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

Catad_pgroup NSAIDs

Ketorol for injection - official instructions for use

Registration number:

Trade name of the drug:

Ketorol ®

International non-proprietary 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

Clear, colorless or light yellow solution.

Pharmacotherapeutic group:

non-steroidal anti-inflammatory drug.

ATX code: M01AB15

Pharmacological properties

Pharmacodynamics

Non-steroidal anti-inflammatory drug (NSAID), has a pronounced analgesic effect, has an anti-inflammatory and moderate antipyretic effect. 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, which play an important role in the pathogenesis of pain, inflammation and fever. Ketorolac is a racemic mixture of the [-]S and [+]R enantiomers, with the analgesic effect 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 breathing, does not cause drug dependence, does not have a sedative and anxiolytic effect.

Pharmacokinetics

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

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

The volume of distribution (V d) with intramuscular injection is 0.136-0.214 l / kg, with intravenous injection - 0.166-0.254 l / kg. In patients with renal insufficiency, the volume of distribution of the drug can be doubled, 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 reached 2 hours after the first dose and is 7.3 ng / ml, 2 hours after the second dose of ketorolac (when using the drug 4 times a day) - 7.9 ng/l. About 10% of ketorolac crosses 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 by 91% by the kidneys, 6% - through the intestines.

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

With the introduction of 30 mg of ketorolac intramuscularly, the total clearance is 0.023 l / h / kg (0.019 l / h / kg in elderly patients); in patients with renal insufficiency (at a plasma creatinine concentration of 19-50 mg / l) - 0.015 l / h / kg. With the introduction of 30 mg of ketorolac 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 with injuries, toothache, pain in the postoperative period, with oncological and rheumatic diseases, myalgia, arthralgia, neuralgia, sciatica. It is intended for symptomatic therapy, reducing pain and inflammation at the time of use. It does not affect the progression of the disease.

Contraindications

Hypersensitivity to ketorolac;

Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to 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 disease (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 grafting;

Simultaneous reception 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 the high risk of bleeding;

Pregnancy, childbirth, lactation;

Children under 16 years of age (safety and efficacy not established).

Carefully

Bronchial asthma, coronary heart disease, congestive heart failure, edematous syndrome, arterial hypertension, cerebrovascular diseases, pathological dyslipidemia or hyperlipidemia, impaired renal function (creatinine clearance 30-60 ml/l), diabetes mellitus, cholestasis, sepsis, systemic lupus erythematosus, peripheral arterial disease, smoking, older age (over 65 years), history of gastrointestinal ulceration, alcohol abuse, severe physical illness, concomitant therapy with the following drugs: antiplatelet agents (eg, clopidogrel), oral glucocorticosteroids (eg, prednisolone ), selective serotonin reuptake inhibitors (eg citalopram, fluoxetine, paroxetine, sertraline).

Dosage and administration

Intravenously, intramuscularly.

A solution of the drug Ketorol ® is used in minimally effective doses, selected in accordance with the intensity of pain. If necessary, you can simultaneously prescribe narcotic analgesics in reduced doses.

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

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

Side effect

The frequency of side effects is classified according to 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 individual 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 those with perforation and / or bleeding - abdominal pain, spasm or burning in the epigastric region, melena, coffee grounds vomiting, nausea, heartburn and others), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the urinary system: rarely - acute renal failure, back pain with or without hematuria and / or azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increase or decrease in urine volume, nephritis, edema of renal origin.

From the sense organs: rarely - hearing loss, tinnitus, visual impairment (including blurred vision).

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

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

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

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

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

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

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

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

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

Overdose

Symptoms: abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function, metabolic acidosis.

Treatment: gastric lavage, administration of adsorbents (activated charcoal) and symptomatic therapy (maintenance of vital body functions). Not sufficiently excreted by dialysis.

Interaction with other drugs

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.

Do not use the drug 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, with methotrexate - hepato- and nephrotoxicity. The joint appointment of ketorolac and methotrexate is possible only when using low doses of the latter (to control the concentration of methotrexate in the blood plasma).

Probenecid reduces the plasma clearance and volume of distribution of ketorolac, increases its plasma concentration and increases its half-life. Against the background of the use of ketorolac, a decrease in the clearance of methotrexate and lithium and an increase in the toxicity of these substances are possible. Co-administration with indirect anticoagulants (for example, 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 decreases). 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 a violation of platelet aggregation. Increases plasma concentration of verapamil and nifedipine.

