Composition
Ketorolac (Ketorolac trometamine) – 10.00 mgsupportable substances: microcrystalline cellulose-122.41 mg corn starch-44.76 mg colloidal silicon dioxide (aerosil) – 1.83 mg magnesium stearate-1.00 mg Shell composition: Hypromellose-2.91 mgtitan dioxide-1.25 mgmacrogol 400 (polyethylene glycol 400) – 0.68 mgtalk-0.16 mg
Pharmacological action
Ketorolac has a pronounced analgesic effect, also has an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with non-selective inhibition of cyclooxygenase enzyme activity in peripheral tissues, which results in inhibition of prostaglandin biosynthesis-modulators of pain sensitivity, thermoregulation, and inflammation. Ketorolac does not affect opioid receptors, does not depress breathing, does not cause drug dependence, does not have a sedative and anxiolytic effect. After oral use, the onset of analgesic action is noted, respectively, in 1 hour, the maximum effect is achieved in 1-2 hours.
Indications
Severe to moderate pain syndrome: – injuries; – toothache;- pain in the postpartum and postoperative period;- oncological diseases; – myalgia;- arthralgia; – neuralgia;- sciatica;- dislocations, sprains; – rheumatic diseases.
Contraindications
- Hypersensitivity (including to other non-steroidal anti-inflammatory drugs);
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);
- erosive-ulcerative lesions of the gastrointestinal tract (GIT), active gastrointestinal bleeding;
- inflammatory bowel disease (including ulcerative colitis, Crohn’s disease);
- diseases of the bone marrow and blood (leukopenia, including a history of thrombocytopenia, hypocoagulation (including hemophilia)), myelosuppression, bleeding or high risk of their development;
- severe renal insufficiency (creatinine clearance (CC) of less than 30 ml/min), confirmed hyperkalemia;
- severe hepatic impairment or active liver disease;
- status after conducting coronary artery bypass surgery;
- preventive analgesia before and during extensive surgical interventions due to the high risk of bleeding;
- active cerebrovascular disease (including intracranial hemorrhage or suspected it); pregnancy;
- childbirth;
- the period of breastfeeding; children up to age 16 years (safety and efficacy have not been established);
- concurrent use with probenecid;
- the simultaneous use with pentoxifylline; the simultaneous use with acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (including cyclooxygenase-2 inhibitors);
- concurrent use of lithium salts;
- the simultaneous use of anticoagulants (including warfarin and heparin).
With caution:
Bronchial asthma; presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis; postoperative period; chronic heart failure; edematous syndrome; arterial hypertension; moderate renal failure (creatinine clearance 30-60 ml/min); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; coronary heart disease; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes mellitus * peripheral arterial diseases; a history of gastrointestinal ulcers, the presence of Helicobacter pylori infection; long-term use of NSAIDs; severe somatic diseases; thyroid diseases; tuberculosis; simultaneous use of oral glucocorticosteroids (including prednisone), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); elderly (over 65 years of age).
Side effects
the incidence of adverse events (AES) classified according to the recommendations of the world health organization defined as: very often – at least 10%; often – not less than 1% but < 10%; infrequently – no more than 0.1% but < 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely, including isolated cases – less than 0.01%; frequency unknown (frequency cannot be determined based on available data).
Interaction
Concomitant use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium supplements, glucocorticosteroids, ethanol, or corticotropin may significantly increase the risk of adverse reactions, including the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding.
How to take, course of use and dosage
Inside, once or repeatedly, depending on the severity of the pain syndrome. A single dose is 10 mg (1 tablet), with repeated use it is recommended to take 10 mg up to 4 times a day, depending on the severity of pain. The maximum daily dose should not exceed 40 mg. The duration of the course should not exceed 5 days. To reduce the risk of adverse events, the minimum effective dose of ketorolac should be used in the shortest possible course.
Overdose
Symptoms: abdominal pain, nausea, vomiting, peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis. Treatment: gastric lavage, use of adsorbents (activated charcoal) and symptomatic therapy (maintenance of vital functions in the body). Ketorolac is not sufficiently eliminated by hemodialysis.
Active ingredient
Ketorolac
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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