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

Active ingredient

Composition

How to take, the dosage

The drug is given by deep intramuscular injection.

The drug should not be given intravenously.

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

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

Ankylosing spondylitis: 15 mg daily.

Depending on the therapeutic effect, this dose may be reduced to 7.5 mg daily.

In patients with an increased risk of adverse reactions (history of GI disease, presence of cardiovascular risk factors), it is recommended to start treatment with a dose of 7.5 mg daily.

In patients with significant renal impairment who are on hemodialysis, the dose should not exceed 7.5 mg daily.

General recommendations

Because 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

The drug should not be used concomitantly with other NSAIDs.

The total daily dose of the drug used in different dosage forms should not exceed 15 mg. Intramuscular administration of the drug is indicated only during the first few days of therapy. Thereafter, treatment continues 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.

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

Interaction

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

– Anticoagulants for oral administration, heparin for systemic use, thrombolytics – concomitant use with meloxicam increases the risk of bleeding. In case of concomitant use it is necessary to monitor closely the blood clotting system.

– Antiplatelet drugs, serotonin reuptake inhibitors – concomitant use with meloxicam increases the risk of bleeding due to inhibition of platelet function. In case of concomitant use, close monitoring of the clotting system is necessary.

Lithium drugs – NSAIDs increase plasma levels of lithium by reducing its excretion by the kidneys. Concomitant use of meloxicam with lithium drugs is not recommended. If concomitant use is necessary, it is recommended that the concentration of lithium in plasma be closely monitored throughout the course of the use of lithium drugs.

– Contraception – There is evidence that NSAIDs may decrease the effectiveness of intrauterine contraceptive devices, but this has not been proven.

Diuretics – The use of NSAIDs in patients who are dehydrated is accompanied by a risk of acute renal failure.

– Antihypertensives (beta-adrenoblockers, angiotensin-converting enzyme inhibitors, vasodilators, diuretics). NSAIDs reduce the effect of antihypertensive drugs, due to inhibition of prostaglandins that have vasodilatory properties.

– Angiotensin II receptor antagonists, as well as angiotensin converting enzyme inhibitors, when combined with NSAIDs, increase decrease glomerular filtration, which thus may lead to acute renal failure, especially in patients with impaired renal function.

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

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

When co-administered with oral antidiabetic agents (e.g., sulfonylurea derivatives, nateglinide), CYP2C9-mediated interactions are possible, which may lead to increased blood concentrations of both these drugs and meloxicam.

No significant pharmacokinetic interactions have been found with concomitant use of antacids, cimetidine, digoxin and furosemide.

Special Instructions

Patients with gastrointestinal diseases should be monitored regularly. If gastrointestinal ulceration or gastrointestinal bleeding occurs, the drug should be discontinued.

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

Serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis may develop when using the drug. Therefore, special attention should be paid to patients who report adverse reactions of 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, mucous membrane changes or other signs of hypersensitivity occur, discontinuation of the drug should be considered.

There are cases of increased risk of serious cardiovascular thrombosis, myocardial infarction, angina attack, possibly with fatal outcome, when taking NSAIDs. This risk increases with long-term use of the drug, as well as in patients with the above-mentioned diseases in the history and predisposition to such diseases.

NSAIDs inhibit the renal synthesis of prostaglandins, which are involved in maintaining renal perfusion. Use of NSAIDs in patients with decreased renal blood flow or reduced circulating blood volume may lead to decompensation of latent renal insufficiency. After discontinuation of NSAIDs, renal function usually returns to baseline.

. The elderly patients, patients with dehydration, congestive heart failure, cirrhosis of the liver, nephrotic syndrome, or acute renal dysfunction, patients taking diuretics, angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, and patients who have undergone serious surgical procedures that lead to hypovolemia are at highest risk for 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 may lead to retention of sodium, potassium and water, and also to decrease the natriuretic action of diuretics. As a result, in predisposed patients, signs of heart failure or hypertension may increase. Therefore, close monitoring of such patients is necessary, and they should be kept adequately hydrated. Prior to the beginning of treatment renal function investigation is necessary.

