Aertal tablets p / o 100mg, No. 60

Х Relief of inflammation and pain in lumbago, toothache, periarthritis, rheumatic lesions of soft tissues, for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis.
Х The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Inside. The tablets should be swallowed whole with plenty of water. AertalЃ can be taken with food.

Adverse events can be minimized by using the lowest effective dose and reducing the duration of treatment needed to control symptoms.

Adults

The recommended dose is 1 tablet 100 mg 2 times / day (morning and evening). The maximum recommended dose is 200 mg / day.

Special patient groups

Patients with hepatic impairment. The dose of aceclofenac should be reduced in patients with mild to moderate hepatic impairment. The recommended starting dose is 100 mg / day.

Patients with renal impairment. There is no evidence of the need to reduce the dose of aceclofenac in patients with mild renal impairment, but caution should be exercised when using AertalЃ.

Elderly patients (over 65 years old). As a rule, there is no need to reduce the dose, however, the precautions specified in the section 'Special instructions' should be observed.

Children under 18. The use of the drug AertalЃ in children is contraindicated due to the lack of data on efficacy and safety.

White film-coated tablets, round, biconvex; the letter 'A' is engraved on one side.

1 tab.

aceclofenac 100 mg

Excipients: microcrystalline cellulose pH 102, microcrystalline cellulose pH 101, povidone K-30, glyceryl distearate (type I), croscarmellose sodium.

• Hypersensitivity to aceclofenac and / or any of the excipients of the drug;

• bronchospasm, urticaria, rhinitis after taking acetylsalicylic acid or other NSAIDs in history (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, bronchial asthma);

• bleeding or perforation of the gastrointestinal tract associated with taking NSAIDs in history;

• peptic ulcer or duodenal ulcer, or a history of bleeding (two or more overt and proven episodes of ulcer or bleeding);

• ulcerative colitis and Crohn's disease (in the acute phase);

• period after coronary artery bypass grafting; acute bleeding or bleeding disorders or bleeding disorders (hemophilia);

• chronic heart failure (NYHA class II-IV), coronary artery disease, peripheral artery disease and / or cerebral artery disease;

• severe liver failure or active liver disease;

• severe renal failure (CC <30 ml / min);

• pregnancy;

• breastfeeding period;

• children under 18 years of age.

  Carefully

• Diseases of the liver, kidneys and gastrointestinal tract in history, bronchial asthma, arterial hypertension, decreased BCC (including immediately after major surgical interventions); chronic renal failure of mild and moderate severity (CC 60-30 ml / min); chronic hepatic failure of mild to moderate severity; chronic heart failure (NYHA class I); history of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, Crohn's disease (without exacerbation), ulcerative colitis (without exacerbation), symptoms indicating the presence of gastrointestinal diseases; SLE, porphyria, hematological diseases, hematopoietic disorders, dyslipidemia / hyperlipidemia, diabetes mellitus, severe somatic diseases; long-term use of NSAIDs; elderly age; smoking, alcoholism.

Pharmacological characteristics

Pharmacodynamics
Aceclofenac has anti-inflammatory, analgesic and antipyretic effects. It inhibits the synthesis of prostaglandins and, thus, affects the pathogenesis of inflammation, pain and fever. In rheumatic diseases, the anti-inflammatory and analgesic effect of aceclofenac contributes to a significant decrease in the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the patient.
Pharmacokinetics
Absorption
After oral administration, aceclofenac is rapidly absorbed, its bioavailability is close to 100%. The maximum concentration (Cmax) in blood plasma is reached 1.25-3 hours after ingestion. Food intake slows down absorption, but does not affect its degree.
Distribution
Aceclofenac is highly bound to plasma proteins (> 99.7%). Aceclofenac penetrates into the synovial fluid, where its concentration reaches 60% of its plasma concentration. The volume of distribution is 30 liters.
Metabolism.
It is believed that aceclofenac is metabolized by the CYP2C9 isoenzyme to form the 4-OH-aceclofenac metabolite, whose contribution to the clinical effect of the drug is likely to be minimal. Diclofenac and 4-OH-diclofenac are among the numerous metabolites of aceclofenac.
Withdrawal The
average elimination half-life (t1 / 2) is 4-4.3 hours. The ground clearance is 5 l / h. Approximately 2/3 of the dose taken is excreted by the kidneys, mainly in the form of conjugated hydroxymetabolites. Only 1% of the dose after oral administration is excreted unchanged.

