Meloxicam-alsi pills 15mg N20
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Description
Meloxicam has anti-inflammatory, analgesic, antipyretic effect.
Active ingredients
Meloxicam
Release form
Pills
Composition
Meloxicam 15 mg; Auxiliary substances: pregelatinized starch (starch 1500) - 60.0 mg, microcrystalline cellulose - 122.6 mg, sodium citrate dihydrate - 40.0 mg, colloidal silicon dioxide (Aerosil 380) - 1.2 mg, magnesium stearate - 1.2 mg.
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 mg and 15 mg of its concentration is proportional to the dose. Equilibrium concentrations are 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 more than 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 0.4–1.0 mcg / ml with a dose of 7.5 mg, and 0.8–2.0 mcg / ml with a dose of 15 mg (given, respectively, Cmin and Cmax values). Meloxicam penetrates histohematogenous barriers, the concentration in the synovial fluid reaches 50% of the maximum concentration of the drug in the plasma. Almost completely metabolized in the liver to form four 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 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% of the dose of the drug, respectively), the activity of which probably varies individually; Less than 5% of the daily dose is excreted unchanged through the intestine; in the urine, the drug is found in unchanged form only in trace amounts. The half-life (T1 / 2) of meloxicam is 15-20 hours. Plasma clearance averages 8 ml / min. In the elderly, the clearance of the drug is reduced. The volume of distribution is low and averages 11 l.; Hepatic or renal failure of moderate severity does not significantly affect the pharmacokinetics of meloxicam.
Indications
Symptomatic treatment: - osteoarthritis. - rheumatoid arthritis. - Ankylosing spondylitis (ankylosing spondylitis) and other inflammatory and degenerative diseases of the joints, accompanied by pain.
Contraindications
- hypersensitivity to the active substance or auxiliary components. - is contraindicated in the period after coronary artery bypass surgery. - uncompensated heart failure. - Anamnestic data about the attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete intolerance syndrome of acetylsalicylic acid - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma). - erosive and ulcerative changes of the mucous membrane of the stomach or duodenum 12, active gastrointestinal bleeding. - inflammatory bowel disease (ulcerative colitis, Crohn's disease). - cerebrovascular bleeding or other bleeding. - severe liver failure or active liver disease. - severe renal failure in patients not undergoing dialysis (CC less than 30 ml / min), progressive kidney disease, including confirmed hyperkalemia. - pregnancy, breastfeeding period. - children's age up to 15 years.With care: ischemic heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, QA less than 60 ml / min. Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (eg, warfarin). antiplatelet agents (eg, acetylsalicylic acid, clopidogrel). oral glucocorticosteroids (eg, prednisone). selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline). To reduce the risk of adverse events from the gastrointestinal tract, use the minimum effective dose of the shortest possible course.
Precautionary measures
Use for violations of liver function. The drug is contraindicated in patients with severe liver failure. Application for violations of renal function. The drug is contraindicated in patients with severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 ml / min), progressive kidney diseases, including confirmed hyperkalemia. Use in children Contraindications: children up to 15 years. Use in elderly patients Elderly people clearance of the drug is reduced.
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation.
Dosage and administration
The drug is taken orally during the meal once a day. Recommended dosing regimen: Rheumatoid arthritis: 15 mg / day. Depending on the therapeutic effect, the dose can be reduced to 7. 5 mg / day. Osteoarthritis: 7. 5 mg / day. With the ineffectiveness of the dose can be increased to 15 mg / day. Ankylosing spondylitis: 15 mg / day. The maximum daily dose should not exceed 15 mg. In patients with an increased risk of side effects, as well as in patients with severe renal insufficiency who are on hemodialysis, the dose should not exceed 7. 5 mg / day.
Side effects
On the part of the digestive system: more than 1% - dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea. 01-1% - transient increase in the activity of liver transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, gastrointestinal bleeding (including latent), stomatitis. less than 0. 1% - gastrointestinal perforation, colitis, hepatitis, gastritis. From the side of blood-forming organs: more than 1% - anemia. 0. 1-1% - change in blood formula, including leukopenia, thrombocytopenia. On the part of the skin: more than 1% - itching, skin rash. 0. 1-1% - urticaria. less than 0. 1% - photosensitivity, bullous rash, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis. On the part of the respiratory system: less than 0. 1% - bronchospasm. Of the nervous system: more than 1% - dizziness, headache. 0. 1-1% - vertigo, tinnitus, drowsiness. less than 0, 1% - confusion, disorientation, emotional lability. Since the cardiovascular system: more than 1% - peripheral edema. 0. 1-1% - increase in blood pressure, heartbeat, "flush" of blood to the skin of the face. From the urinary system: 0. 1-1% - hypercreatininemia and / or increase in serum urea. less than 0, 1% - acute renal failure. connection with the reception of meloxicam has not been established - interstitial nephritis, albuminuria, hematuria. On the part of the senses: less than 0. 1% - conjunctivitis, blurred vision, including blurred vision. Allergic reactions: less than 0. 1% - angioedema, anaphylactoid / anaphylactic reactions.
Overdose
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, bleeding in the gastrointestinal tract, acute renal failure, liver failure, respiratory failure, asystolia. Treatment: there is no specific antidote. With an overdose of the drug should be a gastric lavage, taking activated charcoal (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 nonsteroidal anti-inflammatory drugs (as well as with acetylsalicylic acid) increases the risk of erosive and ulcerative lesions and gastrointestinal bleeding.With simultaneous use with antihypertensive drugs, may decrease the effectiveness of the latter. With simultaneous use with lithium preparations, cumulation of lithium and an increase in its toxic action are possible (it is recommended to control the concentration of lithium in the blood). With simultaneous use with methotrexate, the side effect of the latter on the hematopoietic system is enhanced (the risk of anemia and leukopenia, periodic monitoring of the complete blood count is shown). With simultaneous use with diuretics and cyclosporine increases the risk of developing renal failure. With simultaneous use with intrauterine contraceptives may reduce the effectiveness of the latter. With simultaneous use with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (requires periodic monitoring of blood clotting). With simultaneous use of Kolestiramine, as a result of binding meloxicam, its excretion through the gastrointestinal tract increases. When used simultaneously with selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases.
special instructions
Care should be taken when using the drug in patients with a history of peptic ulcer and duodenal ulcer, as well as in patients undergoing treatment with anticoagulants. These patients have an increased risk of erosive and ulcerative diseases of the gastrointestinal tract. Caution should be exercised and monitor renal function when using the drug in elderly patients, patients with chronic heart failure with symptoms of circulatory failure, in patients with cirrhosis of the liver, as well as in patients with hypovolemia as a result of surgical interventions. In patients with renal insufficiency, if creatinine clearance is more than 25 ml / min, correction of the dosage regimen is not required. 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 during treatment there are allergic reactions (itching, skin rash, urticaria, photosensitivity), you should consult a doctor to decide whether to stop taking the drug. Meloxicam, like other NSAIDs, can mask the symptoms of infectious diseases. The use of meloxicam, as well as other drugs that block prostaglandin synthesis, may affect fertility, therefore it is not recommended for women who want to become pregnant. Influence on the ability to drive vehicles and control mechanisms. The use of the drug can cause the occurrence of undesirable effects in the form of headache and dizziness, drowsiness. You should abandon driving and maintenance of machines and mechanisms that require concentration.