Compound
Composition of tablets: ketorolac (10 mg/tablet), MCC, lactose, corn starch, colloidal silicon dioxide, Mg stearate, Na carboxymethyl starch (type A).
The film shell contains: hypromellose, propylene glycol (additive E1520), titanium dioxide; dyes brilliant blue (22%) and quinoline yellow (78%) - olive green.
Composition of the solution: ketorolac (30 mg per milliliter), octoxynol, EDTA, Na chloride, ethanol, propylene glycol (additive E1520), Na hydroxide, water for injection.
Gel composition: ketorolac (20 mg per gram of gel), propylene glycol (additive E1520), dimethyl sulfoxide, carbomer 974P, Na methyl and propyl parahydroxybenzoate, tromethamine (trometamol), Drimon Inde flavoring, ethanol, glycerol, purified water.
Release form
- Tablets in p/o 10 mg, package No. 20. Ketorol tablets (INN - Ketorolac) are biconvex, round in shape, covered with a green coating (the core is white or close to white). On one side there is an imprint in the shape of the letter “S”.
- Solution for IM and IV administration 30 mg/ml, package No. 10. Ketorol injections are available in 1 ml ampoules, each of which has a breaking point and a ring in the upper part.
- Gel 2% for external use, tubes 30 g, packaging No. 1. Ketorol gel is a homogeneous, characteristically smelling, transparent (or translucent) substance.
Pharmacodynamics and pharmacokinetics
What is ketorolac?
The active substance Ketorol is a mixture in which the [+]R and [-]S enantiomers are present in equal quantities, and the analgesic effect is due to the [-]S form.
Pharmacodynamics
The drug is a powerful analgesic with anti-inflammatory properties and moderate antipyretic activity .
Its mechanism of action is associated with the ability to indiscriminately inhibit the activity of the COX 1 and 2 enzyme, mainly in peripheral tissues. As a result, the biosynthesis of Pg, a modulator of thermoregulation, pain sensitivity and inflammation, slows down.
Ketorolac does not affect opiate receptors, does not have anxiolytic or sedative effects, does not depress respiration, and does not lead to the development of drug dependence.
The analgesic effect of the drug is more pronounced in comparison with analogues. The effect of its use is comparable to the analgesic effect of morphine .
After injection into the muscle and oral administration, the pain begins to decrease after 0.5 and 1 hour, respectively. To achieve the maximum effect, it takes from 60 to 120 minutes.
Pharmacokinetics
Absorption in the digestive canal when taken orally is rapid. TSmax after taking 1 tablet on an empty stomach - 40 minutes.
Fatty foods reduce the Cmax in the blood while simultaneously increasing the TCmax up to 1 hour 40 minutes.
99% of the dose taken is bound to plasma proteins. With hypoalbuminemia, the concentration of free substance in the blood increases.
Bioavailability is one hundred percent (regardless of the method of administration of the drug).
When administered parenterally, the substance is absorbed quickly and completely.
Equilibrium concentration of Css when Ketorol is administered intravenously or intramuscularly at a dose of 120 mg/day. (4 injections of 30 mg) and when taken orally at a dose of 40 mg/day. (1 tablet in 4 doses) is achieved after 24 hours. The highest values of this indicator are observed with parenteral administration of 1 ml of solution 4 times a day.
The substance passes into breast milk: when a nursing woman takes 1 tablet of Tmax ketorolac in milk - 2 hours.
More than 50% of administered ketorolac is biotransformed in the liver with the formation of pharmacologically inactive metabolites . The substance is excreted mainly in the form of glucuronic metabolites and p-hydroxyketorolac. 91% of the dose taken is excreted by the kidneys, 6% - with the contents of the intestines.
In patients with healthy kidneys, the elimination half-life averages 5.3 hours.
In older people, T1/2 lengthens, in young people it shortens.
The functional state of the liver does not affect the pharmacokinetics of the drug. In case of kidney damage, in which the plasma concentration of creatinine is 19-50 mg/l, the half-life is extended to 10.3-10.8 hours; if renal failure is more severe, this figure exceeds 13.6 hours.
It is not excreted during hemodialysis .
Ketorol Insta tablets dispersible in the oral cavity 10 mg No. 10x2
Name
Ketorol insta
Description
Light yellow, round, flat tablets engraved with an “I” on one side and smooth on the other.
Main active ingredient
Ketorolac tromethamine - 10 mg.
Release form
pills
Dosage
10 tablets in a blister made of aluminum/desiccant/aluminum foil, 1 blister in a cardboard box with instructions for use.
special instructions
pharmachologic effect
Non-steroidal anti-inflammatory drugs. ATX code: M01 AB15.
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 inhibition of the cyclooxygenase enzyme, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of prostaglandins - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture
—
S and
+
P enantiomers, with the analgesic effect due to
—
S shape. The drug does not affect opioid receptors, does not depress respiration, does not inhibit intestinal motility, does not have a sedative or anxiolytic effect, does not cause drug dependence, and does not affect the progression of the disease. Ketorolac inhibits platelet aggregation and increases bleeding time. The functional state of platelets is restored 24-48 hours after discontinuation of the drug.
Pharmacokinetics
Ketorolac tromethamine is rapidly and completely absorbed after oral administration with a peak plasma concentration of 0.87 mcg/ml 50 minutes after a single 10 mg dose. In healthy volunteers, the terminal plasma half-life averages 5.4 hours. In older people (average age 72 years) it is 6.2 hours. More than 99% of ketorolac in blood plasma is protein bound. In humans, after single or multiple doses, the pharmacokinetics of ketorolac is linear. Steady-state plasma levels are achieved after one day when administered 4 times daily. No changes were observed with long-term dosing. After a single intravenous dose, the volume of distribution is 0.25 l/kg, the half-life is 5 hours, and the clearance is 0.55 ml/min/kg. The main route of excretion of ketorolac and its metabolites (conjugates and p-hydroxymetabolites) is urine (91.4%), and the rest is excreted in feces. A diet rich in fat reduces the rate of absorption, but not the volume, while antacids do not affect the absorption of ketorolac.
