Ketokam®
Often - more than 3%. less often - 1-3%, rarely - less than 1%.
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; less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach; rarely - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the stool or melena, vomiting with blood or " coffee grounds", nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.
From the urinary system
: rarely - acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), increased urination; increase or decrease in urine volume, nephritis, edema of renal origin.
From the senses
: rarely - hearing loss, ringing in the ears, visual impairment (including blurred vision).
From the respiratory system
: rarely - bronchospasm or dyspnea, rhinitis, pulmonary edema, 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, fainting.
From the cardiovascular system
: less often - increased blood pressure.
From the hematopoietic organs
: rarely - anemia, eosinophilia, leukopenia.
From the hemostasis system
: rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding.
From the skin
: less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with or without chills, flushing, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens syndrome). Johnson), toxic epidermal necrolysis (Lyell's syndrome).
Allergic reactions
: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).
Others
: often - swelling and (face, legs, ankles, fingers, feet, weight gain); less often - increased sweating; rarely - swelling of the tongue, fever.
Ketocam 10mg No. 20 tablets
Ketocam 10mg No. 20 tablets
Release form
Pills.
20 pcs Pharmacological action
Pharmaceutical group: NSAIDs. Pharmaceutical action: NSAIDs. It has a pronounced analgesic effect, and also has anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with non-selective inhibition of the activity of COX and COX2, which catalyzes the formation of PG 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 intramuscular administration and oral administration, the onset of the analgesic effect is observed after 0.5 and 1 hour, respectively, the maximum effect is achieved after 1-2 hours and 2-3 hours. Pharmacokinetics: Absorption when taken orally is rapid, bioavailability is 80-100%; with intramuscular injection - complete and rapid. Cmax after oral administration of 10 mg -0.82-1.46 mcg/ml, TCmax - 10-78 minutes; after intramuscular administration of 30 mg Cmax - 1.74-3.1 µg/ml, 60 mg - 3.23-5.77 µg/ml, TCmax - 15-73 min and 30-60 min, respectively; Cmax after IV infusion of 15 mg is 1.96-2.98 mcg/ml, 30 mg is 3.69-5.61 mcg/ml. Communication with plasma proteins - 99%. The time to reach Css with parenteral and oral administration is 24 hours when administered 4 times a day (above subtherapeutic) and is 15 mg - 0.65-1.13 μg/ml with intramuscular administration, 30 mg - 1.29-2.47 μg/ml, with i.v. in infusion 15 mg - 0.79-1.39 mcg/ml, 30 mg - 1.68-2.76 mcg/ml; after oral administration of 10 mg - 0.39-0.79 mcg/ml. Volume of distribution - 0.15-0.33 l/kg. In patients with renal failure, the volume of distribution of the drug may increase by 2 times, and the volume of distribution of its R-enantiomer by 20%. Penetrates into breast milk: when the mother takes 10 mg of ketorolac, Cmax in milk is reached 2 hours after taking the first dose and is 7.3 ng/ml, 2 hours after taking the second dose of ketorolac (when using the drug 4 times a day) - 7.9 ng/ml l. More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. It is excreted 91% by the kidneys, 6% through the intestines. T1/2 in patients with normal renal function is an average of 5.3 hours (3.5-9.2 hours after intramuscular administration of 30 mg, 4-7.9 hours after intravenous administration of 30 mg and 2.4-9 hours after oral administration of 10 mg). T1/2 increases in elderly patients and shortens in young ones. Liver function has no effect on T1/2. In patients with impaired renal function with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l), T1/2 is 10.3-10.8 hours, with more severe renal failure - more than 13.6 hours. The total clearance is at i.v. m administration 30 mg - 0.023 l/h/kg (0.019 l/h/kg in elderly patients), intravenous infusion 30 mg - 0.03 l/h/kg, oral administration 10 mg - 0.025 l/h/kg; in patients with renal failure with a plasma creatinine concentration of 19-50 mg/l, with intramuscular administration of 30 mg - 0.015 l/h/kg, with oral administration of 10 mg - 0.016 l/h/kg. Not excreted by hemodialysis.
