Aertal® (Airtal®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceAceclofenacAceclofenac
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    • Dosage form: & nbspfilm coated tablets
    Composition:

    One tablet contains:

    Active substance: aceclofenac 100 mg.

    Excipients: cellulose microcrystalline 89.2 mg; povidone 6.6 mg; glyceryl distearate, type I 2.6 mg; croscarmellose sodium 6.6 mg.

    Shell composition

    Sepyphylm 752 white 9 mg: hypromellose 40%, microcrystalline cellulose 32%, titanium dioxide 20%, macrogol stearate, type 18%.

    Description:

    Round, biconvex tablets of white color, covered with a film membrane, about 8 mm in diameter. On one side is engraved the letter "A".

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    M.01.A.B   Derivatives of acetic acid

    M.01.A.B.16   Aceclofenac

    Pharmacodynamics:

    Aceclofenac has an anti-inflammatory, analgesic and antipyretic effect.Oppresses the synthesis of prostaglandins and, thus, affects the pathogenesis of inflammation, the onset of pain and fever. In rheumatic diseases, the anti-inflammatory and analgesic effect of aceclofenac contributes to a significant reduction in the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the patient.

    Pharmacokinetics:

    Suction

    After oral administration aceclofenac quickly absorbed, its bioavailability is close to 100%. The maximum concentration (Cmah) in the blood plasma is achieved after 1.25 - 3 hours after ingestion. Eating slows down absorption, but does not affect its extent.

    Distribution

    Aceclofenac binds to a high degree with plasma proteins (> 99.7%). Aceclofenac penetrates into the synovial fluid, where its concentration reaches 60% of its concentration in the plasma. The volume of distribution is 30 liters.

    Metabolism

    It is believed that aceclofenac is metabolized by isoenzyme CYP2C9 with the formation of a metabolite of 4-OH-aceclofenac, 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.

    Excretion

    Average 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 ingestion is displayed unchanged.

    Indications:

    - Management of inflammation and pain syndrome with lumbago, toothache, periarthritis, rheumatic soft tissue injury, for symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis.

    - The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

    Contraindications:

    - erosive and ulcerative lesions of the gastrointestinal tract in the phase of exacerbation (including ulcerative colitis, Crohn's disease);

    - gastrointestinal bleeding or suspicion of it;

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

    - hypersensitivity to aceclofenac or drug components;

    - severe hepatic insufficiency or active liver disease;

    - disorders of hematopoiesis and coagulation;

    - severe renal failure (creatinine clearance <30 ml / min), progressive kidney disease, confirmed hyperkalemia;

    - severe heart failure;

    - period after aorto-coronary bypass surgery;

    - pregnancy and lactation;

    - children's age till 18 years.

    Carefully:

    Diseases of the liver, kidney and gastrointestinal tract in the anamnesis, the presence of infection Helicobacter pylori, bronchial asthma, arterial hypertension, decreased circulating blood volume (including immediately after extensive surgical interventions), coronary heart disease, chronic renal, hepatic and cardiac insufficiency, creatinine clearance less than 60 ml / min, ulcerative gastrointestinal (GI) in the anamnesis, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, old age, prolonged use of NSAIDs, severe somatic diseases, alcoholism.

    Pregnancy and lactation:

    Pregnancy

    Aertal®, film-coated tablets, 100 mg is contraindicated in pregnancy. Information on the use of aceclofenac in pregnancy is absent. The inhibition of the synthesis of prostaglandins 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:

    - having cardiopulmonary toxicity, can cause premature closure of the Botallov duct with the development of pulmonary hypertension;

    - may 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 influence the duration of bleeding due to the antiaggregant effect, which can develop even after the application of very low doses;

    - the drug can inhibit uterine contractions, resulting in delayed delivery or prolonged labor.

    Lactation

    Aertal®, film-coated tablets, 100 mg should not be taken while breastfeeding.Data on the isolation of aceclofenac with human milk are not available; when a radioactive 14C-aceclofenac to lactating rats, no appreciable transfer of radioactivity into the milk was observed.

