Ketanov, 10 mg 20 pcs.

Pharmgroup:

NSAIDs.

Pharmaceutical action:

Ketorolac has a pronounced analgesic effect, also has anti-inflammatory and moderate antipyretic effects.

The mechanism of action is related to non-selective inhibition of COX-1 and -2 enzyme activity, mainly in peripheral tissues, with the consequence of inhibition of PG biosynthesis – modulators of pain sensitivity, thermoregulation and inflammation. Ketorolac is a racemic mixture of [-]S- and [+]R-enantiomers, and the analgesic effect is due to the [-]S form.

The drug Ketanon has no effect on the opioid receptors, does not suppress respiration, does not cause addiction and has no sedative and anxiolytic effects.

In terms of the analgesic effect, it is comparable with morphine and is significantly superior to other NSAIDs.

After intravenous and per oral administration the onset of analgesic effect is noted after 0.5 and 1 hour respectively, the maximum effect is reached after 1-2 hours.

Pharmacokinetics:

After oral administration Ketanov® is well absorbed in the GI tract – Cmax in plasma (0.7-1.1 mcg/ml) is reached 40 min after an empty stomach dose of 10 mg. Fat-rich food decreases the drug Cmax in blood and delays its achievement by 1 h. 99% of the drug is bound to plasma proteins, and in case of hypoalbuminemia the amount of free substance in blood increases. Bioavailability is 80-100%.

Absorption when administered in m/m is complete and rapid. After 30 mg of the drug is administered in the m/m, Cmax is 1.74-3.1 µg/ml, 60 mg – 3.23- 5.77 µg/ml, Tmax is 15-73 and 30-60 min, respectively.

The time to reach equilibrium concentration (CSS) with parenteral and oral administration is 24 h when administered 4 times a day (above subtherapeutic) and is 0.65-1.13 mcg/ml, 1.29-2.47 mcg/ml when administered v/m in 15 mg dose; 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, the distribution volume of the drug may increase 2-fold and its R-enantiomer by 20%.

Transfers to breast milk: after maternal administration of the first and second dose of ketorolac (10 mg) the Cmax in milk is reached after 2 hours and is 7.3 and 7.9 ng/l, respectively.

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. 91% is excreted by the kidneys, 6% is excreted through the intestine.

The T1/2 in patients with normal renal function is on average 5.3 h (3.5-9.2 h after 30 mg i.v. and 2.4-9 h after 10 mg oral administration). 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 with plasma creatinine concentration of 19-50 mg/l (168-442 μmol/l) T1/2 is 10.3-10.8 h, in more severe renal failure – more than 13.6 h.

The total clearance is 0.023 l/kg/h (0.019 l/kg/h in elderly patients) when administered by injection in 30 mg doses, and 0.025 l/kg/h when administered orally in 10 mg doses; in renal failure with creatinine concentration in blood plasma of 19-50 mg/l, when administered intravenously at a dose of 30 mg – 0.015 l/kg/h, when administered orally at 10 mg – 0.016 l/kg/h.
It is not eliminated during hemodialysis.

Indications

Pain syndrome of moderate and severe intensity of different genesis (including in the postoperative period, in cancer).

Active ingredient

Ketorolac

Composition

1 tablet contains ketorolac tromethamine 10 mg.

How to take, the dosage

In adults, 10 mg every 4-6 hours is administered orally. In severe pain the dose can be increased to 20 mg 3-4 times a day.

The maximum daily dose of the drug (for any dosage form) is 90 mg.

Interaction

Concomitant use of Ketorolac with other NSAIDs increases the risk of side effects.

In vitro Ketorolac decreases the binding of warfarin to plasma proteins.

.

Special Instructions

The drug should be administered with caution in patients with impaired hepatic and/or renal function.

Please note that long-term use of the drug increases the risk of adverse effects of the digestive system.

Ketanov does not cause the formation of drug dependence.

Prescribed by the doctor

.

Contraindications

– gastric and duodenal ulcer in the acute phase;
– gastrointestinal bleeding;
– bronchial asthma;
– expressed cerebro-vascular disorders;
– moderate and expressed renal function disorders, risk of renal failure with hypovolemia and dehydration;
– history of blood clotting disorders;
– hemorrhagic diathesis;
– concomitant use with other NSAIDs;
– pregnancy;
– childbirth;
– lactation (breastfeeding);
– childhood and adolescence under 16 years of age;
– hypersensitivity to ketorolac and other NSAIDs.

.

Side effects

Digestive system disorders: stomatitis, nausea, constipation, dyspepsia, gastritis, gastrointestinal erosive ulcers, dry mouth.

CNS and peripheral nervous system disorders: drowsiness, dizziness, nervousness, paresthesias.

Urinary system disorders: frequent urination, acute renal failure, nephrotic syndrome, interstitial nephritis.

Metabolism disorders: increase in plasma creatinine and/or urea levels.

Water-electrolyte balance: hypokalemia, hyponatremia.

Cardiovascular system: bradycardia, BP changes.

coagulant system disorders: thrombocytopenia, purpura, hematoma formation, nasal bleeding, prolongation of clotting time.

Respiratory system: dyspnea.

Allergic reactions: urticaria.

Other: thirst.

.

Overdose

In experimental studies after a single administration of 100 mg/kg body weight the animals showed symptoms such as decreased activity, diarrhea, difficulty in breathing, vomiting.

.

Similarities

Dolac, Ketorol, Ketonov, Ketorolac, Ketorolac Rompharm