Antigen challenge studies performed two to four hours after initial drug
instillation indicated activity was maintained for at least two and four hours.
In an environmental study, levocabastine HCl instilled four times daily was
shown to be significantly more effective than its vehicle in reducing ocular
itching associated with seasonal allergic conjunctivitis.
After instillation in the eye, levocabastine is systemically absorbed.
However, the amount of systemically absorbed levocabastine after therapeutic
ocular doses is low (mean plasma concentrations in the range of 1-2 ng/ml).
Levocabastine HCl is indicated for the temporary relief of the signs and
symptoms of seasonal allergic conjunctivitis.
This product is contraindicated in persons with known or suspected
hypersensitivity to any of its components. It should not be used` while soft
contact lenses are being worn.
For topical use only. Not for injection.
PRECAUTIONS:
Information for Patients: SHAKE WELL BEFORE USING. To prevent
contaminating the dropper tip and suspension, care should be taken not to touch
the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle
tightly closed when not in use. Do not use if the suspension has discolored.
Store at controlled room temperature. Protect from freezing.
Carcinogenesis, Mutagenesis, and Impairment of Fertility:
Levocabastine was not carcinogenic in male or female rats or in male mice when
administered in the diet for up to 24 months. In female mice, levocabastine
doses of 5,000 and 21,500 times the maximum recommended ocular human use level
resulted in an increased incidence of pituitary gland adenoma and mammary gland
adenocarcinoma possibly produced by increased prolactin levels. The clinical
relevance of this finding is unknown with regard to the interspecies differences
in prolactin physiology and the very low plasma concentrations of levocabastine
following ocular administration.
Mutagenic potential was not demonstrated for levocabastine when tested in
Ames' Salmonella Reversion test or in Escherichia coli , Drosophila
melanogaster , a mouse Dominant Lethal Assay or in rat Micronucleus test.
In reproduction studies in rats, levocabastine showed no effects on fertility
at oral doses of 20 mg/kg/day (8,300 times the maximum recommended human ocular
dose).
Teratogenic Effects: Pregnancy Category C. Levocabastine has been
shown to be teratogenic (polydactyly) in rats when given in doses 16,500 times
the maximum recommended human ocular dose. Teratogenicity (polydactyly,
hydrocephaly, brachygnathia), embryotoxicity, and maternal toxicity were
observed in rats at 66,000 times the maximum recommended ocular human dose.
There are no adequate and well-controlled studies in pregnant women.
Levocabastine should be used during pregnancy only if the potential benefit
justifies the potential risk to the fetus.
ADVERSE REACTIONS:
The most frequent complaint with the use of levocabastine HCl is that of
mild, transient stinging and burning (15%) and headache (5%).
Other adverse experiences which have been reported in approximately 1-3% of
patients treated with Livostin include visual
disturbances, dry mouth, fatigue, pharyngitis, eye pain/dryness, somnolence, red
eyes, lacrimation/discharge, cough, nausea, rash/erythema, eyelid edema, and
dyspnea.