Ketorol Express, 10 mg 20 pcs.

NSAID, has a pronounced analgesic effect, has anti-inflammatory and moderate antipyretic effects. The mechanism of action is associated with non-selective inhibition of COX activity – COX-1 and COX-2, catalyzing formation of prostaglandins from arachidonic acid, which play an important role in the pathogenesis of inflammation, pain and fever.

Ketorolac is a racemic mixture of [-]S- and [+]R-enantiomers with analgesic effect caused by [-]S-form.

The drug does not affect opioid receptors, does not depress respiration, does not cause drug addiction, has no sedative and anxiolytic action.
After oral administration the onset of analgesic effect is noted after 1 hour, the maximum effect is achieved after 1-2 hours.

Pharmacokinetics

Absorption

After oral administration, ketorolac is well absorbed from the GI tract, Cmax in plasma (0.7-1.1 mcg/ml) is reached 40 min after an empty stomach dose of 10 mg. High-fat food decreases Cmax in blood and delays its achieving by 1 h. Bioavailability – 80-100%.

Distribution

Binding to plasma proteins is 99% , with hypoalbuminemia the amount of free substance in blood increases. Time to reach Css (0.39-0.79 mcg/ml), when administered orally 10 mg ketorolac 4 times/day (above subtherapeutic dose), is 24 hours. Vd – 0.15-0.33 l/kg.

Penetrates into breast milk: after maternal administration of 10 mg ketorolac Cmax in breast milk is reached after 2 hours and is 7.3 ng/ml after the first dose and 7.9 ng/ml after the second dose of the drug.

Metabolism

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.

Excretion
Excreted by the kidneys (91%) and through the gut (6%).T1/2 in patients with normal renal function is 2.4-9 h after an oral dose of 10 mg.When taken orally at a dose of 10 mg, total clearance is 0.025 l/h/kg.

Pharmacokinetics in special clinical cases

In patients with renal insufficiency, the Vd of ketorolac may increase twice and the Vd of its R-enantiomer by 20%.T1/2 is increased in older patients and decreased in younger patients.
Liver function disorders have no effect on T1/2. In patients with impaired renal function, with plasma creatinine concentration of 19-50 mg/l (168-442 μmol/l), T1/2 is 10.3-10.8 h, with more severe renal failure – more than 13.6 h.

When administered orally at a dose of 10 mg, total clearance in patients with renal insufficiency (at plasma creatinine concentration of 19-50 mg/l) is 0.016 l/kg.

Not excreted by hemodialysis.

Indications

Pain syndrome of severe to moderate severity:

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

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