Aceclagin tablets 200mg, No. 30

• Relief of inflammation and pain in lumbago, toothache, periarthritis of the shoulder scapula, rheumatic lesions of soft tissues; for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis;

• Symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

• dysmenorrhea.

The drug is taken orally. The tablets should be swallowed whole with plenty of water.

The recommended daily dose for adults is 200 mg with a single dose (1 tablet / day).

White or off-white film coated modified release tablets, oblong, biconvex, engraved with 'UT' on one side and 'CL CR' on the other side.

1 tab.

aceclofenac 200 mg

Excipients: microcrystalline cellulose - 159.5 mg, povidone K30 - 19.5 mg, croscarmellose sodium - 9.7 mg, sodium stearyl fumarate - 15.3 mg, poloxamer 407 - 4.5 mg, hypromellose - 40.5 mg, carbomer 941 - 2.5 mg.

• Hypersensitivity to aceclofenac or auxiliary components of the drug;

• bronchospasm, rhinitis or urticaria 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);

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

• gastrointestinal bleeding or suspicion of it;

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

• period after coronary artery bypass grafting;

• severe liver failure or active liver disease; severe renal failure (CC <30 ml / min), progressive kidney disease, confirmed hyperkalemia;

• disorders of hematopoiesis and coagulation;

• pregnancy;

• breastfeeding period;

• age up to 18 years.

• With care: a history of liver, kidney and gastrointestinal tract diseases, bronchial asthma, arterial hypertension, a decrease in BCC (including after major surgical interventions), coronary artery disease, chronic renal, hepatic and heart failure, CC less than 60 ml / min, ulcerative history of gastrointestinal tract damage, Helicobacter pylori infection, dyslipidemia / hyperlipidemia, diabetes mellitus, severe somatic diseases, prolonged use of NSAIDs, smoking, alcoholism, old age.

pharmachologic effect

Aceclofenac has anti-inflammatory, analgesic, 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. 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 bound to plasma proteins (> 99.7%). Aceclofenac penetrates into the synovial fluid, where its concentration reaches 60% of the level 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. Diclofenac and 4-OH-diclofenac are among the numerous metabolites of aceclofenac.

Withdrawal

Average T1 / 2 when taking modified release tablets is about 5 hours. Clearance is 5 l / h. Approximately 2/3 of the dose taken is excreted by the kidneys, mainly in the form of conjugated hydroxy metabolites. 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 function, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia.

From the immune system: rarely - anaphylactic reactions, including shock, hypersensitivity.

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

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, worsening of the course of arterial hypertension; very rarely - palpitations, flushing of the skin, 'hot flashes' (short-term feeling of heat, accompanied by 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 and soft tissue infections have been observed when taking NSAIDs during chickenpox disease.

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

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

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.

Application during pregnancy and lactation

Pregnancy

The use of the drug AceclaginЃ is contraindicated during 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:

• possessing cardiopulmonary toxicity, they can cause premature closure of the botallov's duct with the development of pulmonary hypertension;

• can cause impaired renal function of the fetus, which can progress to renal failure in combination with polyhydramnios.

In late pregnancy:

• the drug can affect the duration of bleeding due to the antiplatelet effect, which can develop even after very low doses;

• the drug can suppress uterine contractions, leading to delayed labor or prolonged labor.

Breastfeeding period

The drug should not be taken while breastfeeding. There are no data on the allocation of aceclofenac in human milk. In preclinical studies with the introduction of radioactive 14C-aceclofenac, a noticeable transfer of radioactivity into milk was not observed.

Fertility

NSAIDs can interfere with fertility and are 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 liver disease in the active stage.

With care: history of liver disease, chronic liver failure.

Application for impaired renal function

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

With care: a history of kidney disease, chronic renal failure, CC less than 60 ml / min.

Application in children

The use is contraindicated under the age of 18 years.

Use in elderly patients

The drug should be prescribed with caution to elderly patients.

special instructions

Avoid the simultaneous use of the drug AceclaginЃ 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, ulceration or perforation of the gastrointestinal tract with a fatal outcome was observed with any NSAID intake at any time of treatment, as in the presence of appropriate symptoms and a history of serious gastrointestinal diseases (including gastric ulcer and duodenal ulcer, Crohn's disease, ulcerative colitis) , 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. Consideration should be given to the use of combination therapy with protective drugs (for example, misoprostol or proton pump inhibitors). Such treatment is necessary for patientswho take low-dose aspirin or other drugs that negatively affect the gastrointestinal tract.

