Ketorol instructions for use injections intramuscular composition. Solution for intramuscular and intravenous administration

Catad_pgroup NSAIDs

Ketorol for injection - official instructions by application

Registration number:

Trade name of the drug:

Ketorol ®

International nonproprietary name of the drug:

ketorolac.

Dosage form:

solution for intravenous and intramuscular administration.

Compound

1 ml of solution contains:

active substance: ketorolac tromethamine (ketorolac trometamol) 30 mg;

excipients : octoxynol 0.07 mg, disodium edetate 1 mg, sodium chloride 4.35 mg, ethanol 0.115 ml, propylene glycol 400 mg, sodium hydroxide 0.725 mg, water for injection up to 1 ml.

Description

Transparent, colorless or light yellow solution.

Pharmacotherapeutic group:

non-steroidal anti-inflammatory drug.

ATX code:М01АВ15

Pharmacological properties

Pharmacodynamics

A non-steroidal anti-inflammatory drug (NSAID), has a pronounced analgesic effect, has anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with non-selective inhibition of the activity of cyclooxygenase (COX) - COX-1 and COX-2, which catalyzes the formation of prostaglandins from arachidonic acid who play important role in the pathogenesis of pain, inflammation and fever. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, and the analgesic effect is due to the [-]S form. The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs.

The drug does not affect opioid receptors, does not depress respiration, does not cause drug dependence, and does not have a sedative or anxiolytic effect.

Pharmacokinetics

The pharmacokinetics of ketorolac after single and repeated intravenous and intramuscular administration is linear.

At intramuscular injection absorption is complete and rapid. The maximum concentration of the drug (Cmax) after intramuscular administration of 30 mg is 1.74-3.1 μg/ml, 60 mg is 3.23-5.77 μg/ml, time to reach maximum concentration (T Cmax) is 15-73 min and 30-60 min, respectively. Cmax after intravenous administration of 15 mg – 1.96-2.98 µg/ml, 30 mg – 3.69-5.61 µg/ml, T Cmax – 0.4-1.8 min and 1.1-4 ,7 min, respectively. Communication with plasma proteins – 99%. Time to reach equilibrium drug concentration (Css) at parenteral administration 30 mg 4 times a day – 24 hours; with intramuscular administration, 15 mg – 0.65–1.13 µg/ml, 30 mg – 1.29-2.47 µg/ml.

The volume of distribution (V d) with intramuscular administration is 0.136-0.214 l/kg, with intravenous administration - 0.166-0.254 l/kg. In patients with renal failure the volume of distribution of the drug can double, and the volume of distribution of its R-enantiomer can increase by 20%.

Penetrates into breast milk: when the mother takes 10 mg of ketorolac, Cmax in milk is achieved 2 hours after taking the first dose and is 7.3 ng/ml, 2 hours after taking the second dose of ketorolac (when using the drug 4 times a day) - 7.9 ng/l. About 10% of ketorolac passes through the placenta.

More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys, and the pharmacologically inactive p-hydroxyketorolac. It is excreted 91% by the kidneys, 6% through the intestines.

Half-life (T 1/2) in patients with normal function kidneys – 3.5-9.2 hours after parenteral administration of 30 mg. T1/2 increases in elderly patients and shortens in young ones. Changes in liver function do not affect T1/2. In patients with impaired renal function, with a plasma creatinine concentration of 19-50 mg/l (168-442 µmol/l), T1/2 - 10.3-10.8 hours, with more severe renal failure - more than 13, 6 hours

When ketorolac 30 mg is administered intramuscularly, the total clearance is 0.023 l/h/kg (0.019 l/h/kg in elderly patients); in patients with renal failure (with a plasma creatinine concentration of 19-50 mg/l) – 0.015 l/h/kg. When 30 mg of ketorolac is administered intravenously, the total clearance is 0.03 l/h/kg.

Not excreted by hemodialysis.

Indications for use

Pain syndrome of strong and moderate severity of various origins for injuries, toothache, pain in the postoperative period, for cancer and rheumatic diseases, myalgia, arthralgia, neuralgia, radiculitis. Intended for symptomatic therapy, reducing pain and inflammation at the time of use. Does not affect the progression of the disease.

Contraindications

Hypersensitivity to ketorolac;

Complete or incomplete combination bronchial asthma, recurrent nasal or sinus polyposis and intolerance acetylsalicylic acid and other NSAIDs (including history);

Erosive and ulcerative changes in the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding; cerebrovascular or other bleeding;

Inflammatory bowel diseases (Crohn's disease, ulcerative colitis) in the acute phase;

Hemophilia and other bleeding disorders;

Decompensated heart failure;

Liver failure or active liver disease;

Severe renal failure (creatinine clearance less than 30 ml/min), progressive kidney disease, confirmed hyperkalemia;

Postoperative period after coronary artery bypass surgery;

Concomitant use with probenecid, pentoxifylline, acetylsalicylic acid and other NSAIDs (including cyclooxygenase-2 inhibitors), lithium salts, anticoagulants (including warfarin and heparin);

The drug is not used for prophylactic pain relief before and during major surgical interventions due to high risk bleeding;

Pregnancy, childbirth, lactation;

Children under 16 years of age (safety and effectiveness have not been established).

With caution

Bronchial asthma, ischemic disease heart disease, congestive heart failure, edema syndrome, arterial hypertension, cerebrovascular diseases, pathological dyslipidemia or hyperlipidemia, renal dysfunction (creatinine clearance 30-60 ml/l), diabetes mellitus, cholestasis, sepsis, systemic lupus erythematosus, diseases peripheral arteries, smoking, old age(over 65 years old), anamnestic data on the development of ulcerative lesions gastrointestinal tract, alcohol abuse, severe somatic illnesses, concomitant therapy the following drugs: antiplatelet agents (eg, clopidogrel), oral corticosteroids (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Directions for use and doses

Intravenously, intramuscularly.

A solution of the drug Ketorol ® is used in minimally effective doses, selected according to the intensity of pain. If necessary, narcotic analgesics can be prescribed at the same time in reduced doses.

For parenteral use in patients aged 16 to 64 years with a body weight exceeding 50 kg, no more than 60 mg is administered intramuscularly (including oral administration). Usually - 30 mg every 6 hours; intravenously - 30 mg (no more than 6 doses in 2 days). Intramuscularly, in adult patients weighing less than 50 kg or with chronic renal failure (CRF), a single dose of no more than 30 mg is administered (including oral administration); usually – 15 mg (no more than 8 doses in 2 days); intravenously - no more than 15 mg every 6 hours (no more than 8 doses in 2 days). The maximum daily doses for intramuscular and intravenous administration are 90 mg/day for patients from 16 to 64 years of age with a body weight exceeding 50 kg; adult patients weighing less than 50 kg or with chronic renal failure, as well as elderly patients (over 65 years of age) - for intramuscular and intravenous administration 60 mg. The duration of treatment should not exceed 2 days.

