Aertal tablets p/o 100mg №10×6

Name:
Aertal tabl p / captivity. about. 100mg in bl. in pack. No. 10×6
Description:
Round, biconvex, white, film-coated tablets, about 8 mm in diameter. On one side of the tablet engraved “A” text Main active ingredient Aceclofenac Release form Tablets Dosage 100 mg Pharmacological properties Pharmacodynamics Aceclofenac is a non-steroidal agent with anti-inflammatory and analgesic effects. It is believed that the mechanism of action of this drug is based on the inhibition of prostaglandin synthesis Pharmacokinetics Absorption: After oral administration, aceclofenac is rapidly absorbed, its bioavailability is almost 100%. The maximum plasma concentration is reached approximately 1.25 to 3 hours after ingestion. Eating slows down absorption, but does not affect its extent. Distribution: Aceclofenac is highly bound to plasma proteins (>99.7%). Aceclofenac penetrates the synovial fluid, where its concentration reaches approximately 60% of its plasma concentration. The volume of distribution is approximately Excretion: The average elimination half-life is 4-4.3 hours. The clearance is 5 l/h. Approximately two-thirds of the dose taken is excreted in the urine, mainly in the form of conjugated hydroxy metabolites. Only 1% of a single oral dose is excreted unchanged. Aceclofenac is probably metabolized by CYP2C9 to the main metabolite 4-OH-aceclofenac, whose contribution to the clinical effect of the drug is likely to be minimal. Diclofenac and 4-OH-diclofenac have been found among many metabolites. Special populations: There are no differences in the pharmacokinetics of aceclofenac in elderly patients. A slower elimination of aceclofenac was observed in patients with reduced liver function after a single dose of the drug. In a multiple dose study at 100 mg once daily, no differences in pharmacokinetic parameters were observed between participants with mild to moderate liver cirrhosis and healthy volunteers. In patients with mild or moderate renal impairment, there were no clinically significant differences in pharmacokinetic parameters after a single dose. Indications for use In osteoarthritis, rheumatoid arthritis and ankylosing spondylitis and other diseases of the musculoskeletal system, accompanied by pain (for example, humeroscapular periarthritis and other extra-articular manifestations of rheumatism). To relieve pain (such as low back pain, toothache and primary dysmenorrhea). Route of administration and doses Undesirable effects can be minimized by reducing the duration of treatment necessary to control symptoms (see section “Precautions for use”), Aertal film-coated tablets, 100 mg is intended for oral administration; The tablet should be swallowed with at least half a glass of water. Aertal 100 mg film-coated tablets can be taken with meals. Adults: The maximum recommended dose is 200 mg per day, taken in two separate 100 mg doses (one film-coated tablet in the morning and one in the evening). Children: There are no data on the efficacy and safety of taking the drug in children. Elderly: Usually there is no need to reduce the dose; however, the precautions indicated in the Precautions for Use section must be followed. Hepatic insufficiency: The dose of aceclofenac should be reduced in patients with mild or moderate liver disease. The recommended starting dose is 100 mg daily (see Precautions for Use). Renal insufficiency: There is no evidence of the need to reduce the dose of aceclofenac in patients with mild renal impairment, but caution should be exercised when using Aertal film-coated tablets, 100 mg (see section “Precautions for use”). Use during pregnancy and lactation Pregnancy There are no data on the use of aceclofenac during pregnancy. Inhibition of prostaglandin synthesis may adversely affect the course of pregnancy and/or development of the embryo/fetus. Data from epidemiological studies indicate an increased risk of miscarriage, heart disease and gastroschisis after the use of prostaglandin synthesis inhibitors in early pregnancy. The absolute risk of heart disease increases from less than 1% to about 1.5%. The risk increases with increasing dose and duration of treatment. In animals, administration of prostaglandin synthesis inhibitors results in pre- and post-implantation fetal death and embryonic and fetal mortality. In addition, there is an increased incidence of various malformations, including heart disease, in animals receiving prostaglandin synthesis inhibitors during organogenesis. During the first and second trimester of pregnancy, drugs containing aceclofenac are not prescribed unless absolutely necessary. If aceclofenac is being taken by