Indications for use
Ketorol Insta, orally dispersible tablets, 10 mg, is used for the short-term treatment of acute pain (including postoperative pain) of moderate to severe 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 due to the possibility of increasing the frequency and severity of adverse reactions. Before taking Ketorol Ineta, consider the potential benefits and risks and options for using another drug. Use the lowest effective dose for the shortest possible time. Patients should be switched to alternative treatment as quickly as possible.
Directions for use and doses
The duration of the course of use of Ketorol Ineta should not exceed 5 days; long-term use, as well as oral administration at a dose of more than 40 mg per day, is not recommended. To reduce the risk of side effects, it is recommended to use the minimum effective dose for the minimum time required to relieve pain. From 17 to 64 years: 10 mg every 4-6 hours as needed. It is not recommended to use the drug in doses exceeding 40 mg per day. For patients receiving ketorolac parenterally and prescribed oral ketorolac tablets, 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 mg), and The dosage of the oral form of the drug should not exceed 40 mg per day. Patients should be switched to oral administration of the drug as early as possible. Elderly patients Elderly patients have a higher risk of developing severe complications, particularly from the digestive tract. During treatment with NSAIDs, the patient's condition should be regularly monitored; a longer interval between doses of the drug is usually recommended, for example, 6-8 hours. Dispersible tablets can be used in patients with swallowing dysfunction. Can be taken without drinking water. The tablet is placed on the tongue, kept in the mouth until it is completely dissolved (do not chew), then swallowed.
Use during pregnancy and lactation
The safety of ketorolac during pregnancy 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 Ketorol Insta is contraindicated during breastfeeding.
Precautionary measures
The maximum duration of use, including the use of parenteral forms, should not exceed 5 days. 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 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 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. Ketorol Ineta should be used with caution in patients receiving concurrent 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. If gastrointestinal bleeding or ulceration occurs in patients receiving Ketorol Ineta, 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. The drug should be used with caution in 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, Ketorol Ineta should be discontinued. Fluid retention and edema Fluid retention and edema have been reported during the 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. Ketorol Ineta 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, hyperemia, 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 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 Ketorol Ineta. 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. 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. Ketorol Ineta 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.
Interaction with other drugs
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 salicylate concentrations (300 mcg/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 be metabolized by it or other drugs. Therefore, ketorolac is not expected to alter the pharmacokinetics of other drugs.
Contraindications
Hypersensitivity to ketorolac or any component of the drug; patients with an active peptic ulcer, with recent gastrointestinal bleeding or perforation, with 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); do not use as an analgesic before and during surgery; 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 to severe renal failure (serum creatinine concentration more than 160 µmol/l; suspected or confirmed cerebrovascular bleeding, bleeding diathesis, including coagulation disorders and a high risk of bleeding; concomitant treatment with other non-steroidal anti-inflammatory drugs (NSAIDs) (including selective inhibitors cyclooxygenase), acetylsalicylic acid, warfarin, pentoxifylline, probenecid or lithium salts; hypovolemia, dehydration; pregnancy, labor, childbirth and breastfeeding; children under 16 years of age; erosive and ulcerative lesions and inflammatory diseases of the oral cavity.
Compound
Active ingredient: ketorolac tromethamine – 10 mg; excipients - microcrystalline cellulose, hydrated colloidal silicon dioxide; antioxidant butylated hydroxyanisole, mannitol crospovidone, sucralose, mint flavor, quinoline yellow dye (E104), magnesium stearate.
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.
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 without or with 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. To prevent possible side effects, one should strive to use the minimum effective doses of the drug, strictly adhere to the established dosages and administration regimens, take into account the patient’s condition (age, renal function, state of the gastrointestinal tract, water-electrolyte metabolism and hemostatic system), as well as possible drug interactions with combination therapy.
Storage conditions
Store at a temperature not exceeding 25°C. Keep out of the reach of children.
Buy Ketorol Insta tab. dispers. in the oral cavity 10 mg per bl. in pack No. 10x2 in the pharmacy
Price for Ketorol Insta tab. dispers. in the oral cavity 10 mg per bl. in pack №10x2
Instructions for use for Ketorol Insta tab. dispers. in the oral cavity 10 mg per bl. in pack №10x2
Indications for use
Ketorol tablets: what does the tablet form of the drug help with?
The medicine helps reduce moderate/severe pain and inflammation, but does not affect the progression of the disease.
Tablets are effective for toothache , headaches , pain that occurs during menstruation, after injuries, in the postoperative and postpartum periods, against the background of cancer, with damage to peripheral nerves, with radiculopathy , arthralgia , myalgia , sprains, dislocations, rheumatic diseases .
What does injection medicine help with?
Ketorol in ampoules, like the tablet form of the drug, is used to relieve pain of moderate and severe intensity.
Parenteral administration of the drug is preferable in situations where it is necessary to quickly relieve pain, and also if the patient cannot take it orally (for example, with a peptic ulcer or due to the gag reflex).
Indications for use of Ketorol: what is the gel used for?
Local application of the gel helps reduce pain and inflammation in:
- injuries (inflammation and bruises of soft tissues, including after injury; bursitis , synovitis , ligament damage, epicondylitis , tendonitis );
- myalgia;
- arthralgia;
- radiculitis;
- neuralgia;
- rheumatic diseases.
Frequently asked questions about Ketorol
How to take Ketorol?
