Active substanceKetorolacKetorolac
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  • Dosage form: & nbsppills
    Composition:

    One tablet contains ketorolac trometamol (ketorolac tromethamine) - 10 mg;

    Excipients: lactose monohydrate 85.9 mg, potato starch 20 mg, magnesium stearate 1.4 mg, silicon dioxide colloid (aerosil) 0.7 mg, microcrystalline cellulose 22 mg.

    Description:

    Tablets are almost white or white with a yellowish hue of color, flat cylindrical with a facet.

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

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:

    NSAIDs have a pronounced analgesic effect, it also has an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with a non-selective inhibition of the activity of cyclooxygenase 1 and 2 (COX1 and COX2) catalyzing the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. By the strength of the analgesic effect comparable to morphine, it significantly exceeds other NSAIDs.

    After oral administration, the onset of analgesic action is noted after 1 h,the maximum effect is achieved in 2-3 hours.
    Pharmacokinetics:

    Absorption at intake - fast, bioavailability - 80-100%; The maximum concentration (Cmah) after oral administration of 10 mg - 0.82-1.46 μg / ml, the time to reach the maximum concentration (TCmax) - 10-78 mil; The connection with plasma proteins is 99%,

    Time to reach equilibrium concentration (Css) - 24 h with the appointment of 4 times a day and is - 0,39-0,79 m kg / m l.

    The volume of distribution is 0.15-0.33 l / kg. In patients with renal insufficiency, the volume of distribution of the drug can be increased 2-fold, and the volume of its distribution R- enantiomer - by 20%.

    Penetrates into breast milk: when the mother receives 10 mg of ketorolac Cmah in milk is achieved 2 hours after the first dose and is 7.3 l g / ml, 2 hours after the second dose of ketorolac (using the drug 4 times a day) - 7.9 ng / l.

    More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxycetorolac. It is excreted 91% by the kidneys, 6% by the intestine.

    The half-life (T1 / 2) in patients with normal renal function is an average of 5.3 hours (2.4-9 hours after oral administration of 10 mg).T1 / 2 increases in elderly patients and is shortened in young patients.

    The liver function does not affect T1 / 2. In patients with impaired renal function with a creatinine concentration in the plasma of 19-50 mg / l (168-442 μmol / l) T1 / 2 - 10,3-10,8 h, with more pronounced renal failure - more than 13.6 hours.

    The total ground clearance is 0.025 l / h / kg; in patients with renal insufficiency with a creatinine concentration in the plasma of 19-50 mg / l - 0.016 l / h / kg.

    He is removed by hemodialysis.

    Indications:

    Pain syndrome of strong and moderate severity: trauma, toothache, postoperative pain, oncological diseases, myalgia, arthralgia, neuralgia, sciatica, ligament damage, rheumatic diseases.

    Contraindications:

    Hypersensitivity, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis); intolerance of medicines (LS) pyrazolone series, hypovolemia (regardless of the cause that caused it), erosive and ulcerative lesions of the gastrointestinal tract (GIT) in the acute stage, hypocoagulation (incl.haemorrhage), bleeding or high risk of their development, severe renal failure (CC less than 30 ml / min), severe hepatic insufficiency or active liver disease, condition after aortocoronary shunting, confirmed hyperkalaemia, pregnancy, inflammatory bowel disease, childbirth and breastfeeding , children under 16 years of age (safety and efficacy not established).

    Carefully:

    Bronchial asthma; presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis; postoperative period, chronic heart failure, edematous syndrome, arterial hypertension, impaired renal function (plasma creatinine below 50 mg / l), cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, simultaneous administration with other NSAIDs, coronary heart disease, cerebrovascular diseases , dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, creatinine clearance less than 60 ml / min, peptic ulcer lesions in history, presence of infection N.pylori, long-term use of NSAIDs, severe somatic diseases,simultaneous administration of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), the elderly (over 65 years).

    Dosing and Administration:

    When administered orally to patients aged 16 to 64 years with a body weight exceeding 50 kg, the recommended dose is 20 mg at the first reception, then 10 mg 4 times a day, but not more than 40 mr/ day.

    Adult patients with a body weight of less than 50 kg or with kidney failure - 10 mg in the first dose and then 10 mg 4 times a day.

    The maximum daily dose for oral administration is 40 mg.

    The duration of treatment should not exceed 5 days.

    Side effects:

    Often - more than 3%, less often - 1-3%. rarely - less than 1%.

    From the digestive system: often - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; rarely - decreased appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and / or bleeding - abdominal pain, spasm and burning in the epigastric region,blood in feces or melena, vomiting with blood or the type of "coffee grounds," nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

    From the urinary system: rare - acute renal failure, back pain, hematuria, azotemia, hemolytic uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increase or decrease in urine volume, nephritis, edema of renal genesis.

    From the sense organs: rarely: hearing loss, ringing in the ears, impaired vision (including blurred vision).

    From the respiratory system: rarely - bronchospasm or dyspnoea, rhinitis, pulmonary edema, laryngeal edema (shortness of breath, difficulty breathing)

    From the side of the central nervous system: often - headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, cramps, stiffness in the neck muscles and / or back), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis, fainting.

    From the side of the cardiovascular system: less often - an increase in blood pressure (BP).

    On the part of the organs of hematopoiesis: rarely - anemia, eosinophilia, leukopenia.

    From the side of the hemostasis system: rarely bleeding from a postoperative wound, epistaxis, rectal bleeding.

    From the skin: less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with chills or without, hyperemia, densification or flaking of the skin, enlargement and / or soreness of palatine tonsils), urticaria, malignant exudative erythema (Stevens- Johnson), toxic epidermal necrolysis (Lyell's syndrome).

    Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin discoloration, skin rash, hives, skin itch, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, heaviness in thoracic cell, wheezing).

    Other: often - swelling (face, legs, ankles, fingers, feet, weight gain); less often - increased sweating, rarely - swelling of the tongue, fever.

    Overdose:

    Symptoms: abdominal pain, nausea, vomiting, erosive-ulcerative gastrointestinal lesion, impaired renal function, metabolic acidosis.

    Treatment: symptomatic (maintenance of vital body functions). Dialysis is ineffective.

    Interaction:

    Co-administration with paracetamol increases the nephrotoxicity of ketorolac.

    Admission with other NSAIDs, glucocorticosteroids, ethanol, corticotropin, calcium preparations increases the risk of ulceration of the gastrointestinal mucosa and the development of gastrointestinal bleeding.

    Simultaneous administration with anticoagulant drugs - coumarin and indanedione derivatives, heparin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet drugs, cephalosporins, valproic acid and acetylsalicylic acid (ASA) increases the risk of bleeding.

    Reduces the effect of antihypertensive and diuretic drugs (reduces the synthesis of prostaglandins in the kidneys).

    The appointment together with methotrexate increases hepato- and nephrotoxicity (their joint appointment is possible only with the use of low doses of the latter and control of its concentration at plasma).

    When appointing with other nephrotoxic drugs (including with drugs of gold), the risk of developing nephrotoxicity increases.

    Drugs that block tubular secretion, reduce the clearance of ketorolac and increase its concentration in the plasma.

    Increases the effect of narcotic analgesics.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    Before prescribing the drug, it is necessary to clarify the question of the previous allergy to the drug or NSAIDs.

    Hypovolemia increases the risk of developing nephrotoxic adverse reactions.

    If necessary, you can prescribe in combination with narcotic analgesics.

    It is not recommended to use as medicines for premedication, maintenance of anesthesia.

    When co-administered with other NSAIDs, fluid retention, cardiac decompensation, increased blood pressure may occur, the effect on platelet aggregation stops after 24-48 hours.

    Patients with blood clotting disorder are appointed only with a constant control of the number of platelets, it is especially important for postoperative patients requiring careful control of hemostasis.

    The risk of developing drug complications increases with prolonged treatment (in patients with chronic and pain) and increased oral dose of the drug more than 40 mg / day.

    To reduce the risk of NSAID-gastropathy, antacid medicines are prescribed, misoprostol, omeprazole.

    To reduce the risk of developing undesirable phenomena from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

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

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:

    Tablets of 10 mg.

    Packaging:

    10 tablets in a blister pack.

    2 blisters with instructions for use in a pack of cardboard.

    Storage conditions:

    Store in a 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 the product after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014251 / 01
    Date of registration:14.08.2008 / 12.02.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:LEKHIM-KHARKOV, CJSC LEKHIM-KHARKOV, CJSC Ukraine
    Manufacturer: & nbsp
    Representation: & nbspAlfa Grand TD, LLCAlfa Grand TD, LLCRussia
    Information update date: & nbsp07.01.2018
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