Ophthalmic Antihistamine
PREGNANCY RECOMMENDATION: No Human Data—Probably Compatible
BREASTFEEDING RECOMMENDATION: No Human Data—Probably Compatible
PREGNANCY SUMMARY
No reports describing the use of alcaftadine in human pregnancy have been located. The animal data suggest low risk. Moreover, antihistamines, in general, are considered compatible with pregnancy.
FETAL RISK SUMMARY
Alcaftadine is an antihistamine indicated for the prevention of itching associated with allergic conjunctivitis. It is available as a 0.25% ophthalmic solution. Minimal amounts are measured in the plasma and concentrations of alcaftadine were below the level of detection (10 pg/mL) at 3 hours. The drug is metabolized to an active carboxylic acid metabolite that was undetectable in the plasma 12 hours after a dose. Plasma protein binding for the parent drug and active metabolite were about 39% and 63%, respectively. The elimination half-life of the active metabolite was about 2 hours (1).
Reproduction studies have been conducted in rats and rabbits. No evidence of impaired female reproduction or fetal harm was observed in these species at oral doses that produced plasma exposures that were about 200 and 9000 times, respectively, the human plasma exposure at the recommended human ocular dose (RHOD) (1).
No evidence of mutagenic or genotoxic effects was observed in multiple assays. There also was no evidence of fertility impairment in male and female rats at oral doses producing plasma exposures that were about 200 times the human plasma exposure at the RHOD (1).
It is not known if alcaftadine or its active metabolite crosses the human placenta. The molecular weight of the parent drug (about 307) and moderate protein binding imply that exposure of the embryo and/or fetus is possible, but the minimal amounts in the plasma suggest that any exposure would be clinically insignificant.
BREASTFEEDING SUMMARY
No reports describing the use of alcaftadine during human lactation have been located. The molecular weight of the parent drug (about 307) and moderate protein binding imply that the drug and possibly the active carboxylic acid metabolite will be excreted into breast milk. However, the minimal plasma concentrations that occur after ocular use suggest that the risk to a nursing infant will be nil. Moreover, antihistamines, in general, are considered compatible with breastfeeding.
Reference
1.Product information. Lastacaft. Allergan, 2010.