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Dosage form: & nbspfilm-coated tablets
Composition:

Each film-coated tablet contains:

Active substance: Amtolmethine guacyl 600 mg.

Excipients: lactose monohydrate 40.1 mg, hypromellose (15 cps) 6.0 mg, lactose monohydrate (Flowlac 100) 120.3 mg, silicon dioxide colloid 1.6 mg, sodium carboxymethyl starch (type-A) 24.0 mg, magnesium stearate 8.0 mg;

film sheath: hypromellose (5cps) 12.5 mg, titanium dioxide 6.25 mg, macrogol 400 1.25 mg.

Description:Capsule pills, covered with a film shell from white to almost white, with a characteristic odor.
Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug
ATX: & nbsp
  • Derivatives of acetic acid
  • Pharmacodynamics:

    Amtolmethine guacyl is a non-steroidal anti-inflammatory drug (NSAID), a nonselective inhibitor of cyclooxygenase (COX). Amtolmethine guacyl is the precursor of tolmetine. Has anti-inflammatory, analgesic, antipyretic, desensitizing effect, has a gastroprotective effect. Suppresses inflammatory factors, reduces platelet aggregation; oppresses COX1 and COX2, disrupts the metabolism of arachidonic acid, reduces the formation of prostaglandins (including in the focus of inflammation), suppresses the exudative and proliferative phases of inflammation.Reduces the permeability of capillaries; stabilizes the lysosomal membranes; inhibits synthesis or inactivates mediators of inflammation (prostaglandins, histamine, bradykinins, cytokines, complement factors). It blocks the interaction of bradykinin with tissue receptors, restores disturbed microcirculation, and reduces pain sensitivity in the inflammatory focus. Affects thalamic centers of pain sensitivity; reduces the concentration of biogenic amines with algogenic properties; increases the threshold of pain sensitivity of the receptor apparatus. Eliminates or reduces the intensity of pain syndrome, reduces morning stiffness and swelling, increases the amount of motion in the affected joints after 4 days of treatment.

    Protective action amtolmethine guacyl on the gastric mucosa is realized by stimulating capsaicin receptors (also called vanilloid receptors) present in the walls of the gastrointestinal tract. Due to the fact that amtolmethine guacyl there is a vanillin group, it can stimulate capsaicin receptors, which in turn causes the release of the peptide encoded by the calcitonin gene (PCHA) and the subsequent increase in the production of nitric oxide (NO).Both of these actions create a counterbalance to the negative effect caused by a decrease in the amount of prostaglandins due to inhibition of COX. Amtolmethine guacyl well tolerated by patients with prolonged use (within 6 months).

    Pharmacokinetics:

    Suction amtolmethine guacyl after oral administration is rapid and complete. Basically, the drug is concentrated in the walls of the stomach and intestines, where a very high concentration is maintained for 2 hours after ingestion. After suction amtolmethine guacyl immediately undergoes hydrolysis by plasma esterases with the formation of three metabolites: MED5, tolmetine and guiacaul, which are transformed to the active metabolite of tolmetine, which penetrates into tissues, providing a pharmacological action. The main way of metabolism of tolmetin is the oxidation of the methyl group in the benzene ring to the carboxyl ring. The time to reach the maximum concentration (TСmах) after ingestion - 20-60 minutes.

    The connection with plasma proteins is 99%. The half-life (T1/2) in adults - about 5 hours. Within 24 hours the drug is almost completely removed from the body in the form of glucuronides (with urine - 80%, with bile - 20%).

    Indications:

    Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, articular syndrome with exacerbation of gout, bursitis, tendovaginitis.

