Ketorol solution for intramuscular injection 30mg/ml in ampoules 1 ml No. 10×1

Name:
Ketorol solution for i / m introduction. 30mg/ml in amp. 1ml in pack. No. 10
Description:
Transparent colorless or pale yellow liquid, in yellow ampoules, 1 ml USP type 1. The main active ingredient Ketorolac Release form 1 ml in yellow glass ampoules with a label, 10 ampoules in a blister pack with a label, one blister packing in a cardboard box with instructions for medical use. On the ampoule, there may be a dot and a red break line. Dosage 30mg/ml in amp. 1ml in pack. №10 Pharmacodynamics Ketorolac, being a non-steroidal anti-inflammatory drug, has an analgesic, antipyretic and anti-inflammatory effect. The mechanism of action at the biochemical level is the inhibition of the cyclooxygenase enzyme, mainly in peripheral tissues, which results in inhibition of the biosynthesis of prostaglandins – modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of the -S and -P enantiomers, with the analgesic effect due to the -S form. The drug does not affect opioid receptors, does not depress respiration, does not inhibit intestinal motility, does not have a sedative and anxiolytic effect, does not cause drug dependence, does not affect the progression of the disease. Ketorolac inhibits platelet aggregation and increases bleeding time. The functional state of platelets is restored within 24-48 hours after discontinuation of the drug. The pharmacokinetics of the bioavailability of ketorolac after oral administration ranges from 80% to 100%. The maximum plasma concentration is reached within 30-60 minutes. The pharmacokinetics of ketorolac under the conditions of prescribing medium therapeutic doses is a linear function. The equilibrium concentration of the drug in plasma is 50% higher than that determined after a single dose. More than 99% of the drug binds to plasma proteins, resulting in an apparent volume of distribution of less than 0.3 l / kg. Ketorolac is metabolized mainly with the formation of conjugated forms of glucuronic acid, which are excreted through the kidneys. Metabolites do not have analgesic activity. The half-life of the drug is on average 5 hours. Indications for use Short-term relief of moderate and severe acute pain in the postoperative period. Treatment should be started only in a hospital, the maximum duration of treatment is 2 days. Dosage and administration Ketorol is intended for intramuscular injection, the drug should not be used for epidural or spinal administration. The solution is injected slowly intramuscularly (deep into the muscle). The onset of the analgesic effect is about 30 minutes with its maximum severity within 1-2 hours, the average duration of analgesia is 4-6 hours. The introduction of the drug several times a day for more than 2 days is not recommended, since in most cases patients do not need longer pain relief therapy, or can be transferred to oral ketorolac. In this case, the duration of the use of ketorolac parenterally and orally should not exceed a total of 5 days. To achieve the maximum analgesic effect in the early postoperative period, it is possible to use ketorolac and narcotic analgesics together, the daily dose of the latter in this case is reduced. Ketorolac has no effect on addiction to opioids and does not increase the respiratory depression or sedation associated with them. Selection and dose adjustment should be made in accordance with the intensity of pain and the response to the administration of the drug. To minimize side effects, it is recommended to use the lowest effective dose for the shortest possible course of treatment. adults; The usually recommended initial dose of Ketorol is 10 mg followed by 10-30 mg every 4-6 hours. In the early postoperative period, it is permissible to administer the drug every 2 hours, if necessary. The maximum daily dose is 90 mg / day. in patients weighing less than 50 kg – no more than 60 mg / day. Elderly patients (over 65): it is recommended to use the drug at the lowest effective dose, the total dose should not exceed 60 mg / day. Due to the higher risk of side effects in this group of patients, the minimum possible duration of treatment is recommended, as well as regular monitoring of the patient’s condition to exclude gastrointestinal bleeding. Children: The safety and efficacy of ketorolac in children have not been established and the drug is not recommended for use in children under 16 years of age. Patients with impaired renal function: the use of ketorolac is contraindicated in patients with severe and moderate renal impairment. In the case of mild renal impairment, the use of Ketorol at a dose of not more than 60 mg / day is acceptable. If necessary, joint parenteral and oral administration of Ketorol, the total daily dose should not exceed 90 mg (60 mg in persons over 65 years of age, with a body weight of less than 50 kg or impaired renal function), while