The drug Ketanov is used in medicine for effects on pain centers different type. The active component of ketorolac in the composition of the drug reduces body temperature and reduces the manifestations of inflammatory processes. The drug is comparable in strength to morphine, but differs in that such narcotic anti-inflammatory drugs affect motor skills and muscle function, while Ketan painkillers do not. The drug does not disrupt the respiratory system and does not lead to dependence on its intake.
Description of the drug Ketanov
pharmachologic effect
In the human body, the drug has the following effect:
- moderately reduces fever;
- reduces inflammation;
- helps with pain by blocking the production of biologically active substances.
The drug Ketanov shows a maximum concentration one hour after an intramuscular injection - activity is observed when combined with blood proteins after using a normalized dose of 10 mg, in percentage terms, such relationships reach 99%. At the same time, accumulations are not observed even when using increased norms of the drug.
In the body, the drug is modified by a number of biochemical processes and is excreted from the body by the urinary system 8-12 hours after ingestion. If there is a violation in the functioning of the kidneys or the patient has reached retirement age, then the excretion time slows down and depends on the degree of change in the functioning of the urinary system.
Pharmacodynamics of anesthetic tablets Ketanov
The work of the drug in the body is associated with blocking the biological synthesis of pain, inflammatory and thermoregulatory modulators (PG). A racemic mixture of [-] S- and [+] R-enantiomers in the form of [-] S predominantly works in peripheral tissues and inhibits the activity of COX-1 and COX-2 enzymes.
There is no activity of Ketanov tablets when acting on opioid receptors, therefore, there was no dependence on intake, respiratory failure, anxiolytic and sedative effects. Power of action similar to morphine, and various non-steroidal anti-inflammatory drugs, the drug is superior in action. The patient feels a significant reduction in pain half an hour after administration or administration, and the maximum effect is manifested after 1-1.5 hours.
Pharmacokinetics of the drug
Absorption of the drug occurs in the stomach and intestines, from where it enters the bloodstream. Simultaneous intake of fatty foods doubles the absorption time. Hypoalbuminemia contributes to an increase in the concentration of Ketanov in the blood. The composition allows to obtain the bioavailability of the drug at the level of 80-100%.
Time to reach working blood concentration:
More than half of the dose taken is metabolized in the liver, with the formation of pharmacologically inactive metabolites, the main of which are glucuronides and hydroxyketorolac. Metabolites leave the body a person through the genitourinary system by 91%, the rest is excreted through the intestines. Withdrawal occurs during the periods:
Instructions for use of Ketanov tablets
Indications for the use of the drug
The drug is prescribed to patients to relieve pain in diseases:
- joint pain;
- rheumatism, neuritis and neuralgia with unspecified etiology;
- dorsalgia;
- myalgia;
- radiculopathy;
- constant pain without signs of relief;
- pain of unspecified etiology after surgery.
Method of using the drug
The injection form of Ketanov in ampoules is used intramuscularly, the initial dosage is 10 mg. It is allowed, if necessary, to increase the rate after 4-5 hours until reaching 30 mg. The maximum allowable rate is 90 mg for young and middle-aged patients, and for pensioners and those whose body weight is less than 50 kg, it is reduced to 60 mg. With this dosage, it is not allowed to use the drug for more than 2 days.
The tablet form is prescribed to patients after 5-6 hours, 1 piece each, the total duration of therapy cannot last more than 7 days. The dosage of the drug in each case is prescribed by the doctor. For elderly patients, the rate of the drug should be reduced.
Features of using Ketanov
For the treatment of patients who have persistent hypertension, other similar diseases, changes in blood clotting, constant medical supervision and monitoring of platelet count is indicated. This is important for the control of hemostasis during the period after operations. The termination of reception of drug is made without preliminary decrease in a dosage.
The effect of the drug on platelet aggregation becomes less and stops after a day or two, depending on the prescribed rate, after the drug is discontinued. If the patient suffers from hypovolemia, then this gives an additional risk for the occurrence of unwanted renal reactions. If necessary, the joint use of Ketanov simultaneously with analgesics of the narcotic group is allowed.
It is not allowed to use the drug in case of supporting anesthesia in the practice of obstetric activities. For people working with precise mechanisms, drivers and workers in a high-risk area, work should be suspended while taking the drug, since drowsiness often develops, there is dizziness.
Ketanov: side effects
Frequent side effects occur in more than 3% of cases of drug prescription. Less frequent manifestations are observed in 3% of patients, rare cases are observed when using Ketanov, side effects occur in less than 1% of patients.
The digestive system responds to drug therapy most often in older people (over 65 years old), as well as those who suffer from ulcers and erosions of the stomach and intestines. Patients experience symptoms of diarrhea, gastralgia, in less rare cases, stomatitis develops in the oral cavity, constipation, nausea, and fullness in the stomach is felt. Very rarely, taking the drug causes erosion and ulcers of the intestines and stomach with bleeding or perforation. This side effect is accompanied by vomiting in the form of coffee grounds, spasms, chalky, heartburn and burning in the stomach. Side effects affect the pancreas (acute pancreatitis develops), liver (hepatitis, cholestatic jaundice).
On the part of the kidneys, the side effect is manifested in the appearance of acute insufficiency, the lumbar region hurts, azotemia and hematuria may join, uremic hemolytic anemia, purpura, and thrombocytopenia develop. Patients note an increase or decrease in urine output, frequent urge to urinate, swelling from poor kidney function.
In rare cases, hearing loss occurs appearance of tinnitus, vision deteriorates, objects are not clearly distinguished. The respiratory system malfunctions in the form of dyspnea, bronchial spasms, runny nose, shortness of breath, difficult breathing and laryngeal edema.
Frequent side effects from the nervous system are headache, constant desire to sleep. Rare effects are aseptic meningitis, fever, convulsions, weakening of muscle tissue on the back or in the neck. And also rarely develop depressive states, psychoses, hallucinations appear.
Blood pressure rises, pulmonary edema develops, fainting occurs. In the blood system, changes rarely include the appearance of anemia, leukopenia, eosinophilia. In the postoperative period, bleeding from the wound, nose rarely joins, rectal bleeding occurs. Sometimes a rash appears on the skin, dermatitis with a feverish course may develop, the surface of the body flakes off, the tonsils swell in the sky. At the injection site, the skin burns and pain is felt.
Allergic manifestations rarely occur in the form of anaphylactic reactions, including symptoms:
Contraindications
There are diseases in which the drug is prescribed with caution, the doctor monitors the patient's well-being:
- cholecystitis, cholestasis;
- bronchial asthma;
- impaired renal function with plasma creatinine below 50 mg / l;
- arterial hypertension;
- chronic heart failure;
- active hepatitis;
- polyps in the nose and throat;
- systemic lupus erythematosus.
Interaction with other medical devices
With caution, the drug should be prescribed simultaneously with NVPS, acetylsalicylic acid, calcium agents, corticotropin and ethanol, since the interaction of these drugs leads in some cases to bleeding from the intestines and stomach due to the appearance of ulcers on their walls.
The simultaneous use of paracetamol increases the effect of toxic substances on the kidneys, methotrexate causes the same effect on the liver. Simultaneous use with methotrexate is allowed, provided that the latter is prescribed in the smallest doses.
Probenicide helps to reduce distribution of ketorolac and increases its accumulation in the blood plasma, in addition, with the simultaneous use of Ketan tablets and probenecid, the time of excretion from the body increases. At the same time, the clearance of lithium and methotrexate decreases, which contributes to an increase in the toxic effect.