a woman who is planning a pregnancy or is in the first or second trimester of pregnancy, the dose should be as low as possible and the duration of treatment as short as possible. During the third trimester of pregnancy, all inhibitors of prostaglandin synthesis: may affect the fetus, with cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension); can affect the fetus, causing kidney dysfunction, which can lead to kidney failure and oligohydramnios. Mothers and newborns at the end of pregnancy: the drug may affect the duration of bleeding, due to the antiplatelet effect, which can develop even after the use of very low doses; the drug can inhibit uterine contractions, leading to delayed labor or prolonged labor. Thus, the use of aceclofenac is contraindicated in the third trimester of pregnancy (see sections “Contraindications” and “Precautions for use”). Lactation: There is no information on the penetration of aceclofenac into breast milk. However, there was no noticeable penetration of the labeled radioisotope (C14) of aceclofenac into the milk of lactating rats. The decision to continue / stop breastfeeding or the use of aceclofenac is made after assessing the benefits of breastfeeding for the child and the benefits of taking aceclofenac for the mother. The use of aceclofenac should be avoided during pregnancy and lactation, unless the potential benefit to the mother outweighs the possible risks to the fetus. Fertility: The use of Aertal, as well as other cyclooxygenase/prostaglandin synthesis inhibitors, may reduce fertility and is not recommended for women planning children. Women who have difficulty conceiving or are undergoing fertility testing should stop taking Aertal. Precautions Avoid concomitant use of Aertal and other NSAIDs, including selective cyclooxygenase-2 inhibitors. Undesirable effects can be minimized by using the minimum effective dose and reducing the duration of treatment necessary to control symptoms (see section “Method of application and dose” and a description of the risks for the gastrointestinal tract and cardiovascular system below). Influence on the gastrointestinal tract Bleeding, ulceration or perforation of the gastrointestinal tract with a fatal outcome was observed with any NSAID during any period of treatment, both with dangerous symptoms and without them, both with a history of serious pathological conditions of the gastrointestinal tract, 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 who have had an ulcer, especially if it was accompanied by hemorrhage or perforation (see section “Contraindications”), and in elderly patients. These patients should take the lowest effective dose of the drug. They need combination therapy with protective drugs (for example, misoprostol, or proton pump inhibitors), and such therapy is also necessary for patients who take small doses of aspirin or other drugs that adversely affect the state of the gastrointestinal tract (see section “Interaction with other drugs). Patients with gastrointestinal disease, including the elderly, should report any unusual gastrointestinal symptoms (especially bleeding), including when first taking the drug. Particular caution should be observed in patients taking concomitant drugs 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) (see section “Interaction with other drugs). If bleeding or gastrointestinal ulcers occur in patients taking Aertal, treatment should be discontinued. Influence on the cardiovascular and central nervous system For patients with arterial hypertension and / or congestive heart failure of mild or moderate degree, appropriate monitoring and special instructions are necessary, since fluid retention and edema associated with NSAIDs have been reported. Clinical studies and epidemiological data show that the use of some NSAIDs (particularly at high doses and with long-term use) may slightly increase the risk of arterial thrombotic events (eg, myocardial infarction or stroke). There is no reliable data on the absence of this risk when taking aceclofenac. Patients with uncontrolled hypertension, heart failure (NYHA functional class I), congestive heart failure, cardiovascular risk factors (eg, hypertension, hyperlipidemia, diabetes mellitus, and smoking), and a history of cerebral hemorrhage , special care should be taken when taking aceclofenac. Aceclofenac should be taken with caution and under the supervision of a physician in patients with the following conditions, as there is a risk of exacerbation of the disease (see section “Side effect”): – Symptoms indicating the presence of a disease of the gastrointestinal tract, including its upper and lower parts, – History