When administered intravenously, the dose must be administered over at least 15 seconds. Intramuscular injection is given slowly, deep into the muscle. The onset of analgesic action is noted after 30 minutes, maximum pain relief occurs after 1-2 hours. The analgesic effect lasts about 4-6 hours.

Side effect

Frequency side effects classified depending on the frequency of occurrence of the case: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including some messages.

From the digestive system: often (especially in elderly patients over 65 years of age with a history of erosive and ulcerative lesions of the gastrointestinal tract) - gastralgia, diarrhea; less often - stomatitis, flatulence, constipation, vomiting, feeling of fullness in the stomach; rarely - nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding - abdominal pain, spasm or burning in the epigastric region, melena, vomiting like “coffee grounds”, nausea, heartburn and others), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the side of urine excretory system: rarely - 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.

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

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

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

From the cardiovascular system: less often – increased blood pressure; rarely – pulmonary edema, fainting.

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

From the hemostasis system: rarely – bleeding from a postoperative wound, nosebleed, rectal bleeding.

From the outside skin: less often – skin rash(including maculopapular rash), purpura; rarely - exfoliative dermatitis (fever with or without chills, redness, thickening or peeling of the skin, swelling and/or tenderness of the tonsils), urticaria, Stevens-Johnson syndrome, Lyell's syndrome.

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

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

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

Overdose

Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesion gastrointestinal tract, renal dysfunction, metabolic acidosis.

Treatment: gastric lavage, administration of adsorbents (activated carbon) and symptomatic therapy (maintaining vital body functions). Not eliminated sufficiently by dialysis.

Interaction with other drugs

The simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, including cyclooxygenase-2 inhibitors, calcium preparations, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers of the gastrointestinal tract and the development of gastrointestinal bleeding.

The drug should not be used simultaneously with other NSAIDs (including cyclooxygenase-2 inhibitors), as well as simultaneously with probenecid, pentoxifylline, acetylsalicylic acid, lithium salts, anticoagulants (including warfarin and heparin). Do not use with paracetamol for more than 2 days. Co-administration with paracetamol increases nephrotoxicity, and with methotrexate - hepato- and nephrotoxicity. Co-administration of ketorolac and methotrexate is possible only when using low doses of the latter (monitor the concentration of methotrexate in the blood plasma).

Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its concentration in the blood plasma and increases its half-life. With the use of ketorolac, the clearance of methotrexate and lithium may decrease and the toxicity of these substances may increase. Simultaneous administration with indirect anticoagulants(eg, warfarin), heparin, thrombolytics, antiplatelet agents, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding. Reduces the effect of antihypertensive and diuretic drugs (the synthesis of prostaglandins in the kidneys is reduced). When combined with narcotic analgesics, the doses of the latter can be significantly reduced.

Antacids do not affect the complete absorption of the drug.

The hypoglycemic effect of insulin and oral hypoglycemic drugs increases (dose recalculation is necessary). Co-administration with valproic acid causes disruption of platelet aggregation. Increases the plasma concentration of verapamil and nifedipine.

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

It is necessary to take into account possible interactions when ketorolac is simultaneously prescribed with cyclosporine, zidovudine, digoxin, tacrolimus, quinolone drugs, selective serotonin reuptake inhibitors, and mifepristone.

Special instructions

Ketorol® has two dosage forms (tablets coated film-coated, and solution for intravenous and intramuscular administration). The choice of method of drug administration depends on the severity of the pain syndrome and the patient’s condition.

Before prescribing the drug, it is necessary to clarify the issue of a previous allergic reaction to the drug or NSAID. Due to the risk of developing allergic reactions The first dose is administered under close medical supervision.

Hypovolemia increases the risk of nephrotoxic adverse reactions.

If necessary, can be prescribed in combination with narcotic analgesics.

The drug should not be used together with NSAIDs (including cyclooxygenase-2 inhibitors), since joint reception with other NSAIDs, fluid retention, cardiac decompensation, and increased blood pressure may occur. The effect on platelet aggregation ceases after 24–48 hours.

The drug may change the properties of platelets.

Patients with blood coagulation disorders are prescribed only with constant monitoring of platelet counts, especially important for postoperative patients who require careful monitoring of hemostasis.

The risk of developing drug complications increases with lengthening of treatment (in patients with chronic pain) and increasing the dose of the drug to more than 90 mg/day. To reduce risk adverse events The minimum effective dose should be used in the shortest possible short course.

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

The influence of a medicinal product for medical use on the ability to drive vehicles and machinery

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

Release form

Solution for intravenous and intramuscular administration, 30 mg/ml.

1 ml in Class I (USP) dark glass ampoules. At the top of the ampoule there is a ring and a breaking point. A label is placed on the ampoule.

10 ampoules with instructions for use are placed in a PVC/aluminum blister.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Do not freeze!

Keep out of the reach of children!

Best before date

Do not use after the expiration date stated on the package.

Conditions for dispensing from pharmacies

According to the recipe.

Manufacturer

Dr. Reddy's Laboratories Ltd., India

Dr. Reddy's Laboratories Ltd., India

Address of production place

Unit-I, Plot No. 137, 138 & 146, S.V.CO-OP, Industrial Estate, Bollaram, Jinnaram Mandal, Medak District, India.

Send information about complaints and adverse drug reactions to:

Representative office of Dr. Reddy's Laboratories Ltd.

each ampoule contains ketorolac tromethamine 30 mg, as well as excipients: ethyl alcohol 95% 0.121 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

Description

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

Pharmacological action

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 enzyme cyclooxygenase mainly in peripheral tissues, the consequence of which is 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, and does not cause drug dependence. 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 intramuscular administration ranges from 80% to 100%. The pharmacokinetics of ketorolac under conditions of mid-therapeutic parenteral doses is a linear function. The equilibrium concentration of the drug in plasma is 50% higher than that determined after a single administration. 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 pain, mainly in the postoperative period.

Contraindications

Bronchial asthma, Full or partial syndrome of nasal polyps, bronchospasm, angioedema in the anamnesis.

Gastric ulcer and duodenum during an exacerbation, as well as a history of ulcers or gastrointestinal bleeding, the presence or suspicion of gastrointestinal or intracranial bleeding. History of blood clotting disorders, conditions with a high risk of bleeding, bleeding diathesis, coagulopathies, hemorrhagic stroke, therapy with heparin in low doses. Surgical interventions with a high risk of bleeding or the risk of incomplete stopping.

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.

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 NSAIDs on cardiovascular system fetus (risk of infection 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.

Directions for use and doses

Ketorol is intended for intramuscular injections, 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 early postoperative period Maybe sharing ketorolac and narcotic analgesics, 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 10-30 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 at a dose of 10-15 mg every 4-6 hours, 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 renal impairment: The use of ketorolac is contraindicated in patients with severe to 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

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, itchy skin, rash, stomatitis, vomiting, constipation, flatulence, 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 hemostasis system), as well as possible drug interactions with combination therapy.

