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

    1 tablet contains:

    active substance: ketorolac (ketorolac tromethamine) 10 mg;

    Excipients: core - cellulose microcrystalline 120 mg, lactose (milk sugar) 69 mg, magnesium stearate 1 mg; shell - hypromellose (hydroxypropylmethylcellulose) 2.5 mg, talc 0.84 mg, titanium dioxide 0.83 mg, macrogol-6000 (polyethylene oxide-6000) 0.83 mg.

    Description:

    The tablets covered with a film membrane of white color, round, biconcave. On the cut is white or almost white.

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

    M.01.A.B.15   Ketorolac

    Pharmacodynamics:

    Ketalgin® (ketorolac) is a non-steroidal anti-inflammatory drug (NSAID). Ketorolac has a pronounced analgesic effect, has also an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with nonselective inhibition of cyclooxygenase activity (COX1 and COX2), catalyzing the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever.Due to the strength of the analgesic effect, it is comparable with morphine, it is significantly superior to other NSAIDs.

    After oral administration, the beginning of the analgesic effect is observed after 1 hour, the maximum effect is achieved in 2-3 hours.

    Pharmacokinetics:

    Absorption at intake - fast, bioavailability - 80-100%. The maximum concentration in blood Cmax after oral administration of 10 mg - 0.82-1.46 μg / ml, the time to reach the maximum concentration of Tcmax - 10-78 min. The connection with plasma proteins is 99%. Time to reach the stationary (equilibrium) concentration Css when administered orally - 24 hours when administered 4 times a day (above the sub-therapeutic) and 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 distribution of the drug can be increased 2-fold, and the volume of its distribution R-enantiomer by 20%.

    The drug penetrates into breast milk: when taking the mother 10 mg ketorolac CmOh in milk is achieved 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) and is 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 kidneys, and hydroxyketorolac.

    The drug is 91% kidney, 6% - through the intestines. Half-life T1/2 in patients with normal renal function averages 5.3 hours (2.4-9 hours after oral administration of 10 mg). T1/2 increases in elderly patients and is shortened in young people. The function of the liver 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 is 10.3-10.8 hours, with more severe renal failure - more than 13.6 hours.

    The total clearance is 10 mg - 0.025 l / kg / h when taken orally; 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 / kg / h.

    The drug 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.

    Contraindications:

    Hypersensitivity to ketorolac or auxiliary substances, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (including history), hypovolemia (regardless of the cause), erosive and ulcerative lesions gastrointestinal tract in the acute stage, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation, blood loss (including hemophilia), bleeding or high risk of their development, decompensated heart failure, severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia, a period after aortocoronary bypass surgery, lactose intolerance , lactase deficiency or glucose-galactose malabsorption, severe hepatic insufficiency or active liver disease, pregnancy (III trimester), childbirth and the period of breastfeeding tions, children under 16 years of age (safety and efficacy have not been established).

    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.

    Carefully:

    Hypersensitivity to other NSAIDs, ischemic heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia, diabetes, peripheral arterial disease, smoking, kidney failure (creatinine clearance less than 60 ml / min), bronchial asthma, cholecystitis; postoperative period, arterial hypertension, active hepatitis, sepsis, systemic lupus erythematosus, pregnancy (I and II trimesters), anamnestic data on ulcerative lesions of the gastrointestinal tract, presence of Helicobacter pylori infection, elderly age (over 65), simultaneous reception with others NSAIDs, prolonged use of NSAIDs, frequent alcohol use, severe physical illness, concomitant therapy with the following drugs: antiplatelet agents (eg clopidogrel), oral glucocorticosteroids (eg, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).

    If you have any of the diseases / conditions listed in this section, be sure to consult a doctor before taking the drug.

    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:

    Ingestion. The maximum daily dose for oral administration is 40 mg. The duration of treatment should not exceed 5 days.

    When administered orally to patients aged 18 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 or with renal insufficiency, elderly patients - 10 mg in the first dose and then 10 mg 4 times a day.

    A minimum effective dose should be used with the minimum possible short course.
    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 gastrointestinal 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 by type "coffee grounds", nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

    From the urinary system: rarely - acute renal failure, back pain, hematuria, azotemia, hemolytic uraemic syndrome (hemolytic anemia, renal failure, 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 side of the central nervous system: often - headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, convulsions, neck and / or neck stiffness), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis.

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

    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, redness, densification or flaking of the skin, swelling and / or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome .

    Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (skin discoloration of the face, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, wheezing).

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

    Overdose:

    Symptoms (with a single administration): abdominal pain, nausea, vomiting, erosive-ulcerative lesions of the gastrointestinal tract, 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. It is inadmissible simultaneous use with probenecid, pentoksifillinom, lithium salts (see section "Contraindications").

    Admission with acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), hydrocorticosteroids, ethanol, corticotropin, preparations of Ca2+ 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, warfarin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet drugs, cephalosporins, valproic and acetylsalicylic acid increases the risk of bleeding.

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

    Assignment together with methotrexate when using low doses of the latter and monitoring its concentration in the plasma).

    At appointment with other nefrotoksicnymi preparations (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.
    Special instructions:

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

    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 means for premedication, maintenance of anesthesia.

    When combined with other NSAIDs, fluid retention, cardiac decompensation, and hypertension 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 drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

    The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.

    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. To reduce the risk of developing PPA-gastropathy antacids are prescribed, misoprostol, omeprazole.

    The drug is not used for preventive analgesia before and during extensive surgery because of the high risk of bleeding (see section "Contraindications").
    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, one 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:Tablets, film-coated, 10 mg.
    Packaging:

    For 10 or 20 tablets in a contour mesh package.

    1, 2 or 3 contour squeeze packs together with instructions for use in a pack of cardboard.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001934
    Date of registration:23.06.2010 / 11.09.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp02.01.2018
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