Indications
Pain syndrome of severe and moderate severity: injuries, toothache, pain in the postpartum and postoperative period, cancer, myalgia, arthralgia, neuralgia, radiculitis, dislocations, sprains, rheumatic diseases.
Contraindications
Hypersensitivity, “aspirin” triad (a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to ASA and pyrazolone-type drugs), hypovolemia (regardless of the cause), erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, hypocoagulation (including hemophilia), bleeding or a high risk of their development, severe renal failure (plasma creatinine above 50 mg/l), liver failure, period of childbirth, lactation, childhood (under 16 years - safety and effectiveness have not been established). Carefully. Hypersensitivity to other NSAIDs, bronchial asthma, the presence of factors that increase gastrointestinal toxicity: alcoholism, smoking and cholecystitis; postoperative period, CHF, edema syndrome, arterial hypertension, renal dysfunction (plasma creatinine below 50 mg/l), cholestasis, active hepatitis, sepsis, SLE, concomitant use with other NSAIDs, old age (over 65 years), pregnancy.
special instructions
Use with caution in patients with impaired liver and kidney function, chronic heart failure, arterial hypertension, in patients with erosive and ulcerative lesions of the gastrointestinal tract and a history of bleeding from the gastrointestinal tract.
Ketorolac should be used with caution in the postoperative period in cases where particularly careful hemostasis is required (including after resection of the prostate gland, tonsillectomy, in cosmetic surgery), as well as in elderly patients, because The half-life of ketorolac is prolonged and plasma clearance may be reduced. In this category of patients, it is recommended to use ketorolac in doses close to the lower limit of the therapeutic range. If symptoms of liver damage, skin rash, or eosinophilia appear, ketorolac should be discontinued. Ketorolac is not indicated for use in chronic pain syndrome.
Impact on the ability to drive vehicles and operate machinery
If drowsiness, dizziness, insomnia or depression appear during treatment with ketorolac, special care must be taken when engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.
Compound
Active substance: ketorolac tromethamine 10.00 mg. Excipients: microcrystalline cellulose 150.50 mg, corn starch (dried) 56.00 mg, magnesium stearate 1.00 mg, colloidal silicon dioxide 2.00 mg. Coating composition: universal coating* 8.00 mg.
*- composition of the universal shell: hypromellose, titanium dioxide, polyethylene glycol, talc.
Directions for use and doses
For adults, when taken orally - 10 mg every 4-6 hours, if necessary - 20 mg 3-4 times a day.
For intramuscular administration, a single dose is 10-30 mg, the interval between injections is 4-6 hours. The maximum duration of use is 2 days.
Maximum doses: when taken orally or intramuscularly - 90 mg/day; for patients weighing up to 50 kg, with impaired renal function, as well as for persons over 65 years of age - 60 mg/day.
Side effects
From the cardiovascular system: rarely - bradycardia, changes in blood pressure, palpitations, fainting.
From the digestive system: possible nausea, abdominal pain, diarrhea; rarely - constipation, flatulence, feeling of gastrointestinal fullness, vomiting, dry mouth, thirst, stomatitis, gastritis, erosive and ulcerative lesions of the gastrointestinal tract, liver dysfunction.
From the central nervous system and peripheral nervous system: anxiety, headache, drowsiness are possible; rarely - paresthesia, depression, euphoria, sleep disturbances, dizziness, changes in taste, visual disturbances, motor disorders.
From the respiratory system: rarely - respiratory failure, attacks of suffocation.
From the urinary system: rarely - increased frequency of urination, oliguria, polyuria, proteinuria, hematuria, azotemia, acute renal failure.
From the blood coagulation system: rarely - nosebleeds, anemia, eosinophilia, thrombocytopenia, bleeding from postoperative wounds.
Metabolism: possible increased sweating, swelling; rarely - oliguria, increased levels of creatinine and/or urea in the blood plasma, hypokalemia, hyponatremia.
Allergic reactions: possible skin itching, hemorrhagic rash; in isolated cases - exfoliative dermatitis, urticaria, Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic shock, bronchospasm, Quincke's edema, myalgia.
