Most infections of a bacterial or viral origin known to medicine can be treated with conventional drugs. However, there are pathogens that have adapted to the so-called hospital conditions. The fight against them is a very difficult task, because many drugs simply do not work on them. The antibiotic "Linezolid" refers to such drugs, with which you can fight with the so-called hospital or other infections that are resistant to other types of drugs. It is about him that will be discussed in this article.
Description
The drug "Linezolid" instruction refers to antimicrobial agents of a wide spectrum of action. By its basic properties and characteristics, it belongs to the class of oxazolidinones, which in terms of strength and spectrum of action on microorganisms are superior in many respects to Vancomycin and other drugs with a similar composition.
Today, there are several types of antimicrobial agents Linezolid. The release form most commonly used in therapy is film-coated tablets containing 400 or 600 mg of active ingredient. In addition, in medical practice, an infusion solution is often used, each milliliter of which contains 2 mg of the active substance, and powder (granules) for the preparation of a suspension, the concentration of the active substance in which is 100 mg per 5 ml of the finished product.
Indications for use
As stated at the beginning of the article, the Linezolid preparation is recommended for use in the presence of infections caused by bacteria resistant to other antibiotics. These include both gram-positive and gram-negative microorganisms belonging to the anaerobic or aerobic types that have developed resistance to methicillin, glycopeptide compounds, penicillin and other antibiotics.
The list of diseases in which the use of the drug "Linezolid" is indicated, the instruction includes:
- hospital or community-acquired pneumonia;
- skin infections;
- soft tissue infection;
- other infections caused by antibiotic-resistant strains of Enterococcus.
As a rule, before using this drug, studies are conducted to identify the resistance of pathogens to other drugs. If none are found, treatment is carried out with the help of other antimicrobial drugs.
Contraindications
The main and most significant contraindication to the use of the antibiotic "Linezolid" instructions for use calls hypersensitivity to it. It is also not recommended to use the drug for the treatment of patients who take other drugs from the group of MAO inhibitors. In addition, it is not recommended to prescribe this drug in conjunction with tricyclic antidepressants and substances that can increase blood pressure (epinephrine, dopamine, tryptan and others).
Linezolid (tablets, solution for infusion and suspension) is contraindicated in diseases such as arterial hypertension, thyrotoxicosis, carcinoid or seratonin syndrome, pheochromocytosis. The presence of these contraindications should be detected before starting treatment with this drug.
The mechanism of action of the drug in the body
The action of the drug "Linezolid" is due to its ability to block the process of translation of protein structures in bacterial cells. Due to this, the reproduction of microorganisms stops, and their death occurs. Resistance to the drug in most bacteria is produced very slowly.
After it enters the body, the active substance of the drug forms the metabolite hydroxyethyl glycine. The degree of its connection with plasma proteins reaches 31%. In the course of laboratory studies, it was found that this compound penetrates into all tissues and organs. It also has the ability to pass through the placenta into the fetus and into breast milk (this property of the drug was reflected in the recommendations for taking the drug by pregnant and lactating women).
The half-life of the active substance and its metabolite from the body is 4.5-5 hours. Excretion is carried out through the urinary system (50% in the form of a metabolite and 35% unchanged) and through the digestive tract (at least 9%). Complete elimination occurs within 8-12 hours from the time of taking the drug.
How to take Linezolid
Specialists draw attention to the fact that the patient in most cases cannot independently decide on the method of taking Linezolid. The instruction, tablets, solution and emulsion in which are considered not as separate preparations, but as forms of one medicine, contains comprehensive information on this issue. Below are the main points regarding the dosage and duration of therapy.
The medicine "Linezolid" instructions for use recommends the use of the following schemes:
- The solution for infusion is administered intravenously 2 times a day. A single dose is 400-600 mg of the active substance. The duration of treatment depends on the severity of the disease and its localization. As a rule, most infections require a period of at least 10 and no more than 14 days, and only with diseases caused by enterococcus, therapy lasts from 2 to 4 weeks.
- The drug "Linezolid" (tablets) is also taken 2 times a day in an amount of 400 or 600 mg per dose. For patients aged 5 to 14 years, the dosage is calculated based on body weight and is 10 mg per 1 kg of weight 2 times a day. The maximum dose per oral dose (oral) should not exceed 600 mg. The duration of therapy is determined by the same indicators as discussed above.
- The granules from which the emulsion is made are used according to the above scheme. The calculation of the dosage in this case must be carried out on the basis of the same recommendations.
Since the medicine “Linezolid” is prescribed exclusively by prescription and is used only in a hospital setting, an overdose of this agent and the appearance of pronounced adverse reactions are practically excluded. Doctors in their reviews mention cases of excessive accumulation in the body of the active substance of the drug and its metabolites due to impaired functioning of the urinary organs and liver. The consequences of such overdoses are usually very quickly eliminated, as the patient undergoes treatment under the constant supervision of specialists.
Drug interaction
Since one of the dosage forms of Linezolid is intended for intravenous administration, it is important that this drug is fully compatible with the main solutions used during treatment (5% glucose solution, 0.9% sodium chloride solution and ringer's solution).