Combined use with indirect anticoagulants, thrombolytics, cefoperazone, heparin, antiplatelet agents, cefotetan increases the risk of bleeding. Due to a decrease in the production of PG in the kidneys, the effect of diuretics and antihypertensive drugs is reduced. Helps increase the effect of opioid analgesics, which is why it is recommended to reduce their intake rate.
Helps enhance the effects of hypoglycemic drugs and insulin, so the dosage is reduced. Antacids, when used together, have no effect on the degree of absorption. Platelet aggregation is disturbed due to the joint interaction of Ketones and valproate. Accumulation of nifedipine and verapamil in the blood increases when used together in treatment.
With an intramuscular injection, the drug is not mixed with morphine sulfate, hydroxyzine and promethazine, since their interaction causes precipitation.
Storage and holiday conditions
Ketanov in the form of tablets and injections in ampoules is stored in a dark and dry place at temperatures up to 25 ° C. The manufacturer specifies a shelf life of 2 years. The drug is dispensed in pharmacies by prescription.
Instruction
Compound
active substance: ketorolac tromethamine;
I coated tablet contains ketorolac tromethamine 10 mg;
Excipients: microcrystalline cellulose, corn starch, magnesium stearate, talc, anhydrous colloidal silicon dioxide, hypromellose, macrogol, titanium dioxide (E 171).
Pharmacotherapeutic groupsA
Nonsteroidal anti-inflammatory and antirheumatic drugs.
ATS code: M01AB15.
Indications
Ketanov film-coated tablets, 10 mg is used for the short-term treatment of acute pain (including postoperative pain) of moderate intensity, only as a continuation of previous parenteral (intramuscular or intravenous) therapy in a hospital setting, if necessary. The total duration of parenteral and oral therapy with ketorolac should not exceed 5 days.
Contraindications
Hypersensitivity to ketorolac or any component of the drug; patients with active peptic ulcer, with recent gastrointestinal bleeding or perforation, with a history of peptic ulcer or gastrointestinal bleeding; bronchial asthma, rhinitis, angioedema or urticaria caused by the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (due to the possibility of severe anaphylactic reactions); bronchial asthma in history; do not use as an analgesic before and during surgery; - severe heart failure; complete or partial nasal polyp syndrome, Quincke's edema or bronchospasm; do not use in patients who have had surgery with a high risk of hemorrhage or incomplete bleeding and in patients who receive anticoagulants, including low doses of heparin (2500-5000 units every 12 hours); hepatic or moderate and severe renal insufficiency (creatinine clearance in blood serum is more than 160 µmol/l); suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, including bleeding disorders and a high risk of bleeding; simultaneous treatment with other non-steroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase inhibitors), acetylsalicylic acid, warfarin, pentoxifylline, probenecid or lithium salts; hypovolemia, dehydration; the period of pregnancy, contractions, childbirth and breastfeeding; children's age up to 16 years.
Dosage and administration
Tablets are preferably taken during or after meals. The drug is recommended only for short-term use (up to 5 days). In order to minimize side effects, the drug should be used at the lowest effective dose for the shortest period of time necessary to control symptoms. Before starting treatment, it is necessary to achieve normovolemia. Adult Ketans are prescribed 10 mg every 4-6 hours if necessary. It is not recommended to use the drug in doses that exceed 40 mg per day. Opioid analgesics (eg, morphine, pethidine) can be used in parallel, ketorolac does not affect the binding of opioid drugs and does not increase the respiratory depression or sedation that is characteristic of opioids. For patients who receive parenteral ketorolac and who are prescribed ketorolac orally in tablet form, the total combined daily dose should not exceed 90 mg (60 mg for the elderly, patients with impaired renal function and patients weighing less than 50 kg), and the dosage of the oral form of the drug should not exceed 40 mg per day if the use of the drug release form is changed. Patients should be switched to oral administration of the drug as soon as possible.
Elderly patients
Elderly patients have a higher risk of developing severe complications, in particular from the digestive tract. During treatment with NSAIDs, you should regularly monitor the patient's condition, usually a longer interval between the use of the drug is recommended, for example 6-8 hours.
Adverse reactions
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, sensation gastric overflow, melena, rectal bleeding, ulcerative stomatitis, vomiting, hemorrhage, perforation, pancreatitis, exacerbation of colitis and Crohn's disease.
From the side of the central nervous system: anxiety, visual impairment, optic neuritis, drowsiness, dizziness, increased sweating, dry mouth, nervousness, paresthesia, functional disorders, depression, euphoria, convulsions, inability to concentrate, insomnia, increased fatigue, agitation, vertigo, impaired taste and vision, myalgia, unusual dreams, confusion, hallucinations, hyperkinesia, hearing loss, tinnitus, psychotic reactions, thought disorders.
Infectious diseases: aseptic meningitis (especially in patients with autoimmune diseases such as systemic lupus erythematosus, mixed connective tissue disease), neck stiffness, headache, nausea, vomiting, fever, confusion.
Metabolism and nutrition: anorexia, hyponatremia, hyperkalemia.
So sides of the urinary system: increased frequency of urination, oliguria, acute renal failure, hemolytic uremic syndrome, flank pain (with/without hematuria), elevated serum urea and creatinine, interstitial nephritis, urinary retention, nephrotic syndrome, infertility, renal failure.
From the side of the liver: abnormal liver function, hepatitis, jaundice and liver failure, increased functional tests.
From the side of the cardiovascular system: flushing, bradycardia, pallor, hypertension, hypotension, palpitation, chest pain, edema, heart failure.
Data from clinical and epidemiological studies suggest that the use of some NSAIDs, especially at high doses and for a long time, may be associated with an increased risk of developing arterial thromboembolic complications (myocardial infarction or stroke).
co sides of the respiratory system: epistaxis, shortness of breath, asthma, pulmonary edema.
From the blood system: purpura, thrombocytopenia, neutropenia, agranulocytosis, aplastic and hemolytic anemia.
From the side of the skin: itching, urticaria, skin photosensitivity, Lyell's syndrome, bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (very rarely), exfoliative dermatitis, maculopapular rashes.
Impact on reproductive function:
The use of ketorolac, as well as any drug that inhibits the synthesis of cyclooxygenase / prostaglandin, can cause infertility.
Hypersensitivity: hypersensitivity reactions have been reported that include non-specific allergic reactions and anaphylaxis, respiratory tract reactivity including asthma, worsening of asthma, bronchospasm, laryngeal edema or dyspnea, and a variety of skin disorders that include various types of rash, pruritus, urticaria , purpura, angioedema, and in single cases, exfoliative and bullous dermatitis (including epidermal necrolysis and erythema multiforme).
Such reactions may occur in patients with or without known hypersensitivity to ketorolac or other non-steroidal anti-inflammatory drugs. They can also be seen in individuals with a history of angioedema, bronchospastic reactivity (eg, asthma and nasal polyps). Anaphylactoid reactions such as anaphylaxis can be fatal.
Other: postoperative wound bleeding, hematoma, prolongation of bleeding, asthenia, edema, weight gain, fever, excessive thirst, fatigue, malaise, fever, chest pain.
Overdose
Symptoms: headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding; rarely - diarrhea, disorientation, agitation, coma, drowsiness, dizziness, tinnitus, loss of consciousness, sometimes convulsions. In cases of severe poisoning, acute renal failure and liver damage are possible.
