Meloxicam

Meloxicam is a drug of the oxicam class. The drug is a NSAID substance from the enolic acid subgroup; it has analgesic, anti-inflammatory, and also antipyretic effects on the body.

Due to selective suppression of the activity of the isoenzyme COX-2, the anti-inflammatory and analgesic activity of the drug develops in the future. The drug Meloxicam has a selectivity coefficient IS50, which is equal to 2.

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Indications Meloxicam

It is used to eliminate the symptoms of the following pathologies:

• exacerbations during arthrosis (short-term effect);
• polyarthritis, which has a chronic form (long-term effect);
• rheumatoid arthritis (long-term exposure);
• Bechterew's disease.

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Release form

The drug is released in tablets of 7.5 or 15 mg. There are 20 pieces inside the cell plate.

In addition, it is sold in the form of an injection (i/m) liquid, inside ampoules with a capacity of 1.5 ml (15 mg of the active element), 5 pieces inside a pack.

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Pharmacokinetics

It is absorbed almost completely in the digestive tract. After oral administration, absolute bioavailability is about 89%. After 5-6 hours from the moment of a single oral administration, the plasma Cmax indicator is observed. After 3-5 days of constant repeated administration, an equilibrium level of the drug is observed.

Equilibrium values of the drug (Cmin/Cmax) are in the range of 0.4-1.0 mg/l after oral administration of 7.5 mg of the drug, and 0.8-2.0 mg/l after taking 15 mg. The Cmax level remains unchanged with prolonged use. Taking with food does not change the intensity of drug absorption.

With intramuscular injections, the bioavailability level is also 89%, and plasma Cmax values are noted after 1 hour. In the case of using average therapeutic doses of the drug (7.5 or 15 mg), linear pharmacokinetics are noted.

The affinity of the drug to the intraplasmic protein is quite high (this especially concerns albumin – up to 99%). 50% of the plasma values are noted inside the synovium. The level of distribution volume is on average up to 11 liters (individual variation limits – 30-40%). Metabolic processes are realized with intrahepatic enzymes.

Elimination occurs in equal parts through the intestines and kidneys; 4 metabolic elements of the drug (without therapeutic activity) are found in the urine. The main metabolite is 5'-carboxymeloxicam, which is equal to 60% of the applied portion and is formed during the oxidation of intermediate components (for example, the substance 5'-hydroxymethylmeloxicam). The latter is excreted unchanged by 9%.

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Dosing and administration

The tablets are taken once a day, with food. The medicine should be washed down with plain water (0.25 l).

The injection liquid can only be administered intramuscularly; intravenous use of the substance is prohibited. Intramuscular injections should be used during the first days of treatment, and then the patient should be transferred to oral tablets.

In case of exacerbation of arthrosis, 7.5 mg of the drug is used once a day. If the medicinal effect is insufficient, the dose can be increased to 15 mg.

In case of rheumatoid arthritis or Bechterew's disease, 15 mg of the drug is administered once a day. When the required medicinal effect is achieved, the daily dose is reduced to 1-time use of 7.5 mg per day. It is prohibited to use more than 15 mg of Meloxicam per day.

People undergoing dialysis, as well as people with renal insufficiency, should use a maximum of 7.5 mg per day. In mild or moderate forms of the disorder (the level of CC is more than 25 ml per minute), it is permissible not to reduce the dosage of the drug.

Elderly people with arthritis of rheumatoid origin or with Bechterew's disease, if long-term therapy is required, should take 7.5 mg of the substance per day. If it is necessary to use a higher dose, but with the risk of negative symptoms, the daily dosage is maintained at 7.5 mg.

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Use Meloxicam during pregnancy

Meloxicam should not be prescribed during pregnancy.

Contraindications

Main contraindications:

• ulcers affecting the gastrointestinal tract (both those present in the acute phase and those present in the anamnesis);
• severe intolerance caused by the action of the active element or other components of the drug, and in addition to other NSAIDs, including aspirin. It is strictly forbidden to prescribe to people who develop nasal polyps, urticaria, Quincke's edema or symptoms of bronchial asthma after the introduction of any NSAID;
• bleeding affecting the gastrointestinal tract;
• breast-feeding;
• having cerebrovascular bleeding;
• severe liver or kidney failure;
• bleeding affecting other organs;
• having a strong CH intensity that cannot be corrected.

