Active substanceKetorolacKetorolac
Similar drugsTo uncover
  • Akyular LS
    drops d / eye 
    Allergen, Inc.     USA
  • Vatorlak
    solution w / m in / in 
    Novator Pharma, LLC     United Kingdom
  • Dolac
    solution w / m in / in 
  • Dolac
    pills inwards 
  • Dolomin®
    solution w / m in / in 
  • Cetadrope®
    drops d / eye 
  • Ketalgin®
    pills inwards 
  • Ketalgin®
    solution w / m in / in 
  • Ketanov®
    pills inwards 
  • Ketanov®
    solution w / m 
  • Ketokam®
    pills inwards 
  • Ketolac®
    solution w / m in / in 
    ALTAYVITAMINS, CJSC     Russia
  • Ketolac®
    pills inwards 
    ALTAYVITAMINS, CJSC     Russia
  • Ketorol®
    solution w / m in / in 
  • Ketorol®
    gel externally 
  • Ketorol®
    pills inwards 
  • Ketorolac
    pills inwards 
    VERTEKS, AO     Russia
  • Ketorolac
    solution w / m in / in 
  • Ketorolac
    pills inwards 
  • Ketorolac
    solution w / m 
  • Ketorolac
    solution w / m in / in 
    ELFA NPC, CJSC     Russia
  • Ketorolac
    pills inwards 
  • Ketorolac
    solution w / m in / in 
    BIOSINTEZ, PAO     Russia
  • Ketorolac
    solution w / m in / in 
    ELLARA, LTD.     Russia
  • Ketorolac
    pills inwards 
    LEKHIM-KHARKOV, CJSC     Ukraine
  • Ketorolac
    pills inwards 
  • Ketorolac
    solution w / m in / in 
  • Ketorolac
    solution w / m 
    TRIVIUM-XXI, LLC     Russia
  • Ketorolac
    solution w / m in / in 
  • Ketorolac
    solution w / m 
  • Ketorolac - SOLOFARM
    solution w / m in / in 
    GROTEKS, LLC     Russia
  • Ketorolac Rhompharm
    solution w / m in / in 
  • Ketorolac-OBL
    pills inwards 
  • Ketorolak-Eskom
    solution w / m in / in 
    ESKOM NPK, OAO     Russia
  • Ketofril®
    pills inwards 
  • Ketofril®
    solution w / m in / in 
  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    Composition per ml:

    active substance: ketorolac trometamol (ketorolac tromethamine) 30 mg;

    Sunauxiliaries: sodium chloride 4.35 mg, disodium edetate (disodium ethylenediamine-N,N,N,N-tetraacetic acid 2-water [Trilon B]) 0.5 mg, water for injection up to 1 ml.

    Description:

    Transparent liquid of yellowish color.

    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 cyclooxygenase 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.

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

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

    After intramuscular injection, the beginning of analgesic effect is observed after 0.5 h, the maximum effect is achieved in 1-2 hours.

    Pharmacokinetics:

    Bioavailability - 80-100%, absorption at intramuscular injection - complete and fast. After intramuscular injection of 30 mg, the maximum concentration in the blood plasma is (CmOh) 1.74-3.1 μg / ml, 60 mg - 3.23-5.77 μg / ml, the time to reach the maximum concentration, respectively - 15-73 min and 30-60 min; FROMmOh after intravenous infusion 15 mg - 1.96-2.98 mcg / ml, 30 mg - 3.69-5.61 mcg / ml. Time to reach equilibrium concentrations (Css) with parenteral administration - 24 hours when administered 4 times a day (above the sub-therapeutic) and is 15 mg-0.65-1.13 μg / ml with intramuscular injection, 30 mg-1.29-2.47 μg / ml, with intravenous infusion of 15 mg - 0.79-1.39 μg / ml, 30 mg - 1.68-2.76 μg / ml.

    99% of the drug binds to blood plasma proteins and the hypoalbuminemia increases the amount of free substance in the blood.

