Meloksikam-Teva - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 77.2 / 69.7 mg, microcrystalline cellulose 56.0 / 56.0 mg, sodium citrate dihydrate 18.0 / 18.0 mg, povidone-KSO 6.0 / 6.0 mg, crospovidone 12.0 / 12.0 mg, silicon dioxide colloid 1.5 / 1.5 mg, magnesium stearate 1.8 / 1.8 mg.

Description:

Tablets 7.5 mg

Round cylindrical tablets with bevel, yellow color, with light "marble". On one side, the dividing risk on the other is the engraving "MLX 7,5".

Tablets 15 mg

Tablets are oval in shape of yellow color, with a light "marble". On one side of the separating risk on the other is the engraving "MLX 15".

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, which has anti-inflammatory and antipyretic effect. Anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), involved in the biosynthesis of prostaglandin in the inflammatory region. Less meloxicam It acts on cyclooxygenase-1 (COX-1) involved in prostaglandin synthesis, protecting the mucosa of the gastrointestinal tract (GIT) and participate in the regulation of blood flow in the kidney.

Pharmacokinetics:

Absorption. Meloksikam is well absorbed from the gastrointestinal tract, as evidenced by high absolute bioavailability (90%) after ingestion.After a single application of meloxicam, the maximum plasma concentration in the plasma is reached within 5-6 hours. Simultaneous intake of food and inorganic antacids does not alter absorption. When using the drug inside (in doses of 7.5 and 15 mg), its concentrations are proportional to the doses. Steady state of pharmacokinetics is achieved within 3-5 days. 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 C_m_in and C_max in the period of steady state of pharmacokinetics), although the values beyond this range were also noted.

The maximum concentration of meloxicam in plasma during the steady state of pharmacokinetics is reached 5-6 hours after ingestion.

Distribution. Meloksikam very well binds to plasma proteins, mainly with albumin (99%). It penetrates into the synovial fluid, the concentration in the synovial fluid is approximately 50% of the concentration in the plasma.The volume of distribution after repeated oral administration of meloxicam (at doses ranging from 7.5 mg to 15 mg) is about 16 liters, with a coefficient of variation from 11 to 32%.

Metabolism. Meloksikam is almost completely metabolized in the liver with the formation of 4 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 degree (9% of the dose value). In vitro studies have shown that CYP2C9 plays an important role in this metabolic transformation, the CYP3A4 isoenzyme plays an additional role. 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.

Excretion. It is excreted equally through the intestines and kidneys, mainly in the form of metabolites. In unchanged form with feces less than 5% of the daily dose is excreted, in the urine in unchanged form the drug is found only in trace amounts. The average half-life of meloxicam varies from 13 to 25 hours.

Plasma clearance is an average of 7-12 ml / min after a single dose of meloxicam.

Insufficiency of liver and / or kidney function. Lack of liver function, as well as mild renal failure, does not significantly affect the pharmacokinetics of meloxicam. The rate of excretion of meloxicam from the body is much higher in patients with moderate renal insufficiency. Meloksikam worse binds to plasma proteins in patients with terminal renal failure. In terminal renal failure, an increase in the volume of distribution can lead to higher concentrations of free meloxicam, so in these patients the daily dose should not exceed 7.5 mg.

Elderly patients. Older patients have similar pharmacokinetic parameters in comparison with young patients. In elderly patients, the average plasma clearance during the equilibrium state of pharmacokinetics is slightly lower than in young patients. Older women have higher AUC values (area under the concentration-time curve) and a longer half-life, compared to young patients of both sexes.

Indications:

Symptomatic treatment:

- osteoarthritis (arthrosis, degenerative joint diseases), including painful component;

- rheumatoid arthritis;

ankylosing spondylitis;

- other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathies, dorsopathies (eg, sciatica, lower back pain, shoulder periarthritis, etc.) accompanied by pain.

Contraindications:

- Hypersensitivity to the active ingredient or auxiliary components of the drug.

- Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs because of the existing probability of cross-sensitivity (including history).

- Erosive-ulcerative lesions of the stomach and duodenum in the acute stage or recently transferred.

- Inflammatory bowel disease - Crohn's disease or ulcerative colitis in the stage of exacerbation.

- Severe hepatic insufficiency.

- Severe renal failure (if hemodialysis is not performed, creatinine clearance is less than 30 ml / min, and also with confirmed hyperkalemia), progressive kidney disease.

- Active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of coagulation system diseases.

- Expressed uncontrolled heart failure.

- Pregnancy.

- Breast-feeding.

- Therapy of perioperative pain during coronary artery bypass grafting.

