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Mechanism of Action
Olopatadine is a mast cellstabilizer and a histamine H1 antagonist. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.
Systemic bioavailability data upon topical ocular administration of PATADAY™ (olopatadine hydrochloride ophthalmic solution) solution are not available. Following topical ocular administration of olopatadine 0.15% ophthalmic solution in man, olopatadine was shown to have a low systemic exposure. Two studies in normal volunteers (totaling 24 subjects) dosed bilaterally with olopatadine 0.15% ophthalmic solution once every 12 hours for 2 weeks demonstrated plasma concentrations to be generally below the quantitation limit of the assay ( < 0.5 ng/mL). Samples in which olopatadine was quantifiable were typically found within 2 hours of dosing and ranged from 0.5 to 1.3 ng/mL. The elimination half-life in plasma following oral dosing was 8 to 12 hours, and elimination was predominantly through renal excretion. Approximately 60 - 70% of the dose was recovered in the urine as parent drug. Two metabolites, the mono-desmethyl and the N-oxide, were detected at low concentrations in the urine.
Results from clinical studies of up to 12 weeks duration demonstrate that PATADAY™ (olopatadine hydrochloride ophthalmic solution) solution when dosed once a day is effective in the treatment of ocular itching associated with allergic conjunctivitis.
Last reviewed on RxList: 1/27/2011
This monograph has been modified to include the generic and brand name in many instances.
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