Mifloksan

Clear solution with yellow color.
Each mL contains: Moxifloxacin HCl equivalent to Moxifloxacin 5 mg.
Excipients/Inactive Ingredients: Sodium Chloride, Boric Acid, Disodium Tetraborate Decahydrate, Water for Injection.

Pharmacology: Moxifloxacin is a fourth-generation fluoroquinolone antibacterial agent active against a broad spectrum of Gram-positive and Gram-negative ocular pathogens, atypical microorganisms and anaerobes.
Microbiology: Moxifloxacin has activity against a wide range of Gram-positive and Gram-negative microorganisms. Moxifloxacin inhibits the topoisomerase II (DNA gyrase) and topoisomerase IV required for bacterial DNA replication, transcription, repair, and recombination.
The C8-methoxy moiety of moxifloxacin also lessens the selection of resistant mutants of Gram-positive bacteria compared to C8-H moiety found in older fluoroquinolones. Moxifloxacin's bulky C-7 substituent group interferes with the quinolone efflux pump mechanism of bacteria.
Moxifloxacin is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Fluoroquinolones, including moxifloxacin, differ in chemical structure and mode of action from β-lactam antibiotics, macrolides and aminoglycosides. Therefore organisms resistant to these drugs may be susceptible to moxifloxacin. Resistance to moxifloxacin develops slowly via multiple-step mutations and occurs at a general frequency between 10^-9 to 10^-11 for Gram-positive bacteria.
Moxifloxacin has been shown to be active against most strains of the following microorganisms.
Aerobic Gram-positive Microorganisms: Corynebacterium species; Micrococcus luteus including erythromycin, gentamicin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus aureus (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus epidermidis including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus haemolyticus (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus hominis (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus warneri (including erythromycin resistant strains); Staphylococcus pneumoniae (including penicillin, erythromycin, gentamicin, tetracycline and/or trimethoprim resistant strains); Streptococcus viridans group (including penicillin, erythromycin, tetracycline, and/or trimethoprim resistant strains).
Aerobic Gram-negative Microorganisms: Acinetobacter lwoffii; Haemophilus influenzae (including ampicillin resistant strains); Haemophilus parainfluenzae.
Other Microorganism: Chlamydia trachomatis.
The following organisms are considered susceptible when evaluated using systemic breakpoints. However, a correlation between the systemic breakpoint and the ophthalmological efficacy has not been established. The list of the organisms is provided as guidence only in assessing the potential treatment of conjungtival infections. Moxifloxacin exhibits minimal inhibitory concentrations (MICs) of 2 μg/mL or less (systemic susceptible breakpoint) against most (≥90%) strains of the following ocular pathogens.
Aerobic Gram-positive Microorganisms: Listeria monocytogenes; Streptococcus saprophyticus; Streptococcus agalactiae; Streptococcus mitis; Streptococcus pyogenes; Streptococcus group C, G and F.
Aerobic Gram-negative Microorganisms: 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 species; Prevotella species; Propionibacterium acnes.
Other Microorganisms: Chlamydia pneumoniae; Legionella pneumophila; Mycobacterium avium; Mycobacterium marinum; Mycoplasma pneumoniae.
Special Populations: The pharmacokinetic parameters of oral moxifloxacin are not significantly altered by mild, moderate or severe renal impairment. No dosage adjustment of MIFLOKSAN ophthalmic solution is necessary in patients with renal impairment.
Pharmacokinetic parameters of oral moxifloxacin were not significantly altered in patients with mild to moderate hepatic insufficiency (child-pugh classes A and B).
Studies are not performed in patients with severe hepatic impairment (child-pugh classes C). Because of the low systemic exposure by the topical route of administration, no dosage adjustment of MIFLOKSAN ophthalmic solution is needed in patients with hepatic impairment.

MIFLOKSAN ophthalmic solutions is indicated for the treatment of bacterial keratitis caused by susceptible strains of the following organism: Aerobic Gram-positive Microorganisms: Corynebacterium species; Micrococcus luteus (including erythromycin, gentamicin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus aureus (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus epidermidis (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus haemolyticus (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus hominis (including methicillin, erythromycin, gentamicin, ofloxacin, tetracycline, and/or trimethoprim resistant strains); Staphylococcus warneri (including erythromycin resistant strains); Staphylococcus pneumoniae (including penicillin, erythromycin, gentamicin, tetracycline and/or trimethoprim resistant strains); Streptococcus viridans group (including penicillin, erythromycin, tetracycline, and/or trimethoprim resistant strains).
Aerobic Gram-negative Microorganisms: Acinetobacter lwoffii; Haemophilus influenzae (including ampicillin resistant strains); Haemophilus parainfluenzae.
Other Microorganisms: Chlamydia trachomatis.

