LEM
Active material: Meloxicam
When ATH: M01AC06
CCF: NSAIDs. Of selective COX-2 inhibitor
ICD-10 codes (testimony): M05, M15, M45
When CSF: 05.01.01.07.01
Manufacturer: OP OBOLENSKOE CJSC (Russia)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Pills from white to a yellowish tinge to the light yellow color, Valium, Slight marbling.
| 1 tab. | |
| meloxicam | 7.5 mg |
Excipients: lactose, polyvinylpyrrolidone (povidone), magnesium stearate, microcrystalline cellulose, colloidal silicon dioxide (aэrosyl), potato starch, sodium croscarmellose.
10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (4) – packs cardboard.
Pills from white to a yellowish tinge to the light yellow color, Valium, with Valium, Slight marbling.
| 1 tab. | |
| meloxicam | 15 mg |
Excipients: lactose, polyvinylpyrrolidone (povidone), magnesium stearate, microcrystalline cellulose, colloidal silicon dioxide (aэrosyl), potato starch, sodium croscarmellose.
10 PC. – packings Valium planimetric (1) – packs cardboard.
10 PC. – packings Valium planimetric (2) – packs cardboard.
10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (4) – packs cardboard.
Pharmacological action
NSAIDs. It has analgesic, antipyretic and anti-inflammatory action.
The mechanism of anti-inflammatory action due to inhibition of the enzymatic activity of COX-2, participating in the biosynthesis of prostaglandins in areas of inflammation. To a lesser extent meloxicam acts on Cox-1, involved in the synthesis of prostaglandin, protecting the gastrointestinal mucosa and takes part in the regulation of blood flow in the kidney.
Pharmacokinetics
Absorption
After ingestion meloxicam well absorbed from the gastrointestinal tract, absolute bioavailability – 89%. Receiving simultaneously with food did not affect the absorption. The amount of concentration in the employment drug meloxicam oral doses 7.5 and 15 mg is proportional to dose.
Distribution
The equilibrium is achieved within 3-5 regular admission days. Prolonged (more 1 year) application of meloxicam concentrations value is similar to Css, which is established after the first days of dosing. Linking plasma protein is more 99%. Before the drug 1 time / day Cssmin and Cssmax They differ to a small extent and form at reception 7.5 mg 0.4-1.0 ug / ml, and when receiving 15 mg - 0.8-2.0 ug / ml, respectively. Meloxicam permeates through gistogematicalkie barriers, concentration in synovial fluid reaches 50% Cmax plasma. Vd averages 11 l.
Metabolism
Meloxicam is almost completely metabolized in the liver with the formation of four pharmacologically active metabolites. The core is 5′-karʙoksimeloksikam, which is formed by oxidation of the intermediate metabolite (5′-gidroksimetilmeloksikama). In in vitro studies found, that biotransformation occurs when participation CYP2S9, additional importance of CYP3A4. In the formation of two other metabolites participates peroxidase, activity is, probably, individually varies.
Deduction
Is displayed equally in the feces and urine, primarily as metabolites (5′-karʙoksimeloksikam – to 60%, 5′-gidroksimetilmeloksikam – 9%, and 2 other- 16% and 4% respectively). Faeces in unaltered form appears less 5% from daily dose, in the urine as unchanged drug is detected in only trace amounts. T1/2 – 15-20 no. The plasma clearance averages 8 ml / min.
Pharmacokinetics in special clinical situations
In the elderly the ground clearance of the drug is reduced.
In patients with hepatic or renal insufficiency moderately pharmacokinetics Meloxicam is not significantly changed.
Testimony
Cimptomaticheskaya therapy:
-osteoarthritis;
-Rheumatoid arthritis;
-ankylosing spondylitis (ankylosing spondylitis).
Dosage regimen
At revmatoidnom ARTHRO The recommended dose is 15 mg / day; Depending on the therapeutic effect dose can be reduced to 7.5 mg / day.
At osteoarthritis the drug is prescribed in a dose 7.5 mg / day, in the absence of effective dose can be increased up to 15 mg / day.
At ankylosing spondylitis daily dose is 15 mg. The maximum daily dose should not exceed 15 mg.