the dose of the drug taken orally should not exceed 40 mg / day. day It is recommended that the patient be transferred to the oral form of the drug as soon as possible. Use during pregnancy and lactation Efficacy and safety have not been established. Drugs that affect the synthesis of prostaglandins, including ketorolac, can cause reduced fertility, and therefore are not recommended for use by women planning pregnancy. The safety of the drug in pregnant women has not been studied. In a study on rats and rabbits at toxic doses, no teratogenic effect was detected. In rats, prolongation of the gestation period and delayed delivery were noted. Due to the known negative effect of NSAIDs on the fetal cardiovascular system (risk of occlusion of the ductus arteriosus), ketorolac is contraindicated in pregnant women. The use of ketorolac during childbirth is not recommended due to the increased risk of bleeding in the mother and child. Ketorolac penetrates into milk, and therefore is not recommended for use during lactation. Precautions Ketorolac can cause severe adverse reactions from the digestive tract at any stage of drug therapy with or without warning symptoms, such adverse reactions can be fatal. The risk of serious gastrointestinal bleeding is dose dependent, but side effects may occur even with short therapy. In addition to a history of peptic ulcer, provoking factors are the simultaneous use of oral corticosteroids, anticoagulants, long-term therapy with non-steroidal anti-inflammatory drugs, smoking, drinking alcohol, and old age. If you suspect the development of adverse reactions from the gastrointestinal tract, ketorolac should be canceled. NSAIDs should be used with caution in patients with Crohn’s disease and a history of ulcerative colitis due to the possibility of worsening the course of the disease. Ketorolac inhibits platelet aggregation and prolongs bleeding time, platelet function returns to normal within 24-48 hours after discontinuation of the drug. In patients receiving anticoagulant therapy, the use of ketorolac may increase the risk of bleeding. Patients who are already taking anticoagulants or who require low-dose heparin should not receive ketorolac. In patients taking other drugs that affect hemostasis, ketorolac should be used with caution. In patients who underwent surgery with a high risk of bleeding or incomplete hemostasis, ketorolac should not be used. Like other NSAIDs, ketorolac inhibits prostaglandin synthesis and may have a toxic effect on the kidneys, so it should be used with caution in patients with impaired renal function or a history of kidney disease. The risk group includes patients with impaired renal function, hypovolemia, heart failure, impaired liver function, patients who use diuretics, and elderly patients. Fluid retention, sodium chloride, hypertension, oliguria and peripheral edema have been observed in some patients taking NSAIDs, including ketorolac, therefore it should be used with caution in patients with hypertension, heart failure, before administration of the drug, fluid and electrolyte imbalance should be corrected. Clinical studies and epidemiological data suggest that the use of some NSAIDs, especially at high doses and for a long time, may be associated with an increased risk of arterial thrombotic complications such as myocardial infarction or stroke. It is impossible to exclude such a risk for Ketorolac. To minimize the potential risk of developing adverse cardiovascular events in patients using NSAIDs, the lowest effective dose should be used for the shortest possible period of time. Ketorolac should only be administered to patients with uncontrolled hypertension, congestive heart failure, established ischemic heart disease, peripheral arterial and/or cerebrovascular disease after a thorough assessment of all the advantages and disadvantages of such treatment. Ketorolac should be used with caution in patients with impaired liver function or a history of liver disease. Significant increases (more than three times normal) in serum ALT and ACT were observed in controlled clinical trials in less than 1% of patients. In addition, isolated cases of severe hepatic reactions have been reported, including jaundice, fulminant hepatitis, hepatic necrosis and liver failure, in some cases fatal. If signs of impaired liver function appear, ketorolac should be discontinued. The use of the drug in patients with systemic lupus erythematosus or connective tissue diseases may be associated with an increased risk of developing aseptic meningitis. There have been reports of serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. The highest risk of these reactions exists at the beginning of treatment. It was reported about the development of serious anaphylactic and anaphylactoid reactions, such as bronchospasm, laryngeal edema, angioedema, anaphylactic shock. Ketorolac should not be used in patients with