Overdose

Overdose of ketorolac with a single dose or reuse usually manifests itself as abdominal pain, peptic ulcers stomach or erosive gastritis, impaired renal function, hyperventilation, metabolic acidosis, these symptoms are cured after stopping the drug.

Interaction with other drugs

Ketorolac slightly reduces the degree of protein binding of warfarin.

In vitro studies have shown the effect of therapeutic doses of salicylates on the degree of binding of ketorolac to plasma proteins downward from 99.2% to 97.5%.

Ketorol injections

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.

Noted possible interaction ketorolac and non-depolarizing muscle relaxants, leading to the development of apnea.

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

Described rare cases development seizures when ketorolac is combined with anticonvulsants(phenytoin, carbamazepine).

Hallucinations may occur in the background simultaneous administration ketorolac and psychostimulant drugs (fluoxetine, thiothixene, alprazolam).

Features of application

Prescription for patients with impaired liver function: 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.

For patients with renal failure or a history of kidney disease: Ketorolac should be administered with caution.

Prescription for elderly patients: since patients of this age group develop more often adverse reactions, the minimum effective dose (daily dose) should be used therapeutic dose no more than 60 mg for patients over 65 years of age).

Precautions

Before administering ketorolac, hypovolemia and hypoproteinemia should be eliminated, as well as 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. With extreme caution, ketorolac is prescribed simultaneously with anticoagulants.

Self-medication can be harmful to your health.
You should consult your doctor and read the instructions before use.

Ketorolac is an NSAID with pronounced analgesic, antipyretic and anti-inflammatory effects. The mechanism of action is associated with blockade of the COX enzyme 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, with the analgesic effect due to the [-]S-form. Ketorolac does not affect opioid receptors and respiratory function, does not have a sedative or anxiolytic effect, and does not cause drug dependence. Ketorolac also inhibits platelet aggregation. The ability of platelets to aggregate is restored after 24-48 hours. The drug does not cause withdrawal syndrome after stopping its use.
After oral administration, Ketorolac is rapidly absorbed and completely absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is achieved on average 44 minutes after taking 10 mg and is 0.7-1.1 mcg/ml.
In patients over 65 years of age The half-life of ketorolac end products compared to young healthy volunteers increases to 7 hours (4.3-8.6 hours). Total plasma clearance decreases to 0.019 l/kg.
The pharmacokinetics of ketorolac after single and repeated use does not change and is linear. Equilibrium concentrations of the drug in the blood plasma are achieved when the drug is administered every 6 hours throughout the day. The clearance of the drug with repeated use remains constant. Ketorolac is 99% bound to plasma proteins, the degree of binding does not depend on the concentration of the drug in the blood.
Metabolites of ketorolac are excreted from the body by the kidneys, 94% of the administered dose is excreted in the urine, 6% is excreted in the feces.
In patients with impaired renal function the elimination of ketorolac slows down, which is manifested by a prolonged half-life and decreased clearance compared to young healthy individuals.
In patients with liver dysfunction no changes were noted in the pharmacokinetics of ketorolac, but the time to reach the maximum concentration of the drug in the blood plasma and the half-life are slightly increased compared to young healthy volunteers.

Indications for use of the drug Ketorol

Elimination of strong and moderate acute pain of various origins and localizations:

  • early postoperative period, pain relief after gynecological, orthopedic, laparoscopic manipulations, after injuries, burns;
  • elimination of attacks of renal colic, hepatic colic, bone pain due to sickle cell anemia;
  • toothache;
  • acute neuralgia, neuritis, radicular pain, pain with herpes zoster;
  • elimination of migraine attacks.

Use of the drug Ketorol

Ketorol is not indicated for the treatment of chronic pain syndrome, but is used only in cases of acute pain.
For a single oral dose, the single dose is 10 mg.
When repeated use, the drug is prescribed at a dose of 10-30 mg every 4-6 hours, depending on the severity and duration of the pain syndrome. The maximum daily dose should not exceed 120 mg.
When transferring patients from parenteral to oral administration of the drug, the full daily dose of Ketorol should not exceed: for patients under 65 years of age - 120 mg; for patients over 65 years of age and patients with impaired renal function - 60 mg.
Taking Ketorol tablets after a meal rich in fat is accompanied by a decrease in the maximum concentration of ketorolac in the blood plasma and slows down the time to reach it by 1 hour.
The duration of treatment for oral administration is no more than 5 days.

Contraindications to the use of the drug Ketorol

Hypersensitivity to ketorolac or other NSAIDs, allergic reactions to acetylsalicylic acid; so-called aspirin asthma; peptic ulcer of the stomach and duodenum in the active phase, as well as a history of ulcer with perforation or gastrointestinal bleeding; severe renal dysfunction (plasma creatinine level more than 5 mg/100 ml); high risk of postoperative bleeding, incomplete hemostasis; congestive heart failure (water retention in the body is noted); children under 16 years of age.

Side effects of the drug Ketorol

Nausea, dyspepsia, abdominal pain, erosive gastritis, peptic ulcer, drowsiness, anxiety, urticaria, angioedema.

Special instructions for the use of the drug Ketorol

Since adverse reactions from the central nervous system (drowsiness, dizziness, headache) develop during the use of Ketorol, it is recommended to avoid performing work that requires increased attention and quick response.
Prescribing Ketorol during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus and only as prescribed by a doctor.
If it is necessary to prescribe Ketorol during breastfeeding, the issue of stopping breastfeeding should be decided.

Interactions of the drug Ketorol

With the combined use of probenecid and Ketorol, an increase in the concentration of ketorolac in the blood plasma and an extension of its half-life from the body are noted.
When prescribing methotrexate and Ketorol in combination, it should be noted that NSAIDs reduce the clearance of methotrexate and thereby increase its toxicity. Ketorol does not affect the ability of digoxin to bind to plasma proteins. With the combined use of Ketorol and salicylates (at a concentration in the blood plasma of 300 μg/ml), the binding of Ketorol to blood plasma proteins decreases from 99 to 97%.
Warfarin, paracetamol, phenytoin, ibuprofen, naproxen, piroxicam do not affect the binding of ketorolac to plasma proteins.
Clinical trials have not revealed important interactions of Ketorolac with warfarin or heparin, but the administration of Ketorolac and drugs that affect hemostasis, including anticoagulants (warfarin or heparin in low doses - 2500-5000 units 2 times a day) and dextrins may increase the risk of bleeding.
The use of Ketorol tablets after a meal rich in fat may be accompanied by a decrease in the maximum concentration in the blood plasma and a delay in its achievement by 1 hour.
Antacids do not affect the absorption of ketorolac in the gastrointestinal tract.

Ketorol drug overdose, symptoms and treatment

With single or repeated use, it manifests itself as abdominal pain, nausea, vomiting, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, hyperventilation. In these cases, gastric lavage with the introduction of adsorbents (activated carbon) and symptomatic therapy is recommended.

