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Zyvox is a new generation antibiotic. It contains an artificial component of linezolid, which belongs to the category of oxazolidinones.




J01XX08 Linezolid

Indications of zivoksa

Indicated for the elimination of infectious pathologies, caused by germs that are sensitive to linezolid. In the case of diseases that are triggered by gram-negative microorganisms, it is required to resort to a combined treatment of various antibacterial drugs.

Zyvox used for:

  • Hospital / community-acquired pneumonia;
  • infectious processes within the skin with its appendages (on complications occurring background);
  • infectious processes within the skin appendages (without complications), among which are caused by pyogenic streptococci, and in addition to the substance methicillin sensitive Staphylococcus aureus types;
  • infectious processes caused by enterococci (including also resistant strains relative to vancomycin).

Release form

It is produced in tablet form (in one blister 10 tablets) or in the form of a parenteral solution (the volume of packets with infusions is 300 ml). The package contains 1 blister plate or 10 packets with infusion.


Testing the drug in vitro has shown that it is active against a variety of microbial species, among which both forming and not forming a protective membrane.

The mechanism of drug exposure is related to the fact that it can selectively block protein synthesis inside microbial cells, disrupting the processes of translation occurring in the ribosomes of bacteria.

During the testing, it was possible to identify resistance against linezolid in such microbes: influenza rod, pseudomonas, moraxella cataris, and also enterobacteria and Neisseria species.

In the case of a cross randomly selected (placebo-controlled) test, it was found that the active substance had no particular effect on the QT interval.


Absorption of the active ingredient from the gastrointestinal tract is quite high, and the bioavailability index reaches 100%. The lowest and peak concentrations of the substance, as well as the period of their achievement (depending on the dosage and form of drugs):

  • single use of 400 mg (in a tablet) - a peak value of 8.1 μg / ml (with a possible deviation of up to 1.83), reaching a period of: 1.52 hours (with a deviation of up to 1.01);
  • 400 mg (tablet) with a regimen of 1 every 12 hours - a peak level of 11 μg / ml (with a deviation of up to 4.37), a minimum level of 3.08 μg / ml (deviation to 2.25), a period of achievement: 1 , 12 hours (with a deviation of up to 0.47);
  • a single dose of 600 mg (in a tablet) - a peak value of 12.7 μg / ml (with a deviation of up to 3.96), a period of achievement: 1.28 hours (with a possible deviation of 0.66);
  • 600 mg (tablet) with a dosage regimen of 1 every 12 hours - a peak value of 21.2 μg / ml (with a possible deviation of up to 5.78), a minimum level of 6.15 μg / ml (with a deviation of up to 2.94), the period of achievement: 1.03 hours (deviation 0.62);
  • single injection IM 600 mg - peak level 12.9 μg / ml (with possible deviation up to 1.6), period reaching 0.5 hours (with a deviation of up to 0.1);
  • in / m administration of 600 mg of medication every 12 hours - a peak level of 15.1 μg / ml (with a possible deviation of up to 2.52), a minimum of 3.68 μg / ml (deviation up to 2.36), a period of achievement : 0.51 hours (with a deviation of up to 0.03).

It should be taken into account that with a large amount of fat in food, the peak level of the substance (after oral intake) is lowered by 17%. At the same time, the period of reaching this indicator is also extended, up to 2.2 hours.

Linezolid is well distributed inside the tissues, about 31% of the component is bound inside the serum. The average index of the distribution volume is 40-50 liters.

Metabolism of the active component is realized with the formation of 2 basic inactive derivatives. One of them is formed by means of an enzymatic pathway, and the second one is on the contrary non-enzymatic. Tests have shown that the metabolism of linezolid hemoprotein P450 is minimally involved.

Removal of drugs is mainly carried out through the kidneys (65%). About 30% of the substance is excreted unchanged, and another 50% in the form of derivatives. The average index of the kidney cleansing rate is approximately 40 ml / minute (similar figures indicate net tubular reabsorption). Approximately 10% of the substance is excreted through the intestines in the form of derivatives.

Use of zivoksa during pregnancy

The effect of the drug on human fertility, but also the course of pregnancy and the development of the fetus, has not been studied. In animal tests, the drug demonstrated reproductive toxicity, from which it can be concluded that there is a potential danger to humans. Pregnant women should be prescribed medication solely under the supervision of the treating doctor, and also if the patient has strict testimony.

Animal testing has shown that linezolid is able to pass into breast milk. Since there is a danger to the child, it is not recommended to use drugs during lactation. If a medicine is needed, it is necessary to cancel breastfeeding for the period of treatment.


Among the contraindications of drugs:

  • patient intolerance to the active ingredient of the drug, as well as other antibiotics that fall into this category;
  • patients during the period of using MAO inhibitors, and in addition, within 2 weeks after the completion of the treatment course with their use;
  • children age less than 12 years.

If the patient has problems with hepatic function, the medicine is prescribed only after assessing the benefits and all possible risks, and also exclusively under the supervision of the doctor.

