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What does Ketorol help with and how long does it last? Instructions for the use of Ketorol in ampoules Ketorol highest single dose.

Compound

Each ampoule contains ketorolac tromethamine 30 mg, as well as excipients: ethyl alcohol 95% 0.125 ml, sodium chloride 4.35 mg, disodium EDTA 1.0 mg, octoxynol 0.07 mg, sodium hydroxide 0.725 mg, propylene glycol 400 mg, water for injection up to 1 ml

Pharmacotherapeutic group

Nonsteroidal anti-inflammatory and antirheumatic drugs. ATX code: M01 AB15.

Description

Transparent, colorless or pale yellow liquid, in yellow ampoules, volume 1 ml, USP 1 type.

Pharmacological properties

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 of [-]S and [-]P enantiomers, and the analgesic effect is due to the [-]S form. 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: the bioavailability of ketorolac after oral administration ranges from 80% to 100%. Maximum plasma concentration is achieved within 30-60 minutes. The pharmacokinetics of ketorolac under conditions of mid-therapeutic doses is a linear function. The equilibrium concentration of the drug in plasma is 50% higher than that determined after a single dose. More than 99% of the drug is bound to plasma proteins, resulting in an apparent volume of distribution of less than 0.3 l/kg.

Ketorolac is metabolized primarily to form conjugated forms of glucuronic acid, which are excreted through the kidneys. Metabolites do not have analgesic activity. The half-life of the drug averages 5 hours.

Indications for use

Short-term relief of moderate and severe acute pain in the postoperative period. Treatment should be started only in a hospital setting, the maximum duration of treatment is 2 days.

Directions for use and doses

Ketorol is intended for intramuscular injection; the drug should not be used for epidural or spinal administration. The solution is injected slowly intramuscularly (deep into the muscle). The onset of the analgesic effect is about 30 minutes with its maximum severity within 1-2 hours, the average duration of analgesia is 4-6 hours.

Administration of the drug several times a day for more than 2 days is not recommended, since in most cases patients do not require longer-term analgesic therapy, or can be switched to oral ketorolac. In this case, the duration of use of ketorolac parenterally and orally should not exceed 5 days in total.

To achieve maximum analgesic effect in the early postoperative period, it is possible to use ketorolac and narcotic analgesics together; the daily dose of the latter in this case is reduced. Ketorolac does not affect addiction to opioids and does not increase associated respiratory depression or sedation.

Dose selection and adjustment should be made in accordance with the intensity of pain and response to the drug. To minimize side effects, it is recommended to use the minimum effective dose for the shortest possible course of treatment.

Adults; The usually recommended initial dose of Ketorol is 10 mg, followed by 10-30 mg every 4-6 hours. In the early postoperative period, it is permissible to administer the drug every 2 hours, if necessary. The maximum daily dose is 90 mg/day. in patients weighing less than 50 kg - no more than 60 mg/day.

Elderly patients (over 65): It is recommended to use the drug in the lowest effective dose, the total dose should not exceed 60 mg/day. Due to the higher risk of side effects in this group of patients, the minimum possible duration of treatment and regular monitoring of the patient’s condition to exclude gastrointestinal bleeding are recommended. Children: The safety and effectiveness of ketorolac in children have not been confirmed; the drug is not recommended for use in children under 16 years of age.

Patients with impaired renal function: the use of ketorolac is contraindicated in patients with severe and moderate renal impairment. In case of mild renal dysfunction, it is permissible to use Ketorol in a dose of no more than 60 mg/day.

If it is necessary to combine parenteral and oral administration of Ketorol, the total daily dose should not exceed 90 mg (60 mg in persons over 65 years of age, with a body weight of less than 50 kg or impaired renal function), while the dose of the drug taken orally should not exceed 40 mg/ days It is recommended to quickly transfer the patient only to the oral form of the drug.

Side effect

From the gastrointestinal tract: anorexia, feeling of abdominal discomfort, feeling of fullness of the stomach, nausea, dyspepsia, gastrointestinal pain, epigastric pain, diarrhea, flatulence, belching, vomiting, constipation, erosive and ulcerative changes, bleeding and perforation of the gastrointestinal tract (sometimes fatal) , vomiting blood, blood in the stool, gastritis, peptic ulcer, pancreatitis, ulcerative stomatitis, esophargitis, exacerbation of Crohn's disease and colitis.

From the liver and biliary tract: liver dysfunction, liver failure, jaundice, hepatitis, hepatomegaly, increased activity of liver transaminases.

From the nervous system: headache, dizziness, fainting, increased fatigue, weakness, irritability, dry mouth, increased thirst, mood changes, anxiety, impaired concentration, euphoria, nervousness, confusion, paresthesia, unusual dreams, depression, drowsiness, disturbance sleep, insomnia, hallucinations, agitation, hyperkinesia, convulsions, pathological thoughts, aseptic meningitis, stiff neck, anxiety, vertigo, disorientation, thinking disorder.

From the senses: disturbance of taste, blurred vision, optic neuritis, tinnitus, decreased and loss of hearing.

From the musculoskeletal system: myalgia.

From the outsideurinarysystems: pain at the site of the kidney projection, dysuria, frequent urination, oliguria, hematuria, proteinuria, increased levels of urea and creatinine in the blood serum, hyponatremia, hyperkalemia, urinary retention, renal failure, interstitial nephritis, papillary necrosis, nephrotic syndrome, hemolytic uremic syndrome.

From the cardiovascular system: pallor, hyperemia, chest pain, palpitations, bradycardia, heart failure, arterial hypertension, edema. Data from clinical and epidemiological studies suggest 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 outside blood: purpura, leukopenia, eosinophilia, neutropenia, agranulocytosis, aplastic anemia, hemolytic anemia, thrombocytopenia, a possible decrease in the rate of blood clotting, the occurrence of hemorrhages under the skin, hematomas, nosebleeds, prolongation of bleeding time, increased bleeding of postoperative wounds.

From the respiratory system: shortness of breath, tachypnea, bronchospasm, complication of asthma, pulmonary edema.

From the reproductive system: infertility (in women).

From the skin: itching, urticaria, photosensitivity, Lyell's syndrome, exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome, skin rashes, including maculopapular and weeping, changes in facial skin color.

Allergic reactions: anaphylactic and anaphylactoid reactions, urticaria, bronchospasm, laryngeal edema, angioedema, eyelid edema, periorbital edema, exfoliative dermatitis, bullous dermatosis.

From the body as a whole: general malaise, swelling, fever, increased sweating, weight gain; pain, swelling and hyperemia at the injection site. 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, concomitant diseases, liver function, kidney function, state of water-electrolyte metabolism and hemostatic system), as well as possible drug interactions with combination therapy.

