Alenthal tablets 100mg, No. 20

• Relief of inflammation and pain in lumbago, toothache, periarthritis of the shoulder scapula, rheumatic lesions of soft tissues;

• symptomatic treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis.

• 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 tablet should be swallowed whole with plenty of water.

The drug should be taken for as short a period of time as possible. The course of treatment is prescribed by the doctor individually.

Usually, adults are prescribed 1 table. 100 mg 2 times a day (morning and evening).

Film-coated tablets of white or almost white color, round, biconvex; in cross section, the core is white or almost white.

1 tab.

aceclofenac 100 mg

Excipients: microcrystalline cellulose - 82.6 mg, croscarmellose sodium - 8.0 mg, povidone K-30 - 6.4 mg, sodium stearyl fumarate - 3.0 mg.

• Hypersensitivity to aceclofenac or drug components;

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

• gastrointestinal bleeding or suspicion of it;

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

• severe liver failure or active liver disease;

• disorders of hematopoiesis and coagulation;

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

• severe heart failure;

• period after coronary artery bypass grafting;

• pregnancy;

• breastfeeding period;

• age up to 18 years.

With care: history of liver, kidney and gastrointestinal tract diseases; presence of Helicobacter pylori infection; bronchial asthma; arterial hypertension; decrease in BCC (including immediately after major surgical interventions); coronary heart disease; chronic renal, hepatic and heart failure; Cl creatinine less than 60 ml / min; history of ulcerative lesions of the gastrointestinal tract; cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes; peripheral arterial disease; smoking; elderly age; long-term use of NSAIDs; alcoholism; severe somatic diseases; defects in hemostasis; the risk of developing cardiovascular thrombosis (myocardial infarction, acute cerebrovascular accident - ischemic, hemorrhagic stroke); systemic lupus erythematosus; long-term use of NSAIDs; taking corticosteroids, anticoagulants, antiplatelet agents,serotonin reuptake inhibitors.

pharmachologic effect

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

Suction

After oral administration, aceclofenac is rapidly absorbed, its bioavailability is close to 100%. Cmax in blood plasma is reached within 1.25-3 hours after ingestion. Food intake slows down absorption, but does not affect its degree.

Distribution

Aceclofenac is highly associated with blood plasma proteins (> 99.7%). Aceclofenac penetrates into the synovial fluid, where its concentration reaches 60% of its concentration in blood plasma. Vd 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-aceclofenac are among the numerous metabolites of aceclofenac.

Withdrawal

Average 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.

Side effect

From the hematopoietic system: rarely - anemia; very rarely - inhibition of bone marrow activity, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia.

From the side of metabolism: very rarely - hyperkalemia, weight gain.

Allergic reactions: rarely - anaphylactic reactions, including shock, hypersensitivity.

From the side of the psyche: very rarely - depression, unusual (atypical) dreams, insomnia.

From the nervous system: often - dizziness; very rarely - paresthesia, tremor, drowsiness, headache, dysgeusia (taste perversion).

From the side of the organ of vision: rarely - visual impairment.

On the part of the organ of hearing and the labyrinth: very rarely - vertigo, tinnitus.

From the side of the cardiovascular system: rarely - heart failure, increased blood pressure; very rarely - tachycardia, flushing of the skin, 'hot flashes' (short-term feeling of heat, accompanied by increased sweating), vasculitis.

From the respiratory system: rarely - shortness of breath; very rarely - bronchospasm.

From the digestive system: often - dyspepsia, abdominal pain, nausea, diarrhea; infrequently - flatulence, gastritis, constipation, vomiting, ulceration of the oral mucosa; rarely - melena, ulceration of the gastrointestinal mucosa, hemorrhagic diarrhea, hemorrhages of the gastrointestinal mucosa; very rarely - stomatitis, vomiting of blood, intestinal perforation, worsening of Crohn's disease and ulcerative colitis, pancreatitis.

