Meloxicam is an effective anti-inflammatory and pain reliever

Pharmacological properties of the drug Meloxicam-ratiopharm

Meloxicam is an NSAID of the oxicam group with anti-inflammatory, analgesic and antipyretic properties that are associated with selective inhibition of the COX-2 isoenzyme. The selectivity coefficient IC50 for meloxicam is 2. Meloxicam is almost completely absorbed from the gastrointestinal tract. Absolute bioavailability after oral administration is about 89%. After a single oral dose, the maximum concentration in the blood plasma is reached after 5–6 hours. With repeated administration, an equilibrium state is achieved after 3–5 days from the start of use. When taken orally at a dose of 7.5 or 15 mg of meloxicam 1 time per day, the concentration in the blood plasma (Cmin–Cmax) at steady state reaches 0.4–1.0 mg/l (7.5 mg) or 0.8– 2.0 mg/l (15 mg), respectively. With long-term use, the concentration in the blood plasma at steady state does not change. Absorption does not change when taken simultaneously with food. The bioavailability of meloxicam after intramuscular administration is 89%. The maximum concentration in the blood is achieved 1 hour after administration. Meloxicam has a high degree of binding to blood proteins, mainly albumin (99%). Meloxicam enters the synovial fluid, the concentration in it is equal to the concentration in the blood plasma. The volume of distribution is on average 11 liters. Individual variations are approximately 30–40%. Meloxicam is metabolized by liver enzymes. Four different pharmacologically inactive metabolites of meloxicam have been identified in urine. The main metabolite, 5'-carboxymeloxicam (60%), is formed by oxidation of intermediate metabolites 5'-hydroxymethylmeloxicam. The amount of 5'-hydroxymethylmeloxicam released unchanged is 9%. In vitro , it was found that the initial stage of this transformation is carried out mainly through CYP 2C9 with minor participation of CYP 3A4. The formation of two other metabolites (16 and 4% of the dose taken, respectively) is associated with the action of peroxidase. Meloxicam is excreted mainly in the form of metabolites, in equal parts with urine and feces. Meloxicam is detected in urine in insignificant (trace) quantities. The average half-life is about 20 hours. The total plasma clearance averages 8 ml/min. When administered orally in therapeutic doses (7.5 and 15 mg), meloxicam exhibits linear pharmacokinetics.

Meloxicam is an effective anti-inflammatory and pain reliever

One of the common anti-inflammatory drugs is meloxicam. Meloxicam belongs to the oxicam group.

Oxicams are a group of medications that are nonsteroidal anti-inflammatory drugs, or NSAIDs. Meloxicam is available in 7.5 mg tablets. Meloxicam is available in yellow tablets with a flat-cylindrical shape.

Meloxicam has anti-inflammatory, analgesic and antipyretic effects on the body. Basically, these effects are due to the effect on the enzyme cyclooxygenase. The anti-inflammatory effect of this drug has been tested on all standard biological models of inflammation.

With the development of inflammation, a large amount of prostaglandins (PGs) are released into the blood, which cause the main manifestations and symptoms. Meloxicam inhibits the action of PG. Two forms of the cyclooxygenase enzyme circulate in the human body: COX 1 and COX 2. COX 1 works constantly, COX 2 is activated only during inflammation. Meloxicam inhibits more COX2 in the body than COX1. Therefore, its use has far fewer side effects than other non-steroidal anti-inflammatory drugs. This fact has been proven during tests on various systems, both in laboratory conditions and in clinical trials. In addition, it was proven that greater blocking of COX-2 than COX-1 depended on the dosage of the drug.

When the drug is taken orally, meloxicam enters the bloodstream from the gastrointestinal tract. The maximum concentration of the substance occurs after 6 hours. The absorption of the drug is not affected by food or taking antacids.

Meloxicam, when entering the body, binds to proteins in the plasma, with 99% of the substance bound to albumin. In addition, it enters the synovial fluid of the joints, and the concentration of the substance is 50% of the concentration of the substance in the blood.

