Ketorolac, 30 mg/ml 1 ml 10 pcs

Pharmacotherapeutic group: NSAIDs

Pharmacological action

NSAIDs, has pronounced analgesic (analgesic) effect, also has anti-inflammatory and moderate antipyretic effect.

The mechanism of action is related to non-selective inhibition of COX-1 and COX-2 enzymes activity, mainly in peripheral tissues, which results in inhibition of prostanglandin biosynthesis – modulators of pain sensitivity, inflammation and thermoregulation. Ketorolac is a racemic mixture of R(+) and S(-)-enantiomers, where the analgesic (analgesic) effect is due to the S(-)-enantiomer.

Ketorolac does not affect opioid receptors, does not suppress breathing, is not addictive and has no sedative or anxiolytic effects.

The analgesic (analgesic) effect is comparable to morphine and is significantly superior to other NSAIDs.

After oral administration, the onset of analgesic (analgesic) effect is noted in 1 hour respectively, the maximum effect is achieved after 2-3 hours.

After intravenous administration the onset of analgesic (analgesic) effect is noted after 0.5 h, the maximum effect is achieved after 1-2 h.

Pharmacokinetics

Indications

Pain syndrome of strong and moderate severity: trauma, toothache, pain in the postoperative period, cancer, myalgia, arthralgia, neuralgia, sciatica, sprains, sprains, rheumatic diseases.

It is intended for symptomatic therapy, to reduce pain and inflammation at the time of use, has no effect on the progression of the disease.

Active ingredient

Composition

How to take, the dosage

Ketorolac should be used orally once or repeatedly depending on the severity of the pain syndrome. A single dose is 10 mg; when repeatedly administered, it is recommended to take 10 mg up to 4 times per day, depending on the severity of the pain. The maximum daily dose should not exceed 40 mg. If taken orally, the duration of the course should not exceed 5 days.

In case of intravenous or intravenous administration, depending on the patient’s age and the severity of the pain syndrome, the single dose can vary from 10 mg to 60 mg. The frequency and duration of administration is determined individually.

The maximum daily dose with intravenous and intravenous administration for adults under 65 years of age and children over 16 years is 90 mg; for elderly patients over 65 years of age or with impaired renal function – 60 mg.

Continuous intravenous infusion should not last more than 24 hours.

If parenteral administration, the duration of treatment should not exceed 5 days.

When changing from parenteral administration to oral administration, the total daily dose of ketorolac in both dosage forms on the day of transfer should not exceed: 90 mg for adults under 65 years of age and children over 16 years and 60 mg for elderly patients over 65 years or with impaired renal function. At the same time, the dose of ketorolac for oral administration on the day of transfer should not exceed 30 mg.

Interaction

Concomitant use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium preparations, GCS, ethanol, corticotropin may lead to the formation of GI ulcers and development of gastrointestinal bleeding.

The co-administration with paracetamol increases nephrotoxicity, with methotrexate – hepatotoxicity and nephrotoxicity.

The co-administration of ketorolac and methotrexate is possible only with the use of low doses of the latter (monitor the plasma concentration of methotrexate).

The use of ketorolac may decrease clearance of methotrexate and lithium and increase their toxicity.

The simultaneous use with indirect anticoagulants, heparin, thrombolytics, antiaggregants, cefoperazone, cefotetan and pentoxifylline increases the risk of bleeding.

Reduces the effect of hypotensive and diuretic drugs (reduces the synthesis of prostaglandins in the kidneys).

In concomitant use with opioid analgesics, the doses of the latter may be significantly reduced because their effects are enhanced.

When used concomitantly, it increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (recalculation of the dose is necessary).

The co-administration with valproic acid causes impairment of platelet aggregation.

Enhances plasma concentrations of verapamil and nifedipine.

When administered with other nephrotoxic drugs (including gold drugs) the risk of nephrotoxicity increases.

Probenecid and drugs that block tubular secretion decrease clearance of ketorolac and increase its plasma concentrations.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Pharmaceutically incompatible with tramadol solution, lithium preparations.

Special Instructions

When combined with other NSAIDs, fluid retention, cardiac decompensation, and arterial hypertension may be observed.

Antacids, misoprostol, omeprazole are prescribed to reduce the risk of NSAID gastropathies.

The effect on platelet aggregation persists for 24-48 h.

Hypovolemia increases the risk of adverse reactions from the kidneys.

If necessary, it may be prescribed in combination with opioid analgesics.

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

In patients with clotting disorders, use only with continuous monitoring of platelet counts, especially in the postoperative period, requiring close monitoring of hemostasis.

Impact on driving and operating machinery

Because a significant number of patients develop CNS side effects when using ketorolac (drowsiness, dizziness, headache), it is recommended to avoid performing work requiring increased attention and quick reaction (driving, operating machinery).

Contraindications

The complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, and intolerance to acetylsalicylic acid or other NSAIDs (including a history of history); urticaria, rhinitis, caused by taking NSAIDs (history); intolerance to pyrazolone drugs; dehydration, hypovolemia (regardless of the cause); bleeding or high risk of bleeding; condition after coronary artery bypass grafting; confirmed hyperkalemia; inflammatory bowel diseases; acute gastrointestinal erosive and ulcerative lesions, peptic ulcers; hypocoagulation (incl.including hemophilia; severe renal insufficiency (CKG

Side effects

Gastrointestinal system: often (especially in elderly patients over 65 years with a history of gastrointestinal erosive ulcers) – gastralgia, diarrhea; less frequently – stomatitis, flatulence, constipation, vomiting, feeling of fullness of the stomach; rarely – decreased appetite, nausea, erosive ulcers of the GI tract (including perforation and/or bleeding – abdominal pain, spasm or burning of the epigastric region, melena, vomiting blood or “coffee grounds” type.including with perforation and/or bleeding – abdominal pain, epigastric spasm or burning, melena, vomiting with blood or “coffee grounds” type, nausea, heartburn), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

Urinary system disorders: rare – acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), increased frequency of urination, increased or decreased volume of urine, nephritis, edema of renal genesis.

Nervous system disorders: often – headache, dizziness, somnolence; rarely – aseptic meningitis (including fever, severe headache, cramps, neck and/or back stiffness), hyperactivity (including mood changes, anxiety), hallucinations, depression, psychosis.

Cardiovascular system: less frequently – increase in BP; rarely – fainting.

Respiratory system disorders: rarely – bronchospasm, dyspnea, rhinitis, pulmonary edema, laryngeal edema (including shortness of breath, difficulty in breathing).

Senses: rarely – hearing loss, tinnitus, visual impairment (including blurred vision).

Hematopoietic system: rarely – anemia, eosinophilia, leukopenia.

With the blood coagulation system: rarely – bleeding from the postoperative wound, nasal bleeding, rectal bleeding.

Skin disorders: less frequently – skin rash (including maculopapular), purpura; rarely – exfoliative dermatitis (including fever with/without chills, redness, thickening or peeling of the skin, swelling and/or pain of the palatine tonsils), urticaria, Stevens-Johnson syndrome, Lyell syndrome.

Allergic reactions: rarely – anaphylaxis or anaphylactoid reactions (including changes in complexion, skin rash, urticaria, skin itching, tachypnea or dyspnea, eyelid edema, periorbital edema, shortness of breath, difficulty in breathing, heaviness in the chest, wheezing).

Local reactions: less frequently, burning or pain at the injection site.

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

Pregnancy use

Similarities