Meloxicam-Teva, pills 15mg 20pcs

Composition

Active ingredient:

meloxicam 15 mg.

Auxiliary substances: lactose monohydrate 69.7 mg, microcrystalline cellulose 56.0 mg, sodium citrate dihydrate 18.0 mg, povidone-KZO 6.0 mg, crospovidone 12.0 mg, colloidal silicon dioxide 1.5 mg, magnesium stearate 1.8 mg

Pharmacological action

Nonsteroidal Anti-inflammatory drug (NSAID)ATX:

M. 01. A. C. 06 Meloxicam

M. 01. A. C Oxycams

Pharmacodynamics : Meloxicam is a nonsteroidal anti-inflammatory drug with 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 prostaglandin biosynthesis in the inflammatory region. 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 (GIT) and is involved in the regulation of blood flow in the kidneys. Pharmacokinetics:

Absorption.

Meloxicam is well absorbed from the gastrointestinal tract, as evidenced by its high absolute bioavailability (90%) after oral use. After a single application of meloxicam, the maximum concentration of the drug in plasma is reached within 5-6 hours. Simultaneous intake of food and inorganic antacids does not change the absorption. When using the drug inside (in doses of 7.5 and 15 mg), its concentrations are proportional to the doses. A stable state of pharmacokinetics is achieved within 3-5 days. The range of differences between the maximum and basal concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-1.0 mcg / ml when using a dose of 7.5 mg, and 0.8-2.0 mcg/ml when using a dose of 15 mg (Cmin and Cmax values are shown, respectively, during the steady state of pharmacokinetics), although values outside the specified range were also noted.

The maximum concentration of meloxicam in plasma during the steady state of pharmacokinetics is reached 5-6 hours after oral use.

Distribution.

Meloxicam binds very well to plasma proteins, mainly albumin (99%). Penetrates the synovial fluid, the concentration in the synovial fluid is approximately 50% of the plasma concentration. The volume of distribution after repeated oral use of meloxicam (in doses from 7.5 mg to 15 mg) is about 16 liters, with a coefficient of variation from 11 to 32%.

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 the oxidation of an 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 CYP3A4 isoenzyme plays an additional role. The formation of the other two metabolites (which make up 16% and 4% of the drug dose, respectively) involves peroxidase, the activity of which probably varies individually.

Output.

It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. In unchanged form, less than 5% of the daily dose is excreted in the feces, and in the urine in unchanged form, the drug is detected only in trace amounts. The average half-life of meloxicam varies from 13 to 25 hours.

Plasma clearance averages 7-12 ml / min after a single dose of meloxicam.

Insufficient liver and/or kidney function. Hepatic insufficiency, as well as mild 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 moderate renal insufficiency. Meloxicam does not bind well to plasma proteins in patients with end-stage renal failure. In end-stage renal failure, increased volume of distribution may lead to higher concentrations of free meloxicam, so the daily dose should not exceed 7.5 mg in these patients.

Elderly patients. Elderly patients compared with young patients have similar pharmacokinetic parameters. In elderly patients, the mean plasma clearance during steady-state pharmacokinetics is slightly lower than in young patients. Older women have higher AUC values (area under the concentration-time curve) and a longer half-life, compared to younger patients of both sexes.

Indications

Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis (Ankylosing spondylitis), etc. inflammatory and degenerative joint diseases accompanied by pain syndrome.

It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.

Use during pregnancy and lactation

Teratogenic effects. Meloxicam increased the incidence of cardiac septal defects (a rare complication) when using an oral dose of 60 mg / kg / day (64.5 times higher than the 15 mg/day dose for an adult weighing 50 kg in terms of body surface area) and embryoletality at oral doses ≥5 mg/kg / day (5.4 times higher than the human dose as described above) in rabbits treated with meloxicam during organogenesis.

Meloxicam showed no teratogenicity in rats at oral doses of 4 mg / kg / day (approximately 2.2 times higher than the human dose as described above) during organogenesis. An increase in the stillbirth rate was observed in rats at oral doses ≥1 mg / kg / day during organogenesis.

Non-teratogenic effects. Meloxicam caused a decrease in such indicators as fertility index, live birth rate, neonatal survival at oral doses ≥0.125 mg/kg/day (approximately 0.07 times the human dose as described above) in rats during pregnancy and lactation.

Meloxicam passes through the placental barrier. No adequate and strictly controlled studies have been conducted in pregnant women. Use during pregnancy is possible if the expected effect of therapy exceeds the potential risk to the fetus.

