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Meloxicam (7.5 mg; 15 mg)

Pharmacodynamics

Meloxicam is a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the area of inflammation. When used in high doses, long-term use and individual characteristics of the organism, COX-2 selectivity decreases. Suppresses the synthesis of prostaglandins in the area of inflammation to a greater extent than in the gastric mucosa or kidneys, which is associated with relatively selective inhibition of COX-2. Less commonly causes erosive and ulcerative changes in the gastrointestinal tract (GIT). To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandins that protect the gastrointestinal mucosa and are involved in the regulation of blood flow in the kidneys.

Pharmacokinetics

Well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Concomitant food intake does not alter absorption. When using the drug orally in doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Equilibrium concentration is achieved within 3-5 days. With long-term use of the drug (more than 1 year), concentrations are similar to those observed after the first achievement of a steady state of pharmacokinetics.

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 is 0.4-1.0 mcg/ml when using a dose of 7.5 mg, and 0.8-2 when using a dose of 15 mg. 0 µg/ml (the values of Cmin and Cmax are given, respectively). Meloxicam penetrates histohematic barriers, the concentration in synovial fluid reaches 50% of the maximum concentration of the drug in plasma. Almost completely metabolized in the liver to form four pharmacologically inactive derivatives. The main metabolite, 5′-carboxy-meloxicam (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 CYP2C9 plays an important role in this metabolic transformation, and the CYPZA4 isoenzyme is of additional importance. Peroxidase is involved in the formation of the other two metabolites (constituting, respectively, 16% and 4% of the drug dose), the activity of which probably varies individually.

It is excreted equally through the intestines and kidneys, mainly in the form of metabolites.

Less than 5% of the daily dose is excreted unchanged through the intestines; the drug is found unchanged in urine only in trace amounts.

The half-life (T) of meloxicam is 1/2 15-20 hours. Plasma clearance averages 8 ml/min. In elderly people, drug clearance is reduced. The volume of distribution is low, averaging 11 liters.

Moderate hepatic or renal impairment does not significantly affect the pharmacokinetics of meloxicam.

Pharmacological properties of the drug Meloxicam-lugal

Anti-inflammatory, analgesic, antipyretic agent. The mechanism of action is due to the selective inhibition of COX-2, which leads to inhibition of the biosynthesis of proinflammatory prostaglandins at the site of inflammation. Due to its low affinity for COX-1, the drug in therapeutic doses does not have a negative effect on the biosynthesis of cytoprotective prostaglandins in the gastrointestinal tract and kidneys, and does not suppress the functional activity of platelets. It is a chondroneutral drug and does not affect the synthesis of proteoglycan by chondrocytes of articular cartilage. When taken orally, meloxicam is well adsorbed in the gastrointestinal tract, bioavailability is 89%. Concomitant food intake does not affect the absorption of the drug. The maximum concentration in the blood is achieved after 5–6 hours. A stable therapeutic concentration in the blood is achieved 3–5 days after the start of administration. Plasma protein binding is 99%. It undergoes biotransformation in the liver, mainly through oxidation with the formation of 4 inactive metabolites. The main role in the metabolism of meloxicam is played by the enzymes CYP 2CP and CYP 3A4, as well as peroxidase. The volume of distribution of the drug is low - on average 11 l, plasma clearance - 8 ml/min. The half-life is about 20 hours, which allows it to be taken once a day. Excretion from the body is carried out by the kidneys and intestines in equal proportions; 5% of the daily dose is excreted unchanged by the intestines. The drug passes through histohematic barriers and penetrates well into the synovial fluid, where its concentration is 50% of the level in the blood plasma. In elderly people, only a slight increase in the half-life of the drug and a decrease in plasma clearance are noted (especially in women). There were no significant changes in the pharmacokinetics of meloxicam and no increase in the risk of side effects when the drug was prescribed to patients with hepatic or moderate renal impairment (creatinine clearance 20–40 ml/min).

Use of the drug Meloxicam-lugal

Adults and adolescents over 15 years of age, taken orally during meals with a small amount of liquid. The dosage regimen is set individually, taking into account the intensity of the inflammatory process and the severity of the pain syndrome. For rheumatoid arthritis and ankylosing spondylitis, the drug is usually prescribed at a dose of 15 mg once a day; if a positive therapeutic effect is achieved, the dose can be reduced to 7.5 mg once a day. For osteoarthritis, the daily dose is 7.5 mg; if necessary, it is increased to 15 mg/day. The highest daily dose is 15 mg. In persons with an increased risk of side effects, in patients with renal failure or on hemodialysis, treatment should begin with a dose of 7.5 mg/day. In patients with moderate renal failure (creatinine clearance 25 ml/min), as well as in patients with clinically non-progressive liver cirrhosis, no dose reduction is required. The drug is not prescribed to children under 15 years of age.

