Active ingredients: ketorolac; 1 tablet includes a ketorolak (in the form of a ketorolak of a trometamin) 10 mg;
other components: lactoses monohydrate, cellulose microcrystallic, krospovidon, magnesium stearate.
Dosage form. Tablets.
Farmakoterapevtichesky group. Nonsteroid anti-inflammatory and antirheumatic drugs.
ATC code. M01A B15.
Acute pain syndrome of high and average intensity: at injuries, a dentagra, pains in the puerperal and postoperative period, at oncological diseases, a mialgiya, arthralgias, neuralgia, radiculitises, dislocations, stretchings, rheumatic diseases.
Contraindications of Ketolonga.
Hypersensitivity to drug components. Intolerance of acetylsalicylic acid and medicines derivative of pyrazyl ketone. A hypovolemia (irrespective of the reason that caused it). Digestive tract erosive cankers in a stage an aggravation. Hypocoagulation (including hemophilia). Internal and external bleedings or high risk of their development. A heavy renal failure (creatinine of plasma is higher than 50 mg/l). Liver failure.
Way of use and dose.
To patients age from 16 to 65 years with body weight less than 50 kg or to patients with a renal failure – 10 mg in the first reception, and further on 10 mg to 4 times a day.
Patients are from 16 to 65 years old with body weight that exceeds 50 kg, the recommended dose makes 20 mg in the first reception, further on 10 mg to 3 times a day, but no more than 40 mg/days.
The maximum daily dose at oral administration makes 40 mg. The course use of drug till 5 days is possible.
From the alimentary system: gastralgia, diarrhea (emergence frequency more than 3%); stomatitis, a meteorism, a lock, vomiting, feeling of overpopulation a stomach (frequency of emergence is up to 3%); loss of appetite, nausea, digestive tract erosive cankers with perforation and/or bleeding, an abdominal pain, a spasm or burning in epigastric area, blood in Calais or a melena, vomiting with blood or as "a coffee thick", nausea, heartburn, cholestatic jaundice, hepatitis, a hepatomegalia, acute pancreatitis (frequency of emergence is up to 1%).
From an urinary system: acute renal failure, back pain, hamaturia, azotemia, gemolitikouremichesky syndrome (hemolitic anemia, renal failure, thrombocytopenia, purpura), increase of an urination, increase or decrease in volume of urine, nephrite, hypostases of renal genesis (emergence frequency less than 1%).
From the central nervous system: a headache, dizziness, drowsiness, it is rare – aseptic meningitis (fever, a severe headache, spasms, muscle tension of a neck and/or back), a hyperactivity (change of mood, concern), hallucinations, a depression, psychosis, unconscious states (emergence frequency more than 3%).
From CCC: increase of arterial pressure (frequency of emergence is up to 3%).
From bodies hemopoiesis: anemia, a leukopenia, an eosinophilia (frequency of emergence is up to 1%).
From integuments: skin rash (including makulo-papular rash), purpura (frequency of emergence from 1 to 3%); exfoliative dermatitis (fever with a fever or without, a hyperemia, consolidation or a peeling of skin, increase and/or morbidity of subpalatine tonsils), the small tortoiseshell, a malignant exudative erythema (Stephens-Johnson's syndrome), a toxic epidermal necrolysis a Lyell's disease (frequency of emergence is up to 1%).
From sense bodys: decrease in hearing, a ring in ears, a vision disorder, an illegibility visual perception (frequency of emergence is up to 1%).
From system of a hemostasis: bleeding from a postoperative wound, nasal bleeding, rectal bleeding (frequency of emergence is up to 1%).
Allergic reactions: an anaphylaxis or anaphylactoid reactions (change of skin color of the person, skin rash, the small tortoiseshell, an itch of skin, a tachypnea or dispnoe, swell age, periorbital hypostasis, an asthma, difficulty of breath, weight in a thorax, breath with whistle (emergence frequency to 1%).
Others: face edemas, shins, fingers, a foot, a paraglossa, increase of body weight (frequency of emergence is up to 3%); the raised potovydeleniye, fever (emergence frequency to 1%).
Treatment: symptomatic (support of the vital functions of an organism). A dialysis – ineffective.
Use during pregnancy or feeding by a breast.
Drug of contraindications to pregnant women (perhaps premature closing of Botalova channels) and to women during feeding by a breast.
Children. Efficiency and safety of drug at children is not established. Drug of contraindications to children to 16-year age.
Features of use.
Before purpose of drug it is necessary to find out a question about an average allergy to drug or other non-steroidal anti-inflammatory drugs.
With care drug is appointed the patient with bronchial asthma, existence of factors that increase gastrointestinal toxicity: alcoholism, to tobacco smoking and cholecystitis. The special attention at purpose of drug is paid to patients in the postoperative period, with chronic heart failure, an edematous syndrome, arterial hypertension, a renal failure (creatinine of plasma is higher than 50 mg/l), a cholestasia, active hepatitis, sepsis, a system lupus erythematosus that at the same time accept non-steroidal anti-inflammatory drugs, to elderly people.
The hypovolemia increases risk of development of nephrotoxic side reactions.
