Ketonof-LF instructions for use

Ketorolac-LF tablets p/o 10 mg No. 10x5

Name

Ketorolac-lf.

Release forms

Pills.

INN

Ketorolac.

Pharmacotherapeutic group

Nonsteroidal anti-inflammatory and antirheumatic drugs. Derivatives of acetic acid and their analogues. ATX code М01АВ15

Compound

Each tablet contains: active substance: ketorolac tromethamine – 10 mg; excipients: microcrystalline cellulose, corn starch, colloidal silicon dioxide anhydrous, magnesium stearate, lactose monohydrate, Opadry II white (partially hydrolyzed polyvinyl alcohol, titanium dioxide, macrogol/PEG, talc).

Indications for use

Ketorolac-LF, film-coated tablets, 10 mg is used for short-term treatment of acute pain (including postoperative pain) of moderate intensity, only as a continuation of previous parenteral (intramuscular or intravenous) therapy in a hospital setting, if necessary. The total duration of parenteral and oral therapy with ketorolac should not exceed 5 days.

Directions for use and dosage

For oral administration. The maximum daily dose is 4 tablets (40 mg). The duration of the course is no more than 5 days. The dosage regimen is set individually depending on the pain syndrome. To minimize side effects, the drug should be used at the lowest effective dose for the shortest period of time necessary to control symptoms. For children under 16 years of age, use is contraindicated. Adults from 16 to 64 years old, with a body weight exceeding 50 kg, are prescribed 1 tablet (10 mg) 3-4 times a day. For adults over 64 years of age, and/or with a body weight of less than 50 kg, and/or with impaired renal function, the frequency of use of the drug is reduced to 1-2 times a day.

Side effect

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 central nervous system: anxiety, blurred vision, optic neuritis, drowsiness, dizziness, increased sweating, dry mouth, nervousness, paresthesia, functional disorders, depression, euphoria, convulsions, inability to concentrate, insomnia, increased fatigue, agitation, vertigo , impaired taste and vision, myalgia, unusual dreams, confusion, hallucinations, hyperkinesia, hearing loss, tinnitus, psychotic reactions, thinking disorders. Infectious diseases: aseptic meningitis (especially in patients with autoimmune diseases such as systemic lupus erythematosus, mixed connective tissue disease), stiff neck, headache, nausea, vomiting, fever, confusion. Metabolism and nutrition: anorexia, hyponatremia, hyperkalemia. From the urinary system: increased urinary frequency, oliguria, acute renal failure, hemolytic uremic syndrome, flank pain (with/without hematuria), increased serum urea and creatinine, interstitial nephritis, urinary retention, nephrotic syndrome, infertility, renal failure. From the liver: impaired liver function, hepatitis, jaundice and liver failure, increased functional tests. From the cardiovascular system: flushing of the face, bradycardia, pallor, hypertension, hypotension, palpitation, chest pain, edema, heart failure. Data from clinical and epidemiological studies indicate that the use of certain NSAIDs, especially in high doses and for long periods of time, may be associated with an increased risk of arterial thromboembolic complications (myocardial infarction or stroke). From the respiratory system: nosebleeds, shortness of breath, asthma, pulmonary edema. From the blood system: purpura, thrombocytopenia, neutropenia, agranulocytosis, aplastic and hemolytic anemia. Skin: itching, urticaria, photosensitivity of the skin, Lyell's syndrome, bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rare), exfoliative dermatitis, maculopapular rashes. Effect 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, which include nonspecific allergic reactions and anaphylaxis, respiratory tract reactivity including asthma, worsening asthma, bronchospasm, laryngeal edema or shortness of breath, and a variety of skin disorders that include various types of rashes, itching , urticaria, purpura, angioedema, and in isolated 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 may also occur in individuals with a history of angioedema, bronchospastic reactivity (eg, asthma, and nasal polyps). Anaphylactoid reactions, such as anaphylaxis, can be fatal. Others: postoperative bleeding from a wound, hematoma, prolongation of bleeding, asthenia, edema, weight gain, increased body temperature, excessive thirst, fatigue, malaise, fever, chest pain.

