Generic Name: Ozenoxacin
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
Ozenoxacin is a quinolone antibacterial.1
Uses for Xepi
Ozenoxacin has the following uses:
Ozenoxacin is a quinolone anti-infective indicated for the topical treatment of impetigo due to Staphylococcus aureus or Streptococcus pyogenes in adult and pediatric patients 2 months of age and older: 1
Xepi Dosage and Administration
Ozenoxacin is available in the following dosage form(s) and strength(s):
Cream, 1%. Each gram of cream contains 10 mg of ozenoxacin. 1
It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:
Dosage & Administration Section
Apply a thin layer of ozenoxacin 1% cream topically to the affected area twice daily for 5 days.1
Affected area may be up to 100 cm2 in adult and pediatric patients 12 years of age and older or 2% of the total body surface area and not exceeding 100 cm2 in pediatric patients less than 12 years of age.1
For topical use only.1
Not for oral, ophthalmic, intranasal, or intravaginal use.1
Cautions for Xepi
Potential for Microbial Overgrowth
The prolonged use of ozenoxacin cream may result in overgrowth of nonsusceptible bacteria and fungi. If such infections occur during therapy, discontinue use and institute appropriate supportive measures.1
There are no available data on the use of ozenoxacin cream in pregnant women to inform a drug associated risk. Systemic absorption of ozenoxacin in humans is negligible following topical administration of ozenoxacin (up to twice the concentration of the marketed formulation). Due to the negligible systemic exposure, it is not expected that maternal use of ozenoxacin cream will result in fetal exposure to the drug.1
Animal reproduction studies were not conducted with ozenoxacin cream. However, toxicity studies conducted in pregnant rats and rabbits administered the oral form of ozenoxacin showed no significant adverse developmental effects (at >10,000 times the maximum human plasma concentration seen with dermal application of ozenoxacin).1
The estimated background risk of major birth defects and miscarriage for the indicated population are unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.1
No data are available regarding the presence of ozenoxacin in human milk, and the effects of ozenoxacin on the breastfed infant or on milk production. However, breastfeeding is not expected to result in exposure of the child to ozenoxacin due to the negligible systemic absorption of ozenoxacin in humans following topical administration of ozenoxacin. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for ozenoxacin cream and any potential adverse effects on the breast-fed child from ozenoxacin or from the underlying maternal condition.1
The safety and effectiveness of ozenoxacin cream in the treatment of impetigo have been established in pediatric patients 2 months to 17 years of age. Use of ozenoxacin cream in pediatric patients (2 months to 17 years of age) is supported by evidence from adequate and well-controlled studies in which 251 pediatric patients received at least one dose of ozenoxacin cream. The median age of the patients enrolled in the clinical trials was 10 years; 3 % of patients were 2 months to less than 2 years of age, 55% of patients were 2 to less than 12 years of age, 11% of patients were 12 to less than 18 years of age, and 31% of patients were 18 years of age or older. In these studies, the maximum dose applied was approximately 0.5 g of ozenoxacin cream (approximately 5 mg of ozenoxacin) applied twice daily for up to 5 days (i.e., up to 10 applications total).1
The safety profile of ozenoxacin cream in pediatric patients 2 months and older was similar to that of adults.1
The safety and effectiveness of ozenoxacin cream in pediatric patients younger than 2 months of age have not been established.1
Clinical studies of ozenoxacin cream did not include sufficient numbers of subjects aged 65 and older to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.1
Common Adverse Effects
Adverse reactions (rosacea and seborrheic dermatitis) were reported in 1 adult patient treated with ozenoxacin cream.1
It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:
Please see product labeling for drug interaction information.
Actions and Spectrum
Mechanism Of Action
Ozenoxacin is a quinolone anti-infective. The mechanism of action involves the inhibition of bacterial DNA replication enzymes, DNA gyrase A and topoisomerase IV. Ozenoxacin has been shown to be bactericidal against S. aureus and S. pyogenes organisms.1
Ozenoxacin has been tested in combination with 17 other commonly used antimicrobial agents against S. aureus and S.pyogenes. Antagonism interactions with ozenoxacin were observed with ciprofloxacin against S. aureus.1
Ozenoxacin has been shown to be active against most isolates of the following microorganisms, both in vitro and in clinical infections.1
- Gram-positive bacteria
Staphylococcus aureus (including methicillin-resistant isolates)1
The mechanism of quinolone resistance can arise through mutations of one or more of the genes that encode DNA gyrase or topoisomerase IV. Resistant organisms will typically carry a combination of mutations within gyrA and parC subunits.1
Overall the frequency of resistant mutants selected by ozenoxacin is ≤10-10.1
Advice to Patients
Advise patients (and/or their caregivers or guardians) using ozenoxacin cream of the following information and instructions:1
Use ozenoxacin cream as directed by the healthcare practitioner. As with any topical medication, patients and caregivers should wash their hands after application if the hands are not the area for treatment.1
Ozenoxacin cream is for external use only. Do not swallow ozenoxacin cream or use it in the eyes, on the mouth or lips, inside the nose, or inside the female genital area.1
The treated area may be covered by a sterile bandage or gauze dressing.1
Use the medication for the entire time recommended by the healthcare practitioner, even though symptoms may have improved.1
Notify the healthcare practitioner if there is no improvement in symptoms within 3 days after starting use of ozenoxacin cream.1
AHFS First Release. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
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.
Medimetriks Pharmaceuticals Inc.
AHFS Drug Information. © Copyright 2018, Selected Revisions January 8, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Medimetriks Pharmaceuticals, Inc.. Xepi (ozenoxacin) TOPICAL prescribing information. 2017 Dec.