Active substanceKetorolacKetorolac
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: ketorolac trometamol (ketorolac tromethamine) 10.0 mg;

    Excipients: cellulose microcrystalline 77.9 mg, lactose 49.3 mg, croscarmellose sodium 1.4 mg, magnesium stearate 1.4 mg.

    Description:

    Tablets from white to white with a creamy shade of color, flat-cylindrical with a bevel.

    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 cyclooxygenase 1 and 2 activity, mainly in peripheral tissues, which results in inhibition of 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.

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

    By the strength of the analgesic effect comparable to morphine, it significantly exceeds other NSAIDs.

    After oral administration, the beginning of the analgesic effect is noted, respectively, after 1 h, the maximum effect is achieved in 1-2 hours.

    Pharmacokinetics:

    After ingestion, the preparation is quickly and completely absorbed from the digestive tract. The intake of food does not affect the degree of absorption, but can somewhat slow its speed. The maximum concentration of ketorolac in the plasma after ingestion of 10 mg is 0.88-2.69 μg / ml and is reached 45-60 minutes after ingestion. Bioavailability is 80-100%. 99% of ketorolac binds to blood plasma proteins and the amount of free substance in the blood increases with hypoalbuminemia.

    The time to achieve an equilibrium concentration when taken orally - 24 hours when administered 4 times a day (above the sub-therapeutic) d is 10 mg - 0.39-0.79 μg / ml after oral administration. 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 a mother receives 10 mg of ketorolac, the maximum concentration in milk is reached 2 hours after the first dose and is 7.3 ng / ml,2 hours after the second dose of ketorolac (with the drug 4 times a day) - is 7.9 ng / ml.

    More than 50% of the administered dose is metabolized in the liver with the formation of a pharmacologically inactive metaboliteComrade. 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 averages 5.3 hours. T1/2 lengthens 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 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.

    It is not excreted during hemodialysis.

    Indications:

    Pain syndrome of strong and moderate severity: trauma, toothache, pain in the postpartum and postoperative period, myalgia, arthralgia, neuralgia, sciatica, sprains, sprains, rheumatic diseases, oncological 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 the components of the drug;

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);

    - urticaria, rhinitis caused by taking an NSAID (in history);

    - intolerance of drugs pyrazolone series;

    - hypovolemia (regardless of the cause that caused it);

    - erosive and ulcerative lesions of the gastrointestinal tract in the stage of exacerbation;

    - 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;

    - inflammatory, intestinal diseases;

    - condition after aorto-coronary bypass surgery;

    - confirmed hyperkalemia;

    - pregnancy;

    - the period of childbirth;

    - lactation period;

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

    Carefully:

    - Bronchial asthma;

    - presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis;

    - postoperative period;

    - chronic heart failure;

    - edematous syndrome;

    - arterial hypertension;

    - impaired renal function (creatinine clearance 30-60 ml / min);

    - cholestasis;

    - sepsis;

    - systemic lupus erythematosus;

    - simultaneous reception with other NSAIDs;

    - cardiac ischemia;

    - cerebrovascular diseases;

    - dyslipidemia / hyperlipidemia;

    - diabetes;

    - diseases of peripheral arteries;

    - clearance of creatinine 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 physical illness;

    - simultaneous administration of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline);

    - Older age (over 65 years).

    Dosing and Administration:

    Adults and children over 16 years of age: inside once or repeatedly depending on the severity of the pain syndrome.

    A single dose of 10-20 mg, with repeated admission is recommended to take 10 mg to 4 times a day, depending on the severity of pain.

    The maximum daily dose should not exceed 40 mg.

    When administered, the duration of the course should not exceed 5 days.

    Side effects:

    Often - more than 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, melena, vomiting like "coffee grounds", nausea, heartburn, etc. .), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

    From the urinary system: rarely acute renal failure, back pain with or without hematuria and / or azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased 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 shortness of breath, rhinitis, laryngeal edema (difficulty breathing).

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

    From the side of the cardiovascular system: less often - increased blood pressure, rarely - pulmonary edema, fainting.

    From the hematopoiesis: rarely - anemia, eosinophilia, leukopenia

    From the side of the hemostasis system: rarely bleeding from a postoperative wound, nosebleeds, rectal bleeding.

    From the skin: less often - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with chills or without, redness, densification or flaking of the skin, swelling and / or tenderness of the tonsils), hives, Stevens-Johnson syndrome, Lyell's syndrome.

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

    Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (facial skin discoloration, skin rash, hives, skin itch, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, whistlingbreathing).

    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, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis.

    Treatment: gastric lavage, administration of adsorbents (Activated carbon) and the conduct of symptomatic therapy (maintenance of vital body functions). It is not excreted sufficiently by dialysis.

    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.

    Joint application with paracetamol increases nephrotoxicity, with methotrexate - hepato- and nephrotoxicity of the latter. Joint application of ketorolac and methotrexate is possible only with low doses of the latter (it is necessary to monitor the concentration of methotrexate in the blood plasma).

    Probenecid and drugs that block tubular secretion, reduces plasma clearance and the volume of distribution of ketorolac, 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 and the increased toxicity of these substances are possible.

    Simultaneous use 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.

    Antacids do not affect the full absorption of the drug.

    Increases hypoglycemic action of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

    Joint application with valproic acid causes disruption of platelet aggregation.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Increases the concentration in the blood plasma of verapamil and nifedipine.

    When used with other nephrotoxic drugs (including with gold preparations), the risk of developing nephrotoxicity increases.

    Special instructions:

    Before prescribing the drug, it is necessary to clarify the question of the previous allergy to the drug or other NSAIDs.

    The effect on platelet aggregation is stopped after 24-48 hours. Patients with blood clotting disorder are prescribed a drug only with a constant control of the number of platelets, especially important in the post-operation period, which requires careful control of hemostasis.

    Hypovolemia increases the risk of adverse reactions from the kidneys.

    If necessary, you can prescribe in combination with narcotic analgesics.

    Do not apply simultaneously with paracetamol for more than 5 days.

    To reduce the risk of developing NSAID-gastropathy appointed antacid drugs, misoprostol, omeprazole. Also, to reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be applied with the minimum possible short course.

    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.

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

    As 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 that requires increased attention and quick response (driving vehicles, working with mechanisms, etc.).

    Form release / dosage:

    Tablets of 10 mg.

    Packaging:

    For 10, 20 or 25 tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil.

    1, 2, 5 or 10 contour cell packs of 10 tablets, 1 or 5 contour packs of 20 tablets or 2 or 4 contour packs of 25 tablets together with the instructions for use are placed in a pack of 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:

    3 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000243
    Date of registration:31.08.2010
    The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia
    Manufacturer: & nbsp
    Representation: & nbspVERTEKS CJSC VERTEKS CJSC Russia
    Information update date: & nbsp03.04.2012
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