Contraindications

Hypersensitivity to ketorolac or any component of the drug. Patients with active peptic ulcer disease, recent gastrointestinal bleeding or perforation, or a history of peptic ulcer disease 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). History of bronchial asthma. Do not use as an analgesic before or during surgery. Severe heart failure. Complete or partial nasal polyp syndrome, angioedema 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 failure (serum creatinine more than 160 µmol/l). Suspected or confirmed cerebrovascular bleeding, bleeding diathesis, including coagulation disorders and high risk of bleeding. Concomitant treatment with other non-steroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase inhibitors), acetylsalicylic acid, warfarin, pentoxifylline, probenecid or lithium salts. Hypovolemia, dehydration. The period of pregnancy, labor, childbirth and breastfeeding. Children's age up to 16 years.

Overdose

Symptoms: headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding; rarely - diarrhea, disorientation, agitation, coma, drowsiness, dizziness, ringing in the ears, loss of consciousness, sometimes convulsions. In cases of severe poisoning, acute renal failure and liver damage are possible. Anaphylactoid reactions have been observed after therapeutic use of NSAIDs, which may occur after overdose. Treatment: gastric lavage, use of activated carbon. It is necessary to ensure sufficient diuresis. Kidney and liver function should be carefully monitored. Patients should be monitored for at least 4 hours after ingestion of a potentially toxic amount. Frequent or prolonged seizures should be treated with intravenous diazepam. Other measures may be prescribed depending on the patient's clinical condition. Therapy is symptomatic.

Precautionary measures

The maximum duration of treatment should not exceed 5 days. Effect on fertility. The use of ketorolac, like any drug that inhibits cyclooxygenase/prostaglandin synthesis, may impair fertility and is not recommended for use by women who are planning to become pregnant. For women who are unable to become pregnant or are undergoing fertility investigations, discontinuation of ketorolac should be considered. Gastrointestinal bleeding, ulceration and perforation. Gastrointestinal bleeding, ulceration or perforation, which may be fatal, has been reported with the use of NSAIDs at any time during treatment, with or without warning symptoms or in the case of a history of severe gastrointestinal disorders. The risk of severe gastrointestinal bleeding depends on the dosage of the drug. This particularly applies to elderly patients who use ketorolac at an average daily dose of more than 60 mg. For these patients, as well as for patients who are concomitantly using low doses of acetylsalicylic acid or other drugs that may increase gastrointestinal risk, combination treatment with protective agents (eg, misoprostol or proton pump inhibitors) should be considered. The drug Ketorolac-LF is used with caution in patients who are receiving concurrent drug treatment that may increase the risk of ulceration or bleeding, such as oral corticosteroids, selective serotonin reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid. If gastrointestinal bleeding or ulceration occurs in patients receiving Ketorolac-LF, the course of treatment should be discontinued. Respiratory dysfunction. Caution is required when using the drug in patients with bronchial asthma (or with a history of asthma), since NSAIDs have been reported to accelerate the onset of bronchospasm in such patients. Effect on the kidneys. Prostaglandin biosynthesis inhibitors (including NSAIDs) have been reported to have nephrotoxic effects. The drug should be prescribed with caution to patients with impaired renal, cardiac, or liver function, since the use of NSAIDs may lead to deterioration of renal 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 renal condition of such patients should be carefully monitored. As with other drugs that inhibit prostaglandin synthesis, increases in serum urea, creatinine and potassium have been reported during use of ketorolac tromethamine, which may occur after a single dose. Disorders of the cardiovascular system, kidneys and liver. Prescribe the drug with caution to patients with conditions that lead to a decrease in blood volume and/or renal blood flow, when renal prostaglandins play a supporting role in ensuring renal perfusion. In these patients, renal function should be monitored. The volume reduction should be corrected and serum urea and creatinine levels and the volume of urine excreted carefully monitored until the patient becomes normovolemic. In patients on renal dialysis, the clearance of ketorolac was reduced by approximately half the normal rate, and the terminal half-life was approximately tripled. Patients with impaired liver function due to cirrhosis did not have any clinically significant changes in ketorolac clearance or terminal half-life. Borderline increases in one or more liver function tests may occur. 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, the drug should be discontinued. Fluid retention and swelling. Fluid retention and edema have been reported during use of ketorolac and should be used with caution in patients with cardiac decompensation, hypertension, or similar conditions. Cardiovascular and cerebrovascular effects. There is currently insufficient information to assess such a risk for ketorolac tromethamine. Patients with uncontrolled hypertension, congestive heart failure, diagnosed coronary artery disease, peripheral arterial disease and/or cerebrovascular disease should be under medical supervision. Systemic lupus erythematosus and mixed connective tissue diseases. In patients with systemic lupus erythematosus and various mixed connective tissue diseases, the risk of developing aseptic meningitis increases. Dermatological reactions. The drug should be discontinued at the first signs of a skin rash, damage to the mucous membranes or any other signs of hypersensitivity. Anaphylactic (anaphylactoid) reactions. As with the use of other NSAIDs, anaphylactic (anaphylactoid) reactions (including anaphylaxis, bronchospasm, flushing, rash, hypotension, laryngeal edema, Quincke's edema) may occur in patients who have no or no history of hypersensitivity to aspirin, other NSAIDs or ketorolac. This set of symptoms may also occur in individuals with a history of bronchospastic reactivity (eg, asthma) and nasal polyps. Anaphylactoid reactions, such as anaphylaxis, can be fatal. Therefore, ketorolac should not be taken by patients with a history of asthma, and by patients with complete or partial nasal polyp syndrome, angioedema and bronchospasm. If anaphylactoid reactions occur, seek emergency medical attention. Hematological effects. Patients with bleeding disorders should not be prescribed the drug. Patients receiving anticoagulant therapy may have an increased risk of bleeding if ketorolac is used concomitantly. Patients receiving other medications that may affect the rate of bleeding control should be carefully monitored when ketorolac is prescribed 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 times, the duration of bleeding increased, but did not exceed the normal range of 2-11 minutes. In contrast to the long-term effects resulting from the use of acetylsalicylic acid, platelet function returns to normal within 24-48 hours after discontinuation of ketorolac. Ketorolac should not be prescribed to patients who have undergone surgery with a high risk of bleeding or incomplete control of bleeding. Caution should be used if mandatory bleeding control is critical. Ketorolac-LF is not an anesthetic agent and does not have sedative or anxiolytic properties; therefore, it is not recommended as a pre-operative sedative to maintain anesthesia. Should not be used in patients with rare hereditary diseases: congenital galactosemia, lactase deficiency, glucose/galactose malabsorption syndrome.

Children

Not for use in children under 16 years of age.

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 cardiovascular system of the fetus (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 bleeding to occur in both mother and baby. Ketorolac is excreted into breast milk in small quantities, therefore the drug Ketorolac-LF is contraindicated during breastfeeding.

Impact on the ability to drive vehicles and operate machinery

Some patients may experience drowsiness, dizziness, vertigo, insomnia, fatigue, blurred vision or depression when using ketorolac. If patients experience the above or other similar side effects, they should not drive or operate machinery.