Special instructions for the use of the drug Meloxicam-lugal

Prescribe with caution to patients with a history of gastric or duodenal ulcers, as well as to patients receiving anticoagulant therapy. If peptic ulcers or gastrointestinal bleeding occur, the drug should be discontinued. Caution should be used in elderly patients with impaired liver, kidney and heart function, as well as in debilitated and debilitated patients. If changes in liver function parameters occur, treatment with meloxicam should be discontinued and control laboratory tests should be performed. NSAIDs inhibit the synthesis of renal prostaglandins, which are involved in maintaining normal levels of renal blood flow. Therefore, when prescribing NSAIDs to patients with reduced renal blood flow or volume, there is a risk of developing decompensation of renal function. In rare cases, drugs in this group can provoke interstitial nephritis, glomerulonephritis, necrosis of the renal medulla, or nephrotic syndrome. The possible negative effect of NSAIDs on the kidneys must be taken into account when prescribing meloxicam to patients with dehydration, chronic heart failure, liver cirrhosis, nephrotic syndrome, severe renal impairment, as well as patients taking diuretics who have undergone surgery leading to hypovolemia. In patients of these categories, diuresis and renal function should be monitored from the start of treatment with meloxicam. Meloxicam can cause sodium, potassium, and fluid retention, resulting in an increased risk of progression of heart failure and hypertension (arterial hypertension) in predisposed patients. If side effects from the central nervous system (drowsiness, etc.) or visual impairment occur, patients should stop driving vehicles and operating mechanisms that require concentration.

Side effects of the drug Meloxicam-lugal

from the gastrointestinal tract: dyspepsia, nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; rarely - esophagitis, stomatitis, belching, erosive and ulcerative lesions of the gastrointestinal tract, gastrointestinal bleeding, transient changes in liver function (increased levels of liver transaminases or bilirubin); in some cases - intestinal perforation, colitis. From the central and peripheral nervous system: headache; rarely - dizziness, tinnitus, drowsiness; in some cases - changes in mood, disorientation. From the cardiovascular system: edema, rarely - increased blood pressure, tachycardia. From the urinary system: rarely - changes in laboratory parameters of renal function (increased levels of creatinine and/or urea in the blood); in some cases - OPN. From the hematopoietic system: rarely - anemia, leukopenia, thrombocytopenia. Dermatological reactions: itching, rash; rarely - urticaria; in some cases - photosensitivity, bullous reactions, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Allergic reactions: in some cases - angioedema, immediate hypersensitivity reactions (including anaphylactic and anaphylactoid). Other: in some cases - conjunctivitis, blurred vision (blurredness).

Drug interactions Meloxicam-lugal

When meloxicam is used simultaneously with other NSAIDs, the risk of developing erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. The combined use of the drug with anticoagulants, fibrinolytics, and antiplatelet agents should be avoided due to the increased risk of bleeding. When used simultaneously with diuretics, the risk of developing acute renal failure in patients with dehydration increases, and therefore patients taking meloxicam in combination with diuretics should receive a sufficient amount of fluid. In this category of patients, renal function should be examined before initiating meloxicam therapy. Meloxicam reduces the effectiveness of β-adrenergic receptor blockers, ACE inhibitors, vasodilators, diuretics, and intrauterine contraceptives. Meloxicam may enhance the hematotoxicity of methotrexate, and therefore, when used simultaneously, laboratory monitoring of peripheral blood is necessary. Meloxicam increases the nephrotoxicity of cyclosporine, so renal function should be monitored when used concomitantly. With the simultaneous use of meloxicam with lithium preparations, an increase in the level of lithium in the blood plasma is noted. Cholestyramine accelerates the elimination of meloxicam. Pharmacokinetic interaction of meloxicam with hypoglycemic drugs is possible, as well as with substances that modify activity or are metabolized by CYP 2C9 or CYP 3A4. There were no clinically significant interactions with antacids, cimetidine, or digoxin.