Ketorolak

Ketorolak – drug with analgeziruyushchy, febrifugal and antiinflammatory action.

Form of release and structure

Ketorolak release in the following dosage forms:

• Solution for intravenous and intramuscular administration: yellowish color, transparent (on 1 ml in ampoules, on 5, 10 ampoules in pallets, on 1 or 2 pallets in a cardboard pack; on 2 ml in dark glass ampoules, on 10 ampoules in a cardboard pack);
• Solution for intramuscular introduction: transparent, light yellow color (on 1 ml in ampoules, on 5 ampoules in pallets, on 1 or 2 pallets in a cardboard pack or on 5 or 10 ampoules in a cardboard pack; on 2 ml in dark glass ampoules, on 10 ampoules in a cardboard pack);
• Tablets (on 10 pieces in blister strip packagings, on 1, 2, 5, 10 packagings in a cardboard pack; on 20 pieces in blister strip packagings, on 1 packaging in a cardboard pack; on 25 pieces in blister strip packagings, on 2, 4 packagings in a cardboard pack; on 10 pieces in polymeric banks, after 1 bank in a cardboard pack);
• Tablets, coated: white, biconvex (on 10 pieces in blister strip packagings, on 1-3, 5 packagings in a cardboard pack);
• Tablets, film coated: biconvex, round, almost white or white; on cross section two layers are visible (on 10 pieces in blister strip packagings, on 1-5, 10 packagings in a cardboard pack; on 20, 100 pieces in banks, after 1 bank in a cardboard pack).

For intravenous and intramuscular administration enters into structure of 1 ml of solution:

• Active agent: a ketorolaka трометамол – 30 mg (a ketorolaka трометамин);
• Auxiliary components: sodium chloride, эдетат dinatrium (salt disodium ethylene diamine-N, N,N', N' - tetraacetic acid 2-water (Trilonum of B)), water for injections.

For intramuscular introduction is a part of 1 ml of solution:

• Active agent: a ketorolaka трометамол – 30 mg;
• Auxiliary components: a dihydrate of an edetat of dinatrium (Trilonum of B), ethanol (alcohol in terms of anhydrous), propylene glycol, sodium chloride, sodium hydroxide (1M solution), water for injections.

Active agent is a part of 1 tablet: a ketorolaka трометамин – 10 mg.

In structure of 1 tablet, coated, enters:

• Active agent: a ketorolaka трометамол – 10 mg (a ketorolaka трометамин);
• Auxiliary components: lactose, potato starch, microcrystallic cellulose, calcium stearate, Opadry II.

In structure of 1 tablet, film coated, enters:

• Active agent: a ketorolaka трометамол – 10 mg (a ketorolaka трометамин);
• Auxiliary components: microcrystallic cellulose, magnesium stearate, talc, кросповидон (коллидон TsL), milk sugar (monohydrate of lactose).

Structure of a cover: oksipropilmetiltsellyuloz (gipromelloz), titanium dioxide, talc, propylene glycol, macrogoal 4000 (poly(ethylene oxide) 4000, polyethyleneglycol 4000).

Indications to use

Ketorolak appoint at a pain syndrome of moderate and strong expressiveness, including injuries, a dentagra, pains during the postoperative period, oncological diseases, a mialgiya, neuralgia, an arthralgia, radiculitis, rheumatic diseases, stretchings, dislocations.

Ketorolak does not render influence on progressing of a disease. Drug should be used only for a symptomatic treatment, reduction of an inflammation and pain at the time of use.

Contraindications

• The rhinitis, urticaria caused by reception of non-steroidal anti-inflammatory drugs (in the anamnesis);
• Full or partial combination recuring polypose of okolonosovy bosoms and a nose and bronchial asthma with intolerance of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);
• Dehydration, hypovolemia (regardless of the reason, it caused);
• Intolerance of drugs of a pyrazolon row;
• Bleedings, high risk of their emergence;
• The confirmed hyperpotassemia;
• State after performing aortocoronary shunting;
• Digestive tract erosive cankers (at an aggravation), round ulcers;
• Inflammatory diseases of intestines;
• Hypocoagulation (including hemophilia);
• Heavy renal failure (at clearance of creatinine it is less than 30 ml in a minute);
• The hemorrhagic stroke (suspected or confirmed);
• Active diseases of a liver or heavy liver failure;
• Hemopoiesis disturbance;
• Hemorrhagic diathesis;
• Age up to 16 years (efficiency and safety of use of drug for this age group of patients are not established);
• Pregnancy and period of breastfeeding (lactation);
• Childbirth;
• Hypersensitivity to components of drug and other non-steroidal anti-inflammatory drugs.

For treatment of chronic pains drug should not be used.