of ulcer, bleeding or perforation of the gastrointestinal tract – Ulcerative colitis, – Crohn’s disease, – Bleeding tendency, SLE (systemic lupus erythematosus), porphyria, and disorders of hematopoiesis and hemostasis. Aceclofenac should be used with caution and under medical supervision in patients with a history of hemorrhagic stroke. Effects on the liver and kidneys Taking NSAIDs can cause a dose-dependent reduction in prostaglandin formation and sudden renal failure. The importance of prostaglandin to ensure renal blood flow should be considered when taking the drug in patients with impaired cardiac, renal or hepatic function, in patients receiving diuretics or in patients after surgery, as well as in elderly patients. Caution should be exercised when taking the drug in patients with mild or moderate hepatic and renal impairment, as well as in patients with other conditions predisposing to fluid retention in the body. In these patients, the use of NSAIDs can lead to impaired renal function and fluid retention. Caution should also be exercised when taking Aertal in patients taking diuretics or in individuals at increased risk of hypovolemia. The minimum effective dose and regular medical monitoring of kidney function are required. Renal events usually resolve after discontinuation of aceclofenac. Aceclofenac should be discontinued if changes in liver function tests persist or worsen, clinical signs or symptoms of liver disease develop, or other manifestations occur (eosinophilia, rash). Hepatitis can develop without prodromal symptoms. The use of NSAIDs in patients with hepatic porphyria may provoke an attack. Hypersensitivity and skin reactions As with other NSAIDs, the drug may 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 observed very rarely after taking NSAIDs (see section “Side Effects”). The highest risk of these reactions in patients is observed at the beginning of taking the drug, and the development of these adverse reactions is observed during the first month of taking the drug. If a skin rash, lesions on the oral mucosa, or other signs of hypersensitivity occur, aceclofenac should be discontinued. In special cases, with chickenpox, complications can occur: serious infections of the skin and soft tissues. At present, the role of NSAIDs in worsening the course of these infections cannot be ruled out. Therefore, you should avoid taking Aertal, film-coated tablets, 100 mg for chicken pox. Hematological disorders Aceclofenac can cause reversible inhibition of platelet aggregation (see section “Interaction with other drugs”). Respiratory system disorders Caution should be exercised when taking the drug in patients with bronchial asthma at present or in history, since taking NSAIDs can provoke the development of sudden bronchospasm in such patients. Elderly Caution should be exercised when taking the drug in elderly patients, tk. they are more likely to experience side effects (especially bleeding and perforation of the gastrointestinal tract) when taking NSAIDs. Complications can lead to death. In addition, older patients are more likely to suffer from diseases of the kidneys, liver or cardiovascular system. Long-term use All patients receiving long-term treatment with non-steroidal anti-inflammatory drugs should be closely monitored (eg complete blood count, liver and kidney function tests). Interactions with other drugs No drug interaction studies have been conducted, with the exception of warfarin. Aceclofenac is metabolized by cytochrome P450 2C9, and 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 sulfafenazole. As with other drugs of the NSAID group, the risk of pharmacokinetic interaction with other drugs that are excreted from the body by active renal secretion, such as methotrexate and lithium preparations, also increases. Aceclofenac is almost completely bound to plasma albumin and, therefore, there is the possibility of displacement-type interactions with other drugs that bind to proteins. Due to the lack of studies on the pharmacokinetic interaction of aceclofenac, the following information is based on data on other NSAIDs: Simultaneous use should be avoided: Methotrexate: NSAIDs inhibit 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 and digoxin: Some NSAIDs inhibit the renal clearance of lithium and digoxin, resulting in increased serum concentrations of both. Co-administration should be avoided unless frequent monitoring of lithium and digoxin concentrations is carried out. Anticoagulants: NSAIDs inhibit platelet aggregation and damage the mucosal lining of the gastrointestinal tract, which can lead to an increase in the effect of anticoagulants and an increased risk of gastrointestinal bleeding in patients taking anticoagulants. The co-administration of aceclofenac and oral anticoagulants of the coumarin group, ticlopidine and thrombolytics should be avoided unless the patient’s condition is closely monitored. Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) when used together with NSAIDs may increase the risk of bleeding from the gastrointestinal tract (see section “Precautions for use”). The following combinations require dose selection and use with caution: Methotrexate: Be aware of the possible interaction of NSAIDs and methotrexate, even at low doses of methotrexate, especially in patients with impaired renal function. When taken simultaneously, kidney function indicators should be monitored. Caution should be exercised if both drugs, NSAIDs and methotrexate, were taken within 24 hours, as the concentration of methotrexate may increase, which will increase the toxicity of this drug. Cyclosporine, tacrolimus: When NSAIDs are taken concomitantly with cyclosporine or tacrolimus, the risk of increased nephrotoxicity due to a decrease in renal prostacyclin formation should be considered. Therefore, while taking it, you should carefully monitor the indicators of kidney function. Other NSAIDs: While taking acetylsalicylic acid or other NSAIDs, the incidence of side effects may increase, so caution should be exercised. Corticosteroids: increased risk of ulcers or bleeding from the gastrointestinal tract (see section “Precautions for use”) 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. Co-administration with potassium-sparing diuretics may lead to an increase in potassium; therefore, it is necessary to regularly monitor the content of potassium in the blood serum. Aceclofenac did not affect blood pressure control when co-administered with bendrofluazid, although interactions with other diuretics cannot be ruled out. Antihypertensive drugs: NSAIDs may also reduce the effect of antihypertensive drugs. Co-administration of 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 be increased in some patients with impaired renal function, such as elderly or dehydrated patients. Therefore, when combined with NSAIDs, caution should be exercised, especially in elderly patients. Patients should consume the required amount of fluid and be under appropriate supervision (monitoring of kidney function at the beginning of joint use and periodically during treatment). Hypoglycemic agents: Clinical studies show that diclofenac can be used in conjunction 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, the doses of drugs that can cause hypoglycemia should be adjusted. Zidovudine: Concomitant use of NSAIDs and zidovudine increases the risk of haematological toxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV (+) patients with hemophilia receiving zidovudine and ibuprofen. Contraindications Aceclofenac is contraindicated in the following cases: Hypersensitivity to the active substance or other excipients listed in the “Composition” section; Patients in whom substances with the same effect (for example, acetylsalicylic acid or other NSAIDs) provoked attacks of asthma, bronchospasm, acute rhinitis or urticaria; or if there is hypersensitivity to these substances; Patients who have had cases of bleeding or perforation of the gastrointestinal tract due to the use of NSAIDs. Patients with acute, recurrent or possible gastric or duodenal ulcer or bleeding history (two or more clear and proven episodes of ulcer or bleeding); Patients with acute bleeding or diseases accompanied by bleeding (hemophilia or bleeding disorders); Heart failure (NYHA functional class II-IV), ischemic heart disease, peripheral arterial disease, or cerebrovascular disease. Severe violations of the liver and kidneys. During pregnancy, especially in the last trimester, except for serious indications for use. In this case, you should use the minimum effective dose (see section “Use during pregnancy and during breastfeeding”). Composition Each tablet contains: Active ingredient: 100 mg of aceclofenac Excipients: Core: glycerol distearate, croscarmellose sodium, povidone, microcrystalline cellulose. Shell: sepifilm 752, white (hydroxypropyl methylcellulose, microcrystalline cellulose, titanium dioxide (E 171), macrogol stearate (type I)). Overdose There is no evidence of an overdose of aceclofenac in humans. Symptoms include headache, nausea, vomiting, epigastric pain, gastrointestinal irritation, gastrointestinal bleeding, rarely diarrhea, confusion, agitation, coma, drowsiness, dizziness, tinnitus, hypotension, respiratory depression, syncope, rarely seizures . In case of severe