Oxycamox - instructions for use, doses, side effects, contraindications

1 tablet contains: active substance: meloxicam 7.5 mg; Excipients: corn starch 22.00 mg, pregelatinized starch 9.50 mg,silicon dioxide colloidal anhydrous 0.80 mg, sodium citrate dihydrate 10.00 mg, lactose monohydrate 43.00 mg, cellulose microcrystalline 66.40 mg, magnesium stearate 0.80 mg.

Dosage of 15 mg

1 tablet contains: active substance: meloxicam 15 mg;

Excipients: corn starch 44.00 mg, pregelatinized starch 19.00 mg, silicon dioxide colloidal anhydrous 1.60 mg, sodium citrate dihydrate 20.00 mg, lactose monohydrate 86.00 mg, cellulose microcrystalline 132,80 mg, magnesium stearate 1, 60 mg.

Description:Round flat tablets from light yellow to light yellow with a weak greenish shade of color, with a risk on one side and a bevel.

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

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:

Meloxicam is a non-steroidal anti-inflammatory drug (NGTG), which has an anti-inflammatory, analgesic, and antipyretic effect.

The mechanism of pronounced anti-inflammatory effect of meloxicam is associated with inhibition of the enzyme cyclooxygenase-2 (COX-2), which participates in the synthesis of prostaglandins (PG) almost exclusively in the inflammatory region. Due to the relatively selective inhibition of COX-2 meloxicam suppresses the synthesis of prostaglandins (PG) in the inflammatory region to a greater extent than in the mucous membrane of the stomach or kidneys, due to a smaller effect on COX-1, less often causes erosive and ulcerative lesions of the gastrointestinal tract (GIT). In vitro determined that meloxicam (in doses of 7.5 mg and 15 mg) more actively inhibits COX-2, having a greater inhibitory effect on the production of PG E₂ (the reaction controlled by COX-2) than on the production of thromboxane participating in the process of blood coagulation (reaction controlled by COX-1). In vitro shown, that meloxicam in recommended doses does not affect platelet aggregation and bleeding time, in contrast to nonselective inhibitors of COX (indomethacin, diclofenac, ibuprofen and naproxen), which significantly suppressed platelet aggregation and increased bleeding time. These effects depended on the size of the dose. The selectivity of the action of meloxicam decreases with its administration in high doses, long-term use and individual characteristics of COX-2.

Pharmacokinetics:

Meloksikam is well absorbed in the digestive tract, when ingested bioavailability is 89%, eating does not affect the absorption of the drug.The equilibrium concentration in the blood plasma is reached in 3-5 days from the moment of the beginning of the drug intake. When administered, the maximum concentration (C_m_Oh) in the blood plasma is achieved after 5-6 hours The drug does not cumulate. Communication with plasma proteins is more than 99%. The difference between C_m_Oh and the minimum concentration of meloxicam when taken once in day is relatively small and lies within 0.4-1 μg / ml for a dose of 7.5 mg and 0.8-2 μg / ml for a dose of 15 mg (the values of C_min and C_m_Oh). Meloksikam penetrates through gistogematicheskie barriers, the concentration in the synovial fluid reaches 50% of C_ma_x in the blood plasma.

Meloksikam is almost completely metabolized in the liver with the formation of four pharmacologically active metabolites. The main metabolite, 5'-carboxymeloxicam (60% of the dose value), is formed by oxidation of the intermediate metabolite, 5'-hydroxycarboxymeloxicam, which is also excreted, but to a lesser extent (9% of the dose value). Research in vitro showed that in this metabolic transformation an important role is played by the isoenzyme СUR2С9, somewhat less important is the isozyme SURZA4.In the formation of the other two metabolites (which constitute, respectively, 16% and 4% of the dose value), peroxidase takes part, the activity of which is likely to have high individual variability.

It is excreted mainly in the form of metabolites through the intestine and kidneys in equal proportions. 5% of the daily dose is excreted unchanged through the intestine, in the urine unchanged drug is detected only in trace amounts.

The half-life (T_1/2) meloxicam is 15-20 hours. The average plasma clearance is 8 ml / min, but it can decrease in old age. The volume of distribution is about 11L. Hepatic and renal failure of mild to moderate severity does not significantly affect the pharmacokinetics of meloxicam. With a severe degree of kidney failure due to a decrease in the elimination of the drug, the daily dose should not exceed 7.5 mg.

Indications:

Symptomatic therapy of the following diseases:

osteoarthritis;

- rheumatoid arthritis;

- ankylosing spondylitis;

- gout;

- other inflammatory and degenerative joint diseases accompanied by pain syndrome.

