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

Description:Tablets from light yellow to yellow with a greenish tinge color flat-cylindrical shape. Light marble is allowed. Tablets with a dosage of 15 mg have a dividing risk on one side.

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

ATX: & nbsp

M.01.A.C.06 Meloksikam

M.01.A.C Oksikamy

Pharmacodynamics:Has anti-inflammatory, antipyretic and analgesic effect. The mechanism of action is due to the inhibition of cyclooxygenase-2 (COX-2) activity, involved in the biosynthesis of prostaglandins in the inflammatory region. Less meloxicam acts on cyclooxygenase-1 (COX-1), involved in the synthesis of prostaglandins protecting the mucous membrane of the gastrointestinal tract (GIT) and taking part in the regulation of blood flow in the kidneys.

Pharmacokinetics:

Suction

Well absorbed from the digestive tract. Absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not affect suction. Concentration of meloxicam when taking the drug, inside at doses of 7.5 mg and 15 mg is proportional to the dose.

Distribution

The equilibrium state is achieved in the treatment of 3-5 days of regular admission.With long-term use of the drug for more than 1 year, the equilibrium concentration of meloxicam in plasma is similar to the equilibrium concentration (Css), which was established after the first days of taking the drug. Binding to plasma proteins is more than 99%. When taking the drug 1 time / day, the minimum equilibrium concentration (Css_min) and the maximum equilibrium concentration (Css_max) differ to a small extent and is 7.5 mg 0.4-1.0 μg / ml, and 15 mg 0.8-2.0 μg / ml, respectively. Meloksikam penetrates through the histohematological barriers, the concentration in the synovial fluid reaches 50% of the maximum concentration (C_max) in the plasma. The volume of distribution (Vd) averages 11 liters.

Metabolism

Meloksikam is almost completely metabolized in the liver with the formation of four pharmacologically inactive metabolitol. The main is 5'-carboxymelloxicam, which is formed by oxidation of the intermediate metabolite - (5'-hydroxymethylmeloxicam). In vitro studies found that biotransformation takes place with the participation of the isoenzyme CYP2C9, the isozyme CYP3A4 has an additional significance. The formation of the other two metabolites involved peroxides whose activity is probably individually varied.

Excretion

It is excreted equally with feces and urine, mainly in the form of metabolites (5'-carboxymelloxicam - up to 60%, 5'-hydroxymethylmeloxicam - 9%, and the other two - 16% and 4%, respectively). With feces, less than 5% of the daily dose is excreted unchanged, in urine, in unchanged form, the drug is found only in trace amounts. The half-life (T_1/2) - 15-20 hours. The plasma clearance is an average of 8 ml / min.

Pharmacokinetics in special clinical cases

In elderly people, the clearance of the drug is reduced.

In patients with hepatic or renal insufficiency of moderate severity, the pharmacokinetics of melocaeca a do not change significantly.

Indications:

Symptomatic therapy:

osteoarthritis;

- rheumatoid arthritis;

ankylosing spondylitis (Bekhterev'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 (including to NSAIDs of other groups);

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and near nasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs;

- Stomach ulcer and duodenal ulcer in the phase of exacerbation;

- Inflammatory bowel disease;

- bleeding of various genesis (including from the gastrointestinal tract, cerebrovascular);

- severe renal failure - creatinine clearance (CC) less than 30 ml / min (if hemodialysis is not performed);

progressive kidney disease;

- severe hepatic failure or active liver disease;

- severe heart failure;

- bronchial asthma caused by the intake of acetylsalicylic acid;

- confirmed hyperkalemia;

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

- children's age till 12 years;

- Pregnancy;

- lactation (breastfeeding);

- Hypersensitivity to the components of the drug.

Carefully:Elderly age, ischemic heart disease (CHD), chronic heart failure (CHF), cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, KK 30-60 ml / min, ulcerative lesions of the gastrointestinal tract in history, infection H pylori, prolonged use of NSAIDs, alcoholism, severe somatic diseases, simultaneous administration of oral glucocorticosteroids (GCS) (incl.prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline). For rectal administration (in addition): inflammatory diseases of the rectum and anal area, rectal or anal bleeding (including in the anamnesis).

Pregnancy and lactation:Contraindicated in pregnancy and lactation.

Dosing and Administration:

With rheumatoid arthritis, the recommended dose is 15 mg / day; depending on the therapeutic effect, the dose can be reduced to 7.5 mg / day.

With osteoarthritis, the drug is prescribed in a dose of 7.5 mg / day, in the absence of effect, the dose can be increased to 15 mg / day.

