Asenapine: A new focus on the treatment of mania

Cruz, Núria; Vieta, Eduard

doi:10.1016/S2173-5050(11)70016-4

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Abstract

Development

Asenapine, recently marketed in United States and ready to be so in Europe, is a multimodal action second-generation antipsychotic, with high affinity for multiple dopaminergic (D2, D3 y D4), serotonergic (5HT1A, 5HT2B, 5HT2C, 5HT6 y 5HT7) and adrenergic (α1A, α2A, α2B y α2C) receptors. Asenapine has to be administered sublingually. After going through succesfully the preliminary phases of development, several clinical trials have been completed in two main indications: schizophrenia and mania. This article summarizes the available evidence on its safety and efficacy in acute mania and provides some prospect on its clinical immediate and future applications.

Conclusions

Asenapine is effective and generally well tolerated in the treatment of moderate-to-severe acute mania associated to bipolar I disorder. The sublingual administration may be a challenge (coadministration with food or other drugs needs to be avoided) but also an opportunity (improved treatment adherence). Due to its multimodal receptor profile, it may cause several side-effects, but most of those are relatively mild, with none being particularly outstanding. In Europe, asenapine is indicated for the treatment of acute mania only, but several trials are being conducted in schizophrenia and bipolar depression.

Keywords:

Asenapine

Antipsychotic

Mania

Bipolar disorder

Resumen

Desarrollo

La asenapina, recientemente comercializada en Estados Unidos y presta a serlo en Europa, es un antipsicótico de segunda generación con acción multimodal, derivada de su afinidad por múltiples receptores dopaminérgicos (D2, D3 y D4), serotonérgicos (5HT2A, 5HT2B, 5HT2C, 5HT6 y 5HT7) y adrenérgicos (αa1A, α2A, α2B y α2C). Su administración se realiza por vía sublingual. Tras culminar las fases iniciales de desarrollo, se han conducido diversos ensayos clínicos en dos indicaciones principalmente: esquizofrenia y manía. Este artículo sintetiza la evidencia científica de su eficacia y seguridad en manía aguda y adelanta algunas de sus posibilidades clínicas inmediatas y futuras.

Conclusiones

La asenapina es eficaz y generalmente bien tolerada en el tratamiento de la manía aguda moderada o grave asociada al trastorno bipolar tipo I. Su administración sublingual plantea el reto de evitar su coadministración con comida u otros fármacos, pero puede suponer una ventaja para la adherencia terapéutica. Por su perfil multimodal, puede asociarse a diversos efectos adversos, pero destaca por la baja intensidad de todos ellos, sin ninguno que sobresalga por encima de los demás. En Europa está indicada solamente para la manía aguda, pero se están realizando también numerosos ensayos en esquizofrenia y en depresión bipolar.

Palabras clave:

Asenapina

Antipsicótico

Manía

Trastorno bipolar

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