Because of high risk of development of bleeding Ketorolak do not apply as means to the supporting anesthesia, premedication, and also anesthesia before and during surgeries (including obstetric practice).

Ketorolak it is necessary to apply with care at the following diseases / states:

• Arterial hypertension;
• Bronchial asthma;
• Chronic heart failure;
• Cholecystitis;
• Functional disturbances of kidneys (at creatinine of plasma it is lower than 50 mg/l);
• Cholestasia;
• Sepsis;
• Active hepatitis;
• System lupus erythematosus;
• Polyps of a mucous membrane of a nasopharynx and nose, concomitant use with other non-steroidal anti-inflammatory drugs;
• Cerebrovascular diseases;
• Existence of the factors increasing toxicity of digestive tract including tobacco smoking and alcoholism;
• Edematous syndrome;
• Postoperative period;
• Lipidemia / дислипидемия;
• Coronary heart disease;
• Diseases of peripheral arteries;
• Diabetes mellitus;
• The clearance of creatinine is less than 60 ml in a minute;
• Digestive tract cankers in the anamnesis;
• Helicobacter pylori infection;
• Heavy somatopathies;
• Advanced age (65 years are more senior);
• Long use of non-steroidal anti-inflammatory drugs;
• Concomitant use of peroral glucocorticosteroids (including Prednisolonum), antiagregant (including klopidogret), anticoagulants (including warfarin), selective serotonin reuptake inhibitors (including tsitalopra, пароксетин, fluoxetine, sertraline).

Route of administration and dosage

Ketorolak in the form of tablets accept inside.

Depending on weight of a pain syndrome drug is used once (in a dose of 10 mg) or repeatedly (on 10 mg to 4 times a day).

The maximum daily dose – 40 mg.

Ketorolak's solution is entered deeply intramusculary or intravenously (struyno) slowly (not less than 15 seconds) in the smallest effective doses which select depending on intensity of pain and reaction of the patient. If necessary perhaps simultaneous use with opioid analgetics in the reduced doses.

Depending on weight of a pain syndrome the adult single dose at single introduction (intramuscular or intravenous) makes 10-30 mg. To patients 65 years are more senior or at functional disturbances of kidneys usually appoint 10-15 mg.

At repeated parenteral administration of Ketorolak apply the following modes of dosing:

• Intramuscular introduction: adults up to 65 years and children of 16 years – 10-60 mg in the first introduction, then – each 6 hours on 10-30 mg (usually – on 30 mg); elderly patients (of 65 years) or at functional disturbances of kidneys – each 4-6 hours on 10-15 mg;
• Intravenous administration: adults up to 65 years and children of 16 years – 10-30 mg struyno in the first introduction, then – each 6 hours on 10-30 mg, an initial dose at continuous infusion by means of an infuzomat – 30 mg, then the speed of infusion makes 5 mg an hour; elderly patients (of 65 years) or at functional disturbances of kidneys – each 6 hours struyno on 10-15 mg.

The maximum daily dose of Ketorolak at intramuscular and intravenous administration makes:

• Adults up to 65 years and children of 16 years – 90 mg;
• Elderly patients (of 65 years) or at functional disturbances of kidneys – 60 mg.

Continuous intravenous infusion should not continue longer than 24 hours.

Course duration at Ketorolak's reception inside and at parenteral administration should not be longer than 5 days.

Upon transition from intramuscular and intravenous administration to reception Ketorolaka inside the total daily dose in day of transfer should not be more:

• Adults up to 65 years and children of 16 years – 90 mg;
• Elderly patients (of 65 years) or at functional disturbances of kidneys – 60 mg.

At the same time in day of transition the drug dose in the form of tablets should not be more than 30 mg.

Side effects

During Ketorolak's use development of disturbances from some systems of an organism which are shown with various frequency is possible (it is frequent –> 3%; less often – 1-3%; seldom – < 1%):

