Expiration date: 06/2026

Description 

Round tablets biconvex shaped, film-coated white or almost white. In cross section, the kernel white, or almost white.

Clinico-pharmacological group

Nonsteroidal anti-inflammatory drugs

Dosage form

Tablets, film-coated

Composition

Active substance: Aceclofenac 100 mg.

Excipients: core: Calcium stearate - 3 mg, talc - 9 mg, Silicon dioxide colloidal (Aerosil) - 1, 5 mg, microcrystalline Cellulose - 85 mg, Croscarmellose sodium (Primerose) - 10, 5 mg, Lactose monohydrate (milk sugar) - 91 mg kernel Weight is 300 mg. the shell: Polymer (hydroxypropyl methylcellulose) - 6, 4 mg, Macrogol - 4000 (polyethylene oxide-4000) - 2, 5 mg Titanium dioxide (titanium dioxide) - 1, 1 mg, Weight pills is 310 mg.

Pharmacological properties

Pharmacodynamics. Aceclofenac is a derivative of phenylacetic acid, inhibits cyclooxygenase I and II types. Has anti-inflammatory, analgesic and antipyretic activity. Inhibits the synthesis of prostaglandins and, thus, affect the pathogenesis of inflammation, pain and fever. In rheumatic diseases anti-inflammatory and analgesic effect aceclofenac contributes to a significant decrease in severity of pain, morning stiffness, swelling of joints that improves a functional condition of the patient. 

Pharmacokinetics. Aceclofenac rapidly and completely absorbed after ingestion. The time to reach maximum concentration is 1, 25-3 h Penetrates into synovial fluid, where its concentration reaches 57% of the plasma concentration and time to maximum concentrations 2-4 h later than in plasma. The volume of distribution is 25 l. 

Connection with plasma proteins (albuminami) is 99 %. Aceclofenac circulates mostly in unchanged form, the major metabolite is 4'-hydroxyacetophenone. 

The half-life is 4 hours Excreted by the kidneys, mainly in the form hydroxypropionic (about 2/3 of the administered dose). 

With caution

Diseases of the liver, kidneys and gastrointestinal tract in the anamnesis, bronchial asthma, hypertension, and a reduction in circulating blood (incl. after surgery), ischemic heart disease, mild or moderate chronic renal insufficiency (creatinine clearance 30 to 60 ml/min), mild or moderate hepatic insufficiency, chronic heart failure, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, diseases of peripheral arteries, Smoking, older age, prolonged use of NSAIDs in history, frequent alcohol use, concomitant therapy the following medications: - anticoagulants (e.g., warfarin); - antiplatelet agents (e.g. acetylsalicylic acid, clopidogrel); oral corticosteroids (e.g. prednisone); selective inhibitors of reverse takeover serotonin (e.g., citalopram, fluoxetine, paroxetine, sertraline).

Indications for use

Symptomatic treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis. Relief of inflammation and pain in lumbago, toothache, scapulohumeral periarthritis, rheumatic lesions of soft tissues. 

Contraindications

• erosive-ulcerative defeat of the gastrointestinal tract in acute phase, gastro-intestinal bleeding, or suspected it; 
  
• anamnestic data on the bronchial mast, hives, rhinitis after taking acetylsalicylic acid or other NSAIDs (complete or partial syndrome of intolerances acetylsalicylic acid - rhinosinusitis, urticaria, polyps are nasal mucosa, bronchial asthma); 
  
• hypersensitivity to aceclofenac or product components; 
  
• since the coronary artery bypass surgery; 
  
• severe hepatic impairment or active liver disease;
  
• severe renal failure (creatinine clearance less than 30 ml/min), a progressive kidney disease, hyperkalemia; 
  
• inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase; 
  
• decompensated heart failure; 
  
• violation of hematopoiesis and coagulation; 
  
• pregnancy and breastfeeding; 
  
• lactase deficiency (lactose intolerance); 
  
• children up to age 18 years. 
  

Pregnancy

The use of drugs in pregnancy and lactation is contraindicated. 

Method of application and doses

The drug should be taken in the minimum effective dose for the shortest period of time. 

Inside. Tablets are swallowed whole, squeezed enough liquid. 

The dose for all indications: 

Adults appoint 100 mg 2 times a day, 1 tablet in the morning and 1 in the evening. 

The course of treatment prescribed by the doctor individually. 

Hepatic insufficiency: patients with moderate-to-severe hepatic failure should reduce the dose of aceclofenac. The recommended initial dose is 100 mg daily. 

Renal insufficiency: there is no evidence that the dose of aceclofenac should be reduced in patients with mild renal impairment, but we recommend taking with caution. 

