PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is for topical use only and not for injection or oral use.
Carcinogenesis, Mutagenesis, Impairment of Fertility: Olopatadine administered
orally was not carcinogenic in mice and rats in doses up to 500 mg/kg/day and
200 mg/kg/day, respectively. Based on a 40 ÂµL drop size, these doses were 78,125
and 31,250 times higher than the maximum recommended ocular human dose (MROHD).
No mutagenic potential was observed when olopatadine was tested in an in
vitro bacterial reverse mutation (Ames) test, an in vitro mammalian
chromosome aberration assay or an in vivo mouse micronucleus test. Olopatadine
administered to male and female rats at oral doses of 62,500 times MROHD level
resulted in a slight decrease in the fertility index and reduced implantation
rate; no effects on reproductive function were observed at doses of 7,800 times
the maximum recommended ocular human use level.
Pregnancy: Pregnancy Category C. Olopatadine was found not to be teratogenic
in rats and rabbits. However, rats treated at 600 mg/kg/day, or 93,750 times
the MROHD and rabbits treated at 400 mg/kg/day, or 62,500 times the MROHD, during
organogenesis showed a decrease in live fetuses. There are, however, no adequate
and well controlled studies in pregnant women. Because animal studies are not
always predictive of human responses, this drug should be used in pregnant women
only if the potential benefit to the mother justifies the potential risk to
the embryo or fetus.
Nursing Mothers: Olopatadine has been identified in the milk of nursing
rats following oral administration. It is not known whether topical ocular administration
could result in sufficient systemic absorption to produce detectable quantities
in the human breast milk. Nevertheless, caution should be exercised when PATANOL
(olopatadine hydrochloride ophthalmic solution) 0.1% is administered to a nursing
Pediatric Use: Safety and effectiveness in pediatric patients below
the age of 3 years have not been established.
Geriatric Use: No overall differences in safety or effectiveness have
been observed between elderly and younger patients.