Interaction with other drugs

Ketorolac easily binds to plasma proteins (average value 99.2%), and the degree of binding depends on the concentration. Cannot be used simultaneously with ketorolac. Due to the possibility of side effects, ketorolac should not be prescribed with other NSAIDs, including selective cyclooxygenase-2 inhibitors, or in patients receiving acetylsalicylic acid, warfarin, lithium, probenecid, cyclosporine. NSAIDs should not be prescribed within 8-12 days after using mifepristone, since NSAIDs may weaken the effect of mifepristone. Medicines in combination with ketorolac should be prescribed with caution. In healthy normovolemic individuals, ketorolac reduces the diuretic effect of furosemide by approximately 20%; therefore, the drug is prescribed with particular caution to patients with cardiac decompensation. NSAIDs may worsen heart failure, reduce glomerular filtration rate, and increase plasma levels of cardiac glycosides when coadministered 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 renal dysfunction, especially in patients with a reduced blood volume in the body. There is a possible risk of nephrotoxicity if NSAIDs are prescribed 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, caution is required when coadministering corticosteroids due to the increased risk of gastrointestinal ulceration or bleeding. There is an increased risk of gastrointestinal bleeding if NSAIDs are prescribed in combination with antiplatelet agents and selective serotonin reuptake inhibitors. Caution is advised if methotrexate is coadministered 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 have an increased risk of developing seizures. Concomitant 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 people who have hemophilia and who are treated with both zidovudine and ibuprofen. The following drugs are unlikely to interact with ketorolac. Ketorolac did not affect the binding of digoxin to plasma protein. In vitro studies indicate that at therapeutic concentrations of salicylate (300 μg/ml) and higher, ketorolac binding was reduced by approximately 99.2% to 97.5%. Therapeutic concentrations of digoxin, warfarin, paracetamol, phenytoin and tolbutamide did not affect the binding of ketorolac to plasma protein. Because ketorolac is a highly active drug and its available plasma concentration is low, it is not expected to significantly replace other drugs that bind to plasma proteins. There is no evidence from animal or human studies 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 mechanisms of enzyme induction or inhibition.

Storage conditions

In a place protected from moisture and light at a temperature not exceeding 25 °C. Keep out of the reach of children.

Best before date

2 years. Do not use after the expiration date stated on the packaging.

Package

10 tablets each in a blister pack made of polymer film and aluminum foil. Two, three or five blister packs along with instructions for medical use in a cardboard pack.

Vacation conditions

On prescription.

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Instructions for use for Ketorolac-LF tablets p/o 10 mg No. 10x5

Effect on fertility. The use of ketorolac may impair fertility and is not recommended for use by women who are planning to become pregnant. For women who are unable to become pregnant or are undergoing fertility investigations, discontinuation of ketorolac should be considered.

Kidney and liver disorders. The drug is prescribed with caution to patients with impaired renal and liver function. In patients with mild renal impairment, lower doses of ketorolac are prescribed, and the renal condition of such patients should be carefully monitored. As with other drugs that inhibit prostaglandin synthesis, increases in serum urea, creatinine and potassium have been reported during use of ketorolac, which may occur after a single dose.

The drug should be prescribed with caution to patients with conditions that lead to a decrease in blood volume and/or renal blood flow. In these patients, renal function should be monitored. The volume reduction should be corrected and serum urea and creatinine levels and the volume of urine excreted carefully monitored until the patient becomes normovolemic. In patients on renal dialysis, the clearance of ketorolac was reduced by approximately half the normal rate, and the terminal half-life was approximately tripled. Patients with impaired liver function due to cirrhosis did not have any clinically significant changes in ketorolac clearance or terminal half-life. Borderline increases in one or more liver function tests may occur. 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, the drug should be discontinued.

Cardiovascular and cerebrovascular effects. When using ketorolac, blood pressure monitoring is necessary for patients suffering from arterial hypertension and heart failure. This is due to fluid retention and the development of edema when using NSAIDs.

Clinical studies and epidemiological data suggest that the use of coxibs and some other NSAIDs (especially at high doses) may increase the risk of arterial thrombosis (eg, myocardial infarction or stroke). Although ketorolac does not increase the incidence of thrombotic events such as myocardial infarction, there is insufficient data to completely rule out such a risk.

In patients with uncontrolled hypertension and heart failure, coronary artery disease, peripheral arterial disease and/or cerebrovascular disease, ketorolac should be prescribed after a careful assessment of the risk/benefit ratio. A similar approach before starting treatment should be applied to patients with risk factors for cardiovascular disease (for example, hypertension, hyperlipidemia, diabetes mellitus, smoking).