Side effects

The undesirable effects listed below are presented by system-organ classes according to MedDRA classification with the following frequency: common: ?1/100 to <1/10; uncommon: ?1/1000 to <1/100; rare: ?1/10000 to <1/1000; very rare: <1/10000. 

The blood and lymphatic system: rarely – anemia; very rarely bone marrow depression, granulocytopenia, neutropenia, hemolytic anemia. 

The immune system: rarely – anaphylactic reaction (including shock), hypersensitivity. 

From the metabolism and nutrition: very rarely – hyperkalemia. 

Psychiatric disorders: very rare – depression, unusual dreams, insomnia. 

From the nervous system: often – dizziness; very rarely – paresthesia, tremor, drowsiness, headache, dysgeusia. 

From the body of the vision: rarely – visual disturbances. 

On the part of the organ of hearing and labyrinth: very rarely – vertigo, ringing in the ears. 

Of the cardiovascular system: rarely- heart failure, hypertension, aggravated hypertension; very rarely – tachycardia, congestion, vasculitis. 

The respiratory system of the chest and mediastinum: rarely – dyspnea; very rarely – bronchospasm. 

The gastro-intestinal tract: often – neuralgia, pain in the abdomen, nausea, diarrhea; infrequent – flatulence, gastritis, constipation, vomiting, ulcers of the mucous membrane of the oral cavity; rare – melena, ulcer of the gastrointestinal tract, diarrhea with blood, gastro-intestinal bleeding; very rarely – stomatitis, vomiting blood, stomach ulcer, perforation of the small bowel, worsening of Crohn's disease and ulcerative colitis, pancreatitis. 

The liver and biliary tract: often – increased activity of "liver" enzymes; very rarely – liver damage (including hepatitis), increase of alkaline phosphatase activity of blood. 

The skin and subcutaneous tissue: often – itching, rash, dermatitis, urticaria; rare – angioneurotic edema; very rarely – purpura, eczema, reactions of the skin and mucous membranes, bullous skin reactions, including Stevens-Johnson syndrome and acute epidermal necrolysis. 

The kidneys and urinary tract: rarely – increased concentration of blood urea, increased creatinine concentration in blood: very rarely – interstitial nephritis, nephrotic syndrome, renal failure.

Overdose

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

Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy. There is no specific antidote. Forced diuresis, hemodialysis, blood transfusions ineffective. 

Use with other drugs

Studies of drug interactions have not been conducted, with the exception of warfarin. 

Aceclofenac metabolized by cytochrome system P450 – CYP2C9, and the data in vitro indicate that aceclofenac can be an inhibitor of this enzyme. Therefore, the potential risk of pharmacokinetic interaction with phenytoin, cimetidine, tolbutamide, phenylbutazone, amiodarone, miconazole and sulfaphenazole. 

As with other NSAIDs there is a risk of pharmacokinetic interaction with drugs, metabolism which takes place in the liver, such as methotrexate and drugs lithium. 

Aceclofenac almost entirely associated with plasma proteins and is, therefore, necessary to consider the possibility of substitution of other drugs strongly bind to plasma proteins. 

Due to the absence of pharmacokinetic interaction studies, the following data are based on information obtained by other NSAIDs: 

You should avoid the following combinations 

NSAIDs inhibit tubular secretion of methotrexate, and this also may be a metabolic interaction leading to a decrease clearance of methotrexate. Therefore, during treatment with high doses of methotrexate, you should always avoid the appointment of NSAIDs. 

Some NSAIDs inhibit the excretion of lithium by the kidneys which leads to elevated concentrations of lithium in serum. Should avoid this combination if it is impossible to conduct frequent monitoring of lithium concentration in blood serum. 

NSAIDs inhibit platelet aggregation and damage the mucous membrane of the gastrointestinal tract, which can increase the activity of anticoagulants and increase the risk of bleeding from the mucosa of the gastrointestinal tract in patients taking anticoagulants. 

You should avoid the combination of aceclofenac with oral anticoagulants of the coumarin group, ticlopidina, with thrombolytic drugs and heparin in the absence of careful control. 

With the following combinations may require dose adjustment and precautions 

It is necessary to consider the possible interaction of NSAIDs and methotrexate, especially in patients with renal insufficiency. When taking both drugs requires monitoring of kidney function. You should take precautions while taking NSAIDs and methotrexate for 24 h as the concentration of methotrexate may increase, leading to increased toxicity of methotrexate. 

It is assumed that the NSAIDs together with cyclosporine or tacrolimus increases the risk of nephrotoxicity due to decreased synthesis of prostacyclin in the kidney. Therefore the simultaneous administration of drugs it is important to monitor renal function. 

Simultaneous treatment with acetylsalicylic acid and other NSAIDs may increase the incidence of adverse reactions, and therefore, caution is required in their joint reception. 

