Ketorol, 30 mg/ml 1 ml 10 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) – 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 it is comparable with morphine and is 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.

Pharmacokinetics

The pharmacokinetics of ketorolac after single and multiple intravenous and intramuscular administration is linear.

When administered intramuscularly absorption is complete and rapid. Maximal concentration of the preparation (Cmax) after intramuscular introduction of 30 mg is 1.74-3.1 µg/ml, after 60 mg – 3.23-5.77 µg/ml; time of reaching the maximum concentration (TCmax) is 15-73 and 30-60 minutes, respectively. Cmax after intravenous administration of 15 mg – 1.96-2.98 mcg/ml, 30 mg – 3.69-5.61 mcg/ml, TCmax – 0.4-1.8 min and 1.1-4.7 min, respectively.

The binding to plasma proteins is 99%. Time of reaching of equilibrium concentration (Css) in parenteral administration of 30 mg 4 times per day – 24 hours; in intramuscular administration of 15 mg – 0.65-1.13 mkg/ml, of 30 mg – 1.29-2.47 mkg/ml.

Distribution volume (Vd) in intramuscular administration – 0.136-0.214 l/kg, in intravenous – 0.166-0.254 l/kg. In patients with renal insufficiency the drug distribution volume may increase twice, and the distribution volume of its R-enantiomer – by 20%.

Indications

Pain syndrome of strong and moderate severity of different origin in trauma, toothache, pain in the postoperative period, in cancer and rheumatic diseases, myalgia, arthralgia, neuralgia, radiculitis.

Preferred to symptomatic therapy, to reduce pain and inflammation at the time of use. It has no effect on the progression of the disease.

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

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