Other: possible fever.
Local reactions: pain at the injection site.
Drug interactions
When ketorolac is used concomitantly with other NSAIDs, additive side effects may develop; with pentoxifylline, anticoagulants (including heparin in low doses) - the risk of bleeding may increase; with ACE inhibitors - there may be an increased risk of developing renal dysfunction; with probenecid - the plasma concentration of ketorolac and its half-life increase; with lithium preparations - a decrease in the renal clearance of lithium and an increase in its concentration in plasma is possible; with furosemide - reducing its diuretic effect.
When using ketorolac, the need for the use of opioid analgesics for pain relief is reduced.
Conditions for dispensing from pharmacies Dispensed with a doctor's prescription
Ketorolac Ketocam tablet film 10 mg x20
INSTRUCTIONS for the use of the medicinal product for medical use KETOCAM® Registration number: Trade name of the drug: Ketocam® International nonproprietary name: Ketorolac Dosage form: film-coated tablets Composition: Each film-coated tablet contains: Active substance: ketorolac tromethamine 10, 00 mg Excipients: microcrystalline cellulose 150.50 mg, corn starch (dried) 56.00 mg, magnesium stearate 1.00 mg, colloidal silicon dioxide 2.00 mg. Coating composition: universal coating* 8.00 mg. *- composition of the universal shell: hypromellose (65.00%), titanium dioxide (20.00%), macrogol (13.00%), talc (2.00%). Description: Almost white, round, biconvex film-coated tablets.
Pharmacotherapeutic group: non-steroidal anti-inflammatory drug (NSAID). ATC code: [M01AB15] Pharmacological action: Pharmacodynamics Ketorolac has a pronounced analgesic effect, and also has anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with non-selective inhibition of the activity of the enzyme cyclooxygenase 1 and 2, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of prostaglandins - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, and the analgesic effect is due to the [-]S form. The drug does not affect opioid receptors, does not depress respiration, does not cause drug dependence, and does not have a sedative or anxiolytic effect. The strength of the analgesic effect is comparable to morphine, significantly superior to other non-steroidal anti-inflammatory drugs. After oral administration, the onset of the analgesic effect is noted after 1 hour, the maximum effect is achieved after 2-3 hours. Pharmacokinetics When taken orally, ketorolac is well absorbed in the gastrointestinal tract - the maximum concentration (Cmax) in the blood plasma (0.7-1. 1 mcg/ml) is achieved 40 minutes after taking a 10 mg dose on an empty stomach. Communication with plasma proteins – 99%. Bioavailability – 80-100%. The equilibrium concentration (Css) is achieved after 24 hours when administered 4 times a day and after oral administration of 10 mg is 0.39-0.79 mcg/ml. The volume of distribution is 0.15-0.33 l/kg. In patients with renal failure, the volume of distribution may increase by 2 times for the S-enantiomer and by 20% for the R-enantiomer. Penetrates into breast milk: when the mother takes 10 mg of ketorolac, the maximum concentration (Cmax) in milk is reached 2 hours after taking the first dose and is 7.3 ng/ml, 2 hours after taking the second dose of ketorolac (when using the drug 4 times a day). day) – 7.9 ng/ml. More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. It is excreted 91% by the kidneys, 6% through the intestines. The half-life (T1/2) in patients with normal renal function is 2.4-9 hours after oral administration of 10 mg. T1/2 lengthens in elderly patients and shortens in young ones. Liver function has no effect on T1/2. In patients with impaired renal function with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l), T1/2 is 10.3-10.8 hours, with more severe renal failure - more than 13.6 hours. The total clearance is when taken orally 10 mg - 0.025 l/h/kg, in case of renal failure with a creatinine concentration in the blood plasma of 19-50 mg/l when taken orally 10 mg - 0.016 l/h/kg. Not excreted by hemodialysis. Indications for use Pain syndrome of severe and moderate severity: trauma, toothache, pain in the postpartum and postoperative period, cancer, myalgia, arthralgia, neuralgia, sciatica, ligament damage, rheumatic diseases.