Storage conditions for the drug Ketorol

Tablets - in a dry place, protected from light at a temperature of 15-25 ° C.

List of pharmacies where you can buy Ketorol:

  • Saint Petersburg

Arthrosis, osteochondrosis, trauma, tooth extraction, painful menstruation, inflammatory processes - all these diseases and pathological processes may be accompanied by acute pain, which is usually not relieved by traditional analgesics. However, Ketorol, a powerful pain reliever from the group of non-steroidal anti-inflammatory drugs, can often help in such cases. How effective is this drug, when should it be taken, what contraindications and side effects does it have?

Operating principle

The active component of Ketorol is ketorolac, which is a derivative of acetic acid. Ketorolac – relatively new drug, which appeared in the late 1980s. However, he quickly gained recognition throughout the world. Currently, ketorolac is used for symptomatic therapy various diseases, widely used in gynecology, surgery, ophthalmology.

The mechanism of action of ketorolac is a non-selective effect on a special enzyme - cyclooxygenase, which, in turn, is responsible for the synthesis of prostaglandins from arachidonic acid in the body. It is prostaglandins that are responsible for such phenomena as pain, inflammation and fever. Ketorol acts mainly in peripheral tissues.

Unlike many other non-steroidal anti-inflammatory drugs (NSAIDs), Ketorol mainly has only an analgesic effect, and its antipyretic and anti-inflammatory effect is relatively weak. The analgesic effect of ketorolac, however, is quite strong and is comparable to the analgesic effect of morphine, which is considered in medicine to be a kind of standard among painkillers. The analgesic effect of ketorolac is superior to similar effect all other NSAIDs and is second only to the effect of some narcotic analgesics.

Ketorol does not affect opioid receptors and the central nervous system, does not cause drug dependence, sedative and anxiolytic effects, does not depress respiration (unlike opioid analgesics), does not affect intestinal motility, does not lead to urinary retention, bradycardia, tachycardia or changes in blood pressure.

Ketorol, like almost all other NSAIDs, affects blood clotting and prolongs bleeding time, although these changes do not exceed dangerous limits. However, it is worth remembering this for people who have diseases that impair blood clotting or may cause severe internal bleeding (for example, hemophilia or stomach ulcers).

Release form

Ketorol can be purchased in pharmacies in three main forms. Firstly, these are tablets intended for oral administration. Ketorol tablets are round, biconvex, covered with a green coating, white inside. On one side there is the Latin letter S. Each Ketorol tablet contains 10 mg of active ingredient.

Secondly, this is a solution intended for parenteral (intravenous or intramuscular) administration. The solution is contained in ampoules, and 1 ml of solution contains 30 mg of the active substance.

In addition, there is a 30 g gel for external use. Each tube of gel contains 600 mg of ketorolac. The concentration of the active substance in the gel is 2% (20 mg per 1 g).

Excipients in the tablet:

  • microcrystalline cellulose,
  • lactose monohydrate,
  • corn starch,
  • silicon dioxide,
  • magnesium stearate,
  • hypromellose,
  • titanium dioxide

Excipients in Ketorol solution:

  • octoxynol,
  • disodium edetate,
  • sodium chloride,
  • ethanol,
  • sodium hydroxide,
  • water.

The solution is produced in packs of 10 ampoules, tablets - in packs of 20 pcs. Ketorol is produced by the Indian pharmaceutical company Dr. Reddy's Laboratories.

The shelf life of tablets and solution is 3 years, gel – 2 years. Tablets and solution for parenteral administration are available with a prescription; a prescription is not required for the gel.

Analogues

Structural analogues of the drug, that is, medicines containing ketorolac as an active substance, are:

  • Ketanov,
  • Adolor,
  • Dolak,
  • Dolomin,
  • Ketalgin,
  • Ketolak,
  • Ketofril,
  • Ketokam,
  • Ketonal (gel only).

You can also find other NSAIDs in pharmacies, but it should be remembered that most of them differ significantly from Ketorol in their principle of action and indications.

Pharmacokinetics

Ketorol is quickly absorbed into the blood when taken orally. Fat-rich foods reduce the maximum concentration of the drug in the blood and slow down its onset. Ketorol is able to pass into breast milk, partially (approximately 10% of the drug) penetrates the placental barrier. Moreover, the bioavailability of the drug is about 100%, regardless of the dosage form. When administered parenterally, Ketorol begins to act faster than when taking tablets. The maximum concentration of the drug in the blood when taking tablets is observed after 1 hour, and the maximum healing effect comes a little later and lasts 4-6 hours. When administered parenterally, the maximum concentration depends on the route of administration (intramuscular or intravenous), as well as on the dose.

The highest concentration in the blood and the time of the highest concentration after intramuscular administration:

Maximum concentration in the blood and time of maximum concentration after intravenous administration:

Ketorol is metabolized 50% in the liver. It is excreted from the body mainly by the kidneys (91%) and intestines (6%).

The half-life in patients with unimpaired renal function is on average 5.3 hours. This value is slightly higher for young patients and lower for elderly patients. In patients with impaired renal function (creatinine clearance 19-50 ml/min), the half-life rate increases to 10.3-10.8 hours. With even lower creatinine clearance, the time is extended to 13.6 hours. Liver function does not affect the half-life.

Indications

Indications for use of tablets and solution are almost the same. The choice of a particular dosage form is dictated by considerations such as speed of action and the patient's condition. The solution is indicated for use where it is most needed quick effect. In addition, sometimes the patient for some reason cannot take the pills (unconsciousness, vomiting, stomach ulcers, problems with swallowing). In this case, it is also worth using injections. In all other cases, tablets are indicated for use.

Ketorol is indicated for use, first of all, if it is necessary to get rid of pain of various origins:

  • toothache;
  • injuries;
  • dislocations and muscle strains;
  • bruises and inflammation of soft tissues;
  • ligament damage;
  • pain with bursitis, tendonitis, epicondylitis, synovitis;
  • myalgia;
  • neuralgia;
  • radiculitis;
  • arthrosis;
  • oncological diseases;
  • headaches;
  • pain due to various inflammatory processes;
  • postoperative pain;
  • postpartum pain;
  • wounds;
  • joint and bone pain;
  • pain due to rheumatism.

Ketorol is more suitable for relieving severe and medium degree gravity. For the relatively weak pain other drugs are indicated for use. In addition, Ketorol should not be used long time, over 5 days. This means that for chronic pain it is also necessary to use other drugs.

Reviews

Reviews about the drug are mostly positive. Patients and doctors note the high effectiveness of the product and its reasonable price. However, there are also patients in whom the drug caused adverse reactions, and doctors point out that the drug is not intended for long-term use and cannot be used during pregnancy.

Contraindications

Ketorol has a number of contraindications. First of all, this is hypersensitivity to the components of the drug. In addition, it should not be given to children under 16 years of age (in tablet or injection form). This is due to the fact that when children take the drug, there is a high probability of developing side effects, such as nephritis, depression, hearing impairment, and pulmonary edema.

