Azidrop, eye drops 15 mg/g, bottles 0.25 g, 6 pcs.

Azidrop (eye drops 15 mg/g vial 0.25 g No. 6)

A country

France
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Active substance

Azithromycin

Compound

Active ingredient: azithromycin dihydrate 15 mg (in terms of azithromycin 14.3 mg); Excipient: medium chain triglycerides up to 1 g.

pharmachologic effect

Azithromycin is a broad-spectrum antibacterial agent belonging to the azalide class, inhibits protein synthesis by binding to the 50S ribosomal subunit, slows down the growth and reproduction of bacteria, and has a bactericidal effect in high concentrations. Acts on extra- and intracellular pathogens. Active against gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except those resistant to erythromycin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans group, Staphylococcus epidermidis, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilusducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Prevotella bivia, Clostridium perfringens, Peptostreptococcus spp; as well as Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi. Inactive against gram-positive bacteria resistant to erythromycin. Pharmacokinetics: If the drug is used twice a day, a sufficient therapeutic concentration of azithromycin in the tear fluid is ensured. The half-life of tear fluid is approximately 12 hours. The concentration of azithromycin in the blood plasma after instillation of Azidrop eye drops at the recommended dose is less than the detection threshold (less than 0.0002 mcg/ml).

Indications for use

Treatment of conjunctivitis caused by pathogens sensitive to the drug, including Chlamydia trachomatis, in adults and children over 1 year of age.

Mode of application

Locally. Adults and adolescents (from 12 to 17 years old), children (from 2 to 11 years old): instill one drop into the conjunctival sac of the affected eye twice a day (morning and evening) for three days. If there is no positive dynamics within 3 days of using the drug, you should consult a doctor and reconsider the treatment. Children (from 1 year to 2 years) When treating trachomatous conjunctivitis, no dose adjustment is required. There is no sufficient experience in the treatment of purulent bacterial conjunctivitis using Azidrop eye drops in children under 2 years of age. In the elderly, no dosage adjustment is required in elderly patients. Patients should follow the following recommendations: - hands should be washed thoroughly before instilling drops and after the procedure, - should not touch eyes and eyelids with the dropper tip of the bottle - after one-time use, the dropper tube must be thrown away along with the remaining residue. Do not use the remaining solution in the dropper tube for the next instillation.

Interaction

Interaction studies of Azidrop with all specific drugs have not been conducted. Due to the lack of detectable concentrations of azithromycin in blood plasma when instilled with eye drops, interactions are not expected with any of the drugs that interact with azithromycin when administered orally.

Side effect

Side effects observed during studies of the drug Azidrop, eye drops, are systematized in accordance with the World Health Organization (WHO) classification by frequency of occurrence: Immune system disorders. Very rare: hypersensitivity, angioedema (Quincke's edema). Eye disorders. .Very common: ocular discomfort (itching, burning, tingling) after instillation of the drug. Common: blurred vision, sensation of “sticking” of the eyelids, a foreign body in the eye. Uncommon: lacrimation. Very rare: eczema, erythema, swelling of the eyelids, eye allergies, conjunctival hyperemia, allergic conjunctivitis, conjunctivitis, keratitis.

Contraindications

Individual hypersensitivity to azithromycin and other macrolide antibiotics, as well as components of the drug, age less than 1 year. Use during pregnancy and lactation Since systemic exposure to azithromycin is insignificant, no harmful effects of the drug are expected during pregnancy. Azidrop, eye drops, can be used for treatment pregnant women as prescribed by the attending physician, if the expected therapeutic effect for the mother exceeds the risk of developing possible side effects in the fetus. There is limited evidence that azithromycin is excreted in breast milk, but given the low doses and low systemic availability, exposure in newborns is extremely low. Thus, treatment using the drug Azidrop during breastfeeding is acceptable. Children under one year of age There is not enough experience in the treatment of trachomatous conjunctivitis and purulent bacterial conjunctivitis using Azidrop eye drops in children under one year of age.