Application during pregnancy and lactation

Pregnancy
AertalЃ, film-coated tablets, 100 mg is contraindicated in pregnancy. There is no information on the use of aceclofenac during pregnancy.
Inhibition of prostaglandin synthesis can adversely affect the course of pregnancy and / or the development of the embryo / fetus.
During the third trimester of pregnancy, all inhibitors of prostaglandin synthesis:
Х possessing cardiopulmonary toxicity, can cause premature closure of the Botallov duct with the development of pulmonary hypertension;
Х can cause impaired renal function of the fetus, which can progress to renal failure in combination with polyhydramnios.
Mothers and newborns in late pregnancy: the drug can affect the duration of bleeding due to the antiplatelet effect, which can develop even after very low doses;
Х the drug can suppress uterine contractions, leading to delayed labor or prolonged labor.
Lactation
AirtalЃ, film-coated tablets, 100 mg should not be taken during breastfeeding. There are no data on the allocation of aceclofenac in human milk; When radioactive 14C-aceclofenac was administered to lactating rats, no noticeable transfer of radioactivity into milk was observed.
Fertility
Non-steroidal anti-inflammatory drugs (NSAIDs) can interfere with fertility and are not recommended for women planning a pregnancy.

Side effect

Blood and lymphatic system disorders
Rare: anemia;
Very rare: bone marrow suppression, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia;
Immune system disorders
Rare: anaphylactic reactions including shock, hypersensitivity;
Nutrition and metabolic disorders
Very rare: hyperkalemia;
Mental disorders
Very rare: depression, unusual (atypical) dreams, insomnia;
Nervous system disorders
Often: dizziness;
Very rare: paresthesia, tremors, drowsiness, headache, dysgeusia (taste perversion);
Violations of the organ of vision
Rare: visual impairment;
Hearing and labyrinth disorders
Very rare: vertigo, tinnitus;
Cardiac disorders
Rare: heart failure;
Very rare: heart palpitations;
Vascular disorders
Rarely: increased blood pressure;
Very rare: flushing of the skin, 'hot flashes' (short-term feeling of heat, accompanied by sweating), vasculitis;
Disturbances from the respiratory system, chest and mediastinal organs
Rarely: shortness of breath;
Very rare: bronchospasm;
Disorders from the gastrointestinal tract
Often: dyspepsia, abdominal pain, nausea, diarrhea;
Uncommon: flatulence, gastritis, constipation, vomiting, ulceration of the oral mucosa;
Rarely: melena, ulceration of the mucous membrane of the gastrointestinal tract, hemorrhagic diarrhea, hemorrhages of the mucous membrane of the gastrointestinal tract;
Very rare: stomatitis, vomiting of blood, intestinal perforation, worsening of Crohn's disease and ulcerative colitis, pancreatitis;
Liver and biliary tract disorders
Often: increased activity of 'hepatic' enzymes;
Very rare: liver damage (including hepatitis), increased alkaline phosphatase activity;
Skin and subcutaneous tissue disorders
Uncommon: itching, rash, dermatitis, urticaria;
Rarely: angioedema;
Very rare: purpura, eczema, severe reactions from the skin and mucous membranes (including Stevens-Johnson syndrome and toxic epidermal necrolysis);
In some cases, serious skin and soft tissue infections have been observed when taking NSAIDs during chickenpox disease.
Renal and urinary tract disorders
Uncommon: increased serum urea and creatinine;
Very rare: nephrotic syndrome, renal failure, interstitial nephritis;
Systemic disorders and complications at the injection site
Very rarely: edema, fatigue, muscle spasms of the lower extremities;
Laboratory findings
Very rare: weight gain.
If the patient has noticed a worsening of any of the listed adverse events or the occurrence of an adverse event not specified in this instruction, he should contact the attending physician.

Overdose

There is no evidence of an overdose of aceclofenac in humans.
Possible symptoms: nausea, vomiting, pain in the stomach, dizziness, headache, hyperventilation phenomena with increased convulsive readiness.
Treatment: gastric lavage, the introduction of activated carbon, symptomatic therapy. Forced diuresis, hemodialysis is not effective enough.

