Zyvox granules for suspension 100mg / 5ml 66g №1 bottle


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Zyvox granules for suspension 100mg / 5ml 66g №1 bottle

pharmachologic effect

Antibacterial drug belongs to the class of oxazolidinones. The mechanism of drug action is due to inhibition of protein synthesis in bacteria. Linezolid, due to its binding to bacterial ribosomes, prevents the formation of the functional initiating complex 70S, which is a component of the translation process during protein synthesis.

The drug is in charge of the drugs in relation to aerobic gram-positive bacteria: Corynebacterium jeikeium, Enterococcus faecalis (including glycopeptide-resistant strains), Enterococcus faecium (including glycopeptide-resistant strains), Enterococcus casseliflavus, Enterococcus gallinarum, Listeria montect-citrate-citrate-citrate-citrate-citrate-chethecus cactincus cyllinarum, chemoctectus gallinarum, necrosis-resistant, non-toxic. Staphylococcus aureus (strains with intermediate sensitivity to glycopeptides), Staphylococcus epidermidis (including methicillin-resistant strains), Staphylococcus haemolyticus, Staphylococcus lugdunensis, Streptococcus agalactiae, Streptococcus intermedius, Streptococcus intermedius, Streptococcus agalactiae, Streptococcus intermedius, Streptococcus agalactiae, Streptococcus agalactiae, Streptococcus agalactiaus nicillin and penicillin-resistant strains), Streptococcus spp. (streptococci groups C and G), Streptococcus pyrogenes, Streptococcus viridans; aerobic gram-negative bacteria: Pasteurella canis, Pasteurella multocida; anaerobic gram-positive bacteria: Clostridium perfringens, Peptostreptococcus spp. (including Peptostreptococcus anaerobius); anaerobic gram-negative bacteria: Bacteroides fragilis, Prevotella spp .; Chlamydia pneumoniae.

Legionella spp., Moraxella catarrhalis, Mycoplasma spp. Are moderately sensitive to the drug.

The drug resistant to Haemophilus influenzae, Neisseria spp., Enterobacteriaceae, Pseudomonas spp.

There was no cross-resistance between Zyvox and aminoglycosides, beta-lactam antibiotics, folic acid antagonists, glycopeptides, linkosamides, quinolones, rifamycins, streptogramines, tetracyclines, chloramphenicol.

Resistance to Zyvox develops slowly through a multistage mutation of 23S ribosomal RNA and occurs at a frequency of less than 1x10-9-1x10-11.

The in vitro post-antibiotic effect of Zyvox is about 2 hours for Staphylococcus aureus, in vivo (in experimental animal studies) - 3.6 hours and 3.9 hours for Staphylococcus aureus and Staphylococcus pneumoniae, respectively.


The active ingredient of the drug Zyvox is (s) -linezolid, which is biologically active and metabolized in the body to form inactive derivatives. The solubility of linezolid in water is about 3 mg / ml and does not depend on pH in the range of 3-9.

The average pharmacokinetic parameters (standard deviation / SD /) of linezolid in healthy volunteers after a single and multiple (until Css linezolid in the blood) ingestion is given in the tables.

1. Dosing regimen of Zyvox Cmax (SD) mcg / ml Cmin (SD) mcg / ml Tmax (SD) h
pills 600 mg once 12.7 (3.96) - 1.28 (0.66)
2 times / day 21.2 (5.78) 6.15 (2.94) 1.03 (0.62)
Suspension for oral administration 600 mg once 11.0 (2.76) - 0.97 (0.88)

2. Dosing regimen of Zyvox AUC (SD) μg x h / ml T1 / 2 (SD) h Cl (SD) ml / min
pills of 600 mg of one-time 91.4 (39.3) 4.26 (1.65) 127 (48)
2 times / day 138 (42.1) 5.4 (2.06) 80 (29)
Suspension for oral administration 600 mg once 80.8 (35.1) 4.6 (1.71) 141 (45)
SD - standard deviation

Tmax - time to reach Cmax

AUC - area under the concentration-time curve

T1 / 2 - half-life

Cl - system clearance

Cmin - the minimum concentration in plasma


After oral administration, linezolid is rapidly and rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached after 2 hours. Absolute bioavailability is about 100%. The degree of absorption after taking the drug inside in the form of a suspension is similar to that when taking the drug in the form of pills. Food intake does not affect the absorption of linezolid. Css is achieved on 2-3 days of taking the drug.


The equilibrium state is reached on the 2-3 day of the drug. Linezolid is rapidly distributed in tissues with good perfusion.

Vd when reaching Css in healthy volunteers is on average 40-50 liters. Binding to plasma proteins is 31% and does not depend on the concentration of linezolid in the blood.


It has been established that cytochrome P450 isoenzymes are not involved in the linezolid metabolism in vitro. Linezolid also does not inhibit the activity of the clinically important cytochrome P450 isoenzymes (1A2, 2C9, 2C19, 2D6, 2E1, 3A4). Metabolic oxidation leads to the formation of 2 inactive metabolites - hydroxyethylglycine (which is the main metabolite in humans and is formed as a result of a non-enzymatic process) and aminoethoxyacetic acid (formed in smaller quantities). Other inactive metabolites are also described.


