Composition, form of production and packaging
The tablets covered with a film membrane of white or almost white color, round, biconcave; the core is white or almost white in cross section.
aceclofenac 100 mg
Excipients: cellulose microcrystalline - 82.6 mg, croscarmellose sodium - 8 mg, povidone K-30 - 6.4 mg, sodium stearyl fumarate - 3 mg.
Composition of the film coat: hypromellose - 3.6 mg, talc - 1.2 mg, titanium dioxide - 0.66 mg, macrogol 4000 - 0.54 mg or: dry film-coating mixture - 6 mg, including hypromellose (60%), talc (20 %), titanium dioxide (11%), macrogol 4000 (9%).
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (6) - packs cardboard.
15 pcs. - packings cellular planimetric (2) - packs cardboard.
15 pcs. - packings cellular planimetric (4) - packs cardboard.
20 pcs. - packings of cellular contour (1) - packs cardboard.
20 pcs. - packings cellular planimetric (3) - packs cardboard.
20 pcs. - polyethylene cans (1) - packs of cardboard.
30 pcs. - polyethylene cans (1) - packs of cardboard.
60 pcs. - polyethylene cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
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.
After ingestion, aceclofenac is rapidly absorbed, its bioavailability is close to 100%. With MAX in the blood plasma is achieved through 1.25-3 hours after ingestion.Eating slows down absorption, but does not affect its extent.
Aceclofenac binds highly to plasma proteins (> 99.7%). Aceclofenac penetrates into the synovial fluid, where its concentration reaches 60% of its concentration in the blood plasma. V d is 30 liters.
It is believed that aceclofenac is metabolized by the isoenzyme CYP2C9 to form a metabolite of 4-OH-aceclofenac, whose contribution to the clinical effect of the drug is most likely minimal. Diclofenac and 4-OH-aceclofenac are among the numerous metabolites of aceclofenac.
The average T 1/2 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.
- relief of inflammation and pain syndrome with lumbago, toothache, humeroscapular periarthritis, rheumatic soft tissue damage;
- symptomatic treatment of rheumatoid arthritis, osteoarthritis, 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.
Inside. The tablet should be swallowed whole, with enough water.
Usually adults are prescribed 1 tab. 100 mg 2 times / day (morning and evening).
Classification of the incidence of adverse events (WHO): 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, including individual messages.
On the part of the blood and lymphatic system: rarely - anemia; very rarely - oppression of bone marrow, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia.
From the immune system: rarely - anaphylactic reactions, including shock, hypersensitivity.
Disorders from 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 the labyrinth: very rarely - vertigo, noise in the ears.
From the cardiovascular system: rarely - heart failure, increased blood pressure; very rarely - tachycardia, skin hyperemia, "hot flashes" (short-term fever, accompanied by increased sweating), vasculitis.
From the respiratory, thoracic and mediastinal organs: rarely - shortness of breath; very rarely - bronchospasm.
From the digestive tract: often - dyspepsia, abdominal pain, nausea, diarrhea; infrequently - 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 gastrointestinal mucosa; very rarely - stomatitis, vomiting of blood, perforation of the intestine, worsening of Crohn's disease and ulcerative colitis, pancreatitis.
From the liver and biliary tract: often - increased activity of "liver" enzymes; very rarely - damage to the liver (including hepatitis), increased activity of AP.
From the skin and subcutaneous tissue: infrequently - itching, rash, dermatitis, urticaria; rarely - angiopoietic edema; 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.
From the side of the kidneys and urinary tract: infrequently - increased concentrations of urea and creatinine in the blood plasma; very rarely - nephrotic syndrome, renal failure, interstitial nephritis.
Systemic disturbances: very rarely - increased fatigue, spasms of the muscles of the lower extremities.
Metabolic disorders: very rarely - hyperkalemia, weight gain.
- 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;
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);
- hypersensitivity to aceclofenac or drug components;
severe hepatic insufficiency or active liver disease;
- disorders of hematopoiesis and coagulation;
- severe renal failure (CK <30 ml / min), progressive kidney disease, confirmed hyperkalemia;
- severe heart failure;
- period after aorto-coronary bypass surgery;
- Pregnancy and the period of breastfeeding;
- age to 18 years.
