Several variants of the Ketorol preparation are available: in ampoules - a substance for injective administration, in aluminum tubes - ointment for local application, in blisters - tablets for oral administration. The doctor chooses a specific option based on the characteristics and needs of the patient. Combination of external and internal use is possible. Sometimes a course of injections is prescribed first, then the medication is replaced with a tablet form. The key to successful treatment is to strictly follow the doctorās instructions.
general information
In Ketorol ampoules it is contained in the form of a specific solution intended for introduction into muscle tissues. The substance is colorless or tinted to a yellowish tint. The solution should be transparent, when examined with the naked eye, it is impossible to see individual particles. In case of violation of the structure of the drug, precipitation or color change to another medication can not be used, it must be disposed of. The use of spoiled substances is a risk to the health and life of the patient.
In the ampoule "Ketorol" is contained in an amount of 1 ml, of which the active component is 30 mg. The main compound is Ketorolac tromethamine. As additional manufacturer applied:
- sodium chloride and hydroxide;
- ethanol;
- purified prepared water;
- propylene glycol;
- disodium edetate;
- octoxynol.
Ampoules with Ketorol are made of tinted glass, packaged in blisters. One contour package contains a dozen ampoules. Blisters are placed in cardboard boxes, which indicate the name of the medication, the amount of the drug inside, the concentration of the active compound in one ampoule. The name of the manufacturer, the rules for dispensing funds from pharmacies, the expiration date and production date, and the conditions under which the substance should be stored are also indicated on the outside.
Ketorol: what is it?
The action of Ketorol produced in ampoules is anesthetic, depressing inflammatory foci. The drug belongs to the number of anti-inflammatory non-steroidal agents, that is, it does not have hormonal substances in its composition. Ketorolac, on which the medication is based, has a pronounced analgesic effect. The tool inhibits inflammatory processes, reduces fever. The latter quality is rated as moderate.
The analgesic āKetorolā produced in ampoules acts due to the ability of ketorolac to selectively inhibit the activity of enzymes - the first, second COX. The processes are most pronounced in peripheral tissues. Slows down the production of prostaglandins, substances 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, of which one, 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 muscles) are relatively safe, since the active component does not interact with opioid receptors. Under the influence of non-steroidal anti-inflammatory activity of the respiratory system does not slow down. The absence of dependence on the drug has been proven. "Ketorol" is not characterized by soothing, anxiolytic effects. The severity of the analgesic effect allows you to compare the substance with morphine. āKetorolā is much stronger than other anti-inflammatory non-steroid medicines available to modern people.
The manufacturer points to the āKetorolā produced in ampoules in the instructions for use: the intramuscularly administered drug is effective 30 minutes after the injection. The most pronounced effect is an hour or two after the procedure.
Kinetics
With the introduction of āKetorolā produced in ampoules, the bioavailability of the active component intramuscularly reaches 100%. Shortly after the injection, the main compound is absorbed from the injection point. Ketorolac penetrates the systemic circulation. When using 30 mg of the active compound, the maximum concentration in blood plasma reaches an average of 3.1 Ī¼g / ml. With a twice as large dose, the parameter may increase to 5.77 Ī¼g / ml. To achieve such indicators when using 30 mg, 15-73 minutes are enough, for a twice as large dosage, the time period is from half an hour to an hour.
With plasma proteins, as indicated in the instructions for intramuscular administration of āKetorolā (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 all the substance received in the body is involved in such a reaction. An increase in the free compound in the circulatory system against the background of hypoalbuminemia is possible.
The use of Ketorol produced in ampoules intramuscularly allows you to achieve an equilibrium concentration of ketorolac in the circulatory system with a four-time use of the drug per day 24 hours after the start of the therapeutic course. When using a substance in doses of 15 mg, the equilibrium concentration reaches 1.13 Ī¼g / ml, with a twice as high - 2.47 Ī¼g / ml. The volume of distribution is estimated at 0.15-0.33 l / kg.