Interaction with other medicinal products

With the exception of warfarin, drug interaction studies have not been conducted. Aceclofenac is metabolized by the CYP2C9 isoenzyme; in vitro data indicate that aceclofenac may be an inhibitor of this enzyme. Thus, the risk of pharmacokinetic interaction is possible when taken simultaneously with phenytoin, cimetidine, tolbutamide, phenylbutazone, amiodarone, miconazole and sulfaphenazole. As with other non-steroidal anti-inflammatory drugs, the risk of pharmacokinetic interaction with other drugs that are excreted from the body by active renal secretion, such as methotrexate and lithium drugs, increases. Aceclofenac almost completely binds to blood plasma albumin and, therefore, there is a possibility of displacement interactions with other drugs,binding to proteins.
The following is class-specific information for NSAIDs:
Methotrexate: NSAIDs inhibit the tubular secretion of methotrexate; moreover, there may be a slight metabolic interaction, which leads to a decrease in the clearance of methotrexate. Therefore, when using high doses of methotrexate, NSAIDs should be avoided.
Lithium and Digoxin: Some NSAIDs inhibit the renal clearance of lithium and digoxin, resulting in increased serum concentrations of both substances. Concomitant use should be avoided unless frequent monitoring of lithium and digoxin concentrations is performed.
Anticoagulants: NSAIDs inhibit platelet aggregation and damage the lining of the gastrointestinal tract, which can increase the effect of anticoagulants and increase the risk of gastrointestinal bleeding while taking anticoagulants. Avoid the combined use of aceclofenac and oral anticoagulants of the coumarin group, ticlopidine and thrombolytics, unless careful monitoring of the patient's condition is carried out.
Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs), when used together with NSAIDs, may increase the risk of gastrointestinal bleeding.
Cyclosporine, tacrolimus: When taking NSAIDs concomitantly with cyclosporine or tacrolimus, the risk of increased nephrotoxicity due to a decrease in renal prostacyclin formation should be considered. Therefore, when taken simultaneously, you should carefully monitor the indicators of renal function.
Other NSAIDs: While taking acetylsalicylic acid or other NSAIDs, the incidence of side effects may increase, so caution should be exercised.
Glucocorticosteroids: Increases the risk of ulcers or gastrointestinal bleeding.
Diuretics: Aceclofenac, like other NSAIDs, can inhibit the activity of diuretics, can reduce the diuretic effect of furosemide and bumetanide and the antihypertensive effect of thiazides. Co-administration with potassium-sparing diuretics can lead to an increase in serum potassium.
Aceclofenac did not affect blood pressure control when used together with bendrofluazide, although interactions with other diuretics cannot be ruled out.
Antihypertensive drugs: NSAIDs can also reduce the effect of antihypertensive drugs. Co-administration of angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists and NSAIDs can lead to impaired renal function. The risk of acute renal failure, which is usually reversible, may increase in some patients with impaired renal function, such as the elderly or dehydrated. Therefore, when used together with NSAIDs, caution should be exercised. Patients should consume the required amount of fluid and be under appropriate supervision (monitoring of renal function at the beginning of joint use and periodically during treatment).
Hypoglycemic agents: Clinical studies show that diclofenac can be used in conjunction with oral hypoglycemic agents without affecting their clinical effect. However, there are isolated reports of hypoglycemic and hyperglycemic effects of the drug. Thus, when taking aceclofenac, it is necessary to adjust the doses of drugs that can cause hypoglycemia.
Zidovudine: With the concomitant use of NSAIDs and zidovudine, the risk of hematological toxicity increases. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive (human immunodeficiency virus) patients with hemophilia receiving zidovudine and ibuprofen.

