Flupentixol
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Flupentixol is a thioxanthene neuroleptic used to treat schizophrenia and depression.
Flupentixol is a thioxanthene neuroleptic used to treat schizophrenia and depression.
The mechanism of action of flupentixol is not completely understood. The antipsychotic actions are mainly thought to arise from cis(Z)-flupentixol, the active stereoisomer, acting as an antagonist at both dopamine D and D receptors with equal affinities. Schizophrenia is a mental illness characterized by positive (such as hallucinations and delusions) and negative (such as affect flattening and apathy) symptoms. While several neurotransmitter systems are implicated in the pathophysiologic processes leading to the development of symptoms, the dopamine and glutamate systems have been extensively studied. It is generally understood that positive symptoms of schizophrenia arise from a dysregulated striatal dopamine pathway, leading to hyperstimulation of D receptors. Many antipsychotic agents work by blocking D receptors as antagonists; similarly, cis(Z)-flupentixol, the active stereoisomer, is an antagonist at D receptors. However, there is now evidence that antipsychotic agents can work by blocking other dopamine receptor subtypes, such as D, D, or D receptors. One study showed that cis(Z)-flupentixol is an antagonist at both dopamine D and D receptors with equal affinities, and binds to D3 and D4 receptors with lower affinities. It also binds to alpha-1 adrenoceptors. Antidepressant effects of flupentixol are understood to be mediated by antagonism at 5-HT receptors, which are commonly downregulated following repeated antidepressant treatment. Flupentixol also binds to 5-HT receptors.
Flupentixol is indicated for maintenance therapy of chronic schizophrenic patients whose main manifestations do not include excitement, agitation or hyperactivity. It is indicated for the management of depression in adult patients who may, or may not, also be showing signs of anxiety. Flupentixol in combination with melitracen is indicated to manage symptoms of anxiety, depression, and asthenia in adults.
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