It was revealed that ketorolac passes into breast milk. The manufacturer indicates this, describing the features of the application. "Ketorol" (in ampoules - solution for injection intramuscularly), used in an amount of 10 mg four times a day, causes the ketorolac content in breast milk to increase to 7.3 ng / ml a couple of hours after the substance is administered. A couple of hours after repeating the procedure, the maximum concentration of ketorolac in milk reaches 7.9 ng / ml.
What is going on in the body?
For produced in ampoules "Ketorol" application 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 the drug to be prescribed with caution if impaired functionality or pathology of the organ are suspected. Ketorolac processing products - glucuronides, hydroxyketorolac.
The excretion of ketorolac is mainly carried out through the kidneys. Thus, up to 91% of the substance is excreted from the body. The elimination pathway of approximately 6% of the substance is the intestinal tract. Glucuronides are eliminated with urine.
The elimination half-life is estimated at 5.3 hours if the kidneys function normally. In the instructions contained in the package with Ketorol ampoules, the manufacturer must indicate that the interval varies from 3.5 to 9.2 hours when injected 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 the solution from Ketorol ampoules, choose the dosage, taking into account the individual characteristics of the case. In particular, with renal failure, a change in dosage, frequency of injection is necessary, since there is a risk of double the volume of distribution relative to the norm. The volume of distribution of the active enantiomer, which determines the analgesic effect, may increase by 20%.
The half-life of ketorolac in young patients is less than average, in old age is longer. It was found that usually it is not necessary to adjust the dose when applying the solution from Ketorol ampoules if the liver is malfunctioning, since the functioning of this organ does not affect the half-life. In a specific 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 period exceeds 13.6 hours.
With creatinine clearance within 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 value is 0.019 l / kg / h.
Hemodialysis is ineffective if it is necessary to remove the active substance from the body.
Features of use
You can buy medicine only if the patient has a prescription for Ketorol in ampoules. Free release 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 medium, high level. The drug is effective in pain syndrome of different origin. It is prescribed during the rehabilitation period after surgery. Indications for use of Ketorol in ampoules are oncological diseases, accompanied by severe pain. You can use a non-steroidal anti-inflammatory only after prior consultation with a doctor. It is important to enter the substance correctly, otherwise there is a risk of local damage.
Sometimes patients ask, using "Ketorol" in ampoules, is it possible to drink alcoholic beverages or it is forbidden. The manufacturer of the drug draws attention: the combination of medication and alcohol is strictly not recommended.
The nuances of therapy
Ketorol is sold in ampoules according to the prescription of the attending doctor. The tool is used in a minimum dosage, giving the desired result. The selection of volumes must be carried out in practice. The drug is injected deep into muscle tissue. Specific doses are selected based on the strength of the pain, the response of the body to an anti-inflammatory agent. If Ketorol is ineffective in itself, you can supplement the non-steroid drug with opioid painkillers. They are used in the smallest possible amounts.
For the treatment of adults under the age of 65, Ketorol is used in one of two programs:
- 10-30 mg of ketorolac once;
- 10-30 mg with intervals between treatments at 4-6 hours
The program is determined by the doctor, assessing the severity of pain.
From the age of 65 years and older, as well as in case of malfunction of the renal functionality, Ketorol is used in an amount of 10-15 mg. It is possible to repeat every 4-6 hours, if the condition requires it.
For persons under 65 years of age, the maximum dose of ketorolac per day is 90 mg. For patients older, as well as suffering from impaired renal functionality, it is allowed to use up to 60 mg.
According to reviews, in Ketorol ampoules are used no more than five days. If necessary, continue the therapeutic course, transfer the patient to an orally used form. On the day the composition is changed for people under 65, 90 mg of ketorolac is allowed, of which not more than 30 mg in tablets. For people over 65 years old - 60 mg, of which in tablets - no more than half.
