Movalis pills 7.5 mg 20 pcs
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Active ingredients
Meloxicam
Release form
Pills
Composition
1 tablet contains; Active ingredient: meloxicam - 7.5 mg; Excipients: sodium citrate dihydrate - 15 mg (30 mg), lactose monohydrate - 23.5 mg (20 mg), microcrystalline cellulose - 102 mg (87.3 mg ), povidone K25 - 10.5 mg (9 mg), colloidal silicon dioxide - 3.5 mg (3 mg), crospovidone - 16.3 mg (14 mg), magnesium stearate - 1.7 mg.
Pharmacological effect
Non-steroidal anti-inflammatory drug (NSAIDs), is a derivative of enolic acid and has anti-inflammatory, analgesic and antipyretic effects. The pronounced anti-inflammatory effect of meloxicam is established on all standard models of inflammation .; The mechanism of action of meloxicam is its ability to inhibit the synthesis of prostaglandins - known inflammatory mediators .; Meloxicam in vivo inhibits the synthesis of prostaglandins at the site of inflammation to a greater extent than in the gastric mucosa or kidneys. These differences are associated with more selective inhibition of COX-2 compared with COX-1. Inhibition of COX-2 is believed to provide the therapeutic effect of NSAIDs, whereas inhibition of a constantly present COX-1 isoenzyme may be the cause of side effects from the stomach and kidneys .; The selectivity of meloxicam with respect to COX-2 was confirmed in various test systems, both in vitro and in vivo. The selective ability of meloxicam to inhibit COX-2 is shown when using in vitro human whole blood as a test system. It was found that meloxicam (at doses of 7.5 mg) more actively inhibited COX-2, exerting a greater inhibitory effect on the production of prostaglandin E2, stimulated by lipopolysaccharide (reaction controlled by COX-2) than on the production of thromboxane involved in the process of blood coagulation (reaction controlled COX-1). These effects depended on the magnitude of the dose. Ex vivo studies have shown that meloxicam (at a dose of 7.5 mg) did not affect platelet aggregation and bleeding time .; In clinical studies, side effects from the gastrointestinal tract in general occurred less frequently when taking meloxicam 7.5 mg than when taking other NSAIDs, which were compared. This difference in the frequency of side effects from the gastrointestinal tract, mainly due to the fact that while taking meloxicam, such phenomena as dyspepsia, vomiting, nausea, abdominal pain were less common.The frequency of perforations in the upper GI tract, ulcers and bleeding, which were associated with the use of meloxicam, was low and depended on the dose of the drug.
Pharmacokinetics
Suction; Meloxicam is well absorbed from the gastrointestinal tract, as evidenced by the high absolute bioavailability (90%) after oral administration. After a single use of meloxicam max in plasma is achieved within 5-6 hours. Simultaneous ingestion of food and inorganic antacids does not alter absorption. When using the drug inside (in doses of 7.5 and 15 mg), its concentration is proportional to the dose. The steady state pharmacokinetics is achieved within 3-5 days. The range of differences between max and min of the drug after its administration 1 time / day is relatively small and amounts to 0.4-1.0 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, Cmin values are given and Cmax in the period of steady state pharmacokinetics), although values outside the specified range were also noted. Cmax in the plasma during the steady state pharmacokinetics is achieved within 5-6 hours after ingestion .; Distribution; Meloxicam binds very well to plasma proteins, especially albumin (99%). Penetrates into the synovial fluid, the concentration in the synovial fluid is approximately 50% concentration in plasma. Vd after repeated oral administration of meloxicam (in doses from 7.5 mg to 15 mg) is about 16 liters, with a coefficient of variation from 11 to 32%; Metabolism; Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive derivatives. 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). In vitro studies have shown that the CYP2C9 isoenzyme plays an important role in this metabolic transformation, CYP3A4 isoenzyme plays an additional role. Peroxidase is involved in the formation of two other metabolites (constituting 16% and 4% of the dose of the drug, respectively), the activity of which probably varies individually .; Derivation; It is excreted equally through the intestines and the kidneys, mainly in the form of metabolites. In an unchanged form with feces less than 5% of the daily dose is excreted, in the urine the drug is found in unchanged form only in trace amounts. The average T1 / 2 meloxicam varies from 13 to 25 hours.Plasma clearance averages 7-12 ml / min after a single dose of meloxicam .; Pharmacokinetics in special clinical situations; Insufficiency of liver function, as well as poorly expressed renal insufficiency, does not have a significant effect on the pharmacokinetics of meloxicam. The rate of elimination of meloxicam from the body is significantly higher in patients with moderately severe renal insufficiency. Meloxicam binds worse to plasma proteins in patients with end-stage renal disease. In terminal renal failure, an increase in Vd can lead to higher concentrations of free meloxicam, therefore, in these patients the daily dose should not exceed 7.5 mg. Elderly patients compared with young patients have similar pharmacokinetic indicators. In elderly patients, the mean plasma clearance during the period of equilibrium pharmacokinetics is slightly lower than in younger patients. Older women have higher AUC values and a longer T1 / 2, compared with younger patients of both sexes.
