored for skin reactions. The highest risk of developing these reactions was noted during the first weeks of treatment. Meloxicam should be discontinued at the first symptoms or signs of Stevens-Johnson syndrome or toxic epidermal necrolysis (eg, progressive skin rash, often blistering, or mucosal lesions). The best outcome in the treatment of Stevens-Johnson syndrome and toxic epidermal necrolysis was observed with early diagnosis and immediate withdrawal of the suspect drug. Early drug withdrawal was associated with a better prognosis. If Stevens-Johnson syndrome or toxic epidermal necrolysis has developed while taking meloxicam, this drug should not be re-administered to this patient in the future. Hepatic and renal function tests As with most NSAIDs, elevations in serum transaminases, elevations in serum bilirubin or other liver function tests, as well as elevations in creatinine and blood urea, and other laboratory abnormalities have been reported rarely. In most cases, the violations were temporary and unexpressed. The development of a pronounced deviation from the norm or its persistence requires discontinuation of the use of meloxicam and an appropriate examination. Functional renal failure NSAIDs, by inhibiting the vasodilating action of renal prostaglandins, can cause functional renal failure as a result of a decrease in glomerular filtration. This response is dose-dependent. It is recommended that diuresis and renal function be carefully monitored at the start of treatment or after dose increases in patients with the following risk factors: older age; concomitant therapy with ACE inhibitors, angiotensin II antagonists, sartans, diuretics; hypovolemia (regardless of cause); congestive heart failure; renal insufficiency; nephrotic syndrome; lupus nephropathy; severe liver dysfunction (serum albumin < 25 g / l or Child-Pugh score? 10). In rare cases, NSAIDs can cause interstitial nephritis, glomerulonephritis, medullary necrosis of the kidney or nephrotic syndrome. The dose of meloxicam for patients with end-stage renal disease on hemodialysis should not exceed 7.5 mg. No dose reduction is required in patients with mild to moderate renal insufficiency (i.e. patients with creatinine clearance greater than 25 ml/min). Sodium, Potassium and Water Retention The use of NSAIDs can lead to retention of sodium, potassium and water and may affect the natriuretic effect of diuretics. In addition, it is possible to reduce the antihypertensive effect of antihypertensive drugs. As a result, predisposed patients may develop or increase edema, symptoms of heart failure or hypertension. Clinical observation is recommended for these patients. Hyperkalemia The risk of developing hyperkalemia is increased in patients with diabetes mellitus or in concomitant therapy with drugs that increase the level of potassium in the blood. In such cases, it is necessary to regularly monitor the level of potassium in the blood. Other Warnings and Precautions Elderly debilitated and malnourished patients are more susceptible to adverse reactions and therefore require careful monitoring. As with other NSAIDs, special care must be taken when prescribing the drug to elderly patients who often have impaired renal, hepatic and cardiac functions. Elderly patients also have an increased incidence of adverse reactions with NSAIDs, especially gastrointestinal bleeding and gastrointestinal perforation, which can be fatal. Meloxicam, like other NSAIDs, may mask the symptoms of an infectious disease. As a drug that inhibits cyclooxygenase/prostaglandin synthesis, meloxicam may affect fertility and is therefore not recommended for women who have difficulty conceiving. In this regard, women undergoing examination for this reason are advised to stop taking meloxicam. The medicinal product contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency and glucose-galactose malabsorption should not take this medicinal product. Interactions with other drugsDrug interaction studies have only been performed in adults. risk of hyperkalemia. Some drugs or therapeutic groups may contribute to the development of hyperkalemia: potassium salts, potassium-sparing diuretics, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists, non-steroidal anti-inflammatory drugs, heparins (low molecular weight or unfractionated), cyclosporine, tacrolimus and trimethoprim. The development of hyperkalemia may depend on the presence of risk factors. The risk of developing hyperkalemia increases with the simultaneous use of the above drugs and meloxicam. Other NSAIDs and acetylsalicylic acid. Simultaneous use with other NSAIDs, including acetylsalicylic acid, in anti-inflammatory doses (? 500 mg once or ? 