Anaphylactoid reactions have been observed after the therapeutic use of NSAIDs, which may occur after an overdose.
Treatment: gastric lavage, the use of activated charcoal. It is necessary to provide sufficient diuresis. The function of the kidneys and liver should be carefully monitored. Patients should be observed 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 clinical condition of the patient. Therapy is symptomatic.
Use during pregnancy or lactation
The safety of ketorolac during pregnancy in humans has not been established. Given the known effect of NSAIDs on the fetal cardiovascular system (risk of premature closure of the ductus arteriosus), ketorolac is contraindicated during pregnancy, labor and childbirth. The onset of labor may be delayed and the duration prolonged, with an increased tendency for both mother and child to bleed.
Ketorolac is excreted in breast milk in small amounts, so Ketanov is contraindicated during lactation.
Children
Do not apply to children under 16 years of age.
Application features
The maximum duration of treatment should not exceed 5 days.
Impact on fertility
The use of ketorolac, as with any drug that inhibits cyclooxygenase/prostaglandin synthesis, may impair fertility and is not recommended for use in women who plan to become pregnant. For women who are unable to conceive or are undergoing fertility tests, discontinuation of ketorolac should be considered.
Gastrointestinalbleeding, ulceration and perforation
Gastrointestinal bleeding, ulceration, or perforation, which can be fatal, has been reported with NSAIDs used at any time during treatment with or without warning symptoms or with a history of severe gastrointestinal disturbances. The risk of developing severe gastrointestinal bleeding depends on the dosage of the drug. This, in particular, applies to elderly patients who use ketorolac in an average daily dose above 60 mg. For these patients, as well as for patients who are simultaneously using low doses of acetylsalicylic acid or other drugs that may increase the risk to the digestive tract, combination treatment with protective agents (for example, misoprostol or proton pump inhibitors) should be considered. Ketanov should be used with caution in patients receiving concomitant medications that may increase the risk of ulceration or bleeding, such as oral corticosteroids, selective serotonin reuptake inhibitors, or antiplatelet agents such as acetylsalicylic acid. In the event of gastrointestinal bleeding or ulceration in patients receiving Ketanov, 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 it has been reported that NSAIDs in such patients accelerate the onset of bronchospasm.
Effect on the kidneys
Inhibitors of prostaglandin biosynthesis (including NSAIDs) have been reported to have nephrotoxic effects. With caution, the drug is prescribed to patients with impaired renal function, heart, liver, since the use of NSAIDs can lead to a deterioration in kidney function. Patients with mild impairment of renal function are prescribed lower doses of ketorolac (those that do not exceed 60 mg per day intramuscularly or intravenously), and the condition of the kidneys in such patients should be carefully monitored. As with other drugs that inhibit prostaglandin synthesis, there have been reports of increases in serum urea, creatinine and potassium while taking ketorolac tromethamine, which can occur after taking a single dose.
Cardiovascular, kidney and liver disorders
With caution, the drug is prescribed to patients with conditions that lead to a decrease in blood volume and / or renal blood flow, when renal prostaglandins play a supporting role in ensuring renal perfusion. In these patients, renal function should be monitored. The decrease in volume should be corrected and the serum urea and creatinine levels, as well as the volume of urine that is excreted, should be carefully monitored until the patient becomes normovolemia. In patients who are on renal dialysis, the clearance of ketorolac was reduced by approximately half of the normal rate, and the terminal half-life increased by approximately three times. Patients with impaired liver function due to cirrhosis had no clinically significant changes in ketorolac clearance or terminal half-life. Marginal increases in values may be observed on one or more liver function tests. These abnormalities may be temporary, may remain unchanged, or may progress with continued treatment. If clinical signs and symptoms indicate the development of liver disease or if systemic manifestations are observed, Ketanov should be discontinued.
Fluid retention and swelling
Fluid retention and edema have been reported during the use of ketorolac, so it should be administered with caution to patients with cardiac decompensation, arterial hypertension or similar conditions.
Cardiovascular and cerebrovascular effects
There is currently insufficient information to assess this risk for ketorolac tromethamine. Patients with uncontrolled arterial hypertension, congestive heart failure, diagnosed coronary heart disease, peripheral arterial disease and / or cerebrovascular disease should be under medical supervision.
Systemic lupus erythematosus and mixed connective tissue diseases
Patients with systemic lupus erythematosus and various mixed connective tissue diseases have an increased risk of developing aseptic meningitis.
Dermatological
Ketanov should be discontinued at the first sign of a skin rash, mucosal lesions, or any other sign of hypersensitivity.
Anaphylactic (anaphylactoid)reactions
As with other NSAIDs, anaphylactic (anaphylactoid) reactions (including anaphylaxis, bronchospasm, hyperemia, rash, 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 complex of symptoms can also be observed in individuals who have a history of bronchospastic reactivity (eg, asthma) and nasal polyps. Anaphylactoid reactions such as anaphylaxis can be fatal. Therefore, ketorolac should not be taken in patients with a history of asthma and in patients with complete or partial nasal polyp syndrome, angioedema, and bronchospasm. If anaphylactoid reactions occur, seek emergency medical attention.
Hematological effects
Patients with bleeding disorders should not be prescribed Ketanov. Patients receiving anticoagulant therapy may have an increased risk of bleeding if ketorolac is used concomitantly. The condition of patients who receive other drugs that can affect the rate of bleeding should be carefully monitored when prescribing ketorolac to them. In controlled clinical trials, the incidence of significant postoperative bleeding was less than 1%. Ketorolac inhibits platelet aggregation and prolongs bleeding time. In patients with normal bleeding time, the duration of bleeding increased, but did not go beyond the normal range of values of 2-11 minutes. In contrast to the long-term effect as a result of the use of acetylsalicylic acid, platelet function returns to normal within 24-48 hours after the withdrawal of ketorolac. Ketorolac should not be given to patients who have undergone surgery with a high risk of bleeding or incomplete bleeding. Caution should be exercised if mandatory bleeding control is critical. Ketanov is not an anesthetic and does not have sedative or anxiolytic properties, therefore it is not recommended as a premedication before surgery to maintain anesthesia.
The ability to influence the reaction rate when driving vehicles or working with other mechanisms
Some patients may experience drowsiness, dizziness, vertigo, insomnia, fatigue, blurred vision or depression when using Ketorolac. If patients experience the above or other similar side effects, they should not drive or operate machinery.
Interaction with other medicinal products and other forms of interaction
Ketorolac readily binds to plasma proteins (mean value 99.2%), and the degree of binding depends on the concentration.
Cannot be used simultaneously withketorolac
Due to the possibility of side effects, ketorolac should not be administered with other NSAIDs, including selective cyclooxygenase-2 inhibitors, or in patients receiving acetylsalicylic acid, warfarin, lithium, probenecid, cyclosporine. NSAIDs should not be administered within 8-12 days after the use of mifepristone, since NSAIDs may weaken the effect of mifepristone.
Medicines in combination with ketorolac should be administered with caution.
