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Besifloxacin Hydrochloride

Class: Antibacterials
VA Class: OP210
Chemical Name: (+)-7-[(3R)-3-aminohexahydro-1H-azepin-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride
Molecular Formula: C19H21ClFN3O3•HCl
CAS Number: 405165-61-9
Brands: Besivance

Introduction

Antibacterial; 8-chloro fluoroquinolone.1

Uses for Besifloxacin Hydrochloride

Bacterial Ophthalmic Infections

Topical treatment of conjunctivitis caused by Aerococcus viridans, CDC coryneform group G, Corynebacterium pseudodiphtheriticum, C. striatum, Haemophilus influenzae, Moraxella catarrhalis, M. lacunata, Pseudomonas aeruginosa, Staphylococcus aureus, S. epidermidis, S. hominis, S. lugdunensis, S. warneri, Streptococcus mitis group, S. oralis, S. pneumoniae, or S. salivarius.1 2 3 5

Many cases of mild, acute bacterial conjunctivitis resolve spontaneously without anti-infective therapy.6 17 18 19 Although topical ophthalmic anti-infectives may shorten time to resolution and reduce severity and risk of complications,6 17 18 19 avoid indiscriminate use of topical anti-infectives.6 17

Treatment of acute bacterial conjunctivitis generally is empiric;6 17 18 use of a broad-spectrum topical ophthalmic antibacterial usually recommended.6 17 18 In vitro staining and/or cultures of conjunctival material may be indicated in diagnosis and management of recurrent, severe, or chronic purulent conjunctivitis or when acute conjunctivitis does not respond to initial empiric topical treatment.6 17 18

Besifloxacin Hydrochloride Dosage and Administration

Administration

Ophthalmic Administration

Apply 0.6% ophthalmic suspension topically to the eye.1

For topical ophthalmic use only;1 do not inject subconjunctivally and do not introduce directly into anterior chamber of the eye.1

Wash hands prior to administration.1

Invert the closed bottle containing besifloxacin ophthalmic suspension and shake once prior to each use.1

Avoid contaminating applicator tip with material from eye, fingers, or other source.1

Dosage

Available as besifloxacin hydrochloride;1 dosage expressed in terms of besifloxacin.1

Pediatric Patients

Bacterial Ophthalmic Infections
Conjunctivitis
Ophthalmic

Children ≥1 year of age: Instill 1 drop of 0.6% suspension in the affected eye(s) 3 times daily (give doses 4–12 hours apart) for 7 days.1

Adults

Bacterial Ophthalmic Infections
Conjunctivitis
Ophthalmic

Instill 1 drop of 0.6% suspension in the affected eye(s) 3 times daily (give doses 4–12 hours apart) for 7 days.1

Cautions for Besifloxacin Hydrochloride

Contraindications

  • Manufacturer states none known.1

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity

Although besifloxacin is not used systemically, consider that hypersensitivity reactions have been reported with systemic quinolones, even following a single dose.1

Immediately discontinue at first sign of rash or hypersensitivity reaction.1

Administration Precautions

For topical ophthalmic use only;1 not for injection into the eye.1

Superinfection

Prolonged use may result in overgrowth of nonsusceptible organisms (e.g., fungi).1

If superinfection occurs, discontinue besifloxacin ophthalmic suspension and institute appropriate therapy.1

Patient Monitoring

Whenever clinical judgment dictates, examine patient with the aid of magnification (e.g., slit lamp biomicroscopy) and, if appropriate, fluorescein staining.1 2

Contact Lenses

Do not wear contact lenses during treatment with besifloxacin ophthalmic suspension or if any signs or symptoms of bacterial conjunctivitis are present.1

Specific Populations

Pregnancy

Category C.1

Data not available regarding use of besifloxacin 0.6% ophthalmic suspension in pregnant women.1

Lactation

Although not measured in human milk, presumed to be distributed into human milk.1

Use with caution in nursing women.1

Pediatric Use

Safety and efficacy not established in children <1 year of age.1

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.1

Common Adverse Effects

Conjunctival redness.1

Interactions for Besifloxacin Hydrochloride

No formal drug interaction studies using besifloxacin 0.6% ophthalmic suspension.1

Besifloxacin Hydrochloride Pharmacokinetics

Absorption

Bioavailability

After topical application of besifloxacin 0.6% ophthalmic suspension to each eye 3 times daily for 16 doses, maximum plasma concentrations of the drug were <1.3 ng/mL.1

