Ketorolac tablets and injections: instructions for use, price, what the drug is used for

Release form

Ketorolac tablets are white-coated, biconvex. 10 such tablets in contour packaging; 1,2, 5 or 10 packs in a paper pack. 10 such tablets in a polymer jar; one such jar in a pack of paper. 25 of these tablets in contour packaging; 2 or 4 packs in a paper pack.
Ketorolac (i.v., i.m.) in ampoules contains a transparent solution of white-yellow color. 1 or 2 ml of this solution in an ampoule; 5 ampoules in contour packaging, 1 or 2 such packages in a cardboard box. 1 or 2 ml of this solution in an ampoule; 10 such ampoules in a cardboard box.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

It has a strong analgesic effect, moderate antipyretic and anti-inflammatory effect.

They are associated with indiscriminate inhibition of the enzyme cyclooxygenase of the first and second types in peripheral tissues, resulting in inhibition of the synthesis of prostaglandins - mediators of pain, inflammation and thermoregulation.

The drug has no effect on opioid receptors, does not cause addiction, does not depress breathing, and does not have a sedative or anxiolytic effect.

The strength of the analgesic effect is comparable to morphine and superior to other drugs in its group.

After oral administration, the analgesic effect is recorded after one hour, the greatest effect – after one to two hours. After an intramuscular injection, the onset of the analgesic effect is recorded after 30 minutes, the greatest effect – after one to two hours.

Pharmacokinetics

When taken internally and when administered by injection, it is actively absorbed from the intestines and tissues. The maximum concentration in the blood is recorded after 40-50 minutes, both after oral administration and after intramuscular injection. Eating does not affect absorption. Plasma protein binding is about 99%.

The half-life is approximately 6 hours. 90% of the dose is excreted by the kidneys, in its original form - 60%; the remaining amount is excreted through the digestive tract.

Ketorolac, 10 mg, film-coated tablets, 20 pcs.

Ketorolac has a pronounced analgesic effect and also has anti-inflammatory and moderate antipyretic effects.

The mechanism of action is associated with non-selective inhibition of the activity of the enzyme cyclooxygenase 1 and 2, mainly in peripheral tissues, resulting in inhibition of the biosynthesis of prostaglandins - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, and the analgesic effect is due to the [-]S form.

The strength of the analgesic effect is comparable to morphine, significantly superior to other non-steroidal anti-inflammatory drugs.

The drug does not affect opioid receptors, does not depress respiration, does not cause drug dependence, and does not have a sedative or anxiolytic effect. After intramuscular administration, the onset of analgesic effect is noted after 0.5 hours, the maximum effect is achieved after 1-2 hours.

Pharmacokinetics

When taken orally, Ketorolac is well absorbed from the gastrointestinal tract - the maximum concentration (Cmax) in the blood plasma (0.7-1.1 mcg/ml) is achieved 40 minutes after taking a dose of 10 mg on an empty stomach. Food rich in fat reduces the maximum concentration of the drug in the blood and delays its achievement by 1 hour. 99% of the drug binds to blood plasma proteins and with hypoalbuminemia the amount of free substance in the blood increases.

Bioavailability - 80-100%. The time to reach equilibrium concentration (Css) with oral administration is 24 hours when administered 4 times a day (above subtherapeutic) and after oral administration of 10 mg is 0.39-0.79 mcg/ml. The volume of distribution is 0.15-0.33 l/kg.

In patients with renal failure, the volume of distribution of the drug may increase by 2 times, and the volume of distribution of its R-enantiomer by 20%.

Penetrates into breast milk: when the mother takes 10 mg of ketorolac, Cmax in milk is achieved 2 hours after taking the first dose and is 7.3 ng/ml, 2 hours after taking the second dose of ketorolac (when using the drug 4 times a day) it is 7.9 ng/ml. More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites.

The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. It is excreted 91% by the kidneys, 6% through the intestines.

The half-life (T1/2) in patients with normal renal function averages 5.3 hours. T1/2 increases in elderly patients and shortens in young ones. Liver function has no effect on T1/2. In patients with impaired renal function with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l). T1/2 - 10.3-10.8 hours, with more severe renal failure - more than 13.6 hours. Not excreted by hemodialysis.