Studies evaluating the effect of meloxicam on arterial duct closure in humans have not been conducted. The use of meloxicam in the third trimester of pregnancy should be excluded.

Childbirth and delivery. Studies in rats have shown that meloxicam, like other agents that inhibit PG synthesis, increases the number of stillbirths, causes delayed delivery and delivery at oral doses of ≥1 mg / kg / day (approximately 0.5 times the human dose as described above), and reduces the number of surviving pups at oral doses of 4 mg/kg/day (approximately 2.1 times the human dose as described above) during organogenesis. Similar observations were observed in rats receiving oral doses ≥0.125 mg / kg / day (approximately 0.07 times the human dose as described above) during pregnancy and lactation.

The effects of meloxicam on labor and delivery in humans are unknown.

Category of action on the fetus according to the FDA-C.

The use of meloxicam, as well as other drugs that block the synthesis of PG, can affect fertility, so it is not recommended for women who want to become pregnant.

Meloxicam is excreted in the milk of lactating rats, with milk concentrations exceeding plasma concentrations. It is not known whether meloxicam passes into the breast milk of women, so you should stop breastfeeding during treatment or avoid using meloxicam during breastfeeding.

Contraindications

-Hypersensitivity to the active ingredient or auxiliary components of the drug.

– Complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs due to the existing probability of cross-sensitivity (including in the anamnesis).

– Erosive and ulcerative lesions of the stomach and duodenum in the acute stage or recently transferred.

– Inflammatory bowel diseases – Crohn’s disease or ulcerative colitis in the acute stage.

– Severe liver failure.

– Severe renal insufficiency (if hemodialysis is not performed, creatinine clearance is less than 30 ml / min, as well as with confirmed hyperkalemia), progressive kidney disease.

– Active gastrointestinal bleeding, recent cerebrovascular bleeding, or an established diagnosis of diseases of the blood coagulation system.

– Severe uncontrolled heart failure.

– Pregnancy.

– Breast-feeding.

– Therapy of perioperative pain during coronary artery bypass grafting.

– Children under 12 years of age.

– Rare hereditary galactose intolerance (the maximum daily dose of meloxicam 7.5 mg and 15 mg contains 47 mg and 20 mg of lactose, respectively).

With caution:Coronary heart disease; cerebrovascular diseases; chronic heart failure; dyslipidemia/hyperlipidemia; diabetes mellitus; peripheral arterial diseases, smoking, renal failure (creatinine clearance 30-60 ml / min); anamnestic data on the development of ulcerative lesions of the gastrointestinal tract; the presence of Helicobacter pylori infection; elderly age; long-term use of NSAIDs; frequent alcohol consumption, severe somatic diseases; concomitant therapy with the following drugs: anticoagulants (e. g., warfarin), antiplatelet agents (e. g., acetylsalicylic acid, clopidogrel), oral glucocorticoids (e. g., prednisone), selective serotonin reuptake inhibitors (e. g., citalopram, fluoxetine, paroxetine, sertraline).

Side effects

Frequency: often-more than 1%; infrequently-0.1-1%; rarely-0.01-0.1%; very rarely-less than 0.01%.

From the digestive system: often-dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequently-transient increase in the activity of “liver” transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, gastrointestinal bleeding (including hidden), stomatitis; rarely-gastrointestinal perforation, colitis, hepatitis, gastritis.

From the hematopoietic organs: often-anemia; infrequently-changes in the blood formula, including leukopenia, tromocytopenia.

From the skin: often-pruritus, skin rash; infrequently-urticaria; rarely-photosensitization, bullous rashes, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the respiratory system: rarely-bronchospasm.

From the nervous system: often – dizziness, headache; infrequently-vertigo, tinnitus, drowsiness; rarely-confusion, disorientation, emotional lability.

From the cardiovascular system: often-peripheral edema; infrequently-increased blood pressure, palpitations, “flushes” of blood to the skin of the face.

From the urinary system: infrequently-hypercreatininemia and / or increased serum urea concentration; rarely – acute renal failure; association with meloxicam intake has not been established – interstitial nephritis, albuminuria, hematuria.

From the sensory organs: rarely-conjunctivitis, visual impairment, including blurred vision.

Allergic reactions: rarely-angioedema, anaphylactoid / anaphylactic reactions.

Interaction

When used concomitantly with acetylsalicylic acid and other NSAIDs, the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

When used concomitantly with antihypertensive agents, the effectiveness of the latter may decrease. When used concomitantly with lithium preparations, lithium can accumulate and increase its toxic effect (monitoring of lithium concentration in the blood is recommended).

