Ketorolac tablets p/o 10mg №10×2

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Ketorolac tablets 10mg per cell. pack No. 10×2
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Film-coated tablets, white, with a biconvex surface. The main active ingredient Ketorolac Release form tablets Dosage 10 mg Pharmacological properties Pharmacodynamics Non-steroidal anti-inflammatory drug (NSAID), 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 the activity of COX1 and COX2, which catalyze the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs. After oral administration, the onset of analgesic action is noted after 1 hour, the maximum effect is achieved after 2-3 hours. Pharmacokinetics Absorption After oral administration, ketorolac is well absorbed from the gastrointestinal tract. The maximum concentration (Cmax) in blood plasma is reached 40 minutes after taking the drug on an empty stomach at a dose of 10 mg and is 0.7–1.1 μg / ml. Fat-rich food reduces the Cmax of ketorolac in the blood and delays the time to reach Cmax by 1 hour. Distribution Plasma protein binding is 99%. With hypoalbuminemia, the amount of free substance in the blood increases. The time to reach equilibrium concentration (Css) when administered orally at a dose of 10 mg 4 times a day is 24 hours. Penetrates into breast milk. Metabolism More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides and p-hydroxyketorolac. Withdrawal Excreted by the kidneys (91%) and through the intestines (6%). Glucuronides are excreted in the urine. T? in patients with normal renal function, it averages 5.3 hours (2.4–9 hours after oral administration at a dose of 10 mg). The total clearance is at a dose of 10 mg – 0.025 l / kg / h. Pharmacokinetics in special clinical situations In patients with renal insufficiency, Vd of ketorolac may increase by 2 times, and Vd of the R-enantiomer by 20%. T? lengthens in older patients and shortens in younger patients. Liver function does not affect T?. In patients with impaired renal function at a plasma creatinine concentration of 19–50 mg/l (168–442 µmol/l) T? is 10.3-10.8 hours, with more severe renal failure – more than 13.6 hours. The total clearance in patients with renal insufficiency at a plasma creatinine concentration of 19-50 mg / l at a dose of 10 mg – 0.016 l / kg /h Not excreted by hemodialysis. Ketorolac 10 mg film-coated tablets are used for the short-term treatment of acute pain (including postoperative pain) of moderate intensity, only as a continuation of previous parenteral (intramuscular) therapy in a hospital setting, if necessary. The total duration of parenteral and oral therapy with ketorolac should not exceed 5 days. Dosage and administration Tablets are preferably taken during or after meals. The drug is recommended only for short-term use (up to 5 days). In order to minimize side effects, the drug should be used at the lowest effective dose for the shortest period of time necessary to control symptoms. Before starting treatment, it is necessary to achieve normovolemia. For adults, Ketorolac is prescribed 10 mg every 4 to 6 hours as needed. It is not recommended to use the drug in doses that exceed 40 mg per day. Opioid analgesics (eg, morphine, pethidine) can be used in parallel, ketorolac does not affect the binding of opioid drugs and does not increase the respiratory depression or sedation that is characteristic of opioids. For patients who receive parenteral ketorolac and who are prescribed ketorolac orally in tablet form, the total combined daily dose should not exceed 90 mg (60 mg for the elderly, patients with impaired renal function and patients weighing less than 50 kg) , and the dosage of the oral form of the drug should not exceed 40 mg per day, if the use of the drug release form is changed. Patients should be switched to oral administration of the drug as soon as possible. Elderly Patients Elderly patients have a higher risk of developing severe complications, particularly in the digestive tract. During treatment with NSAIDs, you should regularly monitor the patient’s condition, usually a longer interval between the use of the drug is recommended, for example 6-8 hours. Use during pregnancy and lactation The safety of ketorolac during pregnancy in humans has not been established. Given the known effect of NSAIDs on the fetal cardiovascular system (risk of premature closure of the ductus arteriosus), ketorolac is contraindicated during pregnancy, labor and childbirth. The onset of labor may be delayed and the duration prolonged, with an increased tendency for both mother and child to bleed. Ketorolac is excreted in breast milk in small amounts, so the drug is contraindicated during lactation. Precautions The maximum duration of treatment should not exceed 5 days. Effects on fertility The use of ketorolac, as with any drug that inhibits cyclooxygenase/prostaglandin synthesis, may impair fertility and is not recommended for use in women who plan to become pregnant. For women who are unable to conceive or are undergoing fertility tests, discontinuation of ketorolac should be considered. Gastrointestinal