In healthy subjects with normovolemia, ketorolac reduces the diuretic effect of furosemide by approximately 20%, therefore, the drug is prescribed with particular caution in patients with cardiac decompensation. NSAIDs may exacerbate heart failure, decrease glomerular filtration rate, and increase plasma levels of cardiac glycosides when administered concomitantly with cardiac glycosides. Ketorolac and other non-steroidal anti-inflammatory drugs may weaken the effect of antihypertensive drugs. In the case of simultaneous use of ketorolac with ACE inhibitors, there is an increased risk of impaired renal function, especially in patients with a reduced blood volume in the body. There is a possible risk of nephrotoxicity if NSAIDs are co-administered with tacrolimus. Co-administration with diuretics may lead to a weakening of the diuretic effect and an increased risk of NSAID nephrotoxicity. As with all NSAIDs, concomitant corticosteroids should be used with caution due to an increased risk of gastrointestinal ulceration or bleeding. There is an increased risk of gastrointestinal bleeding if NSAIDs are given in combination with antiplatelet agents and selective serotonin reuptake inhibitors. Caution is advised if methotrexate is given concomitantly, as some prostaglandin synthesis inhibitors have been reported to reduce the clearance of methotrexate and therefore possibly increase its toxicity. Patients taking NSAIDs and quinolones may be at an increased risk of developing seizures.
The simultaneous use of NSAIDs with zidovudine leads to an increased risk of hematological toxicity. There is an increased risk of hemarthrosis and hematoma in HIV-infected patients who have hemophilia and who are treated concomitantly with zidovudine and ibuprofen.
The following drugs are unlikely to interact with ketorolac
Ketorolac did not affect the binding of digoxin to plasma protein. Research in vitro indicate that at therapeutic concentrations of salicylate (300 μg / ml) and higher, the binding of ketorolac decreased from approximately 99.2% to 97.5%. Therapeutic concentrations of digoxin, warfarin, paracetamol, phenytoin and tolbutamide did not affect the binding of ketorolac to plasma protein. Since ketorolac is a highly active drug and its plasma concentration is low, it is not expected to significantly replace other drugs that bind to plasma proteins. In animal and human studies, there was no evidence that ketorolac tromethamine induces or inhibits liver enzymes that are capable of metabolizing it or other drugs. Therefore, ketorolac is not expected to alter the pharmacokinetics of other drugs through an enzyme induction or inhibition mechanism.
Pharmacological properties
Pharmacodynamics
Ketorolac tromethamine is a non-narcotic analgesic. It is a non-steroidal anti-inflammatory drug that exhibits anti-inflammatory and weak antipyretic activity. Ketorolac tromethamine inhibits prostaglandin synthesis and is considered a peripheral analgesic. It has no known effect on opiate receptors. After the use of ketorolac tromethamine in controlled clinical trials, no phenomena were observed that would indicate respiratory depression.
Ketorolac tromethamine does not cause pupillary constriction.
Pharmacokinetics
Ketorolac tromethamine is rapidly and completely absorbed after oral administration, with a peak plasma concentration of 0.87 µg/ml 50 minutes after a single 10 mg dose. In healthy volunteers, the terminal plasma half-life is, on average, 5.4 hours. In the elderly (mean age 72 years), it is 6.2 hours. More than 99% of ketorolac in plasma is protein bound. In humans, after the use of single or multiple doses, the pharmacokinetics of ketorolac is linear. Steady-state plasma levels are reached after one day when applied 4 times a day. With long-term dosing, no changes were observed. 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.
On prescription.
Manufacturer
K.K. Therapia A.T., Romania, st. Fabricii, 124, 400632, Cluj-Napoca, Romania.
S.C. Terapia S.A., Romania, str. Fabricii, 124, 400632 Cluj-Napoca, Romania.
Composition and form of release
in a blister 10 pcs.; in a pack of cardboard 1, 2, 3 or 10 blisters.
in ampoules of 1 ml; in a pack of cardboard 5 or 10 pcs.
Description of the dosage form
Pills: round, biconvex, white or off-white coated, engraved with "KVT" on one side.
Injection: clear colorless or pale yellow solution.
pharmachologic effect
pharmachologic effect- antipyretic, anti-inflammatory, analgesic.Pharmacodynamics
Ketorolac has a pronounced analgesic effect, also has an anti-inflammatory and moderate antipyretic effect.
The mechanism of action is associated with non-selective inhibition of the activity of the COX-1 and -2 enzyme, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of PG - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of [-]S- and [+]R-enantiomers, with the analgesic effect due to the [-]S form.
The drug does not affect opioid receptors, does not depress breathing, does not cause drug dependence, does not have a sedative and anxiolytic effect.
The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs.
After i / m administration and oral administration, the onset of analgesic action is noted after 0.5 and 1 hour, respectively, the maximum effect is achieved after 1-2 hours.
Pharmacokinetics
After oral administration, Ketanov ® is well absorbed in the gastrointestinal tract - C max in blood plasma (0.7-1.1 μg / ml) is reached 40 minutes after taking a dose of 10 mg on an empty stomach. Food rich in fats reduces the Cmax of the drug in the blood and delays its achievement by 1 hour. 99% of the drug binds to plasma proteins, and with hypoalbuminemia, the amount of free substance in the blood increases. Bioavailability - 80-100%.
Absorption at the / m introduction - complete and fast. After intramuscular administration of 30 mg of the drug, C max is 1.74-3.1 μg / ml, 60 mg - 3.23-5.77 μg / ml, T max - 15-73 and 30-60 minutes, respectively.
The time to reach equilibrium concentration (C SS ) with parenteral and oral administration is 24 hours when administered 4 times a day (above subtherapeutic) and is 0.65-1.13 μg / ml with i.m. administration at a dose of 15 mg, 30 mg - 1.29-2.47 mcg / ml; after oral administration of 10 mg - 0.39-0.79 mcg / ml. The volume of distribution is 0.15-0.33 l/kg. In patients with renal insufficiency, the volume of distribution of the drug can increase by 2 times, and its R-enantiomer by 20%.
Penetrates into breast milk: after the first and second doses of ketorolac (10 mg) are taken by the mother, Cmax in milk is reached after 2 hours and is 7.3 and 7.9 ng / l, respectively.
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 by 91% - by the kidneys, 6% - through the intestines.
T 1/2 in patients with normal renal function averages 5.3 hours (3.5-9.2 hours after intramuscular administration of 30 mg and 2.4-9 hours after oral administration of 10 mg). T 1/2 lengthens in elderly patients and shortens in young. Liver function does not affect T 1/2. In patients with impaired renal function, with a plasma creatinine concentration of 19-50 mg / l (168-442 μmol / l), T 1 / 2 is 10.3-10.8 hours, with more severe renal failure - more than 13.6 h.
The total clearance is at a / m administration at a dose of 30 mg 0.023 l / kg / h (0.019 l / kg / h in elderly patients), orally at a dose of 10 mg - 0.025 l / kg / h; with renal failure with a plasma creatinine concentration of 19-50 mg / l with a / m administration at a dose of 30 mg - 0.015 l / kg / h, with oral administration of 10 mg - 0.016 l / kg / h.
Not excreted during hemodialysis.
Indications for Ketanov ®
Pain syndrome of medium and severe intensity of various origins (including in the postoperative period, with oncological diseases).
Contraindications
hypersensitivity to ketorolac or other NSAIDs, "aspirin asthma", bronchospasm, angioedema, hypovolemia (regardless of the cause that caused it), dehydration;
erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, peptic ulcers, hypocoagulation (including hemophilia);
hepatic and / or renal failure (plasma creatinine above 50 mg / l);
hemorrhagic stroke (confirmed or suspected), hemorrhagic diathesis, simultaneous use with other NSAIDs, a high risk of developing or recurrent bleeding (including after surgery), impaired hematopoiesis;
pregnancy, childbirth and lactation;
children under 16 years of age (efficacy and safety have not been established);
pain relief before and during surgery (due to the high risk of bleeding);
treatment of chronic pain.