The drug is taken 1 times per day with meals.
In patients with an increased risk of developing side effects, and y patients with severe renal impairment, hemodialysis, dose should not exceed 7.5 mg / day.
In patients with impaired renal function (QC more 25 ml / min) correction dosing regime is not required.
Side effect
From the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions of the gastrointestinal tract, perforation of the stomach or intestines, bleeding from the gastrointestinal tract (implicit or explicit), increase in liver enzymes, hepatitis, colitis, stomatitis, dry mouth, esophagitis.
Cardio-vascular system: tachycardia, increased blood pressure, feeling the tides.
The respiratory system: exacerbation of bronchial asthma, cough.
CNS: headache, dizziness, noise in ears, disorientation, confusion of thought, sleep disturbance.
From the urinary system: swelling, interstitial nephritis, renal medullary necrosis, urinary tract infection, proteinuria, hematuria, renal failure.
On the part of the organ of vision: conjunctivitis, blurred vision.
Dermatological reactions: itch, skin rash, hives, increased photosensitivity.
From the hematopoietic system: anemia, leukopenia, thrombocytopenia.
Allergic reactions: anaphylactoid reactions (incl. anaphylactic shock), swelling of the lips and tongue, sensitization vasculitis, erythema multiforme exudative (incl. Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
Other: fever.
Contraindications
- “Aspirin” bronchial asthma;
- Gastric ulcer and duodenal ulcer in the acute phase;
- Severe renal insufficiency (unless hemodialysis);
- Severe hepatic impairment;
- Children up to age 15 years;
- Pregnancy;
- Lactation (breast-feeding);
- Hypersensitivity to the drug.
FROM caution the drug should be used in the elderly and in patients with erosive-ulcerous lesions of DIGESTIVE TRACT disorder.
Pregnancy and lactation
The drug is contraindicated during pregnancy. If necessary, the appointment during lactation should decide the issue of termination of breastfeeding.
Cautions
Caution must be exercised in applying the drug in patients, receiving anticoagulant therapy.
Care should be taken to monitor renal function when using the drug in elderly patients, patients with chronic heart failure, in patients with liver cirrhosis, as well as in patients with gipovolemiei as a result of surgical interventions.
Patients, at the same time receiving dioretiki and meloxicam, should be getting enough fluids.
When allergic reactions (itch, skin rash, hives, photosensitivity) should stop taking the drug.
Effects on ability to drive vehicles and management mechanisms
If during treatment with the drug a headache, dizziness, drowsiness, the patient should not engage in potentially hazardous activities, require attention.
Overdose
Symptoms: disturbance of consciousness, nausea, vomiting, epigastric pain, bleeding from the gastrointestinal tract, acute renal failure, hepatic failure, respiratory arrest, asistolija.
Treatment: gastric lavage, administration of activated charcoal (during 1 h after dosing); if necessary, symptomatic therapy. Kolestiramin hastens excretion of meloxicam from the body. Forced diuresis, alkalization of urine, haemodialysis ineffective because of the high degree of binding of meloxicam blood protein. No specific antidote.
Drug Interactions
Together with the use of other NSAIDS (incl. acetylsalicylic acid) increases the risk of erosivno-yazvennah losses and bleeding of the GASTROINTESTINAL TRACT.
If you are applying with antigipertenzivei drugs may reduce the effectiveness of the past.
Together with the use of lithium may develop cumulation of lithium and toxicity (It recommended to control the concentration of lithium in the blood).
In an application with methotrexate increases the risk of anemia and leukopenia (shows the periodic General blood analysis).
Together with the use of diuretics and with ziklosporinom increases the risk of kidney failure.
Together with the use of uterine contraceptive devices may reduce the effectiveness of the past.
While the use of anticoagulants (incl. Heparin, ticlopidine, varfarinom), as well as thrombolytic agents (incl. streptokinazoy, fiʙrinolizinom) It increases the risk of bleeding (a periodic monitoring of blood coagulability).
Together with the use of kolestiraminom increases the excretion of meloxicam through blood (through linking).
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in a dry, protected from light and away from children at a temperature no higher than 25 ° C. Shelf life - 2 year.