bronchial asthma, nasal polyp syndrome, bronchospasm, angioedema in history. If a rash or other manifestations of hypersensitivity appear, treatment with the drug should be discontinued. This medicinal product contains a small amount of ethanol (ethyl alcohol), i.e. less than 100 mg in 1 ml, the sodium content in the medicinal product is less than 1 mmol (23 mg) in 1 ml. Appointment to patients with impaired liver function: administered with caution. While taking ketorolac, an increase in the level of liver enzymes is possible. In the presence of functional abnormalities in the liver while taking ketorolac, a more severe pathology may develop. If signs of liver pathology are detected, treatment should be discontinued. Patients with renal insufficiency or a history of kidney disease: Ketorolac is prescribed with caution. Appointment to elderly patients: since patients of this age group often develop adverse reactions, the minimum effective dose should be used (daily therapeutic dose of not more than 60 mg for patients over 65 years of age). Interaction with other drugs Ketorolac slightly reduces the degree of binding to warfarin proteins. In vitro studies have shown the effect of therapeutic doses of salicylates on the degree of binding of ketorolac to plasma proteins downward from 99.2% to 97.5%. When combined with furosemide, its diuretic effect may be reduced by approximately 20%. Probenecid reduces plasma clearance and volume of distribution of ketorolac increases its concentration in blood plasma and increases its half-life. Against the background of the use of ketorolac, a decrease in the clearance of methotrexate and lithium and an increase in the toxicity of these substances are possible. A possible interaction of ketorolac and non-depolarizing muscle relaxants, leading to the development of apnea, was noted. It is possible that concomitant use with ACE inhibitors may increase the risk of impaired renal function. Rare cases of the development of convulsive seizures have been described when Ketorolac is combined with anticonvulsants (phenytoin, carbamazepine). Perhaps the occurrence of hallucinations against the background of the simultaneous administration of ketorolac and psychostimulant drugs (fluoxetine, thiothixene, alprazolam). The simultaneous use of ketorolac and NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided due to an increased risk of serious adverse reactions. Ketorolac inhibits platelet aggregation, reduces the concentration of thromboxane and prolongs bleeding time. Platelet function returns to normal within 24-48 hours after discontinuation of ketorolac. Although studies do not indicate a significant interaction between ketorolac and anticoagulants, the concomitant use of ketorolac and therapeutic doses of warfarin, prophylactic doses of heparin (2500-5000 units over 12 hours) and dextrans may be associated with an increased risk of bleeding. NSAIDs should not be used within 8 to 12 days of mifepristone administration due to a possible reduction in the effect of mifepristone. The simultaneous use of ketorolac with pentoxifylline increases the risk of bleeding. As with other NSAIDs, caution should be exercised when co-administered with corticosteroids due to an increased risk of gastrointestinal ulceration or bleeding. Ketorolac has been shown to reduce the need for opioid analgesics when used to relieve postoperative pain. Patients who take quinolines at the same time may be at increased risk of seizures. The simultaneous use of NSAIDs with zidovudine leads to an increased risk of hematological toxicity. There is an increased risk of nephrotoxicity when NSAIDs are co-administered with tacrolimus or cyclosporine. NSAIDs can worsen heart failure, reduce glomerular filtration rate, and increase plasma levels of cardiac glycosides when used together. Incompatibility Ketorolac solution for injection should not be mixed in small containers (for example, in one syringe) with morphine sulfate, meperidine hydrochloride, promethazine hydrochloride or hydroxyzine hydrochloride, as this may precipitate ketorolac. Contraindications Bronchial asthma, Complete or partial nasal polyp syndrome, bronchospasm, angioedema in history. Peptic ulcer of the stomach and duodenum during an exacerbation, as well as a history of ulcers or gastrointestinal bleeding, the presence or suspicion of gastrointestinal bleeding. History of blood clotting disorders, conditions with a high risk of bleeding, hemorrhagic diathesis, coagulopathy, hemorrhagic stroke, intracranial bleeding, simultaneous use with anticoagulants (including warfarin, low doses of heparin). Surgical interventions with a high risk of bleeding or the risk of incomplete bleeding. Moderate and severe renal failure (plasma creatinine more than 50 mg / l), risk of renal failure, hypovolemia, dehydration. Pregnancy, childbirth and lactation. Hypersensitivity to ketorolac, aspirin, other