Ketokam pills 10 mg 20 pcs.

Composition

• Active ingredient: ketorolac trometamine 10.00 mg.
• Auxiliary substances: microcrystalline cellulose 150.50 mg, corn starch (dried) 56.00 mg, magnesium stearate 1.00 mg, colloidal silicon dioxide 2.00 mg.

Shell composition: universal shell* 8.00 mg.

* – composition of the universal shell: hypromellose, titanium dioxide, polyethylene glycol, talc.

Pharmacological action

Ketocam 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 COX activity, and COX 2, which catalyzes the formation of PG from arachidonic acid, which play an important role in the pathogenesis of pain, inflammation, and fever. The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs. After intravenous administration and oral administration, the onset of analgesic action is noted in 0.5 and 1 h, respectively, the maximum effect is achieved in 1-2 hours and 2-3 hours. Pharmacokinetics: Absorption by mouth is rapid, bioavailability is 80-100%; with intravenous administration – complete and rapid. Cmax after oral administration of 10 mg -0.82-1.46 mcg / ml, TSmax-10-78 min; after intravenous administration of 30 mg, Cmax – 1.74-3.1 mcg/ml,60 mg-3.23-5.77 mcg/ml, TSmax-15-73 min and 30-60 min, respectively; Cmax after intravenous infusion of 15 mg-1.96-2.98 mcg/ ml,30 mg-3.69-5.61 mcg/ml. Binding to plasma proteins is 99%. The time to achieve Css with parenteral and oral administration is 24 hours when prescribed 4 times a day (above subtherapeutic) and amounts to 15 mg – 0.65-1.13 mcg/ml,30 mg – 1.29-2.47 mcg/ml, with an intravenous infusion of 15 mg-0.79-1.39 mcg / ml,30 mg-1.68-2.76 mcg/ml; after oral administration 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, the 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) – 7.9 ng/l. 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. T 1/2 in patients with normal renal function – an average of 5.3 hours (3.5-9.2 hours after i. m. administration of 30 mg,4-7.9 hours after i. v. administration of 30 mg and 2.4-9 hours after oral administration of 10 mg). T 1/2 increases in elderly patients and is shortened in young patients. Liver function does not affect T 1/2. In patients with impaired renal function at a plasma creatinine concentration of 19-50 mg / l (168-442 mmol/l).1/2 – 10.3-10.8 Total clearance is 30 mg – 0.023 l/h/kg (0.019 l/h/kg in elderly patients),30 mg – 0.03 l/h/kg by intravenous infusion,10 mg – 0.025 l/h/kg by oral administration; in patients with renal insufficiency, plasma creatinine concentrations are 19-50 mg/l,30 mg – 0.015 l/h/kg by intravenous administration,30 mg – 0.015 l/h/kg by oral administration. oral administration of 10 mg – 0.016 l/h/kg. It is not excreted by hemodialysis.

Indications

Severe and moderate pain syndrome: pain in the postpartum and postoperative period, injuries, toothache, cancer, myalgia, arthralgia, neuralgia, sciatica, dislocations, sprains, rheumatic diseases.

Contraindications

Hypersensitivity, hypovolemia (regardless of the cause), erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, hypocoagulation (including hemophilia), bleeding or a high risk of their development, severe renal failure (plasma creatinine above 50 mg/l), liver failure, “aspirin” triad (a combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to ASA and Drugs of the pyrazolone series), the period of labor, lactation, children’s age (up to 16 years-safety and efficacy have not been established). With caution. Hypersensitivity to other NSAIDs, bronchial asthma, presence of factors that increase gastrointestinal toxicity: alcoholism, tobacco smoking and cholecystitis; postoperative period, CHF, edematous syndrome, arterial hypertension, impaired renal function (plasma creatinine below 50 mg / l), cholestasis, active hepatitis, sepsis, SLE, concomitant use with other NSAIDs, elderly (over 65 years), pregnancy.

Side effects

Respiratory system disorders: rarely-respiratory disorders, suffocation attacks.

From the urinary system: rarely – frequent urination, oliguria, polyuria, proteinuria, hematuria, azotemia, acute renal failure.

From the side of the blood coagulation system: rarely-nosebleeds, anemia, eosinophilia, thrombocytopenia, bleeding from postoperative wounds.

From the cardiovascular system: rarely – bradycardia, changes in blood pressure, palpitations, fainting.

From the digestive system: nausea, abdominal pain, diarrhea are possible; rarely-constipation, flatulence, a feeling of fullness of the gastrointestinal tract, vomiting, dry mouth, thirst, stomatitis, gastritis, erosive and ulcerative lesions of the gastrointestinal tract, liver function disorders.

From the central nervous system and peripheral nervous system: anxiety, headache, drowsiness are possible; rarely-paresthesia, depression, euphoria, sleep disorders, dizziness, changes in taste sensations, visual disturbances, motor disorders.

From the side of metabolism: possible increased sweating, edema; rarely-oliguria, increased creatinine and / or urea levels in blood plasma, hypokalemia, hyponatremia.

Allergic reactions: possible skin pruritus, hemorrhagic rash; in isolated cases-exfoliative dermatitis, urticaria, Lyell’s syndrome, Stevens-Johnson syndrome, anaphylactic shock, bronchospasm, angioedema, myalgia.

Other services: possible fever.

Local reactions: pain at the injection site.

Interaction

Concomitant use of ketorolac with other NSAIDs may cause additive side effects; with pentoxifylline, anticoagulants (including low – dose heparin) – may increase the risk of bleeding; with ACE inhibitors – may increase the risk of developing impaired renal function; with probenecid – increase the concentration of ketorolac in plasma and its half – life; with lithium preparations-may decrease the renal clearance of lithium and increase its concentration in plasma; with furosemide-reduction of its diuretic effect.

When using ketorolac, the need for opioid analgesics for pain relief is reduced.

How to take, course of administration and dosage

Adults with oral administration – 10 mg every 4-6 hours, if necessary – 20 mg 3-4 times/day.

With intravenous administration, a single dose is 10-30 mg, the interval between injections is 4-6 hours. The maximum duration of application is 2 days.

Maximum doses: when taken orally or intramuscularly – 90 mg / day; for patients with a body weight of up to 50 kg, with impaired renal function, as well as for persons over 65 years of age – 60 mg/day.

Special instructions

It is used with caution in patients with impaired liver and kidney function, chronic heart failure, arterial hypertension, in patients with erosive and ulcerative lesions of the gastrointestinal tract and a history of bleeding from the gastrointestinal tract.

Ketorolac should be used with caution in the postoperative period in cases where particularly careful hemostasis is required (including after prostate resection, tonsillectomy, cosmetic surgery), as well as in senile patients, since the half-life of ketorolac is prolonged, and plasma clearance may decrease. In this category of patients, it is recommended to use ketorolac in doses close to the lower limit of the therapeutic range. If symptoms of liver damage, skin rash, or eosinophilia occur, ketorolac should be discontinued. Ketorolac is not indicated for use in chronic pain syndrome.

Influence on the ability to drive motor vehicles and manage mechanisms

If drowsiness, dizziness, insomnia or depression occur during ketorolac treatment, special care should be taken when engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions.

Form of production

Pills.

Active ingredient

Ketorolac

Conditions of release from pharmacies

By prescription

Dosage form

of the tablet

Weight

Weight: 20 g.