Clinical perspective on antipsychotic receptor binding affinities

Crapanzano, Calogero; Laurenzi, Pier Francesco; Amendola, Chiara; Casolaro, Ilaria

doi:10.1590/1516-4446-2021-2245

Cited by 3 publications

(1 citation statement)

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“…Olanzapine is characterized by antagonism for D2 receptors as well as for H1, 5HT-2a, 5HT2c and alpha1 receptors. The antagonism of H1, 5HT-2a, 5HT2c, alpha1 and M1 receptors could be the pharmacodynamic mechanism underlying the anti-anxiety properties of olanzapine [ 45 , 47 - 50 ] as shown in several preclinical models: i) 5HT-2a antagonist activity decreases anxiety potentially through 5-HT2A downregulation in the frontal cortex and in the hippocampus [ 51 ]; ii) Dorsal Raphe 5-HT2C antagonist activity prevents anxiety-like behavior through attenuation of increased GABAergic activity [ 52 ]; iii) H1 antagonistic activity reduces anxiety by potentially decreasing adrenergic neuron activation and modulation acetylcholine release [ 53 ]; iv) the alpha1 adrenoceptor antagonism attenuates anxiety-like behavior potentially due to reduction of excessive norepinephrine activity, in line with the noradrenergic theory of anxiety [ 54 , 55 ]; v) the M1 antagonism may ameliorate anxiety by blocking postsynaptic M1 receptors in the ventromedial prefrontal cortex, in line with the cholinergic theory of anxiety [ 56 ]. Another possible hypothesis is linked to the ability to regulate the glutamatergic system.…”

Section: Discussionmentioning

confidence: 99%

Efficacy of Olanzapine in Anxiety Dimension of Schizophrenia: A Systematic Review of Randomized Controlled Trials

Crapanzano¹,

Casolaro

Damiani

et al. 2022

Clin Psychopharmacol Neurosci

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Anxiety symptoms and anxiety disorders are frequent in patients with schizophrenia and are associated with greater severity of both positive and negative symptoms, cognitive impairment, poorer functioning and quality of life. Accumulating evidence suggests that atypical antipsychotics may have a role in treating comorbid anxiety symptoms. A systematic review was conducted following Preferred Reporting Items for Systematic reviews and Meta-Analyses (PRISMA) and Cochrane guidelines, selecting randomized control trials (RCTs) that evaluated efficacy of olanzapine on anxiety symptoms in patients diagnosed with schizophrenia and included anxiety evaluation scales. We searched PubMed and Web of Science databases for articles in English language available until September 2021. We selected 7 studies (3 with primary data analysis, 4 with secondary data analysis) regarding the use of olanzapine in patients with schizophrenia. In fours studies olanzapine was superior to haloperidol in improving anxiety symptoms. Four studies compared olanzapine versus risperidone: in two of them risperidone was superior to olanzapine, although one study was limited by a relatively small sample size. In the other two there were no significant differences between olanzapine and risperidone-treated patients. One study found that olanzapine and clozapine were comparable in terms of efficacy. Although olanzapine was superior to haloperidol in treating anxiety, this symptom was a secondary outcome measure in most of the considered studies. Future RCTs comparing different antipsychotics and larger sample sizes may allow to develop more solid treatment strategies.

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