For adults and adolescents over 16 years of age, the doctor prescribes one tablet - 10 mg during or after meals. The medication is swallowed and washed down with water. If the pain does not stop, you are allowed to take the medicine after four to six hours.
How to take Ketorol for toothache?
The doctor recommends that adult patients take one tablet, which contains a minimum dosage of 10 mg, during or after a meal to prevent stomach irritation. The medication intake is increased to two to three times a day if the pain syndrome recurs. Pain relief occurs within 15 minutes and lasts 6–10 hours.
How often can you take Ketorol?
The medication is prescribed in short courses: five days - for toothache; seven days - after injuries and operations. You should not take more than 4 tablets per day.
Contraindications
Contraindications for parenteral administration and oral administration of Ketorol:
- hypersensitivity to the components of the solution/tablets;
- complete or partial combination of clinical manifestations of aspirin-induced bronchial asthma (NSAID intolerance, asthma attacks, polypous rhinosinusitis );
- the presence of erosions and ulcerative defects on the mucous membrane of the upper gastrointestinal tract;
- bleeding in the active phase (gastrointestinal, cerebrovascular or other);
- worsened inflammatory bowel disease;
- hemophilia and other pathologies of the hemostatic system;
- end stage of heart failure (decompensated heart failure);
- functional disorders or active liver disease;
- confirmed hyperkalemia ;
- postoperative period after CABG;
- renal failure , in which the creatinine does not exceed 30 ml/min, progressive kidney pathologies ;
- pregnancy , childbirth, lactation ;
- age up to 16 years.
Relative contraindications:
- congestive heart failure ;
- bronchial asthma (BA);
- IHD;
- hypersensitivity to NSAIDs;
- pathological dys- or hyperlipidemia ;
- cerebrovascular pathologies;
- arterial hypertension;
- kidney damage, in which the creatinine is below 60 ml/min;
- sepsis;
- cholestasis;
- edema syndrome;
- diabetes;
- SLE;
- chronic obliterating diseases of the arteries of the lower extremities;
- treatment with other NSAIDs, anticoagulants , antiplatelet agents , SSRIs, oral corticosteroids;
- history of ulcerative lesions of the digestive canal;
- smoking;
- old age (over 65 years);
- alcohol abuse;
- severe somatic diseases.
External use of Ketorol is contraindicated in case of hypersensitivity to any of the components of the gel, aspirin asthma , eczema , weeping dermatitis , after the 27th week of pregnancy and during lactation . The gel is not intended for the treatment of open wounds and infected abrasions. The drug is prescribed to adolescents from the age of sixteen.
Ketorol gel should be used with caution in case of hepatic porphyria (at the stage of exacerbation of the disease), severe liver/renal failure , CHF, asthma, in pregnant women (in the 1st and 2nd trimesters) and in the elderly.
Contraindications for use
The drug Ketorol is not used for:
- hypersensitivity in patients to active and auxiliary substances and medications that contain aspirin or belong to the NSAID group;
- bronchial asthma and bronchospasm;
- Quincke's edema;
- ulcers or erosions in the stomach and duodenum, which were complicated by perforation or bleeding;
- hemorrhagic stroke;
- renal dysfunction;
- heart failure, if it is difficult to remove fluid from the body;
- detection of nasal polyps;
- breastfeeding;
- pregnancy due to the development of bleeding after childbirth and oligohydramnios in women, which leads to early closure of the ductus arteriosus and the occurrence of heart pathologies in the baby.
- The medication is also not prescribed:
- up to 16 years old;
- patients before and during operations, since as a result of the drug, platelet aggregation slows down and the risk of bleeding increases.
Side effects
More than 3% of patients with parenteral administration and oral administration of Ketorol experience:
- diarrhea and gastralgia (especially in older people with a history of peptic ulcer disease);
- dizziness , increased drowsiness , headache ;
- swelling (fingers, feet, ankles, legs, face);
- weight gain.
Somewhat less frequently (in 1-3% of patients) the following were recorded:
- flatulence , stomatitis , feeling of fullness in the stomach, vomiting, constipation ;
- increased blood pressure ;
- purpura, rash (including maculopapular) on the skin;
- pain and/or burning sensation at the injection site;
- increased sweating .
Rare side effects that occur in less than 1% of patients:
- nausea;
- formation of erosions on the gastrointestinal mucosa or its ulceration (including with perforation and/or bleeding, the symptoms of which are burning, pain and spasm in the epigastric region, bloody vomiting (coffee grounds), melena, heartburn , nausea, etc.);
- hepatomegaly;
- hepatitis;
- acute inflammation of the pancreas;
- surge arrester;
- cholestatic jaundice;
- lower back pain (sometimes accompanied by azotemia and/or hematuria );
- renal failure dominating the clinical picture , as well as hemolytic anemia and thrombocytopenia ;
- change in urine volume (decrease or increase);
- frequent urination;
- edema of renal origin;
- nephritis;
- hearing loss, tinnitus ;
- visual impairment (blurred perception of visual images);
- rhinitis , bronchospasm , laryngeal edema;
- aseptic meningitis;
- hyperactivity (restlessness, mood swings);
- depression;
- mental disorders;
- hallucinations;
- sudden loss of consciousness;
- edema ;
- swelling of the tongue;
- leukopenia , eosinophilia , anemia ;
- bleeding (from the lower gastrointestinal tract, nose, postoperative wound);
- exfoliative dermatitis;
- Lyell's syndrome , malignant exudative erythema , urticaria ;
- anaphylactoid reactions or anaphylaxis ;
- fever.
When ketorolac , peeling of the skin at the site of application of the gel, urticaria , and itching .
