Active substanceAcetecacinAcetecacin
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  • Rantudil retard
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  • Rantudil Forte
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  • Dosage form: & nbspmodified release capsules
    Composition:

    1 capsule contains:

    active substance:

    acetemethacin 90.0 mg [in powder 30.0 mg, in granulate 60.0 mg]

    Excipients:

    powder - lactose monohydrate 63.0 mg; talcum 3, 5 mg; magnesium stearate 2.8 mg; silicon dioxide colloid 0.7 mg;

    granulate - cellulose 16.5 mg; crospovidone 8.0 mg; magnesium stearate 1.0 mg; povidone 15.0 mg; talc 0.75 mg; titanium dioxide 77.0 mg; triacetin 3.75 mg;

    Capsule body - gelatin 44.406 mg; sodium lauryl sulfate 0.091 mg; ferric oxide yellow oxide 0.083 mg; titanium dioxide 0.462 mg;

    cap capsule - gelatin 30.271 mg; sodium lauryl sulfate 0.061 mg; titanium dioxide 0.308 mg; dye iron oxide yellow 0.040 mg; dye iron oxide brown 0.062 mg; dye iron oxide red 0.216 mg.

    Description:

    Hard gelatin capsules, size 1, with a smooth surface. The color of the capsule cover is brown, the color of the case is light yellow.

    Contents of capsules: powder and granules of light yellow color with a weak greenish tinge.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

       

    M.01.A.B.11   Acetecacin

    Pharmacodynamics:

    Acetecacin is a derivative of indolylacetic acid. Its pharmacological effect is partly due to the effect of indomethacin, the metabolite product of acetemethacin.

    Acetetacin is an anti-inflammatory, analgesic and antipyretic agent and, like other anti-inflammatory drugs, suppresses platelet aggregation.

    The anti-inflammatory effect of acetemethacin has been demonstrated in animal experiments on a large number of models of inflammation. Acetecacin acts at various stages of the inflammatory process. It was found that it inhibits the synthesis of prostaglandins and the release of histamine, and also acts as a bradykinin and serotonin antagonist. It also inhibits the activity of the complement system and the release of hyaluronidase.

    The membrane-stabilizing property of acetemethacin prevents the release of proteolytic enzymes, leading to suppression of exudative and proliferative inflammatory processes.

    Pharmacokinetics:

    Suction:

    After ingestion acetemethacin absorbed quickly and completely.

    Metabolism:

    After taking one dose and after re-taking the drug RANTUDIL RETARD, acetemethacin and indomethacin, which is formed by the metabolism of acetemethacin, are present in the blood in a ratio of 1: 1. There is no evidence of induction of enzymes that destroy acetemethacin.

    Distribution:

    Acetetacin accumulates in the area of ​​inflammation.

    It was found that after six days of treatment with acetemethacin (2 x 90 mg per day) or indometacin (3 x 50 mg per day) six hours after the last intake, the concentrations of the active substance were significantly higher in the synovial fluid, synovial membrane and in the muscles (a also in bone tissue after treatment with acetemethacin), compared to the concentrations found in the blood. In all studied tissues, except synovial fluid and adipose tissue, after receiving acetemethacin concentrations were higher than after taking indomethacin.

    Excretion:

    Acetetacin is excreted by the kidneys and with bile. 40% of the ingested drug is excreted through the kidneys, the remainder is excreted by the intestine. Acetecacin is excreted by the kidneys partially in unmodified form, partly in the form of acetylcin, conjugated with glucuronic acid, in the form of metabolite indomethacin (free and conjugated),esterolysis formed during and after ester cleavage (in metoksilnoy group at position 5) and deacylation (decomp hlorobenzoilnoy p-group) in the form of pharmacologically active compounds,

    Protein binding and elimination half-life:

    Acetetacin binds to plasma proteins. The half-life is approximately 4.5 hours.

    Concentrations in the blood:

    When using the drug with controlled release, the maximum concentration in the blood is reached much later (p <0.05) than when using other forms; concentration in the blood is also significantly lower (p <0.01) two hours after ingestion. However, at 6 and 10 hours, plasma-controlled concentrations of acetemethacin are significantly higher than those of other acetcemetin formulations.

    Indications:

    Pain and impaired motor activity resulting from the following diseases:

    - chronic rheumatoid arthritis (chronic polyarthritis), rheumatoid arthritis;

    - acute pain associated with degenerative joint disease, in particular the large joints and spine (arthrosis, spondylarthritis);

    - Bechterew's disease (rheumatoid spondylitis);

    - bouts of gout;

    - inflammation of the joints, muscles and tendons, tendosynovitis, bursitis;

    - lumbago, ischialgia;

    - inflammation of superficial veins (thrombophlebitis) and vasculitis.

