Ketorol Express oral dispersible pills 10mg, 20pcs

Composition

Each tablet dispersed in the oral cavity contains: Active ingredient: ketorolac trometamine (ketorolac trometamol) 10,000 mg; Excipients: microcrystalline cellulose, silicon dioxide, butylhydroxyanisole, mannitol, crospovidone (type A), sucralose, mint flavor, yellow quinoline dye (E 104), magnesium stearate.

Pharmacological action

of NSAIDs, has a pronounced analgesic effect, has an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with non-selective inhibition of COX – COX-1 and COX-2 activity, which catalyzes the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of inflammation, pain, and fever. Ketorolac is a racemic mixture of [- ] S-and [+]R-enantiomers, and the analgesic effect is due to the [-]S-form. The analgesic effect of ketorolac is comparable to morphine, significantly superior to other NSAIDs. The drug does not affect opioid receptors, does not depress respiration, does not cause drug dependence, does not have a sedative and anxiolytic effect. After oral use, the onset of analgesic action is noted in 1 hour, the maximum effect is achieved in 1-2 hours. pharmacokineticabsorption After oral use, ketorolac is well absorbed from the gastrointestinal tract, Cmax in blood plasma (0.7-1.1 mcg / ml) is reached 40 minutes after use on an empty stomach at a dose of 10 mg. Fat-rich foods reduce the Cmax of ketorolac in the blood and delay its achievement by 1 h. Bioavailability – 80-100%. Distribution Binding to plasma proteins is 99%, with hypoalbuminemia, the amount of free substance in the blood increases. The time to reach Css( 0.39-0.79 mcg / ml), with oral use of 10 mg of ketorolac 4 times/day (the dose is higher than the subtherapeutic one), is 24 hours. Vd – 0.15-0.33 l / kg. Penetrates into breast milk:  after the mother takes 10 mg of ketorolac, Cmax in breast milk is reached in 2 hours and is 7.3 ng / ml after the first dose and 7.9 ng / ml after the second dose of the drug. 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-hydroxyketorolac. Excretion: Excreted by the kidneys (91%) and through the intestines (6%). T1 / 2 in patients with normal renal function is 2.4-9 hours after an oral dose of 10 mg. When taken orally at a dose of 10 mg, the total clearance is 0.025 l / h / kg. Pharmacokinetics in special clinical cases in patients with renal insufficiency, the Vd of ketorolac can increase by 2 times, and the Vd of its R-enantiomer by 20%. T1 / 2 increases in elderly patients and decreases in young ones. Liver function disorders do not affect T1/2. In patients with impaired renal function, with a plasma creatinine concentration of 19-50 mg/l (168-442 mmol/l), T1 / 2 is 10.3-10.8 hours, with more severe renal insufficiency-more than 13.6 hours. With oral use at a dose of 10 mg, the total clearance in patients with renal insufficiency (with a plasma creatinine concentration of 19-50 mg/l) is 0.016 l/h / kg. It is not excreted during hemodialysis.

Indications

Severe and moderate pain syndrome:

• injuries;
• toothache;
• pain in the postoperative period;
• cancer;
• myalgia;
• arthralgia;
• neuralgia;
• sciatica;
• dislocations, 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 (including to other NSAIDs);
• 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;
• active gastrointestinal bleeding;
• inflammatory bowel disease (including ulcerative colitis, Crohn’s disease);
• diseases of the bone marrow and blood (leukopenia, including in the anamnesis; thrombocytopenia; hypocoagulation, including hemophilia),
• myelosuppression;
• bleeding or high risk of their development;
• severe renal failure (CC 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;
• lactation;
• children up to age 16 years (safety and efficacy have not been established);
• concurrent use with probenecid;
• concomitant use with pentoxifylline;
• concomitant use with acetylsalicylic acid and other NSAIDs (including selective COX-2 inhibitors);
• concomitant use with lithium salts;
• concomitant use with anticoagulants (including warfarin and heparin).

