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

Tablets 7.5 mg: round, biconvex tablets, pale yellow or pale yellow with a weak greenish tint of color, the presence of marbling and slight roughness is allowed.

Tablets 15 mg: round, biconvex tablets, with a risk on one side, pale yellow or pale yellow with a weak greenish tinge, the presence of marbling and slight roughness is allowed.

Pharmacotherapeutic group:Nonsteroidal anti-inflammatory drugs

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:Meloksikam - a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic 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 reaching equilibrium concentrations. 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 is 7.5 mg 0.4-0.0 μg / ml, and with a dose of 15 mg 0.8-2, 0 μg / ml, (the values of C_m_inand 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 value), is formed by oxidation of the intermediate metabolite, 5 '- hydroxymethylmeloxicam, which is also excreted, but to a lesser extent (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 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 unchanged output of less than 5% of the daily dose in the urine as unchanged 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 elderly people, 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 have a significant effect on the pharmacokinetics of meloxicam.

Indications:

- Osteoarthritis;

- rheumatoid arthritis;

ankylosing spondylitis (Bechterew's disease).

It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Contraindications:

- Hypersensitivity to the active substance or ancillary components;

- contraindicated in the period after aortocoronary bypass surgery;

Decompensated heart failure;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (including in anamnesis);

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

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

- cerebrovascular bleeding or other bleeding;

- severe hepatic impairment or active liver disease;

- marked renal insufficiency in patients not undergoing dialysis (creatinine clearance less than 30 ml / min), progressive kidney diseases including. confirmed hyperkalemia;

- pregnancy, the period of breastfeeding;

- Children under 15 years.

Due to the presence of lactose in the composition of patients with rare hereditary diseases, such as lactose intolerance,deficiency of lactase or glucosogalactose malabsorption should not be taken.

Carefully:

To reduce the risk of developing adverse events, the minimum effective dose should be used with the minimum possible short course when:

ischemic heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial diseases, smoking, creatinine clearance less than 60 ml / min, anamnestic data on the development of gastrointestinal ulcer, in the presence of Helicobacter pylori infection, in old age, with prolonged use of non-steroidal anti-inflammatory drugs, frequent use of alcohol, severe somatic diseases, concomitant therapy following preparations: anticoagulants (for example, warfarin), antiplatelet agents (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:Contraindicated in 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, 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 gastrointestinal tract: 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 (including 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: more than 1% - peripheral edema; 0.1-1% - increased blood pressure, palpitations, "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, hepatic insufficiency, 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. Kolestyramine accelerates the removal of the drug from the body. Forced diuresis, 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 from 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).

When used simultaneously with colestyramine, as a result of binding meloxicam, its excretion through the gastrointestinal tract is enhanced.

When used simultaneously with selective serotonin reuptake inhibitors, the risk of developing gastrointestinal bleeding 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 in patients who are on anticoagulant 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 more than 30 ml / min, dosage adjustment is not required. In patients on hemodialysis, the dosage of the drug should not exceed 7.5 mg / day.

With a persistent and significant increase in transaminases and changes in other indicators of liver function, the drug should be withdrawn and control tests carried out.

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 stop taking the drug.

Meloxicam, as well as other non-steroidal anti-inflammatory drugs, 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 planning pregnancy.

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. It should abandon the management of vehicles and maintenance of machines and mechanisms that require concentration of attention.

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

Packaging:10 tablets per contour cell pack. For 1 or 2 contour packs with instructions for use in a pack of cardboard.

Storage conditions:List B. Store 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:LSR-007059/09

Date of registration:07.09.2009 / 31.08.2010

Expiration Date:Unlimited

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

REPLEK FARM SCOPE, LLC Russia

Representation: & nbspPharm Company Sotex CJSC Pharm Company Sotex CJSC Russia

Information update date: & nbsp03.08.2017

Illustrated instructions

Instructions

Ameloteks® (Amelotex®)