Carefully- bronchial asthma; cholecystitis; chronic heart failure; arterial hypertension; impaired renal function (plasma creatinine below 50 mg / l); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; old age (over 65 years); polyps of the nasal mucosa and nasopharynx.
Side effects
The frequency of development of side effects is determined as follows: 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 - 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, coffee grounds vomiting, nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.
From the urinary system: rarely - acute renal failure, back pain with or without hematuria and / or azotemia, hemolytic uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increase or decrease in urine volume, nephritis, edema of renal origin.
From the sense organs: rarely - hearing loss, tinnitus, visual impairment (including blurred vision).
From the respiratory system: rarely - bronchospasm or dyspnea, rhinitis, laryngeal edema (shortness of breath, shortness of breath).
From the side of the central nervous system: often - headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, convulsions, neck and / or back muscle stiffness), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis.
From the side of the cardiovascular system: less often - increased blood pressure; rarely - pulmonary edema, fainting.
From the side of the hematopoietic organs: rarely - anemia, eosinophilia, leukopenia.
From the hemostasis system: rarely - bleeding from a postoperative wound, epistaxis, rectal bleeding.
From the side of the skin: less often - skin rash (including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and / or soreness of the palatine 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 (discoloration of the skin of the face, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, shortness of breath, heaviness in the chest, wheezing).
Others: often - edema (face, legs, ankles, fingers, feet, weight gain); less often - excessive sweating; rarely - swelling of the tongue, fever.
Interaction
Simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium preparations, corticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding.
Co-administration with paracetamol increases nephrotoxicity, with methotrexate - hepato- and nephrotoxicity. The joint appointment of ketorolac and methotrexate is possible only when using low doses of the latter (to control the concentration of methotrexate in the blood plasma).
Probenicid reduces plasma clearance and volume of distribution of ketorolac, increases its concentration in blood plasma and increases its half-life. Against the background of the use of ketorolac, a decrease in the clearance of methotrexate and lithium and an increase in the toxicity of these substances are possible. Simultaneous administration with indirect anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding. Reduces the effect of antihypertensive and diuretic drugs (the synthesis of PG in the kidneys decreases). When combined with opioid 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 sodium valproate causes a violation of platelet aggregation. Increases plasma concentration of verapamil and nifedipine.
When administered 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 blood plasma.
Solution for injection should not be mixed in the same syringe with morphine sulfate, promethazine and hydroxyzine due to precipitation. Pharmaceutically incompatible with tramadol solution, lithium preparations.
The injection solution is compatible with physiological saline, 5% dextrose solution, Ringer's solution and Ringer's lactate solution, "Plasmalit" solution, as well as with infusion solutions containing aminophylline, lidocaine hydrochloride, dopamine hydrochloride, short-acting human insulin and heparin sodium salt.
Dosage and administration
Pills. inside, once or repeatedly, depending on the severity of the pain syndrome. Single dose - 10 mg, with repeated admission, it is recommended to take 10 mg up to 4 times a day, depending on the severity of pain; the maximum daily dose should not exceed 40 mg.
When taken orally, the duration of the course should not exceed 5 days.
Injection. V/m(deep), in minimally effective doses, selected in accordance with the intensity of pain and the patient's response. If necessary, opioid analgesics in reduced doses can be additionally prescribed at the same time.
Single doses with a single intramuscular injection:
Patients under 65 years old - 10-30 mg, depending on the severity of the pain syndrome;
Patients over 65 years of age or with impaired renal function - 10-15 mg.
Doses for repeated intramuscular administration:
Patients under 65 years old - 10-30 mg, then - 10-30 mg every 4-6 hours;
Patients over 65 years of age or with impaired renal function - 10-15 mg every 4-6 hours.
The maximum daily dose for intramuscular injection for patients under 65 years of age should not exceed 90 mg, and for patients over 65 years of age or with impaired renal function - 60 mg.
With parenteral administration, the duration of the course of treatment should not exceed 5 days.
When switching from parenteral administration of the drug to oral administration, the total daily dose of both dosage forms on the day of transfer should not exceed 90 mg for patients under 65 years of age and 60 mg for patients over 65 years of age or with impaired renal function. In this case, the dose of the drug in tablets on the day of the transition should not exceed 30 mg.
Overdose
Symptoms: abdominal pain, nausea, vomiting, occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis.
Treatment: gastric lavage, the introduction of adsorbents (activated carbon) and symptomatic therapy (maintenance of vital functions in the body). Not sufficiently excreted by dialysis.
special instructions
The effect on platelet aggregation stops after 24-48 hours.
Hypovolemia increases the risk of adverse reactions from the kidneys. If necessary, it can be prescribed in combination with narcotic analgesics.
Do not use simultaneously with paracetamol for more than 5 days. Patients with impaired blood coagulation are prescribed the drug only with constant monitoring of the number of platelets, which is especially important in the postoperative period, when careful monitoring of hemostasis is required.
Since a significant part of patients, when prescribing Ketanov ®, develop side effects from the central nervous system (drowsiness, dizziness, headache), it is recommended to avoid performing work that requires increased attention and quick reaction (driving vehicles, working with mechanisms, etc.).
Manufacturer
Ranbaxy Laboratories Limited, India
Terms of dispensing from pharmacies
On prescription.
Storage conditions of the drug Ketanov ®
At a temperature not higher than 25 °C.Keep out of the reach of children.
Shelf life of Ketanov ®
3 years.Do not use after the expiry date stated on the packaging.