    Fertility

    Non-steroidal anti-inflammatory drugs (NSAIDs) can affect fertility and are not recommended for use by women planning a pregnancy.

    Dosing and Administration:

    Inside. Tablets should be swallowed whole, with enough water. Usually adults are prescribed 1 tablet 100 mg 2 times a day (one tablet in the morning and one in the evening).

    Side effects:

    The following are undesirable phenomena, information about which was obtained in clinical studies and during post-marketing surveillance; Undesirable phenomena are grouped according to the classes of systems of organs according to the Medical dictionary for regulatory activities (MedDRA) and frequency of occurrence. Very often (> 1/10); often (from> 1/100 to <1/10); infrequently (from> 1/1000 to <1/100), rarely (from> 1/10000 to <1/1000), very rarely (<1/10000).

    Violations of the blood and lymphatic system

    Rare: anemia;

    Rarely: oppression of bone marrow activity, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia;

    Immune system disorders

    Rarely: anaphylactic reactions, including shock, hypersensitivity;

    Disorders of nutrition and metabolism

    Very rarely: hyperkalemia;

    Mental disorders

    Very rarely: depression, unusual (atypical) dreams, insomnia;

    Disturbances from the nervous system

    Often: dizziness;

    Very rarely: paresthesia, tremor, drowsiness, headache, dysgeusia (perversion of taste);

    Disturbances on the part of the organ of sight

    Rarely: impaired vision;

    Violations from the organ of hearing and labyrinth

    Very rarely: vertigo, tinnitus;

    Heart Disease

    Rarely: heart failure;

    Very rarely: heart palpitations;

    Vascular disorders

    Rarely: increased blood pressure;

    Rarely: hyperemia of the skin, "hot flashes" (a brief feeling of heat, accompanied by sweating), vasculitis;

    Disturbances from the respiratory system, chest and organ organs the mediastinum

    Rarely: shortness of breath;

    Very rarely: bronchospasm;

    Disorders from the gastrointestinal tract

    Often: indigestion, abdominal pain, nausea, diarrhea;

    Infrequent: flatulence, gastritis, constipation, vomiting, ulceration of the oral mucosa;

    Rarely: melena, ulceration of the mucous membrane of the gastrointestinal tract, hemorrhagic diarrhea, hemorrhage of the mucous membrane of the gastrointestinal tract;

    Very rarely: stomatitis, vomiting of blood, perforation of the intestine, worsening of Crohn's disease and ulcerative colitis, pancreatitis;

    Disturbances from the liver and bile ducts

    Often: increased activity of "liver" enzymes;

    Very rarely: liver damage (including hepatitis), increased activity of alkaline phosphatase;

    Disturbances from the skin and subcutaneous tissue

    Infrequent: itching, rash, dermatitis, urticaria;

    Rarely: angioedema;

    Very rarely: purpura, eczema, severe reactions from the skin and mucous membranes (including Stevens-Johnson syndrome and toxic epidermal necrolysis);

    In some cases, severe skin infections and soft tissue infections were observed when taking NSAIDs during a disease with chicken pox.

    Disorders from the kidneys and urinary tract

    Infrequent: increased serum levels of urea and creatinine;

    Very rarely: nephrotic syndrome, renal failure, interstitial nephritis;

    Systemic disorders and complications at the site of administration

    Very rarely: edema, fatigue, lower limb spasms;

    Laboratory test data

    Very rarely: weight gain.

    If the patient has noted a worsening of any of the listed adverse events or the occurrence of an undesirable phenomenon not specified in this manual, he should contact the doctor in charge.

    Overdose:

    There is no evidence of an overdose of aceclofenac in humans.

    Possible Symptoms: nausea, vomiting, pain in the stomach, dizziness, headache, hyperventilation with increased convulsive readiness.

    Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy. Forced diuresis, hemodialysis is not effective enough.

