Ketorol, 10 mg 20 pcs.

Pharmacodynamics

Non-steroidal anti-inflammatory drug (NSAID), has a pronounced analgesic effect, anti-inflammatory and moderate antipyretic effect.

The mechanism of action is related to non-selective inhibition of cyclooxygenase (COX) activity – COX-1 and COX-2, catalyzing formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation and fever.

Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, with analgesic effect due to the [-]S form. By the analgesic effect the drug is comparable with morphine and is much superior to other NSAIDs.

The drug does not affect the opioid receptors, does not inhibit respiration, does not cause drug addiction, has no sedative and anxiolytic effects.

After oral administration the development of analgesic effect is noted in 1 hour.

Pharmacokinetics

When taken orally ketorolac is well and quickly absorbed in the gastrointestinal tract (GIT). The bioavailability of ketorolac is 80-100%, maximum concentration (Cmax) after oral administration of 10 mg is 0.82-1.46 mcg/ml, time to reach maximum concentration (TCmax) is 10-78 min. Fat-rich food decreases the maximum blood concentration of the drug and delays its attainment by one hour. The time of reaching the equilibrium concentration (Css) of the drug in per oral administration of 10 mg 4 times per day is 24 hours and the concentration is 0.39-0.79 mcg/ml. The volume of distribution is 0.15-0.33 l/kg. In patients with renal insufficiency the distribution volume of the drug may increase by 2 times, and the distribution volume of its R-enantiomer – by 20%.

Indications

Severe and moderate pain syndrome: trauma, toothache, postpartum and postoperative pain, cancer, myalgia, arthralgia, neuralgia, sciatica, sprains, sprains, rheumatic diseases.

Active ingredient

Ketorolac

Composition

Each film-coated tablet contains:

Active substance:

ketorolaca tromethamine (ketorolaca tromethamol) – 10 mg;

Auxiliary substances:

microcrystalline cellulose 121 mg,

lactose 15 mg,

corn starch 20 mg,

colloidal silica 4 mg,

magnesium stearate 2 mg,

sodium carboxymethyl starch (type A) 15 mg;

coating:

hypromellose 2.6 mg,

propylene glycol 0.97 mg,

titanium dioxide 0.33 mg,

olive green (quinoline yellow 78%, brilliant blue 22%) 0.1 mg.

How to take, the dosage

In tablet form it is used orally in a single dose of 10 mg. In severe pain syndrome the drug is taken repeatedly in a dose of 10 mg up to 4 times a day, depending on the severity of pain.

The maximum daily dose should not exceed 40 mg. The minimum effective dose should be used.

In per oral administration the duration of the course of treatment should not exceed 5 days.

When the drug is changed from parenteral administration to oral administration the total daily dose of both dosage forms on the day of transfer should not exceed 90 mg for patients aged 16 to 65 and 60 mg for patients aged over 65 or with impaired renal function. At the same time, the dose of the drug in tablets on the day of transfer should not exceed 30 mg.

Interaction

Pharmacokinetic interaction with drugs competing for binding to blood plasma proteins is not excluded.

Caution should be exercised when concomitant use of ketorolac with digoxin, phenytoin, lithium drugs, diuretics, cyclosporine, methotrexate, other NSAIDs, hypotensive and antidiabetic agents.

Special Instructions

Ketorol® has two dosage forms (film-coated tablets and solution for injection). The choice of the drug administration method depends on the severity of the pain syndrome and the condition of the patient. The risk of drug complications development increases in case of the duration of treatment longer than 5 days and increasing of oral drug dose more than 40 mg/day.

It is not recommended to use the preparation simultaneously with other NSAIDs (including cyclooxygenase-2 inhibitors), as well as with probenecid, pentoxifylline, acetylsalicylic acid, lithium salts, anticoagulants (including warfarin and heparin).

When combined with other NSAIDs fluid retention, decompensation of cardiac activity, increased blood pressure may be observed. The effect on platelet aggregation is eliminated after 24-48 hours.

Patients with blood clotting disorders are administered only with continuous monitoring of platelet count, especially important for post-surgical patients who require careful monitoring of hemostasis. Antacids, misoprostol, omeprazole are prescribed to reduce the risk of NSAID gastropathy.

During treatment, caution should be exercised when driving motor transport and engaging in other potentially dangerous activities that require high concentration and quick psychomotor reactions.

Contraindications

• High sensitivity to ketorolac;
• complete or incomplete combination of bronchial asthma, recurrent nasal or paranasal sinus polyposis and intolerance to acetylsalicylic acid and other NSAIDs (including history);
• inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;
• Hemophilia and other blood clotting disorders;
• decompensated heart failure;
• hepatic failure or active liver disease;
• explicit renal failure (creatinine clearance less than 30 ml/min), advanced renal disease, confirmed hyperkalemia;
• period after coronary artery bypass surgery;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• pregnancy, childbirth, lactation;
• children under 16 years of age.

With caution:

. Hypersensitivity to other NSAIDs, bronchial asthma, coronary heart disease, congestive heart failure, edema syndrome, arterial hypertension, cerebrovascular disease, pathological dyslipidemia/hyperlipidemia,renal function disorders (creatinine clearance 30-60 ml/min), diabetes, cholestasis, active hepatitis, sepsis, systemic lupus erythematosus, peripheral arterial disease, smoking, concomitant use with other nonsteroidal anti-inflammatory drugs, older age (over 65 years), anamnestic data about the development of gastrointestinal ulcers, alcohol abuse, severe somatic diseases, concomitant therapy with the following drugs anticoagulants (e.g., warfarin), antiaggregants (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (e.g., prednisolone), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).

Side effects

The frequency of side effects is classified according to the frequency of the case: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports.

Digestive system disorders: Frequent (especially in elderly patients older than 65 years with a history of gastrointestinal erosive ulcerative lesions) – gastralgia, diarrhea; less frequent – stomatitis, flatulence, constipation, vomiting, feeling of stomach overflow; Rarely – nausea, erosive-ulcerative lesions of the gastrointestinal tract (including with perforation and/or bleeding – abdominal pain, epigastric spasm or burning sensation, melena, “coffee grounds” type vomiting, nausea, heartburn and others),
cholestatic jaundice, hepatitis, hepatomegaly, acute pancreatitis.

Urinary system disorders: rare – acute renal failure, lower back pain with or without hematuria and/or azotemia, hemolytic-uremic syndrome (hemolytic anemia, renal failure, thrombocytopenia, purpura), frequent urination, increased or decreased volume of urine, nephritis, edema of renal genesis.

The sensory system: rare – hearing loss, tinnitus, visual impairment (including blurred vision).

Respiratory system: rare – bronchospasm, shortness of breath, rhinitis, pharyngeal edema.

The central nervous system: often – headache, dizziness, somnolence; rarely – aseptic meningitis (fever, severe headache, seizures, neck and/or back stiffness), hyperactivity (mood changes, anxiety), hallucinations, depression, psychosis.

Cardio-vascular system: less frequently – increase in blood pressure, rarely – pulmonary edema, fainting.

Blood organs: rare – anemia, eosinophilia, leukopenia.

The hemostatic system: rare – bleeding from the post-operative wound, nasal bleeding, rectal bleeding.

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

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

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

Overdose

Symptoms:Nausea, vomiting, renal dysfunction, abdominal pain, development of peptic ulcers of the stomach or erosive gastritis, metabolic acidosis.

treatment: gastric lavage, conducting symptomatic therapy. and administration of adsorbents (activated charcoal). Ketorolac is not eliminated sufficiently by dialysis.

Similarities

Dolac, Ketorol, Ketonov, Ketorolac, Ketorolac Rompharm