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

It is necessary to take into account possible interactions with the simultaneous administration of ketorolac with cyclosporine, zidovudine, digoxin, tacrolimus, quinolone drugs, selective serotonin reuptake inhibitors, mifepristone.

special instructions

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

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

Hypovolemia increases the risk of nephrotoxic side effects.

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

Do not use the drug in conjunction with NSAIDs (including cyclooxygenase-2 inhibitors), since when taken together with other NSAIDs, fluid retention, cardiac decompensation, and increased blood pressure may occur. The effect on platelet aggregation stops after 24-48 hours.

The drug can change the properties of platelets.

Patients with impaired blood coagulation are prescribed only with constant monitoring of the number of platelets, it is especially important for postoperative patients requiring 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 more than 90 mg / day. To reduce the risk of adverse events, the minimum effective dose should be used in the shortest possible course.

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

Influence of a medicinal product for medical use on the ability to drive vehicles, mechanisms

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

Release form

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

1 ml in class I dark glass ampoules (USP). In the upper part of the ampoule there is a ring and a break point. A label is attached to the ampoule.

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

Storage conditions

In a dry, dark place 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 expiry date stated on the package.

Terms of dispensing from pharmacies

On prescription.

Manufacturer

Dr. Reddy's Laboratories Ltd., India

Production site address

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

Information about complaints and adverse drug reactions should be sent 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

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

pharmachologic effect

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 the inhibition of the cyclooxygenase enzyme, mainly in peripheral tissues, which results in inhibition of the biosynthesis of prostaglandins - modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of the [-]S and [+)P enantiomers, with the analgesic effect 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 and anxiolytic effect, and does not cause drug dependence. Ketorolac inhibits platelet aggregation and increases bleeding time. The functional state of platelets is restored within 24-48 hours after discontinuation of the drug.

Pharmacokinetics

The bioavailability of ketorolac after intramuscular injection ranges from 80% to 100%. The pharmacokinetics of ketorolac under the conditions of prescribing medium therapeutic parenteral doses is a linear function. The equilibrium concentration of the drug in plasma is 50% higher than that determined after a single injection. More than 99% of the drug binds to plasma proteins, resulting in an apparent volume of distribution of less than 0.3 l / kg.

Ketorolac is metabolized mainly with the formation of conjugated forms of glucuronic acid, which are excreted through the kidneys. Metabolites do not have analgesic activity. The half-life of the drug is on average 5 hours.

Indications for use

Short-term relief of moderate and severe pain, mainly in the postoperative period.

Contraindications

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

Peptic ulcer of the stomach 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 coagulation disorders, conditions with a high risk of bleeding, hemorrhagic diathesis, coagulopathy, hemorrhagic stroke, low-dose heparin therapy. Surgical interventions with a high risk of bleeding or the risk of incomplete bleeding.

Moderate and severe renal failure (plasma creatinine more than 50 mg / l), risk of renal failure, hypovolemia, dehydration.

Pregnancy, childbirth and lactation.

Hypersensitivity to ketorolac, aspirin, other NSAIDs or any component of the drug.

Simultaneous use of other NSAIDs (risk of summation of side effects)

Age up to 16 years

Congestive heart failure

The drug is not used for pain relief before and during surgical operations.

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 reduced fertility, and therefore are not recommended for use by women planning pregnancy. The safety of the drug in pregnant women has not been studied. In a study on rats and rabbits at toxic doses, no teratogenic effect was detected. In rats, prolongation of the gestation period and delayed delivery were noted. Due to the known negative effect of NSAIDs on the fetal cardiovascular system (risk of occlusion of the ductus arteriosus), ketorolac is contraindicated in pregnant women. The use of ketorolac during childbirth is not recommended due to the increased risk of bleeding in the mother and child. Ketorolac penetrates into milk, and therefore is not recommended for use during lactation.

Dosage and administration

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

The introduction of the drug several times a day for more than 2 days is not recommended, since in most cases patients do not need longer pain relief therapy, or can be transferred to oral ketorolac. In this case, the duration of the use of ketorolac parenterally and orally should not exceed a total of 5 days.

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

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

Adults: The usual recommended starting 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 is recommended, as well as regular monitoring of the patient's condition to exclude gastrointestinal bleeding. Children: The safety and efficacy of ketorolac in children have not been established and the drug is not recommended for use in children under 16 years of age.