With caution

Bronchial asthma; presence of factors that increase toxicity to the gastrointestinal tract: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; IHD; cerebrovascular diseases; dyslipidemia/hyperlipidemia; diabetes mellitus; diseases of the peripheral arteries; a history of ulcerative lesions of the gastrointestinal tract; the presence of Helicobacter pylori infection; long-term use of NSAIDs; severe somatic diseases; thyroid diseases; tuberculosis; concomitant use of oral corticosteroids (including prednisone), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); elderly (over 65 years).

Side effects

Determination of the frequency of side effects: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (From the digestive system: often (especially in elderly patients over 65 years of age with a history of erosive and ulcerative lesions of the gastrointestinal tract)-gastralgia, diarrhea; infrequently – stomatitis, flatulence, constipation, vomiting, feeling of fullness of 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 coffee grounds vomiting, nausea, heartburn), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis. From the urinary system: rarely-acute renal failure, low back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, oliguria, polyuria, interstitial nephritis, renal edema; frequency unknown-urinary retention. From the side of the senses: rarely-hearing loss, ringing in the ears, visual disturbances (including blurred vision); frequency unknown-taste disorders. Respiratory system disorders: rarely-bronchospasm or dyspnoea, rhinitis, laryngeal edema (shortness of breath, difficulty breathing). From the central nervous system: often-headache, dizziness, drowsiness; rarely-aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis. From the cardiovascular system: infrequently-increased blood pressure; rarely-pulmonary edema, fainting. Hematopoietic disorders: rare-anemia, eosinophilia, leukopenia. From the side of the hemostatic system:rarely-bleeding from a postoperative wound, nosebleeds, rectal bleeding. From the skin: infrequently-skin rash (including maculopapular rash), purpura; rarely-exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and / or soreness of the palatine tonsils), urticaria, Stevens-Johnson syndrome, Lyell’s syndrome. Allergic reactions: rarely – anaphylaxis or anaphylactoid reactions (discoloration of the skin of the face, skin rash, urticaria, pruritus, tachypnea or dyspnea, edema of the eyelids, edema of the tongue, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing). Other: often-edema (face, legs, ankles, fingers, feet, weight gain); infrequently-increased sweating; rarely-fever; frequency unknown-hyperkalemia, hyponatremia.

Interaction

Concomitant use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium supplements, glucocorticosteroids, ethanol, and corticotropin may significantly increase the risk of adverse reactions, including gastrointestinal ulceration and gastrointestinal bleeding. When ketorolac is co-administered with other NSAIDs (including COX-2 inhibitors), fluid retention, decompensation of cardiac activity, and increased blood pressure may occur. Concomitant use of ketorolac with indirect anticoagulants, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding. Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its concentration in blood plasma and increases its T1 / 2. The combined use of ketorolac with valproate causes a violation of platelet aggregation. When using ketorolac with other nephrotoxic drugs (including gold preparations), the risk of developing nephrotoxicity increases. Combined use with paracetamol increases the nephrotoxicity of ketorolac. Drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in blood plasma. The combined use of ketorolac with methotrexate increases the hepatotoxicity and nephrotoxicity of methotrexate. The combined use of ketorolac and methotrexate is possible only when using low doses of the latter. Methotrexate clearance may decrease (it is necessary to monitor the concentration of methotrexate in blood plasma). When ketorolac is used, it is possible to reduce the clearance of lithium, increase its concentration in blood plasma, and increase the toxic effect of lithium. Concomitant use with lithium salts is contraindicated. Ketorolac reduces the effect of antihypertensive and diuretic drugs (reduces the synthesis of prostaglandins in the kidneys). Ketorolac enhances the effect of narcotic analgesics. When combined with opioid analgesics, the doses of the latter can be significantly reduced. Ketorolac enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs, and therefore it is necessary to recalculate the dose of these drugs. Ketorolac increases plasma concentrations of verapamil and nifedipine. Concomitant use of NSAIDs and mifepristone may reduce the effectiveness of mifepristone. NSAIDs are not recommended for use within 8-12 days after the use of mifepristone. Concomitant use of NSAIDs and cyclosporine increases the risk of nephrotoxicity. Concomitant use of NSAIDs and quinolone antibiotics increases the risk of seizures. Concomitant use of NSAIDs and tacrolimus increases the risk of nephrotoxicity. Concomitant use of NSAIDs and zidovudine increases the risk of developing hematological toxicity. When used concomitantly with digoxin, ketorolac does not interfere with the binding of digoxin to plasma proteins. Therapeutic concentrations of digoxin do not affect the binding of ketorolac to plasma proteins. Antacids do not affect the absorption of ketorolac. Myelotoxic drugs increase the manifestations of ketorolac hematotoxicity.

