Meloxicam

Meloxicam is included in the oxycam drug category. The drug is a substance NSAIDs from a subgroup of means of enolievo acid; It has an analgesic, anti-inflammatory, and in addition to this antipyretic effect on the body.

Due to the selective suppression of the activity of COX-2 isoenzyme, the anti-inflammatory and analgesic activity of drugs is further developed. The drug Meloxicam has an IS 50 selectivity coefficient, which is equal to the 2nd.

[1], [2], [3], [4]

Indications Meloxicam

It is used to eliminate the symptoms of such pathologies:

• exacerbations during osteoarthritis (brief effect);
• chronic arthritis (chronic effect);
• arthritis of rheumatoid nature (prolonged exposure);
• ankylosing spondylitis

[5], [6], [7], [8]

Release form

The release of the drug produced in tablets of 7.5 or 15 mg. Inside the cell plate - 20 pieces.

In addition, it is implemented as an injection (v / m) liquid, inside an ampoule with a capacity of 1.5 ml (15 mg of the active element), 5 pieces in a pack.

[9], [10], [11]

Pharmacokinetics

Absorbed almost fully inside the digestive tract. After ingestion, the absolute bioavailability is about 89%. After 5-6 hours after 1 single oral administration, plasma Cmax is observed. After 3-5 days of continuous re-administration, an equilibrium level of drugs is noted.

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

When i / m injections, the level of bioavailability is also equal to 89%, and the values of plasma Cmax are noted already after the expiration of the 1st hour. In the case of the use of medium therapeutic portions of drugs (7.5 or 15 mg), linear pharmacokinetics are noted.

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

Elimination takes place in equal parts through the intestines and kidneys; Inside the urine, 4 metabolic elements of drugs (not having therapeutic activity) are found. The main metabolite is 5'-carboxymeloxicam, which is up to 60% of the portion used and is formed during the oxidation of intermediate components (for example, substances 5'-hydroxymethylmeloxicam). The latter is 9% excreted unchanged.

[12], [13], [14], [15], [16]

Dosing and administration

Tablets are consumed 1 time a day, along with food. It is necessary to wash down the medicine with plain water (0.25 l).

Injection fluid can be administered only intramuscularly, intravenous use of the substance is prohibited. Apply intramuscular injections should be during the first days of treatment, and then transfer the patient to oral pills.

In case of exacerbation of the flow of arthrosis, 7.5 mg of the drug is used 1-fold per day. With insufficient medication exposure can be increased to 15 mg.

In the case of arthritis of rheumatoid nature or ankylosing spondylitis, 15 mg of the drug are administered once a day. Upon reaching the desired medicinal effect, the daily dose is reduced to 1-fold application of 7.5 mg per day. It is forbidden to use more than 15 mg of Meloxicam per day.

Persons who are on dialysis, and in addition, people with kidney failure should use a maximum of 7.5 mg per day. In case of light or moderate forms of violation (the level of CC is more than 25 ml per minute) it is allowed not to reduce the dosage of drugs.

Elderly people with arthritis with a rheumatoid nature, or with ankylosing spondylitis with the need for long-term therapy should be applied daily for 7.5 mg of the substance. If you need to use a higher portion, but with the risk of negative symptoms, the daily dosage is kept at around 7.5 mg.

[19], [20], [21]

Use Meloxicam during pregnancy

You can not assign meloxicam during pregnancy.

Contraindications

The main contraindications:

• ulcers affecting the gastrointestinal tract (as available in the acute phase, and in the presence of a history);
• 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 appoint persons who develop nasal polyps, urticaria, angioedema, or asthma symptoms after the introduction of any NSAIDs;
• bleeding affecting the digestive tract;
• breast-feeding;
• having cerebrovascular bleeding;
• lack of liver or kidney function in severe;
• bleeding that affects other organs;
• having a strong CH intensity that cannot be corrected.

[17]

Side effects Meloxicam

Among the side effects:

