Zithrotrex® (azithromycin) vial

Zithrotrex® (azithromycin) 500 mg

Pharmaceutical form:

Azithromycin IV 500 mg powder for solution for infusion

Azithromycin powder vial 500 mg for infusion

Unique pharmacokinetic advantages and features:

Targeted effect and excellent penetration into lung tissue

Short duration of treatment

High tolerance

Less contraindications and unwanted side effects

Rapid onset of effect

Long-term efficacy

Once-daily administration

Easy administration

Minimum arrhythmogenicity among macrolides

Potential and unique antibacterial effect on atypical pathogens

Suitable post-antibiotic effect

Tissue concentration higher than serum level

Long half-life

Therapeutic applications:

-In the treatment of community-acquired pneumonia with susceptible organisms including Legionella pneumoniae in patients requiring initial intravenous therapy.

-In the treatment of pelvic infections caused by susceptible organisms in patients requiring initial intravenous therapy.

Pharmacodynamic effects:

Azithromycin is the first drug in the macrolide antibiotic subgroup called azalides, which is chemically different from erythromycin.

Mechanism of action:

Azithromycin binds to the 23S rRNA subunit of the 50S ribosomal subunit. Azithromycin blocks protein synthesis by inhibiting the translocation/transpeptidation step of the protein center and inhibiting the assembly of the 50S ribosomal subunit.

Resistance Mechanism:

Two common mechanisms of resistance to macrolides, including azithromycin, are:

Target modification (due to methylation of 23S rRNA)

– active efflux

The occurrence of these resistance mechanisms varies from one bacterial strain to another, and within each strain, the frequency of resistance varies depending on geographical location.

Efflux pumps are produced in a number of bacterial strains, including gram-negative bacteria such as Haemophilus influenzae and Staphylococcus. Efflux pumps are also expressed in Streptococcus and Enterococcus.

Method and dosage:

Adult use:

For the treatment of community-acquired pneumonia:

500 mg in a single daily dose as an intravenous infusion for at least 2 days, followed by intravenous therapy with oral therapy at a dose of 500 mg once a day for 7 to 10 days.

The time of transition from intravenous therapy to oral therapy is determined by the attending physician based on the patient’s clinical response.

In the treatment of pelvic infection:

500 mg in a single daily dose as an intravenous infusion for 1 or 2 days, followed by intravenous therapy with oral therapy at a dose of 250 mg once a day for 7 days.

The time of transition from intravenous therapy to oral therapy is determined by the patient’s clinical response and by the attending physician.

Use in the elderly:

The dosage in elderly patients is prescribed as in adults. Since elderly patients are more susceptible to cardiac arrhythmias, special caution is recommended in prescribing this drug in the elderly due to the risk of cardiac arrhythmias and torsade de points.

Use in children:

The efficacy and tolerability in the treatment of infections in children and adolescents under 16 years of age have not been proven.

In RCT studies, oral azithromycin has been prescribed to children (6 months to 16 years of age).

Recently, clinical guidelines for the administration of Off-Label /Unlabeled intravenous azithromycin in children and infants have been published.

How to prepare and use:

The initial solution is prepared by adding 4.8 mL of distilled water to the vial containing the powder and shaking the vial until the powder is completely dissolved. (Concentration: 100 mg Azithromycin/1mL)

Warning: The drug prepared for intravenous injection should be carefully inspected to ensure the absence of particles in the initial solution. If suspended particles are observed, the solution should be discarded.

Then, to obtain a concentration of 1 to 2 mg of azithromycin per ml, the above prepared solution should be added to a volume of 250-500 ml of a suitable solvent (0.9% sodium chloride, 0.45% sodium chloride, Ringer’s lactate-glucose 5% in water, 5% glucose in 0.45% sodium chloride, 5% glucose in 0.3% sodium chloride, 5% glucose in Ringer’s lactate) using a standard 5 ml syringe.

Final concentration of the solution for infusion solvent volume

1mg/mL 250 mL

2mg/mL 500 mL

Intravenous administration of a 500 mg dose of azithromycin diluted according to the above instructions should be carried out over a period of at least 60 minutes.

Concentration of prepared solution and duration of intravenous infusion:

mg/mL in 3 hours or1

mg/mL in 1 hours2

After preparation and dilution, it should be administered via intravenous infusion.

Warning:

Avoid intramuscular injection with direct intravenous injection.