Meloxicam

When ATH:
M01AC06

Characteristic.

NSAIDs, oxicam derivative. Light yellow solid, practically insoluble in water, very soluble in strong acids and alkalis, very little soluble in methanol. The apparent partition coefficient (log P)_app = 0,1 в n-октанол/буфер pH 7,4. PK values_a meloxicam 1,1 and 4,2. Molecular weight 351,41.

Pharmacological action.
Anti-inflammatory, analgesic, pyretic.

Application.

Inflammatory and degenerative joint diseases, accompanied by pain syndrome: arthritis, incl. rheumatoid arthritis, acute osteoarthritis, chronic polyarthritis; ankiloziruyushtiy spondylitis (ankylosing spondylitis), pain in osteoarthritis and myelitis.

Contraindications.

Hypersensitivity (incl. to other NSAIDs), "Aspirinovaâ" triad (a combination of asthma, recurrent nasal polyposis, and paranasal sinuses and intolerance of aspirin and drugs pirazolonovogo series), gastric ulcer and duodenal ulcer in the acute stage; gastrointestinal, cerebrovascular or any other bleeding / hemorrhage; severe heart failure, severe liver failure, severe renal insufficiency (unless hemodialysis), pregnancy, lactation, Age to 15 years.

Restrictions apply.

Erosive and ulcerative lesions of the gastrointestinal tract in history, Elderly patients. For rectal administration (additionally): inflammatory diseases of the rectum and anal Department, rectal or anal bleeding (incl. history).

Pregnancy and breast-feeding.

Teratogenic effects. Meloxicam increased incidence of cardiac septum defects (a rare complication) using oral dose 60 mg / kg / day (in 64,5 times the dose 15 mg / day for an adult weighing 50 kg based on body surface area) and embrioletalnost at oral doses ≥5 mg / kg / day (in 5,4 times the human dose, as described above) rabbits, meloxicam treated during organogenesis. Meloxicam showed no teratogenicity in rats at oral doses of 4 mg / kg / day (about 2,2 times the human dose, as described above) during the period of organogenesis. Increased frequency of stillbirth was observed in rats at oral doses ≥1 mg / kg / day during organogenesis.

Nonteratogenic effects. Meloxicam caused decrease of these indicators, as an index of fertility, viviparity, neonatal survival with oral doses ≥0,125 mg / kg / day (about 0,07 times the human dose, as described above) rats during pregnancy and lactation.

Meloxicam passes through the placental barrier. There are no adequate and well-controlled studies in pregnant women have not held. Application during pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus.

Research, dedicated to assessing the impact of meloxicam closing of the ductus arteriosus in humans, not carried out. The use of meloxicam in the III trimester of pregnancy should be excluded.

Labor and delivery. In studies in rats show, Chto meloxicam, as well as other means, ingibiruyushtie synthesis NG, increases the number of stillbirths, It causes a delay in labor and delivery at oral doses ≥1 mg / kg / day (about 0,5 times the human dose, as described above) and reduces the number of surviving pups at oral doses doses 4 mg / kg / day (about 2,1 times the human dose, as described above) during the period of organogenesis. Similar observations were noted in rats, treated with oral doses of ≥0,125 mg / kg / day (about 0,07 times the human dose, as described above) during pregnancy and lactation.

The effects of meloxicam on labor and delivery in humans is unknown.

Category actions on the fetus by the FDA — with. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Use of meloxicam, as well as other drugs, blokiruyushtih synthesis NG, It can affect fertility, so it is not recommended for women, wishing to get pregnant.

Meloxicam is excreted into the milk of lactating rats, The concentrations in the milk exceeds plasma concentration. Unknown, Meloxicam penetrates into whether the breast milk of women, so you should stop breast-feeding during treatment or avoid the use of meloxicam during breastfeeding.

Side effects.

From the digestive tract: >1% -neuralgia, nausea, vomiting, abdominal pain, constipation / diarrhea, flatulence; 0,1-1%, stomatitis, Transient changes in liver function tests (increase in transaminases or bilirubin), belching, esophagitis, peptic ulcer, macroscopically visible or hidden gastrointestinal bleeding; <0,1% -gastrointestinal perforation, colitis, gastritis.

From the nervous system and sensory organs: >1% - Headache, dizziness; 0,1-1% of Vertigo, drowsiness, noise in ears; <1% - Conjunctivitis, blurred vision.

Cardio-vascular system and blood (hematopoiesis, hemostasis): >1% - Swelling, anemia; 0,1-1%-raising hell, heartbeat, flushing, changes in hemogram, incl. change in the amount of certain types of white blood cells, leukopenia, thrombocytopenia.

