Mauve

Melbek is a drug from the category of NSAIDs (included in the group of oxycams), as well as a selective inhibitor of COX-2 activity, which contains enolic acid. The active element of the drug is the substance of meloxicam.

The drug has an intense anti-inflammatory, as well as anesthetic and antipyretic effect. Meloxicam helps to slow down the biosynthesis of inflammatory mediators (PGs) by selectively inhibiting the action of COX-2. This process is the main principle of the impact of drugs.

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Indications Melbeka

Used for such problems:

• symptomatic therapy for rheumatoid arthritis;
• elimination of pain in osteoarthritis, degenerative joint lesions, arthrosis and ankylosing spondylitis;
• elimination of pains of various nature (algodysmenorrhea, myalgia, toothache, dorsalgia, pain appearing in connection with injuries or operations, as well as lumboischialgia).

Release form

Pharmaceutical products are manufactured in tablets of 7.5 mg (5, 10 or 30 pieces inside a pack) or 15 mg (10 pieces inside a box).

In addition, it is realized in the form of injection fluid, inside ampoules with a capacity of 1.5 ml (10 pieces in a box).

Also available in the form of rectal suppositories (15 mg volume) - 10 pieces per package.

Pharmacodynamics

In clinical tests, it was found that meloxicam has lower toxicity compared to other substances from the NSAID category (naproxen with piroxicam and diclofenac). The latter also effectively suppress the activity of COX-1 with COX-2, but at the same time they have a negative effect on the digestive tract and kidneys.

The principle of influence of meloxicam is safer, because it selectively slows down the effect of COX-2, having an IC50 COX-1 / COX-2 selectivity factor of 2. This is what explains the lesser severity of the effect of drugs on the gastrointestinal tract and kidneys.

Melbeck does not alter platelet aggregation and bleeding period, if it is applied in specified portions. At the same time, naproxen with indomethacin, ibuprofen and diclofenac significantly prolong the period of bleeding and slow down platelet aggregation.

[2], [3],

Pharmacokinetics

Meloxicam is absorbed at high speed inside the digestive system, regardless of the use of food. Its bioavailability is 89%. After ingestion, blood values of Cmax are fixed after 5-6 hours (after consuming a dose of 7.5 mg, plasma level Cmax is 0.4–1 mg / ml, and after administration of a dose of 15 mg - 0.8–2.0 mg / ml). By the 3-5th day of therapy, equilibrium parameters of drugs are observed.

When i / m using the drug is completely absorbed, after parenteral administration the bioavailability index is almost 100%.

The pharmacokinetic parameters of meloxicam are tied to the size of the dosage in the case of i / m use of 5 and 30 mg of drugs.

Plasma Cmax values are recorded after 60 minutes have passed since the injection. Stable plasma values are observed by the 3-5th day of treatment.

Approximately 99.5% of meloxicam is synthesized with blood protein. The drug level inside synovia is twice as low as the plasma parameters of the substance.

Biotransformation of the drug is performed inside the liver by oxidizing the methyl parts to form 4 metabolic components that do not possess therapeutic activity.

Approximately 42% of the consumed portion of the drug is excreted in the urine, and the remainder in the bile. Less than 5% of the drug is excreted unchanged through the intestines. The term half-life is 20 hours.

Problems with the work of the kidneys or liver do not have a noticeable effect on the pharmacokinetic characteristics of meloxicam. Plasma clearance of drugs is equal to 8 ml per minute (in older people, it decreases). Meloxicam has a low distribution volume (about 11 liters).

[4],

Dosing and administration

The drug can be administered in the m / m way, and also rectally or orally.

A portion of the medication is selected personally. It is required to apply it in the minimum effective portions during the shortest possible time interval.

Tablets should be taken orally with food, without chewing, 1 time a day in a dose of 7.5-15 mg.

Intramuscular injections should be used only during the first days of treatment, and then the patient is transferred to the oral use of drugs.

In the case of complex use of drugs (tablets with injections injections), the total dose per day should not exceed 15 mg.

Suppositories Melbek administered on the 1st unit per day (15 mg).