When applying the drug to a large area of the body, the possibility of developing systemic effects cannot be excluded, including:
- ulceration of the mucous membrane of the digestive canal;
- heartburn , diarrhea , vomiting, nausea, gastralgia ;
- increased activity of liver aspartate and alanine aminotransferase;
- dizziness , headache ;
- hematuria;
- fluid retention;
- hypersensitivity reactions;
- prolongation of bleeding time;
- anemia , leuko- and thrombocytopenia , agranulocytosis .
Instructions for use of Ketorol
Ketorol tablets: instructions for use
The medicine is taken orally from 1 to 4 times a day. A single dose is one tablet. The highest daily dose is four tablets. Treatment should last no more than 5 days in a row.
When switching from parenteral administration to the tablet form of the drug, the total dose of the drug in the form of tablets and solution on the day of transfer should not exceed 90 mg/day if the patient is under 65 years of age, and 60 mg/day if the patient is older than the specified age.
The upper limit of the daily dose of Ketorol in tablets on the day of transition is 30 mg.
Ketorol injections: instructions for use
The solution is intended for intramuscular and intravenous administration. The drug in this dosage form must be used in minimally effective doses.
If necessary, Ketorol can be used in combination with narcotic analgesics (the latter are prescribed in reduced doses).
For patients under 65 years of age, provided that their weight is more than 50 kg, no more than 2 ml of solution can be injected into the muscle once (including oral administration). As a rule, to relieve pain, 1 ml of Ketorol is administered in ampoules every six hours.
Ketorol is administered intravenously in 1 ml doses so that the volume of medication administered over five days does not exceed 15 single doses.
For patients weighing less than 50 kg, as well as patients with chronic renal failure, a single dose when administering Ketorol into the muscle should not exceed 1 ml of solution (including oral administration).
As a rule, the drug is administered in 0.5 ml doses so that the patient receives no more than 20 single doses in five days.
No more than 0.5 ml of solution can be administered intravenously to a patient with chronic renal failure or weighing less than 50 kg every six hours (within five days, no more than 20 single doses).
The upper limit of the daily dose for parenteral administration of Ketorol for patients under 65 years of age weighing more than 50 kg is 90 mg, for patients with chronic renal failure and patients weighing less than 50 kg is 60 mg.
The drug can be used for no more than 5 days in a row.
The IV solution should be administered over at least 15 seconds. Ketorol is injected intramuscularly deep into the muscle and also slowly.
The drug begins to act half an hour after administration. Maximum pain relief is observed an hour or two after the injection.
Ketorol Gel: instructions for use
The gel (ointment) should be applied to washed and dried skin. A single dose of the medicine is a column 1-2 cm long. Ketorol is distributed on the surface of the most painful area with soft massaging movements 3-4 times a day.
Re-use of the drug is possible no earlier than after 4 hours.
The gel can be used no more than 4 times a day. Do not exceed the recommended dose.
If after 10 days of treatment with Ketorol the patient’s condition does not improve or the pain and inflammation intensify, it is necessary to stop using the drug and seek medical help.
Without consulting a doctor, the gel can be used for no more than 10 days.
Additionally
If the drug is used in combination with narcotic analgesics (solution, tablets or suppositories), the dose of the latter may be reduced.
Ketorol (1ml)
INSTRUCTIONS for the use of the medicinal product for medical use KETOROL ® Registration number: LP-001365
Trade name of the drug: Ketorol®
International nonproprietary name of the drug: ketorolac.
Dosage form: solution for intravenous and intramuscular administration.
Composition 1 ml of solution contains: active ingredient: ketorolac tromethamine (ketorolac trometamol) 30 mg; excipients: octoxynol 0.07 mg, disodium edetate 1 mg, sodium chloride 4.35 mg, ethanol 0.115 ml, propylene glycol 400 mg, sodium hydroxide 0.725 mg, water for injection up to 1 ml.
Description Transparent, colorless or light yellow solution.
Pharmacotherapeutic group: non-steroidal anti-inflammatory drug.
ATX code: M01AV15
Pharmacological properties Pharmacodynamics Non-steroidal anti-inflammatory drug (NSAID), has a pronounced analgesic effect, has anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with non-selective inhibition of the activity of cyclooxygenase (COX) - COX-1 and COX-2, which catalyzes the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, and the analgesic effect is due to the [-]S form. The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs. 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.
Pharmacokinetics The pharmacokinetics of ketorolac after single and repeated intravenous and intramuscular administration is linear. When administered intramuscularly, absorption is complete and rapid. The maximum concentration of the drug (Cmax) after intramuscular administration of 30 mg is 1.74-3.1 μg/ml, 60 mg is 3.23-5.77 μg/ml, time to reach maximum concentration (TCmax) is 15-73 min and 30-60 minutes, respectively. Cmax after intravenous administration of 15 mg – 1.96-2.98 mcg/ml, 30 mg – 3.69-5.61 mcg/ml, TCmax – 0.4-1.8 min and 1.1-4.7 min, respectively. Communication with plasma proteins – 99%. The time to reach the equilibrium concentration of the drug (Css) with parenteral administration of 30 mg 4 times a day is 24 hours; with intramuscular administration, 15 mg – 0.65–1.13 µg/ml, 30 mg – 1.29-2.47 µg/ml. The volume of distribution (Vd) with intramuscular administration is 0.136-0.214 l/kg, with intravenous administration - 0.166-0.254 l/kg. In patients with renal failure, the volume of distribution of the drug may double, and the volume of distribution of its R-enantiomer may increase by 20%. Penetrates into breast milk: when the mother takes 10 mg of ketorolac, Cmax in milk is achieved 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/l. About 10% of ketorolac passes through the placenta. 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 the pharmacologically inactive 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 3.5-9.2 hours after parenteral administration of 30 mg. T1/2 increases in elderly patients and shortens in young ones. Changes in liver function do not affect T1/2. In patients with impaired renal function, with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l), T1/2 - 10.3-10.8 hours, with more severe renal failure - more than 13.6 h. When 30 mg of ketorolac is administered intramuscularly, the total clearance is 0.023 l/h/kg (0.019 l/h/kg in elderly patients); in patients with renal failure (with a plasma creatinine concentration of 19-50 mg/l) – 0.015 l/h/kg. When 30 mg of ketorolac is administered intravenously, the total clearance is 0.03 l/h/kg. Not excreted by hemodialysis.
