Meloxicam-Acrichine pills 7.5mg, 20pcs

Composition

1 tablet (7.5 mg) contains:

Active ingredient:

meloxicam – 7.50 mg.

Auxiliary substances:

lactose monohydrate-182.65 mg,

microcrystalline cellulose-37.50 mg,

sodium citrate-11.10 mg,

crospovidone-7.50 mg,

colloidal silicon dioxide-2.50 mg,

magnesium stearate-1.25 mg

Pharmacological action

Pharmacotherapy group: NSAIDs:  

M. 01. A. C. 06 Meloxicam

M. 01. A. C Oxycams

Pharmacodynamics :

Meloxicam is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects.

The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2 (COX-2), which is involved in the biosynthesis of prostaglandins in the inflammatory region. To a lesser extent, meloxicam acts on cyclooxygenase-1 (COX-1), which is involved in the synthesis of prostaglandin, which protects the mucous membrane of the gastrointestinal tract (GIT) and is involved in the regulation of blood flow in the kidneys. Pharmacokinetics:

Absorption rate

It is well absorbed from the gastrointestinal tract, the absolute bioavailability of meloxicam is 89%. Simultaneous food intake does not change absorption. When using the drug inside in doses of 7.5 and 15 mg, its concentrations are proportional to the doses. Equilibrium concentrations are reached within 3-5 days. With prolonged use of the drug (more than 1 year), the concentrations are similar to those observed after the first achievement of a stable state of pharmacokinetics.

Distribution

Binding to plasma proteins is more than 99%. The range of differences between the maximum and basal concentrations of the drug after taking it once a day is relatively small and amounts to 0.4-1.0 mcg / ml when using a dose of 7.5 mg, and 0.8-2.0 mcg/ml when using a dose of 15 mg (the values are shown, respectively Cmin and Cmax).

Meloxicam penetrates through histohematic barriers, the concentration in synovial fluid reaches 50% of the maximum concentration of the drug in blood plasma.

Metabolism

Meloxicam is almost completely metabolized in the liver to form four pharmacologically inactive derivatives. The main metabolite,5’ – carboxymeloxicam (60% of the dose), is formed by oxidation of the intermediate metabolite,5’ – hydroxymethylmeloxicam (9% of the administered dose). In vitro studies have shown that the CYP2C9 isoenzyme plays an important role in this metabolic transformation, while the CYP3A4 isoenzyme plays an additional role. In the formation of the other two metabolites (which make up 16% and 4% of the drug dose, respectively), peroxidase takes part, the activity of which probably varies individually.

Deduction

It is excreted equally in the faeces and urine, mainly in the form of metabolites. With feces in unchanged form, less than 5% of the daily dose is excreted, in the urine in unchanged form, the drug is detected only in trace amounts.

The half-life (T 1/2) of meloxicam is 15-20 hours. The average plasma clearance is 8 ml/min.

In the elderly, the clearance of the drug decreases.

The volume of distribution is low and averages 11 liters.

Indications

Symptomatic treatment:

• osteoarthritis (osteoarthritis, degenerative joint diseases), including those with a painful component;
• rheumatoid arthritis;
• ankylosing spondylitis;
• other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathies, dorsopathies (for example, sciatica, lower back pain, shoulder periarthritis, etc. ), accompanied by pain.

Use during pregnancy and lactation

The use of Meloxicam-Akrikhin is contraindicated during pregnancy.

NSAIDs are known to pass into breast milk, so the use of Meloxicam-Acriquine during breast-feeding is contraindicated.

As a drug that inhibits cyclooxygenase/prostaglandin synthesis, Meloxicam-Acriquine may affect fertility and is therefore not recommended for women planning pregnancy. Meloxicam may delay ovulation. In this regard, in women who have problems with conception and are undergoing examination for such problems, it is recommended to cancel taking the drug Meloxicam-Akrikhin.