    Interaction:

    With the exception of warfarin, studies of drug interactions have not been conducted. Aceclofenac metabolized by isoenzyme CYP2C9; data in vitro show that aceclofenac may be an inhibitor of this enzyme.Thus, the risk of pharmacokinetic interaction is possible with simultaneous administration with phenytoin, cimetidine, tolbutamide, phenylbutazone, amiodarone, miconazole and sulfafenazole. As with other non-steroidal anti-inflammatory drugs, the risk of pharmacokinetic interaction with other drugs is increased, which are excreted through active renal secretion, such as methotrexate and lithium preparations. Aceclofenac almost completely binds to blood plasma albumin and, consequently, there is the possibility of reuptake-type interactions with other drugs that bind to proteins. Below is the class-specific information for NSAIDs:

    Methotrexate: NSAIDs inhibit the tubular secretion of methotrexate; moreover, a small metabolic interaction can occur, which leads to a decrease in the clearance of methotrexate. Therefore, when high doses of methotrexate are used, NSAIDs should be avoided.

    Lithium and digoxin preparations: Some NSAIDs inhibit renal clearance of lithium and digoxin, which leads to an increase in serum concentrations of both substances.Joint use should be avoided if frequent monitoring of lithium and digoxin concentrations is not carried out.

    Anticoagulants: NSAIDs inhibit platelet aggregation and damage the mucous membrane of the gastrointestinal tract, which can lead to increased anticoagulant action and increase the risk of gastrointestinal bleeding while taking anticoagulants. Avoid the combined use of aceclofenac and oral anticoagulants coumarin group, ticlopidine and thrombolytics, unless careful monitoring of the patient's condition is performed.

    Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) when combined with NSAIDs may increase the risk of gastrointestinal bleeding.

    Cyclosporin, tacrolimus: With the simultaneous administration of NSAIDs with cyclosporine or tacrolimus, the risk of increased nephrotoxicity due to decreased renal prostacyclin formation should be considered. Therefore, with simultaneous admission, you should carefully monitor the indicators of kidney function.

    Other NSAIDs: With the simultaneous use of acetylsalicylic acid or other NSAIDs, the incidence of side effects may increase, so caution should be exercised.

    Glucocorticosteroids: the risk of ulcers or gastrointestinal bleeding increases.

    Diuretics: AceclofenacLike other NSAIDs, may inhibit the activity of diuretics, may reduce the diuretic effect of furosemide and bumetanide and antihypertensive effect of thiazide. Joint reception with potassium-sparing diuretics can lead to an increase in the potassium content in the blood serum. Aceclofenac did not affect the control of blood pressure when combined with bendrofluazidom, although it is impossible to exclude interactions with other diuretics.

    Hypotensive drugs: NSAIDs can also reduce the effect of antihypertensive drugs. Co-administration of angiotensin converting enzyme (ACE) inhibitors or antagonists of angiotensin II receptors and NSAIDs can cause renal dysfunction. The risk of acute renal failure, which usually is reversible, may be increased in some patients with impaired renal function, such as the elderly or dehydrated. Therefore, when combined with NSAIDs, care should be taken. Patients should consume the required amount of fluid and be underappropriate supervision (control of kidney 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 some reports of hypoglycemic and hyperglycemic effects of the drug. Thus, when taking aceclofenac, you should correct the dosage of drugs that can cause hypoglycemia.

    Zidovudine: With the simultaneous use of NSAIDs and zidovudine, the risk increases hematological toxicity. 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:

    Avetal®, film-coated tablets, 100 mg and other NSAIDs, including selective inhibitors of cyclooxygenase-2 (COX-2) should be avoided concomitantly.

    Undesirable effects can be minimized by applying the minimum effective dose and reducing the duration of treatment needed to control symptoms.

    Effects on the gastrointestinal tract (GIT)

    Bleeding ulcer or perforation GI deaths were observed when receiving any NSAIDs at any time during the treatment, both with the appropriate symptoms, and the presence of serious gastrointestinal diseases in history (gastric ulcer and duodenal ulcer, Crohn's disease, ulcerative colitis, etc.), So and without them.

    The risk of bleeding, ulceration and perforation of the gastrointestinal tract increased with increasing doses of NSAIDs in patients with peptic ulcer history, especially if it is accompanied by bleeding or perforation, as well as in elderly patients. These patients should take the minimum effective dose of the drug. They need combination therapy with protective agents (for example, misoprostol or proton pump inhibitors). Such treatment is necessary for patients who take small doses of aspirin or other drugs that negatively affect the state of the gastrointestinal tract.

