Meloxicam is an NSAID. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of action is related to inhibition of prostaglandin synthesis as a result of selective inhibition of enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in the biosynthesis of prostaglandins in the area of inflammation.
When administered in high doses, long-term use and individual characteristics of the body, selectivity against COX-2 decreases. Suppresses the synthesis of prostaglandins in the area of inflammation to a greater extent than in the gastric mucosa or kidneys, which is associated with a relatively selective inhibition of COX-2. Less often causes erosive and ulcerative diseases of the gastrointestinal tract. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandins that protect the gastrointestinal mucosa and are involved in the regulation of blood flow in the kidneys.
After oral administration of the drug meloxicam is well absorbed from the gastrointestinal tract, the absolute bioavailability is 89%. Concomitant use with food does not change absorption. Magnitude of meloxicam concentration when administered orally in doses of 7.5 and 15 mg is proportional to the dose.
The relative bioavailability is almost 100% after administration in m/m. After an oral dose of 5 mg, Cmax is 1.62 mcg/ml and is reached within approximately 60 minutes.
Meloxicam exhibits linear pharmacokinetics at doses of 7.5-15 mg when administered by injection.
Css are achieved within 3-5 days of regular administration. With long-term use of the drug (more than 1 year), concentrations are similar to those observed after first achieving steady state pharmacokinetics. Binding to plasma proteins (especially albumin) is more than 99%.
The range of differences between maximum and basal concentrations of the drug after its administration once daily is relatively small and amounts to 0.4-1 mcg/ml with 7.5 mg dose and 0.8-2 mcg/ml with 15 mg dose (Cmin and Cmax values are given, respectively).
Meloxicam penetrates the histohematic barriers, the concentration in synovial fluid reaches 50% of the maximum concentration of the drug in plasma.
The Vd is low and is 11 liters. Interindividual differences are 30-40%.
Meloxicam is almost completely metabolized in the liver to form four pharmacologically inactive metabolites. 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 CYP2C9 isoenzyme plays an important role in this metabolic transformation, CYP3A4 isoenzyme has additional importance. Peroxidase, the activity of which probably varies individually, is involved in the formation of the other two metabolites (constituting, respectively, 16% and 4% of the value of the drug dose).
Extracted equally through the intestine and kidneys, mainly as metabolites. Less than 5% of the daily dose is excreted unchanged in the intestine, the drug is detected only in trace amounts in the urine. T1/2 of meloxicam after oral administration is 15-20 hours, when administered by injection – 20 hours. Plasma clearance averages 8 ml/min.
Pharmacokinetics in special clinical cases
The drug clearance is decreased in elderly persons.
Hepatic or renal insufficiency of moderate severity have no significant effect on the pharmacokinetics of meloxicam.
- rheumatoid arthritis;
- ankylosing spondylitis (Behterev’s disease).
meloxicam (in terms of 100% substance) 7.5 mg;
povidone-12.6 thousand.(polyvinylpyrrolidone low molecular weight medical 12600± 2700),
lactose monohydrate (milk sugar),
crospovidone (collidone CL, collidone SL-M),
How to take, the dosage
The drug Movasin is taken orally with meals in a daily dose of 7.5-15 mg.
Recommended dosing regimen:
- rheumatoid arthritis: 15 mg of Movasin per day. Depending on the therapeutic effect, the dose may be reduced to 7.5 mg per day.
- osteoarthritis: 7.5 mg of Movasin per day. If ineffective, the dose may be increased to 15 mg daily.
- ankylosing spondylitis: 15 mg of Movasin daily.
The maximum daily dose is 15 mg.
In patients at 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 of Movasin per day.
- Simultaneous use of Movasin with other NSAIDs (as well as with acetylsalicylic acid) increases the risk of gastrointestinal erosive ulcers and bleeding;
- Simultaneous use of Movasin with hypotensive drugs may reduce their effectiveness;
- Movasin with lithium may cause cumulation of lithium and increase its toxic effects (control of lithium concentration in the blood is recommended.concomitant use of Movasin with lithium may lead to cumulation of lithium and increase its toxic effects (it is recommended to monitor lithium concentration in the blood);
- Movacin’s concomitant use with methotrexate may have increased side effects of the latter on the hematopoietic system (risk of anemia and leucopenia, periodic control of total blood count);
- Movacin’s concomitant use with diuretic drugs may decrease the effectiveness of the latter drugs
- Movasin concomitant use with intrauterine contraceptives may decrease the effectiveness of the latter;
- Concomitant use of Movasinconcomitant use with anticoagulants (heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (streptokinase, fibrinolysin) increases the risk of bleeding (periodic monitoring of blood clotting is necessary);
- Concomitant use of Movasin with colestyramine accelerates excretion of the drug from the body;
- Concomitant use with selective serotonin reuptake inhibitors increases the risk of bleeding from the GI tract.
