Xaflom^® (Drops) Instructions for Use

Marketing Authorization Holder

Sun Pharmaceutical Industries, Ltd. (India)

ATC Code

S01AE07 (Moxifloxacin)

Active Substance

Moxifloxacin (Rec.INN registered by WHO)

Dosage Form

Xaflom®

Eye drops 0.5%: dropper bottle 5 ml

Dosage Form, Packaging, and Composition

Eye drops in the form of a clear greenish-yellow solution.

Excipients : boric acid – 3 mg, sodium chloride – 6.4 mg, sodium hydroxide solution 10% – to adjust pH to 6.3-7.9, hydrochloric acid solution 10% – to adjust pH to 6.3-7.9, water for injections – up to 1 ml.

5 ml – polyethylene dropper bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group for topical use in ophthalmology

Pharmacotherapeutic Group

Drugs used in ophthalmology; antimicrobials; fluoroquinolones

Pharmacological Action

An antibacterial drug of the IV generation, a fluoroquinolone, has a bactericidal effect. It exhibits activity against a wide range of gram-positive and gram-negative microorganisms, anaerobic, acid-fast and atypical bacteria.

The mechanism of action is associated with the inhibition of topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an enzyme involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme involved in the cleavage of chromosomal DNA during bacterial cell division.

There is no cross-resistance with macrolides, aminoglycosides and tetracyclines. Cross-resistance between systemically used moxifloxacin and other fluoroquinolones has been reported.

Moxifloxacin is active against most strains of microorganisms (both in vitro and in vivo):

Gram-positive bacteria: Corynebacterium spp., including Corynebacterium diphtheriae; Micrococcus luteus (including strains insensitive to erythromycin, gentamicin, tetracycline and/or trimethoprim); Staphylococcus aureus (including strains insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and/or trimethoprim); Staphylococcus epidermidis (including strains insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and/or trimethoprim); Staphylococcus haemolyticus (including strains insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and/or trimethoprim); Staphylococcus hominis (including strains insensitive to methicillin, erythromycin, gentamicin, ofloxacin, tetracycline and/or trimethoprim); Staphylococcus warneri (including strains insensitive to erythromycin); Streptococcus mitis (including strains insensitive to penicillin, erythromycin, tetracycline and/or trimethoprim); Streptococcus pneumoniae (including strains insensitive to penicillin, erythromycin, gentamicin, tetracycline and/or trimethoprim); Streptococcus group viridans (including strains insensitive to penicillin, erythromycin, tetracycline and/or trimethoprim).

Gram-negative bacteria: Acinetobacter Iwoffii; Haemophilus influenzae (including strains insensitive to ampicillin); Haemophilus parainfluenzae; Klebsiella spp.

Other microorganisms: Chlamydia trachomatis.

Moxifloxacin acts in vitro against most of the microorganisms listed below, but the clinical significance of these data is unknown:

Gram-positive bacteria: Listeria monocytogenes; Staphylococcus saprophyticus; Streptococcus agalactiae; Streptococcus mitis; Streptococcus pyogenes; Streptococcus group C, G, F;

Gram-negative bacteria: Acinetobacter baumannii; Acinetobacter calcoaceticus; Citrobacter freundii; Citrobacter koseri; Enterobacter aerogenes; Enterobacter cloacae; Escherichia coli; Klebsiella oxytoca; Klebsiella pneumoniae; Moraxella catarrhalis; Morganella morganii; Neisseria gonorrhoeae; Proteus mirabilis; Proteus vulgaris; Pseudomonas stutzeri;

Anaerobic microorganisms: Clostridium perfringens; Fusobacterium spp.; Prevotella spp.; Propionibacterium acnes.

Other organisms: Chlamydia pneumoniae; Legionella pneumophila; Mycobacterium avium; Mycobacterium marinum; Mycoplasma pneumoniae.

Pharmacokinetics

With topical application, systemic absorption of moxifloxacin occurs: C_max is 2.7 ng/ml, the AUC value is 45 ng×h/ml. These values are approximately 1600 times and 1000 times lower than C_max and AUC after administration of a therapeutic dose of moxifloxacin 400 mg orally. T_1/2 of moxifloxacin from plasma is about 13 hours.

