Active substanceKetorolacKetorolac
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  • Dosage form: & nbspSolution for intravenous and intramuscular injection
    Composition:

    per ml:

    Active substance: ketorolac trometamol (ketorolac tromethamine) 30.0 mg

    Excipients: ethanol 95% (in terms of anhydrous) - 100.0 mg; sodium chloride - 4.35 mg; sodium hydroxide solution 1 M or hydrochloric acid solution 1 M - to pH 6.9-7.9; water for injection - up to 1.0 ml.

    Description:

    A clear solution of light yellow color.

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

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:

    Nonsteroidal anti-inflammatory drug (NSAID), has a pronounced analgesic effect, has also an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with a non-selective inhibition of cyclooxygenase-1 (COX-1) activity and cyclooxygenase-2 (COX-2) catalyzing the formation of prostaglandinsPg) 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 30 minutes, the maximum effect is achieved in 1-2 hours.

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

    Pharmacokinetics:

    Absorption for intramuscular injection is complete and rapid. After intramuscular injection, 30 mg the maximum concentration in the plasma (Cmax) is 1.74-3.1 μg / ml, after the / m administration of 60 mg - 3.23-5.77 μg / ml. Time to reach the maximum concentration (TCmax) in plasma - 15-73 min and 30-60 min respectively. The connection with plasma proteins is 99%.

    Time to reach equilibrium concentration (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 for intramuscular injection, 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 distribution of the drug can be increased 2-fold, and the volume of its distribution R-enantiomer by 20%.

    Penetrates into breast milk: when the mother receives 10 mg of ketorolac CmOh in breast milk is achieved in 2 hours after the first dose and is about 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 - an average of 5.3 hours (3.5 - 9.2 hours after intramuscular injection of 30 mg of drug). T1/2 increases in elderly patients and is shortened in young people. 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 - 10,3-10,8 h, with more severe renal failure - more than 13.6 hours.

    The total clearance is the intramuscular administration of 30 mg drug 0.023 L / h / kg (0,019 l / h / kg in elderly patients, patients with renal failure at a plasma creatinine concentration of 19-50 mg / l 30 mg by intramuscular administration of the preparation - 0.015 liters / 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.

    Designed for symptomatic therapy, reducing pain and inflammation at the time of use; on 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 in the anamnesis).

    Urticaria, rhinitis caused by the use of non-steroidal anti-inflammatory drugs (in the anamnesis).

    Intolerance to medicines of pyrazolone series.

    Dehydration.

    Hypovolemia (regardless of the cause that caused it).

    Bleeding or a high risk of their development.

    Condition after aortocoronary bypass surgery.

    Confirmed hyperkalemia.

    Inflammatory bowel disease.

    Erosive-ulcerative lesions of the gastrointestinal tract in the phase of exacerbation (including ulcerative colitis, Crohn's disease). Peptic ulcers.

    Blood clotting disorders (including hemophilia).

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

    Hemorrhagic stroke (confirmed or suspected).

    Hemorrhagic diathesis, hematopoiesis.

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

    Pregnancy, childbirth and the period of breastfeeding.

    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, as well as for the treatment of chronic pain.

    Carefully:

    Hypersensitivity to other non-steroidal anti-inflammatory drugs (NSAIDs), bronchial asthma, the presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis, postoperative period, chronic heart failure, ischemic heart disease, edematous syndrome; arterial hypertension, impaired renal function (creatinine clearance 30-60 ml / min), cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, simultaneous administration with other non-steroidal anti-inflammatory drugs (NSAIDs),long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs), cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial diseases, history of gastrointestinal ulcers, infection Helicobacter pylori(including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective inhibitors of serotonin reuptake (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 (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 breastfeeding.

    Dosing and Administration:

    Intramuscularly, intravenously.

    The drug is administered intravenously struino for at least 15 seconds or intramuscularly slowly, deep into the gluteal muscle, in minimally effective doses in a minimally short course. If necessary, it is also possible to additionally use opioid analgesics in reduced doses.

    Single doses for single administration:

    - Patients from 16 to 65 years old and weighing more than 50 kg - 60 mg (2 ml) intramuscularly or 30 mg (1 ml) intravenously.

