Zivox (linezolid) solution for infusions 2 mg/ml. 300 ml. vial №1

Description

Zivox (linezolid) solution for infusions 2 mg/ml. 300 ml. vial №1

Composition

active substance: linezolid;

1 ml of solution contains 2 mg of linezolid;

Excipients: sodium citrate dihydrate, citric anhydrous acid, glucose, monohydrate, sodium hydroxide, dilute hydrochloric acid, water for injections.

Dosage form

Solution for infusions.

Basic physical and chemical properties: transparent solution practically without visible particles from colorless to yellow color.

Pharmacotherapeutic group

Antibacterial agents for systemic use. ATX code J01X X08.

Pharmacological properties

Linezolid is a synthetic antibacterial drug that belongs to a new class of antimicrobials – oxazolidinones. It is active in vitro against aerobic gram-positive bacteria and anaerobic microorganisms. Linezolid selectively inhibits bacterial protein synthesis due to its unique mechanism of action. It binds directly to bacterial ribosomes (23S with 50S subunits) and prevents the formation of the 70S functional initiation complex (an important component of the translation process).

The prevalence of acquired resistance may vary geographically and over time for individual species, so it is advisable to rely on local information on the resistance of microorganisms, especially in the treatment of severe infections. If necessary, when the level of resistance of microorganisms at the local level is such that the benefits of using the drug, at least for some types of infections, is in doubt, you should consult an expert.

Sensitive microorganisms:

• gram-positive aerobic microorganisms: Enterococcus faecalis, Enterococcus faecium *, Staphylococcus aureus *, coagulase-negative staphylococci, Streptococcus agalactiae *, Streptococcus pneumoniae *, Streptococcus pyogenes *, Group C strecicoco;
• gram-positive anaerobic microorganisms: Clostridium perfringens, Peptostreptococcus anaerobius, Peptostreptococcus species;
• resistant microorganisms: Haemophilus influenza, Moraxella catarrhalis, Neisseria species, Enterobacteriaceae, Pseudomonas species;
• although linezolid shows some in vitro activity against Legionella, Chlamydia pneumoniae and Mycoplasma pneumoniae, there are insufficient data to confirm clinical efficacy in these cases.

Indication

Treatment of infections caused by susceptible strains of certain microorganisms in the following conditions:

• nosocomial pneumonia;
• community-acquired pneumonia;
• complicated infections of the skin and its structures, in particular infections of the diabetic foot without concomitant osteomyelitis caused by Staphylococcus aureus (methicillin-sensitive and methicillin-resistant isolates), Streptococcus pyogenes or Streptococcus agalactiae;
• uncomplicated infections of the skin and its structures caused by Staphylococcus aureus (only methicillin-sensitive isolates) or Streptococcus pyogenes;
• vancomycin-resistant infections caused by Enterococcus faecium strains, including infections accompanied by bacteremia.

Zivox is not indicated for the treatment of infections caused by gram-negative microorganisms. If a gram-negative pathogen is suspected or detected, specific gram-negative therapy should be initiated immediately.

Contraindication

Hypersensitivity to linezolid or any other component of the drug is known.

Zivox should not be used in patients who are taking any medicines that inhibit monoamine oxidase A and B (eg phenelzine, isocarboxazid, selegiline, moclobemide) or for two weeks after taking them.

Except when it is possible to closely monitor and monitor blood pressure, Zivox should not be prescribed to patients with the following concomitant clinical conditions or concomitant with the following drugs:

• uncontrolled hypertension, pheochromocytoma, carcinoid, thyrotoxicosis, bipolar depression, schizoaffective disorder, acute episodes of dizziness;
• serotonin reuptake inhibitors, tricyclic antidepressants, 5-HT1 serotonin receptor agonists (triptans), direct and indirect sympathomimetics (including adrenergic bronchodilators, pseudoephedrine, phenylpropanolamine), dopineparine, or vasopressorins, vasopressors.

Breastfeeding should be discontinued during use of the drug.

Method of application and dosage

The duration of treatment depends on the pathogen, the location and severity of the infection, as well as the clinical effect.

The recommendations for the duration of therapy, given below, have been used in clinical trials. For some types of infections, a shorter duration of treatment may be appropriate, but this has not been evaluated in clinical trials.

The maximum duration of treatment is 28 days. The safety and efficacy of linezolid for more than 28 days have not been studied.

Nosocomial pneumonia / Nosocomial pneumonia (including forms accompanied by bacteremia) / Complicated infections of the skin and its structures:

• pediatric patients (from birth to 11 years) – 10 mg / kg intravenously or orally every 8 hours for 10-14 days;
• adults and children (12 years of age and older) – 600 mg intravenously or orally every 12 hours for 10-14 days.

Infections caused by Enterococcus faecium resistant to vancomycin, in particular infections accompanied by bacteremia:

• pediatric patients (from birth to 11 years) – 10 mg / kg intravenously or orally every 8 hours for 14-28 days;
• adults and children (12 years of age and older) – 600 mg intravenously or orally every 12 hours for 14-28 days.

Uncomplicated infections of the skin and its structures:

• children under 5 years of age – 10 mg / kg orally every 8 hours for 10-14 days;
• children aged 5–11 years – 10 mg / kg orally every 12 hours for 10–14 days;
• children over 12 years of age: 600 mg orally every 12 hours for 10–14 days;
• adults and children (over 12 years of age) – 400 mg orally every 12 hours for 10-14 days.

Overdose
There is no specific antidote.

No cases of overdose have been reported.

In case of overdose, symptomatic treatment is indicated together with measures to maintain the level of glomerular filtration. Approximately 30% of the administered dose is excreted within 3 hours of hemodialysis, but there are no data on the excretion of linezolid during peritoneal dialysis or hemoperfusion. The two main metabolites of linezolid are also removed by hemodialysis.

Side effects

Diarrhea (8.4%), headache (6.5%), nausea (6.3%) and vomiting (4.0%) were the most commonly reported. The most common side effects that led to discontinuation of the drug were headache, diarrhea, nausea and vomiting. Approximately 3% of patients discontinued treatment due to the development of drug-related adverse reactions.