Meloxicam pills 15 mg 20 pcs
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Active ingredients
Meloxicam
Release form
Pills
Composition
Active ingredient: Meloxicam (Meloxicamum) Concentration of the active substance (mg): 15
Pharmacological effect
Meloxicam is a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in the biosynthesis of prostaglandins in the area of inflammation. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandin, which protects the mucous membrane of the gastrointestinal tract and is involved in the regulation of blood flow in the kidneys.
Pharmacokinetics
Well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam - 89%. Simultaneous ingestion of food does not change the absorption. When using the drug orally in doses of 7.5 and 15 mg, its concentration is proportional to the dose. Equilibrium concentration is reached within 3-5 days. With prolonged use of the drug (more than 1 year), the concentrations are similar to those observed after the first achievement of the equilibrium state. Plasma protein binding is 99%. The range of differences between the maximum and basal concentrations of the drug after it is taken once a day is relatively small and amounts to 0.4-1 μg / ml when using a dose of 7.5 mg, and when using a dose of 15 mg, it is 08-2 μg / ml. Meloxicam penetrates histohematogenous barriers, the concentration in synovial fluid reaches 50% Cmax of the drug in plasma. Almost fully metabolized in the liver with the formation of 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 CYP 2C9 plays an important role in this metabolic transformation, CYP 3A4 isoenzyme is of additional importance. Peroxidase is involved in the formation of two other metabolites (constituting 16% and 4%, respectively, of the dose), the activity of which is likely to vary individually. It is excreted equally in feces and urine, mainly in the form of metabolites. With feces in unchanged form, less than 5% of the daily dose is excreted, in the urine, the drug is found in unchanged form only in trace amounts.T1 / 2 meloxicam is 15-20 hours. Plasma clearance averages 8 ml / min. In the elderly, the clearance of the drug is reduced. Vd is low and averages 11 l. A moderately severe hepatic or renal failure has no significant effect on the meloxicam pharmacokinetics.
Indications
Inflammatory and degenerative diseases of the joints (arthrosis, osteoarthritis), rheumatoid arthritis, ankylosing spondylitis (ankylosing spondylitis).
Contraindications
Peptic ulcer and duodenal ulcer in the acute phase, pronounced abnormal liver function, renal failure (without hemodialysis), pregnancy, childhood and adolescence to 15 years, hypersensitivity to meloxicam and other NSAIDs (including salicylates).
Precautionary measures
Do not exceed the recommended dose. With caution: ischemic heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, creatinine clearance less than 60 ml / min. Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, Helicobacter pylori infections , advanced age, prolonged use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs: - anticoagulants (for example, warfarin); - and thiagregant (for example, acetylsalicylic acid, clopidogrel); - oral glucocorticosteroids (for example, prednisolone); - selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertralin) .To reduce the risk of developing undesirable effects from the gastrointestinal tract, use minimal effective dose of the shortest possible course
Use during pregnancy and lactation
The drug is not recommended for use during pregnancy and lactation.
Dosage and administration
Inside of 7.5-15 mg 1 time / day. The maximum daily dose is 15 mg. Apply topically 2 times / day. Apply a thin layer to clean, dry skin over the lesion and rub it gently for 2-3 minutes.
Side effects
On the part of the digestive system: dyspepsia, nausea, vomiting, abdominal pain, constipation, intestinal colic, diarrhea, esophagitis,stomatitis; rarely - erosive and ulcerative lesions of the gastrointestinal tract. For the central nervous system: dizziness, headache, tinnitus. For the cardiovascular system: increased blood pressure, palpitations, edema, flushes. Urinary system: changes in laboratory parameters of kidney function. side of the hematopoietic system: anemia, leukopenia, thrombocytopenia. Allergic reactions: bronchospasm, photosensitization, pruritus, rash, urticaria.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal tract bleeding, acute renal failure, liver failure, respiratory arrest, asystole. Treatment: no specific antidote; with an overdose of the drug should be a gastric lavage, taking activated carbon (within the next hour), symptomatic therapy. Kolestiramin accelerates the excretion of the drug from the body. Forced diuresis, alkalization of urine, hemodialysis are ineffective due to the high association of the drug with blood proteins.
Interaction with other drugs
With simultaneous use with other NSAIDs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. If used simultaneously with antihypertensive drugs, the effectiveness of the latter can be reduced. action (it is recommended to control the concentration of lithium in the blood). When used simultaneously with methotrexate, the side effect of the latter and the hematopoietic system (the risk of anemia and leukopenia, periodic monitoring of the complete blood count is shown). If used simultaneously with diuretics and cyclosporine, the risk of developing renal failure increases. (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of developing Itiation of bleeding (periodic monitoring of blood clotting parameters is necessary). When used simultaneously with Kolestiramine, as a result of meloxicam binding, its excretion through the gastrointestinal tract increases.
special instructions
Caution should be exercised when using the drug in patients with a history of peptic ulcer or duodenal ulcer, as well as in patients undergoing anticoagulant therapy. These patients have an increased risk of erosive and ulcerative diseases of the gastrointestinal tract. Care should be taken to monitor renal function when using the drug in elderly patients, patients with chronic heart failure with symptoms of insufficient blood circulation, in patients with cirrhosis of the liver, as well as in patients with hypovolemia as a result of surgical interventions. Patients with renal insufficiency, if creatinine clearance is more than 25 ml / min, do not require correction of the dosage regimen. In patients on dialysis, the dosage of the drug should not exceed 7.5 mg / day. Patients taking both diuretics and meloxicam should take a sufficient amount of fluid. If allergic reactions occur during the treatment process (itching, skin rash, urticaria, photosensitization) stop taking the drug and consult a doctor. The effect on the ability to drive vehicles and control mechanisms. The use of the drug can cause undesirable effects in the form of headaches and dizziness, drowsiness. You should abandon driving and maintenance of machines and mechanisms that require concentration.