Contraindications

– hypersensitivity to the active ingredient or auxiliary components of the drug;

– complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs because of the probability of cross-sensitivity (including in the anamnesis);

– erosive-ulcerative lesions of the stomach and duodenum in the acute stage or recently transferred;

– inflammatory bowel disease – Crohn’s disease or ulcerative colitis in the acute stage;

– severe liver failure;

– severe renal insufficiency (if not possible, dialysis, creatinine clearance less than 30 ml/min, and when confirmed hyperkalemia), progressive kidney disease;

active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of diseases of the blood coagulation system;

– severe uncontrolled heart failure;

pregnancy;

breast – feeding;

– the treatment of perioperative pain in the conduct of bypass grafting of the coronary arteries;

– children’s age till 12 years;

– a rare hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution: A history of gastrointestinal diseases (gastric and duodenal ulcers, liver diseases); congestive heart failure; renal failure (creatinine clearance 30-60 ml/min); ischemic heart disease; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes mellitus; concomitant therapy with the following drugs: oral glucocorticosteroids, anticoagulants (including warfarin antiplatelet agents, selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); peripheral arterial diseases; the elderly; long-term use of NSAIDs; smoking; frequent alcohol consumption.

Side effects

Side effects that were considered to be associated with the use of the drug are described below.

Side effects reported with post-marketing use, the association of which with the drug intake was considered as possible, are marked with the * sign.

Within the organ-system classes, the following categories are used for the frequency of side effects: very common (≥ 1/10); common (≥ 1/100, < 1/10); infrequent (≥1/1000, < 1/100), rare (≥1/10000, < 1/1000), very rare (

From the blood and lymphatic system: infrequently-anemia; rarely-changes in the number of blood cells, including changes in the leukocyte formula, leukopenia, thrombocytopenia.

Immune system disorders: infrequently-other immediate hypersensitivity reactions*; frequency unknown – anaphylactic shock*, anaphylactoid reactions*.

From the nervous system: often-headache; infrequently-dizziness, drowsiness.

Mental disorders: often – mood swings*; frequency unknown-confusion*, disorientation*.

From the sensory organs: infrequently-vertigo; rarely-conjunctivitis*, visual disturbances, including blurred vision*, tinnitus.

From the gastrointestinal tract: often-abdominal pain, dyspepsia, diarrhea, nausea, vomiting; infrequently-latent or obvious gastrointestinal bleeding, gastritis*, stomatitis, constipation, bloating, belching; rarely-gastroduodenal ulcers, colitis, esophagitis; very rarely-perforation of the gastrointestinal tract.

From the liver: infrequently-transient changes in liver function indicators (for example, increased activity of transaminases or bilirubin); very rarely-hepatitis*. From the skin and subcutaneous tissues: infrequently-angioedema*, pruritus, skin rash; rarely-toxic epidermal necrolysis*, Stevens-Johnson syndrome*, urticaria; very rarely-bullous dermatitis*, erythema multiforme*; frequency unknown-photosensitization.

From the respiratory system: rarely-bronchial asthma in patients with allergies to acetylsalicylic acid or other NSAIDs.

From the cardiovascular system: infrequently-increased blood pressure, a feeling of “rush” of blood to the face; rarely-palpitations.

From the genitourinary system: infrequently-changes in renal function indicators (increased serum creatinine and/or urea), urinary disorders, including acute urinary retention*; very rarely – acute renal failure*.

From the genitals and breast: infrequently-late ovulation*, frequency unknown – infertility in women*.

Combined use with drugs that depress the bone marrow (for example, methotrexate) can provoke cytopenia.

Gastrointestinal bleeding, ulceration, or perforation can be fatal.

As with other NSAIDs, the possibility of interstitial nephritis, glomerulonephritis, renal medullary necrosis, and nephrotic syndrome is not excluded.

Interaction

Other prostaglandin synthesis inhibitors, including glucocorticoids and salicylates-concomitant use with meloxicam increases the risk of gastrointestinal ulceration and gastrointestinal bleeding (due to the synergistic effect).

Concomitant use with other NSAIDs is not recommended.

Anticoagulants for oral use, heparin for systemic use, thrombolytics-simultaneous use with meloxicam increases the risk of bleeding. In the case of simultaneous use, monitoring of the blood coagulation system is necessary.