Meloxicam is processed in the liver, and 4 inactive components are synthesized. Isoenzymes such as CYP2C9 and CYP3A4 also play a major role in the deactivation process. Thanks to their work, two main metabolites are formed. The enzyme peroxidase is involved in the formation of two other inactive substances.

Meloxicam is removed from the body by the intestines and kidneys. The half-life of the drug takes about a day. In various liver diseases or liver failure, meloxicam is excreted from the body at the same rate. In case of renal failure, the rate of elimination increases significantly. If a patient is diagnosed with end-stage renal failure, there is a high concentration of the active substance in the blood, which requires adjustment of the dosage of the drug. In elderly patients, no significant differences in the pharmacokinetics of the drug were observed.

Meloxicam is prescribed as a symptomatic treatment for various joint diseases, such as osteoarthritis, rheumatoid arthritis, and spondylitis. In addition, the drug is taken to reduce pain and inflammation. At the same time, this drug does not affect the course of the disease.

When taking the drug, it is necessary to take into account a large number of contraindications, such as hypersensitivity to the drug, bronchial asthma, urticaria, nasal polyposis, as well as intolerance to aspirin and NSAIDs of other groups.

In addition, various diseases of the stomach and duodenum (erosions or ulcers), as well as inflammatory processes in the intestines, are also a contraindication for the use of meloxicam. Just as with the use of other NSAIDs, meloxicam is contraindicated in patients with various stages of renal and liver failure. In addition, severe heart disease, bleeding from various parts of the gastrointestinal tract, as well as diseases of the blood coagulation system are contraindications for meloxicam. Meloxicam should also not be taken during pregnancy at any stage or while breastfeeding.

When prescribing meloxicam, the doctor takes into account the patient’s concomitant pathology and, depending on the presence of any diseases, adjusts the dosage of the drug. To exclude the development of various complications from the gastrointestinal tract, the drug is prescribed in a minimum dosage, and the course of treatment is reduced as much as possible.

There are a large number of side or unwanted reactions when taking meloxicam. In this case, anemia, headache, emotional lability, tinnitus, various abdominal pains and other dyspeptic disorders can most often develop. Other possible complications are quite rare.

When taking other medications, it must be remembered that if the patient additionally takes other prostaglandin inhibitors, this may significantly increase the risk of developing ulcers and erosions of the gastrointestinal tract. In addition, simultaneous use of anticoagulants, thrombolytics and other drugs that affect hematopoiesis with meloxicam may increase the risk of bleeding.

It is also not recommended to take meloxicam together with methotrexate, lithium preparations, contraceptives and diuretics. The dosage of the drug is determined depending on the type of disease, stage of exacerbation and concomitant pathology. The drug is prescribed orally. Usually start with 7.5 mg per day, or, if the disease is in the acute stage, start with 15 mg per day and then reduce to 7.5 mg.

In case of overdose, the symptoms are nonspecific: vomiting, nausea, abdominal pain, renal and liver failure, and others. Treatment usually consists of gastric lavage, taking activated charcoal, and forced diuresis.

With long-term use of the drug, constant medical supervision is required, laboratory data and clinical symptoms should be assessed.

Meloxicam is a non-steroidal anti-inflammatory drug that causes fewer side effects than other drugs, but remains quite effective.

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Use of the drug Meloxicam-ratiopharm

The solution for injection is administered only intramuscularly (iv administration is contraindicated). It is advisable to prescribe parenteral administration only during the first days of treatment. For further therapy, it is recommended to use tablets. Arthrosis in the acute phase: dose 7.5 mg/day. If the condition does not improve, you can increase to 15 mg/day. Rheumatoid arthritis, ankylosing spondylitis: dose 15 mg/day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg/day. The daily dose of meloxicam should not exceed 15 mg. Take the daily dose 1 time during meals with a glass of water or other liquid. Special groups of patients Elderly patients with an increased risk of side effects In elderly patients, the recommended dose for long-term therapy of rheumatoid arthritis or ankylosing spondylitis is 7.5 mg / day. In patients with an increased risk of side effects, therapy should be started with a dose of 7.5 mg/day. Impaired renal function In dialysis patients with severe renal impairment, the daily dose of meloxicam should not exceed 7.5 mg. In patients with mild or moderate renal impairment (creatinine clearance more than 25 ml/min), there is no need to reduce the dose. Impaired liver function In patients with mild or moderately severe liver dysfunction, there is no need to reduce the dose of the drug.