Contraindications

Bronchial asthma, complete or partial syndrome of nasal polyps, bronchospasm, history of angioedema. Peptic ulcer of the stomach and duodenum during the period of exacerbation, as well as a history of ulcers or gastrointestinal bleeding, the presence or suspicion of gastrointestinal bleeding. History of blood coagulation disorders, conditions with a high risk of bleeding, hemorrhagic diathesis, coagulopathies, hemorrhagic stroke, intracranial bleeding, simultaneous use with anticoagulants (including warfarin, low doses of heparin). Surgical interventions with a high risk of bleeding or the risk of incomplete stopping of bleeding. Moderate and severe renal failure (plasma creatinine more than 50 mg/l), risk of renal failure, hypovolemia, dehydration. Pregnancy, childbirth and breastfeeding. Hypersensitivity to ketorolac, aspirin, other NSAIDs or any component of the drug. Concomitant use of other NSAIDs (risk of additive side effects) Age under 16 years Congestive heart failure The drug is not used for pain relief before and during surgery. Ketorolac is not used for epidural and intrathecal injections. Severe liver failure. Combined use with lithium preparations, pentoxifylline probenecid. Epidural or intrathecal administration of the drug is contraindicated.

Features of application

Prescription for patients with impaired function liver: prescribed with caution. While taking ketorolac, liver enzyme levels may increase. If there are functional abnormalities in the liver while taking ketorolac, a more severe pathology may develop. If signs of liver pathology are detected, treatment should be stopped.

Patients with renal failure or a history of kidney disease: ketorolac is prescribed with caution.

Purpose elderly patients: Since patients in this age group are more likely to develop adverse reactions, the minimum effective dose should be used (daily therapeutic dose of no more than 60 mg for patients over 65 years of age).

Pregnancy and lactation

Efficacy and safety have not been established. Drugs that affect the synthesis of prostaglandins, including ketorolac, can cause a decrease in fertility, and therefore are not recommended for use by women planning pregnancy. The safety of the drug in pregnant women has not been studied. A study on rats and rabbits at toxic doses did not reveal a teratogenic effect. In rats, prolongation of gestational age and delayed birth were noted. Due to the known negative effect of NSAID drugs on the cardiovascular system of the fetus (risk of occlusion of the ductus arteriosus), ketorolac is contraindicated in pregnant women. The use of ketorolac during labor is not recommended due to the increased risk of bleeding in mother and child. Ketorolac penetrates into milk, and therefore is not recommended for use during lactation.

Impact on laboratory test indicators: it is possible to increase bleeding time when studying coagulation parameters.

Impact on ability to driveand other mechanisms

Since a significant proportion of patients who are prescribed ketorolac 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.

Warnings and Precautions

Ketorolac can cause severe adverse reactions from the digestive tract at any stage of drug therapy after or without warning symptoms; such adverse reactions can be fatal. The risk of serious gastrointestinal bleeding is dose-related, but side effects can occur even with short-term therapy. In addition to a history of peptic ulcer disease, provoking factors are the simultaneous use of oral corticosteroids, anticoagulants, long-term therapy with non-steroidal anti-inflammatory drugs, smoking, drinking alcoholic beverages, and old age. If you suspect the development of adverse reactions from the gastrointestinal tract, ketorolac should be discontinued.

NSAIDs should be used with caution in patients with a history of Crohn's disease and ulcerative colitis due to the possibility of worsening the course of the disease.

Ketorolac inhibits platelet aggregation and prolongs bleeding time; platelet function returns to normal within 24-48 hours after discontinuation of the drug. In patients receiving anticoagulant therapy, the use of ketorolac may increase the risk of bleeding. Patients already taking anticoagulants or requiring low-dose heparin should not receive ketorolac. In patients taking other drugs that affect hemostasis, ketorolac should be used with caution. In patients who have undergone surgery with a high risk of bleeding or incomplete hemostasis, ketorolac should not be used.

Like other NSAIDs, ketorolac inhibits prostaglandin synthesis and may cause kidney toxicity and should therefore be used with caution in patients with impaired renal function or a history of kidney disease. Risk groups include patients with impaired renal function, hypovolemia, heart failure, impaired liver function, patients using diuretics, and elderly patients.

Fluid retention, sodium chloride retention, hypertension, oliguria and peripheral edema have been observed in some patients taking NSAIDs, including ketorolac, so it should be used with caution in patients with hypertension, heart failure, and fluid and electrolyte imbalances should be corrected before administering the drug.

Clinical studies and epidemiological data suggest that the use of some NSAIDs, especially in high doses and for long periods of time, may be associated with an increased risk of arterial thrombotic complications such as myocardial infarction or stroke. Such a risk cannot be excluded for ketorolac. To minimize the potential risk of adverse cardiovascular complications in patients using NSAIDs, the lowest effective dose should be used for the shortest possible period of time. Ketorolac should be prescribed to patients with uncontrolled hypertension, congestive heart failure, established coronary artery disease, peripheral arterial and/or cerebrovascular disease only after a thorough assessment of all the advantages and disadvantages of such treatment.

Ketorolac should be administered with caution to patients with impaired liver function or a history of liver disease. Significant increases (more than three times normal) in serum ALT and AST were observed in less than 1% of patients in controlled clinical studies. In addition, isolated cases of severe hepatic reactions have been reported, including jaundice, fulminant hepatitis, liver necrosis and liver failure, in some cases leading to death. If signs of liver dysfunction appear, ketorolac should be discontinued.

Use of the drug in patients with systemic lupus erythematosus or connective tissue diseases may be associated with an increased risk of developing aseptic meningitis.

There have been reports of serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. The highest risk of these reactions exists at the beginning of treatment.

Serious anaphylactic and anaphylactoid reactions, such as bronchospasm, laryngeal edema, angioedema, and anaphylactic shock, have been reported. Ketorolac should not be used in patients with a history of bronchial asthma, nasal polyp syndrome, bronchospasm, or angioedema. If a rash or other manifestations of hypersensitivity appear, treatment with the drug should be discontinued.

This medicine contains a small amount of ethanol (ethyl alcohol), i.e. less than 100 mg in 1 ml the sodium content of the medicinal product is less than 1 mmol (23 mg) in 1 ml.

Interaction with other drugs

Ketorolac slightly reduces the degree of protein binding of warfarin.

In research in vitro the effect of therapeutic doses of salicylates on the degree of binding of ketorolac to plasma proteins is shown, downward from 99.2% to 97.5%. When combined with furosemide, its diuretic effect may be weakened by approximately 20%.

Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increasing its plasma concentration and increasing its half-life. With the use of ketorolac, the clearance of methotrexate and lithium may decrease and the toxicity of these substances may increase.

A possible interaction between ketorolac and non-depolarizing muscle relaxants has been noted, leading to the development of apnea.

It is possible that simultaneous use with ACE inhibitors may increase the risk of renal dysfunction.

Rare cases of the development of convulsive attacks have been described when ketorolac is combined with anticonvulsants (phenytoin, carbamazepine).

Hallucinations may occur while taking ketorolac and psychostimulant drugs (fluoxetine, thiothixene, alprazolam).

Concomitant use of ketorolac and NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided due to an increased risk of serious adverse reactions. Ketorolac inhibits platelet aggregation, reduces thromboxane concentrations and prolongs bleeding time. Platelet function returns to normal within 24-48 hours after stopping ketorolac. Although studies do not indicate a significant interaction between ketorolac and anticoagulants, concomitant use of ketorolac and therapeutic doses of warfarin, prophylactic doses of heparin (2500-5000 units over 12 hours) and dextrans may be associated with an increased risk of bleeding.

NSAIDs should not be used for 8 to 12 days after mifepristone administration due to the possible decreased effect of mifepristone.

Concomitant use of ketorolac with pentoxifylline increases the risk of bleeding.

