Ketorol ®

General characteristics. Structure:

Each tablet, coated contains: active ingredient - a ketorolaka трометамин 10 mg; excipients - microcrystallic cellulose of 132 mg, peptized starch of corn 30 mg, starch of corn 12.5 mg, silicon dioxide of colloid 1 mg, magnesium stearate of 1.5 mg.

Pharmacological properties:

Pharmacodynamics. кеторолак, being non-steroidal anti-inflammatory drug, has soothing, febrifugal and antiinflammatory effect. The action mechanism at the biochemical level - cyclooxygenase enzyme oppression mainly in peripheral fabrics, is a consequence of what braking of biosynthesis of prostaglandins - modulators of painful sensitivity, thermal control and an inflammation. Ketorolak represents racemic mix [-] of S and [+) P enantiomer at the same time anesthetizing action is caused [-] S by a form. Drug does not influence opioid receptors, does not oppress breath, does not oppress motility of intestines, does not possess sedative and anxiolytic action, does not cause medicinal dependence. Ketorolak oppresses aggregation of thrombocytes and increases a bleeding time. The functional condition of thrombocytes is recovered in 24-48 hours after drug withdrawal.

Pharmacokinetics. Bioavailability of a ketorolak after intake makes from 80% to 100%. The maximum concentration in plasma is reached within 30-60 minutes. The pharmacokinetics of a ketorolak in the conditions of purpose of sredneterapevtichesky doses represents linear function. Equilibrium concentration of drug in plasma for 50% exceeds the similar indicator defined after a single dose. More than 99% of drug contact proteins of a blood plasma, the volume of distribution as a result seeming makes less than 0.3 l/kg.
Ketorolak is metabolized mainly with formation of the conjugated forms of glucuronic acid which are removed through kidneys. Metabolites have no analgesic activity. The elimination half-life of drug averages 5 hours.

Indications to use:

Short treatment of a pain syndrome of average and strong intensity, mainly, at injuries, in the postoperative period, at a radicular syndrome, muscular pains.

Route of administration and doses:

Duration of a course of use of a ketorolak should not exceed 7 days, long reception, and also intake in a dose more than 40 mg a day is not recommended.
Adults: 10 mg each 4 or 6 hours in process of the requirement. A total daily dose upon transition from parenteral administration of drug to intake of 90 mg (60 mg for elderly patients, patients with a renal failure, patients whose weight less than 50 kg), a part of the dose appointed inside at the combined introduction should not exceed 40 mg in day of change of a form of introduction.
Elderly patients: it is recommended to extend intervals between administrations of drug, i.e. 6-8 hours. To patients 65 years are more senior it is recommended to appoint the drug dose corresponding to the lower bound therapeutic.

Features of use:

Appointment to patients with the broken function of a liver: it is appointed with care. During reception of a ketorolak increase in level of enzymes of a liver is possible. In the presence of functional deviations from a liver against the background of reception of a ketorolak development of heavier pathology is possible. At identification of symptoms of pathology of a liver treatment should be stopped.
To patients with a renal failure or diseases of kidneys in the anamnesis: кеторолак it is appointed, being careful.
Appointment to elderly patients: as at patients of this age group side reactions develop more often, it is necessary to use a minimal effective dose (the daily therapeutic dose no more than 60 mg for patients is more senior than 65 years).
Pregnancy and lactation: efficiency and safety are not established.
Food: reduces speed, but absorption of a ketorolak does not influence volume.
Influence on indicators of laboratory researches: increase in a bleeding time at a research of indicators of coagulability is possible.
As at a considerable part of patients at purpose of a ketorolak side effects from the central nervous system (drowsiness, dizziness, a headache) develop it is recommended to avoid performance of work, the requiring special attention and bystry reaction.

Preventions and precautionary measures
Before introduction of a ketorolak it is necessary to eliminate a hypovolemia and a hypoproteinemia, and also to recover water and electrolytic balance.
Delay in an organism of liquid, chloride sodium, the oliguria, increase in concentration of an urea nitrogen and creatinine in plasma were observed at conduct of clinical trials in this connection it is necessary to appoint with care кеторолак to patients with heart failure, arterial hypertension or morbid conditions with similar manifestations.
As кеторолак exerts impact on aggregation of thrombocytes, use for patients with pathology of system of a blood coagulation has to be controlled carefully. With extreme care it is appointed кеторолак along with anticoagulants.

Side effects:

Most often there are gastrointestinal frustration among which more than at 10% of patients nausea, pains in a stomach and intestines, dyspepsia are noted; quite often there is a diarrhea (7%). From the central nervous system disturbances in the form of a headache (17%), drowsiness (6%), dizziness (7%) are characteristic. Hypostases develop in 4% of cases.