Indications
Symptomatic treatment: - osteoarthritis (arthrosis, degenerative diseases of the joints), including with a pain component; - rheumatoid arthritis; - ankylosing spondylitis; - other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathies, dorsopathies (for example, sciatica, lower back pain, shoulder periarthritis), accompanied by pain .;
Contraindications
- A complete or incomplete combination of asthma, recurrent nasal polyposis and paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs (including a history of) due to the current likelihood of cross-sensitivity; - erosive and ulcerative lesions of the stomach and duodenum in the acute stage or recently transferred; - inflammatory bowel disease (Crohn's disease or ulcerative colitis in the acute stage); - severe liver failure; - severe renal failure (if hemodialysis is not performed, CC <30 ml / min, and also with confirmed hyperkalemia); - progressive kidney disease; - active gastrointestinal bleeding,recent cerebrovascular hemorrhage or an established diagnosis of coagulation disorders; - severe uncontrolled heart failure; - therapy of perioperative pain during coronary artery bypass surgery; - pregnancy; - lactation period (breastfeeding); - children's age up to 12 years; - rare hereditary intolerance to galactose (the maximum daily dose of the drug with a dosage of meloxicam 7.5 mg and 15 mg contains 47 mg and 20 mg of lactose, respectively); - Hypersensitivity to the active substance or auxiliary components of the drug.
Use during pregnancy and lactation
The use of the drug Movalis is contraindicated in pregnancy .; It is known that NSAIDs penetrate into breast milk, so the use of Movalis during breastfeeding is contraindicated .; As a drug inhibiting the synthesis of cyclooxygenase / prostaglandin, Movalis may affect fertility, and therefore is not recommended for women planning a pregnancy. Meloxicam can lead to delayed ovulation. In this regard, for women who have problems with conception and are being examined for similar problems, it is recommended that Movalis be discontinued.
Dosage and administration
The drug is taken orally 1 time / day, with meals, drinking water or other liquid .; In osteoarthritis with pain, the daily dose is 7.5 mg, if necessary, the dose can be increased to 15 mg / day; In rheumatoid arthritis, the drug is prescribed at a dose of 15 mg / day, depending on the therapeutic effect, the dose may be reduced to 7.5 mg / day. In ankylosing spondylitis, the drug is prescribed at a dose of 15 mg / day, depending on the therapeutic effect, the dose may be reduced to 7.5 mg / day. The maximum recommended daily dose is 15 mg. In patients with an increased risk of adverse reactions (a history of gastrointestinal diseases, the presence of risk factors for cardiovascular diseases), it is recommended to begin treatment with a dose of 7.5 mg / day; Since the potential risk of adverse reactions depends on the dose and duration of treatment; the minimum effective dose should be prescribed for the shortest possible course .; In patients with severe renal failure on hemodialysis,The dose of Movalis should not exceed 7.5 mg / day. The maximum dose in adolescents aged 12–18 years is 0.25 mg / kg and should not exceed 15 mg. The use of the drug is contraindicated in children under 12 years of age, due to the impossibility of selecting the appropriate dose for this age group .; Combined use; Do not use the drug simultaneously with other NSAIDs .; The total dose of Movalis, used in the form of different dosage forms, should not exceed 15 mg / day.