Distribution

Extent

Penetrates into conjunctiva and aqueous humor;2 maximum concentrations reported are 62.8 and 1.7 mcg/mL, respectively.2

Elimination

Half-life

Average elimination half-life of systemically absorbed drug estimated to be 7 hours.1

Stability

Storage

Ophthalmic

Suspension

15–25°C.1 Protect from light.1

Contains benzalkonium chloride as a preservative.1

Actions and Spectrum

  • Fluoroquinolone anti-infective.1

  • Like other fluoroquinolones, inhibits DNA synthesis in susceptible bacteria via inhibition of DNA topoisomerases (DNA gyrase, topoisomerase IV).1 2

  • Spectrum of activity includes gram-positive aerobic bacteria and some gram-negative aerobic bacteria.1 2

  • Active in vitro and in vivo in conjunctival infections against Aerococcus viridans, CDC coryneform group G, Corynebacterium pseudodiphtheriticum, C. striatum, Haemophilus. influenzae, Moraxella catarrhalis, M. lacunata, Pseudomonas aeruginosa, Staphylococcus aureus, S. epidermidis, S. hominis, S. lugdunensis, S. warneri, Streptococcus mitis group, S. oralis, S. pneumoniae, and S. salivarius.1

  • Cross-resistance between besifloxacin and some other fluoroquinolones reported.1

Advice to Patients

  • Advise patients to avoid contaminating applicator tip with material from the eye, fingers, or other source.1

  • Instruct patients to wash their hands prior to administration of the ophthalmic suspension and to invert the closed bottle and shake once prior to each use.1

  • Importance of completing the entire prescribed course of treatment, even if feeling better after a few days.1

  • Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with besifloxacin or other antibacterials in the future.1

  • Advise patients not to wear contact lenses during treatment with besifloxacin ophthalmic suspension or if any signs or symptoms of bacterial conjunctivitis are present.1

  • Advise patients to immediately discontinue besifloxacin ophthalmic suspension and contact a clinician at first sign of rash or hypersensitivity reaction.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Besifloxacin Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Suspension

0.6% (of besifloxacin)

Besivance

Bausch & Lomb

AHFS DI Essentials. © Copyright 2017, Selected Revisions May 22, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Bausch & Lomb. Besivance (besifloxacin ophthalmic suspension) 0.6% prescribing information. Bridgewater, NJ; 2016 Jun.

2. Karpecki P, DePaolis M, Hunter JA et al. Besifloxacin ophthalmic suspension 0.6% in patients with bacterial conjunctivitis: a multicenter, prospective, randomized, double-masked, vehicle-controlled, 5-day efficacy and safety study. Clin Ther. 2009; 31:514-26. [PubMed 19393842]

3. Tepedino ME, Heller WH, Usner DW et al. Phase III efficacy and safety study of besifloxacin ophthalmic suspension 0.6% in the treatment of bacterial conjunctivitis. Curr Med Res Opin. 2009; 25:1159-69. [PubMed 19323612]

5. McDonald MB, Protzko EE, Brunner LS et al. Efficacy and safety of besifloxacin ophthalmic suspension 0.6% compared with moxifloxacin ophthalmic solution 0.5% for treating bacterial conjunctivitis. Ophthalmology. 2009; 116:1615-23. [PubMed 19643483]

6. Barnes SD, Kumar NM, Pavin-Langston D et al. Microbial Conjunctivitis. In: Bennett JE, Dolin R, and Blaser MJ, eds. Mandell, Douglas, and Bennett's principles and practices of infectious diseases. 8th ed. Philadelphia, PA: Elsevier Saunders; 2015:1392-1401.

17. American Academy of Ophthalmology. Preferred practice pattern (PPP) guidelines: conjunctivitis PPP - 2013. From American Academy of Ophthalmology website. Accessed 17 Oct 2016.

18. Azari AA, Barney NP. Conjunctivitis: a systematic review of diagnosis and treatment. JAMA. 2013; 310:1721-9. [PubMed 24150468]

19. Sheikh A, Hurwitz B, van Schayck CP et al. Antibiotics versus placebo for acute bacterial conjunctivitis. Cochrane Database Syst Rev. 2012; :CD001211. [PubMed 22972049]

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