Indications for use
Pain syndrome of strong and moderate severity of various origins due to injuries, toothache, pain in the postoperative period, with oncological and rheumatic diseases, myalgia, arthralgia, neuralgia, radiculitis. Intended for symptomatic therapy, reducing pain and inflammation at the time of use. Does not affect the progression of the disease.
Contraindications
- hypersensitivity to ketorolac;
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history);
- erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding; cerebrovascular or other bleeding; - inflammatory bowel diseases (Crohn's disease, ulcerative colitis) in the acute phase; - hemophilia and other bleeding disorders; - decompensated heart failure; - liver failure or active liver disease; - severe renal failure (creatinine clearance less than 30 ml/min), progressive kidney disease, confirmed hyperkalemia; — postoperative period after coronary artery bypass grafting;
- simultaneous use with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants (including warfarin and heparin);
- the drug is not used for prophylactic pain relief before and during major surgical interventions due to the high risk of bleeding;
- pregnancy, childbirth, lactation; - children under 16 years of age (safety and effectiveness have not been established).
Carefully
Bronchial asthma, coronary heart disease, congestive heart failure, edema syndrome, arterial hypertension, cerebrovascular diseases, pathological dyslipidemia or hyperlipidemia, renal dysfunction (creatinine clearance 30-60 ml/l), diabetes mellitus, cholestasis, sepsis, systemic lupus erythematosus, peripheral arterial disease, smoking, old age (over 65 years), history of gastrointestinal ulceration, alcohol abuse, severe somatic diseases, concomitant therapy with the following drugs: antiplatelet agents (for example, clopidogrel), oral glucocorticosteroids (for example, prednisolone ), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
Directions for use and doses
Intravenously, intramuscularly. A solution of the drug Ketorol® is used in minimally effective doses, selected according to the intensity of pain. If necessary, narcotic analgesics can be prescribed at the same time in reduced doses. For parenteral use in patients aged 16 to 64 years with a body weight exceeding 50 kg, no more than 60 mg is administered intramuscularly (including oral administration). Usually - 30 mg every 6 hours; intravenously – 30 mg (no more than 15 doses in 5 days). Intramuscularly, in adult patients weighing less than 50 kg or with chronic renal failure (CRF), a single dose of no more than 30 mg is administered (including oral administration); usually – 15 mg (no more than 20 doses in 5 days); intravenously - no more than 15 mg every 6 hours (no more than 20 doses in 5 days). The maximum daily doses for intramuscular and intravenous administration are for patients from 16 to 64 years old with a body weight exceeding 50 kg - 90 mg/day; adult patients weighing less than 50 kg or with chronic renal failure, as well as elderly patients (over 65 years of age) - for intramuscular and intravenous administration 60 mg. The duration of treatment should not exceed 5 days. When administered intravenously, the dose must be administered over at least 15 seconds. Intramuscular injection is given slowly, deep into the muscle. The onset of analgesic action is noted after 30 minutes, maximum pain relief occurs after 1-2 hours. The analgesic effect lasts about 4-6 hours.
Side effect
The frequency of side effects is classified depending on the frequency of occurrence: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%) , including individual messages. 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 - nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, melena, vomiting like “coffee grounds”, nausea, heartburn and others), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis. From the urinary system: rarely - acute renal failure, lower back pain with or without hematuria and/or azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased urine volume, nephritis, 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, rhinitis, 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. From the cardiovascular system: less often - increased blood pressure; rarely – pulmonary edema, fainting. 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, redness, thickening or flaking of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome. Local reactions: less often - burning or pain at the injection site. Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, shortness of breath, swelling of the eyelids, periorbital edema, difficulty breathing, heaviness in the chest, wheezing). Other: often - swelling (face, legs, ankles, fingers, feet, weight gain); less often – increased sweating; rarely - swelling of the tongue, fever.
Overdose
Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis. Treatment: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital body functions). Not eliminated sufficiently by dialysis.
Interaction with other drugs
The simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, including cyclooxygenase-2 inhibitors, calcium preparations, glucocorticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding. The drug should not be used simultaneously with other NSAIDs (including cyclooxygenase-2 inhibitors), as well as simultaneously with probenecid, pentoxifylline, acetylsalicylic acid, lithium salts, anticoagulants (including warfarin and heparin). Do not use with paracetamol for more than 2 days. Co-administration with paracetamol increases nephrotoxicity, and with methotrexate - hepato- and nephrotoxicity. Co-administration of ketorolac and methotrexate is possible only when using low doses of the latter (monitor the concentration of methotrexate in the blood plasma). Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its concentration in the blood plasma and increases its half-life. With the use of ketorolac, the clearance of methotrexate and lithium may decrease and the toxicity of these substances may increase. Co-administration with indirect anticoagulants (for example, warfarin), heparin, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding. Reduces the effect of antihypertensive and diuretic drugs (the synthesis of prostaglandins in the kidneys is reduced). When combined with narcotic analgesics, the doses of the latter can be significantly reduced. Antacids do not affect the complete absorption of the drug. The hypoglycemic effect of insulin and oral hypoglycemic drugs increases (dose recalculation is necessary). Co-administration with valproic acid causes disruption of platelet aggregation. Increases the plasma concentration of verapamil and nifedipine. 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 the blood plasma.