The drug 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 meloxicam or any other component of the drug, other NSAIDs;

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;

- complete or incomplete combination of bronchial asthma with recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid (ASA) or NSAIDs (including in history);

- erosive and ulcerative lesions of the mucous membrane of the stomach or duodenum in the stage of exacerbation;

- gastrointestinal, cerebrovascular bleeding, bleeding from another localization, including history (or suspected bleeding);

- inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the stage of exacerbation;

- severe hepatic insufficiency or liver disease in the active stage;

- chronic renal failure in patients not undergoing hemodialysis (creatinine clearance (CK) less than 30 ml / min);

- progressive kidney disease, including confirmed hyperkalemia;

- condition after aortocoronary bypass surgery;

- Decompensated heart failure;

- pregnancy;

- the period of breastfeeding;

- children's age (up to 15 years).

Carefully:

To reduce the risk of developing dose-dependent adverse effects, the minimum effective dose should be used as short a course as possible.

- cardiac ischemia;

- cerebrovascular diseases;

- compensated heart failure;

- dyslipidemia / hyperlipidemia, diabetes mellitus;

- diseases of peripheral arteries;

- bronchial asthma;

- smoking, frequent use of alcohol;

- chronic renal failure with KK 30-60 ml / min;

- anamnestic data on the development of ulcerative lesions of the digestive tract, the presence of infection of non-Illicobacter pylori;

- elderly age;

- long-term use of NSAIDs;

- severe physical illness;

- concomitant therapy with the following drugs: anticoagulants (for example warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

Meloksikam is contraindicated during pregnancy.

Suppression of GHG synthesis can have an undesirable effect on pregnancy and fetal development. Data from epidemiological studies indicate an increase in the risk of spontaneous abortion, the development of heart defects and a defect in the anterior abdominal wall in the fetus after the use of inhibitors of the synthesis of PG during pregnancy. The absolute risk of heart disease increased from less than 1% to 1.5%. This risk increases with increasing dose and duration of therapy.

In the III trimester of pregnancy, the use of PG synthesis inhibitors can lead to the following disorders in the fetus:

- premature closure of the arterial duct and the development of pulmonary hypertension;

- renal dysfunction with the further development of renal failure with a decrease in the amount of amniotic fluid.

The mother during labor can increase the duration of bleeding and reduce the contractile capacity of the uterus, and as a result, the time of delivery increases.Antiaggregant effect can occur even when taking low doses.

Meloksikam is excreted in breast milk, therefore the use of the drug during breastfeeding is contraindicated. If it is necessary to use the drug during breastfeeding, it is necessary to resolve the issue of stopping breastfeeding.

Dosing and Administration:The drug is taken orally during meals at a daily dose of 7.5-15 mg. The drug should be taken during or after a meal, washed down with water or milk (the volume of the liquid is not less than 100 ml).

The maximum daily dose is 15 mg.

In osteoarthritis and other inflammatory and degenerative diseases of joints accompanied by pain syndrome, the average daily dose is 7.5 mg. In some cases, to achieve a greater effect, the dose is increased to 15 mg per day.

With rheumatoid arthritis and gout, the average daily dose is 15 mg. If necessary, the dose may be reduced to 7.5 mg per day. With ankylosing spondylitis, the average daily dose is 15 mg. If necessary, the dose may be reduced to 7.5 mg per day. In elderly patients and patients with severe renal failure (QC less than 30 ml / min) on hemodialysis, the dose should not exceed 7.5 mg per day.

In case of renal insufficiency of moderate severity (CK 30-60 ml / min), and also with hepatic insufficiency of moderate severity, correction of the dose is not required.

Side effects:

According to the World Health Organization (WHO), undesirable effects are classified according to the frequency of their development as follows: very often (>1/10), often (from >1/100 to <1/10), infrequently (from >1/1000 to <1/100), rarely (from >1/10000 to <1/1000), very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

From the gastrointestinal tract

Often: dyspepsia, nausea, vomiting, abdominal pain, constipation or diarrhea, flatulence;

infrequently: gastrointestinal hemorrhage (including latent), stomatitis, transient increase in activity of "liver" transaminases, hyperbilirubinemia, belching;

rarely: ulcerative lesions of the mucous membrane of the stomach or duodenum, esophagitis, colitis, hepatitis;

rarely: perforation of the gastrointestinal wall.