3 g per day) is not recommended. Corticosteroids (eg, glucocorticoids). With simultaneous use with corticosteroids, care must be taken because of the increased risk of bleeding or perforation of the gastrointestinal tract. Anticoagulants or heparin. Significantly increases the risk of bleeding due to inhibition of platelet function and damage to the mucous membrane of the stomach and duodenum. NSAIDs may enhance the effects of anticoagulants such as warfarin. The simultaneous use of NSAIDs and anticoagulants or heparin in geriatrics or at therapeutic doses is not recommended. In other cases, heparin is prescribed with caution due to an increased risk of bleeding. If it is necessary to prescribe this combination, careful monitoring of the effect of anticoagulants is recommended. Thrombolytics and antiplatelet drugs. Increased risk of bleeding due to inhibition of platelet function and damage to the mucous membrane of the stomach and duodenum. Selective serotonin reuptake inhibitors (SSRIs). Increased risk of gastrointestinal bleeding. Diuretics, ACE inhibitors and angiotensin receptor antagonists. NSAIDs may reduce the effect of diuretics and other antihypertensive drugs. In some patients with impaired renal function (eg, dehydration or elderly patients with impaired renal function), the concomitant use of an ACE inhibitor or angiotensin II receptor antagonist and drugs that block cyclooxygenase may lead to further deterioration of kidney function, up to the development of acute renal failure. insufficiency, which is usually reversible. Thus, this combination should be used with caution, especially in the elderly. In patients, it is necessary to exclude possible dehydration (including latent), to monitor renal function after initiation and periodically during combination therapy. Other antihypertensive drugs (eg beta-blockers). It is possible to reduce the antihypertensive effect of beta-blockers by inhibiting the synthesis of prostaglandins with a vasodilating effect. Calcineurin inhibitors (eg, cyclosporine, tacrolimus) Due to the effect of NSAIDs on the synthesis of renal prostaglandins, nephrotoxicity of calcineurin inhibitors may increase. When conducting this combination therapy, it is necessary to monitor renal function, especially in elderly patients. Deferasirox. Concomitant use of meloxicam and deferasirox may increase the risk of gastrointestinal side effects. In this regard, these drugs should be taken at the same time with caution. lithium preparations. NSAIDs increase the concentration of lithium in plasma by reducing its excretion by the kidneys. The simultaneous use of lithium and NSAIDs is not recommended. If combination therapy is necessary, plasma lithium should be carefully monitored at the start of treatment, when adjusting the dose, and after discontinuing meloxicam. Methotrexate. NSAIDs can reduce the tubular secretion of methotrexate, thereby increasing its plasma concentration. In this regard, the simultaneous use of meloxicam and methotrexate at a dose of more than 15 mg / week is not recommended. The risk of interaction between NSAIDs and methotrexate may also occur in patients using low-dose methotrexate, especially in patients with impaired renal function. Therefore, constant monitoring of blood parameters and kidney function is necessary. With the combined use of meloxicam and methotrexate for 3 days, the risk of increasing the toxicity of the latter increases. Although the pharmacokinetics of methotrexate (15 mg/week) did not change with concomitant treatment with meloxicam, it should be considered that the hematological toxicity of methotrexate may increase with the treatment of NSAIDs. Pemetrexed. If meloxicam and pemetrexed are to be co-administered in patients with mild to moderate renal impairment (creatinine clearance 45-79 ml/min), meloxicam should not be taken for at least 5 days prior to pemetrexed administration, on the day of administration, and for 2 days after administration of pemetrexed. If the combination of meloxicam and pemetrexed is necessary, careful monitoring of the patient is recommended, especially due to myelosuppression and gastrointestinal side effects. In patients with severe renal insufficiency (creatinine clearance < 45 ml / min), the simultaneous use of meloxicam and pemetrexed is not recommended. In patients with normal renal function (creatinine clearance ? 80 ml/min), the use of meloxicam at a dose of 15 mg may lead to a decrease in the clearance of pemetrexed and, consequently, an increase in its side effects. Thus, concomitant use of meloxicam 15 mg and pemetrexed in patients with normal renal function (creatinine clearance ≥ 80 ml/min) should be used with caution. cholestyramine. Cholestyramine accelerates the elimination of meloxicam by reducing the enterohepatic circulation, which leads to an increase in meloxicam clearance by 50% and a decrease in the elimination half-life to 13 ± 3 hours. This interaction is clinically significant. There were no clinically significant pharmacokinetic interactions when taken simultaneously with antacids, cimetidine and digoxin. Contraindications hypersensitivity reactions to meloxicam or any of the excipients or hypersensitivity to substances with a similar effect, for example, NSAIDs, acetylsalicylic acid. Meloxicam should not be prescribed to patients who have experienced symptoms of bronchial asthma, polyps of the nasal mucosa, angioedema or urticaria after the administration of acetylsalicylic acid. acids