Trifluoperazine versus low-potency first generation antipsychotic drugs for schizophrenia

Tardy, Magdolna; Leucht, Stefan; Potapov, Andrey; Engel, Rolf R.; Dold, Markus; Kissling, Werner

doi:10.1002/14651858.cd009396

Cited by 10 publications

(6 citation statements)

References 27 publications

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“…Trifluoperazine is a phenothiazine, and its primary application is for schizophrenia [ 58 ]. It has also been described as modifying P-type ATPase activity [ 59 ], inhibiting HIV-associated apoptosis [ 60 ], and preventing ROS damage by Fe/H2O2 [ 61 ].…”

Section: Resultsmentioning

confidence: 99%

Identification of Non-Electrophilic Nrf2 Activators from Approved Drugs

et al. 2017

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Oxidative damage can lead to a wide range of diseases. Nrf2 is an important transcription factor that regulates many of the cytoprotective enzymes involved in the oxidative stress response. Therefore, targeting the regulation of Nrf2 activation is one logical and effective strategy to prevent or lower the risk of oxidative stress-related diseases. Until now, most research has focused on electrophilic indirect Nrf2 activators, but the risk of ‘off-target’ effects may be associated with these activators. To find novel small non-electrophilic modulators of Nrf2, we started from chemical agents derived from a connectivity map (cMap) and identified 22 non-electrophilic potential Nrf2-activating drugs through a drug repositioning tactic. By determining the expression changes of antioxidant genes in MCF7 cells that were treated with the potential Nrf2 activators using quantitative real-time polymerase chain reaction RT-PCR (real-time polymerase chain reaction) (qRT-PCR), astemizole was found to have a greater scale of upregulating antioxidant genes NQO1, HO-1, and GCLM than the positive control d,l-sulforaphane, although the testing concentration was lower than that of the control. Astemizole is a good potential redox regulator and deserves more pharmacodynamic experimentation to test and verify its feasibility for use as an Nrf2 activator.

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Section: Resultsmentioning

confidence: 99%

Identification of Non-Electrophilic Nrf2 Activators from Approved Drugs

et al. 2017

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“…The structures, original clinical applications, and their identification numbers corresponding to the results in Figure 1C are exhibited in Figure 1D. While these 7 drugs have no common chemical structure, two of them (BPD and TFP) have been shown to target the same protein, calmodulin, and both of them have been clinically applied to the same disorder as antipsychotic drugs [30, 31]. Thus, we focused on these two drugs for further studies.…”

Section: Resultsmentioning

confidence: 99%

“…Here we show anticancer properties and the preclinical therapeutic effects of two representative FDA-approved small-molecule drugs, bepridil (BPD) and trifluoperazine (TFP), which have been used clinically for treatment of schizophrenia and angina, respectively [30, 31]. …”

Section: Introductionmentioning

confidence: 99%

Pharmacological activation of FOXO3 suppresses triple-negative breast cancer in vitro and in vivo

Park

Chung

et al. 2016

Oncotarget

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Triple-negative breast cancer (TNBC) is the most lethal form of breast cancer. Lacking effective therapeutic options hinders treatment of TNBC. Here, we show that bepridil (BPD) and trifluoperazine (TFP), which are FDA-approved drugs for treatment of schizophrenia and angina respectively, inhibit Akt-pS473 phosphorylation and promote FOXO3 nuclear localization and activation in TNBC cells. BPD and TFP inhibit survival and proliferation in TNBC cells and suppress the growth of TNBC tumors, whereas silencing FOXO3 reduces the BPD- and TFP-mediated suppression of survival in TNBC cells. While BPD and TFP decrease the expression of oncogenic c-Myc, KLF5, and dopamine receptor DRD2 in TNBC cells, silencing FOXO3 diminishes BPD- and TFP-mediated repression of the expression of these proteins in TNBC cells. Since c-Myc, KLF5, and DRD2 have been suggested to increase cancer stem cell-like populations in various tumors, reducing these proteins in response to BPD and TFP suggests a novel FOXO3-dependent mechanism underlying BPD- and TFP-induced apoptosis in TNBC cells.

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“…[67] The second generation of antipsychotics has shown less sedative effects in comparison to the first generation, higher costs, and often cause weight gain and other metabolic syndrome symptoms and also may be unavailable easily in some countries. [8] There are limited studies that compared the efficacy of different types of the first generation antipsychotics on sedation of the aggressive behaviors, moreover, their findings are controversial. [7910] Some studies reported the effectiveness of the promethazine, an antihistamine medication, on de-escalation of aggressive patients.…”

Section: Introductionmentioning

confidence: 99%

Comparison of Haloperidol, Promethazine, Trifluoperazine, and Chlorpromazine in Terms of Velocity and Durability of the Sedation among Acute Aggressive Patients: A Randomized Clinical Trial

2019

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Background: Knowledge and skill about sedation of aggressive patients is necessary for each psychiatrist. The purpose of this study was comparing the velocity and durability of sedation induced by the haloperidol, trifluoperazine, promethazine, and chlorpromazine in aggressive patients. Materials and Methods: This randomized clinical trial was done on 76 aggressive patients referred to Psychiatry Emergency Service of Noor Hospital of Isfahan University of Medical Sciences that were randomly divided into four groups of haloperidol, promethazine, chlorpromazine, and trifluoperazine. Patients were evaluated at 30 min intervals for aggressive symptoms, and if they did not respond to intervention after the first 30 min or if they showed aggression again, a same dose of the injected drug was prescribed. The length of sedation time was recorded for each patient. Results: Seventy-six patients with the mean age of 31.89 ± 8.73 years were participated and 63.2% of them were male. Response to intervention after the first injection was seen in 40.8% and 59.2% needed the second injection. The mean time needed for obtaining sedation was 17.38 ± 8.23 and 19.66 ± 4.64 min after the first and second injection, respectively. The mean times of sedation induction were not significantly related to age, gender, type of substance used, type of aggression, and type of psychiatric disorder. Considering the type of drugs, there was no significant difference between velocity and durability effect of sedation after the first and second injection. Conclusion: Comparing the velocity and durability of sedative effect of the four studied drugs on acute aggressive patients, did not show any significant difference between them.

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Trifluoperazine versus low-potency first generation antipsychotic drugs for schizophrenia

Cited by 10 publications

References 27 publications

Identification of Non-Electrophilic Nrf2 Activators from Approved Drugs

Identification of Non-Electrophilic Nrf2 Activators from Approved Drugs

Pharmacological activation of FOXO3 suppresses triple-negative breast cancer in vitro and in vivo

Comparison of Haloperidol, Promethazine, Trifluoperazine, and Chlorpromazine in Terms of Velocity and Durability of the Sedation among Acute Aggressive Patients: A Randomized Clinical Trial

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