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

Excipients: cellulose microcrystalline - 82.6 mg, croscarmellose sodium - 8.0 mg, povidone K-30 - 6.4 mg, sodium stearyl fumarate - 3.0 mg; film sheath: [hypromellose 3.6 mg, talc 1.2 mg, titanium dioxide 0.66 mg, macrogol 4000 (polyethylene glycol 4000) 0.54 mg] or [dry film coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] - 6.0 mg.

Description:

Round biconvex tablets covered with a film coat of white or almost white color. On the cross section, the nucleus is white or almost white in color.

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 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.

Pharmacokinetics:

Suction

After oral administration aceclofenac quickly absorbed, its bioavailability is close to 100%. The maximum concentration (Cmax) in the blood plasma is achieved after 1.25-3 hours after ingestion. Eating slows down absorption, but does not affect its extent.

Distribution

Aceclofenac binds to a high degree with blood plasma proteins (> 99.7%). Aceclofenac penetrates into the synovial fluid, where its concentration reaches 60% of its concentration in the blood plasma. The volume of distribution is 30 liters.

Metabolism

It is believed that aceclofenac is metabolized by isoenzyme CYP2C9 with the formation of the metabolite 4-OY-atseklofnaka, whose contribution to the clinical effect of the drug is likely to be minimal. Diclofenac and 4-OH-aceclofenac are among the numerous metabolites of aceclofenac.

Excretion

The mean half-life (T1/2) is 4-4.3 hours. The ground clearance is 5 liters per hour. 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.

Indications:

Coping 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.

Contraindications:

- erosive and ulcerative lesions of the gastrointestinal tract (GIT) 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 IPVP (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 (creatinine clearance <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.

Carefully:

Diseases of the liver, kidney and gastrointestinal tract in the anamnesis, the presence of infection Helicobacter pylori, bronchial asthma, arterial hypertension, decreased circulating blood volume (including immediately after extensive surgical interventions), coronary heart disease, chronic renal, hepatic and cardiac failure, creatinine clearance less than 60 ml / min, peptic ulcer lesions in history, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, old age, prolonged use of NSAIDs, alcoholism, severe physical illnesses,in patients with hemostasis defects, with the risk of developing cardiovascular thrombosis (myocardial infarction, acute disorders of cerebral circulation (ischemic, hemorrhagic stroke)), systemic lupus erythematosus, prolonged use of NSAIDs, administration of glucocorticosteroids, anticoagulants, antiaggregants, serotonin reuptake inhibitors.

Pregnancy and lactation:

Pregnancy

The drug Alental® 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 the Botallov 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 may affect the duration of bleeding due to antiplatelet effect,which can develop even after application of very low doses; the drug can inhibit uterine contractions, resulting in delayed delivery or prolonged labor.

Breast-feeding

The drug Alental® ns should be taken while breastfeeding. Data on the isolation of aceclofenac with human milk are not available; when a radioactive ¹⁴ C-aceclofenac to lactating rats, no appreciable transfer of radioactivity into the milk was observed.

Fertility

NSAIDs can affect fertility and are not recommended for use by women planning a pregnancy.

Dosing and Administration:

Inside. The tablet should be swallowed whole, with enough water.

Usually adults are prescribed 1 tablet but 100 mg 2 times a day (morning and evening).

Side effects:

Classification of the incidence of adverse events (WHO): Very often> 1/10;

Frequently 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.

From the side 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 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 feeling of heat, accompanied by increased sweating), vasculitis.

From the respiratory, thoracic and mediastinal organs: rarely shortness of breath; 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 mucous membrane of the gastrointestinal tract, hemorrhagic diarrhea, hemorrhages mucous membrane of the gastrointestinal tract; very rarely - stomatitis, vomiting of blood, perforation of the intestine, worsening of Crohn's disease and ulcerative colitis, pancreatitis.

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

From the skin and subcutaneous tissue: infrequently - itching, rash, dermatitis, urticaria; rarely - angioedema; 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 - an increase in the concentration of urea and creatinine in the blood plasma; very rarely - nephrotic syndrome, renal failure, interstitial nephritis.

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

Metabolic disorders: very rarely - hyperkalemia, weight gain.

Overdose:

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.

Treatment:

Gastric lavage, administration of activated charcoal, symptomatic therapy. Forced diuresis, hemodialysis are not effective enough.

Interaction:

With the exception of warfarin, studies of drug interactions have not been conducted. Aceclofenac metabolized by isoenzyme CYP2C9; data in vitro 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 from the body through active renal secretion, such as methotrexate and lithium preparations. Aceclofenac almost completely binds to blood plasma albumin and, consequently, there is the possibility of reuptake-type interactions with other drugs that bind to proteins.

Below is the class-specific information for NSAIDs:

Methotrexate: NSAIDs inhibit the tubular secretion of methotrexate; Furthermore, 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 preparations: some NSAIDs inhibit renal clearance of lithium and digoxin, which leads to an increase in the plasma concentration of both substances. Joint use should be avoided if frequent monitoring of lithium and digoxin concentrations is not carried out.

Anticoagulants: NSAIDs inhibit platelet aggregation and damage the mucous membrane of the gastrointestinal tract, which can lead to increased anticoagulant action and increase the risk of gastrointestinal bleeding while taking anticoagulants. Avoid the combined use of aceclofenac and oral anticoagulants coumarin group, ticlonidine and thrombolytics, unless careful monitoring of the patient's condition is performed.

Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) when combined with NSAIDs may increase the risk of gastrointestinal bleeding.

Cyclosporin, tacrolimus: while taking NSAIDs with cyclosporine or tacrolimus should take into account the risk of increased nephrotoxicity due to decreased formation of renal prostacyclin. Therefore, with simultaneous admission, you should carefully monitor the indicators of kidney function.

Other NSAIDs: while concomitant administration of acetylsalicylic acid or other NSAIDs may increase the incidence of side effects, so caution should be exercised.

Glucocorticosteroids: the risk of ulcers or gastrointestinal bleeding increases.

Diuretics: aceclofenac, like other NSAIDs, can inhibit the activity of diuretics, can reduce the diuretic effect of furosemide and bumstanide and the antihypertensive effect of thiazides. Joint reception with potassium-sparing diuretics can lead to an increase in the potassium content in the blood plasma. Aceclofenac did not affect the control of blood pressure when combined with bendrofluazidom, although it is impossible to exclude interactions with other diuretics.

Hypotensive drugs: NSAIDs can also reduce the effect of antihypertensive drugs. Joint administration of angiotensin-converting enzyme (ACE) inhibitors or antagonists receptors of angiotensin II 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 function of the nights, for example, in elderly patients or in dehydration. Therefore, when combined with NSAIDs, care should be taken. Patients should consume the necessary amount of fluid and be under appropriate supervision (monitoring kidney function at the beginning of the joint application 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 some reports of hypoglycemic and hyperglycemic effects of the drug. Thus, when taking aceclofenac, you should correct the dosage of drugs that can cause hypoglycemia.

Zidovudine: With the simultaneous use of IRIS and zidovudine, the risk increases hematological toxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive (HIV-human immunodeficiency virus) patients with hemophilia receiving zidovudine and ibuprofen.

Mithenriston: aceclofenac can be used 8-12 days after the administration of mycophenolate, since NSAIDs reduce the effect of drugs in this group.

Kolestyramine: other drugs, including NSAIDs, should be used at least 1 hour before or 4-6 hours after the administration of colestyramine to reduce its effect on drug absorption.

Special instructions:

Avoid simultaneous administration of Alental® and other NSAIDs. including selective inhibitors of cyclooxygenase-2 (COX-2).

Undesirable effects can be minimized by applying the lowest effective dose and reducing the duration of treatment required to control symptoms.

Effect on the gastrointestinal tract

Bleeding, ulcer, 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.), and without them.

The risk of bleeding, ulceration and perforation of the gastrointestinal tract increased with increasing doses of NSAIDs in patients with peptic ulcer history, especially if it is 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 (for example, 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 diseases of the gastrointestinal tract, including the elderly, should report any unusual symptoms related to the gastrointestinal tract (especially bleeding), including during the initial dose. 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 antiplatelet agents (such as acetylsalicylic acid).

If there is gastrointestinal bleeding or ulcers, treatment with Alental® should be discarded.

Influence on the cardiovascular and central nervous system

Patients with arterial hypotensionand / or congestive heart failure mild to moderate, require appropriate monitoring, since 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 arterial hypertension, chronic heart failure, established ischemic heart disease, peripheral arterial atherosclerosis and / or cerebral circulation disorders should be careful when taking Alental®. Also, before the first appointment, care should be taken for patients with risk factors for the cardiovascular system (eg, 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®. It is necessary to assign a minimum effective dose and regular medical supervision of the function of the nights. Undesirable effects from the kidneys are usually resolved after discontinuation of aceclofenac.

Admission of aceclofenac should be discontinued if changes in liver function indicators persist or worsen,develop clinical signs or symptoms of liver disease or other manifestations occur (eosinophilia, rash). Hepatitis can develop without prodromal symptoms.

The use of NSAIDs in patients with hepatic porphyria can provoke an attack.

Hypersensitiveand 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 be fatal), 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®.

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® with chicken pox.

Hematologic disorders

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 a history or with a current bronchial asthma, since the use of NSAIDs can provoke the development of sudden bronchospasm in such patients.

Elderly patients

Care should be taken when taking the drug in elderly patients, because they often have side effects (especially bleeding and perforation of the gastrointestinal tract) when taking NSAIDs. Complications can lead to death. Also, elderly patients are more likely to suffer from kidney, liver or cardiovascular diseases.

Long-term use

All patients receiving long-term treatment with NSAIDs should be closely monitored (for example, a general blood test, functional hepatic and renal tests).

Effect on the ability to drive transp. cf. and fur:

It should refrain from driving and other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions, as the drug can cause dizziness and other side effects that cangut to influence these abilities.

Form release / dosage:

Tablets, film-coated, 100 mg.

Packaging:

10, 15 or 20 tablets in a contoured cell pack of a polyvinylchloride or polyvinylchloride / polyvinylidene chloride film and aluminum foil.

20, 30 or 60 tablets in a can of high-density polyethylene.

2, 3 or 6 contour cell packs but 10 tablets. 2 or 4 contourcell packs of 15 tablets, 1 or 3 contiguous cell packs but 20 tablets or one can, together with instructions for medical use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002974

Date of registration:24.04.2015 / 28.10.2015

Expiration Date:24.04.2020

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp24.04.2015

Illustrated instructions

Instructions

Alental® (Alental®)