Overdose

There is no information about cases of overdose. The single-use package contains azithromycin in an amount sufficient to treat both eyes, but not enough to cause adverse reactions after accidental intravenous administration or ingestion of the solution.

special instructions

Eye drops should not be administered as injections or swallowed. Eye drops should not be administered as peri- or intraocular injections. In case of an allergic reaction to the drug, treatment should be discontinued. In case of concomitant treatment with other ophthalmic drugs, Azidrop should be instilled last, after 15 minutes after instillation of another drug. According to existing international recommendations for the treatment of diseases of the eyes and genitourinary tract, which can be highly likely to be transmitted to newborns, non-trachomatous conjunctivitis caused by Chlamydia trachomatis and conjunctivitis caused by Neisseria gonogrhoeae require systemic treatment. With the exception of the treatment of trachomatous conjunctivitis, Azidrop eye drops are not recommended for use in children under two years of age, as there is insufficient clinical information on the treatment in this age group. This type of treatment is not intended for use as a prophylaxis for bacterial conjunctivitis in newborns. The patient should be informed not to continue eye drops after completion of therapy on the third day, even if residual signs of bacterial conjunctivitis are still present. Patients suffering from bacterial conjunctivitis should not wear contact lenses. With systemic use of azithromycin, cases of fulminant hepatitis, which can potentially lead to life-threatening liver failure. When using the drug in ophthalmology, such a risk does not exist, since the systemic effect of the active substance is extremely insignificant. Patients who experience transient blurred vision after using eye drops are not recommended to drive vehicles or operate machinery until vision is restored.

Dispensing conditions in pharmacies

On prescription

Azidrop, 6 pcs., 0.25 g, 15 mg/g, eye drops

Antimicrobial drug for topical use. Azithromycin is a second generation macrolide antibiotic from the azalide group. Inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit and preventing peptide translocation.

Mechanism of resistance

Three mechanisms of resistance to macrolides are noted for different types of bacteria: due to modification of the target of action, modification of the antibiotic, or due to the active release of the antibiotic from the microbial cell using transport systems (efflux). Various efflux systems have been described for bacteria. An important efflux system for streptococci is encoded by the mef gene and leads to macrolide-limited resistance (M phenotype). Modification of the target of action, controlled by the erm-encoded methylase (MLSB phenotype), leads to cross-resistance to different classes of antibiotics.

Cases of cross-resistance to erythromycin, azithromycin, other macrolides and lincosamide and streptogramin B have been described for Streptococcus pneumoniae, group A β-hemolytic streptococci, Enterococcus spp. and Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA). Constitutive mutants in inducibly resistant strains with erm(A) or erm(C) can be isolated in vitro at low frequencies of approximately 10-7 CFU in the presence of azithromycin.

Borderline value

Below are the minimum inhibitory concentrations (MICs) for microorganisms for these indications.

It should be noted that the MIC breakpoints and spectrum of activity presented below are for systemic use. MIC data cannot be used in the case of topical treatment with the drug in the form of eye drops due to different concentrations and physicochemical conditions that may affect the overall activity of the drug at the site of action.

In accordance with EUCAST (European Committee on Antimicrobial Susceptibility Testing), the following MIC breakpoints are defined for azithromycin:

Haemophilus influenzaeS ≤ 0.12 mg/l and R >4 mg/lMoraxella catarrhalisS ≤ 0.5 mg/l and R>0.5 mg/lNeisseria gonorrhoeaeS ≤ 0.25 mg/l and R>0.5 mg/lStaphylococcus spp.S ≤ 1.0 mg/l and R >2.0 mg/l Streptococcus pneumoniaeS ≤ 0.25 mg/l and R>0.5 mg/l Streptococcus A, B, C, GS ≤ 0.25 mg/l and R>0.5 mg/l

EUCAST allows the use of erythromycin to determine the sensitivity of other species of specified bacteria to azithromycin.

The frequency of acquired resistance for individual species may vary depending on geographic region and time. Therefore, it is desirable to have local information on resistance, especially when treating severe infections. If necessary, specialist advice should be sought when the local incidence of resistance is such that the effectiveness of the drug, at least for some types of infection, is doubtful.