Indications for use

Moderate to severe pain syndrome :

toothache;
pain of traumatic etiology;
pain in the postoperative and postpartum period;
pain due to cancer ;
dislocations , sprains ;
arthralgia , neuralgia , myalgia , radiculitis ;
rheumatic diseases.

Used for symptomatic therapy, relief of inflammation and pain at the time of use, does not affect the development of the disease.

Contraindications

Combination (complete or incomplete) of bronchial asthma , intolerance to aspirin (or other drugs in this group) and recurrent polyposis of the paranasal sinuses and nose .
Hypersensitivity.
Hypovolemia.
Intolerance pyrazolone drugs .
Exacerbation of erosive and ulcerative diseases of the gastrointestinal tract.
Hypocoagulation , high risk of bleeding.
Severe kidney or liver damage , liver disease.
Condition after coronary artery bypass surgery .
Hyperkalemia.
3rd trimester of pregnancy, childbirth and lactation.
Inflammatory intestinal lesions.
Age less than 16 years.

Use with caution for: bronchial asthma , alcoholism , chronic heart failure, cholecystitis , postoperative period, arterial hypertension , edema syndrome, kidney damage, active hepatitis, cholestasis, systemic lupus erythematosus, sepsis, coronary heart disease, dyslipidemia , cerebrovascular diseases, peripheral damage arteries, diabetes mellitus, ulcerative lesions of the digestive tract in the past, H. pylori infection, prolonged use of other non-steroidal anti-inflammatory drugs , old age, 1st and 2nd trimesters of pregnancy.

Ketorolac (for injection), 30 mg/ml, solution for intramuscular administration, 1 ml, 10 pcs.

Often - more than 3%, less often - 1-3%, rarely - less than 1%.

From the digestive system: often - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach; rarely - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the stool or melena, vomiting with blood or “coffee grounds” type, nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the urinary system: rarely - acute renal failure, lower back pain, hematuria, azotemia, hemolytic uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), increased urination, increased or decreased urine volume, nephritis, edema of renal origin.

From the senses: rarely - hearing loss, ringing in the ears, visual impairment (including blurred visual perception).

From the respiratory system: rarely - bronchospasm or dyspnea, rhinitis, pulmonary edema, laryngeal edema (shortness of breath, difficulty breathing).

From the central nervous system: often - headache, dizziness, drowsiness, rarely - aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis , fainting conditions.

From the cardiovascular system: less often - increased blood pressure.

From the hematopoietic organs: rarely - anemia, eosinophilia, leukopenia.

From the hemostasis system: rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding.

From the skin: less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with or without chills, flushing, thickening or peeling of the skin, enlargement and/or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Local reactions: less often - burning or pain at the injection site.

Allergic reactions: rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, itching of the skin, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

Other: often - swelling (face, legs, ankles, fingers, feet, weight gain); less often - increased sweating; rarely - swelling of the tongue, fever.

Side effects

Reactions from the circulatory system: changes in pressure, bradycardia , rapid heartbeat , fainting.
Reactions from the digestive system: abdominal pain, diarrhea, flatulence, nausea, constipation , vomiting, thirst , gastritis, stomatitis , erosive and ulcerative changes in the digestive tract, liver damage.
Reactions from the nervous system: paresthesia , anxiety, sleep disturbances , drowsiness , depression , visual disturbances, dizziness , movement disorders.
Reactions from the respiratory system: attacks of suffocation.
Reactions from the genitourinary system: oliguria , increased urination, polyuria, proteinuria, hematuria, azotemia, acute renal failure .
Reactions from the hematopoietic system: nosebleeds, anemia , eosinophilia, thrombocytopenia.
Metabolic reactions: edema , hypokalemia , increased creatinine or urea in the blood, hyponatremia.
Allergic reactions: hemorrhagic rash, Stevens-Johnson syndrome , urticaria , Quincke's edema , Lyell's syndrome , anaphylactic shock, bronchospasm, myalgia .
Other reactions: fever .
Local reactions: pain in the injection area.

Instructions for use KETOROLAC

From the digestive system:

often - gastralgia, diarrhea;

less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach;
rarely - loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, blood in the stool or melena, vomiting with blood or “coffee grounds” type, nausea, heartburn, etc.), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the urinary system:

rarely - acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), increased urination, increased or decreased urine volume, nephritis, edema of renal origin.