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

When using meloxicam (as well as most other NSAIDs) there may be occasional increases in serum transaminase activity or other indicators of liver function. In most cases, these increases were small and transient. If the changes detected are significant or do not diminish over time, the drug should be discontinued and the laboratory changes detected should be monitored.

Weakened or debilitated patients may have a worse tolerance to adverse events, so these patients should be closely monitored.

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, so it is not recommended for women who have difficulty conceiving.

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

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

We should be careful during treatment because of possible cardiovascular and nervous system side effects when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and rapid psychomotor reactions.

Contraindications

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

– Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and sinuses, angioedema or urticaria caused by intolerance to acetylsalicylic acid or other NSAIDs due to the existing possibility of cross-sensitivity (including a history).

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

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

– Severe liver and heart failure.

– Severe renal failure (unless hemodialysis, creatinine clearance less than 30 ml/min), advanced renal disease, including confirmed hyperkalemia.

– Active liver disease.

– Active gastrointestinal bleeding, recent cerebrovascular bleeding or established diagnosis of blood clotting disorders.

– Age under 18 years of age.

– Therapy of perioperative pain during coronary artery bypass grafting.

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

– Pregnancy.

– Breastfeeding period.

– Diseases of the gastrointestinal tract (GIT) in the history (presence of Helicobacter pylori infection).

– Congestive heart failure.

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

– Coronary heart disease.

– Cerebrovascular disease.

– Dyslipidemia/hyperlipidemia.

– Diabetes mellitus.

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

– Peripheral arterial disease.

– Older age.

– Prolonged use of NSAIDs.

– Smoking.

– Frequent use of alcohol.

Side effects

The following are the side effects that have been considered possible due to the use of the drug. Side effects reported in post-marketing use that were considered to have a possible association with the use of the drug are marked with a *.

The following categories are used within the system-organ classes for frequency of adverse effects: very common (≥ 1/10), common (≥ 1/100, < 1/10), infrequent (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (< 1/10000), not established.

Blood and lymphatic system disorders

Infrequent – anemia;

rarely – leukopenia, thrombocytopenia, changes in blood cell count, including changes in the leukocytic formula.

Immune system disorders

Infrequent – other immediate-type hypersensitivity reactions*;

not established – anaphylactic shock*, anaphylactoid reactions*.

Mental disorders

Rarely – change in mood*;

not established – confusion*, disorientation*.

Nervous system disorders

Often – headache;

infrequently – dizziness, somnolence.

Sight, hearing, and labyrinth disorders

Infrequent – vertigo;

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

Cardiovascular disorders

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

Rarely – feeling of palpitations.

Respiratory system disorders

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

Gastrointestinal disorders

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

Infrequent – hidden and overt gastrointestinal bleeding, gastritis*, stomatitis, constipation, abdominal bloating, belching;

Rarely – gastroduodenal ulcers, colitis, esophagitis;

very rarely – gastrointestinal perforation.

Hepatic and biliary tract disorders

Infrequent – transient changes in liver function parameters (e.g., increased transaminase or bilirubin activity);

very rare – hepatitis*.

Skin and subcutaneous tissue disorders

Infrequent – angioedema*, itching, skin rash;

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

very rarely – bullous dermatitis*, erythema multiforme*;

not established – photosensitization.

Renal and urinary tract disorders

Infrequent – changes in renal function parameters (increased serum creatinine and/or urea levels), urinary disorders, including acute urinary retention*;

very rare – acute renal failure*.

Gender and mammary gland disorders

Infrequent – late ovulation*;

not established – infertility in women*.

General disorders and disorders at the site of administration

Often – pain and swelling at the site of administration;

not infrequently – edema.

Co-administration with drugs that depress bone marrow (e.g., methotrexate) may provoke cytopenia.

Gastrointestinal bleeding, ulceration or perforation may be fatal.

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

Overdose

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

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

Pregnancy use

The drug is contraindicated in pregnancy.

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

The use of meloxicam is not recommended in women who are planning to become pregnant, or in women participating in infertility or birth control studies. 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 unclear.

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 susceptibility to bleeding in mother and child and increased risk of edema in mother.

Similarities