Active substanceKetorolacKetorolac
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  • Dosage form: & nbspfilm coated tablets
    Composition:

    Each film-coated tablet contains:

    Active substance: ketorolac tromethamine - 10 mg;

    Auxiliary substances: cellulose microcrystalline 121 mg, lactose 15 mg, corn starch 20 mg, silicon dioxide colloid 4 mg, magnesium stearate 2 mg, sodium carboxymethyl starch (type A) 15 mg,

    coating: hypromellose 2.6 mg, propylene glycol 0.97 mg, titanium dioxide 0.33 mg, olive green (dye quinoline yellow 78%, dye brilliant blue 22%) 0.1 mg.

    Description:

    Round biconvex tablets covered with a film membrane of green color, on one side stamping "S". View on the transverse section: the shell is green and the core is white or almost white.

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

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:

    Nonsteroidal anti-inflammatory drug (NSAID), has a pronounced analgesic effect, has anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with nonselective inhibition of cyclooxygenase (COX) -COG-1 and COX-2 activity catalyzing the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. 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 significantly exceeds other NSAIDs.

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

    After oral administration, the development of analgesic effect is observed after 1 hour.

    Pharmacokinetics:

    Ingestion ketorolac well and quickly absorbed in the gastrointestinal tract (GIT). Bioavailability of ketorolac is 80-100%, the maximum concentration (CmOh) after oral administration of 10 mg - 0.82-1.46 μg / ml, the time to reach the maximum concentration (TFROMmOh) - 10-78 min. Fat-rich food reduces the maximum concentration of the drug in the blood and delays its achievement by an hour. The connection with plasma proteins is 99%.

    The time to reach the equilibrium concentration of the drug (Css) when administered orally 10 mg 4 times a day is 24 hours and the concentration is 0.39-0.79 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 milk is achieved in 2 hours after the first dose and is 7.3 ng / ml, 2 hours after the second dose of ketorolac (using the drug 4 times a day) - 7.9 ng / l.

    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 (T1 / 2) in patients with normal renal function, on average, is 5.3 hours (2.4-9 hours after oral administration of 10 mg). T1 / 2 increases in elderly patients and is shortened in young patients. Infringements of function of a liver does not render influence on 1 \ a- In patients with impaired renal function, at 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.

    With oral administration of 10 mg, the total clearance is 0.025 l / h / kg; in patients with renal insufficiency (at a creatinine concentration in the plasma of 19-50 mg / l) - 0.016 l / h / kg. It is not excreted by hemodialysis.

    Indications:

    Pain syndrome of strong and moderate severity: trauma, toothache,pain in the postnatal and postoperative period, oncological diseases, myalgia, arthralgia, neuralgia, sciatica, dislocations, sprains, rheumatic diseases. It is intended for symptomatic therapy, reducing the intensity of 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 or paranasal sinuses and intolerance Acetylsalicylic acid and other NSAIDs (including in history);

    - erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding; cerebrovascular or other bleeding;

    - inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation;

    - hemophilia and other bleeding disorders;

    - Decompensated heart failure;

    - hepatic insufficiency or active liver disease;

    - marked renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;

    - period after aortocoronary shunting;

    - deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

    - simultaneous administration with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants (including warfarin and heparin);

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

    - pregnancy, childbirth, lactation;

    - children's age till 16 years.

    Carefully:Bronchial asthma, ischemic heart disease, congestive heart failure, edematous syndrome, arterial hypertension, cerebrovascular diseases, pathological dyslipidemia / hyperlipidemia, renal dysfunction (creatinine clearance 30-60 ml / min), diabetes mellitus, cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, peripheral artery disease, smoking, elderly age (over 65), history of development ulcerative lesions of the digestive tract, alcohol abuse, severe somatic diseases,concomitant therapy with the following drugs: antiaggregants (eg, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:

    In the form of tablets used inside a single dose of 10 mg. In severe pain syndrome, the drug is taken repeatedly for 10 mg up to 4 times a day, depending on the degree of pain. The maximum daily dose should not exceed 40 mg. The minimum effective dose should be used. When administered orally, 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 patients from 16 to 65 years and 60 mg for patients older than 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:

    The frequency of side effects is classified according to the incidence of the case: often - (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01% ), including individual messages.

    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 abdominal pain, spasm or burning in the epigastric region, melena, vomiting like "coffee grounds", nausea, heartburn and others) with perforation and / or bleeding; 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, visual impairment (including blurred vision).

    From the respiratory system: rarely - bronchospasm, dyspnea, rhinitis, laryngeal edema.

    From 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 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, epistaxis, 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.

    Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin color change of the face, 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 - swelling (face, legs, ankles, fingers, feet, weight gain); less often - excessive sweating, rarely - swelling of the tongue, fever.

    Overdose:

    Symptoms: abdominal pain, nausea, vomiting, erosive-ulcerative lesions of the gastrointestinal tract, 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, including cyclooxygenase-2 inhibitors, calcium, 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).

    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 and the increased toxicity of these substances are possible.

    Simultaneous appointment with indirect anticoagulants, including heparin and warfarin, 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. 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.Drugs that block tubular secretion, reduce the clearance of ketorolac and increase its concentration in the blood plasma.

    Special instructions:

    Ketorol® has two dosage forms (film-coated tablets and injection solution). Choice of method of administration The drug depends on the severity of the pain syndrome and the patient's condition.

    The risk of developing drug complications increases with prolonged treatment periods of more than 5 days and an increase in the oral dose of the drug more than 40 mg / day.

    Do not use the drug simultaneously with other NSAIDs (including cyclooxygenase-2 inhibitors), as well as with probenecid, pentoxifylline, acetylsalicylic acid, lithium salts, anticoagulants (including warfarin and heparin).

    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.

    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 drug can change the properties of platelets.

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

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

    During the treatment period, care must be taken when driving and other potentially hazardous activities that require increased concentrations attention and speed psychomotor reactions.

    Form release / dosage:

    Tablets, film-coated, 10 mg.

    Packaging:

    For 10 tablets in PA / alum / PE with desiccant / HDPE // PE / aluminum blisters.

    Two blisters along with instructions for use are packed in a cardboard pack.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N015823 / 02
    Date of registration:03.06.2009 / 20.04.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.
    Information update date: & nbsp16.11.2017
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