Antiplatelet drugs, serotonin reuptake inhibitors-concomitant use with meloxicam increases the risk of bleeding due to inhibition of platelet function. In the case of simultaneous use, careful monitoring of the blood coagulation system is necessary.

Lithium preparations-NSAIDs increase the level of lithium in plasma by reducing its excretion by the kidneys. Concomitant use of meloxicam with lithium preparations is not recommended. If concomitant use is necessary, careful monitoring of the plasma lithium concentration is recommended throughout the course of lithium preparations.

Methotrexate-NSAIDs reduce the secretion of methotrexate by the kidneys, thereby increasing its concentration in plasma. Simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. In the case of simultaneous use, careful monitoring of renal function and blood formula is necessary. Meloxicam may increase the hematological toxicity of methotrexate, especially in patients with impaired renal function. With the combined use of meloxicam and methotrexate for 3 days, the risk of increased toxicity of the latter increases.

Contraception-there is evidence that NSAIDs may reduce the effectiveness of intrauterine contraceptive devices, but this has not been proven.

Diuretics-the use of NSAIDs in case of dehydration of patients is associated with the risk of acute renal failure.

Antihypertensive agents (beta-blockers, angiotensin-converting enzyme inhibitors, vasodilators, diuretics). NSAIDs reduce the effect of antihypertensive drugs, due to the inhibition of prostaglandins, which have vasodilating properties.

Angiotensin-II receptor antagonists, as well as angiotensin-converting enzyme inhibitors, when co-administered with NSAIDs, increase the decrease in glomerular filtration, which thereby can lead to the development of acute renal failure, especially in patients with impaired renal function.

Colestyramine binds meloxicam in the gastrointestinal tract, leading to its faster elimination.

NSAIDs acting on renal prostaglandins may increase the nephrotoxicity of cyclosporine.

Deferasirox-caution should be exercised when meloxicam and deferasirox are used simultaneously, as the risk of adverse reactions from the gastrointestinal tract may increase.

Pemetrexed-when meloxicam and pemetrexed are co-administered in patients with creatinine clearance from 45 to 79 ml/min, meloxicam should be discontinued five days before the start of pemetrexed and possibly resumed 2 days after the end of the drug. If the combined use of meloxicam and pemetrexed is necessary, patients should be carefully monitored, especially with regard to myelosuppression and the occurrence of gastrointestinal side effects. In patients with creatinine clearance less than 45 ml/min, meloxicam is not recommended in combination with pemetrexed.

When using medicinal products with meloxicam that have a known ability to inhibit CYP2C9 and/or CYP3A4 (or are metabolized with the participation of these enzymes), such as sulfonylureas or probenecid, the possibility of pharmacokinetic interaction should be taken into account.

When combined with antidiabetic agents for oral use (for example, sulfonylureas, nateglinide), interactions mediated by CYP2C9 are possible, which can lead to an increase in the concentration of both these drugs and meloxicam in the blood. Patients taking meloxicam concomitantly with sulfonylureas or nateglinide should carefully monitor their blood sugar levels due to the possibility of hypoglycemia.

No significant pharmacokinetic interactions were observed with concomitant use of antacids, cimetidine, digoxin, and furosemide.

How to take, course of use and dosage

Inside. The daily dose should be taken in one step, with a meal, with water or other liquid. The maximum recommended daily dose is 15 mg.

Since the potential risk of adverse reactions depends on the dose and duration of treatment, the lowest possible dose and duration of use should be used.

For osteoarthritis, the recommended dose is 7.5 mg per day. If necessary, this dose can be increased to 15 mg per day.

For rheumatoid arthritis, the recommended dose is 15 mg per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.

For ankylosing spondylitis, the recommended dose is 15 mg per day. Depending on the therapeutic effect, the dose can be reduced to 7.5 mg per day.

In patients with an increased risk of adverse reactions (diseases of the gastrointestinal tract in the anamnesis, the presence of risk factors for cardiovascular diseases), it is recommended to start treatment with a dose of 7.5 mg per day (see “Special Instructions”).

In patients with severe renal insufficiency who are on hemodialysis, the dose should not exceed 7.5 mg per day.