Side effects
Below are described the side effects, the connection of which with the use of Movalis was regarded as possible .; The side effects, registered with post-marketing use, which connection with the drug intake was regarded as possible, are marked with *; Inside the systemic organ classes, the following categories are used by the frequency of occurrence of side effects: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10,000, <1/1000); very rarely (<1/10 000); not installed.; From the side of blood and lymphatic system: infrequently - anemia; rarely, changes in the number of blood cells, including changes in leukocyte formula, leukopenia, thrombocytopenia .; On the part of the immune system: infrequently - other immediate type hypersensitivity reactions *; frequency not established - anaphylactic shock *, anaphylactoid reactions * .; From the nervous system: often - headache; infrequently - dizziness, drowsiness .; Mental Disorders: Often - Mood Changes *; frequency not set - confusion *, disorientation * .; From the senses: infrequently - vertigo; rarely, conjunctivitis *, visual impairment, including blurred vision *, tinnitus .; On the part of the gastrointestinal tract: often - abdominal pain, dyspepsia, diarrhea, nausea, vomiting; infrequently - latent or overt gastrointestinal bleeding, gastritis *, stomatitis, constipation, abdominal distention, belching; rarely - gastroduodenal ulcers, colitis, esophagitis; very rarely - gastrointestinal perforation .; From the side of the liver: infrequently - transient changes in indicators of liver function (for example, increased transaminase activity or bilirubin concentration); very rarely - hepatitis * .; On the part of the skin and subcutaneous tissues: infrequently - angioedema, pruritus, skin rash; rarely, toxic epidermal necrolysis *, Stevens-Johnson syndrome *, urticaria; very rarely - bullous dermatitis *,erythema multiforme *; frequency not established - photosensitization .; On the part of the respiratory system: rarely - bronchial asthma in patients with allergies to acetylsalicylic acid or other NSAIDs .; Since the cardiovascular system: infrequently - increase blood pressure, a sense of "tide" of blood to the face; rarely, palpitations .; On the part of the urinary system: infrequently - changes in renal function (increased creatinine and / or urea in the blood serum), urinary disorders, including acute urinary retention *; very rarely - acute renal failure * .; On the part of the genital organs and the mammary gland: infrequently - late ovulation *; frequency not established - infertility in women * .; Combined use with drugs that inhibit bone marrow hematopoiesis (for example, methotrexate) can provoke cytopenia .; Gastrointestinal bleeding, an ulcer or perforation can be fatal .; As with other NSAIDs, the possibility of interstitial nephritis, glomerulonephritis, renal medullary necrosis, nephrotic syndrome is not excluded .;
Overdose
Data on cases associated with overdose of the drug has been accumulated insufficiently. It is likely that symptoms characteristic of an NSAID overdose will be present in severe cases: drowsiness, impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, changes in blood pressure, respiratory arrest, asystole .; Treatment: the antidote is not known, in case of an overdose of the drug should be evacuated stomach contents and general supportive therapy. Kolestyramine accelerates the elimination of meloxicam .;
Interaction with other drugs
With the simultaneous use of other prostaglandin synthesis inhibitors with meloxicam, including GCS and salicylates, increases the risk of gastrointestinal ulcers and gastrointestinal bleeding (due to synergism of action). The simultaneous use of meloxicam and other NSAIDs is not recommended .; Anticoagulants for oral administration, heparin for systemic use, thrombolytic agents with simultaneous use with meloxicam increase the risk of bleeding. In the case of simultaneous use, careful control of the blood coagulation system is necessary .; Anti-platelet drugs, serotonin reuptake inhibitors, while used with meloxicam, increase the risk of bleeding due to inhibition of platelet function.In the case of simultaneous use, careful control of the blood coagulation system is necessary .; NSAIDs increase plasma lithium concentration by reducing its excretion by the kidneys. The simultaneous use of meloxicam with lithium preparations is not recommended. If necessary, the simultaneous use of recommended careful monitoring of the concentration of lithium in the plasma during the entire course of the use of lithium preparations .; NSAIDs reduce tubular secretion of methotrexate, thereby increasing its concentration in plasma. The simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. In the case of simultaneous use, careful monitoring of renal function and blood formula is necessary. Meloxicam may increase the hematological toxicity of methotrexate, especially in patients with impaired renal function. With the combined use of meloxicam and methotrexate for 3 days increases the risk of increased toxicity of the latter .; There is evidence that NSAIDs may reduce the effectiveness of intrauterine contraceptive devices, but this has not been proven .; The use of NSAIDs in the presence of diuretics in the event of dehydration of patients is accompanied by the risk of developing acute renal failure .; NSAIDs reduce the effect of antihypertensive drugs (beta-blockers, ACE inhibitors, vasodilators, diuretics) due to inhibition of prostaglandins with vasodilating properties .; The combined use of NSAIDs and angiotensin II receptor antagonists, as well as ACE inhibitors, enhances the