Aceclagin modified-release pills 200mg, 30pcs

Composition

1 tablet contains:

Active ingredient

aceclofenac 200.0 mg;

excipients:

microcrystalline cellulose 159.5 mg,

povidone-KZO 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.

Shell composition:

Opadray white OY-C-7000 A 12.0 mg: hypromellose 5 cP (E 464) 54.850%, titanium dioxide (E 171) 22.860%. ethylcellulose UsP 13.720%), diethyl phthalate 8.570%.

Pharmacological action

Pharmacotherapy group:  nonsteroidal anti-inflammatory drug (NSAID)CodATH: M 01 AB 16 Pharmacological Propertiespharmacodynamicaceclofenac has anti-inflammatory, analgesic, antipyretic effects. Inhibits the synthesis of prostaglandins and thus, it affects the pathogenesis of inflammation, pain and fever. In rheumatic diseases, the anti-inflammatory and analgesic effect of aceclofenac significantly reduces the severity of pain, morning stiffness, and joint swelling, which improves the patient’s functional state. Pharmacokineticsabsorption. After oral use, aceclofenac is rapidly absorbed. The maximum concentration (Ctax) – in blood plasma is reached in 1.25-3 hours after oral use. Food intake slows down absorption, but does not affect its degree. Distribution. Aceclofenac is highly bound to plasma proteins (>99.7%). Aceclofenac penetrates the synovial fluid, where its concentration reaches 60% of the level of its concentration in blood plasma. The volume of distribution is 30 liters. Metabolism. Aceclofenac is thought to be metabolized by the CYP2C9 isoenzyme to form the 4-OH-aceclofenac metabolite. Diclofenac and 4-OH-diclofenac are among the numerous metabolites of aceclofenac. Output. The average half-life (Ti/g) of modified-release tablets is about 5 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 is excreted unchanged after oral use.

Indications

• Relief of inflammation and pain in lumbago, toothache, scapular periarthritis, rheumatic soft tissue disease, for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis.
• Symptomatic therapy, reduction of pain and inflammation at the time of use, does not affect the progression of the disease.
• Dysmenorrhea.

Use during pregnancy and lactation

Pregnancy

The use of Aceclagin® is contraindicated during pregnancy. There is no information on the use of aceclofenac during pregnancy. Inhibition of prostaglandin synthesis may adversely affect the course of pregnancy and/or the development of the embryo / fetus.

During the third trimester of pregnancy, all prostaglandin synthesis inhibitors are used:

• having cardiopulmonary toxicity, they can cause premature closure of the Botall duct with the development of pulmonary hypertension;
• they can cause impaired fetal kidney function, 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. Breast-feeding period

The drug should not be taken during breast-feeding. There are no data on the excretion of aceclofenac in human milk. In preclinical studies, no significant transfer of radioactivity into milk was observed with the use of radioactive C-aceclofenac.

Fertility

Nonsteroidal anti-inflammatory drugs (NSAIDs) may affect fertility and are not recommended for use by women planning pregnancy.

Contraindications

• Hypersensitivity to aceclofenac or auxiliary components of the drug;
• bronchospasm, rhinitis or urticaria after ingestion of acetylsalicylic acid or other NSAIDs in history (full or partial syndrome of intolerance to acetylsalicylic acid, rhinosinusitis, urticaria, mucosal polyps of the nasal cavity, bronchial asthma);
• erosive-ulcerative lesions of the mucosa of the gastrointestinal tract (GI) tract in acute phase (including ulcerative colitis, Crohn’s disease);
• gastrointestinal bleeding or suspicion of it;
• severe heart failure (II-IV according to the classification of new York heart Association), ischemic heart disease, peripheral arterial disease and /or cerebral arteries;
• the period following the coronary artery bypass surgery;
• severe liver failure or liver disease in the active stage;
• severe renal insufficiency (creatinine clearance <30 ml/min), progressive kidney diseases, confirmed hyperkalemia;
• disorders of blood formation and coagulation;
• pregnancy and lactation;
• children up to age 18 years.

Be wary

of Diseases of liver, kidney and gastrointestinal tract in anamnesis, bronchial asthma, arterial hypertension, reduction of circulating blood volume (including after extensive surgical interventions), ischemic heart disease, chronic kidney and liver and heart failure, creatinine clearance less than 60 ml/min, ulcerative lesions of the gastrointestinal tract in history, the presence of Helicobacter pylori infection, dyslipidemia/hyperlipidemia, diabetes, Smoking, advanced age, prolonged use of NSAIDs, severe somatic diseases, alcoholism.