As with other NSAIDs, caution should be used when coadministered with corticosteroids due to the increased risk of GI ulceration or bleeding.

Ketorolac has been shown to reduce the need for opioid analgesics when they are used to relieve postoperative pain.

Patients taking quinolines concomitantly may be at increased risk of seizures.

Concomitant use of NSAIDs with zidovudine leads to an increased risk of hematological toxicity.

There is an increased risk of nephrotoxicity when NSAIDs are used concomitantly with tacrolimus or cyclosporine.

NSAIDs may worsen heart failure, reduce glomerular filtration rate, and increase plasma levels of cardiac glycosides when used together.

Incompatibility

Ketorolac injection solution should not be mixed in small containers (for example, in the same syringe) with morphine sulfate, meperidine hydrochloride, promethazine hydrochloride or hydroxyzine hydrochloride, as ketorolac may precipitate.

Overdose

An overdose of ketorolac with a single or repeated use is usually manifested by pain in the abdomen, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, hyperventilation, metabolic acidosis, these symptoms are cured after stopping the drug. In these cases, gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy are recommended. Ketorolac is not sufficiently eliminated by dialysis.

Manufactured

Dr. Reddy's Laboratories Ltd.

Village Khol, Nalagarh Road, Baddi, Solan District, Himachal Pradesh, 173205, India.

In this article you can read the instructions for use of the drug Ketorol. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Ketorol in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Ketorol in the presence of existing structural analogues. Use for the treatment of dental, headache and other types of pain, during menstruation in adults, children, as well as during pregnancy and lactation.

What kind of medicine is this

Ketorol is a drug most often used for pain relief in cases of severe pain arising for various reasons. It is used quite widely and for various pathologies.

Drug group

International nonproprietary name or INN: Ketorolac

Trade name: Ketorol

Latin name: Ketorolacum

Compound

Active ingredient: ketorolac trometamol - 0.03 g.

Additional substances: octoxynol - 0.00007 g.

Trilon B - 0.001 g.

sodium chloride - 0.00435 g.

ethanol - 0.115 ml.

propane-1,2-diol - 0.4 g.

caustic soda - 0.000725 g.

water for injection - the volume required to increase the contents of the ampoule to 1 ml.

Mechanism of action and properties

Characteristic

Non-steroidal anti-inflammatory drug or NSAID. Ketorolac in structure consists of two isoforms: S(−) and R(+), can be found in three microcrystalline variants, which have good solubility in water. The dissociation constant of Ketorolac acid is 3.5. Molecule mass: 376.41.

Pharmacodynamics (pharmacology)

Ketorol is an NSAID, acting on the body to suppress pain, inhibit inflammation, and also moderately reduce body temperature.

Mechanism of action

5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid non-selectively counteracts the activity of cyclooxygenase-1 and cyclooxygenase-2, which are catalysts for the synthesis of prostaglandins from arachidonic acid.

Prostaglandins are of great importance in the formation of pain, inflammatory reactions and an excessive increase in the patient’s body temperature.

Ketorol is a mixture of almost identical isomers S(-) and R(+), differing only in their mirror arrangement. It is the S form that causes the analgesic effect.

Ketorol, compared to morphine, shows the same strong analgesic effect, much greater than other NSAIDs.

Pharmacokinetics

The effectiveness of the drug and the speed of its action depend on the method of delivery of the active substance to the body.

When a solution of the drug is administered intramuscularly or into a vein, the effect occurs within 30 minutes and reaches its maximum after 60-120 minutes. Duration of action is from 4 to 6 hours. When administered enterally, the effect begins within 60 minutes, and the maximum effect occurs only after 120-180 minutes.

The bioavailability of the drug is rapid and fully manifested. When the contents of one ampoule are introduced into the muscle (1 ampoule - 30 mg), the highest concentration is from 0.00000174 to 0.0000031 g/ml, when two ampoules are administered - from 0.00000323 to 0.00000577 g/ml.

The time to reach the highest concentration is from 15 to 73 for 30 mg and from 30 to 60 minutes for 60 mg.

The share of interaction with blood plasma proteins is 99%.

The drug may pass into breast milk. 2 hours after administration, the concentration of the drug in milk becomes maximum (7.3 ng/ml).

About half the dose of the drug is converted in the liver into chemically inactive compounds: tetrahydroxy-2-oxanoic acids, which are eliminated by the kidneys, and p-hydroxyketorolac. Excreted by the kidneys (about 91%) and through the gastrointestinal tract (6%).

The half-life of Ketorol depends on the age of the patient: in the elderly it increases, in the young it decreases accordingly. In patients with renal pathologies, the half-life can range from 10 to 13 hours.

Hemodialysis does not affect the metabolism of the drug. The drug may affect the kidneys and liver.

Indications

What does it cure, what is it for and what is the benefit of it? The main use of the drug is pain relief, but it also helps reduce temperature and reduce the intensity of inflammation.

Why is Ketorol prescribed? Typically for symptomatic therapy.

Solutions are injected for severe and moderate pain:

  • For injuries.
  • During dental interventions.
  • For tumors.
  • To relieve pain after surgery.
  • For pain in muscles and joints.
  • With damage to peripheral nerves.
  • For autoimmune diseases, for radiculopathy.

Drops are used for inflammation of the mucous membrane of the eye and after eye surgery.

The gel is used topically for injuries:

  • For bruises.
  • Sprains.
  • For tendon inflammation.
  • Inflammation of the synovial membranes.
  • In inflammatory processes in the joint capsules.
  • For pain in muscles and joints.
  • When nerves remote from the center are affected.
  • For autoimmune diseases.
  • For radiculopathy.

Tablets are used at the same time as solutions.

Release forms

The drug is produced in the form of four dosage forms: a solution for infusions and injections (intramuscular or intravenous) in a 1 ml ampoule, in the form of tablets with a film coating on the outside, in the form of a gel for external use and in the form of eye drops.

What is better solution or tablets? Tablets are easier to use, but the solution is faster and more effective. The gel is used only externally, for example, for soft tissue bruises.

Instructions for use

When administered parenterally to patients from 16 to 64 years of age with a body weight of more than 50 kg, more than 60 mg cannot be injected into the muscle at a time (the dose of the drug taken orally must also be taken into account). Most often, 30 mg every 6 hours. 30 mg is administered intravenously, no more than 6 doses in 28 hours.

If the patient weighs less than 50 kg or has renal pathology, then no more than 30 mg is injected into the muscle at a time, usually 15 mg (no more than 8 times in 48 hours), and no more than 15 mg (less than 8 times) into the vein.

The maximum dose administered per day for patients from 16 to 64 years old and weighing more than 50 kg is 0.09 g (90 mg), for others - 0.06 g (60 mg). Duration of use - up to two days.

The drug must be injected into a vein or muscle slowly. The effect begins after 0.5 hours.

The gel must be spread in a thin layer over the disturbing surface.

The tablets must be taken with a sufficient amount of water.

