Amelotex solution for injection 10mg / ml, 1.5ml No. 3

• Rheumatoid arthritis;

• osteoarthritis;

• ankylosing spondylitis (ankylosing spondylitis);

• inflammatory and degenerative diseases of the joints, accompanied by pain.

V / m, deep - 7.5-15 mg / day. With a slight or moderate decrease in renal function (Cl creatinine> 25 ml / min), as well as with liver cirrhosis in a stable clinical state, dose adjustment is not required. The initial dose in patients with an increased risk of side effects is 7.5 mg / day.

The maximum daily dose is 15 mg, in patients with severe renal failure on hemodialysis, 7.5 mg.

Solution for intramuscular injection

1 amp. (1.5 ml)

active substance: meloxicam 15 mg

excipients: meglumine; glycofurfural; poloxamer 188; sodium chloride; glycerol; sodium hydroxide solution 1 M; water for injections

• Hypersensitivity to the active substance or auxiliary components;

• period after coronary artery bypass grafting;

• uncompensated heart failure;

• anamnestic data about an attack of bronchial obstruction, rhinitis;

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including history);

• erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;

• inflammatory bowel disease (ulcerative colitis, Crohn's disease);

• cerebrovascular or other bleeding;

• severe liver failure or liver disease in the active phase;

• severe renal failure in patients not undergoing dialysis (Cl creatinine <30 ml / min), progressive kidney disease, incl. confirmed hyperkalemia;

• pregnancy;

• breastfeeding period;

• age up to 15 years.

With caution: to reduce the risk of developing adverse events, the minimum effective dose should be used, as short as possible, for coronary artery disease, cerebrovascular diseases, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, Cl creatinine <60 ml / min, anamnestic data on gastrointestinal ulcers, the presence of Helicobacter pylori infection, in old age, with prolonged use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (for example warfarin), antiplatelet agents (for example acetylsalicylic acid), clopidogrel , oral corticosteroids (eg prednisolone), SSRIs (eg citalopram, fluoxetine, paroxetine, sertraline).

pharmachologic effect

NSAIDs. It has analgesic, anti-inflammatory and antipyretic effects. The anti-inflammatory effect is associated with inhibition of the enzymatic activity of COX-2, which is involved in the biosynthesis of prostaglandins in the area of ??inflammation. To a lesser extent, meloxicam acts on COX-1, which is involved in the synthesis of prostaglandin, which protects the gastrointestinal mucosa and takes part in the regulation of blood flow in the kidneys. Suppresses the synthesis of prostaglandins in the area of ??inflammation to a greater extent than in the mucous membrane of the stomach or kidneys, which is associated with a relatively selective inhibition of COX-2. Belongs to the class of oxicams, a derivative of enolic acid. Meloxicam is a 'chondroneutral' drug, does not have a negative effect on cartilage tissue, does not affect proteoglycan synthesis by articular cartilage chondrocytes.

Side effect

From the digestive system: often - dyspepsia, incl. nausea, vomiting, abdominal pain, constipation, flatulence, diarrhea; infrequently - a transient increase in the activity of hepatic transaminases, hyperbilirubinemia, belching, esophagitis, stomach and duodenal ulcers, bleeding from the gastrointestinal tract (including latent), stomatitis; rarely - perforation of the gastrointestinal tract, colitis, hepatitis, gastritis.

From the hematopoietic system: often - anemia; infrequently - a change in the blood count, incl. leukopenia, thrombocytopenia.

From the side of the skin: often - itching, skin rash; rarely - photosensitivity, bullous eruptions, erythema multiforme, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis. When applying the gel for external use, hyperemia, papular-vesicular rashes, peeling are possible.

From the respiratory system: rarely - bronchospasm.

From the side of the nervous system: often - dizziness, headache; infrequently - vertigo, tinnitus, drowsiness; rarely - confusion, disorientation, emotional lability.

From the side of the cardiovascular system: often - peripheral edema; infrequently - increased blood pressure, palpitations, flushes of blood to the skin of the face.

From the urinary system: infrequently - hypercreatininemia and / or increased serum urea concentration; rarely - acute renal failure; the connection with the intake of the drug AmelotexЃ has not been established - interstitial nephritis, albuminuria, hematuria.

From the senses: rarely - conjunctivitis, visual impairment, incl. blurred visual perception. Allergic reactions: infrequently - urticaria; rarely - angioedema, anaphylactoid / anaphylactic reactions. Local reactions: with rectal application - there may be a urge to defecate and a feeling of discomfort, which go away on their own and do not require discontinuation of the drug; itching, burning in the perianal region, irritation of the rectal mucosa; with intramuscular injection - burning and pain at the injection site are possible.

In the event of adverse reactions, incl. not mentioned above, the patient should stop using the drug and consult a doctor.

Application during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding). Suppression of prostaglandin synthesis can have undesirable effects on pregnancy and fetal development. It is known that NSAIDs penetrate into breast milk, therefore, AmelotexЃ is not recommended for use during breastfeeding. The use of meloxicam, like other drugs that block the synthesis of prostaglandins, can affect fertility, so it is not recommended for women planning a pregnancy.

Application for violations of liver function

The use of the drug is contraindicated in severe liver failure or active liver disease.

Application for impaired renal function

The use of the drug is contraindicated in severe renal failure in patients not undergoing dialysis (CC <30 ml / min); progressive kidney disease, incl. with confirmed hyperkalemia. The drug should be prescribed with caution if the CC is <60 ml / min. In patients with renal insufficiency, if CC> 30 ml / min, correction of the dosage regimen is required. In patients with severe renal failure on hemodialysis, the dose should not exceed 7.5 mg / day.

