Ketorolac, pills 10mg, 20pcs

Composition

1 tablet contains:

Active ingredient:

ketorolac trometamine-10 mg,

excipients:

milk sugar (lactose),

potato starch,

polyvinylpyrrolidone low molecular weight (povidone),

magnesium stearate,

talc,

collidone CL M;

shell:

oxypropylmethylcellulose or hydroxypropylmethylcellulose (hypromellose), talc, titanium dioxide, polyethylene glycol 4000, propylene glycol.

Pharmacological action

Ketorolac has a pronounced analgesic effect, also has an anti-inflammatory and moderate antipyretic effect.

The mechanism of action is associated with non-selective inhibition of cyclooxygenase 1 and 2 enzyme activity, mainly in peripheral tissues, which results in inhibition of prostaglandin biosynthesis-modulators of pain sensitivity, thermoregulation, and inflammation. Ketorolac is a racemic mixture of [- ] S and [+]R enantiomers, and the analgesic effect is due to the [-]S form.

 The strength of the analgesic effect is comparable to morphine, significantly superior to other nonsteroidal anti-inflammatory drugs.

 The drug does not affect opoid receptors, does not depress respiration, does not cause drug dependence, does not have a sedative and anxiolytic effect. After intramuscular use, the onset of analgesic action is noted in 0.5 hours, the maximum effect is achieved in 1-2 hours

. Pharmacokinetics

 When taken orally, Ketorolac is well absorbed in the gastrointestinal tract – the maximum concentration (Cmax) in blood plasma (0.7-1.1 mcg / ml) is reached 40 minutes after taking a 10 mg dose on an empty stomach. High-fat foods reduce the maximum concentration of the drug in the blood and delay its achievement by 1 hour. 99% of the drug binds to plasma proteins and with hypoalbuminemia, the amount of free substance in the blood increases.

Bioavailability – 80-100%. The time to reach the equilibrium concentration (Ss) with oral use is 24 hours when prescribed 4 times a day (above subtherapeutic) and is after oral use of 10 mg-0.39-0.79 mcg/ml. The volume of distribution is 0.15-0.33 l / kg.

In patients with renal insufficiency, the volume of distribution of the drug may increase by 2 times, 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) – is 7.9 ng/ml. More than 50% of the administered dose is metabolized in the liver to form pharmacologically inactive metabolites.

The main metabolites are glucuronides, which are excreted by the kidneys, and p-hydroxyketorolac. It is excreted by 91% of the kidneys,6% – through the intestines.

 The elimination half-life (T1 / 2) in patients with normal renal function is on average 5.3 hours. T1 / 2 increases in elderly patients and shortens in young patients. Liver function does not affect T1/2.

In patients with impaired renal function at a plasma creatinine concentration of 19-50 mg / l (168-442 mmol/l). T1/2 – 10.3-10.8 with more severe renal insufficiency-more than 13.6 hours. It is not excreted by hemodialysis.

Indications

Severe and moderate pain syndrome:

• injuries,
• toothache,
• postoperative pain,
• cancer,
• myalgia,
• arthralgia,
• neuralgia,
• sciatica,
• dislocations,
• sprains,
• rheumatic diseases.

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

Use during pregnancy and lactation

Ketorolac is contraindicated during pregnancy, breast-feeding and children under 16 years of age.

Contraindications

• erosive and ulcerative lesions of the gastrointestinal tract,
• past bleeding from the gastrointestinal tract,
• “aspirin” asthma,
• hypersensitivity to progesteroid anti-inflammatory drugs,
• severe hepatic and/or renal failure (creatinine clearance less than 30 ml/min),
• hemorrhagic stroke (confirmed or suspected), hemorrhagic diathesis, hematopoiesis disorder.

The drug is not used for pain relief before and during surgical operations due to the high risk of bleeding, as well as for the treatment of chronic pain.

Side effects

Often-more than 3%, less often-1-3%, rarely-less than 1%.