poisoning, acute renal failure and liver damage are possible. Treatment of poisoning If necessary, symptomatic therapy should be carried out. Within one hour after taking a toxic amount of the drug, activated charcoal should be taken. Alternatively, in adult patients, gastric lavage may be considered within the first hour after a potentially life-threatening dose. Specific interventions such as hemodialysis or hemoperfusion are likely to be ineffective in eliminating NSAIDs due to their high protein binding and extensive metabolism. Good diuresis should be ensured, and kidney and liver function should be carefully monitored. The patient should be observed for at least 4 hours after taking a potentially toxic dose. With the development of frequent or prolonged seizures, intravenous diazepam should be used. Other measures may be necessary depending on the clinical condition of the patient. Treatment of acute NSAID poisoning is mainly supportive and symptomatic therapy. Side effect Gastrointestinal disorders: Most commonly observed side effects are gastrointestinal disorders. Gastric ulcers, perforation or bleeding from the gastrointestinal tract, sometimes fatal, may occur, especially in elderly patients (see section “Precautions for use”). When taking NSAIDs, nausea, vomiting, diarrhea, bloating, constipation, dyspepsia, stomach pain, melena, hematemesis, ulcerative stomatitis, exacerbation of colitis and Crohn’s disease were observed (see section “Precautions for use”). Gastritis was observed less frequently. In connection with the use of NSAIDs, the development of edema, arterial hypertension and heart failure has been reported. Clinical studies and epidemiological data show that some NSAIDs (especially when taken at high doses and long-term use) may slightly increase the risk of arterial thrombotic events (for example, myocardial infarction or stroke) (see section “Precautions for use”). The following table presents adverse events reported from clinical studies and post-marketing surveillance; adverse events are grouped according to Classes of organ systems and frequency of occurrence. Very often (?1/10), often (from?1/100 to <1/10), infrequently (from?1/1000 to <1/100), rarely (from?1/10000 to <1/100) 1,000), very rare (<1/10,000). Organ systems class according to MedDRA (MedDRA) 1/10,000 to <1/1,000) Very rare (<1/10,000) Blood and lymphatic disorders Anemia Bone marrow suppression Granulocytopenia Thrombocytopenia Neutropenia Hemolytic anemia Immune system disorders Anaphylactic reactions (including shock) Hypersensitivity disorders nutrition and metabolism Hyperkalemia Psychiatric disorders Depression Unusual dreams Insomnia Nervous system disorders Dizziness Paresthesia Tremor Drowsiness Headache Dysgeusia (taste perversion) Visual disorders Visual impairment Hearing and labyrinth disorders Vertigo Tinnitus Heart disorders Heart failure Palpitations Vascular disorders Hypertension Worsening of hypertension Skin flushing Hot flushes Vasculitis Respiratory, chest and mediastinal disorders Shortness of breath Bronchospasm Gastrointestinal disorders - intestinal tract Dyspepsia Abdominal pain Nausea Diarrhea Bloating of the intestine Gastritis Constipation Vomiting Ulceration of the oral mucosa Melena Ulceration of the mucosa of the gastrointestinal tract Hemorrhagic diarrhea Hemorrhages in the gastrointestinal tract Stomatitis Hematemesis Bowel perforation Worsening of the course of Crohn's disease and ulcerative colitis Pancreatitis Violations of the side liver and biliary tract Elevated "liver" enzymes Liver damage (including hepatitis) Increased blood alkaline phosphatase Skin and subcutaneous tissue disorders Itching Rash Dermatitis Urticaria Angioedema Purpura Eczema Severe skin and mucosal reactions (including Stevens syndrome) Johnson and toxic epidermal necrolysis) Renal and urinary tract disorders Elevated blood urea and creatinine levels Nephrotic syndrome Renal insufficiency General and injection site disorders Edema Increased fatigue Muscle cramps (in the legs) Effects on laboratory and instrumental studies Weight gain Other class effects observed with NSAIDs: Very rare (<1/10,000): Renal and urinary tract disorders: interstitial nephritis. Skin and subcutaneous tissue disorders: bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rare). Serious skin infections and soft tissue infections have been observed in special cases when taking NSAIDs during chickenpox. See also sections "Precautions for use" and "Interaction with other medicinal products". Storage conditionsStore at a temperature not exceeding 25 °C. Keep out of the reach of children. Buy Aertal tablets p/o 100mg No. 10x6