Application in children

The use of the drug in children under 15 years of age is contraindicated.

Use in elderly patients

The drug should be used with caution in elderly patients.

special instructions

As with other NSAIDs, potentially life-threatening gastrointestinal bleeding, ulcers and perforations can occur during treatment at any time, whether there is a history of alarming symptoms or a history of serious gastrointestinal complications or absence of these signs. The consequences of these complications are generally more serious in elderly patients. Care should be taken when using the drug AmelotexЃ (as well as when using other NSAIDs) in patients with a history of gastrointestinal tract diseases, elderly patients, as well as in patients on anticoagulant therapy. In such patients, the risk of erosive and ulcerative diseases of the gastrointestinal tract is increased. In this case, as well as for the treatment of patients,requiring a low dose of acetylsalicylic acid or other drugs that increase gastrointestinal risk, combination therapy with protective drugs (such as misoprostol or proton pump inhibitors) should be considered. In the event of ulcerative lesions of the gastrointestinal tract or gastrointestinal bleeding, treatment with AmelotexЃ should be discontinued.

Particular attention should be paid to patients reporting the development of adverse events from the skin and mucous membranes (itching, skin rash, urticaria, photosensitivity). In such cases, the question of discontinuing the use of AmelotexЃ should be considered. NSAIDs inhibit the synthesis of prostaglandins in the kidney, which are involved in maintaining renal perfusion. The use of NSAIDs in patients with reduced renal blood flow or reduced BCC can lead to decompensation of latent renal failure. Renal function is usually restored after NSAID discontinuation.

Elderly patients are most at risk of developing this reaction; patients with dehydration, chronic 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 interventions leading to hypovolemia. In such patients, diuresis and renal function should be carefully monitored at the beginning of therapy.

In patients with renal insufficiency, if CC> 30 ml / min, no dosage adjustment is required. In patients with end-stage renal failure on hemodialysis, the dose of AmelotexЃ should not exceed 7.5 mg / day. With a persistent and significant increase in the activity of hepatic transaminases and changes in other indicators of liver function, the drug should be canceled and the identified laboratory changes should be monitored. In patients with cirrhosis of the liver in the stage of compensation, a reduction in the dose of the drug is not required. Patients taking diuretics and AmelotexЃ at the same time should take a sufficient amount of fluids. AmelotexЃ, like other NSAIDs, can mask the symptoms of infectious diseases.

Influence on the ability to drive vehicles and mechanisms

The use of the drug can cause undesirable effects in the form of headaches and dizziness, drowsiness. You should refuse to drive vehicles and maintain machines and mechanisms that require concentration.

Overdose

Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, gastrointestinal bleeding, acute renal failure, liver failure, respiratory arrest, asystole.

Treatment: there is no specific antidote; shown gastric lavage, the use of activated carbon (within the next hour), symptomatic therapy. Cholestyramine accelerates the elimination of the drug from the body. Forced diuresis and hemodialysis are ineffective due to the high degree of binding of the drug to blood proteins.

Drug interactions

With simultaneous use with other NSAIDs (as well as with acetylsalicylic acid), the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. With simultaneous use with antihypertensive drugs (for example, beta-blockers, ACE inhibitors, vasodilators, diuretics), the effectiveness of the latter may decrease due to inhibition of the synthesis of prostaglandins with vasodilating properties. The combined use of NSAIDs and angiotensin II receptor antagonists (as well as ACE inhibitors) enhances the effect of reducing glomerular filtration. In patients with impaired renal function, this can lead to the development of acute renal failure.With simultaneous use with lithium preparations, the accumulation of lithium is possible due to a decrease in renal excretion and an increase in its toxic effect (it is recommended to control the concentration of lithium in the blood plasma if such a combination therapy is necessary). With simultaneous use with methotrexate, NSAIDs can reduce the tubular secretion of methotrexate and, thus, increase the concentration of methotrexate in plasma, increasing its side effect on the hematopoietic system (the risk of anemia and leukopenia, periodic monitoring of a complete blood count is shown). In this regard, in patients receiving methotrexate in high doses (more than 15 mg per week), the simultaneous use of NSAIDs is not recommended. The risk of interaction with the simultaneous use of methotrexate and NSAIDs is also possible in patients receiving low doses of methotrexate,especially in patients with impaired renal function. If necessary, combination therapy should monitor the blood count and renal function. Care must be taken if NSAIDs and methotrexate are used concurrently for 3 days. the concentration of methotrexate in plasma may increase and, as a consequence, toxic effects may occur. The simultaneous use of the drug AmelotexЃ did not affect the pharmacokinetics of methotrexate at a dose of 15 mg per week, however, it should be taken into account that the hematological toxicity of methotrexate increases with the simultaneous administration of NSAIDs. With simultaneous use with diuretics and cyclosporine, the risk of developing acute honorary failure increases. In patients receiving AmelotexЃ and diuretics, it is necessary to maintain adequate hydration of the body.Before starting treatment, a study of renal function is necessary. NSAIDs, acting on renal prostaglandins, can increase the nephrotoxicity of cyclosporine. In the case of combination therapy, renal function should be monitored. With simultaneous use with intrauterine contraceptives, it is possible to reduce the effectiveness of the latter. With simultaneous use with anticoagulants (heparin, ticlopidine, warfarin) as well as with thrombolytic drugs (streptokinase, fibrinolysin), the risk of bleeding increases (periodic monitoring of blood clotting parameters is required). With simultaneous use with cholestyramine, as a result of binding of the drug AmelotexЃ, its excretion through the gastrointestinal tract is enhanced.With simultaneous use with selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases. The possibility of interaction with hypoglycemic drugs for oral administration cannot be ruled out.