    - psoriatic arthritis;

    - inflammation and swelling after surgery and trauma.

    Contraindications:

    - hypersensitivity to the active substance - acetemethacin or indomethacin;

    - violation of hematopoiesis of unknown etiology;

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in history);

    - cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;

    - any active liver disease, marked renal failure (CC less than 30 ml / min);

    - confirmed hyperkalemia;

    - erosive and ulcerative changes in the gastric mucosa and duodenum;

    - Acute or recurrent peptic ulcer in history / bleeding (two or more manifest episodes of ulcerative lesion or bleeding);

    - cardiovascular insufficiency of the III class;

    - period after aortocoronary shunting;

    - In the first and second trimesters of pregnancy, as well as women who are trying to become pregnant, acetemethacin only in case of emergency; the use of acetemethacin in the last trimester of pregnancy and during lactation is contraindicated;

    - children and adolescents (no experience in this category of patients).

    Carefully:

    - in the presence of Crohn's disease, ulcerative colitis or other diseases of the intestine in an anamnesis;

    - with systemic lupus erythematosus (SLE), connective tissue diseases;

    - in the case of hypertension and / or heart failure;

    - in cases of impaired renal or hepatic function;

    - reported cases of hypokalemia in the use of indomethacin, this fact should be taken into account when the recommended intake of potassium-sparing diuretics.

    - in the presence of epilepsy, Parkinson's disease and mental disorders, including in the anamnesis;

    - with hemophilia;

    - in elderly patients;

    - in the case of infections caused by the varicella-zoster virus (chicken pox, shingles) due to the possible increased risk of serious skin complications.

    Pregnancy and lactation:

    Pregnancy:

    In the first and second trimesters of pregnancy should be appointed acetemethacin only in case of emergency. If acetemethacin is used in women who are trying to get pregnant, or in the first and second trimesters of pregnancy, the dose should be so low and the duration of treatment is as short as possible.

    In the third trimester of pregnancy, the use of acetemethacin is contraindicated.

    Lactation:

    The use of the drug is contraindicated, since small amounts of the active substance can enter the breast milk.

    Dosing and Administration:

    Capsules should be swallowed whole, with a sufficient amount of liquid while eating.

    Recommended dose - 1 capsule 1-2 times a day

    Dosage regimen for gout attacks

    The standard recommended dose for the treatment of acute gout attacks, prior to the easing of symptoms, is 180 mg of acetemethacin per day (corresponding to 2 RANTUDIL RETARD capsules).

    The duration of treatment depends on the clinical picture, but therapy in doses exceeding 2 capsules of RANTUDIL RETARD preparation per day should last no more than 7 days.

    Side effects:

    The incidence of side effects is defined as follows (number of patients who showed this reaction):

    Very often:> 1/10;

    Often: <1/10> 1/100;

    Infrequently: <1/100> 1/1000;

    Rarely: <1/1000> 1/10000;

    Very rarely: <1/10000.

    From the gastrointestinal tract:

    Very often: indigestion: nausea, vomiting, flatulence, abdominal pain, loss of appetite.

    Often: ulcerative lesions in the gastrointestinal tract (GIT), sometimes accompanied by bleeding and perforation.

    Infrequent: presence of blood in vomit, feces or with diarrhea.

    Very rarely: stomatitis, inflammation of the tongue, lesion of the esophagus, exacerbation of Crohn's disease or ulcerative colitis, constipation, pancreatitis.

    From the nervous system:

    Often: disorders of the central nervous system, including headache, lethargy / fatigue, dizziness, drowsiness.

    Very rarely: muscular asthenia, hyperhidrosis, dysgeusia, memory disorders, sleep disorders, convulsions.

    From the cardiovascular system:

    Very rarely: increased heart rate, angina pectoris, heart failure, hypertension.

    From the liver and biliary tract:

    Often: increased levels of liver enzymes.

    Infrequent: liver damage (toxic hepatitis with or without jaundice, very rarely: lightning and sometimes without previous symptoms).

    From the side of the circulatory system:

    Very rarely: anemia caused by the loss of latent blood from the digestive tract, hemolytic anemia, pancytopenia (anemia, including aplastic anemia, leukopenia, agranulocytosis, thrombocytopenia). Initial symptoms may include fever, sore throat, superficial lesions in the oral cavity, flu-like conditions, severe fatigue, nosebleeds and subcutaneous bleeding.

    In these cases, you must immediately stop taking the drug and see a doctor. Do not take analgesics and / or antipyretics yourself.

    In the case of prolonged treatment, a blood test should be performed regularly.

    Possible effects on platelet aggregation and increased hemorrhagic diathesis.

    From the immune system:

    Often: reactions of hypersensitivity (rash and itching).