How to take, course of use and dosage

Put the tablet on your tongue, where it will immediately begin to dissolve. Keep in the mouth for a few seconds until completely dissolved, if desired, you can drink liquid. Taking tablets dispersed in the oral cavity does not require mandatory washing down with water, does not affect the increase in saliva production, and allows patients with deviations in the act of swallowing with behavioral and neurological disorders to take the drug. Ketorol ® Express is administered orally once or repeatedly, depending on the severity of the pain syndrome.A single dose is 10 mg, 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. When taken orally, 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. When switching from parenteral use of the drug to oral use, 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 of age and 60 mg for patients over 65 years of age 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.

Overdose

Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis. Treatment: gastric lavage, use of adsorbents (activated charcoal) and symptomatic therapy (maintenance of vital body functions). Hemodialysis is ineffective.

Special instructions

The choice of dosage form of the drug depends on the severity of the pain syndrome and the patient’s condition. Ketorol® is available in the following dosage forms: gel for external use; film-coated tablets; tablets dispersed in the oral cavity; solution for intravenous and intramuscular use. Before using the drug, it is necessary to find out about a previous allergy to the drug or other NSAIDs. Due to the risk of developing allergic reactions, the first dose is taken under the careful supervision of a doctor. Ketorolac inhibits platelet aggregation and increases blood clotting time. The effect on platelet aggregation stops 24-48 hours after taking the drug. Patients with blood clotting disorders are prescribed the drug only when the number of platelets is constantly monitored, which is especially important in the postoperative period, when careful monitoring of hemostasis is required. Hypovolemia increases the risk of developing nephrotoxic adverse reactions. If necessary, it can be used in combination with narcotic analgesics. Do not use with paracetamol for more than 2 days. The risk of adverse reactions increases with prolongation of the course of treatment and an increase in the oral dose of ketorolac more than 40 mg / day. Concomitant use of ketorolac with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including COX-2 inhibitors), lithium salts, anticoagulants (including warfarin and heparin) is contraindicated. It is contraindicated to use ketorolac for preventive pain relief before and during extensive surgical interventions due to the high risk of bleeding. Ketorolac is not recommended for use as a premedication agent and maintenance anesthesia. When using ketorolac, cases of fluid retention, increased blood pressure and edema have been reported. Caution should be exercised when prescribing to patients with heart failure, arterial hypertension. Concomitant use of ketorolac with other NSAIDs can lead to disorders such as decompensation of heart failure and increased blood pressure. According to clinical studies, the use of certain NSAIDs in high doses may lead to an increased risk of arterial thrombotic complications (for example, myocardial infarction, stroke). Although no such complications have been reported with ketorolac, existing data are insufficient to rule out the risk of such complications. To reduce the risk of developing NSAID-induced gastropathy, the use of antacids, misoprostol, as well as drugs that reduce gastric secretion (histamine H2 receptor blockers, proton pump inhibitors) is recommended. To reduce the risk of adverse events, the minimum effective dose of ketorolac should be used in the shortest possible course. Influence on the ability to drive vehicles and mechanisms During treatment, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Ketorolac

Conditions of release from pharmacies

By prescription

Dosage form

Tablets