Patients with gastrointestinal diseases, incl. the elderly should report any unusual gastrointestinal symptoms (especially bleeding), incl. at the first dose of the drug. Particular care should be taken in patients who are simultaneously taking medications that may increase the risk of bleeding or ulcers, such as systemic corticosteroids, anticoagulants (eg, warfarin), selective serotonin reuptake inhibitors, or antiplatelet agents (eg, acetylsalicylic acid).

If gastrointestinal bleeding or ulcers occur in patients taking AceclaginЃ, treatment should be canceled.

Cases of drug-induced pancreatitis are rare. However, cases of pancreatitis have been reported in association with NSAIDs.

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. NSAIDs are associated with fluid retention and edema. Aceclofenac is structurally similar to diclofenac, has a similar metabolism. With regard to diclofenac, there are data indicating an increased risk of thromboembolic complications (for example, myocardial infarction or stroke, in particular, with long-term treatment with high doses). There is also an increased risk of developing acute coronary syndrome associated with taking aceclofenac. Patients with chronic heart failure (I FC according to NYHA classification) and patients with risk factors for the development of complications from the cardiovascular system (for example, arterial hypertension, diabetes mellitus,smoking) should start treatment with aceclofenac only after the informed decision of the doctor. The risk from the cardiovascular system may depend on the dose and duration of treatment, therefore the drug should be prescribed in the lowest effective dose and for the shortest possible period of time.

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 AceclaginЃ 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 using the drug AceclaginЃ in patients with impaired liver and kidney function of mild to moderate severity, as well as in patients with other conditions that predispose to fluid retention in the body. In these patients, the use of NSAIDs can lead to impaired renal function and fluid retention. In patients taking diuretics, individuals with an increased risk of hypovolemia, caution should also be exercised when taking the drug AceclaginЃ. It is necessary to use the minimum effective dose and regular medical monitoring of renal function. Renal adverse events usually resolve after aceclofenac is discontinued. Taking the drug AceclaginЃ should be discontinued if changes in liver function indicators persist or worsen,clinical signs or symptoms of liver disease develop, or other manifestations (eosinophilia, skin 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, aceclofenac can cause allergic reactions, including anaphylactic / anaphylactoid reactions, even when aceclofenac 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 aceclofenac, and the development of these adverse reactions is observed during the first month of taking aceclofenac. If a skin rash, damage to the oral mucosa or other signs of hypersensitivity occurs, you should stop taking AceclaginЃ.

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 AceclaginЃ for chickenpox.

Hematological disorders

Aceclofenac can cause reversible inhibition of platelet aggregation.

Respiratory system disorders

Caution should be exercised when taking AceclaginЃ in patients with bronchial asthma (including a history), because taking NSAIDs can provoke the development of sudden bronchospasm in such patients.

Elderly patients

Care should be taken when taking the drug AceclaginЃ 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).

Due to the antiprostaglandin properties of NSAIDs, caution is advised in women taking mifepristone. when used together with NSAIDs, theoretically, a decrease in the effectiveness of the drug may occur. The clinical significance is unknown.

Influence on the ability to drive vehicles and use 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, intake of activated charcoal, symptomatic therapy; forced diuresis, hemodialysis is not effective enough.

Drug interactions

With the exception of concomitant use with 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 almost completely binds to 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 methotrexate in high doses, NSAIDs should be avoided.

Lithium preparations and digoxin. Some NSAIDs inhibit the renal clearance of lithium and digoxin, which leads to an increase in serum concentrations of both substances. Concomitant use should be avoided unless frequent monitoring of lithium and digoxin concentrations is performed.

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јнтиагрегантные средства и селективные ингибиторы обратного захвата серотонина (SSRIs) при совместном применении с Ќѕ¬ѕ могут увеличивать риск желудочно-кишечного кровотечени¤.

?иклоспорин, такролимус. ѕри 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. ѕри одновременном приеме ацетилсалициловой кислоты или других Ќѕ¬ѕ может увеличитьс¤ частота возникновени¤ побочных ¤влений, поэтому следует соблюдать осторожность.

v —. ¬озрастает риск возникновени¤ ¤звы или желудочно-кишечного кровотечени¤.

?иуретики. јцеклофенак, как и другие Ќѕ¬ѕ, может ингибировать активность диуретиков, уменьшать диуретический эффект фуросемида и буметанида и антигипертензивный эффект тиазидов. ќдновременный прием с калийсберегающими диуретиками может привести к увеличению содержани¤ кали¤ в сыворотке крови. ѕри одновременном применении с калийсберегающими диуретиками необходим контроль кали¤ в сыворотке крови. јцеклофенак не вли¤л на контроль ј? при совместном применении с бендрофлуазидом, хот¤ нельз¤ исключить 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 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¤).

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 simultaneous administration 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.