Active substanceKetorolacKetorolac
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  • Dosage form: & nbspcoated tablets
    Composition:

    One tablet contains:

    active substance: ketorolac tromethamine in terms of dry matter - 10 mg;

    Excipientslactose (sugar milk) 118 mg, potato starch (Extra grade) 30 mg, microcrystalline cellulose 40 mg, calcium stearate 2 mg, Opadrai II (series 85) * 6 mg.

    * Composition Opadar II series 85 (G) code 18490 (white): polyvinyl alcoholpartially hydrolyzed 40,000%, talc 20,000%, macrogol 3350 (polyethylene glycol) 12.350%, lecithin (soybean) 3.500%, titanium dioxide, E 171-20.150%.

    Description:

    Round biconvex tablets, coated with a coat, white.

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

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:

    It has a pronounced analgesic effect, has also an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with nonselective inhibition of cyclooxygenase activity (COX1 and COX2), which catalyzes 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 is much superior to other non-steroidal anti-inflammatory drugs.

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

    Pharmacokinetics:

    Absorption at intake - fast, bioavailability - 80-100%; FROMmah after oral administration of 10 mg - 0.82-1.46 μg / ml, TSmah - 10-78 minutes. The connection with plasma proteins is 99%.

    Time to reach Css at parenteral and oral administration - 24 hours at 4 appointment times a day (subtherapeutic above) and after oral administration of 10 mg - 0,39-0,79 g / ml.

    The volume of distribution is 0.15-0.33 l / kg. In patients with renal insufficiency, the volume of ketorolac distribution may increase 2-fold, and the volume of distribution of ketorolac 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 ng / 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.

    T1 / 2 in patients with normal renal function - 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 clearance is 10 mg - 0.025 l / h / kg with oral administration; in patients with renal insufficiency with a creatinine concentration in the 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, dislocations, sprains, rheumatic diseases.

    It is intended for symptomatic therapy, reducing pain and inflammation at the time of application, the progression of the disease is not affected.

    Contraindications:

    Hypersensitivity, 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 anamnesis), urticaria, rhinitis caused by NSAID (history); 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 (CC less than 30 ml / min ), severe hepatic insufficiency or active liver disease, condition after CABG (aorto-coronary bypass), lactose intolerance, lactase deficiency or glucose-galactose malabsorption, confirmed hyperkalemia, inflammatory e) intestinal diseases (including ulcerative colitis, Crohn's disease) in the acute stage; pregnancy (III trimester), childbirth period, lactation period, children under 16 years of age (safety and efficacy not established); dehydration, simultaneous use with probenecid, pentoxifylline,acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants, including warfarin and heparin, preventive analgesia before extensive surgery, intracranial hemorrhage or suspicion of it.

    Carefully:Bronchial asthma, the presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis; postoperative period, CHF (chronic heart failure), edematous syndrome, arterial hypertension, renal failure of moderate severity (KC from 30 to 60 ml / min), cholestasis, active hepatitis, sepsis, SLE (systemic lupus erythematosus), simultaneous reception with others NSAIDs, coronary artery disease (CHD), cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, history of gastrointestinal lesions, infection H.pylori, long-term use of NSAIDs, severe somatic diseases, simultaneous administration of oral GCS (glucocorticosteroids) (including prednisolone), anticoagulants (including warfarin), antiaggregants (incl.clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), elderly age (over 65 years), pregnancy (I-II trimester).
    Pregnancy and lactation:

    It is not recommended to take the drug during pregnancy (adverse effect on the fetal cardiovascular system - premature closure of the arterial duct), during labor, in the early postpartum period (by inhibiting the synthesis of prostaglandins, it can adversely affect the fetal blood circulation and weaken the contractile activity of the uterus that increases the risk of uterine bleeding) and during lactation.

    Penetrates into breast milk: after taking the mother 10 mg ketorolac 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) - is 7.9 ng / l.

    Oral doses of ketorolac tromethamine 1.5 mg / kg (0.14 MPHP) in rats, used after the 17th day of pregnancy, caused hardship and increased mortality of calves.

    Action category for the fetus by FDA - FROM.

    Dosing and Administration:

    Inside.

    Patients from 16 to 64 years with a body weight exceeding 50 kg, single recommended dose is 10 mg; with repeated admission of 10 mg 4 times a day.

    Adult patients with a body weight of less than 50 kg or with kidney failure a single dose may be less. The dosage regimen is set individually depending on the pain syndrome.

    The maximum daily dose is 40 mg.

    The duration of the course is no more than 5 days.

    Side effects:

    From the digestive system: often - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; rare - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including perforation and / or bleeding - abdominal pain, cramping or burning sensation in the epigastric region, blood in the stool or melena, vomiting blood or 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 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 - increased blood pressure.

    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 frequently - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever, chills or without hyperemia, sealing or skin peeling, swelling and / or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens syndrome Johnson), toxic epidermal necrolysis (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 - swelling (face, legs, ankles, fingers, feet, weight gain); less frequent - increased sweating; rarely - swelling of the tongue, fever.

    Overdose:

    Symptoms: abdominal pain, nausea, vomiting, development of peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis.

    Treatment: gastric lavage, administration of adsorbents (Activated carbon) and symptomatic therapy. Ketorolac is not excreted sufficiently by dialysis.

    Interaction:

    Co-administration with paracetamol increases the nephrotoxicity of ketorolac.

    Admission with other non-steroidal anti-inflammatory drugs, glucocorticosteroid agents, ethanol, corticotropin, preparations of Ca2+ increases the risk of ulceration of the mucous membrane of the gastrointestinal tract and the development of gastrointestinal bleeding.Simultaneous appointment with anticoagulant drugs - derivatives of coumarin and indanedione, heparin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet drugs, cephalosporins, valproic acid and acetylsalicylic acid 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 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 issue of previous allergies to the drug or other non-steroidal anti-inflammatory drugs.Because of the risk of developing allergic reactions, the first dose is taken under close medical supervision.

    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 pain) 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.

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

    During the period of treatment, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, since a significant part of patients with the administration of the drug develop side effects from the central nervous system (incl. drowsiness, dizziness, headache).

    Form release / dosage:

    The tablets covered with a cover of 10 mg.

    Packaging:

    For 10 tablets in a planar cell package.

    1, 2, 3, 5 contour mesh applications in a pack of cardboard.

    For hospitals: 200, 500 contour squares, together with an equal number of instructions for use in a box of corrugated cardboard.

    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:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002140
    Date of registration:12.07.2013 / 10.10.2014
    Expiration Date:12.07.2018
    The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus
    Manufacturer: & nbsp
    Representation: & nbspBORISOVSKIY FACTORY OF MEDPREPARATES, OJSCBORISOVSKIY FACTORY OF MEDPREPARATES, OJSC
    Information update date: & nbsp07.01.2018
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