Patients with impaired renal function: the use of ketorolac is contraindicated in patients with severe and moderate renal impairment. In the case of mild renal impairment, the use of Ketorol at a dose of not more than 60 mg / day is acceptable.

If necessary, joint 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 / day. day It is recommended that the patient be transferred to the oral form of the drug as soon as possible.

Side effect

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

Somewhat less often, but more than 1% of patients develop hypertension, pruritus, rash, stomatitis, vomiting, constipation, flatulence, a feeling of heaviness in the abdomen, sweating and hemorrhagic rash. Less than 1% of patients may experience weight loss, fever, asthenia; palpitations, pallor of the 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, dryness of the oral mucosa, 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; the formation of ulcers in the gastric mucosa, gastrointestinal bleeding, perforation of the walls of the organs 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 observe the established dosages and administration regimens, take into account the patient's condition (age, kidney function, the state of the gastrointestinal tract, water-electrolyte metabolism and the hemostasis system), as well as possible drug interactions. with combination therapy.

Overdose

An overdose of ketorolac with a single or repeated use is usually manifested by pain in the abdomen, the occurrence of peptic ulcers of the stomach or erosive gastritis, impaired renal function, hyperventilation, metabolic acidosis, these symptoms are cured after discontinuation of the drug.

Interaction with other drugs

Ketorolac slightly reduces the degree of warfarin protein binding.

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 injection

When combined with furosemide, its diuretic effect may be reduced by approximately 20%.

Probenecid reduces plasma clearance and volume of distribution of ketorolac increases its concentration in blood plasma and increases its half-life. Against the background of the use of ketorolac, a decrease in the clearance of methotrexate and lithium and an increase in the toxicity of these substances are possible.

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

It is possible that concomitant use with ACE inhibitors may increase the risk of impaired renal function.

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

Perhaps the occurrence of hallucinations against the background of the simultaneous administration of ketorolac and psychostimulant drugs (fluoxetine, thiothixene, alprazolam).

Application features

Appointment to patients with impaired liver function: administered with caution. While taking ketorolac, an increase in the level of liver enzymes is possible. In the presence of functional abnormalities in the liver while taking ketorolac, a more severe pathology may develop. If signs of liver pathology are detected, treatment should be discontinued.

Patients with renal insufficiency or a history of kidney disease: Ketorolac is prescribed with caution.

Appointment to elderly patients: since patients of this age group often develop adverse reactions, the minimum effective dose should be used (daily therapeutic dose of not more than 60 mg for patients over 65 years of age).

Precautionary measures

Before the introduction of Ketorolac, hypovolemia and hypoproteinemia should be eliminated, as well as the water and electrolyte balance should be restored.

Delay in the body of fluid, sodium chloride, oliguria, an increase in the concentration of urea nitrogen and plasma creatinine were observed during clinical studies, and therefore, ketorolac should be used with caution in patients with heart failure, arterial hypertension or pathological conditions with similar manifestations.

Since ketorolac has an effect on platelet aggregation, the use in patients with pathology 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.
It is necessary to consult a doctor, and also 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, as a result of which the biosynthesis of prostaglandins, modulators of pain sensitivity, thermoregulation and inflammation, is inhibited. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, with analgesic effects due to the [-]S form. Ketorolac does not affect opioid receptors and respiratory function, does not have a sedative and 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 a withdrawal syndrome after stopping its use.
After oral administration, Ketorolac is rapidly absorbed and completely absorbed in the gastrointestinal tract. The maximum plasma concentration is reached on average 44 minutes after taking 10 mg and is 0.7-1.1 μg / ml.
In patients over 65 years of age the half-life of the end products of ketorolac compared with young healthy volunteers increases to 7 hours (4.3-8.6 hours). The total plasma clearance is reduced to 0.019 l / kg.
The pharmacokinetics of ketorolac after single and multiple use does not change and is linear. Equilibrium concentrations of the drug in blood plasma are achieved with the introduction of the drug 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.
Ketorolac metabolites 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 excretion of ketorolac slows down, which is manifested by a prolongation of the half-life and a decrease in clearance compared with young healthy individuals.
In patients with impaired liver function no changes in the pharmacokinetics of ketorolac were noted, but the time to reach the maximum concentration of the drug in blood plasma and the half-life increase slightly compared to young healthy volunteers.