special instructions

Avoid the simultaneous administration of the drug AertalЃ, film-coated tablets, 100 mg and other NSAIDs, including selective inhibitors of cyclooxygenase-2 (COX-2).
Adverse events can be minimized by using the lowest effective dose and reducing the duration of treatment needed to control symptoms.
Effect on the gastrointestinal tract (GIT)
Bleeding, ulceration or perforation of the gastrointestinal tract with a fatal outcome was observed with any NSAID intake at any period of treatment, as in the presence of appropriate symptoms and a history of serious gastrointestinal diseases (peptic ulcer and duodenal ulcer, Crohn's disease , ulcerative colitis, etc.), and without them.
The risk of bleeding, ulceration and perforation of the gastrointestinal tract increases with an increase in the dose of NSAIDs in patients with a history of peptic ulcer disease, especially if it was accompanied by bleeding or perforation, as well as in elderly patients. These patients should take the lowest effective dose of the drug. They need combination therapy with protective drugs (such as misoprostol or proton pump inhibitors). Such treatment is necessary for patients who take small doses of aspirin or other drugs that negatively affect the condition of the gastrointestinal tract.
Patients with diseases of the gastrointestinal tract, including the elderly, should report any unusual symptoms associated with the gastrointestinal tract (especially bleeding), including when taking the drug for the first time. Particular caution should be exercised in patients concurrently taking medications that may increase the risk of bleeding or ulceration, such as systemic glucocorticosteroids, anticoagulants (such as warfarin), selective serotonin reuptake inhibitors, or antiplatelet agents (such as acetylsalicylic acid).
If gastrointestinal bleeding or ulcers occur in patients taking AertalЃ, film-coated tablets, 100 mg, treatment should be canceled.
Effects on the cardiovascular and central nervous system
Patients with arterial hypertension and / or mild to moderate congestive heart failure require appropriate monitoring, since fluid retention and edema are associated with the use of NSAIDs.
Clinical studies and epidemiological data show that the use of some NSAIDs (in particular, in high doses and with prolonged use) may not significantly increase the risk of arterial thrombosis (for example, myocardial infarction or stroke). There is no reliable data on the absence of this risk when taking aceclofenac.
Patients with uncontrolled arterial hypertension, chronic heart failure, established ischemic heart disease, atherosclerosis of the peripheral arteries and / or impaired cerebral circulation should be especially careful when taking aceclofenac. Also, before the first dose, caution should be exercised in patients with risk factors for the cardiovascular system (for example, arterial hypertension, hyperlipidemia, diabetes mellitus and smoking).
Effects on the liver and kidneys
Taking NSAIDs can cause a dose-dependent decrease in prostaglandin production and acute renal failure. The importance of prostaglandins for ensuring renal blood flow should be considered when taking the drug in patients with impaired heart, kidney or liver function, in patients receiving diuretics, or in patients after surgery, as well as in the elderly.
Caution should be exercised when prescribing the drug to patients with mild or moderate hepatic and renal dysfunction, as well as to patients with other conditions that predispose to fluid retention in the body. In these patients, NSAIDs can lead to impaired renal function and fluid retention. Patients taking diuretics, persons with an increased risk of hypovolemia, should also be careful when taking the drug AertalЃ, film-coated tablets, 100 mg. It is necessary to prescribe the minimum effective dose and regular medical monitoring of renal function. Renal adverse events usually resolve after aceclofenac is discontinued.
Aceclofenac should be discontinued if changes in liver function indicators persist or worsen, clinical signs or symptoms of liver disease develop, or other manifestations (eosinophilia, rash) occur. Hepatitis can develop without prodromal symptoms.
The use of NSAIDs in patients with hepatic porphyria can provoke an attack.
Hypersensitivity and skin reactions
Like other NSAIDs, the drug can cause allergic reactions, including anaphylactic / anaphylactoid reactions, even if the drug is taken for the first time.
Severe skin reactions (some of which can be fatal), including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported very rarely after taking NSAIDs. The highest risk of these reactions in patients is observed at the beginning of taking the drug, and the development of these adverse reactions is observed during the first month of taking the drug. If you experience a skin rash, damage to the oral mucosa or other signs of hypersensitivity, you should stop taking aceclofenac.
In some cases, with chickenpox, infections of the skin and soft tissues can occur.
Currently, the role of NSAIDs in the worsening of the course of these infections cannot be ruled out. Therefore, you should avoid taking the drug AertalЃ, film-coated tablets, 100 mg for chickenpox.
Hematological disorders
Aceclofenac can cause reversible inhibition of platelet aggregation.
Respiratory system disorders
Care should be taken when taking the drug in patients with a history of bronchial asthma or current, as taking NSAIDs can provoke the development of sudden bronchospasm in such patients.
Elderly patients
Care should be taken when taking the drug in elderly patients, since they often have side effects (especially bleeding and perforation of the gastrointestinal tract) when taking NSAIDs. Complications can be fatal. Also, elderly patients are more likely to suffer from diseases of the kidneys, liver or cardiovascular system.
Long-term use
All patients receiving long-term treatment with non-steroidal anti-inflammatory drugs should be closely monitored (eg, complete blood count, liver and kidney function tests).

Influence on the ability to drive vehicles and work with mechanisms

You should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions, since the drug can cause dizziness and other side effects that may affect these abilities.