Simultaneous use with methotrexate increases the side effect of the latter on the hematopoietic system (there is a risk of anemia and leukopenia.

Periodic monitoring of a general blood test is required). Concomitant use with diuretics and cyclosporine increases the risk of developing renal failure. When used simultaneously with intrauterine contraceptives, the effectiveness of the latter may decrease.

When used concomitantly with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (blood clotting parameters should be periodically monitored).

Simultaneous use with colestyramine increases the elimination of meloxicam through the gastrointestinal tract (as a result of meloxicam binding). No pharmacokinetic interaction was observed when meloxicam was co-administered with antacids.

How to take, course of use and dosage

Osteoarthritis with pain syndrome: 7.5 mg per day. If necessary, this dose can be increased to 15 mg per day.

Rheumatoid arthritis: 15 mg per day. Depending on the therapeutic effect, this dose can be reduced to 7.5 mg per day.

Ankylosing spondylitis: 15 mg per day. Depending on the therapeutic effect, this dose can be reduced to 7.5 mg per day.

In patients with an increased risk of adverse reactions (diseases of the gastrointestinal tract in the anamnesis, the presence of risk factors for cardiovascular diseases), it is recommended to start treatment with a dose of 7.5 mg per day (see Special Instructions).

In patients with severe renal insufficiency who are on hemodialysis, the dose should not exceed 7.5 mg per day.

General recommendations

Since the potential risk of adverse reactions depends on the dose and duration of treatment, the lowest possible dose and duration of use should be used.

The maximum recommended daily dose is 15 mg.

Combined use

Do not use the drug simultaneously with other NSAIDs.

The total daily dose of Meloxicam-Teva used in various dosage forms should not exceed 15 mg.

Teenagers

Maximum dose in adolescents (12-18 years) it is 0.25 mg / kg and should not exceed 15 mg.

Use of tablets

The drug is contraindicated in children under 12 years of age due to the inability to select the appropriate dosage for this age group. The total daily dose should be taken at one time, with a meal, with water or other liquid.

Overdose

Symptoms: increased side effects.

Treatment: gastric lavage, taking activated charcoal (within the next hour), symptomatic therapy.

Colestyramine accelerates the elimination of the drug from the body. Forced diuresis, urine alkalinization, and hemodialysis are ineffective due to the high binding of meloxicam to blood proteins. No specific antidotes or antagonists were found.

Special instructions

It is used with caution for diseases of the upper gastrointestinal tract in the anamnesis, in combination with anticoagulants, myelotoxic drugs, including methotrexate (cytopenia is possible).

The occurrence of gastroduodenal ulcers, gastrointestinal bleeding, side effects from the skin and mucous membranes serves as a basis for discontinuing the drug. If allergic reactions (pruritus, skin rash, urticaria, photosensitization) occur during treatment, you should consult a doctor to decide whether to stop taking the drug. Risk of gastrointestinal complications.

Serious gastrointestinal side effects, including inflammation, bleeding, ulceration, and perforation of the stomach or intestines, may occur at any time when NSAIDs are used without warning symptoms. Elderly patients have a higher risk of serious gastrointestinal complications, and the likelihood of these complications also increases with prolonged use.

Meloxicam, like other NSAIDs, can mask the symptoms of infectious diseases. use of NSAIDs to patients with reduced renal blood flow and BCC may accelerate renal decompensation (after discontinuation of NSAID therapy, renal function usually returns to its previous level).

The risk of such reactions is particularly high in patients with dehydration, congestive heart failure, cirrhosis of the liver, nephrotic syndrome and severe kidney diseases, in patients receiving diuretics, as well as in patients who have undergone significant surgery that led to hypovolemia (careful monitoring of diuresis and renal function is necessary from the beginning of treatment).

In rare cases, NSAIDs may cause interstitial nephritis, glomerulonephritis, renal medulla necrosis, or nephrotic syndrome. If there is a significant deviation from the normal level of serum transaminases and other indicators that characterize liver function, you should stop taking it and conduct control laboratory tests. Use caution in elderly, debilitated and emaciated patients.

The use of meloxicam may cause undesirable effects such as headache and dizziness, drowsiness. In this regard, you should stop driving vehicles, servicing machines and mechanisms, and other activities that require increased concentration of attention.

Form of production

Tablets

Storage conditions

The drug should be stored in a dry place protected from light at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

Tablets