bleeding, ulceration, and perforation Gastrointestinal bleeding, ulceration, or perforation, which can be fatal, has been reported with NSAID use at any time during treatment, with or without warning symptoms, or in severe gastrointestinal disorders. tract in history. The risk of developing severe gastrointestinal bleeding depends on the dosage of the drug. This, in particular, applies to elderly patients who use ketorolac in an average daily dose above 60 mg. For these patients, as well as for patients who are simultaneously using low doses of acetylsalicylic acid or other drugs that may increase the risk to the digestive tract, combination treatment with protective agents (for example, misoprostol or proton pump inhibitors) should be considered. Ketorolac should be used with caution in patients receiving concomitant medications that may increase the risk of ulceration or bleeding, such as oral corticosteroids, selective serotonin reuptake inhibitors, or antiplatelet agents such as acetylsalicylic acid. In the event of gastrointestinal bleeding or ulceration in patients receiving Ketorolac, the course of treatment should be discontinued. Impaired respiratory function Caution is required when using the drug in patients with bronchial asthma (or with a history of asthma), since it has been reported that NSAIDs in such patients accelerate the onset of bronchospasm. Effects on the kidneys Inhibitors of prostaglandin biosynthesis (including NSAIDs) have been reported to have nephrotoxic effects. With caution, the drug is prescribed to patients with impaired renal function, heart, liver, since the use of NSAIDs can lead to a deterioration in kidney function. Patients with mildly impaired renal function are prescribed lower doses of ketorolac (those that do not exceed 60 mg per day intramuscularly or intravenously), and the condition of the kidneys in such patients should be carefully monitored. As with other drugs that inhibit prostaglandin synthesis, there have been reports of increases in serum urea, creatinine and potassium while taking ketorolac tromethamine, which can occur after taking a single dose. Cardiovascular, renal and hepatic disorders Caution is advised in patients with conditions that result in decreased blood volume and/or renal blood flow when renal prostaglandins play a supportive role in renal perfusion. In these patients, renal function should be monitored. The decrease in volume should be corrected and the serum urea and creatinine levels, as well as the volume of urine that is excreted, should be carefully monitored until the patient becomes normovolemia. In patients on renal dialysis, the clearance of ketorolac was reduced by approximately half of the normal rate, and the terminal half-life increased by approximately three times. Patients with impaired liver function due to cirrhosis had no clinically significant changes in ketorolac clearance or terminal half-life. Marginal increases in values may be observed on one or more liver function tests. These abnormalities may be temporary, may remain unchanged, or may progress with continued treatment. If clinical signs and symptoms indicate the development of liver disease or if systemic manifestations are observed, Ketorolac should be discontinued. Fluid retention and edema Fluid retention and edema have been reported during the use of ketorolac, so it should be administered with caution to patients with cardiac decompensation, hypertension or similar conditions. Cardiovascular and cerebrovascular effects There is currently insufficient information to evaluate this risk for ketorolac tromethamine. Patients with uncontrolled arterial hypertension, congestive heart failure, diagnosed coronary heart disease, peripheral arterial disease and / or cerebrovascular disease should be under medical supervision. Systemic lupus erythematosus and mixed connective tissue diseases Patients with systemic lupus erythematosus and various mixed connective tissue diseases have an increased risk of developing aseptic meningitis. Dermatological Ketorolac should be discontinued at the first sign of skin rash, mucosal lesions, or any other sign of hypersensitivity. Anaphylactic (anaphylactoid) reactions As with other NSAIDs, anaphylactic (anaphylactoid) reactions (including anaphylaxis, bronchospasm, hyperemia, rash, arterial hypotension, laryngeal edema, angioedema) may occur in patients with a history of absent or present hypersensitivity to aspirin, other NSAIDs or ketorolac. This complex of symptoms can also be observed in individuals who have a history of bronchospastic reactivity (eg, asthma) and nasal polyps. Anaphylactoid reactions such as anaphylaxis can be fatal. Therefore, ketorolac should not be taken in patients with a history of asthma and in patients with complete or partial nasal polyp syndrome, angioedema, and bronchospasm. If anaphylactoid reactions occur, seek emergency medical attention. Hematological effects Ketorolac should not be administered to patients with bleeding disorders. Patients receiving anticoagulant therapy may have an increased risk of bleeding if ketorolac is used concomitantly. The