Tradename
KETAHOB (KETANOV)
International name
KETOROLACUM M01AB15
Latin name
KETANOV
general characteristics
active substance: 1 ml of solution contains ketorolac trometamol 30 mg;

Excipients: sodium chloride, disodium edetate, ethanol 96%, water for injections, (sodium hydroxide or dilute hydrochloric acid added to adjust the pH).

Farmgroup
Nonsteroidal anti-inflammatory drug with a strong analgesic effect.
Pharmacological properties
Ketorolac tromethamine ((±) -5-benzoyl-2,3-dihydro-1 H-pyrolisidine-1-carboxylic acid combined with 2-amino-2-hydroxymethyl-1,3-propanediol in a ratio of 1: 1) NSAIDs. Has anti-inflammatory and pronounced analgesic effect. Ketorolac acts on the cyclooxygenase pathway for the metabolism of arachidonic acid, inhibiting the biosynthesis of prostaglandins. Like other NSAIDs, ketorolac inhibits platelet aggregation caused by arachidonic acid and collagen, and does not affect ATP-induced aggregation. Ketorolac increases the average period of bleeding, does not affect the number of platelets, prothrombin time or activated partial thromboplastin time. Unlike narcotic analgesics, ketorolac does not exert a depressant effect on the respiratory center and does not cause an increase in pCO2. In contrast to morphine, ketorolac does not affect the state of the myocardium and does not cause hemodynamic disturbances. Ketorolac does not affect psychomotor functions, unlike analgesics of the central action of morphine, buprenorphine, etc. After the / m administration of the drug, the maximum concentrations in the blood plasma are reached after 45-50 minutes. Ketorolac does not undergo significant pre-systemic metabolism. It was found that the maximum concentration in blood plasma in healthy volunteers after IV injection of the drug in a dose of 30 mg is 3 mg / l. There is no cumulation of the drug when administered at a dose of 10-90 mg. Like other NSAIDs, ketorolac slowly binds to plasma proteins (more than 99%), reaches high concentrations in the aqueous humor of the eye. The main pathway of metabolism is binding to glucuronic acid. 10% of the dose of the drug is excreted with feces, more than 90% is excreted in the urine, with 60% unchanged. The average half-life is about 4-6 hours after parenteral administration. In elderly people, the elimination rate decreases, the half-life increases on average to 7 hours after parenteral administration at a dose of 30 mg. In patients with renal insufficiency, excretion of ketorolac is slowed, as evidenced by a decrease in overall clearance, and the elimination half-life increases to 9.62-9.91 hours, which indicates the need for dose adjustment. Penetrates through the placenta and into breast milk.
Pharmacokinetics
In humans, after intramuscular injection, the maximum plasma concentrations are reached after 45-50 minutes. Ketorolac does not lend itself to essential presystemic metabolism. It was revealed that peak plasma concentrations in healthy volunteers after intramuscular injection of 30 mg dose were 3 mg / l. There is no cumulation of the drug when administered at a dose of 10-90 mg. Like other NSAIDs, ketorolac significantly binds to blood plasma proteins (more than 99%) of ketorolac reaches high concentrations in the aqueous humor of the eye. The main pathway of ketorolac metabolism is binding to glucuronic acid. 10% of the dose is excreted with feces, more than 90% is excreted in urine, with 60% in unchanged form. The average half-life is 4-6 hours after parenteral administration. In elderly people, the rate of administration is reduced, the half-life increases, to an average of 7.01 hours after a parenteral dose of 30 mg. In patients with renal failure, excretion of ketorolac is slow, as evidenced by a decrease in total plasma clearance, and the half-life increases (up to 9.6-9.9 hours), which indicates the need for dose adjustment. According to the available data, ketorolac comes from the maternal circulation to the fetal circulation (ratio 0.116). It is also excreted with milk.
Indications for use
For short-term use to eliminate a moderately severe pain syndrome: pain in the postoperative period in general surgery, after gynecological, orthopedic, urological, dental, otolaryngological operations and other surgical interventions; injuries of the musculoskeletal system and soft tissues, including stretching, dislocations, fractures, etc. It is effective for short anesthesia with pain syndrome after the abolition of narcotic drugs, dental pain (pericoronitis, pulpitis, caries, etc.), renal and hepatic colic ( in combination with antispasmodics), pain after childbirth, otitis, ishialgia, fibromyalgia, chronic tissue pathology, osteoarthritis, sciatica, arthrosis, osteochondrosis, pain syndrome in cancer patients.

Dosing and Administration
In / m injected in an initial dose of 10 mg, then 10-30 mg every 4-6 hours if necessary. The drug should be given in the lowest effective dose. The maximum daily dose for adults should not exceed 90 mg, for patients over the age of 65, 60 mg. The maximum duration of parenteral administration of the drug should not exceed 2 days. When transferring a patient from parenteral to oral administration, the total daily dose of ketorolac should not exceed 90 mg for adults and 60 mg for the elderly. Inside prescribe 10 mg every 4-6 hours. The maximum duration of treatment should not exceed 7 days. Patients with a body weight of up to 50 kg, patients over the age of 65 or with impaired renal function are recommended to be prescribed in reduced doses.
Side effects
Drowsiness, nausea, abdominal pain, indigestion, diarrhea, headache and dizziness, constipation, increased excitability, xerostomia, hyperhidrosis, nightmarish dreams, hyperkinesia, myalgia, asthenia, palpitation, tenderness at the injection site.
Contraindications
The period of pregnancy and lactation, childbirth, age of 16 years, polyposis of the nasal cavity, angioedema, asthma, dehydration and hypovolemia, peptic ulcer of the stomach and duodenum, blood clotting disorder, renal failure of moderate or severe degree, hypersensitivity to ketorolac.
Interaction with other drugs
In vitro, ketorolac somewhat reduces the binding of warfarin to plasma proteins. Does not affect the degree of binding of digoxin to blood proteins. At therapeutic concentrations of salicylates in vitro, ketorolac binding decreases from 99.2 to 97.5%, potentially leading to an almost doubling of levels of free ketorolac in the blood; respectively, patients who receive salicylates in high doses, ketorolac should be administered with caution. Digoxin, ibuprofen, naproxen, paracetamol, phenytoin, tolbutamide, piroxicam in therapeutic concentrations do not affect the binding of ketorolac to plasma proteins. In clinical trials, ketorolac was administered simultaneously with morphine without undesirable interactions.
Overdose
There are no clinical data on acute overdose of the drug. In experimental studies after a single injection of 100 mg per 1 kg of body weight, the symptoms in animals were decreased activity, diarrhea, difficulty breathing, vomiting.
Application features
Ketanov in the form of r-ra for injection is intended only for short-term use. In elderly people, the elimination of ketorolac is slowed down, so the drug should be administered under strict medical supervision and in reduced doses. In patients with heart failure, the drug should be used with caution. The inhibition of platelet aggregation persists for 24-48 hours after discontinuation of the drug, therefore it is necessary to monitor patients with blood clotting disorders that receive therapy with Ketanov. Ketorolac is not an agonist or antagonist of drugs, does not have a central opioid-like effect.
Terms and conditions of storage
In a dry, the dark place at a temperature of up to 15 ° C.
Leave conditions
On prescription
Manufacturer and its address
Ranbaxy