Elox SOLOPHARM, 10 mg/ml 1.5 ml 5 pcs.

Meloxicam is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic effects. It belongs to the class of oxycams, derivatives of enolic acid. Anti-inflammatory effect is associated with inhibition of enzymatic activity of cyclooxygenase-2, which is involved in the biosynthesis of prostaglandins in the area of inflammation.

To a lesser extent meloxicam acts on cyclooxygenase-1, which is involved in the synthesis of prostaglandin, protecting the mucosa of the gastrointestinal tract and is involved in the regulation of blood flow in the kidneys.

Indications

Initial therapy and short-term symptomatic treatment for osteoarthritis (arthrosis, degenerative joint diseases), rheumatoid arthritis, ankylosing spondylitis, other inflammatory and degenerative diseases of the musculoskeletal system, such as arthropathy, dorsopathies (for example, sciatica, low back pain, shoulder periarthritis and others), accompanied by pain.

Pharmacological effect

Meloxicam is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic effects. Belongs to the class of oxicams, derivatives of enolic acid. The anti-inflammatory effect is associated with inhibition of the enzymatic activity of cyclooxygenase-2, which is involved in the biosynthesis of prostaglandins in the area of ​​inflammation.

To a lesser extent, meloxicam acts on cyclooxygenase-1, which is involved in the synthesis of prostaglandin, which protects the mucous membrane of the gastrointestinal tract and takes part in the regulation of blood flow in the kidneys.

Special instructions

Patients suffering from diseases of the gastrointestinal tract should be monitored regularly. If ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding occur, the drug must be discontinued.

Gastrointestinal ulcers, perforation, or bleeding may occur at any time during the use of NSAIDs, with or without warning symptoms or a history of serious gastrointestinal complications. The consequences of these complications are generally more serious in older people.

When using the drug, serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis may develop. Therefore, special attention should be paid to patients reporting 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 observed, as a rule, during the first month of treatment. If the first signs of skin rash, changes in mucous membranes or other signs of hypersensitivity appear, discontinuation of the drug should be considered.

Cases have been described when taking NSAIDs to increase the risk of developing serious cardiovascular thrombosis, myocardial infarction, angina, possibly fatal. This risk increases with long-term 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 discontinuation of NSAIDs, renal function usually returns to baseline levels.

Those most at risk for developing this reaction are elderly patients, patients with dehydration, congestive heart failure, liver cirrhosis, nephrotic syndrome or acute renal impairment, patients concomitantly taking diuretics, angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, and patients undergoing major surgery that leads to hypovolemia.

In such patients, diuresis and renal function should be carefully monitored when initiating therapy. The use of NSAIDs in combination with diuretics can lead to sodium, potassium and water retention, as well as a decrease in the natriuretic effect of diuretics. As a result, predisposed patients may experience increased signs of heart failure or hypertension. Therefore, such patients should be closely monitored and adequate hydration maintained. Before starting treatment, a kidney function test is necessary.

In case of combination therapy, renal function should also be monitored.

When using meloxicam (as well as most other NSAIDs), episodic increases in serum transaminase activity or other indicators of liver function are possible. In most cases, this increase was small and transitory. 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.

Weakened or malnourished patients may be less able to tolerate adverse events and should be monitored closely.

Like other NSAIDs, meloxicam may mask the symptoms of an underlying infectious disease.

The use of meloxicam, like other drugs that inhibit cyclooxygenase/prostaglandin synthesis, may affect fertility and is therefore not recommended for women who have difficulty conceiving.

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

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

Impact on the ability to drive vehicles. Wed and fur.:

During the treatment period, due to possible side effects from the cardiovascular and nervous system, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Meloxicam

Composition

1 ml of the drug contains:

Active ingredient:

Meloxicam – 10.0 mg

Excipients:

Tetrahydrofurfuryl macrogol (glycofurol) – 100.0 mg

Poloxamer 188 – 50.0 mg

Meglumine – 6.25 mg

Glycine – 5.0 mg

Sodium chloride – 3.0 mg

10 M sodium hydroxide solution to pH 8.2-8.9

Water for injection – up to 1.0 ml.

Pregnancy

The drug is contraindicated during pregnancy.