    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%. Poorly passes through the blood-brain barrier, penetrates the placenta (10%). In small quantities found in breast milk.

    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 on 91% by kidneys (40% in the form of metabolites), 6% - through the intestine.

    The half-life (T1/2) in patients with normal renal function averages 5.3 hours (3.5-9.2 hours after IM for 30 mg, 4-7.9 hours after IV injection 30 mg). T1/2 lengthens in elderly patients and is shortened in young patients. The function of the liver does not affect T1/2. In patients with impaired renal function with a creatinine concentration in the blood plasma 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 30 mg to 0.023 l / kg / h (0.019 l / kg / h in elderly patients) with IV IM, 30 mg to 0.03 l / kg / h infusion; in patients with renal failure at a plasma creatinine concentrationblood 19-50 mg / l with a / m injection of 30 mg - 0.015 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 use, the progression of the disease is not affected.

    Contraindications:

    Hypersensitivity to ketorolac, 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 taking non-steroidal anti-inflammatory drugs (in anamnesis) , dehydration.

    Intolerance to drugs of pyrazolone, hypovolemia (regardless of the cause), bleeding or a high risk of their development, a condition after aortocoronary bypass surgery, confirmed hyperkalemia, inflammatory bowel disease.

    Erosive-ulcerative lesions of the gastrointestinal tract in the stage of exacerbation, peptic ulcers, hypocoagulation (including hemophilia).

    Severe hepatic and / or renal insufficiency (creatinine clearance less than 30 ml / min).

    Hemorrhagic stroke (confirmed or suspected), hemorrhagic diathesis, hematopoiesis.

    Pregnancy, childbirth and lactation.

    Children under 16 years.

    The drug is not used for anesthesia before and during surgery due to high risk of bleeding, as well as for the treatment of chronic pain.

    Carefully:

    Bronchial asthma; cholecystitis; chronic heart failure; arterial hypertension; impaired renal function (plasma creatinine below 50 mg / l); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; old age (over 65 years); polyps of the nasal mucosa and nasopharynx, simultaneous reception with other non-steroidal anti-inflammatory drugs; presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking; postoperative period, edematous syndrome, ischemic heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus,peripheral arterial disease, creatinine clearance less than 60 ml / min, ulcerative lesions of the gastrointestinal tract in history, presence of H. pylori infection, prolonged use of non-steroidal anti-inflammatory drugs, severe somatic diseases, simultaneous intake of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

    Dosing and Administration:

    Enter deep into the muscle, slowly (or intravenously struino) for at least 15 seconds in minimal effective doses, selected according to the intensity of the pain and the patient's reaction. If necessary, it is also possible to additionally prescribe opioid analgesics in reduced doses.

    Single doses for single intramuscular or intravenous administration:

    - adults up to 65 years and children over 16 years: 10-30 mg, depending on the severity of the pain syndrome,

    - adults over 65 years of age or with impaired renal function: 10-15 mg.

    Doses with multiple parenteral administration:

    intramuscularly

    - adults under 65 years and children over 16 years of age: 10-60 mg in the first administration, then 10-30 mg every 6 hours (usually 30 mg every 6 hours),

    - adults over 65 years of age or with impaired renal function: 10-15 mg every 4-6 hours;

    intravenously

    - adults up to 65 years and children over 16 years of age: 10-30 mg are injected strontaneously, followed by 10-30 mg every 6 hours, with a continuous infusion with an infusomator, the initial dose is 30 mg, and then the infusion rate is 5 mg / h ,

    - adults over 65 years of age or with impaired renal function: injections of 10-15 mg every 6 hours.

    The maximum daily dose for adults up to 65 years and children over 16 years of age should not exceed 90 mg, and for adults over 65 years or with impaired renal function, 60 mg for both intramuscular and intravenous routes of administration.

    Continuous intravenous infusion should not last more than 24 hours.

    For parenteral administration, the duration of treatment should not exceed 5 days.

