Meloksikam-OBL - instructions for use, doses, side effects, contraindications

Excipients: lactose monohydrate, microcrystalline cellulose, povidone (polyvinylpyrrolidone), silicon dioxide colloid (aerosil), potato starch, croscarmellose sodium, magnesium stearate.

Description:

Round flat cylindrical tablets from white with a yellowish shade to light yellow color with a facet; at a dosage of 15 mg - with a risk. A slight "marble" is allowed.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:

Meloxicam is a non-steroidal anti-inflammatory drug that has analgesic, antipyretic and analgesic effects. Anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the inflammatory region. Less meloxicam acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandin, which protects the mucous membrane of the gastrointestinal tract and takes part in the regulation of blood flow in the kidneys.

Pharmacokinetics:

It is well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not change the intake.

When using the drug inside at doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Equilibrium concentrations are achieved 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 a steady state of pharmacokinetics. Binding to plasma proteins is more than 99%. The range of differences between the maximum and basal concentrations of the drug after its administration once a day is relatively small and amounts to a dose of 7.5 mg 0.4-1.0 μg / ml, and when using a dose of 15 mg it is 0.8-2.0 μg / ml, (the values of C_min and C_max).

Meloksikam penetrates through the histohematological 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 with the formation of 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 value).

Research in vitro showed that in this metabolic transformation an important role is played by CYP 2C9, isozyme has an additional value CYP 3A4.In the formation of the other two metabolites (which constitute, respectively, 16% and 4% of the dose), peroxidase takes part, the activity of which probably varies individually.

It is excreted equally with feces and urine, mainly in the form of metabolites. With feces, less than 5% of the daily dose is excreted unchanged, in urine in unchanged form the drug is detected only in trace amounts. Half-life (T_1/2) meloxicam is 15-20 hours. Plasma clearance is an average of 8 ml / min.

In the elderly clearance of the drug is reduced. The volume of distribution is low, and averages 11 liters.

Hepatic or renal insufficiency of moderate severity significantly does not have a significant effect on the pharmacokinetics of meloxicam.

Indications:

- Symptomatic treatment of osteoarthritis;

- symptomatic treatment of rheumatoid arthritis;

- symptomatic treatment of ankylosing spondylitis (Bekhterev's disease).

Contraindications:

- Hypersensitivity to any component of the drug;

- Aspirin bronchial asthma;

- exacerbation of peptic ulcer of the stomach and duodenum;

- severe renal failure (if hemodialysis is not performed);

severe hepatic impairment;

- children under the age of 15;

- Pregnancy;

lactation period.

Carefully:

The drug should be used with caution in elderly patients.

Erosive-ulcerative lesions of the gastrointestinal tract in the anamnesis.

Pregnancy and lactation:The drug is not recommended for use during pregnancy and lactation.

Dosing and Administration:

The drug is taken orally during meals once a day.

Recommended dosing 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 the dose is ineffective, it can be increased to 15 mg per day.

Ankylosing spondyloarthroh: 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 failure who are on hemodialysis, the dose should not exceed 7.5 mg per day.

Side effects:

Organs of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions of the digestive tract, perforation of the stomach or intestines, gastrointestinal bleeding (latent or apparent), increased activity of "hepatic" enzymes, hepatitis, colitis, stomatitis, dryness mouth, esophagitis.

The cardiovascular system: tachycardia, increased blood pressure, sensation of "tides".

Respiratory system: exacerbation of asthma, cough.

central nervous system: headache, dizziness, tinnitus, disorientation, confusion of thoughts, sleep disturbance.

Genitourinary system: edema, interstitial nephritis, renal medullary necrosis, urinary infection, proteinuria, hematuria, renal insufficiency.

The organs of sight: conjunctivitis, blurred vision.

Skin covers: itching, skin rash, urticaria, multi-form exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity.

Hemopoietic system: anemia, leukopenia, thrombocytopenia.

Allergic reactions: anaphylactoid reactions (incl.anaphylactic shock), swelling of the lips and tongue, allergic vasculitis.

Other: fever.

Overdose:

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

Treatment: there is no specific antidote; When an overdose of the drug should be washed stomach, taking activated charcoal (within the next hour, symptomatic therapy.Holestyramine accelerates the removal of the drug from the body.Crossed diuresis, alkalization of urine, hemodialysis - ineffective due to the high connection of the drug with blood proteins.

Interaction:

When used simultaneously with other non-steroidal anti-inflammatory drugs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding of the gastrointestinal tract increases;
With simultaneous use with antihypertensive drugs, it is possible to reduce the effectiveness of the latter;
With simultaneous use with lithium preparations, development of cumulation of lithium and increase of its toxic effect (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 increased (the risk of anemia and leukopenia, periodic monitoring of the general blood test is shown);
With simultaneous use with diuretics and with cyclosporine, the risk of developing kidney failure increases;
With simultaneous use with intrauterine contraceptives, the effectiveness of the latter may be reduced;
When used simultaneously with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring of blood coagulability indices is necessary).
With simultaneous application with colestyramine, as a result of binding meloxicam, its excretion through the digestive tract increases.

Special instructions:

Care should be taken when using the drug in patients who have a history of peptic ulcer and duodenal ulcer, as well as patients who are on anticoagulation therapy. In such patients, the risk of ulcerative-erosive diseases of the gastrointestinal tract is increased.

Caution should be exercised and the indicators of renal function should be monitored when the drug is used in elderly patients, patients with chronic heart failure with circulatory insufficiency, in patients with cirrhosis, as well as in patients with hypovolemia as a result of surgical interventions.

In patients with renal insufficiency, if creatinine clearance is greater than 25 mL / min, dosage adjustment 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 allergic reactions (itching, skin rash, urticaria, photosensitivity) occur during treatment, it is necessary to consult a doctor with the purpose of resolving the issue of stopping the drug.

Effect on the ability to drive transp. cf. and fur:The use of the drug can cause the emergence of unwanted effects in the form of headaches and dizziness, drowsiness. If the above phenomena occur, it is necessary to abandon the management of vehicles and maintenance of machinery and mechanisms.

Form release / dosage:

Tablets, 7.5 mg and 15 mg.

Packaging:

For 10, 15, 20, 30 tablets in a contour mesh package.

By 1, 2, 3 or 4 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000174

Date of registration:07.04.2010 / 09.10.2017

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp22.04.2018

Illustrated instructions

Instructions

Meloksikam-OBL (Meloxicam-OBL)