Ketorolac - instructions for use, dose, side effects, contraindications

Acetic acid derivative, a non-selective reversible cyclooxygenase inhibitor, an enzyme that catalyzes the reaction of the conversion of arachidonic acid to prostaglandin H₂, which is the precursor of the remaining prostaglandins, thromboxane_A2 and prostacyclin. Has anti-inflammatory and analgesic, as well as antipyretic effect. It inhibits the aggregation of platelets.

By analgesic effect comparable to morphine, has some α-blocking and anticholinergic activity.

Pharmacokinetics:

After oral administration, up to 100% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 60 minutes, after intramuscular injection - after 30 minutes. The connection with plasma proteins is 99%.

The therapeutic effect develops 30 minutes after ingestion and 10 minutes after parenteral administration. Analgesic effect lasts for 6-8 hours. Equilibrium concentrations of the drug in blood plasma are achieved with regular administration at an interval of 6 hours.Metabolism in the liver by glucuronization or hydroxylation with the formation of p-hydroxycetorolac, the analgesic activity of which is less than 1% of the starting material.

The half-life is 3.5-9.2 hours. Elimination by the kidneys (91%) and feces (9%).

Indications:

It is used for arresting pain syndrome of moderate and strong intensity of various genesis, including in the postoperative period, with oncological diseases, etc.

ICD-10

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R52.2 Another constant pain

Contraindications:

Stomach ulcer and duodenal ulcer, ulcerative colitis, gastritis, severe renal dysfunction, severe cerebral circulatory insufficiency, hypocoagulation (including hemophilia), hemorrhagic stroke, hemorrhagic diathesis, individual intolerance, children's age.

Carefully:

Bronchial asthma, chronic heart failure, cholecystitis, arterial hypertension, sepsis, active hepatitis, systemic lupus erythematosus, age over 65 years, polyps of the nasal mucosa and nasopharynx, incomplete hemostasis.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Intramuscularly deep slowly, once in an amount of 10-60 mg every 4-6 hours. The maximum duration of parenteral administration is 2 days.

Inside of 10 mg every 4-6 hours, with insufficient effectiveness increase the dose to 20 mg 3-4 times a day.

The highest daily dose: 90 mg.

The highest single dose: 60 mg.

Side effects:

Central and peripheral nervous system: dizziness, headache, drowsiness, rarely - aseptic meningitis, depression, hyperactivity, hallucinations, psychosis.

Respiratory system: rhinitis, difficulty breathing, rarely - dyspnea or bronchospasm.

The system of hematopoiesis: leukopenia, anemia, eosinophilia.

The cardiovascular system: increased blood pressure, rarely - pulmonary edema.

Digestive system: gastralgia, diarrhea, flatulence, constipation, vomiting, abdominal pain, hepatitis, melena, heartburn, hepatomegaly, cholestatic jaundice, acute pancreatitis.

Dermatological reactions: skin rash, exfoliative dermatitis, Lyell's syndrome, urticaria, Stephen-Jones syndrome.

Sense organs: hearing loss, visual impairment, tinnitus.

Urinary system: renal failure, hematuria, proteinuria, nephrotic syndrome, hemolytic uremic syndrome, frequent urination.

Allergic reactions.

Overdose:

Increased side effects, metabolic acidosis.

Treatment is symptomatic. Dialysis is ineffective.

Interaction:

Increases the effectiveness of oral hemocoagulants.

With simultaneous use with barbiturates, narcotic analgesics, caffeine, phenothiazine derivatives, diphenhydramine, phenacetin, analgesic effects are enhanced.

Anti-inflammatory effect increases salicylates and metamizol sodium.

With simultaneous application with alendronate, the risk of developing gastropathy increases.

Preparations of garlic, onion and ginkgo biloba can potentiate the antiaggregant effect of ketorolac and increase the risk of hemorrhagic complications.

Special instructions:

Ketorolac is not intended for long-term use, it is not recommended to use the drug for the purpose of premedication and analgesia in obstetrics.

The effect on platelet aggregation lasts for 1-2 days. It is not recommended joint use with paracetamol for more than 5 days.

Patients receiving ketorolac, it is recommended to refrain from driving a car and working with moving machinery.

Instructions

Ketorolac (Ketorolacum)