Ophthalmic (Anti-infective)
PREGNANCY RECOMMENDATION: No Human Data—Animal Data Suggest Low Risk
BREASTFEEDING RECOMMENDATION: No Human Data—Probably Compatible
PREGNANCY SUMMARY
No reports describing the use of besifloxacin in human pregnancy have been located. The animal data suggest low risk. Because the systemic bioavailability of the antibiotic is very low, the risk to the embryo or fetus also appears to be low.
FETAL RISK SUMMARY
Besifloxacin ophthalmic suspension is a quinolone antimicrobial that is indicated for the treatment of bacterial conjunctivitis caused by susceptible bacteria. Besifloxacin is in the same subclass of ophthalmic antibiotics as ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, norfloxacin, and ofloxacin. Systemic absorption is minimal. Maximum plasma concentrations after bilateral dosing 3 times daily for 16 doses were <1.3 ng/mL (mean 0.43 ng/mL). The average elimination half-life in plasma was about 7 hours (1).
Reproduction studies using oral besifloxacin have been conducted in rats. No skeletal or visceral malformations were observed in fetuses with doses producing maternal plasma concentrations that were >45,000 times the mean plasma concentrations measured in humans (PCH). Increased postimplantation loss, decreased fetal weights, and decreased fetal ossification were noted, but these doses also produced maternal toxicity (reduced body weight gain and food consumption) and mortality. The no-observed-effect level (NOEL) was >11,000 times the PCH. The NOEL also was the same in a prenatal and postnatal development study in rats (1).
Long-term studies in animals for carcinogenicity have not been conducted. The drug was not mutagenic in one test but, similar to other quinolones, was mutagenic in another test. The drug also induced chromosomal aberrations. No impairment of fertility in male and female rats was observed with oral doses that were >10,000 times the daily human ophthalmic dose (1).
It is not known if besifloxacin crosses the human placenta. The molecular weight (about 394 for the free base) and long plasma elimination half-life suggest that the drug will cross to the embryo–fetus. However, the minimal plasma concentrations suggest that the exposure will not be clinically significant.
BREASTFEEDING SUMMARY
No reports describing the use of besifloxacin during human lactation have been located. The molecular weight (about 394 for the free base) and long plasma elimination half-life (7 hours) suggest the drug will be excreted into breast milk. However, the maximum plasma concentrations (<1.3 ng/mL) suggest that exposure of a nursing infant will be clinically insignificant.
Reference
1.Product information. Besivance. Bausch & Lomb, 2009.