AZAMISIN eye drops, suspension

AZAMICIN

International non-proprietary name: Azithromycin

Composition

Active substance: 1 ml of suspension contains 10 mg of azithromycin.

Excipients: mannitol, citric acid, sodium citrate, benzalkonium chloride (preservative), EDTA, polexemar 407, HPMC E5, sodium chloride, sodium hydroxide, purified water.

Description

It is a white, microdisperse, odorless suspension.

Pharmacotherapeutic group

An antibacterial drug belonging to the group of macrolides. Azalid.

ATC code: S01AA26.

Pharmacological properties Pharmacodynamics

Azithromycin is a semisynthetic antibiotic belonging to the second generation macrolide group. Although it is a derivative of erythromycin, it differs from it in its

structure: the addition of a methylene group to the lactone ring with the help of a nitrogen atom. Since it differs from other macrolides, azithromycin belongs to azoles. Thus, azithromycin is a broad-spectrum antimicrobial drug belonging to the azalide group. It binds to the 50S subunit of ribosomes of microorganisms sensitive to azithromycin, inhibits protein synthesis, slows down the development and reproduction of bacteria. When it forms a high concentration at the site of inflammation, it has a bactericidal effect on intracellular and extracellular agents. Azithromycin has been shown to be highly effective against gram-positive and gram-negative microorganisms in a number of in vitro studies.

Azithromycin has bactericidal activity against the following microbes:

Aerobic gram(+) bacteria: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus spp., (belonging to group C, F and G),

Streptococcus viridans, Staphylococcus aureus.

Aerobic gram(-) bacteria: Heamophilus ducreyi, Heamophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila,

Campylobacter jejuni, Helicobacter pylori, Neisseria gonorrhoeae, Gardnerella vaginalis.

Anaerobic bacteria: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.

The preparation is also active against: Chlamydia trachortiatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia

burgdorferi.

Pharmacokinetics

Since azithromycin is a broad-spectrum antibiotic, it reaches its maximum plasma concentration 2-3 hours after oral administration. Since food intake weakens the

absorption of the drug, the drug is taken on an empty stomach. As a result of the conducted studies, it was determined that the tissue concentration of azithromycin is higher than the plasma concentration (about 50 times). After taking the drug in a dose of 500 mg, the concentration of the antibiotic in the lungs, tonsils, prostate gland and other organs is more than MIC90. The bioavailability of the drug is 37%. Azithromycin is mainly excreted unchanged in the bile, and 6% in the urine. The elimination half-life is 2-4 days.

During ophthalmic use, the concentration of azithromycin in blood plasma is very low, equal to 0.0002 μg/ml. Azithromycin has the ability to quickly penetrate into

tissues. It creates a high concentration in tissues and has a bactericidal effect. Since the half-life is long, the bactericidal effect is prolonged.

The concentration of azithromycin in the site of infection is higher than in healthy tissues and varies depending on the degree of inflammatory edema. Despite

creating a high concentration in phagocytes, azithromycin does not significantly affect their function. Azithromycin maintains the bactericidal concentration at the site of inflammation for 5-7 days after the last dose, which allows a short course of treatment of 3 days.

Instructions for use

Local treatment of infectious-inflammatory diseases of bacterial origin caused by agents sensitive to azithromycin in adults and children:

• Bacterial blepharitis

• Bacterial conjunctivitis (including trachomatous conjunctivitis caused by Chlamydia trachomatis)

• Bacterial keratoconjunctivitis, blepharoconjunctivitis

• Bacterial keratitis, endophthalmitis, dacryocystitis.

• Bacterial conjunctivitis caused by Neisseria gonorrhoeae in newborns

Prevention and treatment of infectious complications after ophthalmological operations