Contraindications Hypersensitivity to ketorolac or any other component of the drug, complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (including a history), bronchospasm, angioedema, urticaria, rhinitis caused by taking NSAIDs (history), intolerance to pyrazolone drugs, hypovolemia (regardless of the cause), dehydration, inflammatory bowel diseases, erosive and ulcerative lesions of the gastrointestinal tract in the acute stage (including ulcerative colitis, Crohn's disease), peptic ulcers, hypocoagulation (including hemophilia), bleeding or high risk of bleeding, severe renal failure (creatinine clearance less than 30 ml/min), severe renal failure or active liver disease, condition after coronary artery bypass surgery, confirmed hyperkalemia, hemorrhagic stroke (confirmed or suspected), hemorrhagic diathesis, hematopoietic disorders, concomitant use with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants, including warfarin and heparin , pregnancy, childbirth, breastfeeding, children under 16 years of age (safety and effectiveness of use have not been established). The drug is not used for prophylactic pain relief before and during major surgical interventions due to the high risk of bleeding, as well as for the treatment of chronic pain.
Carefully.
Bronchial asthma, the presence of factors that increase gastrointestinal toxicity: alcoholism and smoking, cholecystitis, postoperative period, ulcerative lesions of the gastrointestinal
history of tract, chronic heart failure, edema syndrome, arterial hypertension, renal dysfunction (Kreatipin clearance 30-60 ml/min), cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, coronary heart disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes diabetes, peripheral artery disease, chronic renal failure (creatinine clearance 34-60 ml/min), Helicobacter pylori infection, long-term use of non-steroidal anti-inflammatory drugs, severe somatic diseases, simultaneous use of oral glucocorticosteroids (including prednisolone), antiplatelet agents ( including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), thyroid disease, tuberculosis, old age (over 65 years).
Use during pregnancy and breastfeeding. It is not recommended to take the drug during pregnancy (adverse effects on the cardiovascular system of the fetus - premature closure of the ductus arteriosus), during childbirth, in the early postpartum period (by inhibiting the synthesis of prostaglandins, it can adversely affect the blood circulation of the fetus and weaken the contractile activity of the uterus, which increases the risk of uterine bleeding) and during breastfeeding.
Method of administration and dosage Ketorolac is used orally 30-60 minutes after a meal, once or repeatedly, depending on the severity of the pain syndrome. When administered orally to patients from 16 to 64 years of age with a body weight exceeding 50 kg, the recommended dose is 20 mg for the first dose, then 10 mg 4 times a day, but not more than 40 mg/day. For adult patients weighing less than 50 kg or with renal failure, a dose of 10 mg is recommended for the first dose and then 10 mg 4 times a day, but not more than 40 mg/day. The maximum daily dose is 40 mg. When taken orally, the duration of the course should not exceed 5 days. Side effects Often - more than 3%, less often - 1-3%, rarely - less than 1%. 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, less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness of the stomach, rarely - decreased loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the stool or melena, vomiting with blood or “coffee grounds” type) , nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis. From the urinary system: rarely - acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), increased urination, increased or decreased urine volume, nephritis, edema of renal origin. From the senses: rarely - hearing loss, ringing in the ears, visual impairment (including blurred visual perception). From the respiratory system: rarely - bronchospasm or dyspnea, rhinitis, pulmonary edema, 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 , fainting conditions. From the cardiovascular system: less often – increased blood pressure. From the hematopoietic organs: rarely – anemia, eosinophilia, leukopenia. From the hemostasis system: rarely – bleeding from a postoperative wound, nosebleeds, rectal bleeding. From the skin: less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with or without chills, flushing, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, erythema maligna exudative (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing). Other: often – swelling (of the face, legs, ankles, fingers, feet, weight gain), less often – increased sweating, rarely – swelling of the tongue, fever. Overdose Symptoms: nausea, vomiting, abdominal pain, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis. Treatment: symptomatic therapy (maintaining vital functions of the body). Dialysis is ineffective.