.concomitant use with diuretics and cyclosporine increases the risk of renal failure;
- Cautious use of the drug Movasin in patients with a history of peptic ulcer disease and duodenal ulcer, as well as in patients on anticoagulant therapy should be observed. These patients have increased risk of gastrointestinal erosive-ulcer disease;
- Cautions should be observed and renal function parameters should be controlled when using Movasin in elderly patients, patients with chronic heart failure (CHF) with signs of circulatory failure, patients with cirrhosis of liver as well as in patients with hypovolemia as a result of surgical operations;
- patients with mild to moderate impairment of renal function (CKR greater than 30 mL/min) do not require dosing adjustments;
- Patients taking diuretics and meloxicam at the same time should take plenty of fluids;
- If allergic reactions occurred during treatment (itching, skin rash, urticaria, photosensitization) it is necessary to contact the doctor to decide on stopping the use of Movasin;
- Meloxicam, as well as other NSAIDs, may mask symptoms of infectious diseases;
- The use of meloxicam, as well as other drugs that block the synthesis of prostaglandins, may affect fertility, so it is not recommended for women who want to become pregnant.
Movasin use may cause undesirable effects such as headache, dizziness, somnolence; therefore, while taking the drug, avoid driving motor transport and operating machinery or machines requiring concentration.
- state after coronary artery bypass surgery;
- decompensated heart failure;
- Complete or incomplete combination of bronchial asthma, recurrent polyposis of nasal mucosa and paranasal sinuses, and intolerance to acetylsalicylic acid and other NSAIDs (incl.ч.
- erosive-ulcerative changes of mucous coat of stomach or duodenum, active gastrointestinal bleeding;
- inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
- severe hepatic failure or active liver disease;
- chronic renal failure in non-dialysis patients (CKR less than 30 ml/min), advanced renal disease (includingч.
- children under 12 years of age (for tablet);
- children under 18 years of age (for IUI solution); pregnancy;
- lactation (breastfeeding);
- high sensitivity to meloxicam and other components of the drug.
The tablet formulation contains lactose, so patients with rare hereditary conditions, such as galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take the drug.
- cerebrovascular disease;
- compensated heart failure;
- sugar diabetes;
- Peripheral arterial disease;
- KKK 30-60 ml/min;
- anamnestic evidence of the development of gastrointestinal ulcers;
- presence of Helicobacter рoolori infection;
- older age;
- long use of NSAIDs;
- frequent use of alcohol;
- severe somatic diseases;
- concomitant therapy with the following drugs: anticoagulants (e.g., warfarin); antiaggregants (e.g., acetylsalicylic acid, clopidogrel); oral GCS (e.g., prednisolone); selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).
To reduce the risk of gastrointestinal adverse events, use the lowest effective dose for the shortest possible course.
Gastrointestinal system: more than 1 % – dyspepsia, including nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; 0.1-1 % – transient increase of “liver” transaminases activity, hyperbilirubinemia, belching, esophagitis, gastroduodenal ulcer, GI bleeding (including hidden gastrointestinal bleeding); less than 0.1
Hidden), stomatitis; less than 0.1% – gastrointestinal perforation, colitis, hepatitis, gastritis.
Hematopoietic organs: more than 1% – anemia; 0.1-1% – blood count changes, including leukopenia, thrombocytopenia.
Skin disorders: more than 1% – itching, skin rash; 0.1-1% – urticaria; less than 0.1% – photosensitization, bullous rash, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis.
Respiratory system disorders: less than 0.1% – bronchospasm.
Nervous system disorders: more than 1% – dizziness, headache; 0.1-1% – vertigo, tinnitus, drowsiness; less than 0.1% – confusion, disorientation, emotional lability.
Cardiovascular system (CVS): more than 1 % – peripheral edema; 0.1-1 % – increase of blood pressure (BP), palpitation, “rushes” of blood to the face.
Urinary system: 0.1-1% – hypercreatininemia and/or increased serum urea; less than 0.1% – acute renal failure; relationship with meloxicam administration is not determined – interstitial nephritis, albuminuria, hematuria.
Sensory organs: less than 0.1% – conjunctivitis, visual impairment, including blurred vision.
Allergic reactions: less than 0.1% – angioedema, anaphylactoid/anaphylactic reactions.
Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, GI bleeding, acute renal failure, liver failure, respiratory arrest, asystole.
Treatment: there is no specific antidote; in case of overdose the drug should be performed gastric lavage, activated charcoal (within the next hour), symptomatic therapy. Forced diuresis, urine alkalinization, hemodialysis are ineffective due to high binding of the drug to blood proteins.
Movalis, Meloxicam, Amelotex, Movasin, Arthrosan, Meloxicam-Teva, Meloxicam DS, Meloxicam Stada, Petcam Tabs, Meloxidil, Elox-SOLofar
|Conditions of storage|
In a dry, light-protected place at a temperature not exceeding 25 °C
Sintez OAO, Russia
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