It is necessary to take into account possible interactions when ketorolac is simultaneously prescribed with cyclosporine, zidovudine, digoxin, tacrolimus, quinolone drugs, selective serotonin reuptake inhibitors, and mifepristone.
special instructions
Ketorol® has two dosage forms (film-coated tablets and solution for intravenous and intramuscular administration). The choice of method of drug administration depends on the severity of the pain syndrome and the patient’s condition.
Before prescribing the drug, it is necessary to clarify the issue of a previous allergic reaction to the drug or 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 prophylactic pain relief, before and during major surgical interventions due to the high risk of bleeding.
The drug should not be used together with NSAIDs (including cyclooxygenase-2 inhibitors), since when taken together with other NSAIDs, fluid retention, cardiac decompensation, and increased blood pressure may occur. The effect on platelet aggregation ceases after 24–48 hours.
The drug may change the properties of platelets.
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 pain) and increasing the dose of the drug to more than 90 mg/day. To reduce the risk of adverse events, the minimum effective dose should be used for the shortest possible short course.
To reduce the risk of developing NSAID gastropathy, misoprostol and omeprazole are prescribed.
The influence of a medicinal product for medical use on the ability to drive vehicles and machinery
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.
Release form
Solution for intravenous and intramuscular administration, 30 mg/ml. 1 ml in Class I (USP) dark glass ampoules. At the top of the ampoule there is a ring and a breaking point. A label is placed on the ampoule. 10 ampoules with instructions for use are placed in a PVC/aluminum blister.
Storage conditions
In a dry place, protected from light, at a temperature not exceeding 25 ° C. Do not freeze! Keep out of the reach of children!
Best before date
3 years. Do not use after the expiration date stated on the packaging.
Conditions for dispensing from pharmacies
On prescription.
Manufacturer
Dr. Reddy's Laboratories Ltd., India Dr. Reddy's Laboratories Ltd., India
Manufacturing address
Unit-I, Plot No. 137, 138 & 146, SVCO-OP, Industrial Estate, Bollaram, Jinnaram Mandal, Medak District, India.
Send information about complaints and adverse drug reactions to:
Representative office: 115035, Moscow, Ovchinnikovskaya embankment, 20, building 1 tel. fax
Overdose
Symptoms of overdose for parenteral use and oral administration: nausea, abdominal pain, vomiting, renal dysfunction, erosive lesions and ulceration of the gastrointestinal mucosa, metabolic acidosis .
If signs of intoxication , the victim is given gastric lavage and enterosorbents . Further treatment is symptomatic. ketorolac to be sufficiently removed from the body.
Cases of overdose with external use of the drug have not been described. If you accidentally ingest the gel, you should empty your stomach (induction of vomiting and taking an enterosorbent ) and consult a doctor.
Interaction
Drug interactions for Ketorol solution and tablets
The use of ketorolac in combination with other NSAIDs, ASA ( acetylsalicylic acid ), ethanol, calcium preparations, corticotropin and corticosteroids can lead to ulceration of the gastrointestinal mucosa and the development of bleeding from ulcerative defects.
Co-administration with Methotrexate increases hepato- and nephrotoxicity, and with Paracetamol - nephrotoxicity. With Methotrexate, ketorolac can be prescribed only if Methotrexate is used in the lowest possible dose (in this case, plasma concentrations of methotrexate ).
Probenecid reduces the volume of distribution and plasma clearance of ketorolac , increases its plasma concentration and increases the half-life. With the use of ketorolac, Methotrexate may decrease , and the toxicity of these substances may increase.
Use in combination with indirect anticoagulants and drugs for thrombolytic therapy , Heparin , cephalosporin antibiotics , antiplatelet agents increases the risk of bleeding.
Ketorolac , acting as an inhibitor of Pg synthesis in the kidneys, reduces the effect of diuretics and antihypertensive drugs .
In the case of simultaneous use with narcotic painkillers, the doses of the latter may be significantly lower.
Antacids do not alter the absorption of ketorolac .
Increases the hypoglycemic effect of oral antidiabetic agents and insulin , which requires dose recalculation.
Combined use with valproic acid provokes a violation of platelet aggregation.
Increases plasma concentrations of Nifedipine and Verapamil .
When combined with other nephrotoxic drugs (for example, with Au preparations), the likelihood of nephrotoxic effects increases.
Drugs that block tubular secretion reduce clearance and increase plasma concentrations of ketorolac .
Drug interactions with topical use of ketorolac
The possibility of pharmacokinetic interaction with drugs competing for binding to plasma proteins cannot be ruled out.
The gel should be used with caution in combination with Phenytoin , other NSAIDs, diuretics , Digoxin , Cyclosporine , Li drugs, Methotrexate , antidiabetic and antihypertensive drugs .
Patients using any of the listed drugs should begin treatment with Ketorol only with the approval of a physician.
Interaction with medications
The drug is not combined with drugs that belong to the following groups:
- NSAIDs, as the frequency of adverse reactions increases;
- muscle relaxants, as breathing is inhibited;
- ACE inhibitors due to the development of kidney dysfunction;
- anticoagulants because the risk of bleeding increases.
The medicine is prescribed carefully together with:
- with cardiac glycosides, as heart failure develops in elderly patients;
- with beta blockers due to a decrease in the hypotensive effect of medications.
special instructions
The choice in favor of one or another dosage form is made taking into account the indications for use and the intensity of pain.
Pills:
Use of Ketorol for more than five days in a row and/or at a dose exceeding the maximum allowable increases the risk of adverse reactions.
The drug should not be prescribed simultaneously with other NSAIDs, since simultaneous use with them leads to cardiac decompensation, fluid retention, and increased blood pressure .