From the digestive system: often (especially in elderly patients over 65 years of age who have a history of erosive and ulcerative lesions of the gastrointestinal tract)-gastralgia, diarrhea; less often-stomatitis, flatulence, constipation, vomiting, feeling of fullness of the stomach; rarely – nausea, erosive and ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding – abdominal pain, spasm or burning in the stomach). epigastric region, blood in the stool or melena, vomiting with blood or like “coffee grounds”, nausea, heartburn, etc. ), cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

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

From the sensory organs: rarely-hearing loss, ringing in the ears, visual impairment (including blurred vision).

From the respiratory system: rarely-bronchospasm or dyspnoea, rhinitis, pulmonary edema, laryngeal edema (shortness of breath, difficulty breathing).

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

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

Hematopoietic disorders: rare-anemia, eosinophilia, leukopenia.

From the side of the hemostatic system: rarely-bleeding from a postoperative wound, nosebleeds, rectal bleeding.

From the skin: less often-skin rash (including maculopapular rash), purpura, rarely-exfoliative dermatitis (fever with or without chills, redness, tightness 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, itchy skin, tachypnea or dyspnea, edema of the eyelids, periorbital edema, shortness of breath, difficulty breathing, heaviness in the chest, wheezing).

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

Interaction

Concomitant use of ketorolac with acetylsalicylic acid or other non-steroidal anti-inflammatory drugs, calcium supplements, glucocorticosteroids, ethanol, corticotropin can lead to the formation of gastrointestinal ulcers and the development of gastrointestinal bleeding.

Co-use with paracetamol increases nephrotoxicity, with methotrexate-hepatotoxicity and nephrotoxicity. Co-use of ketorolac and methotrexate is possible only when using low doses of the latter (monitor the concentration of methotrexate in blood plasma).

When using ketorolac, it is possible to reduce the clearance of methotrexate and lithium and increase the toxicity of these substances. Concomitant use with indirect anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefotetan, and pentoxifylline increases the risk of bleeding.

Reduces the effect of antihypertensive and diuretic drugs (reduces the synthesis of prostaglandins in the kidneys). When combined with opioid analgesics, the doses of the latter can be significantly reduced, as their effect increases. The hypoglycemic effect of insulin and oral hypoglycemic drugs increases (dose recalculation is necessary).

Co-use with valproic acid causes a violation of platelet aggregation. Increases plasma concentrations 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 blood plasma.

The solution for injection should not be mixed in the same syringe with morphine sulfate, promethazine and hydroxyzine because of precipitation.

Pharmacologically incompatible with tramadol solution, lithium preparations. The solution for injection is compatible with 0.9% sodium chloride solution,5% dextrose solution, Ringer’s solution and Ringer’s lactate, Plasmalit solution, as well as with infusion solutions containing aminophylline, lidocaine hydrochloride, dopamine hydrochloride, short-acting human insulin and heparin sodium salt.

How to take it, course of use and dosage

Ketorolac is taken orally, once or repeatedly, depending on the severity of the pain syndrome.

A single dose is 10 mg, with repeated use it is recommended to take 10 mg up to 4 times a day, depending on the severity of pain; the maximum daily dose should not exceed 40 mg.

When taken orally, the duration of the course should not exceed 5 days.

Overdose

Symptoms: abdominal pain, nausea, vomiting, peptic ulcers of the stomach or erosive gastritis, impaired renal function, metabolic acidosis.

Treatment: gastric lavage, use of adsorbents (activated charcoal) and symptomatic therapy (maintenance of vital functions in the body). It is not sufficiently excreted by dialysis.

Special instructions

When combined with other nonsteroidal anti-inflammatory drugs, fluid retention, decompensation of heart activity, and arterial hypertension may occur. The effect on platelet aggregation stops after 24-48 hours.

Hypovolemia increases the risk of adverse reactions from the kidneys. If necessary, it can be prescribed in combination with narcotic analgesics.

Ketorolac is not recommended for use as a premedication agent, maintenance anesthesia and analgesia in obstetric practice.

Do not use simultaneously with paracetamol for more than 5 days. Patients with impaired blood clotting are prescribed the drug only with constant monitoring of the number of platelets, especially in the postoperative period, requiring careful monitoring of hemostasis.

It is recommended to avoid performing work that requires increased attention and quick response (driving vehicles, working with mechanisms, etc. ).

Form of production

Film-coated tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Ketorolac

Conditions of release from pharmacies

By prescription

Dosage form

Tablets