Diseases of the liver, kidney and gastrointestinal tract in history, the presence of Helicobacter pylori infection, bronchial asthma, arterial hypertension, a decrease in the volume of circulating blood (including immediately after extensive surgery), IHD, chronic renal, hepatic and cardiac failure, CC less than 60 ml / min, history of gastrointestinal lesions, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, old age, long-term use of NSAIDs, alcoholism, severe somatic disease (myocardial infarction, acute disorders of cerebral circulation (ischemic, hemorrhagic stroke)), systemic lupus erythematosus, long-term use of NSAIDs, administration of glucocorticosteroids, anticoagulants, antiaggregants, serotonin reuptake inhibitors, in patients with hemostasis defects, with a risk of developing cardiovascular thrombosis .
PREGNANCY AND LACTATION
The drug Alental В® 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, possessing cardiopulmonary toxicity, can cause premature closure of Botall's 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 affect the duration of bleeding due to the antiaggregate effect, which can develop even after applying very low doses; the drug can inhibit uterine contractions, resulting in delayed delivery or prolonged labor.
The drug Alenthal В® should not be taken while breastfeeding. Data on the isolation of aceclofenac with human milk are not available; when administration of radioactive 14 C-aceclofenac and lactating rats, no appreciable transfer of radioactivity into milk was observed.
NSAIDs can affect fertility and are not recommended for use by women planning a pregnancy.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution apply the drug to patients with chronic renal failure.
The use of the drug for patients with severe renal failure (CK <30 ml / min), with progressive kidney disease is contraindicated.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution apply the drug to patients with chronic liver failure.
The use of the drug in patients with severe hepatic insufficiency, with active liver disease is contraindicated.
APPLICATION FOR CHILDREN
The use of the drug for children and adolescents under the age of 18 is contraindicated.
APPLICATION IN ELDERLY PATIENTS
Use precautions with caution in elderly patients.
Avoid simultaneous administration of Alental В® and other NSAIDs. including selective inhibitors of COX-2.
Undesirable effects can be minimized by applying the minimum effective dose and reducing the duration of treatment needed to control symptoms.
Effect on the digestive tract
Bleeding, ulceration or perforation of the gastrointestinal tract with a lethal outcome were observed with the administration of any NSAIDs at any period of treatment, as in the presence of the corresponding symptoms and the presence of serious gastrointestinal diseases in the anamnesis (peptic ulcer of the stomach and duodenum, Crohn's disease, ulcerative colitis, etc.), both 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, 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. They need combination therapy with protective agents (eg, misoprostol or proton pump inhibitors). Such treatment is necessary for patients who take small doses of acetylsalicylic acid or other drugs that adversely affect the condition of the digestive tract.
Patients with gastrointestinal diseases, incl. elderly, should report any unusual symptoms associated with the gastrointestinal tract (especially bleeding), incl. when the drug is taken first. Particular care should be taken in patients who are taking drugs simultaneously, which may increase the risk of bleeding or ulcers, such as systemic glucocorticosteroids, anticoagulants (such as warfarin), selective serotonin reuptake inhibitors, or antiaggregants (such as acetylsalicylic acid).
If there is gastrointestinal bleeding or ulcers, treatment with Alenthal В® should be discontinued.
Effects on the cardiovascular and central nervous system
Patients with arterial hypertension and / or congestive heart failure of mild or moderate degree need appropriate monitoring, because the administration of NSAIDs (in particular in high doses for prolonged use) may not significantly increase the risk of arterial thrombosis (eg, myocardial infarction or stroke). There is no reliable data on the absence of this risk when taking aceclofenac. Patients with uncontrolled hypertension, chronic heart failure, established ischemic heart disease, atherosclerosis of peripheral arteries and / or cerebral circulation disorders should be careful when taking Alental В® . Also, care should be taken before patients with risk factors for the cardiovascular system (for example, hypertension, hyperlipidemia, diabetes, 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 the maintenance of 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 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 Alental В® . It is necessary to appoint a minimum effective dose and regular medical monitoring of kidney function. Undesirable effects from the nights 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, were very rare after NSAID administration. The highest risk of these reactions occurs during the first month of taking the drug. In case of skin rash, damage to the oral mucosa or other signs of hypersensitivity, stop taking Alental В® .
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, you should avoid taking Alental В® with chicken pox.