Indications for use of the drug Ketorol

Elimination of severe and moderate acute pain of various origin and localization:

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

The use of the drug Ketorol

Ketorol is not indicated for the treatment of chronic pain, but is used only in case of acute pain.
With a single oral dose, a single dose is 10 mg.
With repeated administration, the drug is prescribed at 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 total 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 fats 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 the course of treatment for oral administration is no more than 5 days.

Contraindications to the use of the drug Ketorol

Hypersensitivity to ketorolac or other drugs of the NSAID group, 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 ulcers 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 the age of 16.

Side effects of 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 develop during the period of Ketorol use (drowsiness, dizziness, headache), it is recommended to avoid performing work that requires increased attention and a quick response.
The appointment of 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 lactation, the issue of stopping breastfeeding should be resolved.

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 a prolongation of its half-life from the body are noted.
With the combined appointment of methotrexate and Ketorol, 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 administration of Ketorol and salicylates (at a concentration of 300 μg / ml in the blood plasma), the binding of Ketorol to 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 Ketorol with warfarin or heparin, but the appointment 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 fats 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 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 charcoal) and symptomatic therapy is recommended.

Storage conditions of the drug Ketorol

Tablets - in a dry, dark place 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 can be accompanied by acute pain, from which traditional analgesics usually do not save. 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 are its contraindications and side effects?

Operating principle

The active component of Ketorol is ketorolac, which is a derivative of acetic acid. Ketorolac is a relatively new drug that appeared in the late 1980s. However, he quickly won recognition around the world. Currently, ketorolac is used for the symptomatic treatment of various diseases, and is widely used in gynecology, surgery, and 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 the occurrence of pain, inflammation and fever. Ketorol acts mainly in peripheral tissues.

Unlike many other non-steroidal anti-inflammatory drugs (NSAIDs), Ketorol has mainly only an analgesic effect, and its antipyretic and anti-inflammatory effect is relatively weak. The analgesic effect of ketorolac, however, is quite strong and 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 surpasses that of 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 breathing (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, prolongs bleeding time, although these changes do not exceed dangerous limits. However, it is worth remembering this for people who have diseases in which blood clotting is disturbed or severe internal bleeding (for example, hemophilia or stomach ulcers) can be observed.

Release form

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

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

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

Auxiliary substances in the tablet:

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

Auxiliary substances in Ketorol solution:

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

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

Shelf life of tablets and solution - 3 years, gel - 2 years. Tablets and solution for parenteral administration are dispensed by prescription, a prescription is not required for the gel.

Analogues

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

Ketanov,
Adolor,
Dolac,
Dolomin,
Ketalgin,
ketolac,
Ketofril,
Ketokam,
Ketonal (gel only).

Other NSAIDs can also be found in pharmacies, but it should be remembered that most of them differ significantly from Ketorol in terms of the principle of action and indications.

Pharmacokinetics

Ketorol is rapidly absorbed into the blood when taken orally. Food rich in fats reduces the maximum concentration of the drug in the blood and slows down the moment of its onset. Ketorol is able to penetrate into breast milk, partially (about 10% of the drug) penetrates the placental barrier. At the same time, the bioavailability of the drug is about 100%, regardless of the dosage form. Ketorol, when administered parenterally, begins to act faster than when taking tablets. The maximum concentration of the drug in the blood when taking the tablets is observed after 1 hour, and the maximum therapeutic effect occurs a little later and lasts 4-6 hours. With parenteral administration, the maximum concentration depends on the route of administration (intramuscularly or intravenously, as well as on the dose).

The highest concentration in the blood and the time of the highest concentration with intramuscular injection:

Maximum blood concentration and time of maximum concentration when administered intravenously:

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

The half-life in patients with intact 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 increases to 10.3-10.8 hours. With an even lower creatinine clearance, the time is extended to 13.6 hours. Liver function does not affect the half-life.

Indications

Indications for the use of tablets and solution are almost the same. The choice of a particular dosage form is dictated by such considerations as the speed of action and the condition of the patient. The solution is indicated for use where the fastest effect is needed. In addition, sometimes the patient for some reason cannot take 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;
trauma;
sprains and muscle strains;
bruises and inflammation of soft tissues;
ligament damage;
pain in bursitis, tendonitis, epicondylitis, synovitis;
myalgia;
neuralgia;
radiculitis;
arthrosis;
oncological diseases;
headache;
pain in various inflammatory processes;
postoperative pain;
postpartum pain;
wounds;
joint and bone pain;
pain in rheumatism.

