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

for dosage of 7.5 mg: potato starch - 64.5 mg, lactose monohydrate -100 mg, povidone (polyvipilpirrolidop, povidone K-25) 3.2 mg, sodium citrate 18.8 mg, magnesium stearate 2 mg, silicon dioxide colloid (aerosil) - 4 mg;

for dosage of 15 mg: potato starch - 94.5 mg, lactose monohydrate 150 mg, povidone (nolivinilpyrrolidone, povidone K-25) 4.5 mg, sodium citrate 27 mg, magnesium stearate 3 mg, silicon dioxide colloid aerosil) -6 mg.

Description:Tablets from light yellow to yellow color, round, flat-cylindrical, with a facet and a risk. Allowed a slight marbling.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:Arthrosan® is a non-steroidal anti-inflammatory drug (NSAID), which has anti-inflammatory, antipyretic and analgesic effects. It belongs to the class of oxyocams, it is a derivative of enolic acid. The mechanism of action is associated with inhibition of the synthesis of prostaglandins as a result of selective inhibition of the enzymatic activity of cyclooxygenase of the second type (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. It acts less on the first type of cyclooxygenase (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. Due to this selectivity of inhibition of COX-2 activity, the drug less often causes erosive and ulcerative lesions of the gastrointestinal tract.

Pharmacokinetics:

Well absorbed from the gastrointestinal tract, absolute bioavailability - 89%. Simultaneous food intake does not change the absorption of the drug. 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 of treatment. 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%. When applying a dose of 7.5 mg, the minimum concentration (C_m_in) is 0.4 μg / ml, the maximum concentration (C_max) -1.0 μg / ml; when using a dose of 15 mg C_m_in - 0.8 μg / ml, C_max - 2.0 μg / ml. 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 degree (9% of the dose value). In vitro studies have shown that the isoenzyme CYP 2C9 plays an important role in this metabolic transformation, the CYP isoenzyme ZA4 is of additional importance. In the formation of two other metabolites, (corresponding, respectively, to 16% and 4% of the dose), peroxidase, whose activity probably varies, takes part.

The drug penetrates through the histohematological barriers, the concentration in the synovial fluid is 50% of the maximum concentration in the plasma.

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.

Hepatic or renal insufficiency of moderate severity has no significant effect on the pharmacokinetics of meloxicam.

It is excreted in equal proportion with feces and urine, mainly in the form of metabolites.

Through the intestine, less than 5% of the daily dose is excreted unchanged, in urine, in unchanged form, the drug is found only in trace amounts. Half-life (T_1/2) meloxicam is 15-20 hours.

Indications:Symptomatic treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis (Bechterew's disease), osteochondrosis and other inflammatory and degenerative diseases of the musculo-articular system, accompanied by pain syndrome.

Contraindications:

- Hypersensitivity to meloxicam or auxiliary components of the drug; lactose is included, so patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption, should not take the drug;

- heart failure in the stage of decompensation;

- early postoperative period after aorto-coronary bypass;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);

- exacerbation of peptic ulcer of the stomach and duodenum; active gastrointestinal bleeding;

- Inflammatory bowel disease (ulcerative colitis, Crohn's disease in the acute stage);

- cerebrovascular bleeding or other bleeding;

- severe hepatic impairment or active liver disease;

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

- children's age till 15 years;

- Pregnancy; the period of breastfeeding.

Carefully:

The drug should be used with caution in elderly patients and in the presence of the following conditions in history: IHD, congestive heart failure, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral vascular disease, CRF with creatinine clearance 30-60 ml / min; ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection. Long-term use of NSAIDs, alcohol abuse, concomitant anticoagulant therapy (eg, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, sertraline, paroxetine) must be taken into account when prescribing meloxicam.

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

Pregnancy and lactation:The drug is contraindicated for use during pregnancy and during breastfeeding. If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.

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. If necessary, the dose can be reduced to 7.5 mg per day.

- Osteoarthritis, osteochondrosis and other inflammatory and degenerative diseases of the musculo-articular system, accompanied by a pain syndrome: 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, 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, diarrhea, constipation, flatulence; 0.1-1% - transient increase in the activity of "liver" transaminases, hyperbilirubinemia, belching, esophagitis, gastric or duodenal ulcer, gastrointestinal bleeding (latent or apparent), stomatitis; less than 0.1% - perforation of the digestive tract, colitis, hepatitis, gastritis.

On the part of the organs of hematopoiesis: more than 1% - anemia; 0.1-1% - 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 central nervous system: more than 1% - dizziness, headache; 0.1-1% - tinnitus, drowsiness; less than 0.1% - emotional lability, confusion, disorientation.

From the side of the cardiovascular system: more than 1% - peripheral edema; 0.1-1% - increased blood pressure, a feeling of palpitations, hyperemia of the face.

From the urinary system: 0.1-1% - hypercreatininaemia, increased serum concentrationurea; 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, blurred vision.

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

Overdose:

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

Treatment: there are no specific antidotes and antagonists. When the drug is overdosed - gastric lavage, taking activated charcoal (within the next hour), symptomatic therapy. Forced diuresis, alkalinization of urine, hemodialysis are ineffective because of the high connection of the drug with blood proteins.

Interaction:

- With simultaneous use with other non-steroidal anti-inflammatory drugs (including acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding of the gastrointestinal tract increases;

- with simultaneous use with antihypertensive drugs, 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 is increased (the risk of anemia and leukopenia, the periodic monitoring of the general blood test is shown);

- with simultaneous use with diuretics and cyclosporine, the risk of developing renal failure increases;

- with simultaneous use with intrauterine contraceptives, there may be a decrease in the effectiveness of the latter;

- with simultaneous use with anticoagulants (heparin, warfarin), thrombolytic drugs (streptokinase, fibrinolysin), and antiplatelet agents (ticlopidine, clopidogrel, acetyl-isolic acid) increases the risk of bleeding (requires periodic monitoring of the coagulability of blood);

- with simultaneous application with colestyramin, the excretion of meloxicam through the gastrointestinal tract is accelerated;

- when used simultaneously with selective serotonin reuptake inhibitors, the risk of developing gastrointestinal bleeding increases.

Special instructions:

- Caution should be exercised when using the drug in patients who have a history of gastric ulcer and duodenal ulcer and patients on anticoagulant therapy. In such patients, the risk of erosive and ulcerative diseases of the gastrointestinal tract is increased.

- Care should be taken to monitor diurnal diuresis and renal function in elderly patients with reduced BCC and reduced glomerular filtration (dehydration, chronic heart failure, liver cirrhosis, nephrotic syndrome, clinically pronounced renal disease, diuretics, dehydration after large surgical operations).

- In patients with mild to moderate renal function impairment (creatinine clearance 30-60 ml / min), feed and meloxicam, should take a sufficient amount of fluid.

In case of allergic reactions (itching, skin rash, urticaria, photosensitization), it is necessary to consult a doctor in order to resolve the issue of stopping the drug.

Meloksikam, like other NSAIDs, can mask the symptoms of infectious diseases.

The use of meloxicam, as well as other drugs that block the synthesis of staglandins, can affect fertility, so it is not recommended for women who plan pregnancy.

Effect on the ability to drive transp. cf. and fur:In connection with the possibility of headache, dizziness and drowsiness, during the period of treatment, patients should abandon the management of vehicles and perform other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

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

Packaging:For 10, 15, 20 tablets in a contour mesh package. By 1, 2, 3 or 5 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001013

Date of registration:31.05.2010 / 10.04.2015

Expiration Date:Unlimited

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp13.09.2017

Illustrated instructions

Instructions

Arthrosan® (Artrozan)