Universal reference book for medicines

Active substance: ketorolac

Type: NSAIDs with pronounced analgesic effect


Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

NSAID, a pyrrolizine-carboxylic acid derivative.
It has a pronounced analgesic effect, has also an anti-inflammatory and moderate antipyretic effect. The mechanism of action is associated with oppression of the activity of COX, the main enzyme of arachidonic acid metabolism, which is the precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever.
When ingested absorbed from the gastrointestinal tract.
C max in the blood plasma is achieved after 40-50 minutes both after ingestion and after the / m administration.Eating does not affect absorption. Binding to plasma proteins is more than 99%.
T 1/2 - 4-6 h as after oral administration, and after the / m introduction.

More than 90% of the dose is excreted in the urine, in unchanged form - 60%;
The rest is through the intestines.
In patients with impaired renal function and senile age, the rate of excretion decreases, T 1/2 increases.

For short-term relief of moderate and severe pain of various origins.

Adults with oral administration - 10 mg every 4-6 hours, if necessary - 20 mg 3-4 times / day.

With a / m introduction, a single dose of 10-30 mg, the interval between administrations is 4-6 hours. The maximum duration of application is 2 days.

Maximum doses: for oral or / m administration - 90 mg / day;
for patients with a body weight of up to 50 kg, with violations of kidney function, as well as for people over 65 years - 60 mg / day.
From the cardiovascular system: rarely - bradycardia, changes in blood pressure, palpitations, fainting.

From the digestive system: nausea, abdominal pain, diarrhea;
rarely - constipation, flatulence, a feeling of overflow of the gastrointestinal tract, vomiting, dry mouth, thirst, stomatitis, gastritis, erosive and ulcerative lesions of the digestive tract, impaired liver function.
From the central nervous system and peripheral nervous system: anxiety, headache, drowsiness;
rarely - paresthesia, depression, euphoria, sleep disorders, dizziness, changes in taste, visual impairment, motor disorders.
From the respiratory system: rarely - a violation of breathing, attacks of suffocation.

From the urinary system: rarely - increased frequency of urination, oliguria, polyuria, proteinuria, hematuria, azotemia, acute renal failure.

On the part of the blood coagulation system: rarely - nasal bleeding, anemia, eosinophilia, thrombocytopenia, bleeding from postoperative wounds.

From the metabolism: it is possible to increase sweating, swelling;
rarely - oliguria, an increase in the level of creatinine and / or urea in the blood plasma, hypokalemia, hyponatremia.
Allergic reactions: skin pruritus, hemorrhagic rash;
in isolated cases - exfoliative dermatitis, urticaria, Lyell syndrome, Stevens-Johnson syndrome, anaphylactic shock, bronchospasm, Quincke's edema, myalgia.
Other: fever is possible.

Local reactions: pain at the injection site.

Erosion-ulcerative lesions of the gastrointestinal tract in the acute phase, presence or suspicion of gastrointestinal bleeding and / or craniocerebral hemorrhage, blood clotting disorders in the anamnesis, conditions with a high risk of bleeding or incomplete hemostasis, hemorrhagic diathesis, moderate and severe renal dysfunction ( the content of serum creatinine is more than 50 mg / l), the risk of developing renal failure in hypovolemia and dehydration;
"Aspirin triad", bronchial asthma, nasal polyps, angioedema in history, preventive analgesia before and during operation, children and adolescence under 16, pregnancy, childbirth, lactation, hypersensitivity to ketorolac, acetylsalicylic acid and other NSAIDs .
Contraindicated in pregnancy, during labor and during lactation (breastfeeding).

Ketorolac is contraindicated for use as a means for premedication, supporting anesthesia and for anesthesia in obstetric practice, since under its influence it is possible to increase the duration of the first period of labor.
In addition, ketorolac can inhibit uterine contractility and fetal circulation.
Contraindicated in severe violations of kidney function (serum creatinine content more than 50 mg / l), the risk of developing renal failure with hypovolemia and dehydration.

Use with caution in patients with impaired renal function.

Use with caution in patients with impaired hepatic function.

Contraindicated in children and adolescents under 16 years.

Caetorolac should be used with caution in elderly patients.
the half-life of ketorolac is prolonged, and plasma clearance may decrease. In these patients it is recommended to use ketorolac at doses close to the lower limit of the therapeutic range.
They are used with caution in patients with impaired liver and kidney function, chronic heart failure, arterial hypertension, in patients with erosive and ulcerative gastrointestinal lesions and bleeding from the gastrointestinal tract in anamnesis.

Caetorolac should be used with caution in the postoperative period in cases when particularly careful haemostasis is required (including after resection of the prostate, tonsillectomy, cosmetic surgery), as well as in senile patients.
the half-life of ketorolac is prolonged, and plasma clearance may decrease. In this category of patients it is recommended to use ketorolac in doses close to the lower limit of the therapeutic range. If there are symptoms of liver damage, skin rash, eosinophilia, ketorolac should be discarded. Ketorolac is not indicated for use in chronic pain syndrome.
Impact on the ability to drive vehicles and manage mechanisms

If drowsiness, dizziness, insomnia or depression occur during the treatment with ketorolac, special care must be taken during occupations with potentially dangerous activities requiring increased attention and speed of psychomotor reactions.

With the simultaneous use of ketorolac with other NSAIDs, it is possible to develop additive side effects;
with pentoksifillinom, anticoagulants (including heparin in low doses) - may increase the risk of bleeding; with ACE inhibitors - there may be an increased risk of kidney dysfunction; with probenecid - the concentration of ketorolac in the plasma and its half-life increase; with lithium preparations - it is possible to reduce renal clearance of lithium and increase its concentration in plasma;with furosemide - a decrease in its diuretic effect.
When ketorolac is used, the need for opioid analgesics for analgesia is reduced.

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