From the central nervous system

often: headache;

infrequently: dizziness, drowsiness;

rarely: "nightmarish" dreams, disorientation, insomnia, emotional lability;

frequency is unknown: confusion of consciousness.

On the part of the organs of hematopoiesis

infrequently: anemia;

rarely: changes in the blood formula (leukocytopenia, thrombocytopenia);

rarely: agranulocytosis.

Allergic reactions:

infrequently: other allergic reactions;

rarely: angioedema;

frequency is unknown: anaphylactoid / anaphylactic reactions.

From the side of the cardiovascular system

often: peripheral edema;

infrequently: increased blood pressure (BP), "hot flashes" of blood to the skin of the face;

rarely: a feeling of palpitations.

From the respiratory system

rarely: bronchospasm.

From the skin

infrequently: itching, skin rash, angioedema;

rarely: urticaria, Lyell's syndrome (toxic epidermal necrolysis), erythema multiforme (including malignant exudative erythema - Stevens-Johnson syndrome);

rarely: bullous dermatoses;

frequency is unknown: photosensitization.

From the sense organs

rarely: conjunctivitis, visual impairment, incl. blurred vision, tinnitus.

From the urinary system

infrequently: hyperkreatininemia and / or increased serum urea concentration, sodium and water retention, hyperkalemia, edema of the lower limbs;

rarely: acute renal failure in patients with initially elevated risk; communication with the reception of meloxicam is not established - interstitial nephritis, nephrotic syndrome (albuminuria), hematuria.

If any of the side effects listed in the manual are aggravated, or you notice any other side effects not indicated in the instructions, inform the doctor about it.

Overdose:

Symptoms of acute overdose of NSAIDs: dizziness, apathy, nausea, vomiting, pain in the epigastric region. These symptoms are usually reversible and amenable to symptomatic treatment. There may be bleeding from the gastrointestinal tract. Severe poisoning can lead to acute renal failure, acute liver failure, increased blood pressure, respiratory arrest, convulsions, collapse, coma, asystole.

Treatment: gastric lavage no later than 6 hours after admission, forced diuresis, symptomatic therapy. There is no specific antidote, however, the use of colestyramine (4 g three times a day inwards) is shown to reduce the absorption of meloxicam. Hemodialysis is ineffective.

Interaction:

Microsomal oxidation inductors (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites of meloxicam, increasing the risk of severe intoxication.

Inhibitors of microsomal oxidation reduce the risk of hepatotoxic effects of meloxicam (by reducing the production of active metabolites).

The simultaneous use of meloxicam and other NSAIDs is not recommended, since the risk of ulceration of the gastrointestinal mucosa and bleeding may increase.

With the simultaneous use of meloxicam with lithium preparations the excretion of lithium by the kidneys can decrease, which leads to an increase in the concentration of lithium in the serum. This combination should be avoided if this is not possible - it is necessary to carefully monitor the concentration of lithium in the blood before the treatment, during treatment and after the cancellation of meloxicam.

NSAIDs can weaken the effect diuretics and antihypertensive drugs. In patients with impaired renal function (also in dehydrated or elderly patients) simultaneous administration inhibitors of angiotensin-converting enzyme (ACE) or angiotensin II receptor antagonists (APA) with preparations inhibiting cyclooxygenase, can lead to further deterioration of renal function, up to the development of acute renal failure (in most cases reversible).

There may be a decrease in the hypotensive effect beta-blockers.

With the simultaneous use of meloxicam with glucocorticosteroids or selective serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline) increases the risk of ulceration of the gastrointestinal mucosa, which may result in serious gastrointestinal bleeding.

The risk of nephrotoxicity associated with admission cyclosporine, preparations of gold, increases with simultaneous application with meloxicam.

With simultaneous application also increases the hepatotoxicity cyclosporine.

Simultaneous use of meloxicam with methotrexate may lead to an increase in the concentration of the latter in the serum and increase its toxic effect, since NSAIDs reduce the tubular secretion of methotrexate (the risk of anemia and leukopenia, it is recommended that a general blood test be performed periodically).At a dose of methotrexate more than 15 mg / week, joint use of drugs is not recommended. You should also be careful when using methotrexate and meloxicam with reduced kidney function. With the simultaneous use of meloxicam and antiplatelet agents (acetylsalicylic acid, ticlopidine, clopidogrel), anticoagulants (warfarin, heparin) or thrombolytics (alteplase, streptokinase, urokinase) increases the risk of bleeding.

When used simultaneously with intrauterine contraceptives possibly reducing the effectiveness of the latter.

Caffeine enhances the analgesic effect of meloxicam.