Particular caution is required if the patient has such abnormalities (and only if there is the possibility of constant monitoring of blood pressure):

  • manic depression;
  • uncontrolled increase in blood pressure;
  • hyperthyroidism;
  • pheochromocytoma;
  • the presence of acute episodes of dizziness;
  • recurrent schizophrenia.

Side effects of zivoksa

During clinical tests most often among the negative effects of the use of medicines called headaches, nausea, candidiasis, as well as the frustration of a chair. Because of the side reactions 3% Curing cancellation needed medication.

As a result of zyvox patients may experience such negative developments:

  • infectious processes: candidiasis of the vagina or the oral cavity, vaginitis, fungi, and colitis (pseudomembranous sometimes in shape);
  • hematopoietic system: the development of neutrophils, trombotsito-, pantsito- and leukopenia, and in addition the eosinophilia or myelosuppression and anemia (sometimes with sideroblastic form);
  • metabolism: lacticemia or hyponatremia;
  • CNS organs: a metallic taste in the mouth, sleep disorders, convulsions, paraesthesia, dizziness, and with it the development of hypoesthesia or serotonin toxicity. Besides it may occur tinnitus develop optic neuropathy (thus there are such features as the disorder or loss of vision and color vision distortion) or peripheral neuropathy;
  • authorities CCC: the development of thrombosis, phlebitis or arrhythmia, and in addition to this pressure and minor stroke;
  • Gastrointestinal organs: the appearance of vomiting, abdominal pain (local or general), dyspeptic symptoms, but other than that the dryness of the oral mucosa and tongue change color and enamel. The development of glossitis and gastritis, and in addition, pancreatitis or stomatitis;
  • hepatobiliary system: increased ALT values, AST, and with it, alkaline phosphatase, hyperbilirubinemia development and change in the level of liver samples;
  • organs of the urinary system: renal failure, polyuria development, hyperuricemia, as well as hypercreatininemia;
  • Data analysis: increased rates of LDH, lipase to amylase and in addition sugar and creatine phosphokinase; decrease in albumin indicators, and with it the total protein; besides this change in values of potassium to calcium and sodium bicarbonate. In some cases, there was a reduction of sugar indices (in normal conditions of supply), increase in the reticulocytes and a change in the chloride;
  • others: development of hyperhidrosis;
  • allergic reactions: dermatitis, urticaria, alopecia, angioedema and anaphylaxis; beyond that may arise bullous rash or itching;
  • specific effects after parenteral administration: hyperthermia appearance or feeling of thirst, fever or fatigue condition, and pain at the site of administration.

Dosing and administration

Use the drug in 2 ways - parenterally or orally. If the parenteral method was used at the initial stage of the treatment, the patient is allowed to be transferred to the oral route with a similar dosage. Its dimensions are appointed by the attending physician.

To eliminate hospital / out-of-hospital pneumonia, and in addition to this complicated forms of infectious processes in the appendages and skin, 600 mg of the drug are required 2 times per day. This course lasts for 10-14 days.

In the treatment of pathologies caused by Enterococcus fecium, it is usually required to take 600 mg of the drug 2 times a day. The therapeutic course continues for 14-28 days.

When treating uncomplicated infectious processes in the appendages and skin, a dosage of 400-600 mg of LS is required 2 times a day. The treatment course lasts for 10-14 days.

During therapy, it is very important to strictly observe the 12-hour intervals between procedures for the use of drugs. Each 12 hours is allowed to use no more than 600 mg of the drug.

There is no information on the safety of the drug over a period of more than 28 days.

Interactions with other drugs

Combined use of the drug with dopaminergic, vasoconstrictive and sympathomimetic (direct and indirect) drugs can cause an increase in blood pressure.

In the case of simultaneous use with serotonergic drugs, the development of serotonin intoxication is possible. Therefore, such combination of drugs is not recommended, except for situations when both of them are necessary for the patient according to the indications. In this case, the treating doctor will need to carefully monitor the patient's condition and, in case of intoxication develop, decide on the abolition of one of the drugs, taking into account all the risks and the high probability of withdrawal syndrome when stopping the use of serotonergic medication.

During treatment with Zyvox it is recommended to limit the use of products containing a lot of tyramine (taking medicine, it is advisable to eat not more than 100 mg of tyramine). Taking large doses of tyramine together with linezolid can provoke vasoconstrictive action. During the period of therapy, you should eat a limited amount of mature cheeses, yeast extracts and fermented soy products, and drink non-distilled alcoholic beverages.

The active substance of the drug indiscriminately suppresses MAO (reversible effect). Although the dosages used during the period of Zyvox therapy do not have a significant drug effect on MAO, the combined use of these drugs is not recommended.

Linezolid does not affect the pharmacokinetic characteristics of drugs metabolized by the P450 element.

Powerful inductors of the element CYP3 A4 can reduce the exposure indices of linezolid.

Storage conditions

The medicine is contained in a place inaccessible to the child, under standard conditions. Temperature indices - not more than 25 ° С. An open packet of medicinal solution must be used immediately.

Shelf life

Zyvox is usable for 3 years from the date of manufacture of the drug.

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To simplify the perception of information, this instruction for use of the drug "Zivox" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.

Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.

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