- Children under 12 years.

- A rare hereditary intolerance of galactose (in the maximum daily dose of the drug with a dosage of meloc-sikam 7.5 mg and 15 mg contains 47 mg and 20 mg of lactose, respectively).

Carefully:Cardiac ischemia; cerebrovascular diseases; chronic heart failure; dyslipidemia / hyperlipidemia; diabetes; diseases of peripheral arteries, smoking, renal failure (creatinine clearance 30-60 ml / min); anamnestic data on the development of gastrointestinal ulcer; presence of Helicobacter pylori infection; elderly age; long-term use of NSAIDs; frequent use of alcohol, severe physical illness; concomitant therapy with the following drugs: anticoagulants (eg, warfarin), antiplatelet agents (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticoids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

The use of the drug Meloxicam-Teva is contraindicated during pregnancy. It is known that NSAIDs penetrate into breast milk, so the use of the drug Meloxicam-Teva during breastfeeding is contraindicated.

As a preparation inhibiting the synthesis of cyclooxygenase / prostaglandin, Meloxicam-Teva can affect fertility, and therefore is not recommended for women planning a pregnancy. Meloksikam can lead to a delay in ovulation. In this regard, women who have problems with conception and undergoing examination for such problems, it is recommended to cancel the drug Meloksikam-Teva.

Dosing and Administration:

Osteoarthritis with pain syndrome: 7.5 mg per day. If necessary, this dose can be increased to 15 mg per day.

Rheumatoid arthritis: 15 mg per day. Depending on the therapeutic effect, this dose can be reduced to 7.5 mg per day.

Ankylosing spondylitis: 15 mg per day.Depending on the therapeutic effect, this dose can be reduced to 7.5 mg per day.

In patients with an increased risk of adverse reactions (a history of the gastrointestinal disease, the presence of risk factors for cardiovascular disease), it is recommended to start treatment with a dose of 7.5 mg per day (see Special instructions).

In patients with severe renal failure who are on hemodialysis, the dose should not exceed 7.5 mg per day.

General recommendations

Since the potential risk of adverse reactions depends on the dose and duration of treatment, the lowest possible dose and duration of use should be used.

The maximum recommended daily dose is 15 mg.

Combined application

Do not use the drug simultaneously with other NSAIDs.

The total daily dose of the drug Meloxicam-Teva, used in the form of different dosage forms should not exceed 15 mg.

Teens

The maximum dose in adolescents (12-18 years) is 0.25 mg / kg and should not exceed 15 mg.

Use of tablets

The drug is contraindicated for children under 12 years due to the impossibility of selecting the appropriate dosage for this age group.The total daily dose should be taken at one time, during meals, with water or other liquid.

Side effects:

Below are described the side effects, the relationship of which with the use of meloxicam, was regarded as possible.

Side effects registered with post-marketing use, the relationship of which with taking the drug was regarded as possible, marked *.

Within the system-organ classes, the following categories are used for the incidence of side effects: very often (≥1 / 10); often (≥ 1/100, <1/10); infrequently (≥1 / 1,000, <1/100); rarely (≥1 / 10,000, <1 / 1,000); very rarely (<1 / 10,000); not installed.

From the side of the blood and lymphatic system: infrequently, anemia; rarely - changes in the number of blood cells, including changes in the leukocyte formula, leukopenia, thrombocytopenia.

From the immune system: infrequently - other immediate-type hypersensitivity reactions *; not established - anaphylactic shock *, anaphylactoid reactions *.

From the nervous system: often - headache; infrequently - dizziness, drowsiness.

Disorders of the psyche: often - a change in mood *; not established - confusion of consciousness *, disorientation *.

From the sense organs: infrequently - vertigo; rarely - conjunctivitis *, visual impairment, including blurred vision *, tinnitus.

From the gastrointestinal tract: often - abdominal pain, indigestion, diarrhea, nausea, vomiting; infrequently - latent or obvious gastrointestinal bleeding, gastritis *, stomatitis, constipation, bloating, eructation; rarely - gastroduodenal ulcers, colitis, esophagitis; very rarely - perforation of the gastrointestinal tract.

From the side of the liver: infrequently - transient changes in liver function (for example, increased activity of transaminases or bilirubin); very rarely - hepatitis *.

From the skin and subcutaneous tissues: infrequently - angio-edema *, itching, skin rash; rarely - toxic epidermal necrolysis *, Stevens-Johnson syndrome *, urticaria; very rarely - bullous dermatitis *, erythema multiforme *; not established - photosensitivity.

