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 severe and moderate severity: injuries, toothache, pain in the postoperative period, cancer, myalgia, arthralgia, neuralgia, radiculitis, dislocations, sprains, rheumatic diseases.

Intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Pharmacological effect

Pharmacotherapeutic group: NSAIDs

Pharmacological action

NSAIDs have a pronounced analgesic (pain-relieving) effect, and also have anti-inflammatory and moderate antipyretic effects.

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

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

The strength of the analgesic (pain-relieving) effect is comparable to morphine and significantly superior to other NSAIDs.

After oral administration, the onset of analgesic (pain-relieving) effect is observed after 1 hour, the maximum effect is achieved after 2-3 hours.

After intramuscular administration, the onset of analgesic (pain-relieving) effect is noted after 0.5 hours, the maximum effect is achieved after 1-2 hours.

Pharmacokinetics

Special instructions

When used together with other NSAIDs, fluid retention, cardiac decompensation, and arterial hypertension may occur.

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

The effect on platelet aggregation lasts for 24-48 hours.

Hypovolemia increases the risk of developing adverse reactions from the kidneys.

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

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

In patients with blood coagulation disorders, it is used only with constant monitoring of the platelet count, especially in the postoperative period, which requires careful monitoring of hemostasis.

Impact on the ability to drive vehicles and machinery

Since a significant proportion of patients using ketorolac develop side effects from the central nervous system (drowsiness, dizziness, headache), it is recommended to avoid performing work that requires increased attention and quick reaction (driving vehicles, working with machinery).

Active ingredient

Ketorolac

Composition

1 ml contains:

Active substances:

ketorolac trometamol – 30 mg;

Excipients:

propylene glycol – 200 mg,

disodium phosphate dihydrate (trilon B) – 1 mg,

ethanol 95% – 100 mg,

sodium chloride – 4.35 mg,

1M sodium hydroxide solution – up to pH 6.9-7.9,

water for d/i – up to 1 ml.

Pregnancy

The use of the drug is contraindicated during pregnancy, during childbirth and during breastfeeding.

Contraindications

Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history); urticaria, rhinitis caused by taking NSAIDs (history); intolerance to pyrazolone drugs; dehydration, hypovolemia (regardless of the cause); bleeding or a high risk of developing it; condition after coronary artery bypass surgery; confirmed hyperkalemia; inflammatory bowel diseases; erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, peptic ulcers; hypocoagulation (including hemophilia); severe renal failure (creatinine clearance less than 30 ml/min); severe liver failure or active liver disease; hemorrhagic stroke (confirmed or suspected); hemorrhagic diathesis; hematopoietic disorder; pregnancy; childbirth; lactation period (breastfeeding); children under 16 years of age (efficacy and safety have not been established); hypersensitivity to ketorolac and other NSAIDs.

Not used as a means for premedication, maintenance of anesthesia, pain relief before and during surgical operations (including in obstetric practice) due to the high risk of bleeding.

Not indicated for the treatment of chronic pain.

With caution

bronchial asthma; cholecystitis; chronic heart failure; arterial hypertension; impaired renal function (plasma creatinine below 50 mg/l); cholestasis; active hepatitis; sepsis; systemic lupus erythematosus; old age (over 65 years); polyps of the nasal and nasopharyngeal mucosa, simultaneous use with other NSAIDs; the presence of factors that increase gastrointestinal toxicity: alcoholism, smoking; postoperative period, edema syndrome, coronary artery disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, creatinine clearance less than 60 ml/min, history of ulcerative lesions of the gastrointestinal tract, presence of Helicobacter pylori infection, long-term use of NSAIDs, severe somatic diseases, simultaneous use of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Side Effects

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 – loss of appetite, nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding – abdominal pain, spasm or burning in the epigastric region, melena, vomiting with blood or coffee grounds, nausea, heartburn), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

From the urinary system: rarely – acute renal failure, lower back pain, hematuria, azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased urine volume, nephritis, edema of renal origin.

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

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

From the respiratory system: rarely – bronchospasm, dyspnea, rhinitis, pulmonary edema, laryngeal edema (including shortness of breath, difficulty breathing).

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

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

From the blood coagulation system: rarely – bleeding from a postoperative wound, nosebleeds, rectal bleeding.

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

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

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

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

Interaction

The simultaneous use of ketorolac with acetylsalicylic acid or other NSAIDs, calcium preparations, corticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding.

Co-administration with paracetamol increases nephrotoxicity, and with methotrexate – hepato- and nephrotoxicity.

Co-administration of ketorolac and methotrexate is possible only when using low doses of the latter (monitor the concentration of methotrexate in the blood plasma).

With the use of ketorolac, the clearance of methotrexate and lithium may decrease and the toxicity of these substances may increase.

Co-administration with indirect anticoagulants, 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 used simultaneously with opioid analgesics, the doses of the latter can be significantly reduced, because their effect is enhanced.

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

Co-administration with valproic acid causes disruption of platelet aggregation.

Increases the plasma concentration of verapamil and nifedipine.

When prescribed with other nephrotoxic drugs (including gold preparations), the risk of developing nephrotoxicity increases.

Probenecid and drugs that block tubular secretion reduce the clearance of ketorolac and increase its concentration in the blood plasma.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Pharmaceutically incompatible with tramadol solution and lithium preparations.

Manufacturer

Ozon, Russia