From the senses:

rarely:

hearing loss, ringing in the ears, visual impairment (including blurred vision).

From the respiratory system:

rarely - bronchospasm or dyspnea, rhinitis, pulmonary edema, laryngeal edema (shortness of breath, difficulty breathing).

From the central nervous system:

often - headache, dizziness, drowsiness; rarely - aseptic meningitis (fever, severe headache, convulsions, stiffness of the neck and/or back muscles), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis, fainting.

From the cardiovascular system:

less often - increased blood pressure.

From the hematopoietic organs:

rarely - anemia, eosinophilia, leukopenia.

From the hemostasis system:

rarely - bleeding from a postoperative wound, nosebleeds, rectal bleeding.

From the skin:

less often - skin rash (including maculopapular rash), purpura, rarely - exfoliative dermatitis (fever with or without chills, flushing, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, malignant exudative erythema (Stevens syndrome -Johnson), toxic epidermal necrolysis (Lyell's syndrome).

Allergic reactions:

rarely - anaphylaxis or anaphylactoid reactions (change in facial skin color, skin rash, urticaria, skin itching, tachypnea or dyspnea, swelling of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

Other:

often - swelling (face, legs, ankles, fingers, feet, weight gain);

less often - increased sweating, rarely - swelling of the tongue, fever.

Instructions for use of Ketorolac (Method and dosage)

Ketorolac tablets instructions for use recommend using them orally. Single dose - 10 mg. The next time you use it, you can take 10 mg up to four times a day; the highest daily dose should not be more than 40 mg. The duration of treatment is up to 5 days.

Ketorolac injections instructions for use recommend that when administered intramuscularly, stick to a single dose of up to 30 mg once every 4-6 hours. The highest dose is 90 mg (three ampoules) per day. The longest duration of use of the drug is up to 2 days.

Interaction

Use with other drugs from the same group (OKPD - non-steroidal anti-inflammatory drugs ), glucocorticosteroids, corticotropin, ethanol, calcium supplements increases the risk of ulceration of the gastrointestinal tract and bleeding from the stomach and intestines.

Co-administration with heparin , coumarin derivatives, thrombolytics ( Streptokinase, Alteplase ), cephalosporins, antiplatelet agents, valproic acid and aspirin increases the risk of bleeding.

Ketorolac weakens the effect of diuretic and antihypertensive drugs.

Use together with methotrexate increases hepato- and nephrotoxicity .

Ketorolac enhances the effect of narcotic analgesics.

Myelotoxic drugs enhance the hematotoxic effect of the drug.

Ketorolac

Hypersensitivity (including to other non-steroidal anti-inflammatory drugs); complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history); erosive and ulcerative lesions of the gastrointestinal tract (GIT)

Side effect

Gastralgia, diarrhea, headache, dizziness, drowsiness, swelling (face, legs, ankles, fingers, feet, weight gain).

Overdose

Symptoms: abdominal pain, nausea, vomiting, peptic ulcers or erosive gastritis, impaired renal function, metabolic acidosis. Treatment: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital functions in the body). Ketorolac is not sufficiently eliminated by hemodialysis.

Interaction with other drugs

The simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium preparations, glucocorticosteroids, ethanol, corticotropin can lead to a significant increase in the risk of adverse reactions, including the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding. The simultaneous use of ketorolac with anticoagulants (including warfarin, heparin), other NSAIDs, pentoxifylline and probenecid is contraindicated. When ketorolac is used simultaneously with other NSAIDs (including cyclooxygenase-2 inhibitors), fluid retention, cardiac decompensation, and increased blood pressure may occur.

Carefully

Bronchial asthma;

the presence of factors that increase gastrointestinal toxicity:

alcoholism, smoking and cholecystitis;
postoperative period;
chronic heart failure;
edema syndrome;
arterial hypertension;
moderate renal failure (creatinine clearance 30-60 ml/min);
cholestasis;
active hepatitis;
sepsis;
systemic lupus erythematosus;
cardiac ischemia;
cerebrovascular diseases;
dyslipidemia/hyperlipidemia;
diabetes;
peripheral arterial disease;
history of ulcerative lesions of the gastrointestinal tract, presence of Helicobacter pylori infection.