From the respiratory system: rarely - bronchial asthma in patients with an allergy to acetylsalicylic acid or other NSAIDs.

From the cardiovascular system: infrequently - increased blood pressure, a feeling of "tide" of blood to the face; rarely - a heartbeat.

From the genitourinary system: infrequent - changes in renal function (increased serum creatinine and / or urea levels), urination disorders, including acute urinary retention *; very rarely acute renal failure.

From the genitals and the breast: infrequently - late ovulation *; not established - infertility in women *.

Joint application with drugs that depress the bone marrow (for example, methotrexate) can provoke cytopenia.

Gastrointestinal bleeding, ulcer or perforation can lead to death.

As for other NSAIDs, the possibility of interstitial nephritis, glomerulonephritis, renal medullary necrosis, nephrotic syndrome is not ruled out.

Overdose:

Symptoms: impairment of consciousness, nausea, vomiting, epigastric pain - usually reversible. Gastrointestinal bleeding is possible. Severe poisoning can lead to acute renal failure, hepatic failure, respiratory arrest, asystole.

Treatment: there is no specific antidote; in the case of an overdose of the drug should be washed stomach, taking activated charcoal (within the next hour) and symptomatic therapy. In clinical studies it was shown that colestramine, tying meloxicam in the gastrointestinal tract, leads to its faster excretion. Forced diuresis, alkalization of urine, hemodialysis - ineffective because of the high connection with blood proteins.

Interaction:

- Other inhibitors of prostaglandin synthesis, including glucocorticoids and salicylates - concurrent administration with meloxicam increases the risk of ulceration in the gastrointestinal tract and gastrointestinal bleeding (due to synergism of action). Simultaneous reception with other NSAIDs is not recommended.

- Anticoagulants for oral administration, heparin for systemic use, thrombolytic agents - simultaneous administration with meloxicam increases the risk of bleeding. In the case of simultaneous use, careful monitoring of the blood coagulation system is necessary.

- Antiplatelet agents, serotonin reuptake inhibitors - simultaneous administration with meloxicam increases the risk of bleeding due to inhibition of platelet function. In the case of simultaneous use, careful monitoring of the blood coagulation system is necessary.

- Lithium preparations - NSAIDs increase the level of lithium in plasma, by reducing the excretion of it by the kidneys.The simultaneous use of meloxicam with lithium preparations is not recommended. In case of need for simultaneous use, careful monitoring of lithium concentration in plasma is recommended during the whole course of lithium preparations.

- Methotrexate - NSAIDs decrease the secretion of methotrexate by the kidneys, thereby increasing its concentration in the plasma. The simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. In the case of simultaneous use, careful monitoring of kidney function and the blood formula is necessary. Meloksikam may enhance hematological toxicity of methotrexate, especially in patients with impaired renal function. With the combined use of meloxicam and methotrexate for 3 days, the risk increases the toxicity of the latter.

- Contraception - there is evidence that NSAIDs may reduce the effectiveness of intra-uterine contraceptive devices, but this has not been proven.

- Diuretics - the use of NSAIDs in case of dehydration of patients is accompanied by a risk of acute renal failure.

- Antihypertensive agents (beta-adrenoblockers, angiotensin-converting enzyme inhibitors, vaso-dilators, diuretics).NSAIDs reduce the effect of antihypertensive drugs, due to the inhibition of prostaglandins, which have vasodilating properties.

Angiotensin II receptor antagonists, as well as angiotensin-converting enzyme inhibitors when combined with NSAIDs, increase the decrease in glomerular filtration, which can lead to acute renal failure, especially in patients with impaired renal function.

- Kolestyramine, tying meloxicam in the gastrointestinal tract, leads to its faster excretion.

- NSAIDs, acting on renal prostaglandins, can enhance the nephrotoxicity of cyclosporine.

- Pemetrexed - with the simultaneous use of meloxicam and pemetrexed in patients with creatinine clearance from 45 to 79 ml / min, the meloxicam should be discontinued five days before the start of pemetrexed and may be resumed 2 days after the end of the drug intake. If there is a need for the combined use of meloxicam and pemetrexed, patients should be closely monitored, especially with respect to myelosuppression and the occurrence of side effects from the gastrointestinaltract. In patients with creatinine clearance less than 45 ml / min, meloxicam is not recommended together with pemetrexed. When combined with meloxicam, drugs that have a known ability to inhibit CYP2C9 and / or CYP3A4 (or are metabolized by these enzymes), such as sulfonylureas or probenecid derivatives, pharmacokinetic interaction should be considered. When combined with oral antidiabetic agents (for example, derivatives of sulfonylurea, nateglinide), interactions mediated by CYP2C9 are possible, which may lead to an increase in the concentration of both these drugs and meloxicam in the blood. Patients simultaneously taking meloxicam with preparations of sulfonylurea or nateglinide, should carefully monitor blood sugar levels because of the possibility of developing hypoglycemia.

