Ketorol injection for 30mg ml ampoules 1ml N10
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Active ingredients
Ketorolac
Release form
Solution
Composition
1 ml of solution contains: active ingredient: Ketorolaka tromethamine (Ketorolaka trometamol) 30 mg; excipients: octoxynol 0.07 mg, disodium edetate 1 mg, sodium chloride 4.35 mg, ethanol 0.115 ml, propylene glycol 400 mg, sodium hydroxide 0.725 mg, water for injection up to 1 ml.
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 cyclooxygenase (COX) activity, 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.
Pharmacokinetics
The pharmacokinetics of ketorolac after a single and multiple intravenous and intramuscular administration is linear .; With intramuscular administration, absorption is complete and rapid. The maximum concentration of the drug (Cmax) after intramuscular injection of 30 mg - 1.74-3.1 mcg / ml, 60 mg - 3.23-5.77 mcg / ml, the time to reach the maximum concentration (TCmax) - 15-73 minutes and 30-60 min, respectively. Cmax after intravenous administration of 15 mg - 1.96-2.98 μg / ml, 30 mg - 3.69-5.61 μg / ml, TCmax - 0.4-1.8 min and 1.1-4.7 min, respectively. Communication with plasma proteins - 99%. The time to reach the equilibrium concentration of the drug (Css) with parenteral administration of 30 mg 4 times a day - 24 hours; with intramuscular administration, 15 mg - 0.65–1.13 μg / ml, 30 mg - 1.29-2.47 μg / ml .; The volume of distribution (Vd) for intramuscular injection - 0.136-0.214 l / kg, with intravenous - 0.166-0.254 l / kg. In patients with renal insufficiency, the distribution of the drug can be doubled, and the distribution of its R-enantiomer - by 20% .; Penetrates into breast milk: when mother takes 10 mg of ketorolac Cmax in milk is reached 2 hours after taking the first dose and amounts to 7.3 ng / ml, 2 hours after applying the second dose of ketorolac (using the drug 4 times a day) - 7 , 9 ng / l.About 10% of ketorolac passes through the placenta .; 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 the pharmacologically inactive p-hydroxyketolac. Excreted in 91% of the kidneys, 6% - through the intestines .; The half-life (T1 / 2) in patients with normal renal function is 3.5-9.2 h after parenteral administration of 30 mg. T1 / 2 increases in elderly patients and shortens in young. Changes in liver function have 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 .; With the introduction of 30 mg of ketorolac intramuscularly, the total clearance is 0.023 l / h / kg (0.019 l / h / kg in elderly patients); in patients with renal insufficiency (when the concentration of creatinine in the plasma is 19-50 mg / l) - 0.015 l / h / kg. With the introduction of 30 mg ketorolaka intravenous total clearance of 0.03 l / h / kg.; It is not excreted by hemodialysis.
Indications
Pain syndrome of strong and moderate severity of various origin with injuries, toothache, pain in the postoperative period, with cancer and rheumatic diseases, myalgia, arthralgia, neuralgia, radiculitis. Designed for symptomatic therapy, reducing pain and inflammation at the time of use. The progression of the disease is not affected.
Contraindications
hypersensitivity to ketorolac; complete or incomplete combination of bronchial 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 postoperative period after coronary artery bypass surgery; pregnancy, childbirth, lactation; children's age up to 16 years (safety and efficiency are not established) .;
Use during pregnancy and lactation
Contraindicated
Dosage and administration
Intravenous, intramuscularly .; The solution of the drug Ketorol is used in the minimum effective doses, selected in accordance with the intensity of pain. If necessary, you can simultaneously appoint narcotic analgesics in reduced doses .; When parenteral use in patients from 16 to 64 years old with a body weight exceeding 50 kg, no more than 60 mg is administered intramuscularly (taking into account oral administration). Usually, 30 mg every 6 hours; intravenous - 30 mg (not more than 15 doses for 5 days). Intramuscularly to adult patients with a body weight of less than 50 kg or with chronic renal insufficiency (CRF), a single dose of not more than 30 mg is administered (taking into account oral administration); usually 15 mg (not more than 20 doses in 5 days); intravenously - no more than 15 mg every 6 hours (no more than 20 doses in 5 days) .; The maximum daily doses for intramuscular and intravenous administration are for patients from 16 to 64 years old with a body weight exceeding 50 kg - 90 mg / day; adult patients with a body weight of less than 50 kg or with CKD, as well as older patients (over 65 years) - for intramuscular and intravenous administration of 60 mg. The duration of treatment should not exceed 5 days; When administered intravenously, the dose must be administered in no less than 15 seconds. Intramuscular injection is carried out slowly, deep into the muscle. The onset of the analgesic effect is noted after 30 minutes, maximum analgesia occurs within 1-2 hours. The analgesic effect lasts about 4-6 hours.
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, impaired vision (including blurred visual perception) .; On the part of the respiratory system: rarely - bronchospasm, rhinitis, 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, 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 .; Local reactions: less often - burning or pain at the injection site .; Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (discoloration of the skin, skin rash, urticaria, itchy skin, shortness of breath, eyelid edema, periorbital edema, difficulty breathing, chest pain, 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 NSAIDs, calcium, glucocorticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding .; Do not use the drug simultaneously with other NSAIDs .; 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 narcotic 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 (a 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 a solution for intravenous and intramuscular administration). The choice of the method of drug administration depends on the severity of the pain syndrome and the patient's condition Before the appointment of the drug is necessary to clarify the question of a previous allergic reaction to the drug or NSAIDs. Due to the risk of allergic reactions, the first dose is administered under the close supervision of a physician .; Hypovolemia increases the risk of nephrotoxic adverse reactions .; If necessary, you can assign in combination with narcotic analgesics .; It is not recommended to use as a drug for sedation, maintenance of anesthesia during large surgical interventions .; 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 ceases after 24–48 hours; The drug can change the properties of platelets, but does not replace the preventive action of acetylsalicylic acid in cardiovascular diseases .; 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 risk of developing drug complications increases with prolongation of treatment (in patients with chronic pain) and increasing the dose of the drug more than 90 mg / day; To reduce the risk of NSAID-gastropathy, misoprostol and omeprazole are prescribed .; 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.