Aceclofenac can cause reversible inhibition of platelet aggregation.
Disturbance from the respiratory system
Care should be taken when taking the drug to patients with bronchial asthma in an anamnesis or with a current bronchial asthma, tk. the use of NSAIDs can provoke the development of sudden bronchospasm in such patients.
Caution should be exercised when taking the drug in elderly patients. they are more likely to have side effects (especially bleeding and perforation of the digestive tract) when taking NSAIDs. Complications can lead to death. Also, elderly patients are more likely to suffer from kidney, liver or cardiovascular diseases.
All patients receiving long-term treatment with NSAIDs should be closely monitored (for example, a general blood test, functional hepatic and renal tests).
Impact on the ability to manage vehicles and mechanisms
It is necessary to refrain from driving vehicles and practicing other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions, the drug may cause dizziness and other side effects that may affect these abilities.
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.
Gastric lavage, administration of activated charcoal, symptomatic therapy. Forced diuresis, hemodialysis are not effective enough.
With the exception of warfarin, studies of drug interactions have not been conducted. Aceclofenac is metabolized by the CYP2C9 isoenzyme; In vitro data 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 NSAIDs, there is an increased risk of pharmacokinetic interaction with other drugs that are excreted by the active kidney secretion, such as methotrexate and lithium preparations. Aceclofenac almost completely binds to blood plasma albumin and, consequently, there is the possibility of interactions by the type of displacement 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: some NSAIDs inhibit renal clearance of lithium and digoxin, which leads to an increase in the plasma concentration of both substances.Combined use should be avoided, if not carried out frequent monitoring of the concentration of lithium and digoxin.
Anticoagulants: NSAIDs inhibit platelet aggregation and damage the mucous membrane of the gastrointestinal tract, which can lead to increased action of anticoagulants and increase the risk of gastrointestinal bleeding in patients receiving anticoagulants. Combined use should be avoided aceclofenac and peroraliyh coumarin anticoagulants group ticlopidine and thrombolytics, if not carried out careful monitoring of the patient.
Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) or combined with NSAIDs may increase the risk of gastrointestinal bleeding.
Cyclosporin, tacrolimus:while taking NSAIDs with cyclosporine or tacrolimus should consider the risk of increased nefrotokeichnosti because of declining renal prostacyclin formation. Therefore, while taking should carefully monitor renal function.
Other NSAIDs: while taking aspirin or other NSAIDs may increase the incidence of side effects, so caution.
Steroids: increased risk of ulcers and gastrointestinal bleeding.
diuretics:aceclofenac, like other NSAIDs, may inhibit the activity of diuretics, may reduce the diuretic effect of furosemide and bumetanide and antihypertensive effect of thiazide. Co-administration with potassium-sparing diuretics may lead to an increase in the potassium content in the blood plasma. Aceclofenac did not affect blood pressure control when combined with bendrofluazidom, although we can not exclude cooperation with other diuretics.
Antihypertensive drugs:NSAIDs may also reduce the effect of antihypertensive drugs. Joint ACE antagonists or angiotensin II receptor inhibitors 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 elderly patients or dehydration. Therefore, caution should be exercised when used together with NSAIDs. Patients should consume the necessary amount of fluid and under appropriate supervision (monitoring of renal function at the beginning of a joint application and periodically during treatment).
Hypoglycemic agents:Clinical studies show that diclofenac may be used in conjunction with oral hypoglycemic agents without influencing their clinical effect. However, there are isolated reports of hypoglycaemic and hyperglycaemic effects of the drug. Thus, upon receipt of aceclofenac should conduct correction doses of drugs that can cause hypoglycemia.
Zidovudine: while receiving NSAIDs and zidovudine increases the risk of hematologic toxicity. There is evidence of an increase in the risk of hemarthrosis and hematoma in HIV-positive (HIV - human immunodeficiency virus) patients with hemophilia receiving zidovudine and ibuprofen.
mifepristone:aceclofenac could be used 8-12 days after mifepristone. because NSAIDs reduce the effect of the drugs in this group.
Cholestyramine: other drugs, including and NSAIDs, should be applied at least 1 hour before or 4-6 hours after administration of cholestyramine to reduce its effect on the absorption of drugs.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a place protected from light and inaccessible to children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
Do not use after expiry date.