condition of patients who receive other drugs that can affect the rate of bleeding should be carefully monitored when prescribing ketorolac to them. In controlled clinical trials, the incidence of significant postoperative bleeding was less than 1%. Ketorolac inhibits platelet aggregation and prolongs bleeding time. In patients with normal bleeding time, the duration of bleeding increased, but did not go beyond the normal range of values of 2–11 minutes. In contrast to the long-term effect as a result of the use of acetylsalicylic acid, platelet function returns to normal within 24-48 hours after the withdrawal of ketorolac. Ketorolac should not be given to patients who have undergone surgery with a high risk of bleeding or incomplete bleeding. Caution should be exercised if mandatory bleeding control is critical. Ketorolac is not an anesthetic and has no sedative or anxiolytic properties, therefore it is not recommended as a pre-operative premedication to maintain anesthesia. Interaction with other drugs Ketorolac readily binds to plasma proteins (mean value 99.2%), and the degree of binding depends on the concentration. Due to the possibility of side effects, ketorolac should not be administered with other NSAIDs, including selective cyclooxygenase-2 inhibitors, or in patients receiving acetylsalicylic acid, warfarin, lithium, probenecid, cyclosporine. NSAIDs should not be given within 8 to 12 days after mifepristone use, as NSAIDs may reduce the effect of mifepristone. Drugs in combination with ketorolac should be administered with caution. In healthy subjects with normovolemia, ketorolac reduces the diuretic effect of furosemide by approximately 20%, therefore, the drug is prescribed with particular caution in patients with cardiac decompensation. NSAIDs may exacerbate heart failure, decrease glomerular filtration rate, and increase plasma levels of cardiac glycosides when administered concomitantly with cardiac glycosides. Ketorolac and other non-steroidal anti-inflammatory drugs may weaken the effect of antihypertensive drugs. In the case of simultaneous use of ketorolac with ACE inhibitors, there is an increased risk of impaired renal function, especially in patients with a reduced blood volume in the body. There is a possible risk of nephrotoxicity if NSAIDs are co-administered with tacrolimus. Co-administration with diuretics may lead to a weakening of the diuretic effect and an increased risk of NSAID nephrotoxicity. As with all NSAIDs, concomitant corticosteroids should be used with caution due to an increased risk of gastrointestinal ulceration or bleeding. There is an increased risk of gastrointestinal bleeding if NSAIDs are given in combination with antiplatelet agents and selective serotonin reuptake inhibitors. Caution is advised if methotrexate is given concomitantly, as some prostaglandin synthesis inhibitors have been reported to reduce the clearance of methotrexate and therefore possibly increase its toxicity. Patients taking NSAIDs and quinolones may be at an increased risk of developing seizures. The simultaneous use of NSAIDs with zidovudine leads to an increased risk of hematological toxicity. There is an increased risk of hemarthrosis and hematoma in HIV-infected patients who have hemophilia and who are treated concomitantly with zidovudine and ibuprofen. The following medicinal products are unlikely to interact with ketorolac Ketorolac did not affect the binding of digoxin to plasma protein. In vitro studies indicate that at therapeutic higher concentrations of salicylate (300 µg/ml) the binding of ketorolac decreased from approximately 99.2% to 97.5%. Therapeutic concentrations of digoxin, warfarin, paracetamol, phenytoin and tolbutamide did not affect the binding of ketorolac to plasma proteins. Since ketorolac is a highly active drug and its plasma concentration is low, it is not expected to significantly replace other drugs that bind to plasma proteins. In animal and human studies, there was no evidence that ketorolac tromethamine induces or inhibits liver enzymes that are capable of metabolizing it or other drugs. Therefore, Ketorolac is not expected to alter the pharmacokinetics of other drugs through an enzyme induction or inhibition mechanism. Contraindications hypersensitivity to ketorolac or any component of the drug; patients with active peptic ulcer, with recent gastrointestinal bleeding or perforation, with a history of peptic ulcer or gastrointestinal bleeding; bronchial asthma, rhinitis, angioedema or urticaria caused by the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (due to the possibility of severe anaphylactic reactions); a history of bronchial asthma; do not use as an analgesic before and during surgery; severe heart failure; complete or partial nasal polyp syndrome, Quincke’s edema or bronchospasm; do not use in patients who have had surgery with a high risk of hemorrhage or incomplete bleeding control and in patients who receive anticoagulants, including low doses of heparin (2500-5000 units every 12 hours); hepatic or moderate and severe renal insufficiency (serum creatinine clearance