Meloxicam pills 15mg №10

International non-proprietary name:

Meloxicam

Dosage Form:

pills

Composition:

1 pill contains:
The active substance - meloxicam - 7.5 or 15 mg;
Excipients - lactose (milk sugar), microcrystalline cellulose, sodium citrate dihydrate, povidone (polyvinylpyrrolidone), carboxymethyl starch sodium (primogel), colloidal silicon dioxide (aerosil), Calcium stearate.

Description

pills from light yellow till yellow color, flat-cylindrical form with a facet. pills with a dosage of 15 mg are at risk on the one hand. The presence of marbling and minor inclusions is allowed.

Pharmacotherapeutic group:

nonsteroidal anti-inflammatory drug.

Pharmacological properties:

Pharmacodynamics
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 inside the doses of 7.5 and 15 mg of 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 0.4–1.0 mcg / ml with a dose of 7.5 mg and with a dose of 15 mg - 08–2.0 mcg / ml (Cmix and Cmax values ​​are given respectively). Meloxicam penetrates histohematogenous 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 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 derived equally with 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. 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 liters.
Hepatic or renal failure of moderate severity does not significantly affect the pharmacokinetics of meloxicam.

Indications for use:

Symptomatic treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis (ankylosing spondylitis) and other inflammatory and degenerative diseases involving pain syndrome.

Contraindications:

• hypersensitivity to any component of the drug;
• history of an attack of bronchial obstruction, rhinitis, urticaria after taking Acetylsalicylic acid or another NSAID (complete or incomplete intolerance of acetylsalicylic acid - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma (bronchial));
• 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;
• contraindicated in the period after coronary artery bypass surgery;
• decompensated heart failure;
• severe liver failure or active liver disease;
• severe renal failure in patients not undergoing dialysis (creatinine clearance less than 30 ml / min), progressive kidney disease including confirmed hyperkalemia;
• pregnancy, breastfeeding period;
• children's age up to 15 years.

Carefully:

Ischemic heart disease, cerebrovascular diseases, chronic heart failure (CHF), 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, the presence of Helicobacter pylori infections, old age, prolonged use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs:

• anticoagulants (for example, 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.

Dosage and administration:

The drug is taken orally during the meal once a day.
Recommended dosing regimen:

• Rheumatoid arthritis: 15 mg per day. After achieving a therapeutic effect, the dose can be reduced to 7.5 mg per day.
• Osteoarthritis: 7.5 mg per day. If necessary, the dose may 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.
Pregnancy and lactation:
The drug is not recommended for use during pregnancy and lactation.

Side effect:

On the part of the digestive system: more than 1% - dyspepsia, incl. nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1 - 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, incl. leukopenia, thrombocytopenia.
On the part of the skin: more than 1% - itching, skin rash; 0.1 - 1% urticaria; less than 0.1% - photosensitization, bullous eruptions, erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis.
On the part of the respiratory system: less than 0.1% - bronchospasm.
On the part 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.
On the part of the urinary system: 0.1 - 1% - hypercreatininemia and / or an 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.
From the senses: less than 0.1% - conjunctivitis, visual impairment, incl. blurred vision.
Allergic reactions: less than 0.1% - angioedema, anaphylactoid / Anaphylactic reactions .

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 reduce the effectiveness of the latter;
• With simultaneous use with lithium preparations, the development of lithium cumulation and an increase in its toxic action is 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.

Overdose:

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

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, patients with cirrhosis of the liver, as well as patients with hypovolemia as a result of surgical interventions.
• In patients with renal insufficiency, if creatinine clearance is more than 25 ml / min, no adjustment of the dosage regimen is 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, photosensitization), you should stop taking the drug and consult a doctor.

Driving, servicing cars and 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.

Storage conditions:

List B. In a dry, protected from light, out of reach of children, at a temperature not higher than 25 ºС.