Properties
- Form
- khsnari
- Dosage mg
- 15
- Pack
- 5
What is it?
Composition: 1 ml of solution contains: Active substance: Meloxicam 10 mg; Excipients: Meglumine, Glycofurol, Poloxamer 188, Glycine, Sodium Chloride, Sodium Hydroxide, Water for Injection. Pharmacotherapeutic group: Anti-inflammatory and antirheumatic drugs. Non-steroidal anti-inflammatory drugs. Oxicams. Meloxicam. ATC code: M01AC06 Pharmacological properties: Pharmacodynamics: Reclin is a non-steroidal anti-inflammatory drug (NSAID) of the oxicam group, possessing anti-inflammatory, analgesic, and antipyretic effects. The mechanism of the above-mentioned effects is related to meloxicam's ability to inhibit the synthesis of inflammatory mediators – prostaglandins. The ability to selectively inhibit, meaning predominantly inhibiting the specific enzyme cyclooxygenase-2 (COX-2), which participates in the development of inflammation, is important in the mechanism of action. It is believed that COX-2 inhibition provides the therapeutic effect of NSAIDs, while inhibition of the constitutively present isoenzyme COX-1 may be the cause of side effects on the stomach and kidneys. Meloxicam's selectivity towards COX-2 has been confirmed in various test systems, both in vitro and in vivo. The incidence of perforation, ulcers, and bleeding in the upper gastrointestinal tract (GIT) associated with meloxicam intake was found to be low and dose-dependent. Pharmacokinetics: Relative bioavailability is almost 100%. After intramuscular administration of a 5 mg dose, the maximum concentration (Cmax) is 1.62 mcg/ml and is reached in approximately 60 minutes. Meloxicam is well bound to plasma proteins, especially albumin (99%). It reaches synovial fluid, with the concentration in synovial fluid being approximately 50% of the plasma concentration. The volume of distribution (Vd) is low, averaging 11 L. Inter-individual variation is 30-40%. Meloxicam is almost completely metabolized in the liver to form 4 pharmacologically inactive derivatives. The main metabolite, 5'-carboxy meloxicam (60% of the dose), is formed by oxidation of the intermediate metabolite 5'-hydroxy-methyl meloxicam, which is also excreted, but to a lesser extent (9% of the dose). In vitro studies have shown that the isoenzyme CYP2C9 plays a significant role in this metabolic transformation, with CYP3A4 isoenzyme having additional importance. Peroxidase, whose activity is likely to vary individually, participates in the formation of two other metabolites (which account for 16% and 4% of the dose, respectively). It is excreted in equal amounts in feces and urine, primarily in the form of metabolites. Unchanged drug is excreted in feces in less than 5% of the daily dose; the unchanged drug is found in urine only in trace amounts. The mean elimination half-life (T½) is 20 hours. Plasma clearance averages 8 ml/min. Following intramuscular administration of doses of 7.5-15 mg, meloxicam exhibits linear pharmacokinetics. Moderate hepatic or renal insufficiency does not significantly affect the pharmacokinetics of meloxicam. Indications for use: Symptomatic treatment of pain syndrome in osteoarthritis (arthrosis, degenerative joint diseases), rheumatoid arthritis, ankylosing spondylitis. Contraindications: • Hypersensitivity to meloxicam or other components of the preparation; • Hypersensitivity to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (history of bronchial asthma, nasal polyps, angioedema, urticaria after acetylsalicylic acid or other NSAIDs); • Patients taking anticoagulants (risk of intramuscular hematoma development); • Erosive-ulcerative changes/perforation of the gastric and duodenal mucosa (in the exacerbation phase, or recently transferred); • Non-specific ulcerative colitis in the exacerbation phase, Crohn's disease; • Severe hepatic insufficiency, acute stage of liver diseases; • Gastrointestinal bleeding, recent cerebrovascular bleeding, or systemic blood clotting disorders; • Progressive kidney diseases, severe renal insufficiency (if hemodialysis is not performed), creatinine clearance less than 30 ml/min; • Decompensated heart failure; • Postoperative pain syndrome after aortocoronary bypass surgery; • Children and adolescents under 18 years of age; • Pregnancy and lactation. Method and dosage of administration: Reclin solution for injection is intended for intramuscular administration only. Intravenous administration of the solution is contraindicated. Intramuscular administration is used in the first days of therapy. Subsequently, the preparation is taken orally in tablet form. In case of osteoarthritis exacerbation, 7.5 mg is prescribed once a day. If the therapeutic effect is insufficient, the dose can be increased to 15 mg. For Bechterew's disease and rheumatoid arthritis – 15 mg once a day. If a sufficient therapeutic effect is observed, the daily dose is reduced to 7.5 mg once a day. Exceeding the recommended daily dose of Reclin of 15 mg is not recommended. Considering possible incompatibilities, the contents of Reclin ampoules should not be mixed with other medicinal products in the same syringe. In patients with an increased risk of side reactions and severe renal insufficiency on hemodialysis, the dose should not exceed 7.5 mg per day. The dosage regimen of Reclin for intravenous injections in children and adolescents has not yet been determined; this dosage form can only be used in adult patients. Maximum recommended daily dose – 15 mg. Side effects: From the digestive system: nausea, vomiting, abdominal pain, constipation, diarrhea, meteorism, temporary disturbances of liver function biochemical parameters (increased transaminases or bilirubin), belching, erosive-ulcerative lesions of the GIT, occult or manifest gastrointestinal bleeding, stomatitis; From the hematopoietic system: changes in blood count, anemia, leukopenia and thrombocytopenia; From the CNS: dizziness, headache, tinnitus, drowsiness; From the