    When switching from parenteral administration of the drug to its administration inside the total daily dose of both dosage forms on the day of transfer should not exceed 90 mg for adults up to 65 years and children over 16 years and 60 mg for adults over 65 years or with impaired renal function.In this case, the dose of the drug in tablets on the day of transition should not exceed 30 mg.

    Side effects:

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

    From the digestive system: often (especially in elderly patients, over 65 years of age, having a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; rarely - 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 grounds" , nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

    From the urinary system: rarely - acute renal insufficiency, low back pain with or without hematuria and / or 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, 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 C sideHC: 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.

    From the side of the cardiovascular system: less often - increase blood pressure; rarely - faint.

    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, chills or without redness, induration or skin peeling, swelling and / or tenderness of the tonsils), rash, Stevens-Johnson syndrome, Lyell syndrome.

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

    Allergic Reagents: rarely - Anaphylaxis or anaphylactoid reactions (discoloration of the skin of the face, itching of the skin, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, wheezing).

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

    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). Dialysis is ineffective.

    Interaction:

    Simultaneous use of ketorolac with acetylsalicylic acid or other non-steroidal anti-inflammatory drugs, calcium preparations, glucocorticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding.

    Co-administration with paracetamol increases nephrotoxicity, with methotrexate-hepato- and nephrotoxicity.Co-administration of ketorolac and methotrexate is possible only with the use of low doses of ketorolac (control the concentration of methotrexate in the blood plasma).

    Against the background of the use of ketorolac, a decrease in the clearance of methotrexate and lithium and the increased toxicity of these substances are possible.

    Simultaneous administration with indirect anticoagulants, heparin, thrombolytic agents, antiaggregants, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding.

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

    When combined with opioid analgesics, the doses of the latter can be significantly reduced, since their effect is enhanced.

    The hypoglycemic effect of insulin and oral hypoglycemic drugs is increased (dose recalculation is necessary). Co-administration with valproic acid causes disruption of platelet aggregation. Increases the concentration in the blood plasma of verapamil and nifedipine.

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

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

    Solution for injection should not be mixed in one syringe with morphine sulfate, promethazine and hydroxyzine due to precipitation. Pharmaceutically it is not compatible with a solution of tramadol, lithium preparations.

    The solution for injections is compatible with 0.9% sodium chloride solution, 5% dextrose solution, Ringer's and Ringer's lactate solution, Plasmalite solution, as well as with infusion solutions containing aminophylline, lidocaine hydrochloride, dopamine hydrochloride, short-acting human insulin and heparin sodium salt.

    Special instructions:

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

    Hypovolemia increases the risk of adverse reactions from the kidneys. If necessary, you can prescribe in combination with narcotic analgesics.

    Ketorolac is not recommended for use as a means for premedication, supporting anesthesia and anesthesia in obstetric practice.

    Do not use simultaneously with paracetamol for more than 5 days. Patients with blood clotting disorder are prescribed a drug only with a constant control of the number of platelets, especially in the post-operation period, which require close monitoring of the hemostasis.

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

    It is recommended to avoid performing work that requires increased attention and quick response (driving vehicles, working with mechanisms, etc.).

    Form release / dosage:Solution for intravenous and intramuscular injection 30 mg / ml.
    Packaging:

    1 ml of solution in ampoules of light-protective glass.

    10 ampoules are placed in a box of cardboard.

    By 5 or 10 ampoules are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered or foil-free.

    1 a contoured cell package with 10 ampoules or 1, 2 contoured cells with 5 ampoules are placed in a pack of cardboard.

    In each pack, the box is attached instructions for use, the ampullar scarifier.

    When using ampoules with a kink ring or with a notch and a dot the ampoule scaper is not inserted.

    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 expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003584 / 01
    Date of registration:26.12.2008 / 06.03.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia
    Manufacturer: & nbsp
    Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia
    Information update date: & nbsp06.01.2018
    Illustrated instructions
      Instructions
      Up