An ulcerated mouth lesion following one dose of sublingual asenapine

Abstract Purpose: To report the first descriptive case of a mouth lesion following one dose of sublingually administered asenapine. Summary: Asenapine is a second-generation antipsychotic, approved in the United States in August 2009, for the treatment of schizophrenia and acute mania associated with bipolar disorder. It is administered as a sublingual tablet to be taken twice daily. Although the mechanism of action has not been fully elucidated, it is thought to be mediated through a combination of antagonist activity at the dopamine and serotonin 5-HT2A receptors. Sublingual bioavailability is estimated at 35% and is highly plasma protein bound (95%). Oral administration results in low bioavailability (< 2%) due to extensive first-pass metabolism. Adverse tissue reactions identified by the manufacturer include mouth ulcers, blisters, and peeling/sloughing of the contact area. In one manufacturer-sponsored trial, oral paresthesia events were reported for the following administration routes: sublingual (7...