Side effect

  • Gastrointestinal dysfunction: diarrhea, nausea, vomiting, constipation, abdominal pain, peptic ulcer of the stomach or duodenum, bleeding in the stomach cavity, inflammatory diseases of the liver, Gospel disease caused by stagnation of bile, acute inflammation of the pancreas, enlarged liver, perforation of the stomach wall .
  • Renal dysfunction: pain in the lumbar region, blood or increased nitrogen in the urine, hemolytic-uremic syndrome, pollakiuria, kidney inflammation, renal edema.
  • Impaired visual perception, decreased hearing acuity.
  • Convulsive contraction of bronchial smooth muscles, inflammation of the mucous layer of the nasal cavity, swelling of the larynx.
  • Headache, aseptic inflammation of the meninges, increased body temperature, weakness of the neck or back muscles, muscle spasms, mental disturbances, increased activity, feelings of melancholy, hallucinations.
  • Hypertension, acute pulmonary failure, loss of consciousness.
  • Decreased hemoglobin levels in the blood, increased eosinophil levels and/or decreased white blood cell levels.
  • Bleeding from the nasal cavity, bleeding during operations.
  • Urticaria, purpura, inflammatory skin inflammation, erythema effusion, bullous inflammation of the dermis.
  • Burning when applied topically, pain along the vein when administered intravenously.
  • Anaphylactic reactions, skin itching, shortness of breath, hyperemia, Quincke's edema.
  • Increased sweating, weight gain, increased body temperature.

Contraindications

  • Drug intolerance.
  • Information about a history of hypersensitivity reactions when taking NSAIDs.
  • Inflammatory diseases of the mucous layer of the nasal cavity.
  • Bronchial asthma.
  • Insufficient volume of circulating blood.
  • Ulceration of the stomach or duodenum.
  • Hemostasis disorders.
  • Intestinal inflammation.
  • Liver dysfunction.
  • Renal dysfunction.
  • Insufficient or excessive levels of potassium in the blood.
  • Exacerbation of heart failure.
  • Premedication in the preoperative and surgical period.
  • Simultaneous use with drugs that affect blood clotting.
  • Age up to 16 years.
  • Dermatitis.
  • Simultaneous use with probenecid and pentoxifylline.
  • Pregnancy.
  • Lactation.

Use in children

The drug is contraindicated for persons under 16 years of age.

Use during pregnancy and breastfeeding

The drug is prohibited during pregnancy and breastfeeding. It can reduce the contractile activity of the uterus and affect the formation of the fetal circulatory system. In infants, inhibition of prostaglandins may lead to adverse effects.

Use in the elderly

In pensioners, the risk of side effects is increased; the drug must be used with caution.

Driving a car and other mechanisms

Due to the high incidence of adverse reactions, activities that require increased attention are not recommended.

Do I need a prescription?

Ketorol is sold by prescription.

Compatibility with other drugs

In case of drug interactions with other drugs, Ketorol may have an adverse effect. Concomitant use with other NSAIDs, ethyl alcohol or alcohol, glucocorticosteroids, anticoagulants, calcium supplements can cause an ulcerogenic effect and bleeding.

Ketorol should not be prescribed with paracetamol for a period of more than 2 days, because when taken in parallel with paracetamol, toxicity to the kidneys increases, and with methotrexate - toxicity to both the kidneys and liver.

If narcotic analgesics are used together with Ketorol, their dosage can be reduced.

Due to a decrease in prostaglandins in the kidneys, the effectiveness of diuretics and blood pressure lowering drugs is reduced.

Antacids do not affect the absorption of the drug.

When used with glucose-lowering drugs, it increases their effect.

Increases the dose of verapamil and nifedipine in the blood.

Alcohol compatibility

When taken together with alcohol, it can cause inflammation of the mucous layer of the stomach and duodenum. Subsequently, ulcers may form in the gastrointestinal tract, so compatibility with alcohol is dangerous.

Analogues of the drug Ketorol

Structural analogues of the active substance:

  • Adolor;
  • Acular LS;
  • Dolak;
  • Dolomin;
  • Ketalgin;
  • Ketanov;
  • Ketolac;
  • Ketorolac;
  • Ketofril;
  • Toradol;
  • Thorolak.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Compound

active ingredient: ketorolac;

1 ml ketorolac tromethamine 30 mg

Excipients: ethanol, sodium chloride, sodium edetate, octoxynol 9, sodium hydroxide, propylene glycol, water for injection.

Dosage form

Solution for injection.

Basic physical and chemical properties: A transparent, colorless to light yellow liquid that is practically free of visible particles and foreign inclusions.

Pharmacological group

Non-steroidal anti-inflammatory drugs.

ATX code M01A B15.

Pharmacological properties

Pharmacological.

Ketorolac tromethamine is an NSAID that exhibits analgesic activity. The mechanism of action of ketorolac (as well as other NSAIDs) is not fully understood, but may involve suppression of prostaglandin synthesis. The biological activity of ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine does not have sedative or anxiolytic properties.

The maximum analgesic effect of ketorolac is achieved within 2-3 hours. This effect was not statistically significant within the recommended dosage range. The biggest difference between high and low doses of ketorolac is the duration of analgesia. An analgesic dose of ketorolac also has an anti-inflammatory effect.

Pharmacokinetics.

Ketorolac tromethamine is a racemic mixture of the [˗]S- and [+]R-enantiometric forms, with the analgesic activity being due to the S-form. After administration, ketorolac is quickly and completely absorbed. The mean maximum plasma concentration of 2.2 mcg/ml is achieved on average 50 minutes after administration of a single dose of 30 mg.

Linear pharmacokinetics.

In adults, after administration of ketorolac tromethamine in the recommended dosing ranges, the clearance of the racemate does not change. This indicates that the pharmacokinetics of ketorolac tromethamine in adults following single or multiple intramuscular doses of ketorolac tromethamine is linear. At higher recommended doses, there is a proportional increase in the concentrations of free and bound racemate.

The drug does not penetrate the blood-brain barrier well. Ketorolac penetrates the placenta and, in small quantities, into breast milk. 99% of ketorolac in plasma is protein bound over a wide concentration range.

Metabolism.

Ketorolac tromethamine is largely metabolized in the liver. The products of metabolism are hydroxylated and conjugated forms of the derivative product. Metabolic products and some of the unchanged drug are excreted in the urine.

Excretion.

The main route of elimination of ketorolac and its metabolites is renal. Approximately 92% of the administered dose is determined in the urine, 40% in the form of metabolites and 60% in the unchanged form of ketorolac. Approximately 6% of the dose is excreted in the feces. In a study of a single dose of ketorolac 10 mg (n = 9), it was demonstrated that the S-enantiomer is eliminated twice as fast as the R-enantiomer, and clearance is independent of the route of administration. This means that the ratio of plasma concentrations of the S-enantiomer/R-enantiomer after each dose decreases over time. There are little or no differences between the S and R forms in humans.

The half-life of the S-enantiomer of ketorolac tromethamine is approximately 2.5 hours (DM ± 0.4), and the R-enantiomer is 5:00 (DM ± 1.7). Other studies have reported the half-life of the racemate to be 5-6 hours.

Savings.

Ketorolac tromethamine administered as an intravenous bolus every 6 hours for 5 days to healthy volunteers (n = 13) showed no significant differences on days 1 and 5. Trough levels averaged 0.29 μg/mL (SD ± 0.13) on day 1 and 0.55 μg/mL (SD ± 0.23) on day 6. Steady state was achieved after the fourth dose. The accumulation of ketorolac tromethamine in certain patient groups (elderly patients, children, patients with renal failure or liver disease) has not been studied.

Pharmacokinetics in certain groups of patients.