Do not use the drug simultaneously with other NSAIDs. The total daily dose of meloxicam used in different dosage forms should not exceed 15 mg.

Children over 12 years of age

Maximum daily dose in adolescents (12-18 years) it is 0.25 mg / kg and should not exceed 15 mg.

Overdose

Data on drug overdose cases are insufficient. Symptoms associated with an NSAID overdose are likely to be present in severe cases: drowsiness, impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, changes in blood pressure, respiratory arrest, asystole.

Treatment: the antidote is unknown, in case of overdose of the drug, gastric contents should be evacuated and general maintenance therapy should be performed. Colestyramine accelerates the elimination of meloxicam.

Description

Round tablets of light yellow color, with chamfers, on one side the surface is convex with an engraving of 7.5, on the other side it is concave with a deep risk.

Special instructions

Patients suffering from diseases of the gastrointestinal tract should be regularly monitored. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, the drug should be discontinued. Gastrointestinal ulcers, perforations, or bleeding may occur during treatment at any time, either if there are alarming symptoms or if there is a history of serious gastrointestinal complications, or if these signs are absent. The consequences of these complications are generally more serious in the elderly.

When using the drug, such serious skin reactions as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis may develop. Therefore, special attention should be paid to patients who report the development of adverse events from the skin and mucous membranes, as well as hypersensitivity reactions to the drug, especially if such reactions were observed during previous courses of treatment. The development of such reactions is usually observed during the first month of treatment. If the first signs of skin rash, changes in the mucous membranes or other signs of hypersensitivity appear, discontinuation of the drug should be considered.

When taking NSAIDs, cases of increased risk of developing serious cardiovascular thrombosis, myocardial infarction, and angina attack, possibly with a fatal outcome, have been described. This risk increases with prolonged use of the drug, as well as in patients with a history of the above diseases and predisposed to such diseases.

NSAIDs inhibit the synthesis of prostaglandins in the kidneys, which are involved in maintaining renal perfusion. 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 NSAID withdrawal, renal function usually returns to its original level. Elderly patients, patients with dehydration, congestive heart failure, cirrhosis of the liver, nephrotic syndrome or acute renal function disorders, patients who are simultaneously taking diuretics, ACE inhibitors, angiotensin II receptor antagonists, and patients who have undergone major surgical interventions that lead to hypovolemia are most at risk of developing this reaction. In such patients, diuresis and renal function should be carefully monitored at the beginning of therapy.

The use of NSAIDs together with diuretics can lead to sodium, potassium and water retention, as well as to a decrease in the natriuretic effect of diuretics. As a result, predisposed patients may have increased signs of heart failure or arterial hypertension.Therefore, the condition of such patients should be carefully monitored and adequate hydration should be maintained.

Before starting treatment, a study of renal function is necessary. In the case of combination therapy, renal function should also be monitored.

When using the drug (as well as most other NSAIDs), an episodic increase in serum transaminase activity or other indicators of liver function may occur. In most cases, this increase was small and transient. If the detected changes are significant or do not decrease over time, the drug should be discontinued, and the detected laboratory changes should be monitored.

Debilitated or emaciated patients may not tolerate adverse events as well, and such patients should be carefully monitored.

Like other NSAIDs, Meloxicam-Acriquine can mask the symptoms of infectious diseases.

In patients with mild or moderate renal insufficiency (creatinine clearance greater than 25 ml/min), no dose adjustment is required.

In patients undergoing dialysis, the dosage of the drug should not exceed 7.5 mg / day.

In patients with cirrhosis of the liver (compensated), no dose adjustment is required.

The use of meloxicam, as well as other drugs that block the synthesis of prostaglandins, can affect fertility, so it is not recommended for women who want to become pregnant.

Influence on the ability to drive vehicles and mechanisms:

Special clinical studies of the effect of the drug on the ability to drive a car and mechanisms have not been conducted. However, when driving a car and working with mechanisms, you should take into account the possibility of developing dizziness, drowsiness, visual impairment or other disorders of the central nervous system. Patients should be careful when driving a car and operating mechanisms.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use the drug after the expiration date.

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

Tablets