Gastrointestinal disorders: Gastrointestinal ulcers, bleeding and perforation, which can be fatal, occur with all NSAIDs, including ketorolac, at any time during treatment, often without prior symptoms or without a history of serious complications from the gastrointestinal tract. In elderly people, people with a history of gastrointestinal bleeding, in debilitated patients or patients receiving high doses of ketorolac, the risk of developing adverse reactions from the gastrointestinal tract is higher, and the consequences of these adverse reactions can be fatal. These patients should begin treatment with the lowest dose; This may include recommended therapy with misoprostol or proton pump inhibitors. Combination therapy is also prescribed to patients simultaneously receiving low doses of aspirin or its analogues. For elderly people, it is recommended to increase the interval between doses of ketorolac.

NSAIDs should be prescribed with caution to patients with inflammatory bowel diseases (ulcerative colitis, Crohn's disease). Patients with a history of gastrointestinal adverse reactions, especially the elderly, should report any unusual abdominal symptoms, especially during the initial stages of treatment. If adverse reactions from the gastrointestinal tract are detected, it is necessary to discontinue ketorolac. Ketorolac should be prescribed with caution to patients receiving concomitant treatment with oral corticosteroids, selective serotonin reuptake inhibitors, or antiplatelet agents.

Systemic lupus erythematosus and mixed connective tissue diseases. In patients with systemic lupus erythematosus and various mixed connective tissue diseases, the risk of developing aseptic meningitis increases.

Dermatological effects. Ketorolac should be discontinued at the first signs of a skin rash, damage to the mucous membranes or any other signs of hypersensitivity.

Hematological effects. Patients with bleeding disorders should not be prescribed ketorolac. Patients receiving anticoagulant therapy may have an increased risk of bleeding if ketorolac is used concomitantly. Patients receiving other drugs that may affect the rate of bleeding control should be carefully monitored when ketorolac is prescribed 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 times, the duration of bleeding increased, but did not exceed the normal range of 2-11 minutes. In contrast to the long-term effects resulting from the use of acetylsalicylic acid, platelet function returns to normal within 24-48 hours after discontinuation of ketorolac.

The drug is not an anesthetic and does not have sedative or anxiolytic properties; therefore, it is not recommended as a pre-operative sedative to maintain anesthesia.

Use with caution in patients with rare hereditary diseases: congenital galactosemia, lactase deficiency, glucose/galactose malabsorption syndrome.

Ketonal

According to the World Health Organization (WHO), adverse effects are classified according to their frequency as follows: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, < 1/100), rare (≥1/10000, <1/1000) and very rare (<1/10000); frequency unknown (the frequency of events cannot be determined from the available data).

Hematopoietic and lymphatic system disorders

rarely: hemorrhagic anemia; frequency unknown: agranulocytosis, thrombocytopenia, bone marrow dysfunction.

Immune system disorders

frequency unknown: anaphylactic reactions (including anaphylactic shock).

Nervous system disorders

uncommon: headache, dizziness, drowsiness; rarely: paresthesia; frequency unknown: convulsions, disturbance of taste.

Mental disorders

frequency unknown: emotional lability.

Sensory disorders

rarely: blurred vision, tinnitus.

Cardiovascular disorders

frequency unknown: heart failure, increased blood pressure, vasodilation.

Respiratory system disorders

rarely: exacerbation of bronchial asthma; frequency unknown: bronchospasm (especially in patients with hypersensitivity to NSAIDs), rhinitis.

Gastrointestinal disorders

often: nausea, vomiting, dyspepsia, abdominal pain; uncommon: constipation, diarrhea, bloating, gastritis; rarely: peptic ulcer, stomatitis; very rarely: exacerbation of ulcerative colitis or Crohn's disease, gastrointestinal bleeding, perforation.

Liver and biliary tract disorders

rarely: hepatitis, increased activity of liver transaminases, increased bilirubin concentration.

Skin and subcutaneous tissue disorders

uncommon: skin rash, itching; frequency unknown: photosensitivity, alopecia, urticaria, angioedema, erythema, bullous rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis.

Renal and urinary tract disorders

frequency unknown: acute renal failure, nephritis, interstitial nephritic syndrome, nephrotic syndrome, abnormal values ​​of renal function tests.

Other

uncommon: swelling; rarely: weight gain; frequency unknown: increased fatigue.