From the liver and biliary tract: often - increased activity of hepatic enzymes; very rarely - liver damage (including hepatitis), increased ALP activity.

On the part of the skin and subcutaneous tissue: infrequently - 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, serious skin infections and soft tissue infections were observed when taking NSAIDs during chickenpox disease.

From the urinary system: infrequently - an increase in the concentration of urea and creatinine in the blood plasma; very rarely - nephrotic syndrome, renal failure, interstitial nephritis.

Others: very rarely - increased fatigue, muscle spasms of the lower extremities.

Application during pregnancy and lactation

Pregnancy

AlentalЃ 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.

In the third trimester of pregnancy, all inhibitors of prostaglandin synthesis, having cardiopulmonary toxicity, can cause premature closure of the duct botalle with the development of pulmonary hypertension, as well as impaired renal function of the fetus, which can progress to renal failure in combination with polyhydramnios.

Women in late pregnancy and newborns: aceclofenac can affect the duration of bleeding due to the antiplatelet effect, which can develop even after very low doses; aceclofenac can suppress uterine contractions, leading to delayed labor or prolonged labor.

Breast-feeding

AlentalЃ should not be taken during breastfeeding. There are no data on the excretion of aceclofenac in breast milk; When radioactive 14C-aceclofenac was administered to lactating rats, no noticeable transfer of radioactivity into milk was observed.

Fertility

NSAIDs can affect fertility and are not recommended for women planning pregnancy.

Application for violations of liver function

The use of the drug is contraindicated in patients with severe liver dysfunction or active liver disease.

The drug should be used with caution in patients with a history of liver disease, chronic liver failure.

Application for impaired renal function

The use of the drug is contraindicated in patients with severe renal impairment (CC <30 ml / min), progressive kidney disease.

The drug should be used with caution in patients with a history of kidney disease, chronic renal failure.

Application in children

The use of the drug for children and adolescents under the age of 18 is contraindicated.

Use in elderly patients

Use the drug with caution in elderly patients.

special instructions

Avoid the simultaneous administration of AlentalЃ and other NSAIDs, including selective COX-2 inhibitors.

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

Impact on the gastrointestinal tract

Bleeding, ulcer or perforation of the gastrointestinal tract with a fatal outcome was observed when taking any NSAIDs during any period of treatment, both in the presence of appropriate symptoms and the presence of serious gastrointestinal diseases in history (gastric ulcer and duodenal ulcer, Crohn's disease, ulcerative colitis, and others), 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. Such patients should be prescribed the minimum effective dose of the drug. Also, when treating these groups of patients and patients who require the simultaneous use of acetylsalicylic acid in low doses or other drugs that can increase the risk of developing gastrointestinal complications, the need for combination therapy with protective drugs (for example, misoprostol or proton pump inhibitors ).

Patients with gastrointestinal diseases, incl. the elderly should report any unusual gastrointestinal symptoms (especially bleeding), incl. when taking AlentalЃ for the first time. Particular care should be taken in patients concurrently taking 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).

If gastrointestinal bleeding or ulcers occur, treatment with AlentalЃ should be canceled.

Effects on the cardiovascular system and central nervous system

Patients with arterial hypertension and / or mild to moderate congestive heart failure require appropriate follow-up. taking NSAIDs (in particular, in high doses 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 careful when taking AlentalЃ. 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, 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 elderly patients.

Caution should be exercised when prescribing the drug to patients with mild or moderate hepatic and renal impairment, 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, individuals with an increased risk of hypovolemia, should also be careful when taking AlentalЃ. 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 very rare after taking NSAIDs. The highest risk of these reactions occurs during the first month of taking the drug. If a skin rash, damage to the oral mucosa or other signs of hypersensitivity occurs, you should stop taking AlentalЃ.

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 AlentalЃ for chickenpox.

Hematological disorders

Aceclofenac can cause reversible inhibition of platelet aggregation.