    Infrequently: urticaria.

    Very rarely: severe hypersensitivity reactions: edema of the face or eyelids, swelling of the tongue, angioneurosis, respiratory distress, which can lead to an attack of asthma,lowering of blood pressure.

    Very rarely: allergic vasculitis and pneumonitis.

    From the endocrine system:

    Very rarely: hyperglycemia and glucosuria.

    On the part of the organs of vision:

    Uncommon: retinal pigment degeneration, blurred cornea during long-term use of indomethacin, acemetacin main metabolite.

    From the organs of hearing:

    Very rare: tinnitus and hearing loss

    From the skin and subcutaneous tissue:

    Infrequently: alopecia

    Very rarely, eczema, enanthema, erythema, photosensitivity, exfoliative dermatitis and bullous rashes that may also have severe course, e.g., in the form of Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome).

    From the urinary system:

    Infrequent: the development of edema, in particular, in patients with hypertension and / or impaired renal function.

    Very rare: micturition disorders, increase in urea levels in the blood, acute renal failure, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

    In this regard, the indicators of kidney function of the patient should be regularly monitored.

    Overdose:

    Symptoms:

    Given the mechanism of action of the drug, overdose or misuse can cause central nervous system disorders, including headache, dizziness, confusion, drowsiness, convulsions and loss of consciousness right up to coma. In addition, nausea, vomiting, pain in the epigastric region, sweating, abnormal electrolyte balance, arterial hypertension, ankle edema, oliguria, hematuria, respiratory depression are possible.

    Urgent care:

    With symptoms of overdose or in case of an alleged overdose, it is recommended to carry out symptomatic treatment, including gastric lavage, induction of diuresis while maintaining the water balance, and, if necessary, the use of anti-shock measures.

    Antidote:

    The specific antidote is unknown.

    Interaction:

    The following interactions were described with RANTUDIL RETARD in combination with the following preparations:

    Digoxin, lithium, phenytoin:

    There may be an increase in the concentration of these drugs in the blood plasma. Anticoagulants:

    NSAIDs can enhance the action of anticoagulants, for example Warfarin,so with simultaneous application it is recommended to monitor the coagulation of the patient's blood.

    Corticosteroids:

    Increased risk of ulcerative lesions of the gastrointestinal tract or bleeding.

    PNSAIDs, including salicylates:

    Simultaneous administration of several NSAIDs may increase the risk of gastrointestinal ulceration or bleeding due to a synergistic effect, therefore, simultaneous administration of acetemethacin with other NSAIDs should be avoided.

    Probenecid, sulfinpyrazone:

    They can slow the excretion of acetemethacin.

    Antibiotics of penicillin series

    They can slow the excretion of acetemethacin.

    Diuretics and antihypertensive drugs:

    The hypotensive effect of drugs can be weakened. Furosemide accelerates the excretion of acetemethacin.

    Potassium-sparing diuretics:

    Can increase the level of potassium in the blood (hyperkalemia); it is often necessary to monitor the potassium content.

    Antiaggregants and selective serotonin reuptake inhibitors (SSRIsr Increased risk of gastrointestinal bleeding.

    There have been no reports of interactions between acetemethacin and other active substances that also bind to plasma proteins.

    Antacid:

    May decrease the absorption rate of acetemethacin.

    Special instructions:

    ROTARD RETARD should only be used if there is an opportunity to provide emergency assistance:

    - patients with hypersensitivity reactions (eg, asthma attacks, skin reactions or acute rhinitis) on non-steroidal anti-inflammatory drugs / analgesics;

    - patients suffering from asthma, hay fever, edema of the nasal mucosa or chronic respiratory disease;

    Particular caution is needed when RANTARD RETARD is taken concurrently with other drugs acting on the central nervous system, or alcohol;

    Some patients who took RANTUDIL RETARD had an increase in liver and kidney function;

    With a long course of treatment, a hemogram, blood coagulability monitoring, and ophthalmological examination are recommended.

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

    The use of RANTUDIL RETARD can cause side effects, including effects on the central nervous system, so during treatment should refrain from potentially dangerous activity,requiring a high rate of mental and physical reactions (driving, working with machinery, working at height, etc.).

    Form release / dosage:Capsules with a modified release of 90 mg.
    Packaging:

    10 capsules per blister of PVC / PVDC / aluminum foil.

    2, 5 or 10 blisters in a cardboard box together with instructions for use.

    Storage conditions:

    At a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001552
    Date of registration:01.03.2012
    The owner of the registration certificate:Honey Manufacuring GmbHHoney Manufacuring GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspMEDA Pharmaceuticals Switzerland GmbH MEDA Pharmaceuticals Switzerland GmbH Switzerland
    Information update date: & nbsp01.03.2012
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