Side effects

Adverse events reported in clinical trials and post-marketing follow-up are listed below. The frequency of adverse events is classified as follows: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥1/1000 to < 1/100), rare (≥1/10000 to < 1/1000), very rare (From the blood and lymphatic system: rarely-anemia; very rarely – bone marrow suppression, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia. Immune system disorders: 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 (perversion of taste). From the side of the organ of vision: rarely-visual impairment. From the side of the organ of hearing and labyrinth: very rarely – vertigo, tinnitus. From the heart: rarely-heart failure; very rarely-rapid heartbeat. Vascular disorders: rarely-increased blood pressure, worsening of arterial hypertension; very rarely-hyperemia of the skin, “hot flashes” (a short-term feeling of heat accompanied by sweating), vasculitis. Respiratory, thoracic and mediastinal disorders: rarely-dyspnea; very rarely-bronchospasm. From the gastrointestinal tract: 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. colitis, pancreatitis. From the liver and biliary tract: often-increased activity of “liver” enzymes; very rarely-liver damage (including hepatitis), increased activity of alkaline phosphatase. Skin and subcutaneous tissue disorders: infrequently-pruritus. rash, dermatitis, urticaria; rarely-angioedema; very rarely-purpura, eczema, severe skin and mucosal reactions (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 side of the kidneys and urinary tract: infrequently-increased concentration of urea and creatinine in the blood serum; very rarely-nephrotic syndrome, renal failure. Systemic disorders and complications at the injection site: very rarely – edema, increased fatigue, muscle spasms of the lower extremities. If the patient notes a worsening of any of the listed adverse events or the occurrence of an adverse event not specified in these instructions, they should contact their doctor.

Interaction

With the exception of concomitant use with warfarin, no drug interaction studies have 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 co-administered with phenytoin, cimetidine, tolbutamide, phenylbutazone, amiodarone, miconazole and sulfafenazole. As with other NSAIDs, there is an increased risk of pharmacokinetic interactions with other drugs that are eliminated from the body by active renal secretion, such as methotrexate and lithium preparations. Aceclofenac is almost completely bound to plasma albumin and, therefore, there is a possibility of displacement-type interactions with other protein-binding drugs.The following is class-specific information for NSAIDs:Methotrexate. NSAIDs inhibit the tubular secretion of methotrexate; moreover, there may be a small metabolic interaction, which leads to a decrease in the clearance of methotrexate. Therefore, when using high doses of methotrexate, 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. Co-use should be avoided unless lithium and digoxin concentrations are monitored frequently. Anticoagulants. NSAIDs inhibit platelet aggregation and damage the gastrointestinal mucosa, which can lead to increased action of anticoagulants and increase the risk of gastrointestinal bleeding while taking anticoagulants. Concomitant use of aceclofenac and oral coumarin anticoagulants, ticlopidine and thrombolytics should be avoided if the patient’s condition is not carefully monitored. Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) when co-administered with NSAIDs may increase the risk of gastrointestinal bleeding. Cyclosporine, tacrolimus. Concomitant use of NSAIDs with cyclosporine or tacrolimus should take into account the risk of increased nephrotoxicity due to reduced formation of renal prostacyclin. Therefore, when taking it at the same time, renal function indicators should be carefully monitored. Other NSAIDs. When taking acetylsalicylic acid or other NSAIDs at the same time, the frequency of side effects may increase, so caution should be exercised. Glucocorticosteroids (corticosteroids). The risk of ulcers or gastrointestinal bleeding increases. Diuretics. Aceclofenac, like other NSAIDs, may inhibit the activity of diuretics, may reduce the diuretic effect of furosemide and bumetanide, and the antihypertensive effect of thiazides. Concomitant use with potassium-sparing diuretics may lead to an increase in serum potassium. When used concomitantly with potassium-sparing diuretics, serum potassium monitoring is necessary. Aceclofenac did not affect blood pressure control when co-administered with bendrofluazide, although interactions with other diuretics cannot be excluded. Antihypertensive drugs. NSAIDs may also reduce the effect of antihypertensive medications. Concomitant use of angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists and NSAIDs may 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, caution should be exercised when co-administered with NSAIDs. Patients should consume the appropriate amount of fluids and be monitored accordingly (monitoring of renal function at the beginning of co-use and periodically during treatment). Hypoglycemic agents. Clinical studies show that diclofenac can be used in combination with oral hypoglycemic agents without affecting their clinical effect. However, there are separate reports of hypoglycemic and hyperglycemic effects of the drug. Thus, when taking aceclofenac, dose adjustments should be made for drugs that may cause hypoglycemia. Zidovudine. Concomitant use of NSAIDs and zidovudine increases the risk of hematological toxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive (human immunodeficiency virus) patients with hemophilia treated with zidovudine and ibuprofen.

How to take, course of use and dosage

Inside. Tablets should be swallowed whole, washed down with a sufficient amount of water. The recommended daily dose for adults is 200 mg in a single dose (1 tablet per day).