Ketorol is more suitable for the relief of severe and moderate pain. For relatively mild pain, other drugs are indicated for use. In addition, Ketorol should not be used for a long time, more than 5 days. And 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 remedy, its reasonable price. However, there are also patients in whom the drug caused adverse reactions, and doctors indicate 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, it is hypersensitivity to the components of the drug. In addition, it should not be given to children under 16 years of age (in the form of tablets and injections). This is due to the fact that when taking the drug, children are more likely to develop side effects, such as nephritis, depression, hearing loss, and pulmonary edema.

Therefore, for parents who want to save their children from the unpleasant symptoms of acute respiratory infections, flu and colds, Ketorol will not work. It is better to use more effective in this case and safe ibuprofen and paracetamol. 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 allowed 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 overcarrying of the fetus or complicating labor. Ketorol during lactation is prohibited in all forms.

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

- bronchospasm and angioedema in history;
- dehydration;
- ulcers and erosion of the gastrointestinal tract;
- reduced blood clotting;
- insufficiency of liver functions;
- hemorrhagic diathesis;
- hemorrhages in the brain in history or at the current time;
- hematopoietic disorders;
- risk of major bleeding;
- decompensated heart failure;
- high concentration of potassium in the blood;

recent coronary artery bypass grafting;

lactose 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;
ischemic heart disease;
arterial hypertension;
stagnation of bile;
hepatitis;
sepsis;
ulcerative diseases of the gastrointestinal tract in history;
concomitant use of anticoagulants and antiplatelet agents, NSAIDs, selective serotonin reuptake inhibitors, corticosteroids;
in old age (over 65 years);
alcoholism;
polyps of the nasal mucosa and nasopharynx;
renal failure (creatinine clearance less than 60 ml / min);
other serious somatic diseases.

Contraindications for use in the form of a gel are:

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

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

Also, you can not use the drug if the patient suffers from intolerance to other NSAIDs, renal failure (creatinine clearance less than 30 ml / min). With creatinine clearance less than 60 ml / min, the dose should be reduced.

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

Side effects

When Ketorol is taken orally, a number of side effects may occur. However, most of them are not life threatening.

The most common side effects are abdominal pain and diarrhea (more than 3% of cases). These side effects are usually observed in older people who have ulcerative lesions of the gastrointestinal tract. Also, a certain 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 can also cause other types of rare side effects:

Body systems that affect effects	effect types
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, decrease or increase in the amount of urine, nephritis
respiratory system	bronchial spasm, rhinitis, respiratory disorders, laryngeal edema
central nervous system	drowsiness, hyperactivity, aseptic meningitis (neck stiffness, severe headaches, convulsions), hallucinations, hearing impairment, tinnitus, visual disturbances, fainting
blood system	anemia, eosinophilia, leukopenia, nosebleeds
allergic and skin reactions	urticaria, 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, eyelid edema, periorbital edema.

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

Skin reactions are more typical when using the drug in the form of a gel. However, when the drug is applied to a significant surface of the body, systemic side effects are not 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, discontinue treatment with the drug and seek medical advice.

Overdose

When using the gel, an overdose is not possible. Although sometimes the gel can get into the oral cavity, for example, from the lips. In this case, the oral cavity must be rinsed, and if the gel enters the stomach, enterosorbents should be taken. Overdose when taking oral tablets can manifest itself in symptoms such as stomach pain, nausea, vomiting, urinary retention, impaired renal function, acidosis. The formation of ulcerative lesions in the stomach may also be observed.

If an overdose occurs, then it is recommended to do standard gastric lavage procedures for such cases, take sorbents, and carry out symptomatic therapy, that is, therapy aimed at maintaining the efficiency of the main body systems. Hemodialysis with an overdose of the drug is usually not performed, since it is ineffective.

Instructions for use

When using Ketorol in the form of tablets, they should be taken as needed, but not more than 4 tablets per day. The maximum dose is 40 mg per day. The course of treatment is 5 days, unless otherwise prescribed by the attending physician. Tablets must be swallowed without chewing and drinking plenty of water. The effectiveness of Ketorol is not related to 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 the irritation of the gastric mucosa. Therefore, the most optimal time for taking is 2 hours after eating.

