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Active ingredients
Ketorolac
Release form
Pills
Composition
Each tablet, coated, contains: Active ingredient: Ketorolaka tromethamine (Ketorolaka trometamol) - 10 mg; Excipients: 121 mg microcrystalline cellulose, 15 mg lactose, 20 mg corn starch, 4 mg colloidal silicon dioxide, 2 mg magnesium stearate, sodium carboxymethyl starch (type A) 15 mg; coating: hypromellose 2.6 mg, propylene glycol 0.97 mg, titanium dioxide 0.33 mg, olive green (quinoline yellow dye 78%, diamond blue 22%) 0.1 mg.
Pharmacological effect
Non-steroidal anti-inflammatory drug (NSAIDs), has a pronounced analgesic effect, has anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with non-selective inhibition of the activity of cyclooxygenase (COX) - COX-1 and COX-2, which catalyzes 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 of [-] S and [+] R enantiomers, while the analgesic effect is due to the [-] S form. The strength of the analgesic effect is comparable with morphine, far superior to other NSAIDs .; The drug does not affect opioid receptors, does not inhibit respiration, does not cause drug dependence, does not have a sedative and anxiolytic effect. After oral administration, the development of an analgesic effect is noted after 1 h.
Pharmacokinetics
When ingested, Ketorolac is well and quickly absorbed in the gastrointestinal tract (GIT). The bioavailability of ketorolac is 80-100%, the maximum concentration (Cmax) after oral administration of 10 mg is 0.82-1.46 mcg / ml, the time to reach the maximum concentration (TCmax) is 10-78 minutes. High-fat food reduces the maximum concentration of the drug in the blood and delays its achievement for an hour. Communication with plasma proteins - 99% .; The time to reach the equilibrium concentration of the drug (Css) by oral administration of 10 mg 4 times a day is 24 hours and the concentration is 0.39-0.79 mcg / ml .; The volume of distribution is 0.15-0.33 l / kg. In patients with renal insufficiency, the volume of distribution of the drug may increase by 2 times, and the volume of distribution of its R-enantiomer - by 20% .; Penetrates into breast milk: when a mother takes 10 mg of ketorolac Cmax in milk is achieved 2 hours after the first dose and is 7.3 ng / ml,2 h after applying the second dose of ketorolac (when using the drug 4 times a day) - 7.9 ng / l; More than 50% of the administered dose is metabolized in the liver to form pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketolac. Excreted in 91% of the kidneys, 6% - through the intestines .; The elimination half-life (T1 / 2) in patients with normal renal function is on average 5.3 h (2.4-9 h after oral administration of 10 mg). T1 / 2 increases in elderly patients and shortens in young. Impaired liver function has no effect on T1 / 2. In patients with impaired renal function, when the concentration of creatinine in the plasma is 19-50 mg / l (168-442 μmol / l), T1 / 2 - 10.3-10.8 h, with more severe renal failure - more than 13.6 h .; When administered orally, 10 mg total clearance is 0.025 l / h / kg; in patients with renal insufficiency (when the concentration of creatinine in the plasma is 19-50 mg / l) - 0.016 l / h / kg. It is not excreted by hemodialysis.
Indications
Pain syndrome of severe and moderate severity: trauma, toothache, pain in the postpartum and postoperative period, cancer, myalgia, arthralgia, neuralgia, sciatica, sprains, sprains, rheumatic diseases. Designed for symptomatic therapy, reducing the intensity of pain and inflammation at the time of use, does not affect the progression of the disease.
Contraindications
hypersensitivity to ketorolac; a complete or incomplete combination of asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history of); erosive and ulcerative changes of the mucous membrane of the stomach and duodenum 12, active gastrointestinal bleeding; cerebrovascular or other bleeding; inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase; hemophilia and other bleeding disorders; decompensated heart failure; liver failure or active liver disease; severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia; the period after coronary artery bypass surgery; lactase deficiency, lactose intolerance, glucose-galactose malabsorption; pregnancy, childbirth, lactation; children up to 16 years old .;
Use during pregnancy and lactation
Contraindicated
Dosage and administration
In the form of pills used orally in a single dose of 10 mg. In case of severe pain syndrome, the drug is taken repeatedly in 10 mg up to 4 times a day, depending on the severity of the pain. The maximum daily dose should not exceed 40 mg. A minimum effective dose should be used. When taken orally, the duration of the course of treatment should not exceed 5 days .; When switching from parenteral administration of the drug to its oral administration, 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 over 65 or with impaired renal function. In this case, the dose of the drug in pills on the day of transition should not exceed 30 mg.