cardiovascular system: increased blood pressure, "hot flashes", palpitations, edema; From the urinary system: changes in kidney function parameters (increased serum creatinine and/or urea); Allergic reactions: bronchospasm, photosensitization, itching, rash, urticaria. Overdose: Symptoms: nausea, vomiting, abdominal pain, intensification of other side effects of the preparation. Treatment: Conducted according to the symptoms of intoxication and the severity of overdose. Oral administration of 4000 mg of cholestyramine three times increases the elimination rate of meloxicam. Interaction with other medicinal products: When used with other NSAIDs (including acetylsalicylic acid), the risk of erosive-ulcerative lesions and bleeding in the GIT increases. When used with hypotensive drugs, the effectiveness of the latter may decrease. When used with lithium preparations, lithium accumulation and increased toxic effects may develop (control of lithium concentration in blood is recommended). When used with methotrexate, the side effects on the hematopoietic system are enhanced (risk of anemia and leukopenia, periodic control of complete blood count is indicated). When used with diuretics and cyclosporine, the risk of developing renal insufficiency increases. When used with intrauterine contraceptives, the effectiveness of the latter may decrease. When used with anticoagulants (heparin, ticlopidine, warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), as well as fibrinolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic control of blood clotting parameters is necessary). When used with selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases. Special instructions: Before prescribing Reclin, it is necessary to ensure the absence of esophagitis, gastritis, and/or peptic ulcer. Attention should be paid to patients taking meloxicam to prevent recurrence of these diseases. Like other NSAIDs, it should be used with caution in patients with diseases of the upper GIT, as well as in patients undergoing anticoagulant therapy. Ulcers, gastrointestinal bleeding, or perforation may develop with or without corresponding symptoms. In case of development of peptic ulcer or gastrointestinal bleeding, Reclin should be discontinued. Gastrointestinal bleeding, ulcers, or perforation can lead to severe and subsequently fatal outcomes, especially in elderly individuals. Special attention should be paid to patients who have developed adverse effects on the skin and mucous membranes; in such cases, the issue of discontinuing Reclin should be considered. Like NSAIDs, Reclin inhibits the synthesis of renal prostaglandins, which ensure the maintenance of renal blood flow at a sufficient dose. In patients with reduced circulating blood volume and renal perfusion, the administration of NSAIDs may accelerate the decompensation of renal function, although after withdrawal of NSAID therapy, renal function is restored to baseline levels. The risk of developing similar reactions is particularly high in patients with dehydration, congestive heart failure, liver cirrhosis, nephrotoxic syndrome, and severe kidney diseases who are taking diuretics, as well as after major surgery that caused hypovolemia. In such patients, careful monitoring of diuresis and renal function is necessary at the beginning of treatment. In rare cases, Reclin, like other NSAIDs, can cause interstitial nephritis, glomerulonephritis, renal medullary necrosis, or nephrotic syndrome. In rare cases, there have been reports of increased serum transaminase levels or other characteristic changes in liver function parameters; most deviations from normal were transient and insignificant. Dose reduction is not necessary in patients with clinically non-progressive liver cirrhosis. If deviations from normal are pronounced or persistent, Reclin administration should be discontinued and control laboratory tests should be performed. Weakened and debilitated patients tolerate side effects more severely; these patients require careful observation. Like other NSAIDs, Reclin should be used with caution in elderly patients who have more frequent impaired renal, hepatic, or cardiac function. Reclin may contribute to sodium, potassium, and water retention and weaken the natriuretic effect of diuretics. As a result, in the presence of predisposing factors, the administration of the preparation may lead to progression of heart failure and hypertension. Therefore, clinical observation is necessary in patients at risk. Like other NSAIDs, Reclin may mask the symptoms of infectious diseases. If the therapeutic effect is insufficient, exceeding the recommended daily dose and adding other NSAIDs for this treatment is not permissible, as they may increase the toxicity of these drugs, while their simultaneous use has not established therapeutic benefit. If there is no improvement within a few days, therapy correction is necessary. Like other NSAIDs, intramuscular injection may lead to abscess or necrosis at the injection site. Like other NSAIDs that block cyclooxygenase/prostaglandin synthesis, the use of Reclin may affect fertility, therefore it is not recommended for women who wish to become pregnant. Effect of the preparation on the ability to drive vehicles and operate machinery: No specific studies have been conducted on the effect of the preparation on the ability to drive vehicles and operate machinery. Patients with visual impairment, patients experiencing drowsiness, or other central nervous system disorders should refrain from these activities. Dosage form: 1.5 ml solution for injection in ampoules. 5 ampoules are placed in a cardboard box with instructions for use. Storage conditions: Store in a dry, protected from light place at a temperature not exceeding 25°C. Keep out of reach of children! Shelf life is indicated on the packaging. Do not use after the expiry date. Conditions of dispensing from pharmacies: Dispensed by prescription only.
