Bi-ksikam - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Meloksikam - a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is the selective inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the inflammatory region. With the appointment in high doses, long-term use and individual features of the organism, COX2, the selectivity may decrease. Suppresses the synthesis of prostaglandins in the inflammation area to a greater extent than in the mucosa of the gastrointestinal tract and the kidneys.

Pharmacokinetics:Well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam - 89%, does not depend on food intake. When using the drug inside at doses of 7.5 and 15 mg, its concentration in the plasma is dose-dependent.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 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 using a dose of 7.5 mg 0.4-1.0 μg / ml, and when a dose of 15 mg is 0.8-2, 0 μg / ml, (Cmin and Stach, respectively). 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 participation of CYP 2C9, CYP 3A4, peroxidase with the formation of four pharmacologically inactive derivatives. 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. The half-life period (T1 / 2) of meloxicam is 15-20 hours.Plasma clearance is an average of 8 ml / min. In elderly people, the clearance of the drug is reduced. The volume of distribution is low, and averaged 11 liters. Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.

Indications:

Inflammatory and degenerative diseases of the joints, accompanied by pain syndrome:

- rheumatoid arthritis;

- osteoarthrosis;

ankylosing spondylitis (Bechterew's disease).

Contraindications:

- Hypersensitivity to any component of the drug;

- Aspirin bronchial asthma; deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

- exacerbation of peptic ulcer of the stomach and duodenum;

- gastrointestinal, cerebrovascular bleeding or other bleeding;

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

severe hepatic impairment;

- severe heart failure;

- children under the age of 15;

- Pregnancy;

lactation period.

Carefully:The drug should be used with caution in elderly patients, in patients with an erosive-ulcerative lesion of the gastrointestinal tract in an 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 spondylitis: 15 mg per day.

The maximum daily dose should not exceed 15 mg.

In patients with an increased risk of side effects, the initial 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, hyperbilirubinemia, belching.

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

Respiratory system: exacerbation of asthma, cough.

Central nervous system: headache, dizziness, tinnitus, disorientation, confusion of thoughts, sleep disturbance, drowsiness, emotional lability.

Genitourinary system: edema, interstitial nephritis, renal medullary necrosis, urinary infection, proteinuria, hematuria, renal failure, hypercreatininaemia and / or urea increase in serum.

Organs of vision: 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.

The system of hematopoiesis: anemia, leukopenia, thrombocytopenia.

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

Others: fever.

Overdose:

Symptoms: increased side effects.

Treatment: there is no specific antidote; with an overdose of the drug should be washed stomach, taking activated charcoal (within the next hour, symptomatic therapy.) Cholestyramine accelerates the removal of the drug from the body.

Interaction:

When used simultaneously with other non-steroidal anti-inflammatory drugs (including salicylates), 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, an increase in the level of lithium in the plasma is possible (control of the concentration of lithium in the blood is recommended);

With simultaneous use with methotrexate, the hematotoxic effect of the latter increases (periodic monitoring of the general blood test is shown);

With simultaneous application with diuretics and with cyclosporine, there is a potential for the development of acute renal failure in patients with dehydration;

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).

Cholestyramine, binds meloxicam, as a result of its increased excretion through the gastrointestinal tract.

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.

- Care should be taken to monitor kidney function in elderly patients, patients with chronic heart failure with circulatory failure, in patients with cirrhosis, as well as in patients with hypovolemia as a result of surgical interventions.

- In patients with renal insufficiency, if the creatinine clearance is more than 25 ml / min, dosage adjustment is not required.

- In patients who are 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, photosensitization) occur during treatment, you should consult a doctor to decide whether to stop taking the drug.

Effect on the ability to drive transp. cf. and fur:The use of the drug may cause the occurrence of side effects in the form of headaches and dizziness, drowsiness. In these cases, the management of vehicles and the maintenance of machines and mechanisms that require concentration of attention should be abandoned.

Form release / dosage:Tablets 7.5 mg and 15 mg.

Packaging:10 tablets per contour cell pack. For 20 tablets in a jar of polymer materials. Each jar or 1 circuit cell pack for 15 mg tablets, or 2 outline cell packs for 7.5 mg or 15 mg tablets, together 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:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002177

Date of registration:29.12.2011 / 05.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp05.02.2018

Illustrated instructions

Instructions

Bi-ksikam (Bi-Csikam)