Overdose

There are no data on aceclofenac overdose in humans. Possible symptoms: nausea, vomiting, stomach pain, dizziness, headache, hyperventilation with increased convulsive readiness. Treatment: gastric lavage, taking activated charcoal, symptomatic therapy. Forced diuresis, hemodialysis is not effective enough

Special instructions

Concomitant use of Aceclagin and other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors, should be avoided. Adverse events can be minimized by applying the minimum effective dose and reducing the duration of treatment required to control symptoms. Bleeding, ulceration or perforation of the gastrointestinal tract with a fatal outcome were observed when taking any NSAIDs during any period of treatment, both with the presence of appropriate symptoms and the presence of serious gastrointestinal diseases in the anamnesis (gastric and duodenal ulcers, Crohn’s disease, ulcerative colitis, etc. ), and without them. The risk of bleeding, ulceration and perforation of the gastrointestinal tract increases with increasing NSAID dose 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 minimum 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 patients who take small doses of aspirin or other medications that negatively affect the gastrointestinal tract. Patients with gastrointestinal diseases, including the elderly, should report any unusual symptoms associated with the gastrointestinal tract (especially bleeding), including when taking the drug for the first time. Special care should be taken in patients taking concomitant medications that may increase the risk of bleeding or ulceration, such as: systemic corticosteroids, anticoagulants (such as warfarin), selective serotonin reuptake inhibitors, or antiplatelet agents (such as acetylsalicylic acid). If gastrointestinal bleeding or ulceration occurs in patients taking Aceclagin®, treatment should be discontinued. Cases of drug-induced pancreatitis are rare. However, cases of pancreatitis have been reported in association with NSAIDs. Effects on the cardiovascular and central nervous systems Patients with hypertension and / or mild to moderate congestive heart failure need appropriate monitoring, as fluid retention and edema are associated with NSAID use. Aceclofenac is structurally similar to diclofenac and has a similar metabolism. For diclofenac, there is evidence indicating an increased risk of developing thromboembolic complications (for example, myocardial infarction or stroke, in particular with long-term high-dose treatment). There is also an increased risk of developing acute coronary syndrome associated with taking aceclofenac. Patients with chronic heart failure (Class I according to the classification of the New York Heart Association) and patients with risk factors for developing complications from the cardiovascular system (for example, arterial hypertension, diabetes mellitus, smoking) should start treatment with aceclofenac only after an informed decision of the doctor. Risks from the cardiovascular system may depend on the dose and duration of treatment, so the drug should be prescribed at 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 Aceclagin 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 Aceclagin in patients with mild to moderate hepatic and renal impairment, as well as in patients with other conditions predisposing to fluid retention in the body. In such patients, the use of NSAIDs can lead to impaired renal function and fluid retention. Caution should also be exercised when taking Aceclagin in patients taking diuretics and those with an increased risk of hypovolemia. It is necessary to use the minimum effective dose and regular medical monitoring of renal function. Renal adverse events usually resolve after discontinuation of aceclofenac. Aceclagin should be discontinued if changes in liver function persist or worsen, clinical signs or symptoms of liver disease develop, or other manifestations occur (eosinophilia, skin rash). Hepatitis can develop without prodromal symptoms. The use of NSAIDs in patients with hepatic porphyria may trigger an attack. Hypersensitivity and skin reactionsas with other NSAIDs, aceclofenac may cause allergic reactions, including anaphylactic / anaphylactoid reactions, even if 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 very rare after NSAID use. 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 you experience skin rash, damage to the oral mucosa, or other signs of hypersensitivity, you should stop taking Aceclagin. In some cases, chickenpox can cause skin and soft tissue infections.Currently, the role of NSAIDs in worsening the course of these infections cannot be excluded. Therefore, you should avoid taking Aceclagin for chickenpox. Hematological abnormalities Aceclofenac may cause reversible inhibition of platelet aggregation. Respiratory system disorders Caution should be exercised when taking Aceclagin in patients with bronchial asthma (including in the anamnesis), as the use of NSAIDs can provoke the development of sudden bronchospasm in such patients. Elderly patients Caution should be exercised when taking Aceclagin in elderly patients, as they are more likely to experience 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 (for example, general blood tests, liver and kidney function tests). Due to the antiprostaglandin properties of NSAIDs. Caution should be advised for women taking mifepristone, as the combined use with NSAIDs may theoretically reduce the effectiveness of the drug. Clinical significance is unknown. Effects on the ability to drive vehicles and mechanismsit is recommended to refrain from driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, as the drug can cause dizziness and other side effects that may affect these abilities.

Form of production

Modified release film-coated tablets 200 mg.

10 tablets in a PVDC/aluminum foil blister. 1,3 or 10 blisters with instructions for use in a cardboard pack.

Storage conditions

Store at a temperature not exceeding 30 °C.

Keep out of the reach of children.

Shelf

life is 2 years.

Active ingredient

Aceclofenac

Conditions of release from pharmacies

By prescription

Dosage form

Tablets