The effects due to the effect of ketorolac on platelet disappear after 24–48 hours.
Ketorolac can change the properties of platelets, but the drug does not replace the preventive effect of ASA in pathologies of the heart and blood vessels.
To reduce the likelihood of developing NSAID gastropathy , the drug should be taken with Omeprazole , Misoprostol , and antacids .
Before prescribing the solution, you should find out whether the patient has previously had an allergic reaction to the drug or other NSAIDs. Due to the risk of hypersensitivity reactions, the first dose is administered under close medical supervision.
Hypovolemia increases the risk of nephrotoxic effects.
It is not recommended to use the solution as a means to prepare a patient for general anesthesia, as well as to maintain anesthesia during extensive surgical interventions.
During treatment with Ketorol, it is recommended to be careful when driving a car or using machinery.
gel (ointment) is recommended to be applied only to intact skin, avoiding contact with wounds and mucous membranes (including the eyes).
The drug should not be used under dressings made of airtight materials. After applying Ketorol to the skin, you should wash your hands well with soap.
Ketorol gel (2% 30gl)
INSTRUCTIONS for the use of the medicinal product for medical use KETOROL ®
Registration number: LP-001080
Trade name of the drug: Ketorol®
International nonproprietary name of the drug: ketorolac.
Dosage form: gel for external use.
Composition Each 1 g of gel contains: Active substance: ketorolac tromethamine (ketorolac trometamol) – 20 mg; Excipients: propylene glycol 300 mg, dimethyl sulfoxide 150 mg, carbomer 974P 20 mg, sodium methyl parahydroxybenzoate 1.8 mg, sodium propyl parahydroxybenzoate 0.2 mg, tromethamine (trometamol) 15 mg, purified water 390 mg, flavoring "Drimon Inde" (triethyl citrate 0 .09%, castor bean seed oil 0.14%, isopropyl myristate 0.30%, diethyl phthalate 24.15%) 3 mg, ethanol 50 mg, glycerol 50 mg.
Description Homogeneous transparent or translucent gel with a characteristic odor.
Pharmacotherapeutic group: non-steroidal anti-inflammatory drug (NSAID)
ATX code: M01AV15
Pharmacological properties Pharmacodynamics Nonsteroidal anti-inflammatory drug (NSAID) has a pronounced analgesic and anti-inflammatory effect. The mechanism of action is associated with non-selective inhibition of the activity of cyclooxygenase (COX) - COX-1 and COX-2, which catalyzes the formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, and the analgesic effect is due to the [-]S form.
When applied topically, it causes a weakening or disappearance of pain at the site of application of the gel, including pain in the joints at rest and during movement, reduces morning stiffness and swelling of the joints. Helps increase range of motion.
Indications for use
Local application for pain relief:
- for injuries (soft tissue bruise, soft tissue inflammation, including post-traumatic origin, ligament damage, bursitis, tendinitis, epicondylitis, synovitis);
- for pain in muscles (myalgia) and joints (arthralgia), neuralgia, radiculitis, rheumatic diseases.
Intended for symptomatic therapy, reducing the intensity of pain and inflammation at the time of use, does not affect the progression of the disease.
Contraindications
- hypersensitivity to ketorolac or other components of the drug;
- weeping dermatoses, eczema, infected or open wounds (at the site of application of the gel);
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid);
- pregnancy (III trimester);
- period of breastfeeding (lactation);
- children up to 16 years of age.
Precautions for use Exacerbation of hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe renal/liver failure, chronic heart failure, bronchial asthma, old age, pregnancy (I and II trimester).
Directions for use and doses
For external use only.
Before applying the gel, wash and dry the skin surface. Apply a uniform thin layer of gel about 1-2 cm long to the area of maximum pain 3-4 times a day. The application of the drug is carried out with soft massaging movements, through which the gel is distributed over the skin over the affected area.
The drug should be reused no earlier than after 4 hours. Use the drug no more than 4 times a day. Do not exceed the indicated dose.
If symptoms persist or worsen, or there is no improvement after 10 days of using the drug, you should stop treatment and consult a doctor. Do not use the gel for more than 10 days without consulting a doctor.
Possible side effects when using the drug
Local reactions: itching, urticaria, peeling.
If any adverse reactions occur, you should stop using the drug and consult your doctor.
When applying the gel to large areas of the skin, the development of systemic adverse reactions cannot be ruled out: heartburn, nausea, vomiting, diarrhea, gastralgia, ulceration of the gastrointestinal mucosa, increased activity of “liver” transaminases; headache, dizziness; fluid retention, hematuria; allergic reactions (anaphylactic shock, skin rash); thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time.
Symptoms of overdose, measures to assist in case of overdose Cases of overdose with gel have not been described. If you accidentally ingest the gel, you must empty your stomach (by inducing vomiting, taking activated charcoal) and consult a doctor. Further treatment, if necessary, is symptomatic.
Interaction with other drugs Pharmacokinetic interaction with drugs that compete for association with blood plasma proteins is not excluded. Caution should be exercised when using ketorolac simultaneously with digoxin, phenytoin, lithium preparations, diuretics, cyclosporine, methotrexate, other NSAIDs, antihypertensive and antidiabetic agents. Before using the gel, you should consult your doctor if you are using these products or are under medical supervision.
special instructions
It is recommended to apply the drug only to intact areas of the skin, avoiding contact with open wounds. Avoid getting the gel into the eyes and other mucous membranes. Do not use the gel under airtight dressings. After applying the gel, wash your hands with soap. Close the tube tightly after using the gel.
Release form
Gel for external use 2%. 30 g in a laminated aluminum tube, equipped with a membrane to control the first opening. Tube with instructions for use in a cardboard box.
Storage conditions
At a temperature not higher than 25 °C. Do not freeze! Keep out of the reach of children!
