Ketorolac Wellfarm 30 mg/ml 1 ml, 10 pcs.

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID).
ATX code M01AB15
PHARMACOLOGICAL ACTION
Ketorolac has a pronounced analgesic effect, also has anti-inflammatory and moderate antipyretic effect.
The mechanism of action is associated with non-selective inhibition of cyclooxygenase 1 and 2 enzyme activity, mainly in peripheral tissues, resulting in inhibition of prostaglandin biosynthesis – modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of [-]S and [+]R enantiomers, the analgesic effect is due to [-]S form.
By the strength of analgesic effect it is comparable with morphine, is significantly superior to other non-steroidal anti-inflammatory drugs.
The drug does not affect opioid receptors, does not depress respiration, does not cause drug addiction, has no sedative and anxiolytic action.
After intramuscular introduction the onset of analgesic action is observed within 0.5 hours, the maximum effect is reached after 1-2 hours.
Pharmacokinetics
Bioavailability – 80-100 %, absorption by intramuscular introduction is complete and rapid. Maximal concentration in plasma is 1.74-3.1 µg/ml, maximum concentration after intramuscular introduction of 30 mg (Сmax), after 60 mg – 3.23-5.77 µg/ml, time to reach maximal concentration is 15-73 min and 30-60 min, respectively; Сmax after intravenous infusion of 15 mg is 1.96-2.98 µg/ml, 30 mg – 3.69-5.61 µg/ml. Time to reach equilibrium concentrations (Css) when administered parenterally – 24 hours when administered 4 times a day (above subtherapeutic) and is 0.65-1.13 mcg/ml, 1.29-2.47 mcg/ml with intramuscular administration of 15 mg, 1.29-2.47 mcg/ml with intravenous infusion, 0.79-1.39 mcg/ml with intravenous infusion of 15 mg, 1.68-2.76 mcg/ml with infusion of 30 mg.
99% of the drug is bound to plasma proteins, and in case of hypoalbuminemia the amount of free substance in blood increases.
Distribution volume 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%. Passes poorly through the blood-brain barrier, penetrates through the placenta (10%). It is detected in small amounts in breast milk.
More than 50% of the administered dose is metabolized in the liver with the formation of pharmacologically inactive metabolites. The main metabolites are glucuronides, which are excreted by the kidneys and p-hydroxyketorolac.
Excreted 91% by the kidneys (40% as metabolites), 6% through the intestine.
The elimination half-life (T½) in patients with normal renal function is on average 5.3 h (3.5-9.2 h after 30 mg IM, 4-7.9 h after 30 mg IM). lengthened in older patients and shortened in younger patients. Liver function has no effect on T½. In patients with impaired renal function with plasma creatinine concentration of 19-50 mg/l (168-442 μmol/l) T½ is 10.3-10.8 h, with more severe renal impairment more than 13.6 h.
Total clearance is 0.023 l/kg/h (0.019 l/kg/h in elderly patients), intravenous infusion of 30 mg – 0.03 l/kg/h; in patients with renal insufficiency with creatinine concentration in blood plasma of 19-50 mg/l, intravenous administration of 30 mg – 0.015 l/kg/h.
Not excreted by hemodialysis.

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