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 the possible side effects. Some occur relatively frequently. First of all, these are the consequences for the gastrointestinal tract - disorders of the stool and pain in the stomach. Such consequences are more often observed when using the drug by people over 65 years old who have previously suffered an ulcer or erosion of the gastrointestinal tract.
Clinical trials have shown that Ketorol injections can cause:
- jaundice, hepatitis, gas, nausea, vomiting, melena, stomatitis;
- kidney failure, pain in the lower back, anemia, thrombocytopenia, increased frequency of urination, nephritis, edema;
- bronchospasm, apnea, runny nose, swelling of the larynx;
- sick or dizzy, craving for sleep, meningitis, hallucinations, depression, psychosis, tinnitus, impaired vision and hearing;
- high blood pressure, fainting, pulmonary edema;
- anemia, leukemia, eosinophilia;
- bleeding
- skin reactions, urticaria;
- anaphylactic, anaphylactoid response, tachy-, dyspnea, swelling of the eyelids, shortness of breath, respiratory failure;
- burning, soreness at the injection site;
- activation of sweat glands;
- fever.
Strongly impossible!
Even if the patientās condition is on the list of those that Ketorol helps in ampoules, the use of the medication is unacceptable if asthma is detected, attacks of which provoke acetylsalicylic acid and other non-steroidal anti-inflammatory drugs. Contraindications also include:
- bronchospasm;
- dehydration;
- hypovolemia;
- aggravated ulcers, gastrointestinal erosion;
- angioedema;
- failure of the liver, kidneys;
- established, suspected hemorrhagic stroke;
- peptic ulcer;
- blood coagulation too weak;
- hemorrhagic diathesis;
- therapeutic course, including non-steroidal anti-inflammatory;
- increased chance of bleeding;
- inhibition of hematopoietic function;
- bearing a child;
- childbirth;
- lactation;
- age younger than 16 years;
- high level of susceptibility of ketorolac, other drugs from the group of non-steroidal anti-inflammatory.
It is not allowed to use Ketorol if the pain syndrome 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 monitor 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 a ketorolac injection only if it is possible to control the condition of persons of the following groups:
- hypertension;
- patients with sepsis;
- elderly people (over 65 years of age).
Similar limitations apply to diagnoses:
- cholestasis;
- heart failure in a chronic form;
- creatinine clearance less than 50 mg / l;
- lupus erythematosus;
- impaired renal function;
- active hepatitis;
- polyposis of the nasal mucosa, nasopharynx.
Ketorolac affects platelet aggregation from one to two days after the last injection. Against the background of hypovolemia, the likelihood of adverse reactions increases. When combined with paracetamol "Ketorol" can be used up to five days, but not more. As needed, the drug is combined with opioid painkillers. In case of blood coagulation āKetorolā is allowed only if it is possible to control the number of platelets in the circulatory system. This is especially true for people who have recently undergone surgery. It is necessary to monitor hemostasis.
Although Ketorol is a powerful and effective drug, it also has a significant drawback: the predominant percentage of patients who have used Ketorolac have any of the side effects. Since the percentage of dizziness, craving for sleep, and other effects on the central nervous system is quite large, work that requires an increased concentration and reaction rate should be avoided during the therapeutic course of transport management.
Too much!
The following manifestations may indicate an overdose:
- I have a stomachache;
- vomiting, vomiting;
- ulcerative process in the gastrointestinal tract;
- gastritis;
- malfunctioning renal function;
- acidosis.
The patient is shown to undergo therapy in order to maintain functions that are important for life support. Dialysis does not show result, 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 preparations and corticotropin can cause gastrointestinal ulceration and bleeding in these organs.
The combination with paracetamol increases the risk of a toxic effect on the kidneys. When combined with methotrexate, an increase in the toxic effect on the kidneys and liver is possible.