Ketorol injections

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

The solution is injected deep into the muscle. As an injection site, you should choose the outer upper third of the thigh, shoulder, buttock, or other area of the body where the muscles come close to the skin. For injections, small disposable syringes with a capacity of 0.5-1 ml are suitable. Single dosage - 10-30 mg (0.3-1 ml). The largest single dose for intramuscular injection is 2 ml. A second injection can be done 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 with 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. The time of intravenous jet injection of the solution should not be less than 15 s.

The duration of treatment with the parenteral route of administration should not be more than 5 days. With intravenous administration, the total dose for the entire course of treatment should not exceed 15 ml. For patients with reduced kidney function, the elderly (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 for 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 the form of tablets - 30 mg.

Instructions for intramuscular injections

The syringe and needle should be removed from the package immediately before injection. The syringe draws up 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 in order for the air bubbles to separate from the walls and rise up. To remove air, it is necessary to slightly press the piston so that a drop appears on the needle. After that, the syringe is set aside, and the injection site is treated with an antiseptic. At the injection site, the needle is inserted perpendicularly and for its entire length, and then the contents of the syringe are squeezed out slowly and accurately. After the injection, the injection site is again treated with an antiseptic.

Ketorol infusions

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

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

Instructions for applying the gel (ointment)

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

Squeeze out 1-2 cm of gel from a 30 g tube of gel and apply it evenly on the skin surface. With a large area of the treated surface, you can increase the amount of gel. The ointment must be rubbed several times in a circular motion into the skin until the composition is completely absorbed. The surface of the skin on which the gel has been applied can be covered with a 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 application of the gel should not be less than 4 hours. The course of gel treatment is no more than 10 days. If the desired improvement does not occur or if longer use of the drug is necessary, then you should consult your doctor.

Interaction with other drugs

Interaction with other drugs that compete for binding to blood proteins is not excluded.

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

Do 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 the simultaneous use of the drug with ACE inhibitors - in such a case, a negative effect on the kidneys also appears. Since the drug does not affect the action of narcotic analgesics when used simultaneously with them, the dosage of the latter can be reduced in order to reduce the number of negative effects. Antacids do not affect the absorption of the drug from the gastrointestinal tract. Care must be taken when using with cyclosporine, lithium preparations.

Ketorol in the form of a solution cannot be mixed in the same syringe with some 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 can contribute to the development of bleeding.

Use with antidepressants can lead to the development of hallucinations.

When using the drug 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 the preventive effect of acetylsalicylic acid on platelet aggregation. Therefore, patients taking acetylsalicylic acid preparations as anticoagulants in moderate doses should not refuse them. If there is a risk of gastropathy, proton pump inhibitors and antacids are simultaneously prescribed. Against the background of the use of the drug, it is necessary to control the parameters of hemostasis once a week. Elderly people have a higher risk of side effects, so they should use Ketorol in minimal doses. Patients with renal insufficiency with regular use of the drug should monitor the parameters of the kidneys by passing urine tests. In liver diseases, Ketorol should be used with caution and in short courses.

Due to the risk of developing adverse reactions, the introduction of the first dose of the drug should be carried out under close medical supervision.

Since the drug can often cause side effects such as dizziness and drowsiness, during the course of treatment, driving and performing work requiring concentration should be avoided.

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Based on reviews

Pain can occur suddenly, and its growing strength makes it impossible to fully exist. A universal remedy with 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, in 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, removing swelling of soft tissues. How such a multifaceted effect is achieved, indications and contraindications, as well as adverse reactions of the drug, we will analyze 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 able to provide enough multifaceted impact on the body, namely:

eliminates the focus of inflammation by suppressing the synthesis of enzyme compounds of prostaglandins;
relieves acute symptomatic pain;
has an antipyretic effect.

If we talk about the method of its action at the cellular level, then a favorable result is achieved by inhibiting the synthesis of prostaglandins - enzymes that provoke soreness and swelling when violations of natural life 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 eventually is reduced to a minimum.

Pain relief 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 the help of this drug, you can get rid of various types of pain that differ in pathogenesis and type of manifestation.

Ask your question to a neurologist for free

Irina Martynova. Graduated from the Voronezh State Medical University. N.N. Burdenko. Clinical intern and neurologist of BUZ VO "Moscow polyclinic".