Therefore, parents who want to save their children from unpleasant symptoms For acute respiratory infections, flu and colds, Ketorol will not work. It is better to use ibuprofen and paracetamol, which are more effective and safe in this case. Adolescents over 16 years of age can use the drug for the same indications as adults.

Ketorol gel can be used from 12 years of age. In addition, Ketorol is prohibited in the form of tablets and injections for pregnant women. In the form of a gel, Ketorol is approved for pregnant women during the 1st and 2nd trimesters. In the third trimester, Ketorol should not be used even in the form of a gel, as this can lead to post-term pregnancy or complications. labor activity. Ketorol during lactation is prohibited in all forms.

Other contraindications when taken in the form of tablets and injections:

    • history of bronchospasms and angioedema;
    • dehydration;
    • ulcers and erosions of the gastrointestinal tract;
    • decreased blood clotting;
    • insufficiency of liver functions;
    • hemorrhagic diathesis;
    • history or current cerebral hemorrhage;
    • hematopoietic disorders;
    • risk of major bleeding;
    • decompensated heart failure;
    • high concentration of potassium in the blood;

recent coronary artery bypass surgery;

  • milk sugar intolerance;
  • acute phases of Crohn's disease, ulcerative colitis.

Ketorol is taken with caution when:

  • bronchial asthma;
  • hypersensitivity to NSAIDs;
  • congestive heart failure;
  • damage to peripheral arteries;
  • systemic lupus erythematosus;
  • coronary heart disease;
  • arterial hypertension;
  • stagnation of bile;
  • hepatitis;
  • sepsis;
  • history of gastrointestinal ulcers;
  • simultaneous use of anticoagulants and antiplatelet agents, NSAIDs, selective inhibitors serotonin reuptake, GCS;
  • in old age (over 65 years old);
  • alcoholism;
  • polyps of the nasal and nasopharyngeal mucosa;
  • renal failure (creatinine clearance less than 60 ml/min);
  • other severe somatic diseases.

Contraindications for use in gel form are:

  • weeping dermatoses,
  • eczema,
  • wounds and abrasions at the site of application,
  • "aspirin" bronchial asthma,
  • third trimester of pregnancy.

The gel is prescribed with caution in old age (over 65 years), in childhood(up to 16 years), with bronchial asthma, during the 1st and 2nd trimester of pregnancy.

Also, the drug should not be used if the patient suffers from intolerance to other NSAIDs or renal failure (creatinine clearance less than 30 ml/min). If creatinine clearance is less than 60 ml/min, the dose should be reduced.

Ketorol should not be used for prophylactic pain relief before operations, as well as in obstetric practice due to possible violations blood clotting.

Side effects

When taking Ketorol orally, a number of side effects. However, most of them are not life-threatening.

The most common side effects are abdominal pain and diarrhea (in more than 3% of cases). These side effects are usually observed in older people who have gastrointestinal ulcers. Also, a number of patients experience swelling (of the face, legs, ankles, fingers, feet), dizziness, and headaches. Less commonly (in 1-3% of cases), side effects such as increased blood pressure, stomatitis, flatulence, vomiting, constipation, and skin reactions may occur.

Ketorol may also cause other types of rare side effects:

Body systems that are affected by effects types of effects
Gastrointestinal tract constipation, flatulence, nausea, hepatitis, pancreatitis (inflammation of the pancreas)
urinary system acute pain in the kidney area, blood in the urine, frequent urination, decreased or increased amount of urine, nephritis
respiratory organs bronchial spasm, rhinitis, breathing problems, laryngeal edema
central nervous system drowsiness, hyperactivity, aseptic meningitis (stiff neck muscles, severe headaches, convulsions), hallucinations, hearing impairment, ringing in the ears, visual disturbances, fainting
blood system anemia, eosinophilia, leukopenia, nosebleeds
allergic and skin reactions hives, anaphylactic shock, maculopapular rash, purpura, exfoliative dermatitis (expressed as fever, redness, thickening or peeling of the skin, swelling or tenderness of the tonsils), urticaria, Lyell-Johnson syndrome, swelling of the eyelids, periorbital edema.

Sometimes there may be an increase in temperature and increased sweating.

Skin reactions are more common when using the drug in gel form. However, when applying the drug to a significant surface of the body, systemic side effects cannot be excluded:

  • ulcerative pathologies of the gastrointestinal tract,
  • heartburn,
  • diarrhea,
  • stomach pain,
  • hematuria,
  • vomit,
  • nausea,
  • fluid retention,
  • anemia,
  • agranulocytosis,
  • leukopenia,
  • thrombopenia.

If any side effects occur, you should interrupt treatment with the drug and seek medical advice.

Overdose

When using the gel, an overdose is impossible. Although sometimes the gel can get into oral cavity, for example, from the lips. In this case, the oral cavity must be rinsed, and if the gel gets into the stomach, enterosorbents should be taken. An overdose when taking tablets orally can manifest itself in symptoms such as stomach pain, nausea, vomiting, urinary retention, renal dysfunction, and acidosis. There may also be formation ulcerative lesions in the stomach.

If an overdose occurs, it is recommended to perform standard gastric lavage procedures for such cases, take sorbents, and symptomatic therapy, that is, therapy aimed at maintaining the performance of the main systems of the body. Hemodialysis in case of an overdose of the drug is usually not carried out, since it is ineffective.

Instructions for use

When using Ketorol in tablet form, they should be taken as needed, but no more than 4 tablets per day. Maximum dose is 40 mg per day. The course of treatment is 5 days, unless otherwise prescribed by the attending physician. The tablets must be swallowed without chewing and washed down sufficient quantity water. The effectiveness of Ketorol is not associated with food intake, however, when taking the drug immediately after a meal, the substance is absorbed into the blood more slowly and the analgesic effect appears later in this case. On the other hand, taking Ketorol before meals increases irritation of the gastric mucosa. Therefore, most optimal time for administration is 2 hours after meals.

Ketorol injections

Injections are preferable if the fastest possible analgesic effect is required, or the patient cannot take pills for any reason.

The solution is injected deep into the muscle. The injection site should be external upper third thighs, shoulder, buttock or other area of ​​the body where the muscles come close to the skin. Small disposable syringes with a capacity of 0.5-1 ml are suitable for injections. Single dosage – 10-30 mg (0.3-1 ml). The largest single dose for intramuscular administration is 2 ml. A second injection can be given after 4-6 hours. No more than 90 mg of ketorolac (3 ml of solution) can be administered per day.

For people over 65 years of age, or weighing less than 50 kg, or having impaired renal function, the maximum single dose should not exceed 15 mg (0.5 ml). The maximum daily dose in this case is 60 mg. The solution must be administered slowly - this reduces the risk of developing negative reactions. IV time jet injection the solution should not be less than 15 s.

The duration of treatment for parenteral administration should not exceed 5 days. When administered intravenously, the total dose for the entire course of treatment should not exceed 15 ml. For patients with reduced renal function, elderly people (over 65 years of age) or patients weighing less than 50 kg, this value is 10 ml.

