Aceclofenac - instructions for use, dose, side effects, contraindications

Active substance: Aceclofenac
Active substance: Aceclofenac	- 100 mg
Excipients:
Kernel composition: Calcium stearate
Kernel composition: Calcium stearate	- 3 mg
Talc	- 9 mg
Silica colloidal dioxide (aerosil)	- 1.5 mg
Microcrystalline cellulose	- 85 mg
Croscarmellose sodium (admixture)	- 10.5 mg
Lactose monohydrate (milk sugar)	- 91 mg
Mass of the core	300 mg
Shell composition: Hypromellose (hydroxypropylmethylcellulose)
	- 6.4 mg
Macrogol 4000 (polyethylene oxide-4000)	- 2.5 mg
Titanium dioxide (titanium dioxide)	1.1 mg
Weight of a tablet	- 310 mg

Description:Round tablets of biconvex form, covered with a film membrane of white or almost white color. On the cross-section - the core is white or almost white.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

M.01.A.B Derivatives of acetic acid

M.01.A.B.16 Aceclofenac

Pharmacodynamics:

Aceclofenac is a derivative of phenylacetic acid, inhibits cyclooxygenase I and II types. Has 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.

Pharmacokinetics:

Aceclofenac is rapidly and completely absorbed after ingestion. The time to reach the maximum concentration is 1.25-3 hours. It penetrates into the synovial fluid, where its concentration reaches 57% of the plasma concentration level and the time to reach the maximum concentration 2-4 hours later than in the plasma. The volume of distribution is 25 liters.

Connectivity c plasma proteins (albumins) - 99 %. Aceclofenac circulates mainly unchanged, its main metabolite is 4'-hydroxyacetylfenac.

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

Indications:

Symptomatic treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis.

Coping of inflammation and pain syndrome with lumbago, toothache, humeroscapular periarthritis, rheumatic soft tissue damage.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Contraindications:

- Erosive-ulcerative lesions of the gastrointestinal tract in the phase of exacerbation, 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 non-steroidal anti-inflammatory(including in the anamnesis);

- hypersensitivity to aceclofenac or drug components;

- period after aortocoronary shunting;

- severe hepatic impairment or active liver disease;

- severe renal failure (creatinine clearance less than 30 ml / .min), progressive kidney disease, hyperkalemia;

- inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation;

- Decompensated heart failure;

- disorders of hematopoiesis and coagulation;

- pregnancy and the period of breastfeeding;

- deficiency of lactose, intolerance of lactose, glucose-galactose malabsorption;

- children's age till 18 years.

Carefully:

Diseases of the liver, kidney and gastrointestinal tract in the anamnesis, bronchial asthma, arterial hypertension, decrease in the volume of circulating blood (including after surgery), coronary heart disease, chronic renal failure of mild and moderate severity (QC from 30 to 60 ml / min), hepatic insufficiency of mild and moderate severity, chronic heart failure, cerebrovascular diseases, dyslipidemia / hyperlipidemia. diabetes mellitus, peripheral arterial disease, smoking, old age, prolonged use of an NSAID in an anamnesis, the presence of an infection Helicobacter pylori, frequent use of alcohol, concomitant therapy with the following drugs:

- anticoagulants (for example, warfarin);

- antiaggregants (eg, acetylsalicylic acid, clopidogrel);

- oral glucocorticosteroids (for example, prednisolone);

- selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

The drug should be taken in a minimally effective dose, for as short a period of time as possible.

Inside. The tablets are swallowed whole, with a sufficient amount of liquid.

The dose of the drug for all indications:

Adults appoint 100 mg twice a day, 1 tablet in the morning, and 1 - in the evening.

The course of treatment is prescribed by a doctor individually.

Liver failure

Patients with hepatic insufficiency of moderate severity 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 insufficiency, but caution is recommended.

Side effects:

The most common adverse reactions in clinical trials were from the gastrointestinal tract (dyspepsia 7.5%, abdominal pain 6.2%, nausea 1.5%, diarrhea 1.5%); sometimes - dizziness. Also, itching, rashes and changes in the activity of "liver" enzymes and the concentration of creatinine were noted.The undesirable effects listed below are presented according to the system-organ classes in accordance with the classification MedDRA with the following frequency: often: ≥1/100 to <1/10; infrequently: ≥1/1000 to <1/100; rarely: ≥1/10000 to <1/1000; very rarely: <1/10000.

Allergic reactions: skin rash, urticaria, eczema, erythroderma, systemic anaphylactoid reactions, bronchial asthma, in some cases vasculitis, pneumonitis, polymorphic exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

From the immune system: rarely an anaphylactic reaction (including shock), giPersensitivity.