    - Patients over 65 years of age, or with renal insufficiency (serum creatinine 170-442 μmol / L), or a body weight of less than 50 kg is 30 mg (1 ml) intramuscularly or 15 mg (0.5 ml) intravenously.

    Doses with repeated administration:

    - Patients from 16 to 65 years old and weighing more than 50 kg - 30 mg (1 ml) intramuscularly or intravenously as needed every 6 hours. The maximum daily dose should not exceed 90 mg (3 ml).

    - Patients over 65 years of age, or with renal insufficiency (serum creatinine 170-442 μmol / L), or body weight less than 50 kg -15 mg (0.5 ml) intramuscularly or intravenously as needed every 6 hours. The maximum daily dose should not be exceed 60 mg (2 ml).

    The maximum duration of treatment should not exceed 2 days. When switching from parenteral to oral administration, the total daily dose of both dosage forms per daytranslation should not exceed 90 mg for patients under 65 years of age and 60 mg for patients over 65 years of age, or with renal insufficiency, or a body weight of less than 50 kg. In this case, the dose of the drug in tablets on the day of transition should not exceed 30 mg.

    Side effects:

    The frequency of side effects is presented according to the following gradation: very often - more than 10%; often more than 1.0%, but less than 10.0%; infrequently - more than 0,1%, but less than 1,0%; rarely - more than 0.01%, but less than 0.1%; very rarely - less than 0.01%.

    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 those with perforation and / or bleeding that 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 failure, thrombocytopenia, purpura), frequent urination,increase or decrease in the volume of urine, nephritis, edema of renal genesis.

    From the sense organs: infrequently - hearing loss, ringing in the ears, visual impairment (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 (CNS): 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 side of the cardiovascular system: often - increased blood pressure, a feeling of heartbeat.

    On the part of the organs of 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), purpura; infrequently - exfoliative dermatitis (fever with chills or without, hyperemia, densification or flaky skin,and / or soreness 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 reactions (skin discoloration, skin rash, urticaria, skin itching, tachypnea or shortness of breath, eyelid edema, periorbital edema, shortness of breath, 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 administration): abdominal pain, nausea, vomiting, erosive-ulcerative lesions of the gastrointestinal tract (GIT), impaired renal function, metabolic acidosis.

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

    Interaction:

    Simultaneous administration with paracetamol increases the nephrotoxicity of ketorolac. Admission with other non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticosteroids,ethanol, corticotropin, calcium preparations 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 plasma methotrexate concentration).

    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.

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

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

    Special instructions:

    Before prescribing a medicine, it is necessary to clarify the question of the previous allergy to Ketorolac or other non-steroidal anti-inflammatory drugs (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 non-steroidal anti-inflammatory drugs (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, which is especially important for postoperative patients who require close monitoring of hemostasis.

    To reduce the risk of developing adverse events, the drug should be used at the lowest effective dose, with the minimum possible short course.

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

    Effect on the ability to drive transp. cf. and fur:It should refrain from driving and other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.
    Form release / dosage:

    Solution for intravenous and intramuscular injection 30 mg / ml.

    Packaging:

    1 ml or 2 ml in the ampoules of the light-protective glass.By 3 or 5 ampoules per contour cell pack of a polyvinylchloride (PVC) film or a polyethylene-phthalate (PET) film.

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

    By 3 or 6; 5 or 10 ampoules together with the instruction for use and scarifier ampoule in a pack of cardboard with a corrugated liner.

    When using ampoules with a dot or a ring of fracture, the ampoule scaper is not inserted.

    Packing for hospitals. For 4, 5 or 10 contour mesh packages, together with the instructions for use in an amount equal to the number of contour mesh packages, into a pack of cardboard.

    For 50, 100 contour mesh packages together with the instructions for use in an amount equal to the number of contour mesh packages, into a box of corrugated cardboard.

    Storage conditions:

    In 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 the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002623
    Date of registration:16.09.2014 / 01.06.2017
    Expiration Date:16.09.2019
    The owner of the registration certificate:ELLARA, LTD. ELLARA, LTD. Russia
    Manufacturer: & nbsp
    Information update date: & nbsp06.01.2018
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