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

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

Ketorol is almost 99% bound to blood albumin, which increases its bioavailability and increases the effectiveness of exposure. He able to penetrate into all tissues and organs, lingering in breast milk and synovial fluid at a maximum concentration ( but does not accumulate like other similar NSAIDs).

In the process of metabolism, about half of the dosage introduced into the body falls on 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 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 those generally accepted. Since ketorolac tromethamine binds directly to blood proteins, its half-life in the elderly increases several times. At the same time, in a young active organism, half-life can occur much longer.

Composition and form of release

Ketorol is produced in the form of tablets coated with a special soluble green coating. The biconvex shape of the tablet facilitates the process of swallowing the medicine. Each tablet has a special embossing in the form of the Latin letter S. Tablets are packaged in 10 pieces in a plastic blister with a metal coating. The package may have a different number of blisters, from which the price of the drug is radically different.

One Ketorol tablet contains:

The active ingredient is ketorolac tromethamine - 10 mg.
Auxiliary components:

lactose;
corn starch;
cellulose microcrystalline;
colloidal silicon dioxide;
sodium carboxymethyl starch;
titanium dioxide;
hypromellose;
natural diamond dye;
propylene glycol.

The composition of the tablets can be changed by the manufacturer, however, the active substance (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 stopping acute attacks of severe pain, it is better to use injections, which are absorbed faster and reduce the soreness of a certain area of the body. In medical practice, the following scheme is widely used: for the first three days, Ketorol is administered deep intramuscularly, after which the treatment is continued with tablets, gradually reducing the dosage to the minimum.

The dosage depends on the age of the person, the intensity of the pain and the nature of the course of the disease.. To eliminate pain of various etiologies and dislocations, the most appropriate dosage is 10 mg - this is 1 tablet of the drug. 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 allowable dose of ketorolac per day is not more than 40 mg(4 tablets). Its excess 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 neuronal endings;
muscle sprains and;
oncological diseases;
relief of pain in the postoperative and rehabilitation period;
traumatism and violation of the integrity of the bone tissue (fractures, pins, squeezing);
muscular neuralgia and myalgia.

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

Contraindications

not used in therapy, when the patient has the presence of the following indicators:

hypersensitivity to one or more components of the drug;
intolerance to acetylsalicylic acid;
the presence of bronchial asthma and nasal sinus polyposis;
violation of hematopoietic functions, especially in the presence of a low level of coagulability;
children's age up to 16 years;
pregnancy and lactation;
the presence of active bleeding in the organs of 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 grafting;
peptic ulcer of the gastrointestinal tract in the acute stage;
renal insufficiency;
stroke or pre-stroke condition;
hypovolemia.

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

Also draw Special attention on the patient's condition when prescribing Ketorol in the case when the history contains the following diseases:

cardiac ischemia;
chronic arterial hypertension;
impaired functioning of the kidneys and the excretory system as a whole;
diabetes mellitus (with mandatory daily use of insulin);
sepsis and skin pustular lesions of various etiologies;
hepatitis in the activation stage;
serious somatic diseases and disorders of the nervous system.

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

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

Overdose

With a significant increase daily allowable dose ( over 100 mg) is noted severe intoxication organism, which is characterized by the following symptoms:

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

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

Remove the remains of tablets from the digestive tract- it is appropriate only if the time interval from the use of tablets to the detection of an overdose does not exceed 1 hour. You can induce a gag reflex by pressing the back of a tablespoon on the root of the tongue.
Reduce the concentration of toxins- any sorbents that are able to envelop and neutralize the activity of toxins will help with this. These include: Activated carbon (1 tablet per 10 kg of human weight), Sorbex, Polysorb, Enterosgel.
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). Water should be at room temperature, but in no case not cold, which will lead to spasm in the digestive tract. For best results, you can make your own saline solution. To do this, for 1 liter of water use:

1 tablespoon of table salt;
1 tablespoon of sugar;
1 teaspoon baking soda.

The resulting mixture of vital salts is drunk for several days, until the residual manifestations of adverse reactions disappear.

Call an ambulance, as well as inform the local therapist about what happened.

An overdose and its symptoms can occur even when a single dose of Ketorol has been drunk, combined with taking other drugs of the NSAID group, or while using intramuscular injections and tablets. 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 by 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 individual intolerance to the components of the drug, or any drugs of the NSAID group;
people with the presence of cancer, as well as destructive processes in the liver.