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 tract, diarrhea with blood, gastrointestinal bleeding; very rarely - stomatitis, vomiting of blood, gastric ulcer, small intestine perforation, worsening of Crohn's disease and ulcerative colitis, pancreatitis.

From the cardiovascular system: rarely - heart failure, increased arterialabout pressure; very rarely - tachycardia, "hot flashes", vasculitis.

From the liver and bile ducts: often - an increase in the activity of "liver" enzymes; very rarely - liver damage (including hepatitis), increased activity of alkaline phosphatase of blood.

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

Disorders of the psyche: very rarely - depression, atypical dreams, insomnia.

From the skin and subcutaneous tissue: infrequently - itching, rash, dermatitis, urticaria rash; rarely - angioedema; very rarely - purpura, reactions from the skin and mucous membranes, bullous skin reactions.

From the hematopoiesis: thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia, aplastic anemia.

From the side of the blood and lymphatic system: rarely anemia; very rarely - bone marrow depression, granulocytopenia, neutropenia, hemolytic anemia.

From the side of the kidneys and urinary tract: infrequently - increasing the concentration of blood urea, increasing the concentration of the creatinine of the blood; very rarely - interstitial nephritis, nephrotic syndrome, renal failure.

From the respiratory system, chest and mediastinum: rarely shortness of breath; very rarely - bronchospasm.

From the side of the organ of vision: rarely - visual impairment.

From the side of the organ of hearing and labyrinth: very rarely - vertigo, ringing in the ears.

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

Systemic disorders: very rarely - spasms of the muscles of the lower extremities.

Overdose:

Symptoms: dizziness, headache, hyperventilation of the lungs with increased convulsive readiness, nausea, vomiting, abdominal pain.

Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy. There is no specific antidote. Forced diuresis, hemodialysis, blood transfusion are not very effective.

Interaction:

Studies of drug interactions were not conducted, except for warfarin.

Aceclofenac is metabolized by the cytochrome P450 - CYP2C9, and data in vitro indicate that aceclofenac may be an inhibitor of this enzyme. Therefore, there is a risk of pharmacokinetic interaction with phenytoin, cimetidine, tolbutamide, phenylbutazone, amiodarone, miconazole and sulfafenazole.

As with other NSAIDs, there is a risk of pharmacokinetic interaction with drugs that metabolize in the liver, such as methotrexate and lithium preparations.

Aceclofenac almost completely binds to plasma proteins, and, therefore, it is necessary to take into account the possibility of substitution with other drugs, strongly binding to plasma proteins.

In the absence of studies of pharmacokinetic interaction, the following information is based on information obtained by another NSAIDs:

The following combinations should be avoided

NSAIDs suppress the tubular secretion of methotrexate, and metabolic interaction can also occur, leading to a decrease in the clearance of methotrexate. Therefore, during treatment with large doses of methotrexate (more than 20 mg / week), the appointment of an NSAID should always be avoided.

Some NSAIDs inhibit the excretion of lithium by the kidneys, which leads to increased concentrations of lithium in the blood serum. It should not be allowed this a combination if it is impossible to carry out a frequent control of the concentration of lithium in the 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 gastrointestinal mucosa in patients taking anticoagulants.

Avoid the combination of aceclofenac with oral anticoagulants coumarin group, ticlopidine, thrombolytic and heparin in the absence of careful monitoring.

The following combinations may require dose adjustment and adherence to precautions:

It is necessary to take into account the possible interaction of NSAIDs and methotrexate, especially in patients with renal insufficiency. When you take both drugs, you need to monitor kidney function. Precautions should be taken with concurrent administration of NSAIDs and methotrexate within 24 hours, the concentration of methotrexate may increase, leading to increased toxicity of methotrexate. It is assumed that the use of NSAIDs together with cyclosporine or tacrolimus increases the risk of nephrotoxicity due to decreased prostacyclin synthesis in the kidneys. Therefore, while taking drugs, it is important to monitor kidney function.Simultaneous intake of acetylsalicylic acid and other NSAIDs can increase the incidence of adverse reactions, and therefore caution is required when they are taken together.

NSAIDs can reduce the diuretic effect of furosemide, bumetanide and hypotensive effect of thiazide diuretics. Simultaneous treatment with potassium-sparing diuretics can be associated with an increase in potassium concentration in the serum, therefore, a control of the potassium content in the blood is necessary.

NSAIDs can also reduce the effect of certain antihypertensive medications. Angiotensin converting enzyme inhibitors or angiotensin receptor antagonists II in combination with NSAIDs may cause renal failure. The risk of developing acute renal failure, which is usually reversible, may increase in some patients with impaired sleep function, for example in elderly patients or patients experiencing fluid deficiency. Therefore, the combination of such drugs with NSAIDs should be used with caution, patients should receive a sufficient amount of liquid with food, and kidney function should be monitored.

