Elox-Solopharm solution 10mg/ml 1.5ml ampoules, 5pcs

Composition

>1 ml of the drug contains: Active ingredient: Meloxicam – 10.0 mgsupport substances: Tetrahydrofurfuryl macrogol (glycofural) – 100.0 Mgpoloxamer 188-50.0 Mgmegluminum-6.25 Mgglycine – 5.0 mg Sodium chloride-3.0 mg 10 M sodium hydroxide solution up to pH 8.2-8.9 Water for injection – up to 1.0 ml

Pharmacological action

Meloxicam is a nonsteroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. It belongs to the class of oxycams derived from 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 inflammatory region. 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 is involved in the regulation of blood flow in the kidneys.

Indications

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

Use during pregnancy and lactation

The drug is contraindicated during pregnancy.

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

Meloxicam is not recommended for use in women who are planning pregnancy, as well as in women who are participating in infertility studies or birth control. The safety of using this drug during pregnancy has not been proven. The effect of delayed prostaglandin synthesis on embryogenesis during the first two trimesters of pregnancy is not clear.

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

Meloxicam passes into the mother’s milk in small amounts, and in the case of breast-feeding, meloxicam can be detected in the infant’s blood plasma. As a drug that inhibits cyclooxygenase/prostaglandin synthesis, meloxicam may affect fertility and is therefore not recommended for women who have difficulty conceiving. In this regard, in women undergoing examination for this reason, it is recommended to cancel the drug.

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 nasal and paranasal sinus polyposis, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs due to the existing probability of cross-sensitivity (including in the anamnesis).

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

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

– Severe liver and heart failure.

– Severe renal insufficiency (if no hemodialysis is performed, creatinine clearance is less than 30 ml / min), progressive kidney diseases, including confirmed hyperkalemia.

– Active liver disease.

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

– Under 18 years of age.

– Therapy of perioperative pain during coronary artery bypass grafting.

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

– Pregnancy.

– The period of breastfeeding.

With caution:

– A history of diseases of the gastrointestinal tract (GIT) (presence of Helicobacter pylori infection).

– Congestive heart failure.

– Renal insufficiency (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 the peripheral arteries.

– Advanced age.

– Long-term use of NSAIDs.

– Smoking.

– Frequent use of alcohol.

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 (

Disorders of the blood and lymphatic system

Infrequently-anemia;

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

Immune system disorders

Infrequently – other immediate hypersensitivity reactions*;

not established – anaphylactic shock*, anaphylactoid reactions*.

Mental disorders

Rarely – mood swings*;

not established-confusion*, disorientation*.

Nervous system disorders

Often – headache;

infrequently-dizziness, drowsiness.

Visual, hearing and labyrinth disorders

Infrequently-vertigo;

rarely-conjunctivitis*, visual disturbances, including blurred vision*, tinnitus.

Disorders of the heart and blood vessels

Infrequently-increased blood pressure, a feeling of “rush” of blood to the face;

rarely-a feeling of palpitation.

Respiratory system disorders

Rarely-bronchial asthma in patients allergic to acetylsalicylic acid and other NSAIDs.

Disorders of the gastrointestinal tract

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

infrequently – latent and obvious gastrointestinal bleeding, gastritis*, stomatitis, constipation, bloating, belching;

rarely-gastroduodenal ulcers, colitis, esophagitis;

very rarely – perforation of the gastrointestinal tract.

Liver and biliary tract disorders

Infrequently-transient changes in liver function indicators (for example, increased activity of transaminases or bilirubin);

very rarely-hepatitis*.

Skin and subcutaneous tissue disorders

Infrequently-angioedema*, pruritus, skin rash;

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

very rarely-bullous dermatitis*, erythema multiforme*;

not established – photosensitization.

Kidney and urinary tract disorders

Infrequently-changes in renal function indicators (increased serum creatinine and/or urea), urinary disorders, including acute urinary retention*;

very rarely – acute renal failure*.

Disorders of the genitals and mammary glands

Infrequently – late ovulation*;

not established-infertility in women*.

General disorders and disorders at the injection

site Often-pain and swelling at the injection site;

infrequently-edema.

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, 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 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.

– Contraception-there is evidence that NSAIDs can 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 combined 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. – Pemetrexed-when meloxicam and pemetrexed are used simultaneously in patients with creatinine clearance from 45 to 79 ml/min, meloxicam should be discontinued 5 days before the start of pemetrexed and may be resumed 2 days after the end of use. If there is a need for the combined use of meloxicam and pemetrexed, then such patients should be carefully monitored, especially with regard to myelosuppression and the occurrence of side effects from the gastrointestinal tract. In patients with creatinine clearance less than 45 ml/min, meloxicam is not recommended in combination with pemetrexed.

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

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

The drug is administered by deep intramuscular injection.

The drug should not be administered intravenously.

Osteoarthritis with pain syndrome: 7.5 mg per day. If necessary, this dose can be increased to 15 mg per day.

Rheumatoid arthritis: 15 mg per day. Depending on the therapeutic effect, this dose can be reduced to 7.5 mg per day.

Ankylosing spondylitis: 15 mg per day.

Depending on the therapeutic effect, this dose can be reduced to 7.5 mg per day.

In patients with an increased risk of adverse reactions (gastrointestinal diseases 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.

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

General recommendations

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.

The maximum recommended daily dose is 15 mg.

Combined use

Do not use the drug simultaneously with other NSAIDs.

The total daily dose of the drug used in different dosage forms should not exceed 15 mg. Intramuscular use of the drug is indicated only during the first few days of therapy. Further treatment is continued with the use of oral dosage forms. The recommended dose is 7.5 mg or 15 mg once a day, depending on the intensity of pain and the severity of the inflammatory process.

Due to possible incompatibilities, the drug should not be mixed in the same syringe with other medications.

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 overdose of the drug, conduct symptomatic therapy. Forced diuresis, urine alkalinization, and hemodialysis are ineffective due to the high binding of the drug to blood proteins.

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 the course of NSAID use at any time, whether there are alarming symptoms or a history of serious gastrointestinal complications, or in the absence of these signs. 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.

Cases of increased risk of serious cardiovascular thrombosis, myocardial infarction, angina attack, possibly fatal, are described when taking NSAIDs. 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, angiotensin converting enzyme 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 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 meloxicam (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 can mask the symptoms of an underlying infectious disease.

The use of meloxicam, as well as other drugs that inhibit cyclooxygenase/prostaglandin synthesis, can affect fertility, so it is not recommended for women who have difficulty conceiving.

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

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

Influence on the ability to drive vehicles and fur. :

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

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 5 years.

Do not use after the expiration date.

Active ingredient

Meloxicam

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection