Active substanceKetorolacKetorolac
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  • Dosage form: & nbspsolution for intramuscular and intravenous administration
    Composition:

    Per 1 ml:

    active substance: ketorolac trometamol in terms of 100% of the substance 30.00 mg;

    Excipients: sodium chloride 4.35 mg, disodium edetate 1.00 mg, ethyl alcohol rectified from food raw materials 96.3% 100.00 mg, trometamol solution 0.5 M to pH 7.5, water for injection up to 1.0 ml.

    Description:Transparent liquid of light yellow color with a weak smell.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)
    ATX: & nbsp

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:Ketorolaka trometamol refers to non-steroidal anti-inflammatory drugs (NSAIDs), has a pronounced analgesic effect, and has an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with nonselective inhibition of cyclooxygenase 1 (COX1) and cyclooxygenase 2 (COX2) activity catalyzing the formation of prostaglandins (Pg) from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. By force Analgesic effect comparable to morphine, significantly superior to other NSAIDs.

    After intramuscular (intramuscular) administration, the onset of analgesic effect is observed after 0.5 hours, respectively, and the maximum effect is achieved after 1-2 hours.

    Pharmacokinetics:

    Bioavailability is complete and fast. After the / m introduction, 30 mg maximum concentration (Cmah) - 1.74-3.1 μg / ml, 60 mg - 3.23-5.77 μg / ml, the time to reach the maximum concentration (TCmah) - 15-73 min and 30-60 min respectively. After intravenous (iv) infusion at a dose of 15 mg Cmah is 1.96-2.98 mcg / ml, in a dose of 30 mg - Cmah is 3.69-5.61 μg / ml. The connection with plasma proteins is 99%. Time to reach equilibrium concentration (Css) - 24 hours when administered 4 times a day (more than the recommended daily dose) and is 15 mg-0.65-1.13 μg / ml at the IM, 30 mg-1.29-2.47 μg / 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%.

    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 period (T1 / 2) in patients with normal renal function was 5.3 hours on average (3.5-9.2 hours after IM injection 30 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 30 mg to 0.023 l / h / kg, with an IV infusion of 30 mg to 0.03 l / kg / h. It is not excreted by hemodialysis.

    Indications:

    Pain syndrome of strong and moderate severity: trauma, toothache, pain in the 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, a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history), urticaria, rhinitis caused by NSAID administration (in the anamnesis), intolerance to pyrazolone drugs, hypovolemia (regardless of the cause that caused it), erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, hypocoagulation (incl.hemophilia), bleeding or a high risk of development, severe renal impairment (creatinine clearance less than 30 mL / min), severe hepatic impairment or active liver disease, condition after coronary bypass, confirmed hyperkalemia, inflammatory bowel disease, pregnancy (III trimester), childbirth, lactation, children under 16 years of age (safety and efficacy not established).

    Carefully:

    Hypersensitivity to other NSAIDs, bronchial asthma, the presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis; postoperative period, chronic heart failure (CHF), coronary heart disease (CHD), edematous syndrome, hypertension, renal insufficiency moderate severity (QC from 30 to 60 ml / min), cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, simultaneous administration with other NSAIDs, prolonged use of NSAIDs, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial diseases, history of gastrointestinal lesions, infection H.pylori, severe somatic diseases, simultaneous administration of oral glucocorticosteroid agents (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline), elderly age (over 65 years), pregnancy (I and 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, the drug may adversely affect the fetal circulation and weaken the contractile activity of the uterus that increases the risk of uterine bleeding) and during lactation (the drug penetrates into breast milk).

    Dosing and Administration:

    The drug is intended for short-term use.

    The drug is injected intravenously in a jet or intramuscularly slowly, deep into the gluteus muscle. The dosage regimen is set individually, taking into account the severity of the pain syndrome.

    Adult to 65 years of age intramuscularly inject 10-30 mg (0.3-1 ml), then 10-30 mg every 4-6 hours. With an intravenous jet injection (for at least 15 seconds), the initial dose is 10-30 mg, then optionally 10-30 mg every 6 hours.

    The highest single dose: with intravenous administration - 30 mg, with a single intramuscular injection - 60 mg, with repeated intramuscular injection - 30 mg.

    The highest daily dose with any route of administration should not exceed 90 mg. The maximum duration of therapy is 5 days.

    Patients over 65 years of age or patients with impaired renal function (serum creatinine 170-442 μmol / l) intramuscularly or intravenously injected 10-15 mg (0.3-0.5 ml) intramuscularly or intravenously; if necessary, injections are repeated every 4-6 hours. The highest daily dose for both administration routes for this the category of patients should not exceed 60 mg.

    Side effects:

    The incidence of side effects is given in accordance with the classification of the World Health Organization: Often - not less than 10%; often - not less than 1% and less than 10%; infrequently - not less than 0.1% and less than 1%; rarely - not less than 0.01% and less than 0.1%; rarely - less than 0.01%, including isolated cases.

    From the digestive system: very often - gastralgia, dyspepsia, nausea; often - diarrhea, constipation, flatulence, a feeling of overflow of the stomach, vomiting, stomatitis; infrequent - an increase or decrease in appetite, anorexia, 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 grounds", nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

    From the urinary system: infrequently, hematuria, proteinuria, urinary retention, oliguria, polyuria, increased urination, acute renal failure, low back pain with or without hematuria and / or azotemia, interstitial nephritis, hyponatremia, hyperkalemia, hemolytic uremic syndrome (hemolytic anemia, kidney failure, thrombocytopenia, purpura).

    From the sense organs: infrequently - a violation of taste, impaired vision (including blurred vision), decreased hearing, ringing in the ears.

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

    From the central nervous system: very often - headache; often - dizziness, drowsiness, increased sweating; infrequent tremor, unusual dreams, hallucinations, euphoria, extrapyramidal symptoms, vertigo, paresthesia, depression, insomnia, nervousness, polydipsia, dry mouth, pathological thinking, loss of concentration, hyperkinesia, stupor, aseptic meningitis (fever, severe headache, cramps, rigidity of the neck muscles and / or back), psychosis, fainting.

    From the side of the cardiovascular system: often - increased blood pressure; infrequently - palpitation, pallor, syncope, hyperemia.

    On the part of the organs of hematopoiesis: often - purpura, infrequently anemia, eosinophilia.

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

    From the side of the skinin: often - itching, rash (including maculopapular rash); infrequent urticaria, toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema (Stevens-Johnson syndrome), exfoliative dermatitis (fever with chills or without, hyperemia, thickening or flaky skin, enlarged and / or tenderness of the tonsils).

    Local reactions: often - burning or pain at the injection site.

    Allergic reactions: infrequently 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, chest pain, wheezing).

    Other: often - edema (face, legs, ankles, fingers, feet, weight gain); infrequently - weight gain, fever, infection, asthenia, increased sweating, swelling of the tongue.
    Overdose:

    Symptoms (with a single administration): abdominal pain, nausea, vomiting, erosive-ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis.

    Treatment: symptomatic (maintenance of vital body functions). It is not excreted sufficiently by dialysis.

    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 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 increase the manifestation of hematotoxicity of the drug.
    Special instructions:

    Before prescribing a medicine, it is necessary to clarify the question of the previous allergy to ketorolac or other NSAIDs. 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 NSAIDs, 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 developing gastropathy, antacid medicines are prescribed, misoprostol, omeprazole.

    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.

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

    Since a significant part of patients with the administration of ketorolac develop side effects from the central nervous system (drowsiness, dizziness, headache), it is recommended to avoid performing work requiring increased attention and quick response (driving vehicles, working with mechanisms, etc.).

    Form release / dosage:

    Solution for intramuscular and intravenous administration, 30 mg / ml.

    Packaging:

    1 ml of the drug in ampoules.

    For 10 ampoules together with instructions for medical use and a knife for opening ampoules in a cardboard box.

    10 ampoules in a blister pack. 1 blister pack together with a knife for opening ampoules and instructions for medical use in a pack of cardboard.

    For 10 ampoules together with a knife for opening ampoules and instructions for medical use in a pack with a cardboard insert for fixing ampoules from cardboard.

    In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

    Storage conditions:

    In the dark place at a temperature of 15 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002090
    Date of registration:04.06.2013 / 01.06.2015
    Expiration Date:04.06.2018
    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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