Instructions for use of Meloxicam tablets

The dosage and procedure for use depend on the dosage form of the drug:

1. Tablets are consumed in quantities corresponding to a daily dosage of 7.5 to 15 mg. They are taken orally during meals.
2. Intramuscular injections are given to patients over the age of 15 years in the same dosage - from 7.5 to 15 mg per day. After a few days, the injections are stopped and, if necessary, pills are started.
3. Suppositories are administered rectally once a day (each suppository corresponds to a daily dosage of the active substance of 15 mg).

Attention!

If the patient has a kidney problem and is undergoing hemodialysis, the daily dosage should not exceed 7.5 mg. For other varieties of Meloxicam (Prana, Ratiopharm, Lugal), dosage recommendations may be different - they need to be specified in the instructions.

Contraindications to the use of the drug Meloxicam-ratiopharm

Hypersensitivity to meloxicam or other NSAIDs, including acetylsalicylic acid (contraindicated in patients who experience symptoms of asthma, nasal polyps, angioedema or urticaria after taking acetylsalicylic acid or other NSAIDs); During pregnancy and breastfeeding; gastrointestinal ulcers (both in history and in the acute phase); severe liver or kidney failure; gastrointestinal and cerebrovascular bleeding or bleeding of other localization; severe uncorrectable heart failure; age up to 15 years.

Side effects of the drug Meloxicam-ratiopharm

When assessing the frequency of side effects, the following statistics are used as a basis:

From the peripheral blood: often - anemia; sometimes - changes in the blood picture - thrombocytopenia, leukopenia, agranulocytosis. From the immune system: rarely - allergic reactions. From the side of the central nervous system: often - loss of consciousness, headache; sometimes - dizziness, tinnitus; rarely - mood swings, drowsiness and nightmares, confusion. From the side of the organ of vision: rarely - impaired visual acuity. From the cardiovascular system: sometimes - tachycardia, increased blood pressure, skin flushing with a feeling of heat. From the respiratory system: rarely - patients with a history of allergic reactions to acetylsalicylic acid or other NSAIDs may experience asthma attacks. From the gastrointestinal tract: often - pain in the epigastric region, nausea and vomiting, gastralgia, flatulence, constipation or diarrhea; sometimes - gastrointestinal bleeding, gastric ulcer, esophagitis, stomatitis; rarely - gastrointestinal perforation, gastritis, colitis. In elderly patients, peptic ulcers, perforations, or gastrointestinal bleeding may be particularly severe. From the liver and biliary tract: sometimes - impaired liver function; rarely - hepatitis. From the skin: often - itching, skin rash; sometimes - urticaria; rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis/Lyell's syndrome, angioedema of the skin and/or mucous membrane, erythema multiforme, photosensitivity. From the urinary system: sometimes - renal dysfunction (increased concentrations of urea and creatinine in the blood serum); rarely - renal failure. General disorders: often - swelling.

Contraindications and side effects

The drug should not be used if there are such contraindications:

• intolerance to pyrazolone and its derivatives;
• allergic reactions, hypersensitivity to acetylsalicylic acid;
• recurrent nasal polyposis;
• severe kidney damage;
• peptic ulcers of the gastrointestinal tract;
• bronchial asthma;
• period of pregnancy, as well as lactation (at any stage);
• older people take the drug with caution.

Meloxicam suppositories are not allowed to be used in the presence of diseases of the rectum, anal region, if they are chronic. Other contraindications are possible, so be sure to consult a doctor before starting use.