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

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 of acute symptoms for quite a long time;
lowering blood pressure;
drowsiness;
pain in the epigastric part of the abdomen.

Medium frequency(from 1 to 3% of the total mass):

constipation;
flatulence;
stomatitis;
abrupt increase in blood pressure;
skin rash;
increased sweating.

Rare(up to 1%):

vomiting with blood impurities;
ulceration of the mucous membrane of the digestive tract;
spasm of the stomach;
pain and discomfort, indicating the presence of problems with the kidneys;
decrease in the amount of urine excreted;
severe swelling;

tinnitus;
darkening in the eyes;
loss of consciousness;
convulsions;
sudden mood swings;
bronchospasm;
severe shortness of breath and lack of air;
anemia.

In isolated cases:

nosebleeds;
swelling of the larynx;
rhinitis;
thrombocytopenia;
acute pancreatitis;
hepatitis;
fever.

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

urticaria and pruritus;
swelling of the whole body or its individual parts;
labored breathing;
anaphylaxis;
dry mucous membranes.

When diagnosing allergic reactions, treatment with Ketorol is stopped by carrying out the following set of measures:

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

In the presence of allergic reactions to medications that are indicated in the anamnesis, the patient is recommended to take the first medication in a 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 do not have health complaints and chronic diseases. The occurrence of adverse reactions is directly related to the individual characteristics of the patient, his age and general health and lifestyle.

Since the drug is capable of exerting a whole range of adverse reactions on the body, it is possible to take it only after consulting a doctor. Self-medication can cause the development of new diseases, as well as provoke a fatal outcome.

Interaction with other drugs

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

Combining these drugs with Ketorol provokes profuse bleeding of the gastrointestinal tract and the development of serious complications.

Also Not recommended concomitant use of Ketorol with other non-steroidal anti-inflammatory drugs, since overdoses are likely to occur with the ensuing negative consequences for the body.

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

Paracetamol;

preparations containing a small concentration of gold.

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

If a patient has diabetes, an adjustment in the dose of insulin is necessary, since the drug used can affect the level of glucose in the blood and the process of its splitting.

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

Additionally

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

Treatment with Ketorol in patients who have problems in the circulatory system, implies constant control the state and number of platelets produced, as well as the rate of their sedimentation. The sampling of analyzes is carried out both before taking the tablet and after its absorption. A coagulogram performed at least 2 times a day will avoid serious consequences, as well as predict further treatment.

When Ketorol is used by 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 anticancer drugs is unacceptable, since this can provoke serious violations of kidney function, up to their failure.

Advantages over other drugs

Among the most pronounced benefits of using Ketorol, the following qualities can be distinguished:

It is not able to bind to opioid receptors on cell membranes, which allows it to be used as a safe analgesic drug.
It does not affect the performance of the brain and concentration of attention in any way - it can be used when performing work that requires increased concentration of attention and speed of psychomotor reactions.
Does not have a pronounced sedative effect.
It is not addictive, therefore it can be used in the long-term treatment of chronic diseases accompanied by the presence of acute pain, fever and swelling of soft tissues.
Allowed for violations of liver function, since this does not affect the level of absorption and half-life from the body.
It does not have an anxiolytic effect, allowing the use of the drug in violation of psycho-emotional reactions.
Affordable price and good patient tolerance.

Price

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

Terms of 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 the reach of children. Shelf life - 2 years from the date of manufacture, the exact date of which is indicated on the package.

Analogues

The most accessible and no less effective means similar in effect on the body are the following:

Ketorolac, 10 mg, price for 20 pcs. from 26 rubles
, 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 rubles
Tempalgin, price for 20 pcs. from 115 rubles

Similar drugs have their own contraindications and adverse reactions, so it is important to consult a specialist when choosing them. Self-replacement of Ketorol with an analogue can provoke the development of concomitant negative reactions.

Thus, Ketorol in the form of tablets is able to have the same effects on the body as other drugs of the NSAID group. However, he good tolerance and fast response, which is achieved due to easy absorption and metabolism by the liver. He is quite can be combined with drugs of other drug groups in complex therapy, but it requires hospitalization and constant medical monitoring of the patient's condition. Affordable price and the ability to quickly eliminate any kind of pain makes it so popular and in demand in the pharmacology market.

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