Synonyms of nosological groups
| Category ICD-10 | Synonyms of diseases according to ICD-10 |
|---|---|
| M25.5 Joint pain | Arthralgia |
| Pain syndrome in osteoarthritis | |
| Pain in osteoarthritis | |
| Pain in the joints | |
| Joint pain | |
| Joint pain during heavy physical exertion | |
| Painful inflammation of the joints | |
| Painful conditions of the joints | |
| Painful traumatic lesions of the joints | |
| Pain in the shoulder joints | |
| Joint pain | |
| Joint pain | |
| Joint pain due to injury | |
| Musculoskeletal pain | |
| Pain in osteoarthritis | |
| Pain in joint pathology | |
| Pain in rheumatoid arthritis | |
| Pain in chronic degenerative bone disease | |
| Pain in chronic degenerative joint disease | |
| Osteoarticular pain | |
| Rheumatic pain | |
| Rheumatic pains | |
| joint pain | |
| Joint pain of rheumatic origin | |
| Articular pain syndrome | |
| Joint pain | |
| M54 Dorsalgia | Pain in the musculoskeletal system |
| Pain in the spine | |
| Back pain | |
| Back pain | |
| Pain in the spine | |
| Pain in various parts of the spine | |
| Backache | |
| Pain syndrome in the spine | |
| M54.1 Radiculopathy | Pain syndrome with radiculitis |
| Diseases of the spinal column | |
| Acute radicular radiculopathy | |
| Acute sciatica | |
| Subacute radiculitis | |
| Radiculitis | |
| Radiculitis | |
| Radiculitis with radicular syndrome | |
| radiculopathy | |
| Chronic radiculitis | |
| M79.0 Rheumatism, unspecified | degenerative rheumatic disease |
| Degenerative and rheumatic diseases of the tendons | |
| Degenerative rheumatic diseases | |
| Localized forms of soft tissue rheumatism | |
| Rheumatism | |
| Rheumatism with severe allergic component | |
| Articular and extra-articular rheumatism | |
| Rheumatic attack | |
| Rheumatic complaints | |
| Rheumatic diseases | |
| Rheumatic diseases of the intervertebral disc | |
| rheumatic disease | |
| Rheumatic disease of the spine | |
| Rheumatoid diseases | |
| Relapses of rheumatism | |
| Articular and extra-articular rheumatism | |
| Articular and muscular rheumatism | |
| Articular rheumatism | |
| Articular syndrome in rheumatism | |
| Chronic rheumatic pain | |
| Chronic articular rheumatism | |
| M79.1 Myalgia | Pain syndrome in musculoskeletal diseases |
| Pain syndrome in chronic inflammatory diseases of the musculoskeletal system | |
| Pain in the muscles | |
| Muscle soreness | |
| Muscle soreness during heavy physical exertion | |
| Painful conditions of the musculoskeletal system | |
| Pain in the musculoskeletal system | |
| Pain in the muscles | |
| Pain at rest | |
| Muscle pain | |
| Muscle pain | |
| Musculoskeletal pain | |
| Myalgia | |
| Myofascial pain syndromes | |
| muscle pain | |
| Muscle pain at rest | |
| Muscle pain | |
| Muscular pain of non-rheumatic origin | |
| Muscular pain of rheumatic origin | |
| Acute muscle pain | |
| Rheumatic pain | |
| Rheumatic pains | |
| Myofascial syndrome | |
| fibromyalgia | |
| M79.2 Neuralgia and neuritis, unspecified | |
| Brachialgia | |
| Occipital and intercostal neuralgia | |
| neuralgia | |
| Neuralgic pains | |
| Neuralgia | |
| Neuralgia of intercostal nerves | |
| Neuralgia of the posterior tibial nerve | |
| Neuritis | |
| Neuritis traumatic | |
| Neuritis | |
| Neurological pain syndromes | |
| Neurological contractures with spasms | |
| Acute neuritis | |
| Peripheral neuritis | |
| Post-traumatic neuralgia | |
| Chronic neuritis | |
| Essential neuralgia | |
| R52.0 Acute pain | Acute pain syndrome |
| Acute pain syndrome in osteoarthritis | |
| Acute pain syndrome of traumatic origin | |
| Severe neurological pain | |
| severe pain | |
| pain syndrome during childbirth | |
| R52.1 Persistent intractable pain | Pain syndrome in oncological practice |
| Pain syndrome expressed | |
| Pain syndrome in malignant neoplasms | |
| Pain syndrome in oncological diseases | |
| Pain syndrome in tumors | |
| Pain syndrome in cancer patients | |
| Pain in malignant neoplasms | |
| Pain in malignant tumors | |
| Pain in tumors | |
| Pain in cancer patients | |
| Pain with bone metastases | |
| Pain in cancer | |
| malignant pain syndrome | |
| Intense chronic pain | |
| intense pain syndrome | |
| Intense intractable pain syndrome | |
| Intense chronic pain syndrome | |
| Intractable pain | |
| Intractable pain | |
| tumor pain | |
| severe pain | |
| chronic pain | |
| chronic pain syndrome | |
| R52.2 Other persistent pain | Pain syndrome of non-rheumatic origin |
| Pain syndrome in vertebrogenic lesions | |
| Pain syndrome in neuralgia | |
| Pain syndrome in burns | |
| Pain is mild or moderate | |
| neuropathic pain | |
| neuropathic pain | |
| Perioperative pain | |
| Moderate to severe pain | |
| Moderate or mild pain syndrome | |
| Moderate to severe pain syndrome | |
| ear pain with otitis media | |
| R52.9 Pain, unspecified | Obstetric-gynecological pain |
| Pain syndrome | |
| Pain syndrome of inflammatory genesis | |
| Pain syndrome of non-oncological genesis | |
| Pain after injury | |
| Pain syndrome with inflammation of a non-rheumatic nature | |
| Pain syndrome in inflammatory lesions of the peripheral nervous system | |
| Pain in diabetic neuropathy | |
| Pain syndrome in acute inflammatory diseases of the musculoskeletal system | |
| Pain syndrome in tendon pathology | |
| Pain syndrome with spasms of smooth muscles | |
| Pain syndrome with spasms of smooth muscles (renal and biliary colic, intestinal spasm, dysmenorrhea) | |
| Pain syndrome with spasms of smooth muscles of internal organs | |
| Pain syndrome with spasms of smooth muscles of internal organs (renal and biliary colic, intestinal spasm, dysmenorrhea) | |
| Pain syndrome in trauma | |
| Pain syndrome in chronic inflammatory diseases of the musculoskeletal system | |
| Pain syndrome in duodenal ulcer | |
| Pain syndrome in gastric ulcer | |
| Pain syndrome in peptic ulcer of the stomach and duodenum | |
| Pain | |
| Pain during menstruation | |
| Pain syndromes | |
| Pain conditions | |
| Painful leg fatigue | |
| Sore gums when wearing dentures | |
| Pain in exit points of cranial nerves | |
| Painful irregular periods | |
| Painful dressings | |
| Painful muscle spasm | |
| Painful tooth growth | |
| pain | |
| Pain in the lower limbs | |
| Pain in the body | |
| Pain after cholecystectomy | |
| Pain with the flu | |
| Pain in diabetic polyneuropathy | |
| Pain with burns | |
| Pain during sexual intercourse | |
| Pain in colds | |
| Pain in sinusitis | |
| Pain in trauma | |
| Shooting pains | |
| Pain of a traumatic nature | |
| Pain | |
| Postoperative pain | |
| Post-traumatic pain | |
| Pain when swallowing | |
| Pain in infectious and inflammatory diseases of the upper respiratory tract | |
| Burn pain | |
| Pain due to traumatic muscle injury | |
| Pain from injury | |
| Pain during tooth extraction | |
| Pain of traumatic origin | |
| Pain due to spasm of smooth muscles | |
| Severe pain syndrome | |
| Severe pain syndrome of traumatic origin | |
| Non-malignant pain syndrome | |
| Polyarthralgia in polymyositis | |
| postoperative pain | |
| Postoperative pain | |
| Postoperative pain | |
| Post-traumatic pain | |
| post-traumatic pain syndrome | |
| Torpid pain syndrome | |
| Traumatic pain | |
| Traumatic pain | |
| moderate pain | |
| Moderate pain syndrome | |
| moderate pain syndrome | |
| T88.9 Complication of surgery and medical intervention, unspecified | Pain syndrome in the postoperative period |
| Pain syndrome in the postoperative period after orthopedic surgery | |
| Pain after diagnostic procedures | |
| Pain syndrome after diagnostic interventions | |
| Pain after surgery | |
| Pain after surgery | |
| Pain after orthopedic surgery | |
| Pain after removal of hemorrhoids | |
| Pain syndrome after surgery | |
| Pain syndrome when using an excimer laser | |
| Pain in trauma and after surgery | |
| Pain syndromes in dental practice | |
| Painful diagnostic interventions | |
| Painful diagnostic procedures | |
| Painful instrumental diagnostic procedures | |
| Painful instrumental manipulations | |
| Painful healing procedures | |
| Painful manipulation | |
| Painful dressings | |
| Painful therapeutic interventions | |
| Painful surgical procedures | |
| Pain in the area of the surgical wound | |
| Pain in the postoperative period | |
| Pain after diagnostic interventions | |
| Pain after orthopedic surgery | |
| Pain after surgery | |
| Pain during diagnostic procedures | |
| Pain during therapeutic procedures | |
| pain in orthopedics | |
| Pain in the postoperative period | |
| Pain after diagnostic interventions | |
| Pain after sclerotherapy | |
| Pain after dental procedures | |
| Pain after surgery | |
| Postoperative pain | |
| Pain postoperative and post-traumatic | |
| Pain during tooth extraction | |
| Inflammation after surgery and trauma | |
| Inflammation after orthopedic surgery | |
| Inflammatory processes after surgical interventions | |
| Inflammatory syndrome after surgery | |
| Festering postoperative fistulas | |
| Operating wound | |
| Complications after tooth extraction | |
| postoperative pain | |
| Postoperative pain | |
| Postoperative pain syndrome | |
| Postoperative pain |
average rating
Based on reviews
Ketanov - a drug that is widely used as a powerful pain reliever for pain of various origins.