Side effects
The frequency of side effects is classified depending on the frequency of occurrence of the case: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%) , including individual messages .; On the part of the digestive system: often (especially in elderly patients over 65 years old, with a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach; 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 and others), 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, kidney edema .; On the part of the senses: rarely - hearing loss, tinnitus, blurred vision (including blurred visual perception) .; On the part of the respiratory system: rarely - bronchospasm, shortness of breath, rhinitis, laryngeal edema .; From the side of the central nervous system: often - headache, dizziness, drowsiness; rarely, aseptic meningitis (fever, severe headache, cramps, stiff neck and / or back muscles), hyperactivity (mood changes,anxiety), hallucinations, depression, psychosis .; Since the cardiovascular system: less often - increased blood pressure; rarely - pulmonary edema, fainting .; On the part of the blood-forming organs: rarely - anemia, eosinophilia, leukopenia .; On the part of the hemostatic system: rarely - bleeding from a postoperative wound, epistaxis, rectal bleeding .; On the part of the skin: less often - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, hardening or peeling of the skin, swelling and / or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome .; Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (discoloration of the skin, skin rash, urticaria, itchy skin, tachypnea or dyspnea, eyelid edema, periorbital edema, shortness of breath, difficulty breathing, chest heaviness, wheezing) .; Other: often - edema (face, legs, ankles, fingers, feet, weight gain); less often, excessive sweating; rarely - swelling of the tongue, fever.
Overdose
Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, renal dysfunction, metabolic acidosis .; Treatment: gastric lavage, the introduction of adsorbents (activated carbon) and symptomatic therapy (maintaining the vital functions of the body). Not sufficiently eliminated by dialysis.
Interaction with other drugs
The simultaneous use of ketorolac with acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs, calcium supplements, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers of the gastrointestinal tract and the development of gastrointestinal bleeding. Joint appointment with paracetamol increases nephrotoxicity, with methotrexate - hepato-and nephrotoxicity. The joint appointment of ketorolac and methotrexate is possible only when using low doses of the latter (to control the concentration of methotrexate in the blood plasma) .; Probenecid reduces plasma clearance and distribution of ketorolac, increases its concentration in the blood plasma and increases its half-life.Against the background of the use of Ketorolac, the clearance of methotrexate and lithium may be reduced and the toxicity of these substances may increase. Co-administration with indirect anticoagulants, heparin, thrombolytic agents, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding. Reduces the effect of antihypertensives and diuretic drugs (reduced synthesis of prostaglandins in the kidneys). When combined with opioid analgesics, the dose of the latter can be significantly reduced .; Antacids do not affect the completeness of drug absorption .; The hypoglycemic effect of insulin and oral hypoglycemic drugs is increased (dose recalculation is required) .; Joint appointment with valproic acid causes a violation of platelet aggregation. Increases plasma concentration of verapamil and nifedipine .; When administered with other nephrotoxic drugs (including gold medications), the risk of nephrotoxicity increases; 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 pills and injection solution). The choice of the method of administration of the drug depends on the severity of the pain syndrome and the patient's condition .; The risk of the development of drug complications increases with lengthening the treatment time for more than 5 days and increasing the oral dose of the drug more than 40 mg / day. Do not use the drug simultaneously with other NSAIDs .; When taken jointly with other NSAIDs, fluid retention, decompensation of cardiac activity, and an increase in blood pressure may be observed. The effect on platelet aggregation is terminated after 24-48 hours; Patients with impaired blood coagulation are prescribed only with constant monitoring of the number of platelets, it is especially important for postoperative patients requiring careful monitoring of hemostasis .; The drug can change the properties of platelets, but does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases .; To reduce the risk of NSAID-gastropathy, antacid medicines are prescribed, misoprostol, omeprazole; During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.