greater than 160 μmol / l); suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, including bleeding disorders and a high risk of bleeding; simultaneous treatment with other NSAIDs (including selective cyclooxygenase inhibitors), acetylsalicylic acid, warfarin , pentoxifylline, probenecid or lithium salts; hypovolemia, dehydration; the period of pregnancy, labor, childbirth and breastfeeding; children under 16 years of age. Composition One tablet contains: active ingredient: ketorolac tromethamine – 10 mg; excipients: lactose monohydrate, microcrystalline cellulose, magnesium stearate, opadry II (including: polyvinyl alcohol, partially hydrolyzed; talc; macrogol 3350 (polyethylene glycol); lecithin (soy); titanium dioxide (E 171)). Overdose Symptoms: headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding; rarely – diarrhea, disorientation, agitation, coma, drowsiness, dizziness, tinnitus, loss of consciousness, sometimes convulsions. In cases of severe poisoning, acute renal failure and liver damage are possible. Anaphylactoid reactions have been observed after the therapeutic use of NSAIDs, which may occur after an overdose. Treatment: gastric lavage, use of activated charcoal. It is necessary to provide sufficient diuresis. The function of the kidneys and liver should be carefully monitored. The condition of patients should be monitored for at least 4 hours after taking a potentially toxic amount of the drug. Frequent or prolonged seizures should be treated with intravenous diazepam. Other measures may be prescribed depending on the clinical condition of the patient. Therapy is symptomatic. Side effects: From the digestive tract: peptic ulcer, perforation or gastrointestinal bleeding, sometimes fatal (especially in the elderly), nausea, dyspepsia, gastrointestinal pain, abdominal discomfort, hematemesis, gastritis, esophagitis, diarrhea, belching , constipation, flatulence, feeling of fullness in the stomach, melena, rectal bleeding, ulcerative stomatitis, vomiting, hemorrhage, perforation, pancreatitis, exacerbation of colitis and Crohn’s disease. From the side of the central nervous system: anxiety, visual impairment, optic neuritis, drowsiness, dizziness, increased sweating, dry mouth, nervousness, paresthesia, functional disorders, depression, euphoria, convulsions, inability to concentrate, insomnia, increased fatigue, agitation, vertigo, violation of taste sensations and vision, myalgia, unusual dreams, confusion, hallucinations, hyperkinesia, hearing loss, tinnitus, psychotic reactions, thought disorders. Infectious diseases: aseptic meningitis (especially in patients with autoimmune diseases such as systemic lupus erythematosus, mixed connective tissue disease), neck stiffness, headache, nausea, vomiting, fever, confusion. Metabolism and nutrition: anorexia, hyponatremia, hyperkalemia. From the genitourinary and reproductive system: increased frequency of urination, oliguria, acute renal failure, hemolytic uremic syndrome, pain in the side (with / without hematuria), elevated serum urea and creatinine, interstitial nephritis, urinary retention, nephrotic syndrome, infertility , kidney failure. On the part of the liver: abnormal liver function, hepatitis, jaundice and liver failure, an increase in functional tests. From the cardiovascular system: flushing, bradycardia, pallor, hypertension, hypotension, palpitation, chest pain, edema, heart failure. 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). From the respiratory system: epistaxis, shortness of breath, asthma, pulmonary edema. From the blood system: purpura, thrombocytopenia, neutropenia, agranulocytosis, aplastic and hemolytic anemia. From the skin: itching, urticaria, skin photosensitivity, Lyell’s syndrome, bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rarely), exfoliative dermatitis, maculopapular rashes. Impact on reproductive function: the use of ketorolac, like any drug that inhibits the synthesis of cyclooxygenase / prostaglandin, can cause infertility. Hypersensitivity: Hypersensitivity reactions have been reported that include non-specific allergic reactions and anaphylaxis, respiratory tract reactivity including asthma, worsening of asthma, bronchospasm, laryngeal edema or dyspnea, and a variety of skin disorders that include various types of rash, itching , urticaria, purpura, angioedema, and in single cases – exfoliative and bullous dermatitis (including epidermal necrolysis and erythema multiforme). Such reactions may occur in patients with or without known hypersensitivity to ketorolac or other non-steroidal anti-inflammatory drugs. They can also be seen in individuals with a history of angioedema, bronchospastic reactivity (eg, asthma and nasal polyps). Anaphylactoid reactions such as anaphylaxis can be fatal. Others: postoperative wound bleeding, hematoma, prolongation of bleeding, asthenia, edema, weight gain, fever, excessive thirst, fatigue, malaise, fever, chest pain. Storage conditions In a place protected from light and moisture, at a temperature not exceeding 25? Keep out of the reach of children. Buy Ketorolac tablets p/o 10mg No. 10×2