NSAIDs may decrease diuretic effects of furosemide, bumetanide and antihypertensive effect of thiazide diuretics. Concomitant treatment with potassium-sparing diuretics may be associated with an increase of level of potassium in the blood serum, therefore it is necessary to control the content of potassium in the blood. 

NSAIDs can also reduce the effect of some antihypertensive drugs. Angiotensin converting enzyme inhibitors or antagonists of receptors of angiotensin II in combination with NSAIDs can cause kidney failure. The risk of acute renal failure which is usually reversible, may be increased in some patients with impaired renal function, such as elderly patients or patients experiencing a fluid deficit. Therefore, the combination of these drugs with NSAIDs should be used with caution, patients should get enough fluid from food, and should be monitoring of kidney function. 

Was not the effect of aceclofenac on blood pressure when it is taken simultaneously with bendrofluazide, although we can not exclude interaction with other antihypertensive drugs such as beta-blockers. 

Other possible interactions 

It was reported about some cases of hypoglycemia and hyperglycemia. Therefore, aceclofenac is necessary to adjust the dose of drugs that cause hypoglycemia. 

While the use of the drug Aceclofenac: 

• digoxin, phenytoin or lithium preparations can increase the levels in plasma of these drugs; 
  
• diuretics and antihypertensives – can weaken the effect of these medicines; 
  
• kalisberegath dioretikov can lead to the development of hyperglycemia and hyperkalemia; 
  
• other NSAIDs or corticosteroids increases the risk of side effects from the gastrointestinal tract; 
  
• selective inhibitors of serotonin reuptake (citalopram, fluoxetine, paroxetine, sertraline) increases the risk of gastrointestinal bleeding; 
  
• cyclosporine – may increase the toxic effects of the latter on the kidneys; 
  
• antidiabetic agents – can cause Hypo-and hyperglycemia. When this combination of funds is necessary to control the level of sugar in the blood; 
  
• acetylsalicylic acid reduced the concentration of aceclofenac in blood; 
  
• antiplatelet agents and anticoagulants – increased bleeding risk (requires regular monitoring of indicators of blood coagulation). 
  

Special instructions

The severity of adverse reactions can be corrected by lowering the effective single dose necessary to control symptoms. 

Patients with hypertension and/or mild or moderately severe congestive heart failure in history requires appropriate supervision and consultation to the doctor, as was reported fluid retention and edema in the treatment of NSAIDs. 

Data from clinical and epidemiological studies suggests that use of some NSAIDs (particularly at high doses and chronic administration) may increase the risk of arterial thrombosis (for example myocardial infarction or stroke). There is insufficient data to exclude such a risk for aceclofenac. Patients with uncontrolled hypertension, congestive heart failure, coronary heart disease, pathology of peripheral arteries and/or cerebrovascular disease should take aceclofenac only after a careful analysis of the clinical situation. The same caution need to make a decision before long-term treatment of patients with risk of cardiovascular disease (e.g. hypertension, hyperlipidemia, diabetes mellitus and Smoking). 

Aceclofenac must be taken with caution and under close medical supervision to patients suffering from diseases of the gastrointestinal tract, peptic ulcer history, after acute disorders of cerebral circulation, systemic lupus erythematosus, porphyria, disorders of hematopoietic system and blood clotting. 

Patients with Crohn's disease, ulcerative colitis the drug is administered not recommended. 

Caution is necessary in patients with hepatic, renal, or cardiac insufficiency and patients with other diseases likely to develop edema. The NSAIDs this category of patients may lead to deterioration of renal excretion and the occurrence of edema. Patients receiving diuretics, or with increased risk of development of hypovolemia, you must also exercise caution while taking the drug Aceclofenac. 

Caution is necessary in older patients, because they have more frequent side effects. Bleeding from the gastrointestinal tract and/or perforation can be during treatment, especially if the history of a disease of the gastrointestinal tract. In addition, elderly patients are more likely to arise disorders of the liver, kidneys, cardiovascular system. 

All patients receiving long-term treatment with NSAIDs, the necessary monitoring to reduce the risk of adverse reactions (e.g., urinalysis, General and biochemical blood analysis). 

Simultaneous reception of the drug Aceclofenac with any drug, suppresses the activity of cyclooxygenase/prostaglandin, may reduce fertility and is not recommended for women planning pregnancy. Women with history of infertility discontinue use of the drug Aceclofenac. 

Impact on the management of vehicles and mechanisms 

During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions. 

Release form

Tablet film coated 100mg. 

10 tablets are placed in a contour cell package made of polyvinylchloride film and aluminum foil printed patent. 

1, 3, 10 contour cell packages together with instructions for use is placed in cardboard pack. 

Storage conditions

In a dry, protected from light place, at temperatures not above 25 °C. Keep out of the reach of children.

Shelf life

2 years. Do not use after the expiry date printed on the package.