Ketokam, 10 mg 20 pcs.

Ketokam has a pronounced analgesic effect, it also has anti-inflammatory and moderate antipyretic effects. Mechanism of action is related to non-selective inhibition of COX activity, and COX2, catalyzing formation of PG from arachidonic acid, which play an important role in pathogenesis of pain, inflammation and fever. It is comparable with morphine in strength of analgesic effect and is significantly superior to other NSAIDs. After per oral and intravenous administration it is possible to observe analgesic effect in 0.5 and 1 hour respectively, maximal effect is reached after 1-2 and 2-3 hours.
Pharmacokinetics: absorption during oral administration is fast, bioavailability is 80-100%; in intravenous administration – complete and rapid. Cmax after oral administration of 10 mg is -0.82-1.46 µg/mL, Òcmax is 10-78 min; after 30 mg v/m administration Cmax is 1.74-3.1 µg/mL, 60 mg – 3.23-5.77 µg/mL, Òcmax is 15-73 min and 30-60 min respectively; Cmax after 15 mg v/m infusion is 1.96-2.98 µg/mL, 30 mg – 3.69-5.61 µg/mL. The binding to plasma proteins is 99%. Time to reach Css with parenteral and oral administration – 24 h when administered 4 times per day (above subtherapeutic) and is 0.65-1.13 mcg/ml, 1.29-2.47 mcg/ml when administered in v/v infusion of 15 mg – 0.79-1.39 mcg/ml, 30 mg – 1.68-2.76 mcg/ml; after 10 mg oral administration – 0.39-0.79 mcg/ml. The volume of distribution is 0.15-0.33 l/kg. In patients with renal insufficiency distribution volume of the drug may be increased by 2 times, and the distribution volume of its R-enantiomer – by 20%. The T1/2 in patients with normal renal function is on average 5.3 h (3.5-9.2 h after intravenous injection of 30 mg, 4-7.9 h after intravenous injection of 30 mg and 2.4-9 h after oral administration of 10 mg). The T1/2 is longer in elderly patients and shorter in younger patients.
Liver function has no effect on T1/2.
In patients with impaired renal function at creatinine concentration in plasma 19-50 mg/l (168-442 µmol/l) the T1/2 is 10.3-10.8 h, in more severe renal failure – more than 13.6 h. Total clearance is 0.023 l/h/kg (0.019 l/h/kg in elderly patients), intravenous infusion of 30 mg – 0.03 l/h/kg, oral administration of 10 mg – 0.025 l/h/kg; in patients with renal insufficiency with creatinine concentration in plasma of 19-50 mg/l, intravenous infusion of 30 mg – 0.015 l/h/kg, oral administration of 10 mg – 0.016 l/h/kg. It is not excreted by hemodialysis.

Indications

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

Active ingredient

Composition

Shell composition: universal shell* 8.00 mg.

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

How to take, the dosage

In adults, when administered orally, 10 mg every 4-6 hours; if necessary, 20 mg 3-4 times a day.

In case of intravenous injection, a single dose is 10-30 mg, the interval between injections is 4-6 hours. Maximum duration of use is 2 days.

Maximum doses: when given orally or by injection, 90 mg/day; for patients with body weight less than 50 kg, with renal dysfunction, or for patients older than 65 years, 60 mg/day.

Interaction

In concomitant use of ketorolac with other NSAIDs may develop additive side effects; with pentoxifylline, anticoagulants (including heparin in low doses) – may increase the risk of bleeding; with ACE inhibitors – may increase the risk of renal dysfunction; with probenecid – increased plasma concentration of ketorolac and its half-life; with lithium preparations – possible decrease in renal clearance of lithium and increase its concentration in plasma; with furosemide – reduction of its diuretic effect.

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

Special Instructions

With caution use in patients with liver and kidney function abnormalities, chronic heart failure, arterial hypertension, patients with gastrointestinal erosive ulcers and gastrointestinal bleeding in the history.

Ketorolac should be used with caution in the postoperative period in cases where particularly careful hemostasis is required (including after prostate resection, tonsillectomy, in cosmetic surgery) and in elderly patients because the half-life of ketorolac is longer 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, eosinophilia appear, ketorolac should be discontinued. Ketorolac is not indicated for use in chronic pain syndrome.

If during treatment with ketorolac drowsiness, dizziness, insomnia or depression occur, special caution should be exercised during potentially dangerous activities requiring increased attention and rapid psychomotor reactions.

Contraindications

Hypersensitivity, hypovolemia (regardless of the cause), gastrointestinal erosive and ulcerative lesions in the acute stage, hypocoagulation (including hemophilia), bleeding or high risk of bleeding, severe renal insufficiency (plasma creatinine over 50 mg/l), hepatic insufficiency, “aspirin” triad (combination of bronchial asthma, recurrent polyposis of the nose and sinuses and intolerance of ASA and pyrazolone drugs), childbirth, lactation, children (under 16 years old – safety and efficacy have not been established).
With caution. Hypersensitivity to other NSAIDs. Hypersensitivity to other NSAIDs, bronchial asthma, presence of factors increasing gastrointestinal toxicity: alcoholism, smoking and cholecystitis, postoperative period, CHF, edema syndrome, arterial hypertension, renal impairment (plasma creatinine
.

Side effects

Respiratory system: rarely – respiratory disorders, episodes of choking.

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

With the blood-clotting system: rarely – nasal bleeding, anemia, eosinophilia, thrombocytopenia, bleeding from postoperative wounds.

Cardiovascular system disorders: rarely – bradycardia, BP changes, palpitations, fainting.

Gastrointestinal system disorders: nausea, abdominal pain, diarrhea may occur; rarely – constipation, flatulence, feeling of fullness of the stomach, vomiting, dry mouth, thirst, stomatitis, gastritis, erosive and ulcerative lesions of the stomach, liver function disorders.

CNS and peripheral nervous system disorders: anxiety, headache, somnolence may occur; paresthesias, depression, euphoria, sleep disorders, dizziness, altered sense of taste, visual disturbances, motor disorders are rare.

Metabolism disorders: increased sweating, edema may occur; rarely – oliguria, increased plasma creatinine and/or urea levels, hypokalemia, hyponatremia.

Allergic reactions: skin itching, hemorrhagic rash may occur; in single cases – exfoliative dermatitis, urticaria, Lyell syndrome, Stevens-Johnson syndrome, anaphylactic shock, bronchospasm, Quincke’s edema, myalgia.

Others: fever may occur.

Local reactions: pain at the injection site.

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