With simultaneous use of antacids, cimetidine, digoxin and furosemide, no significant pharmacokinetic interactions were identified.

Special instructions:

Patients suffering from diseases of the gastrointestinal tract should be observed regularly. If there is a ulcerative lesion of the gastrointestinal tract or gastrointestinal bleeding, the Meloxicam-Teva preparation must be canceled.

Ulcers of the gastrointestinal tract, perforation or bleeding may occur during the use of NSAIDs at any time, as in the presence of warning signs or information about serious gastrointestinal complications in history, and in the absence of these signs. The consequences of these complications are generally more serious in the elderly.

In applying the drug-Teva Meloxicam can develop such serious skin reactions as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. Therefore, special attention should be given to patients reporting the development of undesirable skin and mucous membrane phenomena, as well as hypersensitivity reactions to the drug, especially if similar reactions were observed during previous courses of treatment. The development of such reactions is observed, as a rule, during the first month of treatment.In the case of the appearance of the first signs of skin rash, changes in mucous membranes or other signs of hypersensitivity, the issue of discontinuing the use of Meloxicam-Teva should be considered.

Cases when taking NSAIDs increase the risk of developing serious cardiovascular thrombosis, myocardial infarction, angina attack, possibly fatal. This risk increases with prolonged use of the drug, as well as in patients with the above mentioned diseases in the history and predisposed to such diseases.

NSAIDs inhibit the synthesis of prostaglandins in the kidneys, which are involved in maintaining renal perfusion. The use of NSAIDs in patients with reduced renal blood flow or a reduced volume of circulating blood can lead to decompensation of the secretive renal failure. After the abolition of NSAIDs, the kidney function is usually restored to its original level. The elderly patients, patients with dehydration, congestive heart failure, liver cirrhosis, nephrotic syndrome or acute renal dysfunction, patients,simultaneously receiving diuretics, ACE inhibitors, angiotensin II receptor antagonists, as well as patients who have undergone major surgery, leading to hypovolemia. In such patients at the beginning of therapy, diuresis and renal function should be carefully monitored.

The use of NSAIDs in conjunction with diuretics can lead to a delay in sodium, potassium and water, as well as a decrease in natriuretic action of diuretics. As a result, predisposing patients may have signs of heart failure or hypertension. Therefore, careful monitoring of the condition of such patients is needed, and adequate hydration should be maintained. Before the beginning of treatment it is necessary to study the function of the kidneys. In the case of combined therapy, kidney function should also be monitored.

When using the drug meloxicam-Teva (as well as most other NSAIDs) may episodic increased activity of transaminases in blood serum or other indicators of liver function. In most cases, this increase was small and transient.If the changes identified are significant or do not decrease over time, the Meloxicam-Teva drug should be discontinued and observed for laboratory changes identified.

Weakened or debilitated patients can tolerate undesirable events worse, which is why such patients should be carefully observed.

Like other NSAIDs, Melok-Sikam-Teva can mask the symptoms of a major infectious disease.

As a preparation that inhibits the synthesis of cyclooxygenase / prostaglandin, Meloxicam-Teva can affect fertility, and therefore is not recommended for women who have difficulty with conception. In this regard, women who are undergoing examination in this regard, it is recommended to cancel the drug Meloksikam-Teva.

In patients with mild or moderate renal failure (creatinine clearance more than 25 ml / min), dose adjustment is not required.

In patients with cirrhosis of the liver (compensated), dose adjustment is not required.

Effect on the ability to drive transp. cf. and fur:Special studies on the effect of the drug on the ability to drive vehicles and mechanisms were not carried out.This activity should be refrained to patients who note that visual effects, drowsiness, or other side effects on the part of the central nervous system occur when the drug is treated.

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

Packaging:

For 10 tablets per blister PVC / PE / PVDC / A1 foil.

For 1 or 2 blisters in a pack of cardboard along with instructions for use.

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 indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-000256

Date of registration:16.02.2011 / 02.05.2017

Expiration Date:Unlimited

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Works Private, Ltd. Co. Hungary

Representation: & nbspTeva Teva Israel

Information update date: & nbsp22.04.2018

Illustrated instructions

Instructions

Meloksikam-Teva (Meloxicam-teva)