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

    1 tablet contains:

    active substance: ketorolac trometamol (ketorolac tromethamine) 0.010 g;

    Excipients: microcrystalline cellulose, milk sugar (lactose), magnesium stearate, hydroxypropylmethylcellulose (hypromellose), titanium dioxide pigment (titanium dioxide), macrogol 4000 - sufficient amount to obtain a film coated tablet weighing 0.205 g.

    Description:

    The tablets covered with a film cover, round, biconcave, white 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 a nonselective inhibition of the activity of COX1 and COX2 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.

    After oral administration, the onset of analgesic action is noted, respectively, in 0.5 -1h, the maximum effect is achieved in 2-3 hours.

    Pharmacokinetics:

    Absorption at intake - fast, bioavailability - 80-100%. FROMmah after oral intake of 10 mg - 0.7-1.1 μg / ml, the time to reach the maximum concentration (TCmah) -10-78 min.

    The equilibrium concentration (Css) is achieved by oral administration - 24 hours when administered 4 times a day (above the sub-therapeutic) and is 10 mg - 0.39-0.79 mkg / ml after oral administration. The connection with plasma proteins is 99%.

    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 Cmah in milk is achieved 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 period (T1 / 2) in patients with normal renal function - about 9 h 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 - 10,3-10,8 h, with more pronounced renal failure - more than 13.6 hours.

    The total clearance is 10 mg - 0.025 l / h / kg with oral administration; in patients with renal insufficiency with a creatinine concentration in the plasma of 19-50 mg / l with oral administration of 10 mg - 0.016 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 to the active substance or ancillary components.

    Anamnestic data on an attack of bronchial obstruction, rhinitis, hives after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, bronchial asthma).

    Erosive-ulcerative lesions of the gastrointestinal tract in the acute stage, peptic ulcers, bleeding or high risk of their development, hypocoagulation (including hemophilia), inflammatory bowel disease (Crohn's disease, ulcerative colitis).

    Severe hepatic impairment or active liver disease.

    Severe renal insufficiency (creatinine clearance less than 30 ml / min), progressive kidney disease.

    Confirmed hyperkalemia.

    Decompensated heart failure.

    Contraindicated in the period after aortocoronary bypass surgery.

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

    III trimester of pregnancy, childbirth and lactation (should refrain from feeding for the period of application of the drug).

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

    Carefully:

    Bronchial asthma, the presence of factors that increase toxicity in relation to the gastrointestinal tract: alcoholism and cholecystitis; chronic heart failure, edematous syndrome, hypertension, renal dysfunction, cholestasis, active hepatitis, sepsis, concurrent use with other NSAIDs, advanced age (over 65 years), pregnancy (I-II trimester).

    Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min.

    Anamnestic data on the development of gastrointestinal lesions, the presence of infection Helicobacter pylori, long-term use of NSAIDs, severe somatic diseases, concomitant therapy with the following drugs:

    - anticoagulants (for example, warfarin);

    - antiaggregants (eg, acetylsalicylic acid, clopidogrel);

    - oral glucocorticosteroids (for example, prednisolone);

    - selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

    To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

    Pregnancy and lactation:

    It penetrates into breast milk in small amounts. Application in the III trimester of pregnancy and lactation is contraindicated (should be abandoned from feeding for the period of application of the drug); in extreme cases, if you need to use the drug during pregnancy, you should compare the benefit to the mother and the risk to the fetus or the baby.

    Dosing and Administration:

    Inside, in the form of tablets, Ketolac® is used once or repeatedly, depending on the severity of the pain syndrome.

    When administered orally to patients aged 16 to 64 years with a body weight exceeding 50 kg, the recommended dose is 20 mg for the first time, then 10 mg 4 times a day, but not more than 40 mg / day.

    Adult patients with a body weight of less than 50 kg, patients older than 64 years or with renal insufficiency - 10 mg in the first dose and then 10 mg 4 times a day.

    The maximum daily dose for oral administration is 40 mg.

    If administered orally, 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 - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, sensation of stomach overflow; rarely - decreased appetite, nausea, erosive and ulcerative lesions of the digestive 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 thick, "nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

    From the urinary system: rarely acute renal failure, back pain, hematuria, azotemia, hemolytic syndrome (hemolytic anemia, renal insufficiency, 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 central nervous system: 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, fainting.

    From the side of the cardiovascular system: less often - increased blood pressure.

    On the part of the organs of 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, hyperemia, densification or flaking of the skin, enlargement and / or soreness of the tonsils), urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

    Allergic reactions: rarely anaphylaxis or anaphylactoid reactions (skin discoloration, 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 - increased sweating, rarely - swelling of the tongue, fever.

    Overdose:

    Symptoms (with a single administration): abdominal pain, nausea, vomiting, erosive-ulcerative gastrointestinal lesion, impaired renal function, metabolic acidosis.

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

    Interaction:

    Co-administration with paracetamol increases the nephrotoxicity of ketorolac.

    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 appointment with anticoagulants - derivatives of coumarin and indanedione, heparin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet agents, cephalosporins, valproic acid and acetylsalicylic acid - increases the risk of bleeding.

    Reduces the effect of antihypertensive and diuretic drugs (reduces the synthesis of prostaglandin 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 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 its concentration in the plasma.

    Increases the effect of narcotic analgesics.

    Myelotoxic drugs - increased hematotoxicity of the drug.

    Special instructions:

    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, 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, it is especially important for postoperative patients requiring careful control of hemostasis.

    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 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 vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets, film-coated, 10 mg each.

    Packaging:

    For 20 tablets in cans of glass or polymer.

    For 10 tablets in contour non-jawed or contoured cell packs.

    Each jar or 2 contour packs together with instructions for use in the pack.
    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005808/09
    Date of registration:17.07.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:ALTAYVITAMINS, CJSC ALTAYVITAMINS, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspALTAYVITAMINS, CJSCALTAYVITAMINS, CJSC
    Information update date: & nbsp02.01.2018
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