During the day you can use no more than 15 mg of the drug. Persons with severe kidney function deficiency, and in addition to those who are on hemodialysis, you can enter a maximum of 7.5 mg of drugs per day.

In the case of mild or moderate impairment of renal function, as well as with compensated hepatic cirrhosis, it is not necessary to change the dose of the drug. People with an increased risk of negative signs should first take 7.5 mg of the drug per day.

The drug solution can not be administered intravenously.

Use Melbeka during pregnancy

When breastfeeding and pregnancy can not be used Melbek.

Contraindications

The main contraindications:

• lack of liver or kidney function in severe;
• established intolerance caused by meloxicam and other components of the drug;
• peptic variety of ulcers affecting the digestive tract (active phase);
• nasal polyposis or BA;
• Quincke edema or urticaria, triggered by the use of aspirin or other drugs from the category of NSAIDs.

Side effects Melbeka

Among the adverse symptoms of medication:

• constipation, bloating, nausea, abdominal pain, diarrhea, belching and vomiting, and besides hepatitis, esophagitis, gastritis, gastroduodenal ulcer, colitis and a temporary increase in transaminase or bilirubin values;
• platelet or leukopenia, as well as anemia;
• itching, stomatitis, epidermal irritation, and urticaria;
• ear noise, mood lability, dizziness, lethargy and headaches;
• hot flashes, palpitations, puffiness and an increase in blood pressure;
• an increase in creatinine or urea, as well as acute renal failure;
• conjunctivitis or a disorder of visual function;
• Quincke edema and intolerance symptoms.

[5], [6]

Overdose

In case of drug poisoning, meloxicam side effects may potentiate.

Gastric lavage is performed, activated carbon is applied, and symptomatic actions are performed.

The rate of excretion of drugs increases cholestyramine. Since meloxicam has a high rate of synthesis with blood protein, the processes of forced diuresis, alkalinization of urine or hemodialysis will be ineffective. The drug does not have an antidote.

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Interactions with other drugs

The combined use of 2 or more drugs from the category of NSAIDs increases the ulcerogenic risk and the likelihood of bleeding inside the gastrointestinal tract due to the synergy of the influence of medicines.

Drugs should not be used together with lithium salts, because NSAIDs are able to weaken the renal excretion of lithium, because of which it can accumulate, developing further toxic effects.

The combination with methotrexate leads to an increase in its toxic effect on hematopoiesis, which is why it is necessary to regularly monitor the dynamics of hemogram readings.

Introduction together with ticlopidine and heparin leads to an increase in their therapeutic properties, which increases the likelihood of bleeding in the GI tract.

The drug weakens the contraceptive properties of the intrauterine device.

Using Melbec and diuretics requires the use of large quantities of fluid.

Meloxicam can weaken the effect of antihypertensive substances (ACE inhibitors, as well as drugs that block the action of β-adrenergic receptors).

Medicines from the category of NSAIDs, ACE inhibitors, as well as antagonists of the endings of angiotensin-2 have synergy with respect to filtration of the glomeruli, which can cause ARF in people with a history of renal dysfunction.

Inside the digestive system, meloxicam can be synthesized with Kolestiramine, which increases the rate of excretion of the first.

The drug should not be combined with cyclosporin - to prevent an increase in the likelihood of the nephrotoxic effect of the latter.

We can not exclude the possibility of the development of drug interactions and hypoglycemic drugs taken by mouth.

[8], [9], [10], [11]

Storage conditions

Melbek is required to keep in a closed place from the children. The temperature level is maximum 25 ° C.

[12]

Shelf life

Melbeck can be used within a 4-year term since the sale of the drug substance.

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Application for children

The drug is not prescribed to children under the age of 15 years.

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Analogs

Analogs of drugs are Movalis, Matarin, Movasin with Meloxicam, Mirlox and Revmoxicam with Mesipol and Amelotex, as well as Bi-Skikam and Artrozan.

Reviews

Melbeck is considered one of the most effective drugs to ease pain in the event of arthrosis or arthritis - that’s what the medical experts say about it in their reviews. At the same time, it is noted that, in comparison with other NSAIDs, this medicine does not have such an intensive negative effect on the digestive system with prolonged use, and this is extremely important for course use of NSAIDs.