Respiratory system disorder

Care should be taken when taking AlentalЃ in patients with a history of bronchial asthma or with ongoing bronchial asthma, because 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, because 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 NSAID treatment should be closely monitored (eg, complete blood count, liver and kidney function tests).

Influence on the ability to drive vehicles and 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, because the drug may cause dizziness and other side effects that may interfere with the indicated abilities.

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 are not effective enough.

Drug interactions

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 NSAIDs, 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 binds to a high degree with blood plasma albumin and, therefore, there is a possibility of displacement interaction with other drugs that bind 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 preparations: Some NSAIDs inhibit the renal clearance of lithium and digoxin, which leads to an increase in plasma concentrations of both substances. Joint use should be avoided unless frequent monitoring of the concentration of lithium and digoxin is carried out.

Anticoagulants: NSAIDs inhibit platelet aggregation and damage the gastrointestinal mucosa, which can increase anticoagulant action 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.

?иклоспорин, такролимус: при одновременном приеме Ќѕ¬ѕ с циклоспорином или такролимусом следует учитывать риск повышенной нефротоксичности из-за снижени¤ образовани¤ почечного простациклина. ѕоэтому при одновременном приеме следует тщательно контролировать показатели функции почек.

?ругие Ќѕ¬ѕ: при одновременном приеме ацетилсалициловой кислоты или других Ќѕ¬ѕ может увеличиватьс¤ частота возникновени¤ побочных ¤влений, поэтому следует соблюдать осторожность.

vлюкокортикоиды: возрастает риск возникновени¤ ¤звы или желудочно-кишечного кровотечени¤.

?иуретики: ацеклофенак, как и другие Ќѕ¬ѕ, может ингибировать активность диуретиков, может уменьшать диуретический эффект фуросемида и буметанида и антигипертензивный эффект тиазидов. —овместный прием с калийсберегающими диуретиками может привести к увеличению содержани¤ кали¤ в плазме крови. јцеклофенак не вли¤л на контроль ј? при совместном применении с бендрофлуазидом, хот¤ нельз¤ исключать взаимодействи¤ с другими диуретиками.

vипотензивные препараты: Ќѕ¬ѕ могут также уменьшать эффект гипотензивных препаратов. —овместный прием ингибиторов јѕ‘ или антагонистов рецепторов ангиотензина II и Ќѕ¬ѕ может привести к нарушению функции почек. –иск возникновени¤ острой почечной недостаточности, котора¤ обычно носит обратимый характер, может возрастать у некоторых пациентов с нарушени¤ми функции почек, например, у пожилых пациентов или при обезвоживании. ѕоэтому при совместном применении с Ќѕ¬ѕ следует соблюдать осторожность. ѕациенты должны потребл¤ть необходимое количество жидкости и находитьс¤ под соответствующим наблюдением (контроль функции почек в начале совместного применени¤ и периодически в ходе лечени¤).

vипогликемические средства: клинические исследовани¤ показывают, что диклофенак может примен¤тьс¤ совместно с пероральными гипогликемическими средствами без вли¤ни¤ на их клинический эффект. ќднако имеютс¤ отдельные сообщени¤ о гипогликемических и гипергликемических эффектах препарата. “аким образом, при приеме ацеклофенака следует провести коррекцию доз препаратов, которые могут вызвать гипогликемию.

«идовудин: при одновременном приеме Ќѕ¬ѕ и зидовудина возрастает риск гематологической токсичности. »меютс¤ данные об увеличении риска возникновени¤ гемартрозов и гематом у ¬»„-положительных пациентов с гемофилией, получающих зидовудин и ибупрофен.

ћифепристон: ацеклофенак может быть использован через 8-12 дней после приема мифепристона. т.к. Ќѕ¬ѕ уменьшают эффект препаратов данной группы.

Cholestyramine: other medicines, incl. and NSAIDs should be used at least 1 hour before or 4-6 hours after taking cholestyramine to reduce its effect on drug absorption.