Zymar eent

Generic Name: Gatifloxacin eent
Class: Antibacterials
Chemical Name: (±-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinoline- carboxylic acid sesquihydrate
Molecular Formula: C19H22FN3O4
CAS Number: 112811-59-3

Introduction

Antibacterial; 8-methoxy fluoroquinolone.1 4

Uses for Zymar

Bacterial Ophthalmic Infections

Treatment of conjunctivitis caused by susceptible Corynebacterium propinquum, Staphylococcus aureus, S. epidermidis, Streptococcus mitis, S. pneumoniae, or Haemophilus influenzae.1

Slideshow: 2014 Update: First Time Brand-to-Generic Switches

Role of topical fluoroquinolones in management of uncomplicated bacterial conjunctivitis not fully elucidated; some clinicians suggest that the drugs be reserved principally for severe bacterial conjunctivitis because of potential development of quinolone resistance, and possibly, cost considerations.8 10 11 12

Zymar Dosage and Administration

Administration

For topical use only.1 Not for injection.1 Not for subconjunctival injection or introduction directly into anterior chamber of the eye.1

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution.1

Avoid contamination of applicator tip.1

Dosage

Pediatric Patients

Bacterial Ophthalmic Infections
Conjunctivitis
Ophthalmic

Children ≥1 year of age: 1 drop of 0.3% solution in the affected eye(s) every 2 hours while awake (up to 8 times daily) for 2 days, then 1 drop up to 4 times daily while awake for the next 5 days.1

Adults

Bacterial Ophthalmic Infections
Conjunctivitis
Ophthalmic

1 drop of 0.3% solution in the affected eye(s) every 2 hours while awake (up to 8 times daily) for 2 days, then 1 drop up to 4 times daily while awake for the next 5 days.1

Cautions for Zymar

Contraindications

  • Hypersensitivity to gatifloxacin, other quinolones, or any ingredient in the formulation.1

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity

Serious, potentially fatal hypersensitivity reactions reported following systemic administration of fluoroquinolones; has occurred with the initial dose.1

If allergic reaction occurs, discontinue use and institute appropriate therapy if indicated.1

General Precautions

Superinfection

Possible overgrowth of nonsusceptible organisms (e.g., fungi) with prolonged use; if superinfection occurs, discontinue gatifloxacin and institute other appropriate therapy.1

Patient Monitoring

Careful monitoring, including slit-lamp biomicroscopy and fluorescein staining when appropriate, may be necessary in some patients.1

Specific Populations

Pregnancy

Category C.1

Lactation

Distributed into milk in rats after systemic administration; not known whether distributed into human milk.1 Use gatifloxacin ophthalmic preparations with caution.1

Pediatric Use

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

Geriatric Use

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

Common Adverse Effects

Conjunctival irritation, increased lacrimation, keratitis, papillary conjunctivitis, chemosis, conjunctival hemorrhage, ocular dryness, ocular discharge/irritation/pain, eyelid edema, headache, ocular redness, reduced visual acuity, taste disturbance.1

Zymar Pharmacokinetics

Absorption

Bioavailability

Serum gatifloxacin concentrations were undetectable (<5 ng/mL) after topical application to one eye of gatifloxacin 0.3 or 0.5% ophthalmic solution in an escalated dosage regimen (2 drops initially, then 2 drops 4 times daily for 7 days, and then 2 drops 8 times daily for 3 days).1

Stability

Storage

Ophthalmic

Solution

15–25°C; protect from freezing.1

Actions and Spectrum

  • Usually bactericidal.1

  • Like other fluoroquinolones, gatifloxacin inhibits bacterial DNA gyrase and topoisomerase IV.1 4 6

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

  • Active against C. propinquum, S. aureus, S. epidermidis, S. mitis, S. pneumoniae, and H. influenzae.1

Advice to Patients

  • Importance of discontinuing drug and informing clinician at first sign of rash or other sign of hypersensitivity.1

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the product.1

  • Importance of not wearing contact lenses in the presence of signs and symptoms of bacterial conjunctivitis.1 Contains benzalkonium chloride,1 which may be absorbed by soft contact lenses.13

  • Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs.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.

Gatifloxacin

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.3%

Zymar (with benzalkonium chloride)

Allergan

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Zymaxid 0.5% Solution (ALLERGAN): 3/$96.89 or 8/$257.60

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Allergan, Inc. Zymar (gatifloxacin) ophthalmic solution 0.3% prescribing information. Irvine, CA; 2004 Aug.

2. Allergan, Inc. Zymar (gatifloxacin) ophthalmic solution 0.3% formulary kit: summary of efficacy and safety. Irvine, CA; 2003.

3. Tepedino ME, Jensen HG. Efficacy and safety of gatifloxacin 0.3% ophthalmic solution compared with ofloxacin 0.3% for treatment of acute bacterial conjunctivitis. Poster presented at the annual meeting of the American Academy of Ophthalmology (AAO) Orlando, FL: 2002 Oct 20-3. Poster No. 165

4. Mah FS. New antibiotics for bacterial infections. Ophthalmol Clin North Am. 2003; 16:11-27. [PubMed 12683245]

5. Zhanel GC, Ennis K, Vercaigne L et al. A critical review of the fluoroquinolones: focus on respiratory tract infections. Drugs. 2002; 62:13-59. [PubMed 11790155]

6. O’Brien T. Conjunctivitis. In: Mandell GL, Bennett JE, Dolin R eds. Principles and practices of infectious diseases. 5th ed. New York: Churchill Livingstone; 2000:1251-6.

7. Limberg MB. A review of bacterial keratitis and bacterial conjunctivitis. Am J Ophthalmol. 1991; 112:2-9S.

8. Thielen TL, Castle SS, Terry JE. Anterior ocular infections: an overview of pathophysiology and treatment. Ann Pharmacother. 2000; 34:235-46. [IDIS 439875] [PubMed 10676832]

9. Bearden DT, Danziger LH. Mechanism of action of and resistance to quinolones. Pharmacotherapy. 2001; 21:224S-32S. [IDIS 472236] [PubMed 11642689]

10. Yolton DP. New antibacterial drugs for topical ophthalmic use. Optom Clin. 1992; 2:59-72.

11. Gwon A for the Ofloxacin Study Group II. Ofloxacin vs tobramycin for the treatment of external ocular infection. Arch Ophthalmol. 1992; 110:1234-7. [IDIS 301536] [PubMed 1520109]

12. Robert PY, Adenis JP. Comparative review of topical ophthalmic antibacterial preparations. Drugs. 2001; 61:175-85. [PubMed 11270936]

13. Allergan, Inc, Irvine, CA: Personal communication.

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