Slightly more rare, but more than at 1% of patients hypertensia, a skin itch, rash, stomatitis, vomiting, locks, a meteorism, feeling of weight in a stomach, perspiration and hemorrhagic rash develop. Less than at 1% of patients weight reduction of a body, fever, an adynamy are possible; heartbeat, pallor of integuments, faints; skin rash; gastritis, proctorrhagias, loss or increase in appetite, eructation; nasal bleedings, anemia, eosinophilia, tremor, sleep disorders, hallucinations, euphoria, extrapyramidal syndromes, paresthesias, depression, nervousness, thirst, dryness mucous mouth, vision disorder, deterioration in attention, hyperkinesias, stupor; asthma, fluid lungs, rhinitis, cough; hamaturia, proteinuria, oliguria, ischuria, polyuria, increase of an urination.

Cases of reactions of hypersensitivity are noted (in the form of an anaphylaxis, anaphylactoid reaction, hypostasis of a throat, a paraglossa); hypotension and rushes of blood to skin; Lyell's disease, Stephens-Johnson's syndrome, exfoliative dermatitis, makulo-papular rash, small tortoiseshell; formation of ulcers in a mucous membrane of a stomach, gastrointestinal bleedings, perforation of walls of bodies of digestive tract, a melena, acute pancreatitis; postoperative wound bleedings, thrombocytopenia, leukopenia; hepatitis, liver failure, cholestatic jaundice; spasms, psychoses, aseptic meningitis; bronchospasm, acute renal failure, pains and areas of kidneys, hamaturia and azotemia, hyponatremia, hyperpotassemia, hemolitic uraemic syndrome.

For the prevention of possible side effects it is necessary to aim to use drug minimal effective doses, to observe precisely set dosages and the modes of introduction, to consider a condition of the patient (age, function of kidneys, a condition of digestive tract, water and electrolytic exchange and system of a hemostasis), and also possible medicinal interactions at a combination therapy.

Interaction with other medicines:

Ketorolak slightly reduces extent of linkng with proteins of warfarin.
In the researches in vitro influence of therapeutic doses of salicylates on extent of linkng of a ketorolak with proteins of plasma towards decrease from 99.2% to 97.5% is shown.
At a combination to furosemide weakening of its diuretic action approximately for 20% is possible.
Probenetsid reduces plasma clearance and the volume of distribution of a ketorolak increases its concentration in a blood plasma and increases the period of its semi-removal. Against the background of use of a ketorolak reduction of clearance of a methotrexate and lithium and strengthening of toxicity of these substances is possible.
The possible interaction of a ketorolak and not depolarizing muscle relaxants leading to development of an apnoea is noted.
It is not excluded that simultaneous use with APF inhibitors can increase risk of a renal failure.
Exceptional cases of development of convulsive attacks at a combination of a ketorolak to anticonvulsant drugs (Phenytoinum, carbamazepine) are described.
Developing of hallucinations against the background of a concomitant use of a ketorolak and psychogogic drugs is possible (флюоксетин, тиотиксен, to alprazola).

Contraindications:

Bronchial asthma, full or partial syndrome of nasal polyps, bronchospasm, Quincke's disease in the anamnesis.
Peptic ulcer of a stomach and duodenum in the period of an aggravation, and also existence in the anamnesis of an ulcer or gastrointestinal bleeding, existence either suspicion of gastrointestinal or intracranial bleeding.
Disturbance of a blood coagulation in the anamnesis, states with high risk of bleedings, hemorrhagic diathesis, coagulopathies, a hemorrhagic stroke, therapy by heparin in low doses. Operative measures with high risk of bleeding or risk of its incomplete stop.
Moderate and heavy renal failure (plasma creatinine more than 50 mg/l), risk of a renal failure, hypovolemia, dehydration.
Pregnancy, patrimonial period and period of feeding by a breast.
Hypersensitivity to a ketorolak, aspirin, other NPVS or any component of drug.
Concomitant use of other NPVP (risk of summation of side effects)
Age up to 16 years
Congestive heart failure
Drug is not used for anesthesia before and during surgeries.
Ketorolak is not applied to epidural and intrathecal introductions.

Overdose:

The overdose of a ketorolak at single or repeated use is usually shown by pains in a stomach, emergence of round ulcers of a stomach or erosive gastritis, a renal failure, a hyperventilation, a metabolic acidosis, the listed symptoms recover after the termination of administration of drug. In these cases the gastric lavage, administration of adsorbents is recommended (absorbent carbon) and performing symptomatic therapy. Ketorolak is not brought sufficiently by means of dialysis.

Storage conditions:

At a temperature to 25ºС. Period of validity: 3 years.

Issue conditions:

According to the recipe

Packaging:

Packaging: 10 tablets in a strip, 2 strips are packed into a cardboard box with the application instruction.