Instill one drop in the affected eye(s) 3 times a day for 7-14 days. The dose may be increased up to 8 times a day depending on clinical symptoms.

With the characteristics of this product, no toxic effects are expected with an ocular overdose of the product, or in the event of accidental ingestion of the contents of one bottle.

MIFLOKSAN ophthalmic solution is contraindicated in patients with a history of hypersensitivity to moxifloxacin, to other quinolones, or to any of the components in this medication.

For ocular use only. Not for injection.
MIFLOKSAN ophthalmic solution should not be injected subconjunctivally, nor should it be introduced directly into the anterior chamber of the eye.
In patients receiving systemically administered quinolones, serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported, some following the first dose. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria, and itching.
If an allergic reaction to moxifloxacin occurs, discontinue use of the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.
As with other anti-infectives, prolonged use may result in overgrowth of non-susceptible organism, including fungi. If superinfection occurs, discontinue use and institute alternative therapy.
Whenever clinical judgement dictates, the patients should be examined with the aid of magnification, such as slit-lamp biomicroscopy, and where appropriate, fluorescein staining. Patients should be advised not to wear contact lenses if they have symptoms of bacterial keratitis.
Tendon inflammation and rupture may occur with systemic fluoroquinolone therapy including moxifloxacin, particularly in older patients and those treated concurrently with corticosteroids. Therefore, treatment with MIFLOKSAN should be discontinued at the first sign of tendon inflammation.
Patient information: Avoid contaminating the applicator tip with the material from the eye, fingers or other source. Systemically administered quinolones have been associated with hypersensitivity reactions, even following a single dose. Discontinue use immediately and contact a physician at first sign of a rash or allergic reaction.
Effects on ability to drive and use machines: Temporary blurred vision or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs at instillation, the patients should wait until their vision clears before driving or using machinery.
Carcinogenesis, mutagenesis, impairment of fertility: Studies have not been performed to evaluate the effect of ocular administration of MIFLOKSAN on fertility.
Use in Children: The safety and effectiveness of MIFLOKSAN ophthalmic solution in pediatric have not been established. There is no evidence that the administration of MIFLOKSAN ophthalmic solution has any effect on weight bearing joints, even though oral administration of some quinolones has been shown to cause arthropathy in immature animals.
Use in the Elderly: No differences in safety and effectiveness between adult patients and elderly.

Pregnancy: MIFLOKSAN ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: MIFLOKSAN has not been measured in human milk, although it can be presumed to be excreted in human milk. At therapeutic doses of MIFLOKSAN ophthalmic solution no effects on the suckling child are anticipated. Caution should be exercised when MIFLOKSAN ophthalmic solution is administered to a nursing mother.

Nonocular adverse events were fever, increasing cough, infection, otitis media, pharyngitis, rash, and rhinitis.
The following adverse reactions are related to treatment (monotherapy with MIFLOKSAN ophthalmic solution) and classified according to the following convention: Very common (≥1/10), common (≥1/100 to <1/10), uncommon (>1/1,000 to ≤1/100), rare (>1/10,000 to ≤1/1,000), or very rare (≤1/10,000). Within each frequency grouping, adverse reactions are presented in decreasing order of seriousness. (See Table 1.)


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Adverse events identified from the post-marketing experience are as follows. The frequency of adverse events cannot be estimated from the existing data. Within each frequency grouping, adverse reactions are presented in decreasing order of seriousness. (See Table 2.)


Click on icon to see table/diagram/image

Unlike some other fluoroquinolones, no clinically significant drug-drug interactions between systemically administered moxifloxacin and itraconazole, theophylline, warfarin, digoxin, oral contraceptives, probenecid, ranitidine or glyburide. Moxifloxacin does not inhibit CYP3A4, CYP2D6, CYP2C9, CYP2C19 or CYP1A2 indicating that moxifloxacin is unlikely to alter the pharmacokinetics of the drugs metabolized by these cytochrome P450 isozymes.
Given the low systemic concentration of moxifloxacin following topical ocular administration of the medicinal product, drug interactions are unlikely to occur.

Use within 4 weeks after opening.
Store at 2°-25°C, in tight containers, protected from light.

Eye Anti-Infectives & Antiseptics

S01AE07 - moxifloxacin ; Belongs to the class of quinolone antiinfectives. Used in the treatment of eye infections.

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