Kolestyramine reduces the absorption of meloxicam, which can be used in overdose therapy with the drug.

With the simultaneous use of meloxicam with hypoglycemic agents for oral administration can enhance their action, thereby contributing to the risk of hypoglycemia.

Special instructions:

The frequency and severity of dose-dependent adverse effects is lower if the drug is administered at the lowest effective dose at the lowest possible short course.

Gastrointestinal bleeding or perforation of the gastrointestinal tract (including fatal) can be observed in the treatment of any NSAID, after various times after the start of treatment, including in patients without previous history of GI and / or any symptoms from the digestive tract. The risk of gastrointestinal bleeding is higher the higher the dose of the drug.

During long-term treatment, control of the peripheral blood pattern, water-electrolyte balance, coagulation system and functional state of the liver and kidneys is necessary.

With prolonged treatment, it is recommended to monitor the potassium concentration (especially in patients with diabetes mellitus).

When using the drug, there may be an increase in the concentration of "liver" enzymes and urea in the blood serum. These changes are usually mild and transitory. In case of pronounced changes, the drug should be discontinued.

Care should be taken when using the drug in patients who have a history of gastric and duodenal ulcer, as well as in patients receiving anticoagulant therapy. In such patients, the risk of erosive and ulcerative gastrointestinal lesions is increased.

When symptoms of gastropathy appear, a thorough examination including esophagogastroduodenoscopy, a blood test with determination of hematocrit, hemoglobin, occult blood feces (after appropriate preparation of the patient) is shown. To prevent the development of gastropathy meloxicam it is recommended to combine with gastroprotectors, for example, misoprostol or proton pump inhibitors.

Long-term use of the drug in patients with diseases of the cardiovascular system (uncontrolled hypertension, heart failure, ischemic heart disease, peripheral arterial occlusive disease and / or cerebrovascular disease), with risk factors for cardiovascular disease (eg, high blood pressure, hyperlipidemia, diabetes mellitus , smoking), should only be carried out after a thorough examination.

Data from clinical and epidemiological studies indicate a slight increase in the risk of developing arterial thrombosis in the treatment of NSAIDs for a long time.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

Patients taking both diuretics and meloxicam, should take a sufficient amount of fluid.

In patients with impaired renal function of mild and moderate severity (CK 30-60 ml / min), correction of the dosing regimen is not required. Meloksikam, as well as other NSAIDs, can mask the symptoms of infectious diseases. The use of the drug is undesirable with the first acute pain (as the use of meloxicam can mask the symptoms of acute pathology).

If on the background of therapy with meloxicam, the improvement does not occur within a few days, the question of the advisability of further therapy should be decided.

If allergic reactions (itching, skin rash, hives, photosensitization) occur during treatment, stop taking the drug immediately and consult a doctor. The greatest risk of severe complications from the skin is observed during the first month of treatment.

In patients with an increased risk of developing side effects, treatment starts with a dose of 7.5 mg.

In patients with dehydration of various etiologies, chronic heart failure, cirrhosis, nephrotic syndrome, diuretics,with clinically pronounced renal disease should monitor daily diuresis and kidney function.

When taking NSAIDs, by inhibiting the synthesis of renal PG and, consequently, reducing the rate of glomerular filtration, a dose-dependent development of renal failure may be observed. At the beginning of therapy (or after increasing the dose), diuresis and renal function should be carefully monitored, especially in patients with the following risk factors: old age, concomitant therapy with ACE II inhibitors, diuretics, hypovolemia (any etiology), heart failure, renal failure, nephrotic syndrome, lupus nephritis (lupus nephropathy), severe hepatic insufficiency (serum albumin <25 g / l or Child-Pugh liver cirrhosis> 10 points).

Meloksikam, like other drugs blocking the synthesis of PG can affect fertility, so it is not recommended for use by women planning a pregnancy.

During the period of treatment, the use of ethanol-containing foods and beverages is not recommended.

The described side effects are most severe in elderly and weakened patients.Care should be taken when treating these patient groups.

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 have not been carried out, nevertheless, care should be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 7.5 mg or 15 mg.

Packaging:

For 10 tablets in a blister of aluminum foil and PVC / PVDC film. For 1, 2, 5 or 10 blisters in a cardboard box together with instructions for medical use.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children!

Shelf life:

2.5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-000273

Date of registration:17.02.2011/01.04.2016

Expiration Date:unlimited

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

CIPLA, Ltd. India

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp25.12.2016

Illustrated instructions

Instructions

Oxycamox® (Oxicamox®)