Melbeck

Melbek is a medicine from the NSAID category (belongs to the oxicam group), and also a selective inhibitor of COX-2 activity, which contains enolic acid. The active element of the medicine is the substance meloxicam.

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

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Indications Melbeka

It is used for the following problems:

• symptomatic therapy for rheumatoid arthritis;
• elimination of pain in osteoarthritis, degenerative joint lesions, arthrosis and Bechterew's disease;
• elimination of pain of various origins (algomenorrhea, myalgia, toothache, dorsalgia, pain arising in connection with injuries or operations, as well as lumbosciatica).

Release form

The pharmaceutical product is produced in tablets of 7.5 mg (5, 10 or 30 pieces per pack) or 15 mg (10 pieces per box).

In addition, it is sold in the form of an injection liquid, inside 1.5 ml ampoules (10 pieces per box).

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

Pharmacodynamics

Clinical tests have shown 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 have a negative effect on the digestive tract and kidneys.

The principle of meloxicam's effect is safer because it selectively slows down the action of COX-2, having a selectivity coefficient IC50 COX-1/COX-2 of 2. This explains the lesser severity of the drug's effect on the gastrointestinal tract and kidneys.

Melbek does not change platelet aggregation and bleeding period if used in the specified doses. At the same time, naproxen with indomethacin, ibuprofen and diclofenac significantly prolong bleeding period and slow down platelet aggregation.

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Pharmacokinetics

Meloxicam is absorbed at high speed in the digestive system, regardless of food intake. Its bioavailability is 89%. After oral administration, blood Cmax values are recorded after 5-6 hours (after taking a 7.5 mg dose, the plasma Cmax level is 0.4-1 mg/ml, and after taking a 15 mg dose - 0.8-2.0 mg/ml). By the 3rd-5th day of therapy, equilibrium drug levels are observed.

When used intramuscularly, the drug is completely absorbed; after parenteral administration, the bioavailability index is almost 100%.

The pharmacokinetic parameters of meloxicam are linked to the dosage size in the case of intramuscular administration of 5 and 30 mg of the drug.

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

Approximately 99.5% of meloxicam is synthesized with blood protein. The level of the drug inside the synovium is half the plasma levels of the substance.

Biotransformation of the drug occurs inside the liver by oxidation of methyl parts to form 4 metabolic components that do not have therapeutic activity.

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

Problems with kidney or liver function do not have a noticeable effect on the pharmacokinetic characteristics of meloxicam. Plasma clearance of the drug is 8 ml per minute (in elderly people it decreases). Meloxicam has a low distribution volume (approximately 11 l).

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Dosing and administration

The drug can be administered intramuscularly, as well as rectally or orally.

The dose of the medicine is selected individually. It is required to use it in minimal effective doses, over the shortest possible period of time.

The tablets should be taken orally with food, without chewing, once 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 oral administration of the drug.

In case of complex use of drugs (tablets together with intramuscular injections), the total daily dose of 15 mg should not be exceeded.

Melbek suppositories are administered 1 piece per day (15 mg).

No more than 15 mg of the drug can be used per day. People with severe renal insufficiency, and in addition to this, people undergoing hemodialysis, can be administered a maximum of 7.5 mg of the drug per day.

In case of mild or moderate weakening of renal function, as well as in case of compensated liver cirrhosis, it is not necessary to change the dose of the drug. People with an increased risk of negative symptoms should initially take 7.5 mg of the drug per day.

The drug solution cannot be used intravenously.

Use Melbeka during pregnancy

Melbek should not be used during breastfeeding or pregnancy.

Contraindications

Main contraindications:

• severe liver or kidney failure;
• established intolerance caused by meloxicam and other components of the drug;
• peptic ulcer, affecting the gastrointestinal tract (active phase);
• nasal polyposis or BA;
• Quincke's edema or urticaria caused by the use of aspirin or other drugs from the NSAID category.

Side effects Melbeka

Side effects of the drug include:

• constipation, bloating, nausea, pain in the abdominal area, diarrhea, belching and vomiting, as well as hepatitis, esophagitis, gastritis, gastroduodenal ulcer, colitis and a temporary increase in transaminase or bilirubin levels;
• thrombocytopenia or leukopenia, as well as anemia;
• itching, stomatitis, epidermal irritation and urticaria;
• tinnitus, mood lability, dizziness, lethargy and headaches;
• hot flashes, palpitations, swelling and increased blood pressure;
• increased creatinine or urea levels, as well as acute renal failure;
• conjunctivitis or visual impairment;
• Quincke's edema and symptoms of intolerance.

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Overdose

In case of poisoning with the drug, the side effects of meloxicam may be potentiated.

Gastric lavage is performed, activated charcoal is used, and symptomatic measures are taken.

The rate of excretion of the drug increases cholestyramine. Since meloxicam has a high rate of synthesis with blood protein, the processes of forced diuresis, alkalization of urine or hemodialysis will be ineffective. The drug has no antidote.

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Interactions with other drugs

The combined use of 2 or more drugs from the NSAID category increases the ulcerogenic risk and the likelihood of bleeding within the gastrointestinal tract due to the synergistic effect of the drugs.

It is impossible to use drugs together with lithium salts, because NSAIDs can weaken the renal excretion of lithium, due to which it can accumulate, developing a toxic effect in the future.

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.

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

The drug weakens the contraceptive properties of the intrauterine device.

The use of Melbek and diuretics requires drinking large amounts of fluid.

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

NSAIDs, ACE inhibitors, and angiotensin-2 receptor blockers have synergy with glomerular filtration, which can lead to acute renal failure in individuals with a history of renal dysfunction.

In the digestive system, meloxicam is capable of synthesizing with cholestyramine, which increases the rate of excretion of the former.

The drug is prohibited to be combined with cyclosporine to prevent an increased likelihood of developing the nephrotoxic effect of the latter.

The possibility of interaction between drugs and orally administered hypoglycemic drugs cannot be ruled out.

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Storage conditions

Melbek should be stored in a dark place, out of reach of children. Temperature level – maximum 25°C.

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Shelf life

Melbek can be used within a 4-year period from the date of sale of the medicinal substance.

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Application for children

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

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Analogues

The analogs of the drug are Movalis, Mataren, Movasin with Meloxicam, Mirlox and Revmoxicam with Mesipol and Amelotex, and also Bi-Xikam and Artrozan.

Reviews

Melbek is considered one of the most effective drugs that relieve pain in case of arthrosis or arthritis - this is what medical specialists say about it in their reviews. At the same time, it is noted that, in comparison with other NSAIDs, this medication does not have such an intense negative effect on the digestive system with prolonged use, and this is extremely important when using NSAIDs in a course.