Interaction with other drugs
Co-administration with paracetamol increases the nephrotoxicity of ketorolac. Use with other NSAIDs, glucocorticosteroids, ethanol, corticotropin, calcium preparations increases the risk of ulceration of the gastrointestinal mucosa and the development of gastrointestinal bleeding. Do not use with paracetamol for more than 2 days. Simultaneous administration with anticoagulants - derivatives of coumarin and indandione, heparin, thrombolytics (alteplase, streptokinase, urokinase), antiplatelet agents, cephalosporins, pentoxifylline, valproic acid and acetylsalicylic acid increases the risk of bleeding. Reduces the effect of antihypertensive and diuretic drugs (reduces the synthesis of prostaglandins in the kidneys). Prescription together with mototrexate increases hepato- and nephrotoxicity (their joint administration is possible only when using low doses of the latter and monitoring its concentration in plasma). When prescribed with other nephrotoxic drugs (including gold preparations), the risk of developing nephrotoxicity increases. Drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in plasma. Increases the effect of narcotic analgesics. Myelotoxic drugs enhance the hematotoxicity of the drug. Probenecid is contraindicated due to a decrease in plasma clearance and volume of distribution of ketorolac, an increase in its concentration in blood plasma and an increase in its half-life. Co-administration with sodium valproate causes disruption of platelet aggregation. Increases the plasma concentration of verapamil and nifedipine. The hypoglycemic effect of insulin and oral hypoglycemic drugs increases (dose recalculation is necessary). Pharmaceutically incompatible with tramadol solution and lithium preparations. Antacids do not affect the degree of absorption of ketorolac. Ketorolac does not alter the binding of digoxin to plasma proteins. Zidovudine, when interacting with ketorolac, may increase the risk of hematological toxicity. Due to the theoretical risk of changes in the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors, NSAIDs should not be prescribed earlier than 8-12 days after discontinuation of mifepristone. Tacrolimus, when interacting with ketorolac, may increase nephrotoxicity due to effects associated with the effect on renal prostaglandins. When interacting with quinolone antibiotics, ketorolac may increase the risk of seizures.
Special instructions Before prescribing the drug, it is necessary to clarify the issue of a previous allergy to the drug or non-steroidal anti-inflammatory drug (NSAID). Due to the risk of allergic reactions, the first dose is administered under close medical supervision. Hypovolemia increases the risk of nephrotoxic adverse reactions. If necessary, can be prescribed in combination with narcotic analgesics. It is not recommended for use as a drug for premedication or maintenance of anesthesia. When taken together with other non-steroidal anti-inflammatory drugs, fluid retention, cardiac decompensation, and increased blood pressure may occur. The effect on platelet aggregation ceases after 24-48 hours. Do not use simultaneously with paracetamol for more than 5 days. Patients with blood coagulation disorders are prescribed only with constant monitoring of platelet counts, especially important for postoperative patients who require careful monitoring of hemostasis. The risk of developing drug complications increases with lengthening of treatment (in patients with chronic diseases) and increasing the oral dose of the drug to more than 40 mg/day. To reduce the risk of developing NSAID gastropathy, antacid medications, misoprostol, and omeprazole are prescribed. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. To reduce the risk of adverse events, the minimum effective dose should be used with the shortest possible short course of ketorolac.
Release form Film-coated tablets, 10 mg 10 tablets in a blister. 1, 2 or 10 blisters along with instructions for use are placed in a cardboard pack. Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children. Shelf life: 3 years. Do not use after the expiration date stated on the package. Dispensing conditions: By prescription.
Address of place of manufacture: Plant: Sec-35, Begampur Khatola Ind. Area, Gurgaon - 122001, India. or Plant: S-7 to S-13 and S-59 to S-64, Siggadi Development Centre, SIDKUL, Siggadi, Kotdwar - 246149, Dist. Pauri Garhwal, Uttarakhand, India.
Supplier: CJSC "CORAL-MED" 119530, Moscow, Ochakovskoe highway, 34, tel./fax. Consumer complaints should be directed to CJSC KORAL-MED.
(information from the official website https://grls.rosminzdrav.ru)
