Amelotex, pills 15 mg, 20 pcs.

Composition

1 tablet contains meloxicam 15 mg

. Pharmacological action

Pharmaceutical group:

NSAIDs.

Pharmaceutical action:

Amelotex is an NSAID that has anti-inflammatory, antipyretic, and analgesic effects. Belongs to the class of oxycams; a derivative of enolic acid.

Meloxicam is a nonsteroidal 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 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 and is involved in the regulation of blood flow in the kidneys.

Pharmacokinetics: 

Amelotex is well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not change absorption. When using the drug Amelotex inside in doses of 7.5 and 15 mg, its concentrations are proportional to the doses. 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 equilibrium concentrations. Binding to plasma proteins 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 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). Meloxicam penetrates through histohematic barriers, the concentration in synovial fluid reaches 50% of the maximum concentration of the drug in plasma.

It is almost completely metabolized in the liver to form four 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 the CYP 2C9 isoenzyme plays an important role in this metabolic transformation, while the CYP 3A4 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.

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, and only trace amounts of the drug are detected unchanged in the urine. The half-life (T 1/2) of meloxicam is 15-20 hours. The average plasma clearance is 8 ml/min. In the elderly, the clearance of the drug decreases. The volume of distribution is low, averaging 11 liters. Moderate hepatic or renal insufficiency does not significantly affect the pharmacokinetics of meloxicam.

Indications

• osteoarthritis;
• rheumatoid arthritis;
• ankylosing spondylitis (Ankylosing spondylitis);
• Amelotex 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

It is contraindicated during pregnancy and lactation.

Contraindications

Hypersensitivity to the Active ingredient or auxiliary components;Contraindicated in the period after coronary artery bypass grafting;uncompensated heart failure;Complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis and intolerance to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (including in the anamnesis);Erosive and ulcerative changes in the gastric or duodenal mucosa, active gastrointestinal bleeding;Inflammatory bowel diseases (ulcerative colitis, Crohn’s disease);Cerebrovascular bleeding or other bleeding; Severe hepatic insufficiency or active liver disease; Severe renal insufficiency in patients not undergoing dialysis (creatinine clearance less than 30 ml / min), progressive kidney diseases, including confirmed hyperkalemia; Pregnancy, breast-feeding; Children under 15 years of age.

C astronotus reduce the risk of adverse events should use the minimum effective dose of the minimum possible short course in ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia/hyperlipidemia, diabetes, peripheral artery disease, Smoking, creatinine clearance less than 60 ml/min, anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection in the elderly, long-term use of nonsteroidal anti-inflammatory drugs, frequent alcohol use, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (e. g. warfarin), antiplatelet agents (e. g. acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (e. g. prednisone), selective serotonin reuptake inhibitors (e. g. citalopram, fluoxetine, paroxetine, sertraline).

Side effects

From the digestive system: nausea, vomiting, belching, abdominal pain, constipation or diarrhea, flatulence, increased activity of “liver” transaminases, hyperbilirubinemia, stomatitis, erosive and ulcerative lesions of the gastrointestinal tract, esophagitis, gastritis, colitis, perforation of the gastrointestinal tract, gastrointestinal bleeding (latent or obvious), hepatitis.

Nervous system disorders: dizziness, vertigo, headache, tinnitus, confusion, drowsiness, disorientation, emotional lability.

From the respiratory system: bronchospasm.

Hematopoietic disorders: anemia, leukopenia, thrombocytopenia.

From the cardiovascular system: peripheral edema, increased blood pressure, “flushes” of blood to the skin of the face and upper chest, palpitations.

From the urinary system: edema, hypercreatininemia, increased concentration of urea in the blood serum. In rare cases-acute renal failure, interstitial nephritis, albuminuria, hematuria.

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

From the skin: pruritus, skin rash, urticaria, photosensitization, bullous rashes, erythema multiforme, toxic epidermal necrolysis.

Allergic reactions: angioedema, anaphylactoid, anaphylactic reactions.

Interaction

When used concomitantly with other nonsteroidal anti-inflammatory drugs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. When used concomitantly with antihypertensive drugs, the effectiveness of the latter may decrease.

When used concomitantly with lithium preparations, it is possible to develop lithium accumulation and increase its toxic effect (monitoring of lithium concentration in the blood is recommended).

When used concomitantly with methotrexate, the side effect of the latter on the hematopoietic system increases (the risk of anemia and leukopenia, periodic monitoring of the general blood test is indicated).

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) increases the risk of bleeding (periodic monitoring of blood clotting parameters is necessary).

When used concomitantly with colestyramine, meloxicam binding increases its excretion through the gastrointestinal tract.

Concomitant use with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

How to take, course of administration and dosage

The drug is taken orally with a meal once a day.

Recommended dosage regimen:

– Rheumatoid arthritis: 15 mg per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day. – Osteoarthritis: 7.5 mg per day. If ineffective, the dose can be increased to 15 mg per day. – Ankylosing spondylitis: 15 mg per 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 per day.

Overdose

Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, respiratory arrest, asystole.

Treatment: there is no specific antidote; in case of overdose of the drug, gastric lavage, taking activated charcoal (within the next hour), symptomatic therapy should be performed. Colestyramine accelerates the elimination of the drug from the body. Forced diuresis and hemodialysis are ineffective due to the high binding of the drug to blood proteins.

Special instructions

In case of peptic ulcers or gastrointestinal bleeding, the development of side effects from the skin and mucous membranes, the drug should be discontinued.

In patients with reduced circulating blood volume and reduced glomerular filtration (dehydration, chronic heart failure, surgery), clinically pronounced chronic renal failure may occur, which is completely reversible after discontinuation of the drug (in such patients, daily diuresis and renal function should be monitored at the beginning of treatment).

If there is a persistent and significant increase in transaminases and changes in other indicators of liver function, the drug should be discontinued and control tests should be performed. In patients with an increased risk of side effects, treatment begins with a dose of 7.5 mg.

In end-stage chronic renal failure in patients undergoing dialysis, the dose should not exceed 7.5 mg / day.

During treatment, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (with dizziness and drowsiness).

Form of production

Pills.

Storage conditions

In a dark place at a temperature of 8 to 25 °C

Shelf

life is 2 years.

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults by doctor’s prescription, Children by doctor’s prescription, Children over 15 years of age

Indications

Sciatica, Rheumatoid Arthritis, Osteoarthritis, Sciatica, Lumbago, Osteoarthritis, Osteochondrosis, Arthritis, Periarthritis

Weight

Weight: 130 gr.