From the respiratory system: exacerbation of asthma, cough.

With the genitourinary system: 0,1-1% — to change the indicators of kidney function (increases in serum creatinine and / or blood urea); <1% - Acute renal failure, interstitial nephritis, glomerulonephritis, renal medullary necrosis, nephrotic syndrome.

For the skin: >1% -skin rash, itch; 0,1-1% urticaria; <0,1% - Photosensitivity, bullous reaction, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Allergic reactions: <0,1% - Angioedema, immediate hypersensitivity reactions, including anaphylactic and anaphylactoid.

Other: <0,1% -bronchospasm, fever.

Cooperation.

In an application with acetylsalicylic acid and other NSAIDs increases the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract. While the use of antihypertensive drugs may reduce the effectiveness of the latter. In an application with lithium possible cumulation of lithium and increase in its toxic action (It recommended to control the concentration of lithium in the blood). Concomitant use with methotrexate enhances side effects of the latter on the hematopoietic system (There is a risk of anemia and leukopenia. Requires periodic monitoring of blood count).

The combined use of diuretics and cyclosporine increases the risk of renal failure.

When using with intrauterine contraceptives may decrease the effectiveness of the latter. While the use of anticoagulants (Heparin, ticlopidine, warfarin), as well as thrombolytic agents (streptokinase, fiʙrinolizin) It increases the risk of bleeding (should periodically monitor the performance of blood clotting).

Simultaneous use with kolestiraminom increases the excretion of meloxicam through blood (by binding meloxicam).

At simultaneous reception of meloxicam with antacids pharmacokinetic interactions were found.

Overdose.

Symptoms: increased side effects.

Treatment: gastric lavage, administration of activated charcoal (within the hour), simptomaticheskaya therapy. Cholestyramine accelerates the elimination of the drug from the body. Forced diuresis, alkalization of urine, hemodialysis is ineffective because of the high regard of meloxicam blood protein. Specific antidotes and antagonists were found.

Dosing and Administration.

Inside, / m, rectally. Dose selected individually, necessary to use the lowest effective dose for a minimum period of time. Inside, while eating, without chewing, in a dose of 7.5-15 mg 1 once a day. V / m administration used only in the first few days after treatment, later moving to oral forms. When combined appointment (tablets and solution for the / m) the total daily dose should not exceed 15 mg. Rectally — one candle (15 mg) per day.

The maximum daily dose - 15 mg, in patients with severe renal insufficiency, in gemodialise — 7,5 mg. With low or moderate decrease in kidney function (creatinine clearance >25 ml / min), as well as in liver cirrhosis in stable clinical condition dose adjustment is required. The starting dose in patients with an increased risk of side effects is 7,5 mg / day.

Precautions.

To use caution in diseases of the upper gastrointestinal tract in history, in combination with anticoagulants, myelotoxicity drugs, incl. metotreksatom (possible cytopenia).

The appearance of gastroduodenal ulcers, GI bleeding, side effects of the skin and mucous membranes serves as a basis for drug withdrawal. If the treatment experienced allergic reactions (itch, skin rash, hives, photosensitivity), you must see a doctor to address the issue of drug discontinuation.

The risk of gastrointestinal complications. Serious side effects from the gastrointestinal tract, including inflammation, bleeding, ulceration and perforation of the stomach or intestines, can occur at any time without the use of NSAIDs symptoms heralding. A higher risk of serious gastrointestinal complications are elderly patients, probability of occurrence of these complications increases as long-term use.

Meloxicam, Like other NSAIDs, may mask the symptoms of infectious diseases.

Appointment of NSAIDs in patients with reduced renal blood flow and the BCC can accelerate renal decompensation (after discontinuation of NSAID kidney function is usually restored to its previous level). Particularly high risk of such reactions in patients with symptoms of dehydration, Congestive heart failure, cirrhosis of the liver, nephrotic syndrome and severe kidney disease, patients, receiving diuretics, and have undergone significant surgery, which led to hypovolemia (from the beginning of treatment should be carefully monitored diuresis and renal function). In rare cases, NSAIDs may cause interstitial nephritis, glomerulonephritis, renal medullary necrosis or nephrotic syndrome. With a significant deviation from the normal level of serum transaminases and other indicators, characterize the function of the liver, discontinue use and spend control laboratory studies. Be wary appoint older, weakened and depleted patients.

The use of meloxicam may cause the occurrence of such undesirable effects, as headache and dizziness, drowsiness. In this connection, it should give up driving, maintenance of machinery and other activities, requiring a high concentration.

Cooperation