If necessary, you can switch from the parenteral form of administration to taking tablets within 1 day. In this case, the maximum daily dose of both forms of the drug should not exceed 90 mg, and the dose of the drug in tablet form should not exceed 30 mg.

Instructions for intramuscular injections

The syringe and needle should be removed from the package immediately before injection. Use a syringe to draw the required amount of solution from the ampoule. Then the syringe should be raised with the needle up and tapped in the direction from the piston to the needle. This is necessary so that the air bubbles separate from the walls and rise up. To remove air, you need to lightly press the piston so that a drop appears on the needle. After this, the syringe is put aside and the injection site is treated with an antiseptic. The needle is inserted into the injection site perpendicularly and over its entire length, and then the contents of the syringe are squeezed out slowly and carefully. After the injection, the injection site is again treated with an antiseptic.

Ketorol infusions

Ketorol from an ampoule can be added to a dropper and used together with other saline solutions. Ketorol is compatible with the following solutions:

Physiological
dextrose 5%
lidocaine
dopamine
Ringer
Ringer-Locke
Plasma-lit
aminophylline
short-acting human insulin
heparin

Instructions for applying the gel (ointment)

The gel should be applied to an intact skin surface free of wounds, burns and abrasions. You should also avoid getting the gel in the eyes, mucous membranes of the mouth and nose.
Before applying the gel, the skin should be washed and dried.

From a 30 g tube of gel, squeeze out 1-2 cm of gel and apply it evenly to the surface of the skin. At large area the treated surface, you can increase the amount of gel. The ointment must be rubbed into the skin several times in a circular motion until the composition is completely absorbed. The surface of the skin on which the gel was applied can be covered with cotton or gauze bandage. However, it should not be tightly closed and should allow some air to pass through.

Do not apply the gel to the skin too often. It is enough to do this 4 times a day. In this case, the intervals between episodes of using the gel should not be less than 4 hours. The course of treatment with gel is no more than 10 days. If the desired improvement does not occur or if longer use of the drug is necessary, you should consult your doctor.

Interaction with other drugs

Interaction with other drugs that compete for binding to blood proteins cannot be ruled out.

When used with drugs that have a toxic effect on the kidneys (for example, gold preparations), Ketorol enhances their negative effect. The combination of Ketorol with some antihypertensive drugs may reduce their effect due to a decrease in the production of prostaglandins in the kidneys. At simultaneous use Ketorol with other NSAIDs or steroidal anti-inflammatory drugs, ethyl alcohol the risk of gastric bleeding increases. Use with NSAIDs can lead to fluid retention in the body and increased blood pressure.

You should not use Ketorol simultaneously with paracetamol for more than 5 days, as this increases the risk of developing kidney pathologies. The same can be said about simultaneous use drugs with ACE inhibitors - in this case it also manifests itself negative impact on the kidneys. Since the drug does not affect the effect of narcotic analgesics when used simultaneously with them, the dosage of the latter can be reduced to reduce the amount negative effects. Antacids do not affect the absorption of the drug from the gastrointestinal tract. Caution must be exercised when used with cyclosporine and lithium preparations.

Ketorol in the form of a solution cannot be mixed in the same syringe with certain medications due to drug incompatibility, for example, with morphine and tramadol.

Ketorol increases the effect of insulin and other hypoglycemic drugs, but at the same time reduces the effectiveness of antihypertensive drugs and furosemide, anti-epileptic drugs. Thrombolytic drugs and anticoagulants may promote bleeding.

Use with antidepressants may lead to the development of hallucinations.

If you use the drug simultaneously with all of the above drugs, you should consult your doctor.

Special instructions

Ketorolac affects blood clotting, but this effect is limited in time and lasts no more than 1-2 hours. Ketorol is not able to replace preventive effects acetylsalicylic acid on platelet aggregation. Therefore, patients taking acetylsalicylic acid drugs in moderate doses as anticoagulants should not refuse them. If there is a risk of gastropathy, inhibitor drugs are prescribed simultaneously proton pump, antacids. While using the drug, it is necessary to monitor hemostasis parameters once a week. Elderly people have a higher risk of side effects, so they should use Ketorol minimal doses. Patients with renal failure with regular use of the drug should monitor kidney function parameters by taking urine tests. For liver diseases, Ketorol should be used with caution and in short courses.

Due to the risk of adverse reactions, the first dose of the drug should be administered under close medical supervision.

Since the drug can often cause such side effects symptoms such as dizziness and drowsiness, then during the course of treatment you should avoid driving and performing work that requires concentration.

Average rating

Based on reviews

Pain can occur suddenly, and its increasing strength makes it impossible to fully exist. A universal remedy, which has a pronounced analgesic effect, is the drug Ketorol. In just 15-20 minutes, the first signs of its beneficial effects on the body will become noticeable, during which the pain will gradually begin to subside until it disappears completely.

In addition to pain relief, Ketorol is capable of eliminate the inflammatory process, relieving swelling of soft tissues. How such a multifaceted effect is achieved, indications and contraindications, as well as adverse reactions of the drug will be discussed further.

Pharmacological effects

The drug Ketorol belongs to the group of NSAIDs (non-steroidal anti-inflammatory drugs). Like many other drugs in this group, the drug is capable of providing sufficient multifaceted impact on the body, namely:

  • eliminates the source of inflammation by suppressing the synthesis of prostaglandin enzyme compounds;
  • relieves acute symptomatic pain;
  • has an antipyretic effect.

If we talk about the method of its influence at the cellular level, then a favorable result is achieved by inhibiting the synthesis of prostaglandins - enzymes that provoke pain and swelling when disturbances of natural vital activity appear in a certain area. Absorbed in the gastrointestinal tract, the active components of the drug combine with protein cells, causing non-selective inhibition of the cyclooxygenase cascade, after which the synthesis of prostaglandins slows down and is ultimately minimized.

Analgesic effect comparable in strength with morphine, however, the use of Ketorol is much more efficient and safer. The main active ingredient is ketorolac tromethamine, which can have a therapeutic effect even in minimal dosages. With this medicine you can get rid of various types pain, differing in pathogenesis and type of manifestation.

Ask your question to a neurologist for free

Irina Martynova. Graduated from Voronezh State Medical University named after. N.N. Burdenko. Clinical resident and neurologist of the Moscow Polyclinic.

Oral administration of the drug provides maximum effectiveness due to complete absorption of the active components in the gastrointestinal tract. The maximum concentration in the blood occurs an hour after taking the medicine. She directly depends on the type of food patient. Predominant in the diet fatty foods(mainly of animal origin) helps slow down the absorption process for several hours. The half-life and formation of active metabolites occurs within 3-5 hours.

Analgesic and antipyretic effects occur immediately after the first dose of the drug, in 25-50 minutes, depending on the dosage. Ketorol is used both to eliminate symptomatic pain and to full treatment serious illnesses, which are characterized by the addition of fever and swelling.

Ketorol binds to blood albumin by almost 99%, which increases its bioavailability and increases its effectiveness. He capable of penetrating all tissues and organs lingering in breast milk And synovial fluid at maximum concentration ( but does not accumulate like others similar drugs NSAIDs).

During metabolism, about half of the dosage introduced into the body is inactive metabolites. The second half (glucuronides and hydroxyketorolac) has a direct effect on the synthesis of prostaglandins, acting locally and selectively.

After active metabolism in the liver, the drug is largely excreted by the kidneys along with urine. A small proportion of Ketorol is excreted from the body through the intestines. In patients with liver problems, the half-life and maximum concentration of the drug may have individual indicators that differ from the generally accepted ones. Since ketorolac tromethamine binds directly to blood proteins, its half-life increases several times in older people. Moreover, in a young active organism, the half-life can occur much longer.

Composition and release form

Ketorol is produced in the form of tablets coated with a special soluble green coating. The biconvex shape of the tablet makes it easier to swallow the medicine. Each tablet has a special embossing in the form of the Latin letter S. The tablets are packaged in 10 pieces in a plastic blister with a metal coating. The package may contain a different number of blisters, which makes the price of the drug radically different.

One Ketorol tablet contains:

  1. Active ingredient – ​​ketorolac tromethamine – 10 mg.
  2. Auxiliary components:
  • lactose;
  • cornstarch;
  • microcrystalline cellulose;
  • colloidal silicon dioxide;
  • sodium carboxymethyl starch;
  • titanium dioxide;
  • hypromellose;
  • natural diamond dye;
  • propylene glycol.

The composition of the tablets may be changed by the manufacturer, but the active ingredient (ketorolac tromethamine) remains unchanged, maintaining the generally accepted dosage of 10 mg.

Application

Ketorol tablets are used in cases where the intensity of pain does not have a life-threatening effect. When docking acute attacks severe pain it's better to use injections, which are absorbed faster and reduce pain in a specific area of ​​the body. Widely used in medical practice next diagram: for the first three days, Ketorol is administered deeply intramuscularly, after which treatment is continued with tablets, gradually reducing the dosage to the minimum.

The dosage depends on the person’s age, the intensity of the pain and the nature of the disease.. To eliminate pain of various etiologies and dislocations, the most suitable dosage is 10 mg - this is 1 tablet of medication. If the pain is severe, the dose can be increased to 20 mg (2 tablets). When prescribing Ketorol as a course, its duration, as well as the dosage, is determined individually.

The maximum permissible dose of ketorolac per day is no more than 40 mg(4 tablets). Exceeding it leads to the development of a number of side effects that can affect the course of the disease, complicating it with additional painful and uncomfortable sensations in the body.

Indications for use drugs of the NSAID group can become the following manifestations:

  • rheumatoid diseases of the musculoskeletal system
  • , toothache;

  • caused by compression of neuron endings;
  • muscle strains and;
  • oncological diseases;
  • relief of pain in the postoperative and rehabilitation period;
  • traumatism and violation of the integrity of bone tissue (fractures, punctures, compression);
  • muscle neuralgia and myalgia.

Typically, the course of treatment with Ketorol is up to 5 days, but in most cases one dose of medication is enough to get rid of severe pain. His don't use in childhood ( up to 16 years old), limited to taking other NSAIDs to relieve fever, fever and inflammation. If necessary long-term use the drug, take a break every 12 days, after which the administration is continued.

Contraindications

not used in therapy, when the patient has presence of the following indicators:
  • hypersensitivity to one or more components of the drug;
  • intolerance to acetylsalicylic acid;
  • the presence of bronchial asthma and sinus polyposis;
  • dysfunction of hematopoiesis, especially in the presence of a low level of coagulation;
  • children under 16 years of age;
  • pregnancy and lactation period;
  • the presence of active bleeding in the gastrointestinal tract;
  • chronic inflammatory processes of the stomach and intestines, which are in the acute stage;


  • hemorrhagic diathesis;
  • lactose intolerance;
  • decompensated heart failure;
  • rehabilitation period after coronary artery bypass surgery;
  • peptic ulcer of the gastrointestinal tract in the acute stage;
  • renal failure;
  • stroke or pre-stroke condition;
  • hypovolemia.

With caution the drug is used if the patient has predisposition to edema and cerebrovascular bleeding.

Also pay special attention on the patient’s condition when prescribing Ketorol in the case where the anamnesis contains the following diseases:

  • coronary heart disease;
  • chronic arterial hypertension;
  • dysfunction of the kidneys and excretory system as a whole;
  • diabetes mellitus (with mandatory daily use of insulin);
  • sepsis and skin pustular lesions of various etiologies;
  • hepatitis in the active stage;
  • serious somatic diseases and nervous system disorders.

It is not recommended to combine the drug with alcohol, since the latter can provoke severe intoxication of the body. If a person has alcohol addiction, its treatment is carried out only in a hospital, after carrying out cleansing droppers and enemas.

When using Ketorol, it is important to limit or completely stop taking other NSAIDs, since the increased concentration active component may cause intoxication, which will lead to the development of side effects.

Overdose

With significant increasing daily permissible dose ( more than 100 mg) is noted severe intoxication organism, which is characterized by the following symptoms:


  • nausea and vomiting;
  • pain in the abdomen;
  • bleeding in the gastrointestinal tract (blood in stool and vomit);
  • dizziness;
  • apathy;
  • cramps and muscle spasms;
  • coldness and sweating of the extremities;
  • disorders of brain activity;
  • slurred speech.

If an overdose is detected, it is necessary to carry out a set of measures aimed at restoring vital functions:

  1. Remove the remaining tablets from the gastrointestinal tract– is appropriate only when the time interval from the use of tablets to the detection of an overdose does not exceed 1 hour. You can call gag reflex by pressing the back of a tablespoon onto the root of the tongue.
  2. Reduce the concentration of toxins– any sorbents that can envelop and neutralize the activity of toxins will help with this. These include: Activated carbon(1 tablet per 10 kg of person’s weight), Sorbex, Polysorb, Enterosgel.
  3. Ensure water-salt balance– achieved by drinking plenty of water, at least 2-3 liters. You need to drink in small sips, but very often (every 2-3 minutes). The water should be at room temperature, but in no case cold, which will lead to spasms in the gastrointestinal tract. To achieve best result can be done saline solution on one's own. To do this, for 1 liter of water use:
  • 1 tablespoon table salt;
  • 1 tablespoon sugar;
  • 1 teaspoon baking soda.

The resulting mixture is vital important salts drink for several days until residual manifestations of adverse reactions disappear.

Call an ambulance medical care , and also inform the local therapist about what happened.

Overdose and its symptoms can appear even when a single dose of Ketorol was taken, combined with other NSAID drugs, or when intramuscular injections and tablets were used simultaneously. Therefore, before starting treatment, the instructions should be carefully studied, and the total doses of NSAIDs entering the body per day should be compared.