To a lesser extent, it has anti-inflammatory and some antipyretic properties.
Manufacturer and cost
Ketanov is produced:
- in the form of coated tablets; 1 tablet - 10 mg of the active substance ketorolac; the cost of 20 tablets is 50 - 60 rubles;
- in the form of ampoules with a solution for injection; 1 ml contains 30 mg of ketorolac; a package of 10 ampoules costs from 100 to 120 rubles.
The manufacturer of the drug is the Indian pharmaceutical company Ranbaxi Laboratories Limited.
Ask your question to a neurologist for free
Irina Martynova. Graduated from the Voronezh State Medical University. N.N. Burdenko. Clinical intern and neurologist of BUZ VO \"Moscow Polyclinic\".
How does the medicine work?
Ketanov is NSAID medication- non-steroidal anti-inflammatory drugs. All drugs in this series have analgesic, anti-inflammatory and antipyretic properties. But in different drugs, individual properties manifest themselves in different ways. Ketanov has the strongest analgesic properties, the rest of the properties characteristic of NSAIDs are slightly expressed in him.
Ketanov inhibits the action of the enzyme cyclooxygenase (COX), which is involved in the formation of prostaglandins that support inflammation and pain. There are 2 forms of COX: COX-1 and COX-2. The first form stimulates the secretion of mucus in the digestive organs (it protects the walls of organs from various influences) and inhibits the formation of blood clots. The second form is involved in the development of inflammation.
NSAIDs that inhibit only COX-2 () are called selective, they have almost no side effects when used correctly. Ketanov suppresses both types of COX, therefore it has a pronounced side effect. But its analgesic properties exceed those of all other drugs in this series and can be comparable to the properties of opiates.
Regardless of the route of entry of the drug into the body (orally or as an injection), the effect of the drug occurs after 40-50 minutes, its duration reaches 4-6 hours. Most of the drug is excreted unchanged from the body through the kidneys. But part of it decomposes in the liver cells, and then excreted in the bile and feces.
Ketanov can be bought at a pharmacy only with a doctor's prescription.
Indications for use
Ketanov - what does this drug help with and to whom is it prescribed? Indications for the appointment of Ketanov can only be intense pain. Assign the drug once or in short courses:
- after any injuries and surgical interventions accompanied by pain;
- in dental practice to relieve and prevent pain, including during painful manipulations;
- with exacerbation of chronic diseases of the musculoskeletal system (arthrosis, arthritis), occurring with severe pain;
- with painful neuralgia of peripheral nerves;
- for pain in cancer patients;
- with stones in the urinary and biliary systems, accompanied by painful colic;
- with renal and hepatic colic in combination with antispasmodics (for example, with).
Dosages and regimens
Dosages of Ketanov depend on the severity of pain and the presence or absence of comorbidities in the patient. Instructions for use, developed by the manufacturers of the drug, clearly stipulate all possible options for prescribing the drug.
Ketanov tablets are prescribed as a single dose of 10 mg (1 tablet). If this is not enough, the drug is prescribed in the same dose 4 times a day for 3-5 days in a row.
Injections are given intramuscularly in the following doses:
- single injection - 10-30 mg as an intramuscular injection;
- for the elderly and patients with chronic renal failure, the dosage is reduced to 10-15 mg; if necessary, injections are given every 4 to 6 hours;
- if a course of treatment is carried out, Ketanov is prescribed intramuscularly according to the same scheme;
- the course of treatment should not exceed 2 days.
Side effects of the drug
For Ketanov, they can be as follows:
- indigestion, stomach pain, nausea, vomiting, diarrhea, flatulence; stomatitis and gastritis may develop;
- toxic effects on the liver with changes in biochemical parameters;
- holding or stopping breathing;
- suppression of the formation of blood clots - the possibility of bleeding;
- bradycardia (rare pulse), accompanied by bouts of strong heartbeat, changes in blood pressure, loss of consciousness;
- headaches, coordination disorders, mood and sleep changes, sensitivity disorders;
- insufficient or excess volume of daily urine, the appearance of pathological changes in the urine (protein and blood), impaired renal function;
- allergic reactions of immediate (urticaria, angioedema, anaphylactic shock) and delayed (severe damage to the integument 24-48 hours after taking Ketanov) type;
- sweating, swelling, fever, soreness at the injection site.
Overdose accompanied by a number of unpleasant symptoms: pain in the upper abdomen, nausea, vomiting (including bloody with internal bleeding), cyanosis of the fingertips and nasolabial triangle. A significant overdose can cause severe kidney damage.
An overdose requires seeking medical attention. As a first aid, the stomach should be washed with water with the addition of adsorbents (20 powdered tablets of activated charcoal per liter of water).
The ambulance doctor, after assessing the condition of the victim, will treat him symptomatically and, if necessary, hospitalize him.
Who is not assigned?
The drug can not be used for:
- stomach ulcer and erosive gastritis;
- hemorrhagic (associated with cerebral hemorrhage) strokes;
- low rates of blood clotting;
- severe diseases of the liver and kidneys with impaired function;
- dehydration of the body;
- bronchospasm from aspirin and NSAIDs;
- hypersensitivity to Ketanov;
- pregnancy, during childbirth and breastfeeding;
- children and adolescents up to 16 years of age.
According to special schemes with a reduced dosage, Ketanov is prescribed to the elderly, patients with chronic disorders of the liver and kidneys, as well as patients with arterial hypertension.
If Ketanov's reception is accompanied by dizziness and fainting, then it is necessary to stop driving during the treatment.
Interaction with other drugs
The use of Ketanov Can be combined with opioid analgesics- this allows you to reduce their dosage, providing high-quality pain relief. The use of Ketanov should not be combined with the following medicines:
- with other drugs from the same series of NSAIDs - this increases the risk of side effects;
- with vasodilators (for example, Pentoxifylline) and anticoagulants (for example, Heparin) - the possibility of bleeding increases;
- with antihypertensive (lowering blood pressure) drugs of a number of ACE inhibitors (Enam, Enap, etc.) - the threat of severe kidney damage;
- with lithium preparations - leads to a delay in the excretion of the latter and its overdose;
- with Furosemide - the diuretic properties of this drug may decrease.
