Several versions of Ketorol are produced: in ampoules - a substance for injective administration, in aluminum tubes - an ointment for topical application, in blisters - tablets for oral administration. The specific option is chosen by the doctor, based on the characteristics and needs of the patient. It is possible to combine external and internal use. Sometimes a course of injections is first prescribed, then the medication is replaced with a tablet form. The key to successful treatment is strict adherence to the doctor's instructions.
General information
In ampoules "Ketorol" is contained in the form of a specific solution intended for injection into muscle tissue. The substance is colorless or slightly yellowish. The solution should be transparent; when studying with the naked eye, it is impossible to see individual particles. In case of violation of the structure of the drug, precipitation or a change in color to another medication, it cannot be used, it must be disposed of. The use of a spoiled substance is a risk to the he alth and life of the patient.
In the ampoule "Ketorol" is contained in an amount of 1 ml,of which the active ingredient is 30 mg. The main compound is ketorolac tromethamine. As additional manufacturer applied:
- sodium chloride and hydroxide;
- ethanol;
- purified treated water;
- propylene glycol;
- edetate disodium;
- octoxynol.
Ampoules with "Ketorol" are made of tinted glass, packed in blisters. One contour package contains a dozen ampoules. The blisters are placed in cardboard boxes, which indicate the name of the drug, the amount of the drug inside, the concentration of the active compound in one ampoule. On the outside, the name of the manufacturer, the rules for dispensing funds from pharmacies, the expiration date and date of production, the conditions under which the substance should be stored are also indicated.
Ketorol: what is it?
Ketorol produced in ampoules has an analgesic effect that suppresses inflammatory foci. The drug belongs to the number of anti-inflammatory nonsteroidal drugs, that is, it does not contain hormonal substances. Ketorolac, on which the drug is based, has a pronounced analgesic effect. The tool inhibits inflammation, reduces fever. The latter quality is rated as moderate.
Ketorol, an anesthetic produced in ampoules, acts due to the ability of ketorolac to indiscriminately inhibit the activity of enzymes - the first, second COX. The most pronounced processes occur in peripheral tissues. Slows down the production of prostaglandinssubstances that cause pain, as well as those responsible for local temperature regulation and the activity of inflammatory processes. Ketorolac is a mixture of several types of enantiomers, one of which, as scientists have proven, has a pronounced analgesic effect on the human body.
According to the instructions for use, Ketorol injections (in ampoules - liquid for injection into the muscle) are relatively safe, since the active ingredient does not interact with opioid receptors. Under the influence of non-steroidal anti-inflammatory, the activity of the respiratory system does not slow down. The absence of dependence on the agent has been proven. "Ketorol" is not characterized by sedative, anxiolytic effects. The severity of the analgesic effect allows you to compare the substance with morphine. "Ketorol" is much stronger than other anti-inflammatory nonsteroidal drugs available to modern man.
The manufacturer points to Ketorol produced in ampoules in the instructions for use: the intramuscularly administered drug acts already 30 minutes after the injection. The most pronounced effect is an hour or two after the procedure.
Kinetics
With the introduction of "Ketorol" produced in ampoules intramuscularly, the bioavailability of the active component reaches 100%. Shortly after injection, the main compound is absorbed from the injection site. Ketorolac penetrates into the systemic circulation. When using 30 mg of the active compound, the maximum concentration in the blood plasma reaches an average of 3.1 μg / ml. At twice the dose, the parameter canrise to 5.77 mcg/ml. To achieve such indicators when using 30 mg, 15-73 minutes are enough, for twice the dosage, the time period is from half an hour to an hour.
With plasma proteins, as indicated in the instructions for use intramuscularly "Ketorol" (ampoules sold in pharmacies contain a solution for such injections), it is indicated that ketorolac is able to enter into strong bonds with plasma proteins. On average, 99% of the total substance that enters the body is involved in such a reaction. There may be an increase in the free connection in the circulatory system against the background of hypoalbuminemia.
The use of Ketorol, produced in ampoules, intramuscularly makes it possible to achieve an equilibrium concentration of Ketorolac in the circulatory system with a four-time use of the drug per day already 24 hours after the start of the therapeutic course. When using the substance in doses of 15 mg, the equilibrium concentration reaches 1.13 μg / ml, with twice as much - 2.47 μg / ml. The volume of distribution is estimated at 0.15-0.33 L/kg.
Ketorolac has been found to pass into breast milk. The manufacturer indicates this when describing the features of the application. "Ketorol" (in ampoules - solution for intramuscular injection), used in an amount of 10 mg four times a day, causes an increase in the content of ketorolac in breast milk to 7.3 ng / ml a couple of hours after the administration of the substance. A couple of hours after repeating the procedure, the maximum concentration of ketorolac in milk reaches 7.9 ng / ml.