In some cases, side effects are observed:

• exacerbation of stomach and intestinal ulcers;
• vomiting, nausea;
• belching;
• bloating;
• constipation;
• diarrhea syndrome;
• headaches;
• dizziness;
• drowsy state;
• leukopenia;
• anemia;
• increased blood pressure;
• skin rashes, itching, other forms of allergies;
• swelling;
• high urea level;
• blood rush to the chest, face, neck.

Special instructions for the use of Meloxicam-ratiopharm

Given the risks associated with the use of meloxicam, the duration of its use should be as short as possible, and the daily dose should be the minimum effective. Before starting treatment with meloxicam, it is necessary to undergo a course of treatment for esophagitis, gastritis, peptic ulcers of the stomach and duodenum (such patients may have a history of relapses during treatment with meloxicam). In patients with a history of gastrointestinal pathology, it is necessary to assess the condition of the digestive tract in order to detect gastrointestinal bleeding. As with the use of other NSAIDs, asymptomatic gastrointestinal bleeding or perforation, sometimes resulting in death, has been reported during treatment with meloxicam. In elderly people, gastrointestinal bleeding or gastrointestinal perforation is more severe. In such cases, treatment with meloxicam is discontinued. Severe life-threatening allergic reactions (such as anaphylactic reactions) may occur when using NSAIDs, including meloxicam. In this case, the use of meloxicam should be stopped immediately and appropriate treatment should be carried out. In isolated cases, NSAIDs can cause interstitial nephritis, glomerulonephritis, necrosis of the hepatic papillae, or nephrotic syndrome. A transient increase in liver function tests is noted. In most cases, these disorders are temporary. In case of persistent violation of these indicators, the use of meloxicam should be discontinued. By causing potassium, sodium and water retention, as well as interacting with diuretics, NSAIDs can worsen the condition of patients with heart failure or hypertension (arterial hypertension). The use of NSAIDs may cause decompensation of latent renal failure. Kidney function returns to normal after discontinuation of therapy. Use with caution in the elderly, with heart failure, liver cirrhosis or renal failure, as well as in patients using diuretics. When treating such patients, it is necessary to monitor diuresis and renal function. The effect of treatment should be regularly monitored, assessing the need for its continuation. Like other drugs that inhibit COX or prostaglandin synthesis, meloxicam may mask the symptoms of infectious diseases (such as fever). In some cases, the drug has a negative effect on reproductive function, so it is not recommended for women planning pregnancy. The tablets contain lactose, so the drug should not be prescribed to patients with hereditary lactose deficiency, galactosemia or glucose/galactose malabsorption syndrome. There is no data on the negative effect of meloxicam on the ability to drive vehicles or operate machinery. If there are disorders of the central nervous system (decreased visual acuity, increased fatigue, dizziness or other disorders), these types of activities are contraindicated.

Indications and contraindications for use

Meloxicam tablets, suppositories and injections are used in the presence of the following diseases:

• rheumatoid type arthritis;
• inflammation, joint degeneration with severe pain;
• Bekhterev's disease;
• osteoarthritis.

Tablets should not be taken if you have the following pathologies:

• intolerance to aspirin, pyrazolone-based drugs;
• bronchial asthma;
• nasal polyposis (at the recurrent stage);
• severe kidney disease;
• pregnancy of any stage;
• GW period;
• peptic ulcers of the digestive organs;
• individual characteristics of the body (intolerance to non-steroidal drugs).

Suppositories should not be used in the presence of hemorrhoids, inflammation, or rectal wounds. Elderly people take all forms of the drug with caution. Before starting a course of treatment, you should consult your doctor.