*for more details, see the instructions for medical use of the drug Ketorolac RU LP-005016 dated 08/28/2018

special instructions

Before prescribing the drug, it is necessary to find out about the presence of a previous allergy to other non-steroidal anti-inflammatory drugs .

Hypovolemia increases the risk of developing kidney toxicity.

If necessary, Ketorolac can be prescribed with narcotic analgesics . The drug should not be used for premedication or to maintain anesthesia.

Do not use the product simultaneously with paracetamol for more than 5 days.

To reduce the risk of developing gastropathy , misoprostol, antacids, and omeprazole are prescribed simultaneously .

To reduce the risk of side effects, the lowest effective dose should be used for the shortest possible course.

During treatment with the drug, you must be careful when driving.

Ketorolac

The simultaneous use of ketorolac with anticoagulants (including warfarin, heparin), other NSAIDs, pentoxifylline and probenecid is contraindicated.

When ketorolac is used simultaneously with other NSAIDs (including cyclooxygenase-2 inhibitors), fluid retention, cardiac decompensation, and increased blood pressure may occur.

The simultaneous use of ketorolac with indirect anticoagulants, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding.

Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its concentration in the blood plasma and increases its half-life.

The combined use of ketorolac with sodium valproate causes a disorder of platelet aggregation.

When using ketorolac with other nephrotoxic drugs (including gold preparations), the risk of developing nephrotoxicity increases. Combined use with paracetamol increases the nephrotoxicity of ketorolac. Drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in the blood plasma.

The combined use of ketorolac with methotrexate increases the hepato- and nephrotoxicity of methotrexate. The combined use of ketorolac and methotrexate is possible only when using low doses of the latter. The clearance of methotrexate may decrease (it is necessary to monitor the concentration of methotrexate in the blood plasma).

With the use of ketorolac, it is possible to reduce the clearance of lithium, increase its concentration in the blood plasma, and increase the toxic effect of lithium. Simultaneous use with lithium salts is contraindicated.

Ketorolac reduces the effect of antihypertensive and diuretic drugs (the synthesis of prostaglandins in the kidneys is reduced).

Ketorolac enhances the effect of narcotic analgesics. When combined with opioid analgesics, the doses of the latter can be significantly reduced.

Ketorolac enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs, and therefore it is necessary to recalculate the dose of these drugs.

Ketorolac increases the plasma concentrations of verapamil and nifedipine.

Concomitant use of NSAIDs and mifepristone may reduce the effectiveness of mifepristone. NSAIDs are not recommended for use within 8-12 days after using mifepristone.

Concomitant use of NSAIDs and cyclosporine increases the risk of nephrotoxicity.

The simultaneous use of NSAIDs and quinolone antibiotics increases the risk of developing seizures.

Concomitant use of NSAIDs and tacrolimus increases the risk of nephrotoxicity.

Concomitant use of NSAIDs and zidovudine increases the risk of hematological toxicity.

When used simultaneously with digoxin, ketorolac does not interfere with the binding of digoxin to plasma proteins. Therapeutic concentrations of digoxin do not affect the binding of ketorolac to plasma proteins.

Antacids do not affect the absorption of ketorolac.

Myelotoxic drugs increase the manifestations of hematotoxicity of ketorolac.

Analogs

Level 4 ATC code matches:
Voltaren

Rapten

Zerodol

Dickloberl Retard

Dikloberl N 75

Dicloberl

Ketanov

Dolak

Panoxen

Naklofen Duo

Naklofen

Olfen-100

Olfen-75

Neurodiclovit

Nizilat

Fanigan

Aertal

Methindol retard

Ortofen

Ketarolac analogues: Ketanov, Ketorol, Ketonort, Ketorolac-Credofarm and others.

Ketarolac price, where to buy

In Russia, the price of Ketorolac No. 10 ampoules is 99-101 rubles, the price of Ketorolac No. 20 tablets is approximately 18 rubles. In Ukraine, ampoules of drug No. 10 cost 54-75 hryvnia, tablets No. 10 cost 9-25 hryvnia.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine
Online pharmacies in KazakhstanKazakhstan

ZdravCity

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