Linezolid is mainly excreted in the urine as hydroxyethylglycine (40%), aminoethoxyacetic acid (10%) and unchanged drug (30-35%). With feces excreted in the form of hydroxyethylglycine (6%) and aminoethoxyacetic acid (3%). Unchanged drug is practically not excreted in the feces.

Pharmacokinetics in special clinical situations

The clearance of linezolid is higher in children and decreases with age.

The pharmacokinetics of linezolid does not change significantly in the group of patients aged 65 years and older.

Some pharmacokinetic differences were noted in women, expressed in slightly lower Vd, a decrease in clearance of approximately 20%, sometimes in higher plasma concentrations.Since T1 / 2 linezolid in women and men does not differ significantly, there is no need to adjust the dose of the drug.

Patients with moderate, moderate and severe renal insufficiency do not require dose adjustment, because There is no relationship between QC and drug excretion through the kidneys. Since 30% of the drug dose is eliminated within 3 hours of hemodialysis, in patients receiving such treatment, linezolid should be prescribed after dialysis.

The pharmacokinetics of linezolid do not change in patients with moderate or moderate hepatic insufficiency, and therefore there is no need for dose adjustment.

Pharmacokinetics in patients with severe hepatic insufficiency has not been studied. However, given that linezolid is metabolized as a result of a non-enzymatic process, it is obvious that liver function does not significantly affect the metabolism of the drug.


Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug (including infections accompanied by bacteremia):

- community-acquired pneumonia;
- hospital pneumonia;
- infections of the skin and soft tissues;
- infections caused by Enterococcus spp. (including vancomycin resistant strains of Enterococcus faecalis and Enterococcus faecium).

For infections caused by gram-negative microorganisms (confirmed or suspected), it is possible to use the drug as part of a combination therapy.

Dosing regimen

Adults take the drug inside 2 times / day.

Indications (including infections accompanied by bacteremia) Single dose Recommended duration of treatment
Community-acquired pneumonia 600 mg 10-14 days
Hospital pneumonia 600 mg 10-14 days
Infections of the skin and soft tissues 400-600 mg, depending on the severity of the disease 10-14 days
Enterococcal infections 600 mg 14-28 days
The duration of treatment depends on the pathogen, localization and severity of the infection.

For children aged 5 years and older, the drug is administered orally at a dose of 10 mg / kg body weight 2 times / day.

The maximum dose for adults and children is 600 mg 2 times / day.

Patients who at the beginning of therapy, the drug was prescribed in / in, in the future can be transferred to any dosage form for oral administration. In this case, dose selection is not required, oral bioavailability is almost 100%.

pills or suspension for oral administration can be taken both with meals and between meals.

Side effect

On the part of the digestive system: at least 1% - taste perversion, nausea, vomiting, diarrhea, abdominal pain (including spastic), flatulence, changes in total bilirubin, ALT, AST, ALP.

From the hemopoietic system: reversible anemia, thrombocytopenia, leukopenia, pancytopenia.

Others: headache, candidiasis; very rarely, cases of peripheral neuropathy and optic nerve neuropathy when used for more than 28 days (the relationship between the use of Zyvox and the development of neuropathy has not been proven).

Adverse reactions do not depend on the dose and, as a rule, do not require cessation of treatment.


- hypersensitivity to linezolid and other components of the drug.

Use during pregnancy and lactation

Adequate and strictly controlled studies of the safety of the drug Zyvoks during pregnancy was not conducted.

The use of Zyvox during pregnancy is possible only in cases where the intended benefit of therapy for the mother outweighs the potential risk.

It is not known whether linezolid is excreted in breast milk of lactating women, therefore special care should be taken when prescribing the drug to the mother during the breastfeeding period.

special instructions

With the development of diarrhea in patients taking Zyvox, like other antibacterial drugs, the risk of pseudomembranous colitis should be considered.

Control of laboratory parameters

In the course of treatment, it is necessary to perform a clinical analysis of blood in patients with an increased risk of bleeding, myelosuppression in history, as well as in patients who receive simultaneously drugs that reduce hemoglobin or platelet count or their functional properties, as well as taking linezolid for more than 2 weeks.

Influence on ability to drive motor transport and control mechanisms

Acceptance of the drug Zyvox does not affect the ability to drive vehicles and control mechanisms.


Currently, overdose cases of the drug Zyvox have not been reported.
Treatment:if necessary, symptomatic therapy is carried out (including it is necessary to maintain the level of glomerular filtration).Approximately 30% of the dose is eliminated within 3 hours during hemodialysis.

Drug interaction

Linezolid is a weak, reversible, non-selective inhibitor of MAO, so in some patients, Zyvox can cause a moderate reversible increase in the pressor action of pseudoephedrine hydrochloride and phenylpropanolamine hydrochloride. Taking this into account, with simultaneous use of Zyvox with adrenergic drugs, it is recommended to reduce the initial doses of the latter and to further select the dose by titration.

Pharmacokinetic interaction

With simultaneous administration of Zyvox with aztreonam and gentamicin, no changes in the pharmacokinetics of linezolid were observed.

Pharmacy sales terms
The drug is available on prescription.
Terms and conditions of storage
The drug should be stored at room temperature (not above 25 ° C).
Vials of granules for the preparation of a suspension for oral administration should be kept tightly closed.
The bottle with the prepared suspension should be stored in a carton box for not more than 3 weeks at room temperature (not above 25 ° C).

It is a drug. Consultation with a doctor is required.