• lesions affecting the blood system: sometimes there are such changes in the testimony of a blood test such as agranulocytosis and thrombocyto- or leukopenia. Anemia often develops;
• visual impairment: occasionally there is a change in visual acuity;
• immune disorders: symptoms of personal intolerance to drugs are rarely noted;
• problems affecting the work of the central nervous system: loss of consciousness and severe headaches are often observed. Sometimes there is dizziness or ear noise. Occasionally, drowsiness, nightmares, confused consciousness, and mood lability are recorded;
• disorders associated with the function of the gastrointestinal tract: often there is gastric discomfort or pain, bloating, constipation or diarrhea, pain that affects epigastrium, vomiting with severe nausea. Occasionally, stomatitis or esophagitis occurs, as well as stomach ulcers or bleeding in the gastrointestinal tract. Occasionally develops colitis, gastritis, or perforation of the gastrointestinal wall. The most severe disorders of the digestive activity are observed in the elderly - an increase in the number of cases of perforation, bleeding in the gastrointestinal zone or peptic ulcers;
• signs affecting the work of the cardiovascular system: sometimes there is tachycardia, an increase in blood pressure, as well as an expansion that occurs with subcutaneous vessels (accompanied by fever);
• urinary function disorders: sometimes there are problems with the work of the kidneys, in which there is an increase in serum values of urea with creatinine. Rarely, renal function failure occurs;
• problems with external breathing: occasionally, individuals with a history of allergies to NSAIDs (especially with respect to aspirin) developed asthma attacks;
• epidermal lesions: rash and itching of an allergic nature are often noted. Sometimes urticaria occurs. Occasionally there is a SSD or TEN, photosensitivity, angioedema, affecting the epidermis or mucous membranes, and in addition to this polyformal erythema;
• disorders affecting the hepatobiliary system: sometimes there are problems with the work of the liver. Hepatitis is rarely reported;
• Other: often marked swelling.

[18]

Overdose

In case of acute poisoning with NSAIDs, drowsiness, vomiting, pain in the abdominal area and nausea appear. Such symptoms are often eliminated with the help of symptomatic substances. Occasionally, bleeding occurs in the gastrointestinal tract.

With intoxication with large portions of drugs, there is a disorder of liver activity, an increase in blood pressure, suppression of respiration, and in addition, the development of seizures of acute renal failure or collapse. Cardiac arrest or coma may occur.

There is information about the appearance of anaphylactoid symptoms in overdose with medication, as well as in the case of the introduction of its therapeutic rations.

It is necessary to perform supportive and symptomatic actions. Therapy is carried out, taking into account the signs of poisoning and their intensity. In clinical tests, it was determined that oral administration of 4 g of colestyramine tripled the rate of elimination of the drug.

[22], [23]

Interactions with other drugs

Pharmacokinetic drug interactions.

NSAIDs, among which the drug Meloxicam, when administered simultaneously with lithium, can increase its serum values to toxic levels, because they weaken the renal excretion of lithium. Therefore, it is impossible to combine the drug with lithium substances. If such a combination is necessary, it is necessary to carefully monitor the values of lithium electrolyte inside the blood serum (before starting the use of the drug, during therapy, as well as for a certain period after the completion of the course).

Kolestyramine increases the rate of elimination of the drug; at the same time, there is a twofold increase in the clearance values of meloxicam, as well as a reduction in its half-life (approximately 13 (± 3) hours). This effect has a significant clinical effect.

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

NSAID drugs reduce the effectiveness of intrauterine contraceptive agents.

Pharmacodynamic drug interactions.

Combined administration of the drug and diuretic drugs requires the reception of sufficient volumes of fluid during therapy. At the same time, you also need to constantly and closely monitor the work of the kidneys (before and during treatment). To conduct such a control should medical professionals.

Thrombolitics and antithrombotic substances in combination with the drug significantly increase the likelihood of bleeding. With this use of drugs you need to periodically monitor the values of blood coagulation potential.

The likelihood of gastrointestinal lesions with an ulcer-erosive nature increases dramatically when used together with NSAIDs from other categories (this includes salicylic acid derivatives). Therefore, this combination can not be used.

When using substances of an ACE inhibitor and other antihypertensive drugs in people with dehydration, acute renal failure may be observed. In addition, the combined introduction of such agents with Meloxicam may lead to the disappearance of the antihypertensive effect.

The combination of drugs with ingestible anticoagulants significantly increases the likelihood of bleeding from various organs - due to damage to the mucous membranes of the gastrointestinal tract, as well as inhibition of platelet activity. Because of this, such combinations do not apply.

The drug weakens the therapeutic effects of hormonal contraception.

With the introduction of drugs potentiated nephrotoxic effect of cyclosporin.

[24]

Storage conditions

Meloxicam is required to be kept at temperatures within the 25 ° C mark.

[25], [26]

Shelf life

Meloxicam can be prescribed for a 24-month term from the moment the drug substance is sold.

[27], [28]

Application for children

Not used in persons under the age of 15.

[29], [30], [31]

Analogs

Analogues of drugs are Amelotex, Movalis, Bi-Hsikam and Movasin with Melbec, and in addition Artrozan, Mesipol and Revmoksikam with Mataren, as well as Mirloks.

[32], [33], [34], [35], [36], [37]