Best before date
2 years. Do not use after the expiration date stated on the packaging.
Conditions for dispensing from pharmacies
Over the counter.
Manufacturer Dr. Reddy's Laboratories Ltd., India Dr. Reddy's Laboratories Ltd., India
Manufacturing Address : Khol, Nalagarh Road, Baddi, Dist. Solan, Himachal Pradesh, India.
Information about complaints and adverse drug reactions should be sent to the following address: Representative office: 115035, Moscow, Ovchinnikovskaya embankment, 20, building 1 tel. fax
Ketorol's analogs
Level 4 ATC code matches:
Voltaren Emulgel
Ultrafastin
Indomethacin
Dicloran
Dicloran Plus
Dolgit
Nise
Ketonal
Febrofeed
Fastum gel
Diclofenac
Finalgel
Bystrumgel
Deep Relief
Butadion
Diklovit
Artrosilene
Olfen
Fanigan Fast
Structural analogues of tablets and solution: Adolor , Vatorlak , Ketanov , Dolak , Dolomin , Ketofril , Ketalgin , Ketorolac , Ketocam .
Drugs with a similar mechanism of action: Arthrotek , Bioran , Voltaren , Diclak , Diclogen , Diclofenac , Indomethacin , Naklofen , Ortofen , Neurodiclovit , Flotac , SwissJet .
Suppositories with a similar effect: Voltaren , Diclak , Diclonate P , Naklofen , Diclofenac , Indomethacin .
What is better - Ketorol or Ketonal?
Ketonal is a drug based on the NSAID ketoprofen (a derivative of propionic acid). The medicine has the same indications for use as Ketorol.
When administered parenterally, the analgesic effect appears within 15-30 minutes. With intravenous infusion of ketorolac , plasma concentrations reach maximum values after 4 minutes.
The difference between ketoprofen and ketorolac is also a shorter half-life - less than 2 hours.
Studies of the effectiveness of drugs for pain relief in postoperative patients have shown that ketorolac provides a faster, more effective and longer-lasting effect than its analogue, and also has a lesser effect on the hemostatic system.
Is it possible to give Ketorol to children?
The annotation states that all dosage forms of the drug are intended for the treatment of patients over 16 years of age (according to Wikipedia, age under 16 years of age is a relative contraindication).
The reason for this restriction is that the use of ketorolac in children can cause visual and hearing impairment, depression , nephritis , pulmonary edema , allergic reactions and other severe complications.
Therefore, it is better to give the child safer means to relieve pain - for example, paracetamol or ibuprofen .
Reviews of Ketorol
Reviews of Ketorol tablets, as well as reviews of injections and gel, are positive in 95-98% of cases. Ketorol helps with toothache, back and muscle pain, and headaches within half an hour, and its effect lasts up to six hours.
Most patients note that when using the medicine in accordance with the instructions, side effects occur extremely rarely. Sometimes the disadvantages of Ketorol are a large number of contraindications and the impossibility of long-term use.
Note!
The description of the drug Ketorol on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
How much do Ketorol tablets, gel and ampoules cost?
The price of Ketorol in tablets in Ukrainian pharmacies is 29-37 UAH. Injections can be bought for 98-105 UAH. The price of Ketorol gel is 55-62 UAH.
In Russia, the average price of Ketorol in tablets is 45 rubles, the price of Ketorol in ampoules is 145 rubles, the cost of ointment (gel) is 215 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Ketorolac tab.
p.p.o. 10 mg 20 pcs JSC Tatkhimfarmpreparaty 38 rub. order - Ketorol solution for intravenous and intramuscular administration. 30mg/ml 1ml 10 pcs.Dr. Reddy's lab.
136 RUR order
- Ketorol gel 2% 30gDr. Reddy's lab.
RUB 283 order
- Ketorol express tab. dispersant in the oral cavity 10 mg 20 pcs.Dr. Reddy's lab.
63 RUR order
- Ketorolac solution for intravenous and intramuscular administration. 30mg/ml amp. 1ml 10 pcs. Biosynthesis JSC
69 RUR order
Pharmacy Dialogue
- Ketorol (amp. i.v. i.m. 30 mg/ml No. 10)Dr. Reddy's
134 RUR order
- Ketorolac (tab.p.pl/vol. 10mg No. 28)Update of PFC CJSC
68 RUR order
- Ketorol (gel tube 2% 30g)Dr. Reddy's
RUB 262 order
- Ketorolac (amp. 30 mg/ml 1 ml No. 10) Sintez (Kurgan) OJSC
89 rub. order
- Ketorol Express (tablet dispensed in half the mouth 10 mg No. 20) Dr. Reddy's Laboratories Ltd.
64 RUR order
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Pharmacy24
- Ketorol 2% 30 g gel Dr. Reddy's Laboratories Ltd., India
72 UAH.order - Ketorol 30 mg/1 ml N10 solution Dr. Reddy's Laboratories Ltd., India
175 UAH order
- Ketorol 10 mg No. 20 tablets Dr. Reddy's Laboratories Ltd., India
75 UAH order
PaniPharmacy
- Ketorol tablets Ketorol film-coated tablets 10 mg No. 20 India, Dr. Reddy's
93 UAH order
- KETOROLAC ampoule Ketorolac r/r d/in. 3% 1ml. No. 10 Ukraine, Health LLC
99 UAH order
- Ketorol ampoule Ketorol solution d/in. 30mg amp. 1ml No. 10 India, Dr. Reddy's
152 UAH order
- KETOROLAC tablets Ketorolac tablets. 10mg No. 10 Ukraine, Health LLC
18 UAH order
- Ketorol gel Ketorol gel 2% 30g India, Dr. Reddy's
85 UAH order
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