or other NSAIDs; history of gastrointestinal bleeding or perforation of the gastrointestinal tract (GIT) associated with previous NSAID therapy; active phase or recurrent gastrointestinal ulcers/bleeds (two or more separate episodes in which the presence of an ulcer or bleeding is confirmed); severe impairment of function liver; severe renal failure without dialysis; gastrointestinal bleeding, cerebrovascular bleeding or other blood clotting disorders in history; third trimester of pregnancy; children and adolescents under 16 years of age; severe heart failure. Composition 1 tablet contains: active substance - meloxicam - 7.5 mg or 15 mg; excipients: microcrystalline cellulose, lactose monohydrate, sodium citrate, anhydrous colloidal silicon dioxide, povidone, crospovidone, magnesium stearate. Overdose Symptoms of acute NSAID overdose are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with maintenance therapy. Gastrointestinal bleeding may occur. Severe poisoning may be accompanied by arterial hypertension, acute renal failure, liver dysfunction, respiratory depression, coma, convulsions, cardiovascular failure and cardiac arrest. Anaphylactoid reactions have been reported with the therapeutic use of NSAIDs, which can also occur with overdose. Treatment: no known antidote. In case of drug overdose, symptomatic therapy should be used. The study showed an acceleration of the elimination of meloxicam with oral administration of 4 g of cholestyramine in 3 doses per day. Side effectEstimation of undesirable effects is based on the following data on the frequency of occurrence: very often (? 1/10), often (? 1/100 to <1/10), infrequently (? 1/1000 to <1/100), rarely (? 1/10,000 to <1/1000), very rare (<1/10,000), not known (cannot be estimated from the available data). Blood and lymphatic system disorders: infrequently: anemia; rarely: abnormal blood test values (including changes in the number of leukocytes), leukopenia, thrombocytopenia. Very rare cases of agranulocytosis have been reported. Immune system disorders: infrequently: allergic reactions, excluding anaphylactic and anaphylactoid ones; unknown: anaphylactic shock, anaphylactic reactions, anaphylactoid reactions. Psychiatric disorders: rarely: mood changes, nightmares; unknown: confusion, disorientation. Nervous system disorders: often: headache; infrequently: dizziness, drowsiness. On the part of the organ of vision: rarely - impaired visual function, including blurred vision; conjunctivitis. On the part of the organ of hearing and labyrinth disorders: infrequently: dizziness; rarely: ringing in the ears. Cardiac disorders: Rare: palpitations. Heart failure associated with the use of NSAIDs has been reported. Vascular disorders: infrequently: increased blood pressure, hot flashes. Respiratory, thoracic and mediastinal disorders: rare: asthma in patients allergic to acetylsalicylic acid and other NSAIDs. From the gastrointestinal tract: very often: dyspepsia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequently: latent or macroscopically visible gastrointestinal bleeding, stomatitis, gastritis, belching; rarely: colitis, gastroduodenal ulcer, esophagitis; very rarely: perforation of the gastrointestinal tract. Gastrointestinal bleeding, ulcers, or perforation can be severe and potentially fatal, especially in elderly patients. On the part of the liver and biliary tract: infrequently: abnormal liver function tests (for example, increased transaminases or bilirubin); very rare: hepatitis. Skin and subcutaneous tissue disorders: infrequently: angioedema, itching, rash; rarely: Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria; very rarely: bullous dermatitis, erythema multiforme; unknown: photosensitivity. From the urinary tract: infrequently: sodium and water retention, hyperkalemia, changes in laboratory tests of kidney function (increased creatinine and / or urea in the blood serum); very rarely: acute renal failure, in particular in patients with risk factors. General disorders and reactions at the injection site: infrequently: edema, including swelling of the lower extremities. Selected Serious and/or Common Adverse Reactions Very rare cases of agranulocytosis have been reported in patients treated with meloxicam and other potentially myelotoxic drugs. Adverse reactions not associated with the use of the drug, but which are generally characteristic of other compounds in this class Organic kidney damage, which probably leads to acute renal failure: Very rare cases of interstitial nephritis, acute tubular necrosis, nephrotic syndrome and papillary necrosis. Medical workers are recommended to send information about any suspected adverse reactions and ineffectiveness of the medicinal product to the address: Republican Unitary Enterprise "Center for Expertise of Tests in Healthcare", Tovarishchesky per., 2a, 220037, Republic of Belarus Storage conditions In a place protected from light and moisture, at a temperature not above 25 °C. Keep out of the reach of children. Buy Meloxicam tablets 7.5 mg No. 10x2 Price for Meloxicam tablets 7.5 mg No. 10x2