Indications

Bacterial conjunctivitis caused by microorganisms sensitive to moxifloxacin.

ICD codes

Dosage Regimen

Topically. For adults, 1 drop into the affected eye 3 times/day. Usually, improvement occurs within 5 days and treatment should be continued for the next 2-3 days. If the condition does not improve after 5 days, the correctness of the diagnosis and/or prescribed treatment should be questioned. The duration of treatment depends on the severity of the condition and the clinical and bacteriological course of the disease.

Adverse Reactions

From the hematopoietic system rarely – decreased hemoglobin.

From the immune system frequency unknown – hypersensitivity.

From the nervous system infrequently – headache; rarely – paresthesia; frequency unknown – dizziness.

From the organ of vision often – eye pain, eye irritation; infrequently – punctate keratitis, dry eye syndrome, subconjunctival hemorrhage, eye itching, conjunctival injection, eyelid edema, eye discomfort; rarely – corneal epithelial defect, corneal disorders, conjunctivitis, blepharitis, conjunctival edema, blurred vision, decreased visual acuity, asthenopia, eyelid erythema; frequency unknown – endophthalmitis, ulcerative keratitis, corneal erosion, increased intraocular pressure, corneal opacity, corneal edema, corneal infiltrates, corneal deposits, allergic eye phenomena, keratitis, corneal edema, photophobia, lacrimation, eye discharge, foreign body sensation in the eyes.

From the cardiovascular system frequency unknown – palpitations.

From the respiratory system rarely – nasal discomfort, laryngeal and pharyngeal pain, foreign body sensation in the throat; frequency unknown – dyspnea.

From the digestive system infrequently – dysgeusia; rarely – vomiting, increased activity of aminotransferases and GGT; frequency unknown – nausea.

From the skin and subcutaneous tissue frequency unknown – erythema, rash, urticaria, pruritus.

Contraindications

Hypersensitivity to moxifloxacin or to other quinolones; breastfeeding period; children under 1 year of age.

Use in Pregnancy and Lactation

There is insufficient experience with use during pregnancy and lactation. Use during pregnancy (FDA category C) is possible only if the expected therapeutic benefit for the mother outweighs the potential risk to the fetus and child. If it is necessary to use during lactation, breastfeeding should be discontinued for the duration of treatment.

Use in Hepatic Impairment

Dose adjustment is not required.

Use in Renal Impairment

Dose adjustment is not required.

Pediatric Use

No adjustment of the dosage regimen is required when used in children from 1 year of age.

Geriatric Use

Dose adjustment is not required.

Special Precautions

Long-term use of the antibiotic may lead to excessive growth of non-susceptible microorganisms, including fungi. If superinfection occurs, the drug should be discontinued and appropriate therapy instituted.

There is insufficient data to draw a conclusion about the efficacy and safety of moxifloxacin for the treatment of bacterial conjunctivitis in newborns, therefore use in patients of this age category is not recommended.

Moxifloxacin is not recommended for prophylactic use or for ex juvantibus therapy (empirical treatment) of gonococcal conjunctivitis, including in the treatment of gonococcal ophthalmia of newborns, due to the large number of Neisseria gonorrhoeae strains resistant to moxifloxacin. Patients with infectious eye diseases caused by Neisseria gonorrhoeae should receive appropriate systemic therapy.

The use of moxifloxacin for the treatment of infectious diseases of the eye caused by Chlamydia trachomatis in patients under 2 years of age is not recommended, since there is no information on the study of the drug in this category of patients. The use of moxifloxacin in patients over 2 years of age with eye diseases caused by Chlamydia trachomatis should be combined with systemic therapy.

In neonatal ophthalmia, patients should receive treatment appropriate to their condition; for example, in the development of conjunctivitis of chlamydial and gonorrheal etiology, such treatment will be systemic therapy.

Effect on the ability to drive vehicles and mechanisms

After using the drug, a temporary decrease in the clarity of visual perception is possible, and until it is restored, it is not recommended to drive a car and engage in activities that require increased attention and reaction.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.