Movasin - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate (sugar milk) - 52.5 mg. 105.00 mg, crospovidone (collidon CL, clolidone CL-M) 4.50 mg, 9.00 mg, talc 4.50 mg, 9.00 mg, magnesium stearate 1.50 mg, 3.00 mg , cellulose microcrystalline - 79.47 mg, 158.94 mg.

Description:Tablets are round, planocylindrical with a bevel, without risks for dosing 7.5 mg, with a risk for dosage of 15 mg, light yellow. On the surface of the tablets, slight marbling is allowed.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:Meloksikam - Non-steroidal anti-inflammatory drug (NSAID), which has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is associated with the inhibition of the synthesis of prostaglandins as a result of selective suppression of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandins in the inflammatory region. When administered in high doses, prolonged use and individual characteristics of the organism, the selectivity for COX-2 decreases. Suppresses the synthesis of prostaglandins in the inflammation region to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2. Less often causes erosive and ulcerative diseases of the gastrointestinal tract (GIT). Less meloxicam acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandins, protecting the mucous membrane of the gastrointestinal tract and taking part in the regulation of blood flow in the kidneys.

Pharmacokinetics:

It is well absorbed from the digestive tract, the absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not change the absorption. 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 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 (the values of the minimum concentration (C_min) and maximum concentration (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'-carboxymelloxicam (60% of the dose value) is formed by oxidation of the intermediate metabolite 5'-hydroxymethylmeloxicam, which is also excreted, but to a lesser degree (9% of the dose value). In vitro studies have shown that in this metabolic transformation an important role is played by the CYP 2C9 isoenzyme, an additional value and is the CYP 3A4 isoenzyme. 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 through the intestines and kidneys, mainly in the form of metabolites. Through the intestine, less than 5% of the daily dose is excreted unchanged, in the urine in unchanged form the drug is found only in trace amounts. The half-life (T_1/2) 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 averages 11 liters.

Liver or renal failure of moderate severity has no 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 meloxicam or excipients of the drug; the composition of the drug includes lactose, so patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption, should not take the drug;

- condition after aortocoronary shunting;

uncompensated heart failure;

- complete and incomplete combination of bronchial asthma, nose polynomia and intolerance of acetylsalicylic acid and other NSAIDs;

- erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;

- Inflammatory bowel disease (ulcerative colitis, Crohn's disease);

- cerebrovascular bleeding or other bleeding;

- severe hepatic failure or active liver disease;

- chronic renal failure in patients not undergoing dialysis (creatinine clearance (CK) less than 30 ml / min), progressive kidney disease, incl. confirmed hyperkalemia;

- pregnancy, the period of breastfeeding;

- Children under 12 years old.

Carefully:

Coronary heart disease (CHD), cerebrovascular disease, the compensated heart failure, dyslipidaemia / hyperlipidemia, diabetes mellitus, peripheral vascular disease, smoking, QC 30-60 ml / min.

A history of the development of ulcerative lesions gastrointestinal tract, the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs:

- anticoagulants (for example, warfarin);

- antiaggregants (for example, acetylsalicylic acid, clopidogrel);

- oral glucocorticosteroids (GCS) (for example, prednisolone);

- selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Pregnancy and lactation:Contraindicated taking during lactation and pregnancy.

Dosing and Administration:

The drug is taken orally during meals at a daily dose of 7.5-15 mg.

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 is 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:

From the digestive system: more than 1% - dyspepsia, incl. nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1% - a transient increase in the activity of "liver" transaminases, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (incl.latent), stomatitis; less than 0.1% - perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.

On the part of the organs of hematopoiesis: more than 1% - anemia; 0.1-1% change in the blood formula, incl. leukopenia, thrombocytopenia.

From the skin: more than 1% - itching, skin rash; 0,1-1% - urticaria; less than 0.1% - photosensitivity, bullous eruptions, erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the respiratory system: less than 0.1% - bronchospasm.

From the nervous system: more than 1% - dizziness, headache; 0,1-1% - vertigo, tinnitus, drowsiness; less than 0.1% - confusion, disorientation, emotional lability.

From the side of the cardiovascular system (SSS): more than 1% - peripheral edema; 0.1-1% - increase in blood pressure (BP), palpitation, "tides" of blood to the skin of the face.

From the urinary system: 0.1-1% - hypercreatininaemia and / or elevated urea in the blood serum; less than 0.1% - acute renal failure; connection with the reception of meloxicam is not established - interstitial nephritis, albuminuria, hematuria.

From the sense organs: less than 0.1% - conjunctivitis, visual impairment, incl. blurred vision.

Allergic reactions: less than 0.1% - angioedema, anaphylactoid / anaphylactic reactions.

Overdose:

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

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. Forced diuresis, alkalinization of urine, hemodialysis - ineffective because of the high connection of the drug with blood proteins.

Interaction:

- With simultaneous use with other NSAIDs (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, there may be a decrease in 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(the risk of anemia and leukopenia, the periodic monitoring of the general blood test is shown);

- with simultaneous application 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;

- with simultaneous use with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (periodic monitoring of blood coagulability);

- with simultaneous application with colestyramin, the excretion of the drug from the body is accelerated;

- when used simultaneously with selective serotonin reuptake inhibitors, the risk of bleeding from the gastrointestinal 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 anticoagulant therapy. These patients increased the risk of erosive and ulcerative gastrointestinal diseases;

- Caution should be exercised and the renal function should be monitored when the drug is used in elderly patients, patients with chronic heart failure (CHF) with circulatory failure, in patients with cirrhosis of the liver, as well as in patients with hypovolemia as a result of surgical interventions;

- in patients with insignificant or moderate decrease in renal function (QC more than 30 ml / min), correction of the dosing regimen is not required;

- patients taking both diuretics and meloxicam, should take a sufficient amount of liquid;

- if allergic reactions (itching, skin rash, urticaria, photosensitization) occur during treatment, it is necessary to consult a doctor with the purpose of resolving the issue of stopping the drug intake;

- meloxicam, as well as other NSAIDs, can mask the symptoms of infectious diseases;

- the use of meloxicam, as well as other drugs blocking the synthesis of prostaglandins, can affect fertility, so it is not recommended for women who want to become pregnant.

Effect on the ability to drive transp. cf. and fur:The use of the drug can cause the occurrence of undesirable effects in the form of headaches and dizziness, drowsiness, so during the period of taking the drug should abandon the management of vehicles and maintenance of machines and mechanisms that require concentration.

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

Packaging:

For 10 tablets in a contour mesh box made of polyvinyl chloride film and aluminum foil.

For 1, 2 contour cells with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000191

Date of registration:18.02.2010 / 30.12.2017

Expiration Date:Unlimited

The owner of the registration certificate:BIOKOM TECHNOLOGY, LLC BIOKOM TECHNOLOGY, LLC Republic of Belarus

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspBIOKOM, CJSCBIOKOM, CJSC

Information update date: & nbsp10.06.2018

Illustrated instructions

Instructions

Movasin® (Movasin®)