Side effects

At risk according to the likelihood of adverse reactions fall:

  • people over 65 years of age with a history of chronic liver disease, as well as peptic ulcer of the gastrointestinal tract;
  • people who have an individual intolerance to the components of the drug, or any drugs from the NSAID group;
  • people with cancer, as well as destructive processes in the liver.

Side effects provoked by Ketorol can be considered taking into account the frequency of occurrence:

  1. Frequent(more than 3% of all cases):

  • diarrhea;
  • heartburn;
  • increased painful urination;
  • swelling of the soft tissues of the face and limbs;
  • headache with persistence acute symptoms for quite a long time;
  • decreased blood pressure;
  • drowsiness;
  • pain in the epigastric abdomen.
  1. Mid frequency(from 1 to 3% of the total mass):
  • constipation;
  • flatulence;
  • stomatitis;
  • sudden increase in blood pressure;
  • skin rash;
  • increased sweating.
  1. Rare(up to 1%):
  • vomiting with blood;
  • ulceration of the mucous membrane of the gastrointestinal tract;
  • stomach spasm;
  • pain and discomfort, indicating the presence of kidney problems;
  • decreased volume of urine excreted;
  • severe swelling;
  • tinnitus;
  • darkening of the eyes;
  • loss of consciousness;
  • convulsions;
  • sudden mood swings;
  • bronchospasm;
  • severe shortness of breath and lack of air;
  • anemia.
  1. In isolated cases:
  • nosebleeds;
  • swelling of the larynx;
  • rhinitis;
  • thrombocytopenia;
  • acute pancreatitis;
  • hepatitis;
  • fever.

In case individual intolerance drug an allergic reaction may develop, which is manifested by the following reactions:

  • urticaria and skin itching;
  • swelling of the whole body or its individual parts;
  • difficulty breathing;
  • anaphylaxis;
  • dry mucous membranes.

When allergic reactions are diagnosed, treatment with Ketorol is stopped using the following set of measures:

  1. Give a person any antihistamine: Suprastin, Diazolin, Finistil.
  2. Provide plenty of fluids.
  3. Call an ambulance.

If there are allergic reactions to medications that are indicated in the anamnesis, the patient is recommended to take the first medication in the hospital, using 1/8 of the daily dosage. In the absence of adverse reactions, the dose is gradually adjusted to the generally accepted dose.

Usually in medical practice Ketorol is well tolerated patients who have no health complaints and chronic diseases. The occurrence of adverse reactions is directly related to individual characteristics patient, his age and general condition health and lifestyle.

Since the drug is capable of causing a whole range of adverse reactions on the body, its use is possible only after consultation with a doctor. Self-medication can cause the development of new diseases and also cause death.

Interaction with other drugs


  • Acetylsalicylic acid;
  • Corticotropins;
  • Calcium-containing vitamin complexes;
  • Ethanol.

The combination of these drugs with Ketorol provokes heavy bleeding of the gastrointestinal tract, as well as the development of serious complications.

Also not recommended simultaneous use of Ketorol with other non-steroidal anti-inflammatory drugs, since overdoses with resulting negative consequences for the body.

The development of nephrotoxicity, as well as serious dysfunction of the excretory system, is achieved through the simultaneous use of Ketorol with the following drugs:

Decreased prostaglandin synthesis has a direct effect on drugs of the diuretic group, reducing their activity. Also efficiency decreases antihypertensive drugs , when their use is combined with Ketorol.

If a patient has diabetes mellitus, the insulin dose needs to be adjusted, since the drug used can affect the level of glucose in the blood and the process of its breakdown.

Simultaneous use Ketorola with Verapamil and Nefidipine, leads to an increase in the concentration of the latter several times. This property is widely used in the treatment of neuralgia and myalgia, when it is necessary to achieve sedative and muscle relaxant effect.

Additionally

Not recommended use the drug as anesthesia for minor surgical interventions, since there is a high probability of bleeding. Not effective during treatment pain syndrome who wears chronic nature.

Treatment with Ketorol for patients who have problems at work circulatory system , implies constant monitoring the state and quantity of platelets produced, as well as their sedimentation rate. Tests are taken both before taking the pill and after it is absorbed. A coagulogram performed at least 2 times a day will help avoid serious consequences, as well as predict further treatment.

When using Ketorol in patients with oncological diseases, it is possible to combine it in small doses opium-containing preparations, since the concentration of the latter will double. However, the combination of Ketolor and antitumor drugs is unacceptable, since this can cause serious impairment of kidney function, including kidney failure.

Advantages over other drugs

Among the most pronounced advantages of using Ketorol, the following qualities can be highlighted:

  1. It is not able to bind to opioid receptors of cell membranes, which allows it to be used as a safe pain reliever.
  2. It does not affect brain performance or concentration in any way - it can be used when performing work that requires increased concentration and speed of psychomotor reactions.
  3. Does not have a pronounced sedative effect.
  4. It is not addictive, so it can be used for long-term treatment chronic diseases accompanied by acute pain, fever and swelling of soft tissues.
  5. Allowed for liver dysfunction, since this does not affect the level of absorption and half-life from the body.
  6. It does not have an anxiolytic effect, allowing the drug to be used for disorders of psycho-emotional reactions.
  7. Affordable price and well tolerated by patients.

Price

Indian Ketorol, containing 2 blisters with 20 tablets in a package, costs 43 rubles. The domestic drug will cost the buyer a little less - 35 rubles. Prices may differ slightly from pharmacy prices, since they completely depend not only on the manufacturer, but also on the markup percentage of pharmacies.

Conditions for dispensing from pharmacies

The drug is available by prescription because it has a pronounced analgesic effect.

Storage conditions and expiration dates

The drug is stored in a cool, dry place out of reach of children. Shelf life is 2 years from the date of manufacture, the exact date of which is indicated on the packaging.

Analogues

The most accessible and no less effective means of similar effects on the body are the following:


  • Ketorolac, 10 mg, price for 20 pcs. from 26 rub.
  • , 10 mg, price for 10 pcs. from 58 rub.
  • Ketotifen, 1 mg, price for 30 pcs. from 70 rub.
  • Ketofril, 10 mg, price for 20 pcs. from 88 rub.
  • Pentalgin, price for 24 pcs. from 141 rub.
  • Tempalgin, price for 20 pcs. from 115 rub.

Similar drugs have their own contraindications and side effects, so when choosing them it is important to consult a specialist. Independent replacement of Ketorol with an analogue may provoke the development of associated negative reactions.

Thus, Ketorol in tablet form can have the same effects on the body as other drugs in the NSAID group. However, he is well tolerated and quick to respond, which is achieved through easy absorption and metabolism by the liver. He's quite can be combined with drugs from other drug groups in complex therapy, but at the same time requires hospitalization and constant medical control for the patient's condition. An affordable price and the ability to quickly eliminate any type of pain make it so popular and in demand in the pharmacological market.



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