No effect of aceclofenac on blood pressure was detected when it was taken concomitantly with bendroflumethiazide, although interaction with other antihypertensive drugs such as beta-blockers can not be ruled out.

Other possible interactions

Individual cases of hypoglycemia and hyperglycemia have been reported. Therefore, for aceclofenac, it is necessary to adjust the dose of drugs that cause hypoglycemia. When used simultaneously with the drug Aceclofenac;

- digoxin, phenytoin, or lithium preparations - plasma concentrations of these drugs may increase;

- diuretics and antihypertensive drugs - the effect of these medicines may be weakened;

- potassium-sparing diuretics - can lead to the development of hyperglycemia and hyperkalemia;

- other NSAIDs or glucocorticosteroids - increased risk of side effects from the gastrointestinal tract;

- selective serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline) - the risk of developing gastrointestinal bleeding increases;

- cyclosporine - can increase the toxic effect of the latter on the kidneys;

- hypoglycemic means - can cause both hypo- and hyperglycemia. With this combination1It is necessary to control the sugar content in the blood;

- acetylsalicylic acid - the concentration of aceclofenac in the blood decreases;

- antiplatelet agents and anticoagulants - increased risk of bleeding (regular monitoring of blood coagulability);

- zidovudine - the risk of hematological toxicity increases.

Special instructions:The severity of adverse reactions can be corrected by reducing the effective single doses, necessary for the control of symptoms.

Patients with hypertension and / or chronic heart failure I-II functional class for NYMA in the anamnesis the proper control and consultation of the doctor is required, tk. reported fluid retention and swelling in the treatment of NSAIDs. Clinical and epidemiological studies suggest that the use of certain NSAIDs (especially in high doses and long-term administration) may increase the risk of arterial thrombosis (eg, myocardial infarction or stroke). There is insufficient data to exclude such risk for aceclofenac.

Patients with uncontrolled hypertension, congestive heart failure, coronary heart disease, peripheral arterial disease and / or cerebrovascular diseases should take aceclofenac only after a thorough analysis of the clinical situation. With the same caution, you need to make a decision before starting long-term treatment of patients at risk of cardiovascular disease (eg, hypertension, hyperlipidemia, diabetes and smokers).

Aceclofenac should be taken with caution and under close medical supervision to patients with gastrointestinal diseases, a history of peptic ulcer, after acute cerebrovascular accident, systemic lupus erythematosus, porphyria, hematopoiesis disorders and blood coagulation disorders.

Aceclofenac can cause reversible inhibition of platelet aggregation.

Patients with Crohn's disease, ulcerative colitis drug is not recommended. Care should be taken in patients with hepatic, renal, heart failure, as well as patients with other diseases predisposed to developing edema.Admission of NSAIDs in this category of patients can lead to deterioration of renal excretion and the development of edema. Patients taking diuretics, or with an increased risk of developing hypovolemia, also need to exercise caution when taking the drug Aceclofenac.

Care should be taken in elderly patients. they have more side effects. Bleeding from the gastrointestinal tract and / or perforation can be during treatment, especially if there is a history of gastrointestinal disease. In addition, elderly patients are more likely to have impaired liver, kidney, cardiovascular system.

All patients receiving long-term treatment with NSAIDs need monitoring in order to reduce the risk of adverse reactions (eg, general urine analysis, general and biochemical blood tests).

Simultaneous reception of the drug Aceclofenac with any drug that suppresses the synthesis of cyclooxygenase / prostaglandin, can reduce fertility and is not recommended for women planning a pregnancy. Women with infertility in the history should stop taking the drug Aceclofenac.

Effect on the ability to drive transp. cf.and fur:During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:Tablets, film-coated 100 mg.

Packaging:

For 10, 20 tablets are placed in a contour cell box made of a polyvinylchloride film and aluminum foil printed lacquered.

10, 20, 30, 40, 60, 90, 100, 200 tablets are placed in polymer cans. If there is no cork sealant, free space in the jar is filled with cotton absorbent cotton or shock absorber.

Each jar, 1, 2, 3, 4, 6, 9, 10 contour mesh packages together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

AT protected from light at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002871

Date of registration:24.02.2015 / 05.11.2015

Expiration Date:Unlimited

The owner of the registration certificate:VELFARM, LLC VELFARM, LLC Republic of San Marino

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp03.10.2017

Illustrated instructions

Instructions

Aceclofenac (Aceclofenac)