Active substanceKetorolacKetorolac
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  • Dosage form: & nbspsolution for intramuscular injection
    Composition:

    1 ml of the solution contains:

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

    Excipients: disodium edetate dihydrate (Trilon B) 1 mg; Ethanol (ethyl alcohol) (in terms of anhydrous) 100 mg; propylene glycol 200 mg; sodium chloride 4.35 mg; sodium hydroxide 1 M solution to pH 6.9-7.9; water for injection up to 1 ml.

    Description:Transparent liquid of light yellow color.
    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 nonselective inhibition of cyclooxygenase 1 and cyclooxygenase 2 activity 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 intramuscular injection, the onset of analgesic effect is observed after 0.5 h, the maximum effect is achieved in 1-2 hours.

    Pharmacokinetics:

    Absorption at intramuscular injection is complete and fast. The maximum concentration (Cmah) after intramuscular injection 30 mg - 2.4 mcg / ml, 60 mg - 4.5 mcg / ml, the time to reach the maximum concentration of 15 to 73 min. The connection with plasma proteins is 99%.

    Time to reach the equilibrium concentration (Css) with parenteral administration - 24 hours, with the appointment of 4 times a day (above the sub-therapeutic) and is 15 mg - 0.9 μg / ml intramuscular injection, 30 mg - 1.9 μg / ml.

    The volume of distribution is 0.15-0.3 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. 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 is about 5 hours on average. 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 increases to 10 hours, with more severe renal failure - more than 13 hours.

    The total clearance is 30 mg - 0.02 l / h / kg (0.019 l / h / kg in elderly patients) when administered intramuscularly, in patients with renal insufficiency with a creatinine concentration in the plasma of 19-50 mg / l with intramuscular injection of 30 mg - 0.015 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 use, the progression of the disease is not affected.

    Contraindications:

    Hypersensitivity.

    Complete or incomplete combination of bronchial asthma, recurring polyposition of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis).

    Hives, rhinitis caused by taking NSAIDs (in history).

    Intolerance to medicines of pyrazolone series.

    Hypovolemia (regardless of the cause that caused it).

    Inflammatory bowel diseases, 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 insufficiency (creatinine clearance less than 30 ml / mni), severe hepatic insufficiency or active liver disease.

    Condition after aortocoronary bypass surgery.

    Confirmed hyperkalemia.

    Simultaneous application with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants, including warfarin and heparin.

    Pregnancy, childbirth, lactation.

    Children under 16 years of age (safety and efficacy not established).

    The drug is not used for preventive analgesia before and during extensive surgery because of the high risk of bleeding.

    Carefully:

    Bronchial asthma, the presence of factors that increase toxicity in relation to the gastrointestinal tract: alcoholism, tobacco smoking and cholecystitis; postoperative period, chronic heart failure, edematous syndrome, hypertension, impaired renal function (plasma creatinine below 50 mg / l), cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, ischemic heart disease, cerebrovascular diseases,dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, creatinine clearance 30-60 ml / min, ulcerative lesions of the gastrointestinal tract in the anamnesis, the presence of infection H. pylori, long-term use of NSAIDs, severe somatic diseases, simultaneous administration of oral glucocorticosteroids (including prednisolone), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline ), elderly age (over 65 years).

    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, the use of the drug is contraindicated, because, by inhibiting the synthesis of prostaglandins, it can adversely affect the blood circulation of the fetus and weaken the contractile activity of the uterus, which increases the risk of uterine bleeding.

    At the time of treatment, breastfeeding should be discontinued, as the drug, by inhibiting the synthesis of prostaglandins, can cause adverse effects in newborns.

    Dosing and Administration:

    Intramuscularly.

    For parenteral administration to patients from 16 to 64 years of age with a body weight exceeding 50 kg, no more than 60 mg is administered intramuscularly for 1 administration; usually 30 mg every 6 hours.

    Adult patients with a body weight of less than 50 kg or with chronic renal failure per 1 injection are administered no more than 30 mg; usually - 15 mg (no more than 20 doses in 5 days).

    Maximum daily doses for patients from 16 to 64 years with a body weight exceeding 50 kg are 90 mg / day; adult patients with a body weight of less than 50 kg or with chronic renal failure, as well as elderly patients (over 65 years of age) - 60 mg.

    The duration of treatment should not exceed 5 days.

    Side effects:

    Very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000, <1/1000) and very rarely (<1/10000).

    From the digestive system: often - gastralgia, diarrhea, stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; infrequent appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including perforation and / or bleeding, which can manifest as 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: infrequent acute renal failure, back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal insufficiency, thrombocytopenia, purpura), frequent urination, increase or decrease in urine volume, nephritis, edema of renal genesis.

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

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

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

    From the cardiovascular system: often - increased blood pressure, a feeling of palpitations.

    From the hematopoiesis: infrequently, anemia, eosinophilia, and leukopenia.

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

    From the skin: often - skin rash (including maculopapular rash), purpura; infrequently - exfoliative dermatitis (fever, chills or without hyperemia, sealing or flaking skin, increase and / or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

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

    Allergic reactions: infrequently - anaphylaxis or anaphylactoid reaction (change in skin color, skin rash, hives, itchy skin, tachypnea and dyspnea, edema of the eyelids, periorbital edema, shortness of breath, heaviness in the chest, wheezing).

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

    Overdose:

    Symptoms (with a single injection): abdominal pain, nausea, vomiting, loss erozivnoyazvennoe gastrointestinal, renal dysfunction, metabolic acidosis.

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

    Interaction:

    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 derivatives of indandione, heparin, warfarin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet drugs, pentoxifylline, cephalosporins, valproic acid and acetylsalicylic acid increase the risk of bleeding.

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

    Probenecid reduces plasma clearance and the volume of ketorolac distribution, increases its concentration in blood plasma and increases its half-life.

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

    Pharmaceutically incompatible with a solution of tramadol, lithium preparations.

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

    At appointment with other nephrotoxic drugs (including with preparations of gold) the risk of development of nephrotoxicity increases.

    Drugs that block tubular secretion, reduce the clearance of ketorolac and increase one hundred concentrations in the plasma.

    Increases the effect of narcotic analgesics.

    Myelotoxic drugs increase manifestations of hematotoxicity of the drug.

    The hypoglycemic effect of insulin and oral hypoglycemic drugs is increased (dose recalculation is necessary).

    Special instructions:

    Before prescribing the drug, it is necessary to clarify the question of the previous allergy to the drug or 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 co-administered with other NSAIDs, fluid retention, cardiac decompensation,increase in blood pressure.

    The effect on platelet aggregation stops after 24-48 hours.

    Do not use with paracetamol for more than 2 days.

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

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

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

    To reduce the risk of developing adverse events 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:

    It should refrain from driving and other activities potentially hazardous activities that require high concentration and speed of psychomotor reactions, because the drug can cause dizziness and other side effects that may affect these abilities.

    Form release / dosage:

    Solution for intramuscular injection 30 mg / ml.

    Packaging:

    1 ml per ampoule of amber or lightproof glass.

    5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

    For 1 or 2 contour packs with a scarifier ampoule and instructions for use in a pack of cardboard.

    When using ampoules with a dot or a ring of fracture, the scarifier is not embedded.

    Storage conditions:

    Store in a 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.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008611/10
    Date of registration:24.08.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspMOSHIMFARM PREPARATES them. NA Semashko OJSC MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia
    Information update date: & nbsp06.01.2018
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