Active substanceKetorolacKetorolac
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  • Dosage form: & nbspfilm coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substance: ketorolac trometamol 10.00 mg;

    Excipients: cellulose microcrystalline 150.50 mg, starch corn (dried) 56.00 mg, magnesium stearate 1.00 mg, silicon dioxide colloid 2.00 mg.

    The composition of the shell: a universal shell * 8.00 mg.

    *- the composition of the universal shell: hypromellose (65.00%), titanium dioxide (20.00%), macrogol (13.00%), talc (2.00%).

    Description:

    Almost white, round, biconvex tablets, covered with a film membrane.

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

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:

    Ketorolac has 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 the enzyme cyclooxygenases 1 and 2, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of prostaglandins - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture [-]S and [+]R enantiomers, while the analgesic effect is due to [-]S form.

    The drug does not affect opioid receptors, does not depress respiration, does not cause drug dependence, does not have sedative and anxiolytic effects.

    By the strength of the analgesic effect comparable to morphine, it is much superior to other non-steroidal anti-inflammatory drugs.

    After oral administration, the beginning of the analgesic effect is noted after 1 h, respectively, the maximum effect is achieved after 2-3 hours.

    Pharmacokinetics:

    Ingestion ketorolac well absorbed in the gastrointestinal tract - maximum concentration (Cmah) in blood plasma (0.7-1.1 μg / ml) is achieved 40 minutes after taking an empty stomach at a dose of 10 mg.

    The connection with plasma proteins is 99%.

    Bioavailability is 80-100%. The equilibrium concentration (Css) is achieved after 24 hours when administered 4 times a day and is 10 mg after oral administration - 0.39-0.79 μg / ml.

    The volume of distribution is 0.15-0.33 l / kg. In patients with renal insufficiency, the volume of distribution can be increased by a factor of 2 for S-enantiomer and 20% for Renantiomer.

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

    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. Half-life (T1/2) in patients with normal renal function is 2.4-9 hours after oral administration of 10 mg. T1/2 lengthens 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 plasma creatinine concentration of 19-50 mg / l (168-442 μmol / L) T1/2 is 10.3-10.8 hours, with more pronounced renal failure - more than 13.6 hours.

    The total clearance is 10 mg - 0.025 l / h / kg when administered orally; with renal failure with a concentration of creatinine in the blood plasma of 19-50 mg / l with oral administration of 10 mg-0.016 l / h / kg.

    It is not excreted by hemodialysis.

    Indications:

    Pain syndrome of strong and moderate severity: trauma, toothache, pain in the postpartum and postoperative period, oncological diseases, myalgia, arthralgia, neuralgia, sciatica,damage to ligaments, rheumatic diseases.

    Contraindications:

    Hypersensitivity, a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including history), urticaria, rhinitis caused by the use of non-steroidal anti-inflammatory drugs (in the anamnesis); intolerance to drugs of pyrazolone series, hypovolemia (regardless of the cause that caused it), erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, hypocoagulation (including hemophilia), bleeding or a high risk of their development, severe renal failure (creatinine clearance less than 30 ml / min), severe hepatic insufficiency or active liver disease, condition after aortocoronary shunting, confirmed hyperkalemia, pregnancy (III trimester), inflammatory diseases intestine, delivery, lactation, children under 16 years of age (safety and efficacy not established).

    Carefully:

    Bronchial asthma, the presence of factors that increase gastrointestinal toxicity: alcoholism and tobacco smoking; 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 nonsteroidal anti-inflammatory drugs, ischemic heart disease , cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, chronic renal failure (creatinine clearance 30-60 ml / min), ulcer s defeat of the gastrointestinal tract in history, the presence of infection H.pylori, long-term use of non-steroidal anti-inflammatory drugs, severe somatic diseases, simultaneous administration of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors ( including citalopram, fluoxetine, paroxetine, sertraline), elderly age (over 65 years), pregnancy.

    Dosing and Administration:

    Ketorolac is administered orally 30 to 60 minutes after ingestion, once or repeatedly, depending on the severity of the pain syndrome.

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

    Adult patients with a body weight of less than 50 kg or with renal insufficiency are recommended a dose of 10 mg in the first dose and then 10 mg 4 times a day, but not more than 40 mg / day.

    The maximum daily dose is 40 mg.

    If administered orally, the duration of the course should not exceed 5 days.

    Side effects:

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

    From the digestive system: often (especially in elderly patients over 65 years of age who have a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; rarely - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and / or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the feces or melena, vomiting with blood or the type of "coffee dense, "nausea, heartburn and other),Cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

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

    From the sense organs: rarely - Hearing loss, ringing in the ears, visual impairment (including blurred vision).

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

    From the central nervous system: often - headache, dizziness, drowsiness, rarely - Aseptic meningitis (fever, severe headache, convulsions, rigidity of the neck and / or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis, fainting.

    From the side of the cardiovascular system: less often - Increased blood pressure.

    On the part of the organs of hematopoiesis: rarely anemia, eosinophilia, and 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, swelling and / or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

    Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin discoloration, skin rash, urticaria, skin itching, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, wheezing).

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

    Overdose:

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

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

    Interaction:

    Co-administration with paracetamol increases the nephrotoxicity of ketorolac.

    Use with other non-steroidal anti-inflammatory drugs, glucocorticosteroids, ethanol, corticotropin, calcium preparations increases the risk of ulceration of the gastrointestinal mucosa and the development of gastrointestinal bleeding.

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

    Reduces the effect of antihypertensive and diuretic drugs (reduces the synthesis of prostaglandin 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 in the plasma).

    At appointment with other nefrotoksicnymi medical products (including with preparations of gold) the risk of development nefrotoksichnosti raises.

    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 - increased hematotoxicity.

    Special instructions:

    Before prescribing the drug, it is necessary to clarify the question of a previous allergy to a drug or a non-steroidal anti-inflammatory drug (NSAID). Because of the risk of developing allergic reactions, the first dose is administered under close supervision of the doctor.

    Hypovolemia increases the risk of developing nephrotoxic adverse reactions.

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

    It is not recommended to be used as a medicine for premedication, maintenance of anesthesia.

    When combined with other non-steroidal anti-inflammatory drugs, fluid retention, cardiac decompensation, and increased blood pressure may occur. The effect on platelet aggregation stops after 24-48 hours.

    Do not use simultaneously with paracetamol for more than 5 days.

    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 diseases) and an increase in the 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 adverse events, a minimum effective dose should be used with the lowest possible short course of ketorolac.

    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, film-coated, 10 mg.

    Packaging:

    10 tablets in a blister pack.

    For 1, 2 or 10 blisters together with the instructions for use are put in a cardboard pack.

    Storage conditions:

    In a dry, 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 the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001958
    Date of registration:26.12.2012
    The owner of the registration certificate: Simpex Pharma Pvt Ltd. Simpex Pharma Pvt Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspKORAL-MED, CJSCKORAL-MED, CJSC
    Information update date: & nbsp12.11.2013
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