    Patients with diseases of the gastrointestinal tract, including the elderly, should report any unusual symptoms related to the gastrointestinal tract (especially bleeding), including during the initial dose.Particular caution should be exercised in patients taking concomitant medications that may increase the risk of bleeding or ulcers, such as systemic corticosteroids, anticoagulants (such as warfarin), selective serotonin reuptake inhibitors or antiplatelet agents (such as acetylsalicylic acid).

    In the event of gastrointestinal bleeding or ulcers in patients taking Aertal®, film-coated tablets, 100 mg treatment should be discontinued.

    Effects on the cardiovascular and neutral nervous system

    Patients with arterial hypertension and / or congestive heart failure, mild or moderate need appropriate observation because NSAID associated with fluid retention and edema.

    Clinical trials and epidemiological data indicate that the use of certain NSAIDs (particularly at high doses and for prolonged use) could be slightly increased 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, peripheral arterial atherosclerosis and / or cerebrovascular accident should be especially careful when taking aceclofenac. Also, before the first dose, care should be taken for patients with risk factors for the cardiovascular system (eg, hypertension, hyperlipidemia, diabetes and smoking).

    Effects on the liver and kidneys

    Taking NSAIDs can cause a dose-related reduction in the formation of prostaglandins 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 administering the drug to patients with impaired hepatic and renal function of mild or moderate degree, as well as to patients with other conditions predisposing to fluid retention in the body.In these patients, NSAIDs can lead to impaired renal function and fluid retention. Patients taking diuretics, people with an increased risk of hypovolemia should also be careful when taking Avertal®, film-coated tablets, 100 mg. It is necessary to appoint a minimum effective dose and regular medical monitoring of kidney function. Undesirable effects from the kidneys are usually resolved after discontinuation of aceclofenac.

    Admission of aceclofenac should be discontinued if changes in liver function are preserved or worsened, 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 lead to death), including exfoliative dermatitis,Stevens-Johnson syndrome and toxic epidermal necrolysis, after the intake of NSAIDs were very rare. The highest risk of these reactions in patients is observed at the beginning of the drug, and the development of these adverse reactions is observed during the first month of taking the drug. In case of skin rash, damage to the oral mucosa or other signs of hypersensitivity, you should stop taking aceclofenac.

    In some cases, with chickenpox, skin and soft tissue infections may occur.

    At present, the role of NSAIDs in worsening of the course of these infections can not be ruled out. Therefore, Avertal®, film-coated tablets, 100 mg with chicken pox should be avoided.

    Hematologic disorders

    Aceclofenac can cause reversible inhibition of platelet aggregation.

    Disturbances from the respiratory system

    Care should be taken when taking the drug in patients with bronchial asthma in the anamnesis or current, since the use of NSAIDs can provoke the development of sudden bronchospasm in such patients.

    Elderly patients

    Care should be taken when taking the drug in elderly patients, because they often have side effects (especially bleeding and perforation of the gastrointestinal tract) when taking NSAIDs. Complications can lead to death. Also, older patients are more likely to suffer from kidney, liver or cardiovascular disease.

    Long-term use

    All patients receiving long-term treatment with nonsteroidal anti-inflammatory drugs should be closely monitored (for example, a general blood test, functional hepatic and renal tests).

    Effect on the ability to drive transp. cf. and fur:

    It is necessary to refrain from driving vehicles and practicing other potentially hazardous activities requiring increased concentration attention and speed of psychomotor reactions, as the drug can cause dizziness and other side effects that can affect these abilities.

    Form release / dosage:Film-coated tablets, 100 mg.
    Packaging:

    For 10 tablets, film-coated in a blister of PA / AL / PVC - film and aluminum foil. By 1,2, 3, 4, 6 or 9 blisters with instructions for use in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013504 / 01
    Date of registration:19.11.2007
    The owner of the registration certificate:Almiral S.A.Almiral S.A. Spain
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp16.06.2014
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