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Ketovarnish (Ketolac)

international and chemical name: ketorolac, trometaminovy salt (±)-5-бензоил-2,3-дигидро-1Н-пиролизин-1-карбоновой acids;

Main physical and chemical characteristics: tablets of rounded shape with an oboyevypukly surface, white or almost white color;

Structure. 1 tablet of Ketolak contains a ketorolak of a trometamin of 10 mg (0,01 g);

other components: lactoses monohydrate, cellulose microcrystallic, potato starch, magnesium stearate, aerosil.

Form of release of medicine. Tablets.

Farmakoterapevtichesky group. Nonsteroid anti-inflammatory and antirheumatic drugs. Ketorolak. Code of automatic telephone exchange M01A B15.

Effect of the medicine. Pharmacodynamics. The anesthetizing, antiinflammatory, febrifugal drug. The mechanism of action of a ketorolak is caused by braking of biosynthesis of prostaglandins by cyclooxygenase-1 braking, and also decrease in formation of other mediators of pain and an inflammation. Does not influence opioid receptors, does not make braking of a respiratory center, does not show sedative and anksiolitichesky action. Drug does not make medicinal dependence and symptoms of cancellation. Slows down aggregation of thrombocytes and can increase hour of bleeding.

Pharmacokinetics. At internal use ketorolak it is quickly and completely absorbed, contacting proteins of plasma more than for 99%. The maximum concentration in blood is reached in 40–50 minutes. Reception of food reduces speed, but absorption of substance in blood does not influence degree. Ketorolak is metabolized in an organism generally by conjugation with glucuronic acid. Removal of a ketorolak results kidneys (to 90%), including in not changed form (~ 58%), in the form of almost inactive metabolite – r-gidroksiketorolaka (~ 11%) and other metabolites, perhaps, conjugates (~ 31%). The elimination half-life makes 4–6 hours. At patients of advanced age (65 years are more senior), and also at a renal failure the plasma clearance of a ketorolak decreases, and time of semi-removal increases. Drug does not kumulirut in an organism.

The analgesic effect develops in 30–40 minutes after use of drug and proceeds till 4-6 o'clock.

Indications to use. Pains of average and strong intensity mainly in the postoperative and posttraumatic period.

Way of use and dose. Drug is not intended for treatment of a chronic pain syndrome.

The mode of a dosage is set individually taking into account intensity of a pain syndrome. The adult, usually, appoint on 1 tablet (10 mg) each 4–6 hours, at the expressed pain syndrome it is possible to increase a single dose to 20 mg. Maximum daily dose of 90 mg. Course of treatment Ketolak no more than 5 days.

To patients age 65 years or with body weight less than 50 kg are more senior, and also appoint drug the patient with a renal failure in lower doses, the maximum daily dose – 60 mg.

Side effect. From a digestive tract: dyspepsia, nausea, pains in epigastriums, in isolated cases – a meteorism, an eructation, vomiting, a lock, digestive tract erosive cankers, an abnormal liver function;

From the central nervous system: a headache, dizziness, drowsiness, sleeplessness, a depression, nervousness, a sleep disorder, excitement, disturbance of concentration of attention, dryness in a mouth;

From an urinary system: frequent urination, an oliguria, a hamaturia, are described cases of an acute renal failure, a nephrotic syndrome, a glomerulonephritis;

From system of turning of blood: formations of hematomas, postoperative bleedings, nasal bleedings, increase in a bleeding time;

Allergic reactions: skin itch, small tortoiseshell, throat hypostasis, bronchospasm.

Contraindications. Erosive and ulcer injuries of a digestive tract to the anamnesis, a renal failure (creatinine of serum is higher than 442 µmol/l), a hypovolemia, dehydration, bronchial asthma, a bronchospasm, blood turning disturbance, high risk postoperative bleedings, an opportunity or existence of gastrointestinal and/or craniocereberal bleedings and disturbances of a hemostasis, pregnancy, the lactation period at women, age are younger than 16 years, individual sensitivity to a ketorolak and other non-steroidal anti-inflammatory drugs is increased.

Overdose. Symptoms: abdominal pains, nausea, vomiting, stomach erosive cankers, hyperventilation, renal failure.

Treatment: suspensions of administration of drug, gastric lavage, symptomatic therapy. The specific antidote does not exist.

Features of use. It is necessary to adhere to care at purpose of drug sick age 65 years, to patients with an abnormal liver function and kidneys, chronic heart failure, an arterial hypertension, bronchial asthma and a bronkhoobstruktivny syndrome, to persons during activity which requires special attention and speed of psychomotor reactions are more senior.

If necessary Ketolak it is possible to appoint in a combination with narcotic analgetics, at the same time their dose can be lowered. It is not recommended to apply to premedication, the supporting anesthesia and for anesthesia in obstetric practice.

The patient with blood turning disturbance drug is appointed with care, under control of number of thrombocytes.

During treatment the delay of speed of psychomotor reactions is observed. Persons whose activity requires special attention and speed of psychomotor reactions need to consider it.

Interaction with other medicines. Simultaneous use of Ketolak with pentoksifilliny, anticoagulants and dextrans increases risk of bleeding. Simultaneous use with inhibitors of an angiotensin-converting enzyme can increase risk of development of renal failures (especially at patients on a hypovolemia). Increases toxicity of a methotrexate, cyclosporine, a gastrotoksichnost of non-steroidal anti-inflammatory drugs and glucocorticoids. At simultaneous use with salts of lithium decrease in excretion of lithium with urine and increase of its concentration in a blood plasma is possible. Probenetsid increases concentration of a ketorolak in plasma and prolongs the period of its semi-removal.

Conditions and periods of storage. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Period of validity – 2 years.

"Ketalginum   Ketoleks"