Elderly patients.

Based on data obtained after a single dose, the half-life of ketorolac tromethamine racemate increased from 5 to 7:00 in elderly patients (65-78 years) compared to young healthy volunteers (24-35 years).

Children. There are no pharmacokinetic data on intramuscular administration of ketorolac tromethamine to children.

Kidney failure.

According to data obtained after a single administration of the drug, the half-life of ketorolac tromethamine in patients with impaired renal function is 6-19 hours and depends on the severity of the impairment. There is almost no correlation between creatinine clearance and total clearance of ketorolac tromethamine in elderly patients and patients with impaired renal function (r = 0.5). In patients with kidney disease, the AUC 8 value of each enantiomer is increased by almost 100% compared to healthy volunteers. The volume of distribution doubles for the S-enantiomer and increases by 1/5 for the R-enantiomer. An increase in the volume of distribution of ketorolac tromethamine indicates an increase in the unbound fraction.

Liver failure.

The half-life, AUC 8 and Cmax in 7 patients with liver disease did not differ significantly from those of healthy volunteers.

Indications

Relief of moderate and severe postoperative pain for a short time.

Contraindications

Hypersensitivity to ketorolac or to any other component of the drug;

  • patients with active peptic ulcer disease, 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)
  • history of bronchial asthma
  • do not use as an analgesic before or during surgery
  • severe heart failure
  • complete or partial syndrome of nasal polyps, angioedema or bronchospasm;
  • do not use in patients who have undergone surgery with a high risk of hemorrhage or incomplete bleeding control and in patients receiving anticoagulants, including low doses of heparin (2500-5000 units every 12:00)
  • hepatic or moderate or severe renal failure (serum creatinine clearance more than 160 µmol/l);
  • suspected or confirmed cerebrovascular bleeding, bleeding diathesis, including blood coagulation disorders and 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 drug is contraindicated during labor and childbirth;
  • patients at risk of renal failure due to decreased fluid volume;
  • Epidural or intrathecal administration of the drug is contraindicated.

Interaction with other drugs and other types of interactions

Ketorolac is highly bound to plasma proteins (on average 99.2%). Ketorolac tromethamine does not alter the pharmacokinetics of other drugs through enzyme induction or inhibition.

Warfarin, digoxin, salicylates and heparin.

Ketorolac tromethamine slightly reduced the binding of warfarin to plasma proteins in vitro and did not change the binding of digoxin to plasma proteins. Research in vitro indicate that at therapeutic concentrations of salicylates (300 μg/ml), ketorolac binding was reduced from approximately 99.2% to 97.5%, indicating a possible twofold increase in unbound ketorolac plasma levels. Therapeutic concentrations of digoxin, warfarin, ibuprofen, naproxen, piroxicam, acetaminophen, phenytoin and tolbutamide do not change the binding of ketorolac tromethamine to plasma proteins.

Acetylsalicylic acid.

When used with acetylsalicylic acid, the binding of ketorolac to plasma proteins decreases, although the clearance of free ketorolac does not change. The clinical significance of this type of interaction is unknown, although, as with other NSAIDs, it is not recommended to co-administer ketorolac tromethamine and acetylsalicylic acid due to the potential increase in the incidence of side effects.

Diuretics.

In some patients, ketorolac can reduce the natriuretic effect of furosemide and thiazides. During concomitant therapy with NSAIDs, the patient should be closely monitored for signs of renal insufficiency and to ensure the effectiveness of the diuretic drugs.

Probenecid.

Concomitant use of ketorolac tromethamine and probenecid resulted in a decrease in the clearance of ketorolac and an increase in its plasma levels and half-life. So, the simultaneous use of ketorolac tromethamine and probenecid is contraindicated.

Lithium.

If NSAIDs and lithium are used concomitantly, patients should be closely monitored for signs of lithium toxicity. Increased plasma lithium concentrations have been reported when administered concomitantly with ketorolac.

Anticoagulants.

Ketorolac tromethamine should be used cautiously with anticoagulants, as concomitant use may enhance the anticoagulant effect.

Cardiac glycosides.

NSAIDs may worsen heart failure, reduce glomerular filtration rate and increase plasma levels of cardiac glycosides when used concomitantly with the latter.

Methotrexate.

Use at the same time with caution.

ACE inhibitors.

The simultaneous use of ACE inhibitors increases the risk of developing renal dysfunction, in particular in patients with a reduced volume of intercellular fluid.

NSAIDs may reduce the hypotensive effect of ACE inhibitors. This interaction should be kept in mind when prescribing NSAIDs with ACE inhibitors.

Anticonvulsants.

Isolated cases of seizures have been reported during the simultaneous use of ketorolac tromethamine and anticonvulsants (phenytoin, carbamazepine).

Psychotropic drugs.

With the simultaneous use of ketorolac and psychotropic drugs (fluoxetine, thiotexene, alprazolam), hallucinations have been reported.

Pentoxifylline.

Concomitant use of ketorolac tromethamine and pentoxifylline increases the risk of bleeding.

Non-depolarizing muscle relaxants.

No formal studies have been conducted on the concomitant use of ketorolac tromethamine and muscle relaxants. Cases of possible interaction between ketorolac and non-depolarizing muscle relaxants have been reported, resulting in apnea.

Cyclosporine. As with all NSAIDs, caution should be exercised when co-prescribing cyclosporine due to the increased risk of nephrotoxicity.

Mifepristone. After using mifepristone for 8-12 days, NSAIDs should not be used as they may reduce the effects of mifepristone.

Corticosteroids.

As with all NSAIDs, caution should be exercised when coadministering corticosteroids due to the increased risk of gastrointestinal bleeding.

Quinolines.

Patients taking quinolines have an increased risk of seizures.

β-blockers.

Ketorolac and other NSAIDs weaken the hypotensive effect of β-blockers.

Zidovudine.

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 with hemophilia who are treated concomitantly with zidovudine and ibuprofen.

Effect on laboratory test results.

Ketorolac inhibits platelet aggregation and may prolong bleeding time.

Features of application

The likelihood of side effects can be minimized by using the lowest effective dose for the shortest amount of time necessary to control symptoms. Physicians should be aware that in some patients, pain relief occurs only 30 minutes after administration.

The combined use of ketorolac tromethamine intramuscularly and orally in adult patients should not exceed 5 days.

Effect on fertility.

For women who are unable to become pregnant and undergo testing for this reason, the use of ketorolac tromethamine should be discontinued. Women with reduced fertility should avoid using the drug.

Effect on the digestive tract.

Ketorolac tromethamine can cause severe adverse reactions from the digestive tract. These side effects can occur in patients using ketorolac tromethamine at any time, with or without warning symptoms, and can be fatal. The risk of clinically serious gastrointestinal bleeding is dose-dependent. But side effects can occur even with short-term therapy. In addition to a history of peptic ulcer disease, provoking factors include the simultaneous use of oral corticosteroids, anticoagulants, long-term therapy with non-steroidal anti-inflammatory drugs, smoking, alcohol consumption, advanced age and poor health in general. Most spontaneous reports of events from the digestive tract concerned elderly or debilitated patients, therefore, when treating this category of patients, special attention should be paid to them and if suspicion arises, ketorolac should be discontinued. For patients at risk, consider alternative therapy that does not include nonsteroidal anti-inflammatory drugs (NSAIDs).

Effect on the circulatory system.

With simultaneous use of ketorolac tromethamine in patients receiving anticoagulant therapy, the risk of bleeding increases. Detailed studies of the simultaneous use of ketorolac and prophylactic low doses of heparin (2500-5000 units every 12:00) have not been conducted, so the risk of bleeding must also be taken into account with this regimen. Patients already taking anticoagulants or requiring low-dose heparin should not receive ketorolac tromethamine. Due to the condition of patients taking other drugs that negatively affect hemostasis, patients should be carefully monitored when administering ketorolac tromethamine. Ketorolac inhibits platelet aggregation and increases bleeding time. In patients with normal bleeding function, its time increased, but did not exceed the normal range, which is 2-11 minutes. In contrast to the prolonged action after taking acetylsalicylic acid, platelet function returns to normal within 24-48 hours after discontinuation of ketorolac. Patients who have undergone surgery with a high risk of bleeding or incomplete hemostasis should not use ketorolac tromethamine. Ketorolac tromethamine is not an anesthetic and does not have sedative or anxiolytic properties.

Use in patients with impaired renal function(see “Contraindications”) Patients with less severe renal impairment should receive lower doses of ketorolac (no more than 60 mg per day, intramuscularly). Such patients must be carefully monitored for their renal condition. Patients should be well hydrated before starting treatment. In patients undergoing hemodialysis, the clearance of ketorolac was reduced by approximately half the normal rate, and the terminal half-life was increased by almost three times.

Effect on the cardiovascular system and cerebral vessels.

Patients with hypertension and/or a history of mild to moderate heart failure should be closely monitored.

To minimize the risk of adverse cardiovascular complications in patients using NSAIDs, the minimum effective dose should be used for the shortest possible period of time. Ketorolac tromethamine should be prescribed to patients with uncontrolled hypertension, congestive heart failure, established coronary artery disease, peripheral arterial and/or cerebrovascular disease only after careful consideration of all the advantages and disadvantages of such treatment. It is also necessary to weigh the advisability of prescribing ketorolac before starting long-term treatment in patients at risk of developing cardiovascular diseases (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, and smokers).

Respiratory system.

The patient's condition should be monitored due to the likelihood of developing bronchospasm.

Use in patients with impaired liver function.

Ketorolac tromethamine should be administered with caution to patients with impaired liver function or a history of liver disease. A significant increase (more than three times the norm) of ALT and AST in the blood serum was observed in less than 1% of patients. In addition, there have been reports of isolated cases of severe hepatic reactions, including jaundice and fatal fulminant hepatitis, liver necrosis and liver failure, in some cases fatal. Ketorolac should be discontinued if clinical symptoms of liver disease or systemic manifestations (eg, eosinophilia, rash) appear.

NSAIDs should be used with caution in patients with a history of Crohn's disease and ulcerative colitis due to the possibility of worsening the course of the disease. Clinical studies and epidemiological data suggest that the use of some NSAIDs, especially at high doses and for long periods of time, may be associated with a small increased risk of arterial thromboembolic events such as myocardial infarction or stroke. Such a risk cannot be excluded for ketorolac. Like other non-steroidal anti-inflammatory drugs, ketorolac inhibits prostaglandin synthesis and may cause renal toxicity and should therefore be used with caution in patients with impaired renal function or a history of renal disease. Risk groups include patients with impaired renal function, hypovolemia, heart failure, impaired liver function, patients on diuretics, and elderly patients. Hypovolemia should be corrected before starting the use of ketorolac. Use of the drug in patients with systemic lupus erythematosus or connective tissue disease may be associated with an increased risk of developing aseptic meningitis. There have been reports of serious skin reactions such as exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. The highest risk of these reactions occurs at the beginning of treatment, with the first manifestations appearing in most cases during the first month of treatment. Patients should stop treatment with the drug at the first appearance of a rash, damage to the mucous membranes, or other manifestations of hypersensitivity. When treating patients with cardiac, renal or hepatic insufficiency who are taking diuretics, or after surgery in patients with hypovolemia, careful monitoring of diuresis and renal function is necessary. The total dose for patients over 65 years of age should not exceed 60 mg. When using ketorolac, cases of fluid retention, edema, NaCl retention, oliguria, increased serum urea nitrogen and creatinine levels have been reported, so ketorolac should be used with caution in patients with cardiac decompensation, arterial hypertension and similar conditions.

This medicine contains small amounts of ethanol (alcohol), less than 100 mg/dose.

This medicinal product contains less than 1 mmol (23 mg)/dose sodium, i.e. practically sodium-free.

Use during pregnancy or breastfeeding

Due to the known effects of non-steroidal anti-inflammatory drugs on the cardiovascular system of the fetus, ketorolac should not be used during pregnancy (especially in the third trimester). The use of ketorolac tromethamine is contraindicated during pregnancy, labor and childbirth.

Do not use during breastfeeding due to the possible negative effects of prostaglandin synthesis inhibitors on infants.

The ability to influence the reaction rate when driving vehicles or other mechanisms

During the period of treatment, it is necessary to refrain from potentially hazardous activities that require increased attention and speed of psychomotor reactions due to the possible development of adverse reactions from the nervous system.

Directions for use and doses

After administration, the analgesic effect is observed after 30 minutes, and maximum pain relief occurs after 1-2 hours. In general, the average duration of analgesia is 4-6 hours. The dose should be adjusted depending on the severity of pain and the patient's response to treatment. Continuous administration of multiple daily doses of ketorolac should not last more than 2 days, since long-term use increases the risk of adverse reactions. Experience with long-term use is limited, as the vast majority of patients were switched to oral administration of the drug or, after the administration period, patients no longer required analgesic therapy. The likelihood of side effects can be minimized by using the lowest effective dose for the shortest amount of time necessary to control symptoms. The drug cannot be administered epidurally or intraspinal.

Adults.

The recommended initial dose of ketorolac tromethamine injection is 10 mg, followed by 10-30 mg every 4-6 hours (if necessary). In the initial postoperative period, ketorolac tromethamine can be administered every 2:00 if necessary. The minimum effective dose should be prescribed. The total daily dose should not exceed 90 mg for young patients, 60 mg for elderly patients, patients with renal failure and body weight less than 50 kg. The maximum duration of treatment should not exceed 2 days. For patients weighing less than 50 kg, the dose should be reduced. The simultaneous use of opioid analgesics (morphine, pethidine) is possible. Ketorolac does not have a negative effect on opioid receptor binding and does not increase respiratory depression or the sedative effect of opioid drugs. For patients who receive the drug parenterally and who are switched to oral ketorolac tromethamine tablets, the total combined daily dose should not exceed 90 mg (60 mg for elderly patients, patients with impaired renal function and those weighing less than 50 kg), and in on the day when the dosage form is changed, the dose of the component should not exceed 40 mg. Patients should be switched to the oral form as quickly as possible.

Treatment. SPECIAL and supportive. There is no specific antidote. If there are symptoms of overdose after using the drug or after a large overdose (when ingesting a dose that is 5-10 times higher than usual) within 4:00, it is necessary to induce vomiting in the patient, take activated charcoal (60-100 g for adults) and / or osmotic laxative. The use of forced diuresis, urine alkalization, hemodialysis or blood transfusion is ineffective due to the high binding of the drug to blood plasma proteins. Single overdoses of ketorolac at different times led to abdominal pain, nausea, vomiting, hyperventilation, peptic ulcers and/or erosive gastritis, impaired renal function, which resolved after discontinuation of the drug.

Adverse reactions

From the digestive system: nausea, vomiting, dyspepsia, abdominal pain, taste changes, erosive and ulcerative lesions of the gastrointestinal tract, bleeding, ulcer perforation, diarrhea, dry mouth, extreme thirst, flatulence, constipation, cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis, stomatitis, feeling of fullness in the stomach, gastritis, esophagitis, belching, hematemesis, ground, exacerbation of colitis and Crohn's disease, liver failure.

From the nervous system: drowsiness, impaired concentration, euphoria, headache, dizziness, anxiety, asthenic syndrome, paresthesia, insomnia, malaise, increased fatigue, agitation, unusual dreams, confusion, vertigo, hyperkinesia; aseptic meningitis (fever, severe headache, convulsions, stiff neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis, fainting, pathological thinking.

From the cardiovascular system: bradycardia, hot flashes, purpura, pallor, rapid heartbeat, chest pain. There have been reports of edema, hypertension and heart failure associated with the use of non-steroidal anti-inflammatory drugs. Increased risk of arterial thromboembolic complications, such as myocardial infarction or stroke.

From the hematopoietic organs: aplastic anemia, hemolytic anemia, agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, neutropenia.

From the respiratory tract: bronchospasm, shortness of breath, pulmonary edema, laryngeal edema, bronchial asthma, exacerbation of bronchial asthma.

From the urinary system: nephrotic syndrome, oliguria, dysuria, increased urinary frequency, hyponatremia, hyperkalemia, increased creatinine and urea levels, interstitial nephritis, urinary retention, low back pain, acute renal failure, hematuria, azotemia, hemolyticouremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura).

From the skin: skin rashes (including maculopapular rash), purpura, exfoliative dermatitis (hyperemia, thickening or peeling of the skin, enlargement and / or soreness of the tonsils), photosensitivity, Lyell's syndrome, bullous reactions.

From the hemostasis system: bleeding from a postoperative wound, nosebleeds, rectal bleeding, increased bleeding time.

From the reproductive system: female infertility.

Allergic reactions: anaphylaxis (can be fatal) or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing, erythema malignant exudative (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), angioedema.

Ketorol is a non-steroidal anti-inflammatory drug that has a pronounced analgesic effect.

Release form and composition

Ketorol is produced in the form:

  • Solution – light yellow (or colorless) transparent (in dark glass ampoules of 1 ml);
  • Gel – transparent (translucent), homogeneous, with a characteristic odor (in aluminum tubes, laminated, 30 g each);
  • Film-coated tablets – biconvex green round, with the letter “S” embossed on one side (in blisters of 10 pcs.);

Active ingredient – ​​ketorolac tromethamine (ketorolac trometamol):

  • In 1 g of gel – 20 mg;
  • 1 tablet contains 10 mg;
  • In 1 ml of solution – 30 mg.

Auxiliary components:

  • Tablets: microcrystalline cellulose – 121 mg, sodium carboxymethyl starch (type A) – 15 mg, magnesium stearate – 2 mg, colloidal silicon dioxide – 4 mg, lactose – 15 mg, corn starch – 20 mg;
  • Solution: sodium hydroxide – 0.725 mg, octoxynol – 0.07 mg, disodium edetate – 1 mg, propylene glycol – 400 mg, sodium chloride – 4.35 mg, water for injection – up to 1 ml, ethanol – 0.115 ml;
  • Gel: tromethamine (trometamol) – 15 mg, propylene glycol – 300 mg, flavoring “Drimon Inde” (triethyl citrate – 0.09%, isopropyl myristate – 0.3%, castor bean seed oil – 0.14%, diethyl phthalate – 24.15 %) – 3 mg, carbomer 974P – 20 mg, glycerol – 50 mg, purified water – 390 mg, dimethyl sulfoxide – 150 mg, sodium propyl parahydroxybenzoate – 0.2 mg, sodium methyl parahydroxybenzoate – 1.8 mg, ethanol – 50 mg.

Composition of the film shell of the tablets: olive green (brilliant blue dye 22%, quinoline yellow dye 78%) – 0.1 mg; hypromellose – 2.6 mg; titanium dioxide – 0.33 mg; propylene glycol – 0.97 mg.

Indications for use

Ketorol is used for pain of severe and moderate severity:

  • Tablets: pain in the postpartum and postoperative period; toothache; rheumatic diseases; injuries; oncological diseases; sprains, dislocations; myalgia, neuralgia, radiculitis, arthralgia;
  • Solution: radiculitis, toothache, myalgia, arthralgia, neuralgia, trauma, pain in the postoperative period, with rheumatic and oncological diseases;
  • Gel: injuries – inflammation and bruise of soft tissues, bursitis, synovitis, ligament damage, epicondylitis, tendonitis; pain in muscles and joints (arthralgia, myalgia); neuralgia; rheumatic diseases; radiculitis.

Contraindications

Contraindications to the use of all forms of the drug are:

  • Incomplete or complete combination of intolerance to acetylsalicylic acid and other NSAIDs, bronchial asthma and recurrent nasal polyposis or paranasal sinuses;
  • Children under 16 years of age;
  • III trimester of pregnancy;
  • Breastfeeding period;
  • Hypersensitivity to the active substance or auxiliary components of the drug.

Contraindications for tablets and solution:

  • Childbirth;
  • Active gastrointestinal bleeding, erosive and ulcerative changes in the mucous membrane of the stomach and duodenum;
  • Cerebrovascular or other bleeding;
  • Hemophilia and other bleeding disorders;
  • Inflammatory bowel diseases (ulcerative colitis, Crohn's disease) in the acute phase;
  • Active liver disease, liver failure;
  • Severe renal failure, confirmed hyperkalemia, progressive kidney disease;
  • Decompensated heart failure;
  • Postoperative period after coronary artery bypass surgery.

With caution:

  • Diabetes mellitus;
  • Cholestasis;
  • Sepsis;
  • Edema syndrome;
  • Smoking;
  • Bronchial asthma;
  • Congestive heart failure;
  • Coronary heart disease;
  • Arterial hypertension;
  • Cerebrovascular diseases;
  • Pathological hyperlipidemia or dyslipidemia;
  • Renal dysfunction;
  • Systemic lupus erythematosus;
  • Peripheral arterial diseases;
  • Simultaneous use with other NSAIDs;
  • Hypersensitivity to other NSAIDs;
  • Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract;
  • Severe somatic diseases;
  • Alcohol abuse;
  • Old age (over 65 years old);
  • Concomitant therapy with anticoagulants, antiplatelet agents, oral corticosteroids, SSRIs.

Contraindications for applying the gel: eczema, weeping dermatoses, wounds at the site of intended application of the drug, infected abrasions.

The gel is used with caution in old age, with bronchial asthma, exacerbation of hepatic porphyria, severe liver or kidney failure, erosive and ulcerative lesions of the gastrointestinal tract, chronic heart failure, in the first and second trimester of pregnancy.