Particular attention should be paid to the condition of patients who, in addition to Linezolid, take adrenergic drugs. If a complete rejection of the latter is not possible, doctors will need to review their dosage.
The medicine "Linezolid" (analogues in composition can also be equated to it) is completely incompatible with the preparations "Chlorpromazine", "Cotrimoxazole", "Diazepam" and "Phenytoin". If the patient before taking the antibiotic took the indicated drugs, it is necessary to maintain the interval of 3 days before starting treatment with Linezolid.
special instructions
As additional recommendations for taking the antibiotic Linezolid, the instructions for use contain information related to pregnant women and people with existing concomitant diseases. In addition, it indicates the possibility of side effects. But first things first.
With regard to taking the drug "Linezolid", reviews of doctors speak of special caution when it is prescribed to pregnant and lactating women. This is due to the fact that the effect of the drug on the developing fetus or newborn is not well understood. As a rule, treatment with its use is advisable only if the risk to the fetus is significantly lower than the expected benefit to the mother.
Severe renal and hepatic insufficiency also require careful use of the drug, because metabolites are excreted mainly by these organs, and the accumulation of these substances in them can lead to a worsening of the patient's condition.
Side effects
Based on the results of clinical observations, adverse reactions from various organs and systems when taking the antibiotic Linezolid most often affect the nervous and digestive systems. In approximately 10% of cases, patients experienced nausea and headaches during treatment. A little less often they were disturbed by diarrhea, dizziness and candidiasis on the oral mucosa.
In addition, experts pointed out such undesirable consequences of using the drug as peripheral neuropathy, convulsions, visual impairment (up to its complete loss), thrombocytopenia, serotonin syndrome, angioedema and anaphylactic shock. Due to the fact that this drug is used exclusively in a hospital setting, grave consequences are most often avoided.
The treatment of unwanted reactions from organs and systems is symptomatic. Discontinuation of the drug is possible only if the severity of side effects is a greater problem than a disease that is treated with the antibiotic in question.
Analogues of the drug "Linezolid"
Readers will probably have a question about whether Linezolid has analogues. Of course, the pharmaceutical market, if not abundant, then has several drugs that are similar in composition to this antimicrobial agent. Such drugs include the Serbian antibiotic Zenix, the Norwegian Zivox and the Israeli Linezolid Teva. The composition of all these drugs as the main active ingredient is linezolid.
Are there any significant differences between the above funds and the drug "Linezolid"? The price of medicines is the main difference. The fact is that having a similar composition, these drugs act on the human body in exactly the same way: they fight the same microorganisms, cause the same side effects, have the same contraindications. The timing and methods of treatment, as well as the dosage, are not much different.
As a rule, more expensive imported analogs of the antibiotic Linezolid are used if this drug is not available in pharmacies. This happens often, because its use by a wide range of patients is practically impossible due to prescription, and not a single pharmacy chain will decide to overexpose the medicine on the shelves. Hence the orders of small batches of medicine and, therefore, the opportunity at some point to sell its entire supply.
Drug cost
Medicines from the group of oxazolidinones are of high cost due to the complex multi-stage synthesis of this substance in pharmaceutical laboratories. What is the price of Linezolid? Tablets (with a content of the main active ingredient of 600 mg, a package of 10 pieces) in pharmacy chains cost at least 18 thousand rubles. The maximum cost of this dosage form is 20 thousand rubles per 10 tablets. A little cheaper is the drug in a dosage of 400 mg. Its price is about 17-18 thousand rubles for 10 tablets.
Linezolid infusion solution can be purchased a little cheaper: a package of 10 packets of 100 ml will cost 7.5-9 thousand rubles, 10 packets of 300 ml each - 15.3-16.2 thousand rubles.
Drugs of the same name, which are an order of magnitude cheaper, most often turn out to be fakes and, at best, have no effect on the patient's body. Nevertheless, procrastination with therapy for those diseases that the Linezolid antibiotic helps to get rid of is very dangerous in itself. That is why experts recommend purchasing this medicine only in pharmacies with a good reputation.
Reviews about the antibiotic "Linezolid"
In various sources, it is rarely possible to find reviews about an antibiotic of this class. This is especially true for information regarding his admission provided by patients. This is due to the fact that most often patients during therapy are in a very serious condition and it is extremely difficult for them to remember all the transferred feelings.
Specialists, in turn, respond extremely positively to Linezolid. According to them, the drug is able to cope even with the most resistant microbes. They also note that the risk of complications caused by side effects or overdose is practically absent. This is due to the fact that the antibiotic is used exclusively in a hospital setting. At the first sign of an allergic or adverse reaction to the drug, all necessary medical procedures are carried out to eliminate them.
So, we examined all the subtleties of the use of the drug "Linezolid". Instructions for use, price and possible reactions to the drug were described by us in this article in sufficient detail. It should be noted that, despite the high cost of the drug, its use is justified in each case. Only the attending physician can decide on the treatment of the patient with this drug.