Ozenoxacin (Monograph)

Brand name: Xepi
Drug class: Antibacterials
VA class: 84:04.04
Chemical name: 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino) pyridin-3-yl]-4-oxoquinoline-3-carboxylic acid
Molecular formula: C₂₁H₂₁N₃O₃
CAS number: 245765-41-7

Medically reviewed by Drugs.com on May 24, 2023. Written by ASHP.

Introduction

Antibacterial; nonfluorinated quinolone anti-infective.

Uses for Ozenoxacin

Impetigo

Topical treatment of impetigo caused by Staphylococcus aureus and Streptococcus pyogenes (group A β-hemolytic streptococci; GAS).

Although impetigo may be self-limiting, anti-infective treatment usually indicated to reduce duration of symptoms and prevent recurrence or transmission to others. Empiric treatment with an appropriate narrow-spectrum anti-infective generally used for initial treatment and considered reasonable for typical cases. Some clinicians suggest in vitro testing (i.e., Gram stain and culture of pus or exudates from skin lesions) to identify causative organism and confirm in vitro susceptibility, especially if impetigo is extensive and/or failed to respond to initial empiric treatment.

Nonbullous and bullous impetigo have been treated with topical and/or systemic anti-infective therapy. Although comparative efficacy of various regimens not established in well-controlled clinical trials, topical anti-infectives generally used for less extensive disease and systemic anti-infectives generally recommended if impetigo is severe or involves numerous lesions or if an outbreak is affecting multiple individuals (e.g., family members, childcare groups, athletic teams).

When empiric treatment used, select appropriate narrow-spectrum anti-infective based on local patterns of resistance reported for S. aureus and S. pyogenes.

Related/similar drugs

cefuroxime, mupirocin topical, cefadroxil, Bactroban, Ceftin, Duricef

Ozenoxacin Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a 1% cream.

Do not apply to eyes or mucous membranes; do not administer orally, intranasally, or intravaginally.

Apply thin layer of cream to affected area. May be applied to a maximum total treatment area of 100 cm² in adults and pediatric patients ≥12 years of age or a maximum of 2% of total body surface area (≤100 cm²) in pediatric patients 2 months through 11 years of age.

Treated area may be covered with sterile bandage or gauze dressing, if desired.

Wash hands after applying the cream, unless the hands are being treated.

Dosage

Pediatric Patients

Skin Infections

Impetigo

Topical

Children ≥2 months of age: Apply thin layer of 1% cream to affected area twice daily for 5 days.

Adults

Skin Infections

Impetigo

Topical

Apply thin layer of 1% cream to affected area twice daily for 5 days.

Prescribing Limits

Pediatric Patients

Skin Infections

Impetigo

Topical

Pediatric patients 2 months through 11 years of age: Maximum treatment area is 2% of total body surface area (≤100 cm²).

Pediatric patients ≥12 years of age: Maximum treatment area is 100 cm².

Adults

Skin Infections

Impetigo

Topical

Maximum treatment area is 100 cm².

Cautions for Ozenoxacin

Contraindications

• Manufacturer states no known contraindications.

Warnings/Precautions

Administration Precautions

For external use only.

Use only for topical application to skin. Not intended for oral, intranasal, ophthalmic, or intravaginal use.

Superinfection

Prolonged use may result in overgrowth of nonsusceptible bacteria and fungi.

If superinfection occurs, discontinue ozenoxacin and institute appropriate therapy.

Specific Populations

Pregnancy

Data not available regarding use in pregnant women. Systemic absorption is negligible following topical application to skin (see Absorption under Pharmacokinetics); maternal use of ozenoxacin 1% cream not expected to result in fetal exposure.

No animal reproduction studies using ozenoxacin. Toxicity studies using oral ozenoxacin in pregnant rats and rabbits have not revealed any significant adverse developmental effects at exposures >10,000 times the maximum human plasma concentrations reported following topical application to skin.