effect of reducing glomerular filtration, thereby leading to the development of acute renal failure, especially in patients with impaired renal function .; Kolestyramine, binding meloxicam in the digestive tract, leads to its more rapid elimination .; NSAIDs, by acting on renal prostaglandins, can enhance cyclosporine nephrotoxicity .; In patients with CK from 45 to 79 ml / min, the use of meloxicam should be stopped 5 days before the start of taking pemetrexed and it is possible to resume 2 days after the end of taking pemetrexed. If there is a need to use meloxicam and pemetrexed together, then patients should be carefully monitored, especially with regard to myelosuppression and the occurrence of gastrointestinal side effects.In patients with QA <45 ml / min, the use of meloxicam together with pemetrexed is not recommended .; When drugs are applied simultaneously with meloxicam, which have a known ability to inhibit CYP2C9 and / or CYP3A4 (or are metabolized with these enzymes), such as sulfonylurea derivatives or probenecid, the possibility of pharmacokinetic interaction should be taken into account .; When used together with antidiabetic agents for oral administration (for example, sulfonylurea derivatives, nateglinide), CYP2C9-mediated interaction may occur, which may lead to an increase in the concentration of both hypoglycemic agents and meloxicam in the blood. Patients simultaneously taking meloxicam with sulfonylurea or nateglinide should be carefully monitored for blood glucose concentration due to the possibility of hypoglycemia.; With the simultaneous use of antacids, cimetidine, digoxin and furosemide, no significant pharmacokinetic interaction has been identified.
special instructions
Patients with gastrointestinal diseases should be monitored regularly. In the event of ulceration of the gastrointestinal tract or gastrointestinal bleeding Movalis must be canceled .; Gastrointestinal ulcers, perforation, or bleeding can occur during the use of NSAIDs at any time, if there are warning signs or information about a history of serious gastrointestinal complications, or in the absence of these signs. The consequences of these complications are generally more severe in the elderly. With the use of Movalis, serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis may develop. Therefore, special attention should be paid to patients reporting the development of adverse events on the skin and mucous membranes, as well as hypersensitivity reactions to the drug, especially if similar reactions have been observed during previous courses of treatment. The development of such reactions is observed, as a rule, during the first month of treatment. In the event of the first signs of skin rash, changes in mucous membranes or other signs of hypersensitivity, the issue of discontinuation of Movalis should be considered; Cases of increasing the risk of developing serious cardiovascular thrombosis, myocardial infarction, an attack of angina pectoris, possibly fatal, while taking NSAIDs are described.This risk increases with long-term use of the drug, as well as in patients with the above mentioned diseases in history and predisposed to such diseases .; NSAIDs inhibit kidney synthesis of prostaglandins, which are involved in maintaining renal perfusion. The use of NSAIDs in patients with reduced renal blood flow or reduced BCC can lead to decompensation of latent renal failure. After abolishing NSAIDs, 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 acute renal dysfunction, patients simultaneously receiving diuretics, ACE inhibitors, angiotensin II receptor antagonists, and also patients who have undergone serious surgery that leads to hypovolemia. In these patients, diuresis and renal function should be carefully monitored at the start of therapy. The use of NSAIDs in conjunction with diuretics can lead to sodium, potassium and water retention, as well as to a decrease in the natriuretic effect of diuretics. As a result, in predisposed patients, signs of heart failure or arterial hypertension may increase. Therefore, careful monitoring of the condition of these patients is necessary, as well as the maintenance of adequate hydration. A study of renal function is needed before treatment begins; In the case of combination therapy, renal function should also be monitored .; When using the drug Movalis (as well as most other NSAIDs), an episodic increase in transaminase activity 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 diminish with time, Movalis should be reversed and monitoring for the identified laboratory changes should be carried out .; Weakened or exhausted patients may be worse tolerated by adverse events, so these patients require careful observation. Like other NSAIDs, Movalis can mask the symptoms of an infectious disease .; As a drug that inhibits the synthesis of COX / prostaglandin, Movalis may affect fertility, and therefore is not recommended for women who have difficulty conceiving.For women undergoing screening for this, it is recommended that Movalis be discontinued; Patients with renal failure of mild and moderate (CK> 25 ml / min) do not require dose adjustment .; Patients with liver cirrhosis (compensated) do not require dose adjustment .; Influence on ability to drive motor transport and control mechanisms; Special clinical studies of the effect of the drug on the ability to drive and mechanisms were not conducted. However, when driving and working with mechanisms, the possibility of developing dizziness, drowsiness, visual impairment or other disorders of the central nervous system should be taken into account. Patients should be careful when driving and operating machinery .;