Ketanov, pills 10mg, 20pcs

Composition

1 tablet contains ketorolac trometamine 10 mg

Pharmacological action

Pharmaceutical group:

NSAIDs.

Pharmaceutical action:  

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

The mechanism of action is associated with non-selective inhibition of COX-1 and -2 enzyme activity, mainly in peripheral tissues, which results in inhibition of the biosynthesis of PH-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 Ketanov does not affect opioid receptors, does not depress respiration, does not cause drug dependence, does not have a sedative and anxiolytic effect.

The strength of the analgesic effect is comparable to morphine, significantly superior to other NSAIDs.

After intravenous use and oral use, the onset of analgesic action is noted in 0.5 and 1 h, respectively, and the maximum effect is achieved in 1-2 h

. Pharmacokinetics:  

After oral use, Ketanov® is well absorbed in the gastrointestinal tract-Cmax in blood plasma (0.7-1.1 mcg / ml) is reached 40 minutes after taking a 10 mg dose on an empty stomach. High-fat food reduces the Cmax of the drug in the blood and delays its achievement by 1 h. 99% of the drug binds to plasma proteins, and with hypoalbuminemia, the amount of free substance in the blood increases. Bioavailability — 80-100%.

Intravenous absorption is complete and rapid. After intravenous use of 30 mg of the drug, Cmax is 1.74–3.1 mcg/ml,60 mg-3.23– 5.77 mcg / ml, and Tmax is 15-73 and 30-60 minutes, respectively.

The time to reach the equilibrium concentration (CSS) with parenteral and oral use is 24 hours when prescribed 4 times a day (above subtherapeutic) and is 0.65 — 1.13 mcg/ml with intravenous use at a dose of 15 mg,1.29 — 2.47 mcg/ml with 30 mg, and 0.39 — 0.79 mcg/ml after oral use of 10 mg. The volume of distribution is 0.15-0.33 l / kg. In patients with renal insufficiency, the volume of distribution of the drug may increase by 2 times, and its R-enantiomer-by 20%.

Penetrates into breast milk: after the mother takes the first and second doses of ketorolac (10 mg), Cmax in milk is reached in 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. It is excreted by 91% – by the kidneys,6% – through the intestines.

T1 / 2 in patients with normal renal function averages 5.3 hours (3.5-9.2 hours after intravenous use of 30 mg and 2.4-9 hours after oral use of 10 mg). T1/2 is prolonged in elderly patients and shortened in young patients. Liver function does not affect T1/2. In patients with impaired renal function, with a plasma creatinine concentration of 19-50 mg/l (168-442 mmol/L), T1 / 2 is 10.3-10.8 hours, with more severe renal insufficiency-more than 13.6 hours.

Total clearance is 0.023 l/kg/h (0.019 l/kg/h in elderly patients) when administered intravenously at a dose of 30 mg,0.025 l/kg/h when administered orally at a dose of 10 mg; in renal insufficiency with a plasma creatinine concentration of 19-50 mg/l when administered intravenously at a dose of 30 mg — 0.015 l/kg/h, when taken orally at 10 mg — 0.016 l/kg/h. It is not excreted during hemodialysis.

Indications

Pain syndrome of moderate and severe intensity of various genesis ( including in the postoperative period, with oncological diseases).

Contraindications

– peptic ulcer of stomach and duodenum in the acute phase; gastrointestinal bleeding; – bronchial asthma; – pronounced cerebrovascular disorders; – moderate and severe renal dysfunction, the risk of developing kidney failure, hypovolemia and dehydration; – disorders of blood coagulation in history; hemorrhagic diathesis; – concomitant use with other NSAIDs; – pregnancy; – delivery; – lactation (breastfeeding); – children’s and teenage age up to 16 years; – hypersensitivity to Ketorolac and other NSAIDs.

Side effects

From the digestive system: stomatitis, nausea, constipation, dyspepsia, gastritis, erosive and ulcerative lesions of the gastrointestinal tract, dry mouth.

From the central nervous system and peripheral nervous system: drowsiness, dizziness, nervousness, paresthesia.

From the urinary system: frequent urination, acute renal failure, nephrotic syndrome, interstitial nephritis.

From the side of metabolism: increased creatinine and / or urea levels in blood plasma.

From the side of the water-electrolyte balance: hypokalemia, hyponatremia.

From the cardiovascular system: bradycardia, changes in blood pressure.

From the side of the blood coagulation system: thrombocytopenia, purpura, hematoma formation, nosebleeds, prolongation of clotting time.

Respiratory system disorders: shortness of breath.

Allergic reactions: urticaria.

Other: thirst.

Interaction

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

In vitro ketorolac reduces the binding of warfarin to plasma proteins.

How to take, course of use and dosage

Adults inside are prescribed 10 mg every 4-6 hours. With 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.

Overdose

There are no clinical data on acute overdose of the drug. In experimental studies, after a single use of 100 mg/kg of body weight in animals, such symptoms as decreased activity, diarrhea, difficulty breathing, vomiting were observed.

Special instructions

Caution should be exercised when prescribing the drug to patients with impaired liver and/or kidney function.

It should be borne in mind that prolonged use of the drug increases the risk of side effects from the digestive system.

Ketanov does not cause the formation of drug dependence.

Available on a doctor’s prescription

Form of production

Film-coated tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Ketorolac

Conditions of release from pharmacies

By prescription

Dosage form

Tablets