Clinical trial data

• Trachomatous conjunctivitis caused by Chlamydia trachomatis

A randomized, double-blind, 2-month comparative study of Azidrop with single-dose oral azithromycin was conducted for the treatment of active trachoma in 670 children aged 1–10 years. The primary efficacy variable was clinical cure at day 60, i.e. absence of active trachoma TF0 (according to the simplified WHO classification of trachoma severity). On day 60, the frequency of clinical cure with Azidrop, used 1 drop 2 times a day for 3 days, was no lower (96.3%) than when taking azithromycin orally (96.6%).

The clinical efficacy of Azidrop, used 1 drop 2 times a day for 3 days, for the treatment and prevention of trachoma in the entire population (from birth) in Northern Cameroon (112,000 subjects) was assessed in a multicenter, open-label, non-comparative phase IV study. Treatment was carried out in 3 periods lasting 1 year. The primary criterion for effectiveness was the prevalence of active trachoma, i.e. trachomatous follicular inflammation or severe trachomatous inflammation (TF+TI0 or TF+TI+). For the analysis, clinical assessment of trachoma was performed each year on 2400 children aged ≥1 and <10 years selected by cluster random sampling. The prevalence of active trachoma (TF+TI0 or TF+TI+) was observed in 31.1% of cases before Azidrop instillation in “year 0” and decreased to 6.3% (1 year), 3.1% (2 year) and 3.1% (3 year). Overall, no serious adverse reactions to the study drug were observed in the population.

• Purulent bacterial conjunctivitis

A randomized, blind comparative study of Azidrop, used 1 drop 2 times a day for 3 days, was conducted with tobramycin (eye drops, 0.3%), used 1 drop every 2 hours for 2 days, and then 4 times a day for for 5 days, for the treatment of purulent bacterial conjunctivitis in 1043 patients (ITT group), including 109 children under 11 years of age, 5 of whom were newborns (0 to 27 days), 38 infants and toddlers (28 days to 23 months). The per-protocol population (n=471) (RR group) included 16 infants and toddlers and did not include neonates. The clinical study was conducted in different regions of Europe, North Africa and India. The primary efficacy variable was clinical cure on day 9 in the RR group and was defined as 0 for bulbar conjunctival injection and for purulent discharge. On day 9, the clinical cure rate with Azidrop (87.8%) was no lower than with tobramycin (89.4%). The microbiological effectiveness of azithromycin was comparable to that of tobramycin.

• Children's population

The efficacy and safety of Azidrop in children and adolescents under 18 years of age was demonstrated in a randomized, investigator-blinded study compared with tobramycin in 282 study patients diagnosed with purulent bacterial conjunctivitis (including 148 patients in the 0 days - < 24 months subgroup). Patients received either Azidrop (1 drop 2 times a day for 3 days) or tobramycin eye drops, 0.3% (1 drop every 2 hours for 2 days, and then 4 times a day for 5 days). The main efficacy criterion was clinical cure of the more affected eye on day 3 in patients with positive bacteriological results on day 0. In patients treated with Azidrop, clinical cure of the more affected eye on day 3 was superior (47%) to this indicator in comparison with patients using tobramycin (28%). On day 7, 89% of patients treated with Azidrop were completely cured, while among patients treated with tobramycin, complete cure was observed in 78% of cases. There were no statistical differences between treatment groups regarding bacteriological resolution at day 7. Azidrop, administered 1 drop 2 times a day for 3 days, was well tolerated in all age groups in a study of a large group of children. Adverse reactions noted in children were also found in adults; no new adverse reactions were identified in children. Moreover, no age-related clinical problems were noted. The short duration of azithromycin therapy (eye drops 1.5%), the small number of instillations required, and the ease of instillation of drops in children were taken into account by both children and parents.

Pharmacokinetics

After instillation of Azidrop eye drops for the treatment of bacterial conjunctivitis at the recommended dose, azithromycin is not detected in the blood of patients (detection limit: 0.0002 μg/ml).

Pharmacokinetic studies were conducted in adults only