What happens in the body?
For Ketorol produced in ampoules, use is allowed strictly under the supervision of a doctor. The doctor takes into account that about half of all the medication received by the patient is transformed in the liver. The metabolites formed in this case do not have pharmacological activity, but the very fact of metabolism in the liver forces one to prescribe the drug with caution if functional disorders or organ pathologies are suspected. Ketorolac processing products - glucuronides, hydroxyketorolac.
Ketorolac excretion is mainly carried out through the kidneys. Thus, up to 91% of the substance is excreted from the body. The route of elimination of approximately 6% of the substance is the intestinal tract. Glucuronides are eliminated in urine.
The half-life is estimated at 5.3 hours if the kidneys are functioning normally. In the instructions contained in the package with Ketorol ampoules, the manufacturer necessarily indicates that the interval varies from 3.5 to 9.2 hours when an injection is made with 30 mg of the active compound. This information must be taken into account when choosing the dosage and frequency of administration for a particular patient.
When injected, the clearance reaches 0.023 l/kg/h. The instructions attached to the Ketorol ampoules indicate that such indicators are characteristic of a single injection of a solution containing 30 mg of Ketorolac.
Special Occasion
Doctors, prescribing injections of a solution from Ketorol ampoules, choose the dosage, taking into account the individual characteristics of the case. In particular, in case of renal failure, it is necessary to change the dosage, the frequency of injections, since there is a risk of increasingtwice the volume of distribution relative to the norm. The volume of distribution of the active enantiomer, which is responsible for the analgesic effect, may increase by 20%.
The half-life of ketorolac in young patients is less than average, in the elderly it is longer. It was found that it is usually not necessary to adjust the dose when using a solution from Ketorol ampoules if the liver is malfunctioning, since the functioning of this organ does not affect the half-life. In a particular case, it is possible that a change will still be needed if other characteristics of the patient's body require it.
In case of impaired renal function, an assessment of creatinine clearance of 19-50 mg / l, the half-life of ketorolac reaches 10.8 hours. If the failure of the kidneys is even more pronounced, the time interval exceeds 13.6 hours.
With creatinine clearance in the range of 19-50 mg / l, the clearance of ketorolac is estimated at 0.015 l / kg / h, if the agent is used in an amount of 30 mg. For the elderly, the average is 0.019 l/kg/h.
Hemodialysis is ineffective when it is necessary to remove the active substance from the body.
Features of use
You can buy a medicine only if the patient has a prescription for Ketorol in ampoules. Free distribution of the drug from pharmaceutical points of sale is prohibited, since improper use can cause serious negative consequences.
"Ketorol" is prescribed if the patient is concerned about pain, assessed as an average, high level. The drug is effective in pain syndrome of different origin. It is prescribed during the rehabilitation period after surgery. For the use of "Ketorol" in ampoules, the indications are oncological diseases, accompanied by severe pain. You can use non-steroidal anti-inflammatory drugs only after prior consultation with the doctor. It is important to inject the substance correctly, otherwise there is a risk of local damage.
Sometimes patients ask, using "Ketorol" in ampoules, you can drink alcoholic beverages or it is forbidden. The manufacturer of the product draws attention: the combination of medication and alcohol is categorically not recommended.
Nuances of therapy
Ketorol is sold in ampoules according to the prescription of the attending doctor. The agent is used in the minimum dosage that gives the desired result. The selection of volumes must be carried out in practice. The drug is injected deep into the muscle tissue. Specific doses are chosen based on the strength of the pain, the body's response to the anti-inflammatory agent. If "Ketorol" is ineffective on its own, you can supplement the nonsteroidal drug with opioid painkillers. They are used in the smallest possible quantities.
For the treatment of adults under 65 years of age, Ketorol is used according to one of two programs:
- 10-30mg ketorolac once;
- 10-30mg with 4-6 hour intervals between treatments
The program is determined by the doctor, assessing the severity of pain.
From 65 years of age and older, as well as in case of failure of renal functionality, Ketorol is used in an amount of 10-15 mg. Mayberepeat every 4-6 hours if condition requires.
For persons under 65 years of age, the maximum daily dose of ketorolac is 90 mg. For older patients, as well as those suffering from impaired renal functionality, up to 60 mg is allowed.
As the reviews confirm, Ketorol ampoules are used for no more than five days. If it is necessary to continue the therapeutic course, the patient is transferred to an orally used form. On the day of changing the composition for persons under 65 years of age, 90 mg of ketorolac is allowed, of which no more than 30 mg are tablets. For persons over 65 years old - 60 mg, of which no more than half are tablets.
Side effects
"Ketorol" in ampoules - a solution intended for local injection into the muscle. Since the drug enters the body, it has a systemic effect, which determines possible side effects. Some occur relatively frequently. First of all, these are the consequences for the gastrointestinal tract - stool disorders and pain in the stomach. Such consequences are more often observed when using the drug by people over 65 years of age who have previously had an ulcer or erosion of the gastrointestinal tract.
