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, 2024. Written by ASHP.

Introduction

Antibacterial; nonfluorinated quinolone anti-infective.^{1 3 4 5 6}

Uses for Ozenoxacin

Impetigo

Topical treatment of impetigo caused by Staphylococcus aureus and Streptococcus pyogenes (group A β-hemolytic streptococci; GAS).^{1 8 9}

Although impetigo may be self-limiting, anti-infective treatment usually indicated to reduce duration of symptoms and prevent recurrence or transmission to others.^{2 14 15} Empiric treatment with an appropriate narrow-spectrum anti-infective generally used for initial treatment and considered reasonable for typical cases.^{15 43} 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,^{2 43 110 292} especially if impetigo is extensive and/or failed to respond to initial empiric treatment.^{2 110}

Nonbullous and bullous impetigo have been treated with topical and/or systemic anti-infective therapy.^{2 14 15 43 110} Although comparative efficacy of various regimens not established in well-controlled clinical trials,^{2 14} topical anti-infectives generally used for less extensive disease and systemic anti-infectives generally recommended if impetigo is severe or involves numerous lesions^{2 14 15 43 110 292} or if an outbreak is affecting multiple individuals (e.g., family members, childcare groups, athletic teams).^{43 292}

When empiric treatment used, select appropriate narrow-spectrum anti-infective based on local patterns of resistance reported for S. aureus and S. pyogenes.^{2 14 15 292}

Ozenoxacin Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a 1% cream.¹

Do not apply to eyes or mucous membranes;¹ do not administer orally, intranasally, or intravaginally.¹

Apply thin layer of cream to affected area.¹ 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.¹

Treated area may be covered with sterile bandage or gauze dressing, if desired.¹

Wash hands after applying the cream, unless the hands are being treated.¹

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.¹

Adults

Skin Infections

Impetigo

Topical

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

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).¹

Pediatric patients ≥12 years of age: Maximum treatment area is 100 cm².¹

Adults

Skin Infections

Impetigo

Topical

Maximum treatment area is 100 cm².¹

Cautions for Ozenoxacin

Contraindications

• Manufacturer states no known contraindications.¹

Warnings/Precautions

Administration Precautions

For external use only.¹

Use only for topical application to skin.¹ Not intended for oral, intranasal, ophthalmic, or intravaginal use.¹

Superinfection

Prolonged use may result in overgrowth of nonsusceptible bacteria and fungi.¹

If superinfection occurs, discontinue ozenoxacin and institute appropriate therapy.¹

Specific Populations

Pregnancy

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

No animal reproduction studies using ozenoxacin.¹ 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.¹

Lactation

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

Consider benefits of breast-feeding and importance of topical ozenoxacin to the woman;¹ also consider potential adverse effects on breast-fed child from the drug or underlying maternal condition.¹

Pediatric Use

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

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;¹ safety profile in this age group similar to that reported in adults.¹

Geriatric Use

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

Common Adverse Effects

Rosacea,^{1 8} seborrheic dermatitis.^{1 8}

Drug Interactions

In vitro, high ozenoxacin concentrations cause weak inhibition of CYP3A4 and 2C9.¹⁰

Potential interactions between ozenoxacin and other drugs not studied to date.¹⁰

Specific Drugs

Ozenoxacin Pharmacokinetics

Absorption

Following topical application of ozenoxacin to skin, only negligible amounts absorbed systemically.¹ Appears to remain in upper skin layers (stratum corneum and epidermidis);¹⁰ does not easily penetrate to lower skin layers.¹⁰

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.¹ 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;¹ no evidence of systemic absorption in any other study participants.¹

Distribution

Plasma Protein Binding

Approximately 80–85%.¹

Elimination

Metabolism

In vitro studies indicate ozenoxacin not metabolized in presence of fresh human skin discs and minimally metabolized in hepatocytes.¹

Elimination Route

Not investigated because systemic absorption following topical application to skin is negligible.¹

Stability

Storage

Topical

Cream

20–25ºC (may be exposed to 15–30°C).¹

Actions and Spectrum

• Nonfluorinated quinolone anti-infective.^{1 3 4 5 6}

• Inhibits bacterial DNA gyrase A and topoisomerase IV, enzymes involved in bacterial DNA transcription and replication.^{1 4 5 11} Bactericidal in vitro against susceptible S. aureus and S. pyogenes (group A β-hemolytic streptococci; GAS).^{1 5 6}

• 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])^{1 3 6 11 12} and S. pyogenes.^{1 3 6 11 12} Although clinical importance unclear, also has in vitro activity against S. epidermidis (including methicillin-resistant S. epidermidis),^{3 6 11 12} S. agalactiae (group B streptococci; GBS),^{3 6 11} and some Corynebacterium.¹²

• Active in vitro against some S. aureus and S. epidermidis with decreased susceptibility or resistance to fluoroquinolones (e.g., ciprofloxacin, levofloxacin, moxifloxacin).^{3 4 5 11 12}

• Resistance to quinolones may be due to mutations in ≥1 of the genes that encode DNA gyrase A or topoisomerase IV.^{1 5} Quinolone-resistant bacteria typically have a combination of mutations within gyrA and parC subunits.^{1 3 6}

Advice to Patients

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

• 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.¹

• Inform patients that treated areas may be covered with sterile bandage or gauze dressing, if desired.¹ Advise patients to wash hands after applying ozenoxacin cream, unless the hands are being treated.¹

• Importance of completing full course of treatment, even if symptoms improve.¹

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

Frequently asked questions

• What is Xepi (ozenoxacin) used to treat?

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