Drug interactions Meloxicam-ratiopharm

Pharmacodynamics: Concomitant use of several NSAIDs (including salicylates) may increase the risk of developing erosive and ulcerative lesions of the gastrointestinal tract due to a synergistic effect, therefore the use of meloxicam with other NSAIDs is not recommended. When using meloxicam with diuretics, the patient must drink sufficient fluids, and regular medical monitoring of renal function is required before and during treatment. Oral anticoagulants: combined use increases the risk of bleeding due to inhibition of platelet function and damage to the mucous membrane of the stomach and intestines. Therefore, combined use with NSAIDs and oral anticoagulants is not recommended. Thrombolytic and antithrombotic drugs: when used in combination with meloxicam, an increased risk of bleeding is possible (periodic monitoring of blood coagulation parameters is necessary). ACE inhibitors and other antihypertensive drugs: simultaneous use in elderly patients with symptoms of dehydration may provoke the development of acute renal failure. In addition, combined use with meloxicam may reduce their hypotensive effect. Cyclosporine: the nephrotoxic effect of cyclosporine is enhanced. Contraception: The effectiveness of birth control may be reduced. Pharmacokinetic Lithium: NSAIDs may increase serum lithium concentrations to toxic levels (decreased renal excretion of lithium). Therefore, the simultaneous use of NSAIDs with lithium preparations is not recommended. If their combined use is necessary, the level of lithium in the blood serum should be carefully monitored before, during and after the end of the course of therapy with meloxicam and lithium preparations. Methotrexate: increases the negative effect on the blood system (threat of anemia and leukopenia). Periodic monitoring of the hemogram is necessary. Cholestyramine accelerates the elimination of meloxicam, increasing the clearance of meloxicam by 50%, reducing its half-life by 13±3 hours. This interaction is of clinical significance. When taken simultaneously with antacids, cimetidine and digoxin, no significant clinical interaction is observed. NSAIDs reduce the effectiveness of contraceptive intrauterine devices.

Meloxicam STADA (tablets)

Meloxicam is intended for symptomatic therapy and should not be taken to prevent exacerbation of diseases.

Caution should be exercised when treating patients with a history of gastrointestinal diseases and in patients receiving anticoagulants. Patients experiencing gastrointestinal symptoms should be monitored regularly. Periodic monitoring of blood clotting parameters is necessary. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, meloxicam should be discontinued.

If allergic reactions (itching, urticaria, skin rash, photosensitivity) occur during treatment, you should consult a doctor to decide whether to stop taking the drug.

The use of NSAIDs in patients with reduced renal blood flow or reduced circulating blood volume may lead to decompensation of latent renal failure. After discontinuation of NSAIDs, renal function usually returns to baseline levels. Elderly patients are most at risk of developing this reaction; patients who experience dehydration; patients with congestive heart failure, liver cirrhosis, nephrotic syndrome or kidney disease; patients receiving diuretics, ACE inhibitors, angiotensin II receptor antagonists; as well as patients who have undergone major surgical procedures leading to hypovolemia. In such patients, diuresis and renal function should be carefully monitored when initiating therapy.

The increase in transaminase activity is usually transient and insignificant. If there is a significant and persistent increase in transaminase activity, meloxicam should be discontinued and liver function monitored.

Weakened or malnourished patients may be less able to tolerate adverse events and such patients should be monitored closely. Caution should be used when treating elderly patients who are more likely to have impaired renal, hepatic and cardiac function.

The use of NSAIDs in combination with diuretics can lead to sodium, potassium and water retention, and affect the natriuretic effect of diuretics. As a result, predisposed patients may experience increased signs of heart failure or hypertension.

Meloxicam, like other NSAIDs, can mask the symptoms of an infectious disease.

The use of meloxicam, like other drugs that block prostaglandin synthesis, can affect fertility, so the drug is not recommended for women wishing to become pregnant.

Meloxicam-ratiopharm overdose, symptoms and treatment

Symptoms of acute NSAID overdose are often accompanied by drowsiness, nausea, vomiting and gastralgia, which usually resolve with symptomatic therapy. Gastrointestinal bleeding may also occur. Severe poisoning can lead to increased blood pressure, acute renal failure, liver dysfunction, respiratory depression, coma, convulsions, collapse and cardiac arrest. Anaphylactoid reactions have been reported during therapeutic doses of NSAIDs in cases of overdose. After an overdose of NSAIDs, patients are given supportive and symptomatic therapy in accordance with the severity of the overdose and intoxication. Clinical studies have found that three doses of 4 g of cholestyramine orally accelerates the elimination of meloxicam.