Clinical trials show Ketorol injections can cause:
- jaundice, hepatitis, increased gas formation, nausea, vomiting, melena, stomatitis;
- kidney failure, lower back pain, anemia, thrombocytopenia, urinary urgency, nephritis, edema;
- bronchospasm, apnea, runny nose, swelling of the larynx;
- sick ordizziness, sleep cravings, meningitis, hallucinations, depression, psychosis, tinnitus, blurred vision and hearing;
- high blood pressure, fainting, pulmonary edema;
- anemia, leuko-, eosinophilia;
- bleeding;
- skin reactions, urticaria;
- anaphylactic, anaphylactoid response, tachy-, dyspnea, puffiness of the eyelids, shortness of breath, respiratory failure;
- burning, soreness at the injection site;
- activation of sweat glands;
- febrile condition.
Absolutely not allowed
Even if the patient's condition is on the list of those that Ketorol helps in ampoules, the use of the medication is unacceptable if asthma is detected, the attacks of which are provoked by acetylsalicylic acid and other non-steroidal anti-inflammatory drugs. Contraindications also include:
- bronchospasm;
- dehydration;
- hypovolemia;
- exacerbated ulcers, erosion of the gastrointestinal tract;
- angioedema;
- lack of liver and kidney function;
- established, suspected hemorrhagic stroke;
- peptic ulcer;
- too weak blood clotting ability;
- hemorrhagic diathesis;
- therapeutic course, including non-steroidal anti-inflammatory drugs;
- increased chance of bleeding;
- inhibition of hematopoietic function;
- carrying a child;
- birth;
- lactation;
- under 16 years of age;
- high level of susceptibility to ketorolac, othersfunds from the group of nonsteroidal anti-inflammatory.
Ketorol should not be used if the pain is chronic.
Special case: instructions for use
Reviews of "Ketorol" in ampoules (in this form of release, the medication is intended for injective administration) contain information that the remedy was sometimes prescribed to asthmatics. This is practiced if there is no more suitable and effective substance, while doctors have the opportunity to control the patient's condition, since the likelihood of side effects is higher than in the general case.
In the instructions for use, the manufacturer indicates the admissibility of administering an injection of ketorolac only if it is possible to control the condition of the persons of the following groups:
- hypertension patients;
- sepsis patients;
- older people (over 65).
Similar restrictions impose diagnoses:
- cholestasis;
- chronic heart failure;
- creatinine clearance less than 50 mg/l;
- lupus erythematosus;
- impaired renal function;
- active hepatitis;
- polyposis of the nasal mucosa, nasopharynx.
Ketorolac affects platelet aggregation one to two days after the last administration of the drug. Against the background of hypovolemia, the likelihood of adverse reactions increases. When combined with paracetamol, Ketorol can be used for up to five days, but no more. As needed, the drug is combined with opioid painkillers. In violation of blood clotting "Ketorol"allowed only if it is possible to control the number of platelets in the circulatory system. This is especially true for individuals who have recently undergone surgery. Hemostasis needs to be monitored.
Although "Ketorol" is a strong and effective tool, it also has a significant drawback: the predominant percentage of patients who used Ketorolac experienced any of the side effects. Since the percentage of occurrence of dizziness, craving for sleep and other effects on the central nervous system is quite high, work that requires increased concentration and reaction speed should be avoided during the therapeutic course of transport management.
Too much
Overdose symptoms may indicate the following:
- stomach hurts;
- vomiting, vomiting;
- ulcerative process in the gastrointestinal tract;
- gastritis;
- failures of kidney functionality;
- acidosis.
The patient is shown therapy in order to maintain functions important for life support. Dialysis does not show results, therefore it is not carried out.
About compatibility
The use of "Aspirin" and "Ketorol", as well as the combination of the drug with other non-steroidal anti-inflammatory drugs, ethanol, hormonal anti-inflammatory drugs, calcium drugs and corticotropin can cause ulcerative lesions of the gastrointestinal tract, bleeding in these organs.
Combination with paracetamol increases the risk of kidney poisoning. When combined with methotrexate, it is possible to increase the poisoningeffect on the kidneys and liver.
Injective administration of "Ketorol" can cause a weakening of the clearance of methotrexate, lithium, and therefore leads to an increase in toxicity. Such combinations are allowed only with the appointment of methotrexate in the minimum dosage and the ability to control its concentration in the blood plasma throughout the course.
Ketorolac clearance, its volume of distribution is reduced when the substance is combined with probenecid. At the same time, the concentration of ketorolac in the plasma component of the blood increases, the half-life period lengthens.