NSAIDs or any component of the drug. Simultaneous use of other NSAIDs (risk of summation of side effects) Age up to 16 years Congestive heart failure The drug is not used for pain relief before and during surgery. Ketorolac is not used for epidural and intrathecal injections. Severe liver failure. Joint use with lithium preparations, pentoxifylline probenecid. Epidural or intrathecal administration of the drug is contraindicated. Composition Each ampoule contains ketorolac tromethamine 30 mg, as well as excipients: ethyl alcohol 95% 0.125 ml, sodium chloride 4.35 mg, disodium EDTA 1.0 mg, octoxynol 0.07 mg, sodium hydroxide 0.725 mg, propylene glycol 400 mg, water for injection up to 1 ml Ketorolac with single or repeated use is usually manifested by pain in the abdomen, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, hyperventilation, metabolic acidosis, these symptoms are cured after discontinuation of the drug. In these cases, gastric lavage, the introduction of adsorbents (activated charcoal) and symptomatic therapy are recommended. Ketorolac is not sufficiently eliminated by dialysis. Side effectsGastrointestinal tract: anorexia, discomfort in the abdomen, feeling of stomach fullness, nausea, dyspepsia, gastrointestinal pain, epigastric pain, diarrhea, flatulence, belching, vomiting, constipation, erosive and ulcerative changes, bleeding and perforation gastrointestinal tract (sometimes fatal), vomiting of blood, blood in the feces, gastritis, peptic ulcer, pancreatitis, ulcerative stomatitis, esophagitis, exacerbation of Crohn’s disease and colitis. From the side of the liver and biliary tract: abnormal liver function, liver failure, jaundice, hepatitis, hepatomegaly, increased activity of hepatic transaminases. From the nervous system: headache, dizziness, fainting, fatigue, weakness, irritability, feeling of dry mouth, increased thirst, mood changes, anxiety, impaired concentration, euphoria, nervousness, confusion, paresthesia, unusual dreams, depression, drowsiness, sleep disturbance, insomnia, hallucinations, agitation, hyperkinesia, convulsions, pathological thoughts, aseptic meningitis, neck stiffness, anxiety, vertigo, disorientation, thinking disorder. From the senses: a violation of taste sensations, blurred vision, optic neuritis, tinnitus, hearing loss and loss. From the musculoskeletal system: myalgia. From the urinary system: pain at the site of the projection of the kidneys, dysuria, frequent urination, oliguria, hematuria, proteinuria, increased levels of urea and creatinine in the blood serum, hyponatremia, hyperkalemia, urinary retention, renal failure, interstitial nephritis, papillary necrosis, nephrotic syndrome, hemolytic uremic syndrome. From the side of the cardiovascular system: pallor, hyperemia, chest pain, palpitations, bradycardia, heart failure, arterial hypertension, edema. Data from clinical and epidemiological studies suggest that the use of some NSAIDs, especially at high doses and for a long time, may be associated with an increased risk of developing arterial thromboembolic complications (myocardial infarction or stroke). On the part of the blood: purpura, leukopenia, eosinophilia, neutropenia, agranulocytosis, aplastic anemia, hemolytic anemia, thrombocytopenia, a decrease in the rate of blood clotting, the occurrence of hemorrhages under the skin, hematomas, nosebleeds, prolongation of bleeding time, increased bleeding of postoperative wounds. On the part of the respiratory system: shortness of breath, tachypnea, bronchospasm, complication of asthma, pulmonary edema. From the reproductive system: infertility (in women). From the skin: itching, urticaria, photosensitivity, Lyell’s syndrome, exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome, skin rashes, including maculopapular and weeping, discoloration of the skin of the face. Allergic reactions: anaphylactic and anaphylactoid reactions, urticaria, bronchospasm, laryngeal edema, angioedema, eyelid edema, periorbital edema, exfoliative dermatitis, bullous dermatosis. On the part of the body as a whole: general malaise, swelling, fever, excessive sweating, weight gain; pain, swelling and hyperemia at the injection site. To prevent possible side effects, one should strive to use the minimum effective doses of the drug, strictly observe the established dosages and administration regimens, take into account the patient’s condition (age, concomitant diseases, liver and kidney function, the state of water-electrolyte metabolism and the hemostasis system), as well as possible drug interactions. with combination therapy. Storage conditionsKeep in a place protected from light at temperatures up to 25°C. Keep out of reach of children. Buy Ketorol solution for intramuscular injection 30mg/ml in ampoules 1 ml No. 10×1 Price for Ketorol solution for intramuscular injection 30mg/ml in ampoules 1 ml No. 10×1 m injection 30mg/ml in 1 ml ampoules No. 10×1