If it is necessary to prescribe the drug during breastfeeding, breastfeeding should be stopped.

The use of meloxicam is not recommended in women planning pregnancy or in women participating in infertility or birth control studies. The safety of this drug during pregnancy has not been proven. The effect of delayed prostaglandin synthesis on embryogenesis during the first two trimesters of pregnancy is unclear.

In the last trimester of pregnancy, the mechanism of action of meloxicam is characterized by inhibition of labor, premature closure of the Ductus arteriosus Botalli in the fetus, an increased susceptibility to bleeding in the mother and child, and an increased risk of edema in the mother.

Meloxicam passes into mother’s milk in small quantities, and in the case of breastfeeding, meloxicam can be detected in the infant’s blood plasma.

As a drug that inhibits cyclooxygenase/prostaglandin synthesis, meloxicam may have an effect on fertility and is therefore not recommended for women who have difficulty conceiving. In this regard, discontinuation of the drug is recommended for women undergoing examination for this reason.

Contraindications

– Hypersensitivity to the active ingredient and auxiliary components of the drug, to acetylsalicylic acid or other NSAIDs.

– 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 NSAIDs due to the existing likelihood of cross-sensitivity (including history).

– Erosive and ulcerative lesions of the stomach and duodenum in the acute stage or recently suffered.

– Inflammatory bowel diseases – Crohn’s disease or ulcerative colitis in the acute stage.

– Severe liver and heart failure.

– Severe renal failure (if hemodialysis is not performed, creatinine clearance less than 30 ml/min), progressive kidney disease, including confirmed hyperkalemia.

– Active liver disease.

– Active gastrointestinal bleeding, recent cerebrovascular bleeding, or an established diagnosis of diseases of the blood coagulation system.

– Age up to 18 years.

– Therapy of perioperative pain during coronary artery bypass surgery.

– Concomitant therapy with anticoagulants, as there is a risk of the formation of intramuscular hematomas.

– Pregnancy.

– Breastfeeding period.

With caution:

– History of gastrointestinal (GIT) diseases (presence of Helicobacter pylori infection).

– Congestive heart failure.

– Renal failure (creatinine clearance 30-60 ml/min).

– Coronary heart disease.

– Cerebrovascular diseases.

– Dyslipidemia/hyperlipidemia.

– Diabetes mellitus.

– Concomitant therapy with the following drugs: anticoagulants, oral glucocorticosteroids, antiplatelet agents, selective serotonin reuptake inhibitors.

– Diseases of peripheral arteries.

– Old age.

– Long-term use of NSAIDs.

– Smoking.

– Frequent drinking of alcohol.

Side Effects

Side effects that were considered possible to be associated with the use of the drug are described below. Side effects registered during post-marketing use, the connection with which the drug was considered possible, are marked with *.

Within systemic organ classes, the following categories are used according to the frequency of side effects: very often (≥ 1/10), often (≥ 1/100, < 1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, < 1/1000), very rarely (< 1/10000), not established.

Blood and lymphatic system disorders

Uncommon – anemia;

rarely – leukopenia, thrombocytopenia, changes in the number of blood cells, including changes in the leukocyte formula.

Immune system disorders

Uncommon – other immediate hypersensitivity reactions*;

not established – anaphylactic shock*, anaphylactoid reactions*.

Mental disorders

Rarely – mood changes*;

not established – confusion*, disorientation*.

Nervous system disorders

Often – headache;

infrequently – dizziness, drowsiness.

Visual, hearing and labyrinthine disorders

Uncommon: vertigo;

rarely – conjunctivitis*, visual impairment, including blurred vision*, tinnitus.

Disorders of the heart and blood vessels

Uncommon – increased blood pressure, a feeling of a “rush” of blood to the face;

rarely – a feeling of palpitations.

Respiratory system disorders

Rarely – bronchial asthma in patients with allergies to acetylsalicylic acid and other NSAIDs.

Gastrointestinal disorders

Often – abdominal pain, dyspepsia, diarrhea, nausea, vomiting;

uncommon – hidden and obvious gastrointestinal bleeding, gastritis*, stomatitis, constipation, bloating, belching;

rarely – gastroduodenal ulcers, colitis, esophagitis;

very rarely – perforation of the gastrointestinal tract.