Combination with indirect anticoagulants may cause bleeding. A similar effect is possible if "Ketorol" is used simultaneously with the means of the following groups:
- thrombolytics;
- heparin;
- antiplatelet agents.
Increased risk of bleeding when combining Ketorolac and:
- cefoperazone;
- cefotetan;
- pentoxifylline.
Pay attention
Under the influence of Ketorolac, the effectiveness of diuretics, means to reduce pressure, is isolated. This is due to the inhibition of the production of prostaglandins by the kidneys.
Antacids do not correct the absorption of the active component of Ketorol.
The combination of the described injections and insulin leads to the activation of its hypoglycemic effect. A similar result is observed with a combination of ketorolac and means for adjusting the concentration of glucose taken orally. To prevent negative consequences, it is necessary to select an individual dosagefunds received.
"Ketorol" and preparations containing sodium valproate, in combination, can cause abnormal platelet aggregation. Against the background of the use of ketorolac, an increase in the content of nifedipine, verapamil in the blood plasma is possible. The combination with substances toxic to the kidneys leads to an increased likelihood of a poisoning effect on the organ. This also applies to the combination with gold preparations.
The use of drugs that inhibit tubular secretion causes a decrease in the clearance of ketorolac, which means that the content of this substance in the plasma component of the blood increases.
Important limitations
It is unacceptable to mix "Ketorol" and sulfate compounds of morphine, hydroxyzine, promethazine in a syringe. Such combinations may cause sedimentation.
Category it is forbidden to combine "Ketorol" and lithium preparations, tramadol - these substances are incompatible, as shown by specific studies.
Compatible solution for injective administration and saline. You can combine "Ketorol" and a five percent dextrose solution, solutions:
- Ringer-lactate;
- Ringer.
Compatible with infusion solutions containing:
- lidocaine;
- dopamine;
- aminophylline;
- insulin (short-term effect);
- heparin in the form of sodium s alt.
Will it help?
Patients to whom the doctor prescribes "Ketorol" often doubt whether to use this remedy:the likelihood of side effects is quite high, but will there be a result from it? In the reviews of people who used Ketorol for intramuscular injection, one can see unequivocal confirmation of the fact that the remedy is effective. Patients who received painkiller injections noted that the analgesic result was pronounced, so the effectiveness of the injection, in their opinion, is more significant than the negative consequences of using the medication.
What to replace
Take into account when choosing analogues: "Ketorol" in ampoules, tablets and forms for external use (ointment, gel) is based on ketorolac. The following preparations for injective administration have been created on the same active substance:
- Dolak.
- Ketanov.
- Ketorolac.
The cost of all the listed medicines is approximately the same, varies between 80-120 rubles. Specific price tags depend not only on the product, but also on the pricing policy of the point of sale.
Ketorol Alternative Tablets:
- Ketorolac.
- Ketanov.
- Dolak.
- Ketokam.
Price varies, depends on the product, the number of doses in the pack. Boxes containing 20 capsules cost just over 30 rubles, while pharmacies charge about 200 rubles for a pack of 100 tablets.
The most popular analogues: "Ketokam"
This remedy is based on Ketorolac and is available in tablet form. It is quite cheap, it is sold in almost any locality in our country, thereforeconsidered accessible to the general public. Often, it is his doctors who prescribe if the patient needs an anesthetic. The drug belongs to the class of anti-inflammatory non-steroidal, relieves pain, inhibits foci of inflammation. The effect on temperature is assessed as moderate.
The active compound "Ketokama", entering the patient's body, affects the COX produced from arachidonic acid. This allows you to correct the reaction of the formation of prostaglandins, under the influence of which inflammatory processes are activated, painful cider. Influence on prostaglandins allows you to eliminate the febrile state.
Shortly after the tablets enter the body, the active compound is absorbed into the circulatory system. Studies have shown that the maximum concentration in the plasma component is achievable in an average of 45 minutes. The absorption process is not corrected by meals. The ability of the active substance to bind to plasma proteins reaches 99%. The half-life is four to six hours.
Up to 90% of the drug that enters the body is eliminated with urine. About 60% is displayed unchanged. Other volumes leave the body through the intestinal tract.
In case of violation of renal functionality, when prescribing "Ketokam" to elderly people, you need to remember about lowering the rate of elimination. The time interval required for the half-life of the drug increases.
Reception features
"Ketokam" is prescribed if necessary to eliminatesevere or moderate pain syndrome. The drug is effective for painful sensations of various origins. For adult patients, the drug is recommended to use a 10 mg tablet with time intervals of 4-6 hours between doses. If necessary, it is allowed to double the volume using Ketocam three to four times daily.
The maximum daily dosage is 90 mg of the active compound. With a weight of less than 50 kg, impaired renal functionality, at the age of 65 years and older, Ketocam is indicated per day in an amount of no more than 60 mg.
