An ulcerated mouth lesion following one dose of sublingual asenapine

Abstract

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 (75.8%), supralingual (55.9%), and buccal (45.7%). Case Report A 35-year-old patient diagnosed with schizophrenia and swallowing problems was on a regimen that included liquid haloperidol via oral syringe. Adherence was problematic and psychotic symptoms were poorly controlled. The patient was prescribed asenapine 5-mg sublingual tablets to be dissolved under the tongue twice daily. Following the first dose, the patient developed an extremely painful ulcerated lip lesion and refused additional doses. The Naranjo Probability Scale was applied and indicated a probable reaction (7 of 12). Conclusions In our patient, the adverse event occurred following one dose. Rechallenge was not attempted. Primary care providers may not be fully aware of the potential severity for this medication-related effect. Based on findings from the manufacturer, clinicians are encouraged to counsel patients and conduct follow-up to determine whether any adverse oral effects were experienced that might have an impact on medication adherence.