Disorders of the liver and biliary tract

Uncommon: transient changes in liver function tests (for example, increased activity of transaminases or bilirubin);

very rarely – hepatitis*.

Skin and subcutaneous tissue disorders

Uncommon – angioedema*, itching, skin rash;

rarely – toxic epidermal necrolysis*, Stevens-Johnson syndrome*, urticaria;

very rarely – bullous dermatitis*, erythema multiforme*;

not established – photosensitivity.

Renal and urinary tract disorders

Uncommon: changes in renal function (increased creatinine and/or urea levels in the blood serum), urinary disorders, including acute urinary retention*;

very rarely – acute renal failure*.

Disorders of the genital organs and mammary glands

Uncommon – late ovulation*;

not established – infertility in women*.

General and administration site disorders

Often – pain and swelling at the injection site;

infrequently – swelling.

Concomitant use with drugs that suppress bone marrow (for example, methotrexate) may cause 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 cannot be excluded.

Interaction

– Other inhibitors of prostaglandin synthesis, including glucocorticoids and salicylates – concomitant use with meloxicam increases the risk of ulcers in the gastrointestinal tract and gastrointestinal bleeding (due to synergistic action). Concomitant use with other NSAIDs is not recommended.

– Anticoagulants for oral administration, heparin for systemic use, thrombolytic agents – simultaneous use with meloxicam increases the risk of bleeding. In case of simultaneous use, careful monitoring of the blood coagulation system is necessary.

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

– Lithium preparations – NSAIDs increase plasma lithium levels by reducing its excretion by the kidneys. The simultaneous use of meloxicam with lithium preparations is not recommended. If simultaneous use is necessary, careful monitoring of plasma lithium concentrations is recommended throughout the course of lithium use.

– Methotrexate – NSAIDs reduce the secretion of methotrexate by the kidneys, thereby increasing its plasma concentration. The simultaneous use of meloxicam and methotrexate (at a dose of more than 15 mg per week) is not recommended. In case of simultaneous use, careful monitoring of renal function and blood count is necessary. Meloxicam may increase the hematological toxicity of methotrexate, especially in patients with impaired renal function.

– 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 accompanied by the risk of developing acute renal failure.

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

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

– Cholestyramine, by binding meloxicam in the gastrointestinal tract, leads to its faster elimination.

– Pemetrexed – with the simultaneous use of meloxicam and pemetrexed in patients with a creatinine clearance of 45 to 79 ml/min, meloxicam should be discontinued 5 days before starting pemetrexed and can be resumed 2 days after the end of treatment. If concomitant use of meloxicam and pemetrexed is necessary, such patients should be closely monitored, especially with regard to myelosuppression and the occurrence of gastrointestinal side effects. In patients with creatinine clearance less than 45 ml/min, taking meloxicam with pemetrexed is not recommended.

NSAIDs, by acting on renal prostaglandins, may enhance the nephrotoxicity of cyclosporine.

When medicinal products known to inhibit CYP2C9 and/or CYP3A4 (or are metabolized by these enzymes), such as sulfonylureas or probenecid, are used with meloxicam, the potential for pharmacokinetic interaction should be taken into account.

When used concomitantly with oral antidiabetic agents (eg, sulfonylureas, nateglinide), interactions mediated by CYP2C9 are possible, which may lead to increased blood concentrations of both these drugs and meloxicam.

Patients taking meloxicam concomitantly with a sulfonylurea or nateglinide should carefully monitor their blood sugar levels due to the possibility of hypoglycemia.

With the simultaneous use of antacids, cimetidine, digoxin and furosemide, no significant pharmacokinetic interactions were identified.

Overdose

Symptoms: nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, respiratory arrest, asystole, lethargy, drowsiness, increased blood pressure, coma, convulsions, cardiovascular collapse, cardiac arrest, anaphylactoid reactions.

Treatment: there is no specific antidote. In case of drug overdose, carry out symptomatic therapy. Forced diuresis, alkalization of urine, hemodialysis are ineffective due to the high binding of the drug to blood proteins.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf life

5 years.

Do not use after the expiration date.

Manufacturer

Grotex LLC, Russia