• Central and peripheral nervous system: often – drowsiness, dizziness, a headache; seldom – aseptic meningitis (including spasms, fever, a severe headache, muscle tension of a back and/or neck), a hyperactivity (including concern, changes of mood), a depression, hallucinations, psychosis;
• Respiratory system: seldom – диспноэ, a bronchospasm, a fluid lungs, rhinitis, throat hypostasis (including an asthma, breath difficulty);
• Cardiovascular system: less often – increase in arterial pressure; seldom – a syncope;
• Alimentary system: often (especially at patients 65 years with digestive tract erosive cankers in the anamnesis are more senior) – diarrhea, a gastralgia; less often – a meteorism, stomatitis, vomiting, a lock, feeling of overflow of a stomach; seldom – nausea, a loss of appetite, digestive tract erosive cankers (including with bleeding and/or perforation – a melena, abdominal pain, burning or a spasm in epigastric area, nausea, vomiting with blood or as "a coffee thick", heartburn), a hepatomegalia, cholestatic jaundice, acute pancreatitis, hepatitis;
• Coagulant system of blood: seldom – rectal and nasal bleeding, bleeding from a postoperative wound;
• System of a hemopoiesis: seldom – an eosinophilia, anemia, a leukopenia;
• Urinary system: seldom – a back pain, an acute renal failure, an azotemia, a hamaturia, a gemolitiko-uraemic syndrome (a renal failure, hemolitic anemia, a purpura, thrombocytopenia), increase or decrease in volume of urine, the speeded-up urination, hypostases of renal genesis, nephrite;
• Integuments: less often – a purpura, skin rash (including makulopapulezny); seldom – exfoliative dermatitis (including fever with/without fever, reddening, a peeling or consolidation of skin, morbidity and/or swelling of palatine tonsils), a Lyell's disease, Stephens-Johnson's syndrome, a small tortoiseshell;
• Sense bodys: seldom – a ring in ears, decrease in hearing, a vision disorder (including an illegibility of visual perception);
• Local reactions: less often – pain or burning in an injection site;
• Allergic reactions: seldom – anaphylactoid reactions or an anaphylaxis (including face skin discoloration, skin rash, a small tortoiseshell, диспноэ or a tachypnea, a skin itch, periorbital hypostasis, hypostases a century, the complicated breath, an asthma, goose breathing, weight in a thorax);
• Others: often – increase in body weight, hypostases (including anklebones, the person, fingers, shins, a foot); less often – the increased perspiration; seldom – fever, a paraglossa.

Special instructions

At simultaneous use of Ketorolak with other non-steroidal anti-inflammatory drugs the liquid delay, development of a decompensation of cordial activity, arterial hypertension can be observed.

For decrease in risk of development of the gastropathies connected using non-steroidal anti-inflammatory drugs appoint мизопростол, antacids, омепразол.

Influence on aggregation of thrombocytes after Ketorolak's use remains within 24-48 hours.

The hypovolemia increases risk of development of side effects from kidneys.

Along with paracetamol it is not necessary to apply Ketorolak longer than 5 days.

To patients with blood coagulation disturbance drug is appointed only at constant control of number of thrombocytes, especially in the postoperative periods demanding careful control of a hemostasis.

Because at a considerable part of patients during therapy side effects from the central nervous system (a headache, dizziness, drowsiness) develop performance of work, the requiring high attention and bystry reactions (work with mechanisms, driving of motor transport), it is not recommended.

Medicinal interaction

At simultaneous use of Ketorolak with some medicines there can be undesirable effects:

• Acetylsalicylic acid or other non-steroidal anti-inflammatory drugs, glucocorticosteroids, calcium drugs, ethanol, corticotropin: formation of ulcers of digestive tract and development of gastrointestinal bleedings;
• Paracetamol: increase in nephrotoxicity;
• Methotrexate: increase gepato-and nephrotoxicity (the concomitant use is possible only at its use in low doses at control of concentration in a blood plasma);
• Methotrexate, lithium: reduction of their clearance and strengthening of toxicity;
• Indirect anticoagulants, heparin, trombolitik, antiagregant, цефоперазон, цефотетан and пентоксифиллин: increase in risk of development of bleeding;
• Probenetsid and the drugs blocking canalicular secretion: decrease in clearance of Ketorolak and increase in its concentration in a blood plasma;
• Hypotensive and diuretic drugs: decrease in their effect;
• Opioid analgetics: strengthening of their action (doses can be significantly reduced);
• Insulin and peroral hypoglycemic drugs: strengthening of hypoglycemic action (recalculation of a dose is necessary);
• Valproic acid: disturbance of aggregation of thrombocytes;
• Verapamil, nifedipine: increase in their concentration in a blood plasma;
• Other nefrotoksichny medicines (including gold drugs): increase in risk of development of nephrotoxicity;
• Miyelotoksichny medicines: strengthening of manifestation of a gematotoksichnost of drug.

Ketorolak in the form of solution for injections to mix in one syringe with morphine sulfate, Hydroxyzinum and promethazine does not follow (because of loss of a deposit).

Ketorolak pharmaceutical is incompatible with drugs of lithium and solution of a tramadol; let's combine from 5% solution of a dextrose (glucose), 0,9% chloride sodium solution, Plazmalit solution, Ringera-laktata solution and Ringera, and also with infusion solutions with the maintenance of Aminophyllinum, hydrochloride of lidocaine, a hydrochloride of a dopamine, insulin of the person of short action and heparin of sodium salt.

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 25 °C.

Period of validity:

• Tablets – 3 years;
• Solution for intravenous and intramuscular administration – 2 years.