Injective administration of Ketorol can cause a weakening of the clearance of methotrexate, lithium, and therefore leads to increased toxicity. Such combinations are allowed only with the appointment of methotrexate in the minimum dosage and the possibility of controlling its concentration in the blood plasma throughout the course.
The clearance of ketorolac, the volume of its distribution is reduced when a substance is combined with probenecid. At the same time, the concentration of ketorolac in the plasma component of the blood increases, the half-life is extended.
Combination with indirect anticoagulants can 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;
- cefotetane;
- pentoxifylline.
Note!
Under the influence of ketorolac, the effectiveness of diuretics, means to reduce pressure, is isolated. This is due to inhibition of kidney production of prostaglandins.
Antacids do not correct the absorption of the active component of Ketorol.
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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 can cause precipitation.
The category forbids combining Ketorol and lithium preparations, tramadol - these substances are incompatible, as specific studies have shown.
Injectable and physiological solution compatible. You can combine Ketorol and a five percent dextrose solution, solutions:
- Ringer-Lactate;
- Ringerās.
Compatibility with solutions for infusions containing:
- lidocaine;
- dopamine;
- aminophylline;
- insulin (short-term effect);
- heparin in the form of a sodium salt.
Will it help?
Patients to whom the doctor prescribes Ketorol often doubt whether it is worth using this remedy: the likelihood of side effects is quite high, but will there be any result from it? In the reviews of persons who used Ketorol for intramuscular administration, one can see unequivocal confirmation of the fact that the tool is effective. Patients who received anesthetics injections noted that the analgesic result was pronounced, therefore, the effectiveness of the injection, in their opinion, is more significant than the negative consequences of using the medication.
How to replace
Take into account when choosing analogues: "Ketorol" in ampoules, tablet and form for external use (ointment, gel) is based on ketorolac. The following drugs for injective administration were created on the same active substance:
The cost of all the medicines listed 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 Alternatives Available in Tablets:
- Ketorolac.
- Ketanov.
- Dolak.
- Ketokam.
The price varies, depending on the product, the number of doses in a pack. Boxes containing 20 capsules cost only a little more than 30 rubles, and about 200 rubles are asked for packaging with a hundred tablets in pharmacies.
The most popular analogues: "Ketokam"
This tool is based on ketorolac, available in tablet form. It is quite cheap, it is sold in almost any locality in our country, therefore it is considered affordable for the masses. Often, it is his doctors who prescribe if the patient needs an anesthetic. The medication belongs to the class of anti-inflammatory non-steroidal, relieves pain, inhibits foci of inflammation. The effect of influence on temperature is rated as moderate.
The active compound āKetokamaā, entering the patientās body, affects the COX produced from arachidonic acid. This allows you to adjust the reaction of formation of prostaglandins, under the influence of which inflammatory processes are activated, pain cider. Effect on prostaglandins eliminates a febrile state.
Shortly after the intake of tablets, the active compound is absorbed into the circulatory system. Studies have shown that maximum plasma concentrations are achievable on average in 45 minutes. The suction process is not adjusted by meals. The ability of the active substance to bind to plasma proteins reaches 99%. The elimination half-life is from four to six hours.
Up to 90% of the medication received in the body is eliminated with urine. About 60% is displayed unchanged. Other volumes leave the body through the intestinal tract.
In case of impaired renal function, when prescribing Ketokam, elderly people need to remember about lowering the elimination rate. The time interval necessary for the half-life of the drug is increasing.
Features of the reception
"Ketokam" is prescribed, if necessary, to eliminate severe or moderate pain. The medication is effective for painful sensations of different genesis. For adult patients, the drug is recommended to use a 10 mg tablet with a time interval of 4-6 hours between doses. If necessary, it is allowed to double the volume using Ketokam three to four times daily.
The maximum dosage for a day is 90 mg of the active compound. With a mass of less than 50 kg, impaired renal functionality, aged 65 years and older, āKetokamā per day is shown in an amount of not more than 60 mg.