Asenapine. A new atypical antipsychotic for the treatment of moderate up to severe manic episodes of bipolar-I-disorder in adults

作者：Volz Hans Peter^*

来源：Psychopharmakotherapie, 2011, 18(5): 212-219.

• Asenapine
• atypical antipsychotics
• bipolar disorder I
• acute mania

Asenapine is a new atypical antipsychotic for the treatment of acute manic episodes of bipolar I disorder in adults. In clinical trials of monotherapy with asenapine the efficacy was significantly higher than that of placebo and combined with a good safety and tolerability profile. Improvements of total scores of the Young Mania Rating Scale (YMRS) seen after 12 weeks were sustained up to 52 weeks.
Adjunctive asenapine was also significantly more effective than placebo in improving YMRS total scores. The clinical trials with asenapine showed a favourable profile of side effects: the risk for extrapyramidal symptoms (EPS) is comparatively low, as is the potential to cause metabolic abnormalities and the risk of increased body weight; the risk for prolactin elevation is very low. Asenapine has a unique profile of receptor affinities and activities. It is an antagonist with strong affinity for a number of serotonergic (5-HT(2A), 5-HT(2B), 5-HT(2C,) 5-HT(6) und 5-HT(7)), adrenergic (alpha(2)) and dopaminergic (e.g. D(3) und D(4)) receptors, but has no affinity for muscarinergic receptors.
In addition the affinity of asenapine for the 5-HT(2A) receptor is 19-fold that of its affinity for the D(2) receptor, which is regarded as predictor of a low EPS risk. With these properties asenapine is a useful alternative in the treatment of bipolar mania. It has a fast onset of action: first effects are visible on the second day of treatment. Asenapine may be of particular use for patients at risk of metabolic abnormalities.

• 出版日期2011-10