Movalis injection solution 15mg 1,5ml ampoule 1,5ml N3
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Active ingredients
Meloxicam
Release form
Solution
Composition
1 vial (1.5 ml) contains: active ingredient: meloxicam - 15.0 mg; excipients: meglumine - 9.375 mg, glycofurfurol - 150 mg, poloxamer 188–75 mg, sodium chloride - 4.5 mg, glycine - 7.5 mg, sodium hydroxide - 0.228 mg, water for injection - 1279.482 mg. ;
Pharmacological effect
Movalis is a nonsteroidal anti-inflammatory drug (NSAID), it is derived from enolic acid and has anti-inflammatory, analgesic and antipyretic effects .; A 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 cyclooxygenase-2 (COX-2) compared with cyclooxygenase-1 (COX-1). Inhibition of COX-2 is believed to provide the therapeutic effects of NSAIDs, whereas inhibition of a constantly present COX-1 isoenzyme may be responsible for 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 and 15 mg) more actively inhibited COX-2, having 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 by COX-1). These effects depended on the magnitude of the dose .; Ex vivo studies have shown that meloxicam (at doses of 7.5 mg and 15 mg) does not affect platelet aggregation and bleeding time .; In clinical studies, side effects from the gastrointestinal tract in general occurred less frequently when taking meloxicam in doses of 7.5 and 15 mg, than when taking other NSAIDs, which were compared. This difference in the frequency of side effects from the gastrointestinal tract is mainly due to the fact that when 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 completely absorbed after i / m administration. Relative bioavailability compared with bioavailability when administered orally is almost 100%. Therefore, when switching from injecting to oral forms, dose selection is not required. After i / m administration of the drug in a dose of 15 mg max is 1.6-1.8 mcg / ml and is reached in approximately 60-90 minutes; Distribution; Meloxicam binds very well to plasma proteins, mainly albumin (99%). Penetrates into the synovial fluid, the concentration in the synovial fluid is approximately 50% concentration in plasma. Vd low, an average of 11 liters. Inter-individual differences are 7-20% .; 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%, respectively, of the dose), 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 13-25 hours. Plasma clearance averages 7-12 ml / min after a single use .; Meloxicam demonstrates linear pharmacokinetics in doses of 7.5-15 mg with i / m administration .; Pharmacokinetics in special clinical situations; Insufficiency of liver function, as well as poorly or moderately severe renal insufficiency, does not significantly affect 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 long T1 / 2, compared with younger patients of both sexes.
Indications
Starting therapy and short-term symptomatic treatment for: - Osteoarthritis (arthrosis, degenerative diseases of the joints); - rheumatoid arthritis; - ankylosing spondylitis; - other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathies of dorsopathy (for example, sciatica, lower back pain, shoulder periarthritis, and others), accompanied by pain .;
Contraindications
- hypersensitivity to the active ingredient or auxiliary components of the drug; - hypersensitivity (including to other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs due to the existing likelihood of cross-sensitivity (in t. hours in history;); - erosive and ulcerative lesions of the stomach and duodenum in the acute phase or recently transferred; - inflammatory bowel disease (Crohn's disease or ulcerative colitis in the acute stage); - severe hepatic and heart failure; - severe renal failure (if hemodialysis is not performed, CC <30 ml / min, and also with confirmed hyperkalemia); - active liver disease; - active gastrointestinal bleeding, recent cerebrovascular bleeding, or an established diagnosis of diseases of the blood coagulation system; - associated therapy with anticoagulants, because there is a risk of intramuscular hematomas; - therapy of perioperative pain during coronary artery bypass surgery; - pregnancy; - lactation period (breastfeeding); - age up to 18 years old .;
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 that inhibits cyclooxygenase / prostaglandin synthesis, Movalis may affect fertility and is therefore 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 administered by deep intramuscular injection. The drug should not be administered in / in .; V / m administration of the drug is shown only during the first few days of therapy. Further treatment is continued with the use of oral dosage forms .; The recommended dose is 7.5 mg or 15 mg 1 time / day, depending on the intensity of pain and the severity of the inflammatory process .; Osteoarthritis with pain syndrome: 7.5 mg / day. If necessary, the dose may be increased to 15 mg / day; Rheumatoid arthritis: 15 mg / day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg / day; Ankylosing spondylitis: 15 mg / day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg / day; 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 .; The maximum recommended daily dose is 15 mg. In patients with severe renal insufficiency who are on hemodialysis, the dose should not exceed 7.5 mg / day; Combined use; Do not use the drug simultaneously with other NSAIDs .; The total daily dose of Movalis, used in the form of different dosage forms should not exceed 15 mg. Given the possible incompatibility, Movalis solution for i / m injection should not be mixed in the same syringe with other drugs .;
Side effects
Below are described the side effects, the relationship of which with the use of the drug Movalis,regarded as possible .; 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 hemopoietic system: infrequently - anemia; rarely - leukopenia, thrombocytopenia, changes in the number of blood cells, including changes in the leukocyte formula .; On the part of the immune system: infrequently - other immediate type hypersensitivity reactions; frequency not established - anaphylactic shock, anaphylactoid / anaphylactic reactions .; From the nervous system: often - headache; infrequently - dizziness, drowsiness .; On the part of the psyche: rarely - changes in mood; frequency is not installed - confusion, disorientation .; From the senses: infrequently - vertigo; rarely - conjunctivitis, visual impairment, including blurred vision, tinnitus .; Since the cardiovascular system: infrequently - increase blood pressure, a sense of "tide" of blood to the face; seldom - heartbeat .; On the part of the respiratory system: rarely - bronchial asthma (in patients with allergies to acetylsalicylic acid or other NSAIDs) .; From the digestive 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 .; On the part of the liver and biliary tract: infrequently - transient changes in indicators of liver function (for example, increased activity of transaminases or bilirubin); very rarely - hepatitis .; From the skin and subcutaneous tissues: infrequently - angioedema, itching, 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 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 .; General disorders and disorders at the injection site: often - pain and swelling at the injection site; infrequently - swelling .; Combined use with drugs that inhibit the bone marrow (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, and 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 in severe cases will be present: drowsiness, disturbances of 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 drug overdose, symptomatic therapy should be used. It is known that Kolestiramine 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 the concentration of lithium in the plasma, 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 by the kidneys, 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 .; 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 .; 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 .; NSAIDs, by acting on renal prostaglandins, can enhance cyclosporine nephrotoxicity .; 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 hypoglycemic 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 meloxicam with 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 alarming symptoms or a history of serious gastrointestinal complications, or in their absence. The consequences of these complications are generally more severe for 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. If the first signs of skin rash, mucous membranes or other signs of hypersensitivity appear, the issue of Movalis should be discontinued; 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 .; Before starting treatment, renal function testing is necessary. 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 serum transaminase activity or other indicators of liver function is possible. In most cases, this increase was small and transient. If the identified changes are significant or do not diminish over 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, and therefore, such patients should be carefully monitored .; Like other NSAIDs, Movalis can mask the symptoms of the underlying 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 withdrawn; In patients with weak and moderate renal failure (CK> 25 ml / min), dose adjustment is not required .; 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. During treatment, patients need to be careful when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions .;