Ketorol maximum daily dose. Is it possible to give Ketorol to children? Switching from intramuscular to internal use

Instructions for use:

Ketorol is an analgesic drug with anti-inflammatory and antipyretic effects.

pharmachologic effect

The active substance of Ketorol is ketorolac, which, by inhibiting the activity of the enzyme cyclooxygenase, helps inhibit the biosynthesis of prostaglandins, which are modulators of inflammation, thermoregulation and pain sensitivity.

The analgesic effect of Ketorol injections can be observed within half an hour after administration, and the maximum effect – after 1-2 hours.

The therapeutic effect of Ketorol lasts for 4-6 hours.

Indications for use

The instructions recommend prescribing Ketorol for moderate or severe pain: muscle and back pain, pain due to joint injuries, sprains, dislocations, postoperative pain, neuralgia, cancer, radiculitis, toothache, migraine, burns, etc.

Instructions for use Ketorol

Ketorol, the use of which is advisable only for acute pain syndrome, and not for the treatment of chronic pain, is available in the form of tablets and solution for intramuscular injection.

Depending on the severity of the pain syndrome, Ketorol tablets can be prescribed once or repeatedly.

The injection solution should be administered deeply intramuscularly. For patients under 65 years of age, Ketorol injections are prescribed in a dose of 10-30 mg once or the same dose every 4-6 hours, while the maximum daily dose should not exceed 90 mg. For patients over 65 years of age, Ketorol injections are given according to the scheme described above, with the only difference being that the maximum single dose should be 15 mg, and the maximum daily dose should be 60 mg. Ketorol injections can be used for no longer than 5 days.

When switching from intramuscular administration to oral administration of Ketorol, the total daily doses of the drug must be taken into account: on the day of transition - 30 mg, for patients over 65 years old - 60 mg, for patients under 65 years old - 90 mg.

Side effects

Ketorol tablets and injections can provoke such undesirable reactions in patients as:

• diarrhea, stomach pain, vomiting, constipation, flatulence, stomatitis, nausea, heartburn;
• lower back pain, acute renal failure, frequent urination, nephritis (inflammation of the kidneys), decreased or increased volume of urine;
• bronchospasm, laryngeal edema, rhinitis;
• headache, drowsiness, dizziness, hyperactivity, depression, ringing in the ears, hearing loss, blurred vision.
• increased blood pressure, fainting, pulmonary edema;
• leukopenia (increase in white blood cells), eosinophilia (increase in the number of eosinophils), anemia (decrease in the number of red blood cells or hemoglobin);
• rectal, nasal, bleeding from postoperative wounds;
• purpura, skin rash, urticaria, Lyell's syndrome (allergic dermatitis as a reaction to drugs), Stevens-Johnson syndrome (the appearance of blisters on areas of the skin and on the mucous membrane of various organs);
• itching, urticaria, change in complexion, skin rash, swelling of the eyelids, difficulty breathing, wheezing, heaviness in the chest;
• weight gain, swelling of the feet, fingers, ankles, legs, face, tongue, increased sweating, fever;
• pain or burning at the injection site of Ketorol.

Contraindications to the use of Ketorol

According to the instructions, Ketorol is not used to treat chronic pain syndrome. The use of Ketorol is contraindicated for:

• bronchospasm (narrowing of the bronchi as a result of muscle contraction);
• “aspirin” asthma (attacks of asthma associated with taking salicylates);
• hypovolemia (decreased blood volume);
• angioedema (limited deep swelling of the mucous membranes or subcutaneous tissue and skin);
• dehydration (dehydration);
• peptic ulcers (ulceration of the mucous membrane of the esophagus as a result of exposure to gastric juice on one of its segments);
• erosive and ulcerative lesions of the digestive tract in the acute phase;
• hypocoagulation (reduced blood clotting);
• hemorrhagic diathesis (diseases of the blood system, which are characterized by a tendency to increased bleeding);
• hemorrhagic stroke (bleeding in the brain caused by rupture of blood vessels);
• liver or kidney failure;
• concomitant use with other anti-inflammatory non-steroidal drugs;
• hemorrhage disorders;
• high risk of bleeding;
• hypersensitivity to ketorolac or other non-steroidal anti-inflammatory drugs.

Ketorol, the use of which must be discussed with the attending physician, is not prescribed to pregnant and lactating women, as well as children and adolescents under 16 years of age.

The instructions recommend using Ketorol with caution for cholecystitis (inflammation of the gallbladder), arterial hypertension, chronic heart failure, bronchial asthma, impaired renal function, sepsis (infection agents entering the blood), active hepatitis, polyps (tissue growths) of the mucous membrane of the nasopharynx and nose , systemic lupus erythematosus (connective tissue disease).

Additional Information

Active ingredient - ketorolac tromethamine - 10 mg; excipients - microcrystalline cellulose, pregelatinized starch, corn starch, colloidal anhydrous silicon dioxide, magnesium stearate (E170). Shell: opadry 03K51148 green (hypromellose 6cP, titanium dioxide (E171), triacetin/glycerol triacetate, iron dioxide yellow (E172), varnish FD&C blue/diamond blue FCF (E133)).

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drugs. ATX code: M01 AB15.

Pharmacologicalproperties

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

Ketorol film-coated tablets 10 mg are used for short-term treatment of acute pain (including postoperative pain) of moderate intensity, only as a continuation of previous parenteral (intramuscular or intravenous) therapy in a hospital setting, if necessary. The total duration of parenteral and oral therapy with ketorolac should not exceed 5 days due to the possibility of increasing the frequency and severity of adverse reactions.

Before taking Ketorol, consider the potential benefits and risks and options for using another drug.

Use the lowest effective dose for the shortest possible time. Patients should be switched to alternative treatment as quickly as possible.

Dosage regimen and method of administration

The duration of the course of use of ketorolac should not exceed 5 days; long-term use, as well as oral administration at a dose of more than 40 mg per day, is not recommended. To reduce the risk of side effects, it is recommended to use the minimum effective dose for the minimum time required to relieve pain.

Adults: 10 mg every 4 or 6 hours as needed. The total daily dose when switching from parenteral administration of the drug to oral administration should not exceed 90 mg (60 mg for elderly patients, patients with renal failure, patients weighing less than 50 kg), and part of the dose prescribed orally for combined administration should not exceed 40 mg per day by changing the form of administration.

Adults weighing less than 50 kg or with impaired renal function: the frequency of use of the drug is reduced to 1-2 times a day.

Side effect

The most common gastrointestinal disorders occur, among which more than 10% of patients experience nausea, pain in the stomach and intestines, and dyspepsia; Diarrhea often occurs (7%). The central nervous system is characterized by disturbances in the form of headache (17%), drowsiness (6%), dizziness (7%). In 4% of cases, edema develops.

Somewhat less frequently, but more than 1% of patients develop hypertension, itching, rash, stomatitis, vomiting, constipation, flatulence, a feeling of heaviness in the abdomen, sweating and hemorrhagic rash. In less than 1% of patients, weight loss, fever, and asthenia are possible; palpitations, pale skin, fainting; skin rash; gastritis, bleeding from the rectum, loss or increase in appetite, belching; nosebleeds, anemia, eosinophilia, tremor, sleep disturbances, hallucinations, euphoria, extrapyramidal syndromes, paresthesia, depression, nervousness, thirst, dry mouth, visual impairment, impaired attention, hyperkinesis, stupor; shortness of breath, pulmonary edema, rhinitis, cough; hematuria, proteinuria, oliguria, urinary retention, polyuria, increased urination.

There have been cases of hypersensitivity reactions (in the form of anaphylaxis, anaphylactoid reaction, laryngeal edema, tongue edema); hypotension and flushing of the skin; Lyell's syndrome, Stevens-Johnson syndrome, exfoliative dermatitis, maculopapular rash, urticaria; formation of ulcers in the gastric mucosa, gastrointestinal bleeding, perforation of the walls of the gastrointestinal tract, melena, acute pancreatitis; postoperative wound bleeding, thrombocytopenia, leukopenia; hepatitis, liver failure, cholestatic jaundice; convulsions, psychoses, aseptic meningitis; bronchospasm, acute renal failure, pain in the kidney area, hematuria and azotemia, hyponatremia, hyperkalemia, hemolytic uremic syndrome.

To prevent possible side effects, one should strive to use the minimum effective doses of the drug, strictly adhere to the established dosages and administration regimens, take into account the patient’s condition (age, renal function, state of the gastrointestinal tract, water-electrolyte metabolism and hemostatic system), as well as possible drug interactions with combination therapy.

Contraindications

Bronchial asthma, complete or partial syndrome of nasal polyps, bronchospasm, angioedema in history.

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 or intracranial bleeding.

History of coagulation disorders, conditions with a high risk of bleeding, bleeding diathesis, coagulopathies, hemorrhagic stroke, low-dose heparin therapy. 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 up to 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.

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 to become pregnant.

Food: reduces the rate, but does not affect the volume of absorption of ketorolac.

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

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.

Applyeducation in pediatric practice

Risk during childbirth: may adversely affect fetal circulation and suppress uterine contractions.

Impact on the ability to drive vehiclessports and working with machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Warnings and Precautions

The course of treatment with Ketorol should not exceed 5 days.

Taking Ketorol can lead to peptic ulcers and gastrointestinal bleeding, which can be fatal.

The use of NSAIDs can lead to the development of cardiovascular diseases, myocardial infarction and stroke.

Ketorol is contraindicated for use in the postoperative period during coronary artery replacement.

Before administering ketorolac, hypovolemia and hypoproteinemia should be eliminated, and water and electrolyte balance should be restored.

Retention of fluid, sodium chloride, oliguria, increased concentrations of urea nitrogen and creatinine in plasma were observed during clinical studies, and therefore ketorolac should be prescribed with caution to patients with heart failure, arterial hypertension or pathological conditions with similar manifestations.

Since ketorolac affects platelet aggregation, use in patients with pathologies of the blood coagulation system should be carefully monitored. Ketorolac is prescribed with extreme caution simultaneously with anticoagulants.

Patients over 65 years of age are more likely to experience adverse reactions characteristic of NSAIDs, so this category of patients is recommended to prescribe doses that are at the lower limit of the therapeutic range.

Drug interactions

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, increases its concentration in the blood plasma and increases its half-life. With the use of ketorolac, the clearance of methotrexate and lithium may decrease and the toxicity of these substances may increase.

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 during simultaneous use of ketorolac and psychostimulant drugs (fluoxetine, thiothixene, alprazolam).

Overdose

An overdose of ketorolac with 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, and 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.

Symptoms of physical pain can come unexpectedly and last for a short time. When the pain syndrome is prolonged, this is a signal of a serious illness that requires emergency treatment. However, until the doctor determines the cause of the debilitating syndrome, a special drug, ketorol, is prescribed to relieve pain, an injection which relieves suffering within 30 minutes, and the analgesic effect lasts about 5 hours.

Basic information about the medication

Ketorol belongs to the group of drugs NSAIDs (non-steroidal anti-inflammatory drugs), a class of derivatives of pyrrolysine-carboxylic acid. Any form of the drug has an analgesic and anti-inflammatory effect with signs of a moderate antipyretic effect. However, after using Ketorol injections, the analgesic effect is much stronger and occurs faster, unlike other types of medication.

1. Gel. A homogeneous transparent substance, used externally, has a characteristic odor, packaged in tubes of 30 g.
2. The tablets are greenish in color, biconvex in shape, packaged in packs of 20 pieces. A distinctive feature of Ketorol tablets is the presence of the letter “S” on one side.
3. Ampoules (glass) of 1 ml with a solution for intramuscular and intravenous administration are equipped with a recess for breaking and a ring. The package contains 10 ampoules.

Reference: Ketorol in tablet and injection form is used to relieve pain not only of moderate intensity, but also to relieve severe pain of various natures. The gel is prescribed to reduce pain and inflammation at the sites of application.

Composition of dosage forms

The active component of any type of drug is the substance ketorolac. The instructions for use indicate that ketorolac is present in varying degrees of concentration in each form of the drug:

• gram of gel contains 20 mg of active substance dissolved in a mixture of purified water, ethyl alcohol and glycerol with the addition of flavor and auxiliary substances;
• the tablet contains 10 mg of ketorolac with the addition of corn starch, cellulose, lactose and other components;
• The attached instructions indicate that the injection solution contains 30 mg of ketorolac, prepared on the basis of deionized water, ethyl alcohol, sodium chloride, and other additional substances.

Clarification: Ketorol injectable form is preferable to prescribe for quick relief of pain, as well as when it is impossible to take pills due to stomach diseases (ulcers, gastritis, gag reflex, etc.). The instructions indicate that Ketorol (ampoules and tablets) is available with a prescription.

Features of the drug's action

The basis for the therapeutic effect of the drug Ketorol, as a representative of the NSAID line, is considered to be the biochemical process of inhibition of a special substance. The enzyme cyclooxygenase promotes the conversion of arachidonic acid into components (prostaglandins) that trigger an inflammation reaction, the development of pain, and an increase in body temperature. Ketorolac, by blocking the action of cyclooxygenase, stops the synthesis of prostaglandins, resulting in the cessation of inflammation, pain syndrome, and increased temperature.

Due to its powerful analgesic effect, comparable to the analgesia of morphine, the drug is primarily used for pain relief; the anti-inflammatory and antipyretic effects are secondary. According to the instructions, one of the main advantages of the symptomatic use of Ketorol is the absence of the following consequences:

• anxiolytic and sedative effects;
• respiratory depression, as well as urinary retention;
• development of drug dependence;
• disorders of the cardiovascular system;
• effects on the functioning of opiate receptors.

Despite the benefits, the instructions for use of the drug warn that Ketorol injections should be prescribed with caution to people suffering from pathologies with a risk of bleeding. The medicine helps to thin the blood while reducing the activity of its coagulation, but without exceeding the normal limit.

Body reaction

When treated with tablets, the active substance of the drug is quickly absorbed in the digestive tract (30-40 minutes). Regardless of the method of ketorol entering the body, the use of the drug ensures 100% bioavailability, but the parenteral form of administration (injections) promotes more complete and rapid absorption of the incoming components.

The method of intramuscular administration of the drug demonstrates its rapid integration into the bloodstream system due to the complete absorption of the active substance from the injection sites. The speed of onset of the analgesic effect after Ketorol injections depends on the strength of the pain syndrome:

• mild pain - the drug will take effect in 20-40 minutes;
• average pain threshold – it will take 30-60 minutes for pain relief;
• High intensity pain will subside 1-2 hours after the injection.

Biotransformation of ketorolac (more than 50% of the administered dose) occurs in the liver with the formation of non-analgesic metabolites. Inactive substances are excreted by the kidneys (91%) and intestines (6%) within 5 hours, faster in young patients than in older people. In some kidney diseases, the half-life of metabolites can extend to 13 hours or more.

Important: the instructions warn that any form of medication should not be used for a long time, since the active substance has a detrimental effect on the gastric mucosa, ulcerating it. In addition, traces of Ketorol are detected in breast milk 2 hours later, even after taking one tablet.

When are injections prescribed?

The use of Ketorol is symptomatic therapy; the drug is prescribed intramuscularly for short-term relief of pain and inflammation during the postoperative period. Injections with minimally effective doses are relevant for the following problems:

• symptoms of arthritis associated with joint inflammation;
• signs of arthrosis caused by degenerative-dystrophic destruction of articular cartilage;
• myalgia (muscle pain) and neuralgia (pinched nerve roots), as a consequence of the inflammatory process.

Due to its rapid analgesic effect, intramuscular administration of Ketorol helps reduce pain and swelling in rheumatic pathology, after a bruise or injury. Courses of injections are prescribed to relieve cancer pain; tablets are used to eliminate dental, headache, and menstrual pain, but chronic pain syndrome is not treated with Ketorol.

Rules for the use of the drug

According to the instructions for the drug, Ketorol tablets should be swallowed whole and washed down with a sufficient amount of water. The tablets should not be crushed or chewed, but can be taken regardless of meals, taking into account the specific dosage:

• single dose - once a day, one Ketorol tablet containing 10 mg of the active substance;
• repeated use - a maximum of 4 times a day, focusing on the severity of the pain syndrome.

Important: do not exceed the maximum daily dose of a short-term course of 5 days. Failure to follow the instructions increases the risk of developing side effects, dangerous complications after treatment with a non-steroidal anti-inflammatory drug.

Solution in ampoules

The instructions indicate that ampoules with Ketorol solution are completely ready for use; the doctor prescribes their use in a certain dosage, which is prohibited from being exceeded. To relieve pain, intramuscular injections are usually indicated in the gluteal region, and less often in the thigh or shoulder. If the doctor has not determined the individual dosage, then for a single administration you can use from 1 to 3 ampoules, taking into account the severity of the pain.

The dosage of Ketorol solution for injections, as an NSAID, is designed for the age group up to 65 years. If a patient switches from injections to tablets, you should carefully consider the total daily dose:

Information: the contents of the ampoule can be added to the dropper with other medicinal solutions compatible with ketorolac. The duration of a continuous course of treatment with injections, which are cheaper than tablets, should not exceed 5 days. If the pain does not go away, you will have to go to the doctor for in-depth diagnostics to identify the cause of the pain.

When injections are contraindicated

The use of Ketorol injections is not prescribed for hypersensitivity to any component of the medicinal solution. The instructions warn that injections are contraindicated:

• for diseases of the bronchopulmonary system, accompanied by swelling of the mucous membranes, bronchospasm;
• with erosive and ulcerative lesions of the mucous organs of the gastrointestinal tract, severe diseases of the liver and kidneys;
• with hematopoietic disorders, high risk of bleeding, including postoperative bleeding;
• with dehydration, hemophilia, polyposis;
• for symptoms of hemorrhagic stroke with cerebral hemorrhage.

Medicines in tablets or ampoules do not relieve pain in pregnant or lactating women, and are not used to relieve pain during labor. The instructions inform you that Ketorol is not used to treat children under 16 years of age and is not combined with other types of NSAIDs. Attention: the appearance of side effects indicates immediate discontinuation of painkiller injections.

Threat of side effects

Most often, the gastrointestinal tract suffers from undesirable manifestations of NSAID treatment, even in injections. Treatment with Ketorol can provoke diarrhea, symptoms of gastralgia; less often, patients complain of constipation, vomiting, flatulence, and there is a possibility of developing focal ulcerations.

According to patient reviews, the drug in injections has a stable effect, but some experience nausea with heartburn after taking the painkiller. Sometimes patients complain of dizziness accompanied by headache, but the symptoms disappear after completing the course.

Infrequently, the response to the administration of Ketorol from the respiratory system is the development of bronchospasm, the appearance of rhinitis, edema of the larynx, even of the lungs. The possibility of ringing in the ears, deterioration of hearing and vision cannot be ruled out. The cardiovascular system may respond to the injection use of Ketorol by increasing blood pressure.

Ketorol®

International nonproprietary name

Ketorolac

Dosage form

Film-coated tablets 10 mg

Compound

One tablet contains

active substance - ketorolac tromethamine 10 mg

Excipients:

microcrystalline cellulose (type 102), pregelatinized corn starch, corn starch, colloidal anhydrous silica, magnesium stearate

shell composition: Opadry 03K51148 green (hypromethylcellulose (6срs), titanium dioxide E171, triacetin/glycerin, iron (III) oxide yellow E172, dye FD&C No. 1 (diamond blue FCF, aluminum varnish 11-13%)

Description

Round, biconvex, olive green film-coated tablets, engraved with "S" on one side and smooth on the other side, with a diameter of (8.20 ± 0.20) mm and a thickness of (3.50 ± 0.20) mm.

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drugs. Derivatives of acetic acid.

ATS code М01АВ15

Pharmacological properties

Pharmacokinetics

When taken orally, ketorolac is well absorbed from the gastrointestinal tract. The maximum concentration in blood plasma (0.7 - 1.1 mcg/ml) is achieved 40 minutes after taking a dose of 10 mg on an empty stomach. Fat-rich foods reduce Cmax and delay its achievement by 1 hour.

Ketorol® is almost completely bound to plasma proteins (> 99%) due to its small volume of distribution (<0.3 л/кг).

The time to reach equilibrium concentration after oral administration is 24 hours when administered 4 times a day. When taken orally 10 mg it is 0.39 - 0.79 mcg/ml.

Almost all the substance circulating in the blood plasma is ketorolac (96%) or its pharmacologically inactive metabolite R-hydroxyketorolac.

The drug passes through the placental barrier by 10%. Found in low concentrations in women's breast milk. It does not pass through the blood-brain barrier well.

The drug is metabolized mainly in the liver, binding to glucuronic acid, and is excreted by the kidneys. Up to 92% of the administered dose of the drug is found in the urine, with 40% in the form of metabolites, 60% in the form of unchanged substance. About 6% of the administered dose is excreted in feces. Metabolites do not have significant analgesic activity.

In elderly patients (over 65 years), the half-life of the terminal phase, compared with that in young people, increases to 7 hours (from 4.3 to 8.6 hours). Total plasma clearance, compared with young people, can be reduced to an average of 0.019 l/hour/kg.

When renal function is impaired, the elimination of ketorolac slows down, as evidenced by a prolonged half-life and a decrease in total plasma clearance compared to young healthy volunteers. The rate of elimination decreases approximately in proportion to the degree of renal impairment, except in patients with severe renal impairment. In such patients, plasma clearance of ketorolac becomes slightly higher than expected for a given degree of kidney damage.

Pharmacodynamics

Ketorol® is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory effects. The main mechanism of action of ketorol, like other NSAIDs, is manifested in its pharmacological effect - inhibition of prostaglandin synthesis. NSAIDs are most active in the periphery.

Ketorol® does not have a sedative or anxiolytic effect and does not affect opioid receptors. Ketorol® does not have a depressant effect on the respiratory center and does not enhance respiratory depression and sedation caused by opioid analgesics. Ketorol® does not cause drug dependence. After abrupt discontinuation of the drug, withdrawal symptoms do not occur.

Indications for use

Pain relief in the postoperative period

Relief of pain in muscles and joints

Post-traumatic pain syndrome

Renal colic

Directions for use and doses

A short course of treatment is prescribed and applied for 7 days; it is not recommended for long-term treatment.

Adults

10 mg every 4 - 6 hours. The daily dose should not exceed 40 mg.

For patients taking ketorol parenterally, the total dose of the drug during combination therapy should not exceed 90 mg per day.

Side effects

Often (more than 3%)

Headache, dizziness, drowsiness

Swelling of the face, legs, ankles, fingers, feet

Weight gain

Less common (1 - 3%)

Skin rash, purpura

Excessive sweating

Rarely (less than 1%)

Acute renal failure, low back pain with or without hematuria and/or azotemia, hemolytic uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased urine volume, nephritis, edema of renal origin

Hearing loss, ringing in the ears, visual impairment

Bronchospasm or dyspnea, rhinitis, laryngeal edema

Anemia, eosinophilia, leukopenia

Bleeding from a postoperative wound, nosebleeds, rectal bleeding

Anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea, eyelid swelling, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing)

Aseptic meningitis (fever, severe headache, convulsions, stiff neck and/or back), hallucinations, depression, psychosis

Exfoliative dermatitis (fever with or without chills, redness, thickening or flaking of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome

Swelling of the tongue, fever.

Contraindications

Hypersensitivity to ketorol, aspirin or other NSAIDs

- “aspirin” asthma, angioedema

Hypovolemia

Dehydration

Erosive and ulcerative lesions of the gastrointestinal tract

Peptic ulcers

Hypocoagulation, including hemophilia

Liver, kidney failure

Hemorrhagic stroke

Bleeding, including after surgery

Hematopoiesis disorder

Pre- and surgical period, due to the high risk of bleeding

Chronic pain

Pregnancy and lactation

Children and teenagers up to 18 years of age

Drug interactions

The simultaneous use of ketorol with acetylsalicylic acid or other NSAIDs, calcium preparations, glucocorticoids, ethanol, corticotropin can lead to the formation of ulcers of the gastrointestinal tract and the development of gastrointestinal bleeding.

Combined use with paracetamol increases nephrotoxicity, and with methotrexate - hepato- and nephrotoxicity. The simultaneous administration of ketorol and methotrexate is possible only when using low doses of the latter.

Probenecid reduces the plasma clearance and volume of distribution of ketorol, increases its concentration in the blood plasma and lengthens the half-life by 2 times. Concomitant use of ketorol and probenecid is contraindicated.

When combined with opioid analgesics, the doses of the latter can be significantly reduced.

The hypoglycemic effect of insulin and oral hypoglycemic drugs increases.

Co-administration with sodium valproate causes disruption of platelet aggregation.

Ketorol® increases the plasma concentrations of verapamil and nifedipine.

When prescribed with other nephrotoxic drugs, including gold preparations, the risk of developing nephrotoxicity increases.

Drugs that block tubular secretion reduce the clearance of ketorol and increase its concentration in the blood plasma.

Ketorol® slightly reduces the binding of warfarin to proteins. When taken simultaneously with furosemide, ketorol reduces the diuretic effect of furosemide by approximately 20%.

When ketorol is taken simultaneously with lithium preparations, the concentration of lithium in plasma increases due to the inhibition of lithium clearance by the kidneys by some NSAIDs.

When taking ketorol and non-depolarizing muscle relaxants simultaneously, patients experience shortness of breath.

When taken with antiepileptic drugs (phenytoin, carbamazepine), the frequency of attacks increases. When taken simultaneously with psychotropic drugs (fluoxetine, thiotixine, alprazolam), patients experience hallucinations.

Simultaneous administration of pentoxifylline may increase the risk of bleeding.

When used simultaneously with furosemide, ketorol reduces the diuretic effect of furosemide by approximately 20%, so the drug should be prescribed with caution in patients with heart failure.

When used simultaneously with ACE inhibitors, ketorol increases the risk of renal dysfunction.

special instructions

Since NSAIDs reduce platelet aggregation, ketorol should be prescribed with caution to patients with blood coagulation disorders.

Use in patients with impaired liver function

When taking ketorol, it is possible to increase the level of liver transaminases. Ketorol® should be prescribed as a short course of treatment to patients with liver diseases.

Use in patients with impaired renal function

Ketorol® is prescribed to patients with impaired renal function with caution under the supervision of urine tests.

Use in elderly patients

When taking ketorol, adverse reactions in elderly patients are more common; it is necessary to prescribe low doses of the drug. Maximum doses should not exceed 60 mg for patients over 65 years of age.

The drug should be taken at intervals of 6 to 8 hours.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Since patients prescribed ketorol develop side effects from the central nervous system (dizziness, drowsiness) and from the sensory organs (hearing loss, ringing in the ears, blurred vision), it is recommended to avoid performing work that requires increased attention and quick reaction.

Overdose

Symptoms: abdominal pain, nausea, vomiting, peptic ulcer of the stomach and duodenum, erosive gastritis, renal dysfunction, metabolic acidosis.

Treatment: gastric lavage, administration of adsorbents (activated carbon), symptomatic treatment.

Release form and packaging

Ketorol is a drug from the group of non-steroidal anti-inflammatory drugs (NSAIDs) with a predominant analgesic effect. Prescribed for the relief of pain of moderate and high intensity. Ketorol is contraindicated during pregnancy and lactation, in childhood, and in patients with liver and kidney failure.

Dosage form

Ketorol for intramuscular injection is a transparent solution of white or white-yellow color, packaged in 1 ml brown glass ampoules. Ampoules are in blisters of 10 pieces, one blister in a cardboard box.

Description and composition

The active ingredient of the drug is tromethamine (30 mg in 1 ml of solution for injection). The drug has a pronounced analgesic effect and a weak anti-inflammatory, antipyretic, and antiaggregation effect. has an analgesic effect due to the inhibition of prostaglandins in peripheral tissues.

Excipients: propylene glycol, sodium chloride, sodium hydroxide, disodium EDTA, octoxynol, ethyl alcohol 95%, water for injection.

Pharmacological group

Ketorol is a medicinal substance with a predominant analgesic effect. Pharmacological group – NSAIDs. The drug has anti-inflammatory, antipyretic, analgesic effects with a significant predominance of the latter.

Pharmacodynamics

Refers to non-steroidal anti-inflammatory drugs. The anti-inflammatory, antipyretic and analgesic effect develops due to disruption of the synthesis of the enzyme cyclooxygenase, resulting in inhibition of the formation of prostaglandins in peripheral tissues. Prostaglandins are mediators that activate the inflammatory response, affect thermoregulation and increase the sensitivity of pain receptors.

It has a strong analgesic effect comparable to opioid analgesics. At the same time, it does not affect opioid receptors, does not inhibit the respiratory center in the brain, does not disrupt intestinal motility, and does not cause a sedative and anxiolytic (anti-anxiety) effect. The drug does not lead to drug dependence. Ketorol can be prescribed simultaneously with opioid analgesics to relieve high-intensity pain, reducing the dose and the negative effect of narcotic painkillers on the body.

Ketorol has an antiaggregation effect - it reduces the ability of platelets to aggregate (stick together) and slows down the formation of blood clots. This leads to increased bleeding time. After discontinuation of the drug, platelet aggregation ability is restored within 1-2 days.

Pharmacokinetics

When administered intramuscularly, the bioavailability of the drug reaches 90%. The analgesic effect develops 30 minutes after administration, the maximum therapeutic effect is observed after 1-2 hours. metabolized in the liver by conjugation to glucuronic acid. Metabolites of the drug do not have an analgesic effect. The drug is excreted in the urine. The half-life is 5 hours.

Indications for use

For adults

Ketorol is prescribed to relieve pain of any etiology. The drug has an analgesic effect for pain of moderate and high intensity. The drug is used for cancer, including in combination with narcotic analgesics to reduce the daily dose of the latter. prescribed in the postoperative period to reduce pain at the surgical site.

For children

Ketorol is not prescribed in childhood.

Ketorol is not prescribed during pregnancy due to penetration of the drug through the blood vessels of the placenta and toxic effects on the fetus. The drug accumulates in breast milk and can lead to poisoning of the baby. If the drug is used during lactation, it is necessary to temporarily stop breastfeeding.

Contraindications

Before prescribing a drug, it is necessary to take into account contraindications to prevent the development of complications of therapy.

1. Individual intolerance to the components of the drug.
2. History of allergic reaction to NSAIDs.
3. Ulcerative lesions of the stomach and intestines in the acute stage.
4. History of gastric and intestinal bleeding.
5. Hemorrhagic stroke.
6. Coagulopathies.
7. Tendency to bleed.
8. Bronchial asthma.
9. Treatment .
10. Moderate to severe renal failure.
11. Moderate to severe liver failure.
12. Heart failure.
13. Childhood.
14. Pregnancy and lactation period.
15. Preoperative period.

Ketorol is prescribed with caution in the elderly (patients over 65 years of age) due to the frequent development of complications such as bleeding from the digestive tract.

Application and dosage

For adults

To eliminate pain, the minimum effective dose is selected, the duration of use usually does not exceed 5 days. The drug is injected deep into the muscle of the gluteal region.

For patients under 65 years of age, Ketorol is prescribed 10-30 mg once or every 4-6 hours. The maximum dosage is 90 mg/day. For patients over 65 years of age, the drug is prescribed 10-15 mg once or every 4-6 hours. The maximum dosage is 60 mg/day. For high-intensity pain, the drug is administered every 2 hours.

For children

The drug is not used in children.

For pregnant women and during lactation

The drug is not prescribed during pregnancy. During lactation, the drug is administered according to the standard regimen. The child is temporarily transferred to artificial formula.

Side effects

Side effects occur at the beginning of therapy and usually resolve on their own within a few days. The risk of progression of side effects is high in patients with renal and hepatic insufficiency.

1. Pain in the lumbar region, swelling, increased diuresis.
2. Nausea, loose stools, abdominal pain, gastric bleeding.
3. Headache, sleep disturbance, ringing in the ears, anxiety.
4. Decreased visual acuity.
5. Anaphylactic reactions, laryngeal edema.
6. Arterial hypertension.
7. Swelling of the face, tongue, feet.
8. Increased sweating.
9. Fever.

Blood tests show eosinophilia, anemia, and less commonly, leukopenia. If side effects progress, the drug is discontinued.

Interaction with other drugs

The use of Ketorol with lithium increases the risk of toxic effects on the liver and kidneys. Prescribing the drug with other NSAIDs, glucocorticosteroids, calcium supplements, ethanol can provoke the formation of ulcers in the digestive tract and the development of internal bleeding.

Simultaneous use with thrombolytics, indirect anticoagulants, antiplatelet agents reduces blood clotting and can cause bleeding. reduces the therapeutic activity of antihypertensive drugs and diuretics. Prescribing Ketorol with insulin and hypoglycemic drugs enhances the effect of the latter, which requires adjustment of their daily dosage.

Use with opioid analgesics allows you to reduce the daily dose of narcotic substances, which has a positive effect on the general condition of patients. Ketorol should not be mixed in the same syringe with morphine, promethazine, due to the formation of a chemical reaction.

special instructions

For elderly patients (over 65 years of age), patients with liver and kidney failure, Ketorol is prescribed in a dosage of no more than 60 mg/day.

Overdose

When using high doses of the drug (more than 90 mg/day), nausea and abdominal pain appear. Ulcers of the stomach and intestines form, and the risk of bleeding from the digestive tract increases. If an overdose occurs, the stomach is washed, adsorbents and symptomatic drugs are prescribed. Hemodialysis is not effective enough.

Storage conditions

The medicine is stored in a dry place, protected from direct sunlight, at a temperature of +7-+20 degrees. Keep out of the reach of children.

Analogues

Instead of Ketorol injections, the following drugs can be used:

1. is a complete substitute for Ketorol. The drug comes in the form of tablets and injection solution. It is contraindicated in patients under 16 years of age, during pregnancy, childbirth and lactation.
2. Dolak is an Indian drug containing as an active ingredient. The medicine comes in ampoules and tablets. Injections can be given intramuscularly and intravenously. It can be prescribed to children if they are over 16 years old. Dolak is prohibited for pregnant women, women in labor and breastfeeding patients.
3. contains as an active ingredient and is a substitute for Ketorol in the clinical and pharmacological group. The medicine is available in capsules for oral administration, gel and rectal suppositories. The drug should not be prescribed to pregnant patients or during lactation. The gel can be used from 6 years of age, suppositories can be inserted from 15 years of age.
4. Ibuprofen-Hemofarm belongs to the Ketorol substitutes in the therapeutic group. It can be prescribed in effervescent tablets from the age of 6 years as an analgesic, anti-inflammatory and antipyretic agent, in film-coated tablets from the age of 12 years. Ibuprofen-Hemofarm should not be prescribed to pregnant patients and mothers who support breastfeeding.

Drug price

The cost of the medicine is on average 128 rubles. Prices range from 36 to 318 rubles.