Directions for use and dosage

The tablets are taken orally. Single dose – 1 pc. In cases of severe pain, depending on the severity of the pain, take 1 piece again. up to 4 times a day. The maximum daily dose should not exceed 4 tablets. It is recommended to use the minimum effective dose. The duration of therapy should not exceed 5 days.

In cases of switching from parenteral administration of Ketorol to oral administration, the total daily dose of both forms of the drug 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. On the day of transition, the dose of tablets should not exceed 30 mg.

The gel is used externally. Before applying it, wash and dry the surface of the skin. Apply and distribute 1–2 cm of gel in a thin, even layer with soft massaging movements to the area of ​​maximum pain 3–4 times a day.

Repeated use of the drug is possible no earlier than after 4 hours. The gel should be used no more than 4 times a day. The specified dose cannot be exceeded.

The solution for intravenous and intramuscular administration is used in minimally effective doses, selected according to the intensity of pain.

For patients aged 16 to 64 years with a body weight exceeding 50 kg, no more than 60 mg is administered intramuscularly once. In most cases, 30 mg of solution is prescribed every 6 hours. 30 mg is administered intravenously, but not more than 15 doses in 5 days.

For adult patients weighing less than 50 kg or with chronic renal failure, no more than 30 mg is administered intramuscularly, usually 15 mg (but not more than 20 doses in 5 days). No more than 15 mg is administered intravenously every 6 hours (up to 20 doses in 5 days).

When administered intravenously, the drug must be administered at least 15 seconds before. Intramuscular injection is given slowly, deep into the muscle.

The maximum daily dose of the solution 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. The duration of therapy for parenteral administration should not exceed 5 days.

Side effects

The use of Ketorol in the form of solution and tablets can cause side effects from some body systems:

  • Urinary system: rarely - nephritis, frequent urination, lower back pain with or without hematuria, azotemia, acute renal failure, increased or decreased urine volume, edema of renal origin, hemolytic-uremic syndrome (renal failure, thrombocytopenia, hemolytic anemia, purpura) ;
  • Digestive system: often (especially in elderly patients over 65 years of age with a history of erosive and ulcerative lesions of the gastrointestinal tract) - diarrhea, gastralgia; less often - flatulence, stomatitis, vomiting, feeling of fullness in the stomach, constipation; rarely - nausea, cholestatic jaundice, acute pancreatitis, hepatitis, hepatomegaly, erosive and ulcerative lesions of the gastrointestinal tract (including with bleeding or perforation - melena, abdominal pain, burning or spasm in the epigastric region, nausea, vomiting like “coffee grounds”, heartburn and others);
  • Sense organs: rarely - ringing in the ears, hearing loss, visual impairment (including blurred visual perception);
  • Central nervous system: often – drowsiness, dizziness, headache; rarely - depression, aseptic meningitis (severe headache, fever, stiffness of the back and/or neck muscles, convulsions), hallucinations, hyperactivity (restlessness, mood changes), psychosis;
  • Respiratory system: rarely - rhinitis, bronchospasm, laryngeal edema (difficulty breathing, shortness of breath);
  • Cardiovascular system: less often - increased blood pressure, rarely - fainting, pulmonary edema;
  • Hematopoietic organs: rarely – leukopenia, eosinophilia, anemia;
  • Hemostasis system: rarely - rectal bleeding, nosebleeds, bleeding from a postoperative wound;
  • Skin: less often – purpura, skin rash (including maculopapular rash); rarely - Stevens-Johnson syndrome, exfoliative dermatitis (pain and/or swelling of the tonsils, thickening, peeling or redness of the skin, fever with or without chills), Lyell's syndrome, urticaria;
  • Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (skin rash, change in facial skin color, itching of the skin, urticaria, swelling of the eyelids, shortness of breath, difficulty breathing, wheezing, heaviness in the chest, periorbital edema);
  • Local reactions: less often - pain or burning at the injection site;
  • Other reactions: often - weight gain, swelling (of feet, ankles, legs, fingers, face); less often – increased sweating; rarely – fever, swelling of the tongue.

The drug in gel form can cause peeling, hives, and itching. When applied to large areas of the skin, systemic adverse reactions may occur - heartburn, diarrhea, nausea, vomiting, gastralgia, ulceration of the gastrointestinal mucosa, allergic reactions, dizziness, headache, fluid retention, prolongation of bleeding time, increased activity of liver transaminases, hematuria, thrombocytopenia , leukopenia, anemia, agranulocytosis.

Special instructions

Before prescribing the drug, it is necessary to find out whether the patient has previously had allergic reactions to Ketorol or NSAIDs. Due to the risk of allergic reactions, the first dose should be administered under close medical supervision.

Hypovolemia increases the risk of developing nephrotoxic adverse reactions.

If necessary, the drug can be used in combination with narcotic analgesics.

When used simultaneously with other NSAIDs, cardiac decompensation, fluid retention, and increased blood pressure may occur. The effect on platelet aggregation ceases after 1-2 days.

The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

In case of blood clotting disorders, the drug is prescribed only with constant monitoring of the platelet count. It is especially important for postoperative patients who require careful monitoring of hemostasis.

The risk of developing drug complications increases with increasing doses of the drug (more than 90 mg per day) and lengthening therapy.

To reduce the risk of developing NSAID gastropathy, omeprazole, misoprostol, and antacid medications are prescribed.

The gel should be applied only to intact areas of the skin and avoid contact with open wounds, eyes and mucous membranes. Do not apply airtight dressings over the drug. After applying the gel, you must wash your hands thoroughly with soap. The tube should be tightly closed after each use.

During therapy, patients should be careful when conducting potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug interactions

The use of ketorolac in combination with calcium supplements, corticotropin, glucocorticosteroids, ethanol, acetylsalicylic acid or other NSAIDs can lead to the development of gastrointestinal ulcers and gastrointestinal bleeding.

Prescribing ketorolac simultaneously with methotrexate is permissible only when using low doses of the latter, and the concentration of methotrexate in the blood plasma should be monitored.

When using ketorolac, the clearance of lithium and methotrexate may decrease and the toxicity of these substances may increase.

Probenecid increases plasma concentrations, increases T1/2, reduces plasma clearance and Vd of ketorolac.

The risk of bleeding when used with ketorolac is increased by heparin, antiplatelet agents, indirect anticoagulants, pentoxifylline, thrombolytics, cefotetan and cefoperazone.

The complete absorption of the drug is not affected by antacids.

Please note that Ketorol:

  • Increases the hypoglycemic effect of oral hypoglycemic drugs and insulin;
  • Reduces the effect of diuretic and antihypertensive drugs;
  • Increases the risk of developing nephrotoxicity when prescribed with other nephrotoxic drugs;
  • Increases the concentration of nifedipine and verapamil in the blood plasma;
  • When used simultaneously with valproic acid, it causes a disorder of platelet aggregation.

It is possible that Ketorol gel may interact pharmacokinetically with drugs that compete for binding to plasma proteins.

Before using the gel, you should consult a doctor if the patient is using phenytoin, digoxin, cyclosporine, other NSAIDs, methotrexate, antihypertensive and antidiabetic drugs, or is under medical supervision.

Terms and conditions of storage

Store at a temperature not exceeding 25 °C in a place protected from light, dry and out of reach of children.

The shelf life of the gel is 2 years, the solution and tablets are 3 years.