Lactation

Not known whether systemically absorbed ozenoxacin distributed into human milk, affects human milk production, or affects breast-fed infants. Systemic absorption is negligible following topical application to skin (see Absorption under Pharmacokinetics); maternal use of ozenoxacin 1% cream not expected to result in exposure in breast-fed child.

Consider benefits of breast-feeding and importance of topical ozenoxacin to the woman; also consider potential adverse effects on breast-fed child from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy of ozenoxacin 1% cream not established in infants <2 months of age.

Safety and efficacy for topical treatment of impetigo in pediatric patients ≥2 months of age is supported by evidence from adequate and well-controlled studies that included pediatric patients 2 months through 17 years of age; safety profile in this age group similar to that reported in adults.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently to ozenoxacin 1% cream than younger patients. Other reported clinical experience has not identified differences in responses between geriatric and younger patients.

Common Adverse Effects

Rosacea, seborrheic dermatitis.

Drug Interactions

In vitro, high ozenoxacin concentrations cause weak inhibition of CYP3A4 and 2C9.

Potential interactions between ozenoxacin and other drugs not studied to date.

Specific Drugs

Ozenoxacin Pharmacokinetics

Absorption

Following topical application of ozenoxacin to skin, only negligible amounts absorbed systemically. Appears to remain in upper skin layers (stratum corneum and epidermidis); does not easily penetrate to lower skin layers.

Systemic absorption following topical application of ozenoxacin creams of varying strengths (up to 2%, twice the strength of commercially available cream) was evaluated in 86 healthy individuals and patients with impetigo. Following single or repeated application of ≤1 g of ozenoxacin cream to intact or abraded skin (surface area ≤200 cm²), systemic absorption occurred at the level of detection (0.489 ng/mL) in 2 study participants; no evidence of systemic absorption in any other study participants.

Distribution

Plasma Protein Binding

Approximately 80–85%.

Elimination

Metabolism

In vitro studies indicate ozenoxacin not metabolized in presence of fresh human skin discs and minimally metabolized in hepatocytes.

Elimination Route

Not investigated because systemic absorption following topical application to skin is negligible.

Stability

Storage

Topical

Cream

20–25ºC (may be exposed to 15–30°C).

Actions and Spectrum

• Nonfluorinated quinolone anti-infective.

• Inhibits bacterial DNA gyrase A and topoisomerase IV, enzymes involved in bacterial DNA transcription and replication. Bactericidal in vitro against susceptible S. aureus and S. pyogenes (group A β-hemolytic streptococci; GAS).

• Gram-positive bacteria: Active in vitro and in clinical infections against S. aureus (including methicillin-resistant S. aureus [MRSA]; also known as oxacillin-resistant S. aureus or ORSA]) and S. pyogenes. Although clinical importance unclear, also has in vitro activity against S. epidermidis (including methicillin-resistant S. epidermidis), S. agalactiae (group B streptococci; GBS), and some Corynebacterium.

• Active in vitro against some S. aureus and S. epidermidis with decreased susceptibility or resistance to fluoroquinolones (e.g., ciprofloxacin, levofloxacin, moxifloxacin).

• Resistance to quinolones may be due to mutations in ≥1 of the genes that encode DNA gyrase A or topoisomerase IV. Quinolone-resistant bacteria typically have a combination of mutations within gyrA and parC subunits.

Advice to Patients

• Importance of applying ozenoxacin 1% cream to affected skin as directed.

• Advise patients that ozenoxacin cream is for external use only and should not be swallowed or used in eyes or nose, on mouth or lips, or inside female genital tract.

• Inform patients that treated areas may be covered with sterile bandage or gauze dressing, if desired. Advise patients to wash hands after applying ozenoxacin cream, unless the hands are being treated.

• Importance of completing full course of treatment, even if symptoms improve.

• Advise patients to notify a clinician if symptoms do not improve within 3 days after starting treatment.

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

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

• Importance of informing patients of other important precautionary information. (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.

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Frequently asked questions

• What is Xepi (ozenoxacin) used to treat?

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