    Pain syndrome (weak and moderate intensity): arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea; pain with injuries, burns. It is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

    Contraindications:Hypersensitivity to amtolmethine, tolmetin; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses, and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis); erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding; cerebrovascular or other bleeding; inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation; hemophilia and other bleeding disorders; Decompensated heart failure; hepatic insufficiency or active liver disease; expressed renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease,confirmed hyperkalemia; period after aorto-coronary bypass surgery; arterial hypertension; congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption; deficiency of glucose-6-phosphate dehydrogenase; pregnancy, lactation, children under 18 years of age.
    Carefully:Hyperbilirubinemia, chronic heart failure, ischemic heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, chronic renal failure (creatinine clearance 30-60 ml / min), ulcerative lesions of the gastrointestinal tract in history, H. pylori, long-term use of NSAIDs, alcoholism, severe somatic diseases, advanced age, simultaneous administration of oral glucocorticosteroids (including prednisolone a), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:Recommended dose amtolmethine guacyl is 600 mg twice a day. Depending on the degree of control of the symptoms of the disease, the maintenance dose can be reduced to 600 mg once a day. The maximum daily dose is 1800 mg. To maintain the gastroprotective effect of the drug, amtolmethine guacyl should be taken on an empty stomach.
    Side effects:

    The frequency of side effects is classified depending on the frequency of occurrence of cases: often - (1-10%), rare (0.1-1%), rare (0.01-0.1%), very rarely (less than 0.01% ), including individual messages.

    From the digestive system: often - nausea; infrequently - dyspepsia, discomfort in the stomach and intestines, bloating; rare - abdominal pain, diarrhea, vomiting, constipation, gastritis, rarely - peptic ulcer, liver function abnormalities.

    From the urinary system: increased urea nitrogen in the blood, urinary tract infection

    From the sense organs: rarely - noise in the ears, visual disturbances.

    From the respiratory system: rarely - bronchospasm, dyspnea, rhinitis, laryngeal edema. From the central nervous system: often - dizziness, headache drowsiness; rarely - depression.

    From the cardiovascular system: often - a rise in blood pressure.

    From the hematopoiesis: rarely - anemia, thrombocytopenia, agranulocytosis, leukopenia.

    From the skin: infrequent skin rash (including maculopapular rash), purpura, rarely exfoliative dermatitis (fever with chills or without, redness, densification or flaking of the skin, swelling and / or tenderness of the tonsils), hives, Stevens-Johnson syndrome, Lyell's syndrome.

    Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin color change of the face, skin rash, hives, skin itch, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, chest pain, wheezing).

    Other: often - weakness; rarely - swelling (face, legs, ankles, fingers, feet, weight gain); rarely - excessive sweating, fever, lymphadenopathy; very rarely - swelling of the tongue.

    Overdose:

    Symptoms: abdominal pain, nausea, vomiting, erosive-ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis.

    Treatment: gastric lavage, administration of adsorbents (Activated carbon) and the conduct of symptomatic therapy (maintenance of vital body functions). There is no specific antidote.

    Interaction:

    Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

    Reduces the effectiveness of uricosuric, hypotensive drugs and diuretics.

    Strengthens the hypoglycemic effect of derivatives of sulfonylurea, the effect of anticoagulants, antiaggregants, fibrinolytic agents, side effects of estrogens, glucocorticosteroids and mineral corticoids. Antacids and colestramine reduce absorption. Increases the concentration in the blood of lithium preparations, methotrexate. In some patients with impaired renal function, co-administration of NSAIDs and angiotensin-converting enzyme (ACE) inhibitors may lead to further impairment of kidney function.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.Treatment should be discontinued 48 hours before the determination of 17-ketosteroids.
    Effect on the ability to drive transp. cf. and fur:During treatment, one should refrain from engaging in potentially dangerous activities that require increased attention and speed of mental and motor reactions.
    Form release / dosage:Film-coated tablets, 600 mg.
    Packaging:For 10 tablets in a blister of opaque PVC / PVDH film / aluminum foil. 2 blisters together with instructions for use in a pack of cardboard.
    Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children!
    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001588
    Date of registration:15.03.2012 / 05.07.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India
    Information update date: & nbsp28.05.2018
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