Studies on the metabolism of haloperidol (HP): The role of CYP3A in the production of the neurotoxic pyridinium metabolite HPP+ found in rat brain following ip administration of HP
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Intranasal delivery of antipsychotic drugs
2017, Schizophrenia ResearchCitation Excerpt :High values of DTP (91%) in the IN solution group suggest that the drug from solution is also transported to a high extent directly from the nasal cavity. The reason for these high values of DTEs and DTPs in this study is the very low value of the brain concentration:blood concentration ratio obtained in IV administration group, which are far lower than previously reported (Marcucci et al., 1972; Igarashi et al., 1995; Katare et al., 2015). Therefore, these high values of DTPs and DTEs should be approached with a degree of caution.
Further evaluation of the tropane analogs of haloperidol
2014, Bioorganic and Medicinal Chemistry LettersHaloperidol-loaded intranasally administered lectin functionalized poly(ethylene glycol)-block-poly(D,L)-lactic-co-glycolic acid (PEG-PLGA) nanoparticles for the treatment of schizophrenia
2014, European Journal of Pharmaceutics and BiopharmaceuticsCitation Excerpt :The regions chosen were the striatum, which contains one of the highest D2 receptor concentrations within the brain, and the olfactory bulb, which has previously been shown to contain the highest nanoparticle concentration of drug within the olfactory bulb 1 h following intranasal administration [1,30]. Striatal concentrations of haloperidol alone following IP injection were similar to those previously reported; however, haloperidol nanoparticles given via IP injection were found to result a similar striatal haloperidol concentration to the free drug [24,38]. This result may be attributable to premature metabolism or endocytosis of circulating nanoparticles by immune/inflammatory cells occurring prior to reaching the BBB when nanoparticles were administered via the IP route.
Brain levels of the neurotoxic pyridinium metabolite HPP+ and extrapyramidal symptoms in haloperidol-treated mice
2013, NeuroToxicologyCitation Excerpt :Two strains did possess significantly higher levels of HPP+ and a higher ratio of HPP+ to haloperidol (NZO/HILtJ and PWK/PhJ), but this did not match the strain distribution of haloperidol-induced motor side effects. The HPP+ levels that we observed after chronic haloperidol treatment (10–60 ng/g of brain tissue) overlap the ranges of those detected in patient brains at post-mortem (Eyles et al., 1997) and in rat brain after acute i.p. injection of 10 mg/kg (Igarashi and Castagnoli, 1992; Igarashi et al., 1995). This is the first study to examine brain HPP+ levels in animals at high and low liability to haloperidol-induced EPS.
Modifications of Mitochondrial Function by Toxicants
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