Is it possible to combine treatment with alcohol?
Drinking alcohol during treatment can cause:
- stop breathing;
- gastric ulcer, accompanied by bleeding;
- toxic hepatitis with impaired liver function.
What to replace?
You can choose a synonym or analogue of Ketanov. Synonyms have the same active substance as Ketanov - ketorolac:
- Ketorol - 10 mg tablets (20 tablets cost 40 - 45 rubles), 3% solution in ampoules (10 ampoules - 150 rubles) and 2% gel (ointment - 200 rubles);
- Ketorolac - tablets of 10 mg (20 pieces cost about 30 rubles) and ampoules with a solution for injection (10 ampoules of 30 mg cost 70-80 rubles).
Synonyms of Ketanov are also produced under the names: Adolor, Ketalgin, Ketofril, Ketrodol, Torolak, etc.
Ketanov's analogues are drugs with a different active ingredient, but having the same therapeutic effect. These are drugs from a series with predominant analgesic properties. There is a correspondence between Ketanov and the following remedies:
- (trade name Ksefokam);
- ( , Naklofen);
Moderate and high pain intensity require the appointment of drugs of general (systemic) action - tablets or injections (all drugs are administered strictly intramuscularly).
How do they respond to the drug?
Patients and specialists speak about this drug mostly positively. Its analgesic properties are unrivaled. But many patients note the appearance of significant side effects, especially from the gastrointestinal tract. Sometimes they appear even after a single use of the drug.FAQ
- which is better - Ketanov or? It depends on what the medicine is used for: Ketanov has pronounced analgesic properties, while Diclofenac has analgesic properties combined with anti-inflammatory and antipyretic;
- will it help? It will help, but it makes sense to use it for severe pain such as migraine;
- Do Ketanov injections relieve exacerbation or only relieve pain? Ketanov relieves pain and partially inflammation; for the full treatment of exacerbation, complex therapy is necessary;
- how long does Ketanov last? The time of action of tablets and injections of the drug is 4 to 6 hours.
Ketanov is the strongest pain reliever that has a pronounced side effect.
Only a specialist can prescribe this drug without adverse health effects.
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In this article, you can read the instructions for using the drug Ketanov. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Ketanov in their practice are presented. We kindly ask you to actively add your reviews about the drug: the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Analogues of Ketanov in the presence of existing structural analogues. Use for the treatment of pain (headache, toothache, during menstruation) in adults, children, as well as during pregnancy and lactation. The mechanism of the analgesic effect.
Ketanov- non-steroidal anti-inflammatory drug, a derivative of pyrrolysine-carboxylic acid. It has a pronounced analgesic effect, also has an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX - the main enzyme of the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The active substance of the drug is Ketorolac.
Pharmacokinetics
When taken orally, it is absorbed from the gastrointestinal tract. Eating does not affect absorption. More than 90% of the dose is excreted in the urine, unchanged - 60%; the rest is through the intestines.
Indications
- for short-term relief of moderate and severe pain of various origins.
Release forms
Film-coated tablets 10 mg.
Solution for intramuscular injection (injections in ampoules for injection) 30 mg / ml.
Other forms of the drug (whether suppositories or suspension) are either fakes of the original drug, or other forms and trade names of the active substance Ketorolac.
Instructions for use and dosing regimen
Adults when taken orally - 10 mg every 4-6 hours, if necessary - 20 mg 3-4 times a day.
With intramuscular injection, a single dose is 10-30 mg, the interval between injections is 4-6 hours. The maximum duration of use is 2 times a day.
Maximum doses: when taken orally or intramuscularly - 90 mg per day; for patients weighing up to 50 kg, with impaired renal function, as well as for persons over 65 years of age - 60 mg per day.
Side effect
- bradycardia;
- changes in blood pressure;
- heartbeat;
- fainting;
- nausea;
- stomach ache;
- diarrhea;
- constipation;
- flatulence;
- feeling of fullness in the gastrointestinal tract;
- vomit;
- dry mouth;
- thirst;
- stomatitis;
- gastritis;
- erosive and ulcerative lesions of the gastrointestinal tract;
- anxiety;
- headache;
- drowsiness;
- depression;
- euphoria;
- sleep disorders;
- dizziness;
- change in taste sensations;
- asthma attacks;
- increased urination;
- nosebleeds;
- anemia, eosinophilia, thrombocytopenia;
- increased sweating;
- swelling;
- hypokalemia, hyponatremia;
- skin itching;
- hemorrhagic rash;
- exfoliative dermatitis;
- hives;
- Lyell's syndrome;
- Stevens-Johnson syndrome;
- anaphylactic shock;
- bronchospasm;
- angioedema;
- fever;
- pain at the injection site.
Contraindications
- erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;
- the presence or suspicion of gastrointestinal bleeding and / or craniocerebral hemorrhage;
- a history of blood clotting disorders;
- conditions with a high risk of bleeding or incomplete hemostasis;
- hemorrhagic diathesis;
- moderate and severe renal dysfunction (serum creatinine more than 50 mg/l);
- the risk of developing renal failure with hypovolemia and dehydration;
- "aspirin triad";
- bronchial asthma;
- polyps of the nasal cavity;
- angioedema in history;
- prophylactic anesthesia before and during surgery;
- children and adolescents up to 16 years of age;
- pregnancy;
- childbirth;
- lactation;
- hypersensitivity to ketorolac, acetylsalicylic acid and other NSAIDs.
Use during pregnancy and lactation
Contraindicated during pregnancy, during childbirth and during lactation (breastfeeding).
Ketanov is contraindicated for use as a means for premedication, maintenance anesthesia and for pain relief in obstetric practice, since under its influence it is possible to increase the duration of the first stage of labor. In addition, ketorolac can inhibit uterine contractility and fetal circulation.
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 bleeding from the gastrointestinal tract in history.
Ketanov 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 senile patients, tk. the half-life of ketorolac is prolonged, and plasma clearance may decrease. 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, eosinophilia appear, ketorolac should be discontinued. Ketorolac is not indicated for use in chronic pain.
Influence on the ability to drive vehicles and control mechanisms
If drowsiness, dizziness, insomnia or depression appear during the period of treatment with Ketorolac, special care must be taken during potentially hazardous activities that require increased attention and speed of psychomotor reactions.
When taken simultaneously with ethanol (alcohol), it can cause bleeding from the gastrointestinal tract.
drug interaction
With the simultaneous use of Ketanov with other NSAIDs, additive side effects may develop; with pentoxifylline, anticoagulants (including heparin in low doses) - an increase in the risk of bleeding is possible; with ACE inhibitors - an increase in the risk of developing impaired renal function is possible; with probenecid - the concentration of ketorolac in plasma and its half-life increase; with lithium preparations - it is possible to reduce the renal clearance of lithium and increase its concentration in plasma; with furosemide - a decrease in its diuretic effect.
With the use of ketorolac, the need for the use of opioid analgesics for the purpose of pain relief is reduced.
Analogues of the drug Ketanov
Structural analogues for the active substance:
- Adolor;
- Acular;
- Dolac;
- Dolomin;
- Ketalgin;
- Ketolac;
- Ketorol;
- Ketorolac;
- Ketorolac Rompharm;
- Ketorolac-OBL;
- Ketorolac-Eskom;
- Ketorolac tromethamine;
- Ketofril;
- Toradol;
- Torolac.
In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.