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Side effects Meloxicam

Side effects include:

• lesions affecting the blood system: sometimes changes in blood test results such as agranulocytosis and thrombocyto- or leukopenia appear. Anemia often develops;
• visual impairment: changes in visual acuity occasionally occur;
• immune disorders: symptoms of personal intolerance to drugs are occasionally observed;
• problems affecting the central nervous system: loss of consciousness and severe headaches are often observed. Sometimes dizziness or tinnitus appear. Occasionally, drowsiness, nightmares, confusion and mood lability are recorded;
• Gastrointestinal disorders: often there is stomach discomfort or pain, bloating, constipation or diarrhea, pain affecting the epigastrium, vomiting with severe nausea. Sometimes stomatitis or esophagitis occurs, as well as an ulcer affecting the stomach or bleeding in the gastrointestinal area. Colitis, gastritis or perforation of the gastrointestinal wall occasionally develops. The most severe digestive disorders are observed in the elderly - an increase in cases of perforation, bleeding in the gastrointestinal area or peptic ulcers;
• signs affecting the functioning of the cardiovascular system: sometimes tachycardia, increased blood pressure, and dilation occurring in the subcutaneous vessels (accompanied by fever) are observed;
• urinary dysfunction: sometimes problems with kidney function occur, with an increase in serum urea and creatinine values. Occasionally, renal failure occurs;
• problems associated with external respiration: rarely, asthma attacks have developed in individuals with a history of allergy to NSAIDs (especially aspirin);
• epidermal lesions: rashes and itching of allergic origin are often observed. Urticaria sometimes occurs. Occasionally, SJS or TEN, photosensitivity, Quincke's edema affecting the epidermis or mucous membranes, and in addition, erythema multiforme appear;
• disorders affecting the hepatobiliary system: sometimes problems with liver function are observed. Hepatitis is rarely recorded;
• Others: swelling is often observed.

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Overdose

Acute NSAID poisoning causes drowsiness, vomiting, abdominal pain, and nausea. These symptoms are often eliminated with symptomatic agents. Gastrointestinal bleeding occasionally occurs.

In case of intoxication with large doses of drugs, liver function is disrupted, blood pressure increases, respiration is suppressed, and in addition, convulsions of acute renal failure or collapse develop. Cardiac arrest or a comatose state may occur.

There are reports of the occurrence of anaphylactoid symptoms in case of drug overdose, as well as in the case of administration of therapeutic doses.

Supportive and symptomatic measures should be taken. Therapy is carried out taking into account the signs of poisoning and their intensity. Clinical tests have shown that oral administration of 4 g of colestyramine increases the rate of drug elimination threefold.

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Interactions with other drugs

Pharmacokinetic drug interactions.

NSAIDs, including Meloxicam, when administered simultaneously with lithium can increase its serum levels to toxic levels, because they weaken the renal excretion of lithium. Therefore, the drug cannot be combined with lithium substances. If such a combination is necessary, it is necessary to carefully monitor the values of lithium electrolyte in the blood serum (before starting to use the drug, during therapy, and for some period after the end of the course).

Cholestyramine increases the rate of drug elimination; at the same time, meloxicam clearance values are doubled and its half-life is shortened (by approximately 13(±3) hours). This effect has significant clinical impact.

Methotrexate increases the negative impact that Meloxicam has on the blood system (there is a high risk of developing anemia or leukopenia). With such a combination, it is necessary to periodically monitor the hemogram readings.

NSAIDs reduce the effectiveness of intrauterine contraceptive devices.

Pharmacodynamic drug interactions.

The combined administration of the drug and diuretic drugs requires the intake of sufficient volumes of fluid during therapy. At the same time, it is also necessary to constantly and carefully monitor the functioning of the kidneys (before and during treatment). Such monitoring should be carried out by medical specialists.

Thrombolytics and antithrombotic agents in combination with the drug significantly increase the likelihood of bleeding. With such use of the drug, it is necessary to periodically monitor the values of blood coagulation potential.

The probability of gastrointestinal lesions of an ulcerative-erosive nature increases sharply when used together with NSAIDs from other categories (this includes derivatives of salicylic acid). Therefore, such a combination cannot be used.

When using ACE inhibitors and other antihypertensive drugs in elderly people with dehydration, acute renal failure may occur. In addition, the combined administration of such drugs with Meloxicam may lead to the disappearance of the antihypertensive effect.

Combination of drugs with orally administered anticoagulants significantly increases the likelihood of bleeding from various organs due to damage to the gastrointestinal mucosa and inhibition of platelet activity. For this reason, such combinations are not used.

The drug weakens the therapeutic effect of hormonal contraception.

When the drug is administered, the nephrotoxic effect of cyclosporine is potentiated.

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Storage conditions

Meloxicam must be stored at a temperature of 25°C.

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Shelf life

Meloxicam can be prescribed for a period of 24 months from the date of sale of the medicinal substance.

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Application for children

Not for use in persons under 15 years of age.

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Analogues

The analogs of the drug are Amelotex, Movalis, Bi-Xikam and Movasin with Melbek, and in addition to this, Artrozan, Mesipol and Revmoksikam with Mataren, as well as Mirloks.

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