With ankylosing spondylitis, the daily dose is 15 mg. The maximum daily dose should not exceed 15 mg.

The drug is taken 1 time / day during meals.

In patients with an increased risk of side effects, as well as in patients with severe renal dysfunction (CC less than 30 ml / min) on hemodialysis, the dose should not exceed 7.5 mg / day.

In patients with impaired renal function (QC more than 30.sh / min) correction of the dosing regimen is not required.

Side effects:

Frequency: often - more than 1%; infrequently - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.01%.

From the digestive system: often - dyspepsia, incl. nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequent - transient increase in the activity of "liver" transaminases, hyperbilirubinemia, eructation, esophagitis, gastroduodenal ulcer, bleeding from the gastrointestinal tract (including latent), stomatitis; rarely - perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.

From the side of the cardiovascular system: often - peripheral edema, infrequently - tachycardia, increased blood pressure (BP), sensation of "hot flashes".

From the respiratory system: rarely - exacerbation of the course of bronchial asthma.

From the central nervous system (CNS): often - headache, dizziness; infrequently - vertigo, noise in the ears, drowsiness; rarely - disorientation, confusion, emotional lability.

From the urinary system: infrequently - hypercreatininaemia and / or increased urea concentration in blood serum; rarely acute renal failure; connection with the reception of meloxicam is not established - interstitial nephritis, albuminuria, hematuria.

Dermatological reactions: often - itching, skin rash; infrequently - hives, rarely - increased photosensitivity, bullous eruptions, erythema multiforme, incl. Stevens-Donsonatoxic epidermal necrolysis syndrome.

On the part of the hematopoiesis system: often - anemia; infrequently - leukopenia, thrombocytopenia.

Allergic reactions: rarely - anaphylactoid reactions (including anaphylactic shock), swelling of the lips and tongue, allergic vasculitis.

Other: fever.

Overdose:

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

Treatment: gastric lavage, reception of activated charcoal (within 1 hour after taking the drug); if necessary, conduct symptomatic therapy. Kolestyramine accelerates the excretion of meloxicam from the body. Forced diuresis, alkalization of urine, hemodialysis are ineffective because of the high degree of binding of meloxicam to blood proteins. There is no specific antidote.

Interaction:

When used simultaneously with other HTTGG1 (including with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding of the gastrointestinal tract increases.

With simultaneous use with antihypertensive drugs, the effectiveness of the latter may be reduced.

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).

When used simultaneously with methotrexate, the likelihood of anemia and leukopenia increases (a general blood test is shown periodically).

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 (including heparin, warfarin), as well as with thrombolytic drugs (including streptokinazoi, fibrinolysin), the risk of bleeding increases (periodic monitoring of blood clotting indices is necessary).

With simultaneous application with colestyramin, the excretion of meloxicam through the digestive tract increases (due to binding).

Special instructions:

Care should be taken when using the drug in patients who have a history of peptic ulcer and duodenal ulcer, and in patients receiving anticoagulant therapy, in this category of patients the risk of development of erosive and ulcerative gastrointestinal lesions is increased.

Caution should be exercised and the renal function should be monitored when the drug is used in elderly patients, patients with chronic heart failure, in patients with cirrhosis of the liver, as well as in patients with hypovolemia as a result of surgical interventions. Patients concurrently taking diuretics and meloxicam, should receive a sufficient amount of liquid.

When allergic reactions (itching, skin rash, urticaria, photosensitivity) occur, stop taking the drug.

Meloksikam, as well as other NSAIDs, can mask symptoms of infectious diseases.

Effect on the ability to drive transp. cf. and fur:Against the background of the use of the drug, the patient should not engage in potentially dangerous activities requiring increased attention. possibly the onset of headache, dizziness, drowsiness.

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

Packaging:

10 tablets per contour cell pack or 50, 60, 70, 80, 90, 100 tablets in a polymer jar. Packing 70, 80, 90, 100 tablets - for hospitals.

Each jar or 1, 2, 3 or 4 contour squares, together with the instruction for use, is placed in a pack of cardboard.

Storage conditions:List B. Store in a dry, the dark place at a temperature of no higher than 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:LSR-000843/10

Date of registration:09.02.2010

Expiration Date:Unlimited

The owner of the registration certificate:PRANAFARM, LLC PRANAFARM, LLC Russia

Manufacturer: & nbsp

PRANAFARM, LLC Russia

Information update date: & nbsp22.04.2018

Illustrated instructions

Instructions

Meloksikam-Prana (Meloxicam-prana)