Current Trends on Antipsychotics: Focus on Asenapine.
2016
Over the years, both first- (FGAs) and second-generation antipsychotics
(SGAs), continue to gain increasing evidence of being effective in the
treatment of psychotic symptoms. Currently, they represent the first-line treatment
of schizophrenia and bipolar disorder, although they are widely used in psychotic
depression and other clinical conditions, such as agitation and/or behavioural
disturbances. Despite representing an indispensable tool for the treatment of
severe psychotic disorders, they are widely known to have a number of unwanted
side effects that the clinician must be aware of, and handle carefully to provide
the patient the best available treatment in the short and long-term. However, even
with respect to the long-term use of some of the most effective SGAs, it is
imperative for clinicians not to overlook the risk linked to the onset of potentially
severe metabolic side effects such as weight gain, dyslipidaemia, insulinresistance
and type II diabetes.
Asenapine is one of the newest SGAs licenced in Europe for the treatment of
manic episodes and in the US for schizophrenia. It belongs to the same class of
clozapine, olanzapine and quetiapine, sharing with them a rather complex
pharmacological binding profile. In fact, asenapine shows a high affinity for the
serotonin (5HT) receptor of the type 2A (5HT2A) and to a lesser extent for the
dopamine receptor of the type 2 (D2), similar to other SGAs. Asenapine behaves
also as an antagonist at the level of 5HT2C, H1 and α2-receptors. Asenapine has
been reported to be effective either in monotherapy or in combination with mood
stabilers (lithium and valproate) in the treatment of manic or mixed episodes, with
a lower propensity to induce, or being followed by, depressive symptoms, when
compared to other SGAs. These unique properties may explain the increasing
interest towards the use of this drug in mixed states, besides schizophrenia and
acute mania.
The aim of this paper was at reviewing current data on pharmacological properties
and clinical use of asenapine, as well as on possible future indication of this SGA.
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