It is not recommended to apply as medicine to premedication, anesthesia supports.
At joint reception with other non-steroidal anti-inflammatory drugs the liquid delay, a decompensation of cordial activity, increase of arterial pressure can be observed. Influence on aggregation of thrombocytes stops in 24–48 hour. Not to use along with paracetamol more than 5 days.
The patient with disturbance of turning of blood appoint only at a constant control of quantity of thrombocytes, it is especially important for postoperative patients who demand careful control of a hemostasis.
The risk of development of medicinal complications grows at treatment continuation (at patients with chronic pains) and increase of a peroral dose of drug more than 40 mg/days.
For decrease in risk of development of the gastropathy caused ketorolaky antiacid medicines, mizoprostol, omeprazol are appointed.
Ability to influence speed of response when driving motor transport or other mechanisms.
During treatment it is necessary to adhere to care during the driving of motor transport and occupations by other potentially unsafe types of activity which need the increased concentration of attention and speed of psychomotor reactions.
Interaction with other medicines and other forms of interactions.
Joint appointment with paracetamol increases nephrotoxicity of a ketorolak.
If necessary it is possible to appoint in a combination with narcotic analgetics that also the drug dose decline leads to strengthening of analgetic effect.
The concomitant use with other nonsteroid medicines, glucocorticosteroids, ethanol, corticotropin, the drugs Ca2 + increases risk of an ulcer of a mucous membrane of a digestive tract and development of gastrointestinal bleedings.
Co-administration with anticoagulating medicines – derivatives of coumarin and an indandion, heparin, trombolitika (an alteplaza, Streptokinasa, an urokinase), antiagregantny medicines, cephalosporins, valproic acid and acetylsalicylic acid increases risk of development of bleedings.
Reduces effect of hypotensive and diuretic medicines, due to decrease in synthesis of prostaglandins in kidneys.
Joint appointment with a methotrexate raises gepato-and nephrotoxicity (their joint appointment is possible only during the using of low doses of the last and control of its concentration in plasma).
At appointment with other nephrotoxic medicines and drugs of gold the risk of development of nephrotoxicity increases.
Medicines, blocking canalicular secretion, reduce clearance of a ketorolak and increase its concentration in plasma.
Increases efficiency of narcotic analgetics.
Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.
Effect of the medicine. Pharmacodynamics. Ketolong-Darnitsa – non-steroidal anti-inflammatory drug on the basis of a ketorolak of a trometaprim. Possesses expressed analgeziruyushchy activity that considerably exceeds other non-steroidal anti-inflammatory drugs, comparative with analgesic activity of morphine. Febrifugal and antiinflammatory action is expressed much more weakly. The action mechanism connected with non-selective blockade of TsOG-1 and TsOG-2 which catalyze formations of prostaglandins from arachidonic acid is the main factors of development of pain. Drug completely stops pain of low and average intensity, and to transfer pain of high intensity to low.
Influence of drug begins in one hour, reaches a maximum in 2–3 hours and continues from 8 to 12 hours.
Pharmacokinetics. It is quickly soaked up in a digestive tract. Bioavailability – 80–100%. Time of achievement of the maximum concentration (TCmax) – 10-78 min. The maximum concentration in blood (Cmax) after oral administration of 10 mg – 0, 82-1, 46 mkg/ml. Communication with proteins of plasma – 99%.
Time of achievement of Css after oral administration of 10 mg – 0, 39–0,79 mkg/ml – the 24th hour at appointment 4 times a day
Distribution volume – 0,15–0, 33 l/kg. At patients with a renal failure the volume of distribution of drug can increase twice, and the volume of distribution of its R-enantiomera – by 20%.
Gets into breast milk: at reception by mother of 10 mg of a ketorolak (Cmax) in milk it is reached in 2 hours after reception of the first dose and makes 7, 3 ng/ml, in 2 hours after use of the following dose of a ketorolak (when using drug 4 times for days) – 7, 9 ng/l. More than 50% of the accepted dose are metabolized in a liver with formation pharmacological of inactive metabolites. The main metabolites is glucuronides which are removed by kidneys, and r-gidroksiketorolak. 6% – through intestines are brought to 91% by kidneys.
Elimination half-life (T1/2) at patients with normal function of kidneys – on average 2, 4–9 hour after oral administration of 10 mg. T1/2 grows in elderly patients and decreases at young people. Function of a liver does not make influence on T1/2. At patients with a renal failure at concentration of creatinine in plasma of 19-50 mg/l
(168 – 442 µmol/l) T1/2 – 10, 3–10, 8 hour, at more expressed renal failure – is more than 13, 6 hour's.
The general clearance makes at oral administration 10 mg – 0,025 l/hour on body weight kg; at patients with a renal failure at concentration of creatinine in plasma of 19-50 mg/l – 0,016 l/hour on body weight kg.
It is not removed by a hemodialysis.
Main physical and chemical properties: tablets of rounded shape with an oboyevypukly surface, white color, with a weak yellowish shade.
Incompatibility. It is undesirable to mix drug with other medicines.
Period of validity. 2 years.
Storage conditions. To store in original packaging, in the place, unavailable to children, at a temperature not above 25 °C.