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Special Problems with Biological Fluids
Published in Joseph Chamberlain, The Analysis of Drugs in Biological Fluids, 2018
Irradiation using X-rays is used routinely in the food industry and in the medical industry to sterilize surgical instruments and de Bree and van Berkel have suggested this approach be used for deactivation of HIV in biological samples.240 It was shown that even relatively high doses of irradiation (up to 10 Mrads), which completely inactivated HIV had no effect on a number of drugs of diverse structure (i.e., fluvoxamine, clovoxamine, flesinoxan, idaverine, N-desmethylidaverine, and eltoprazine) in serum samples. It was concluded that such treatment could be used routinely on biological samples to make them harmless as far as the risk of HIV infection was concerned, provided it was shown that the analyte in question was unaffected by the irradiation.
Recent developments in geriatric psychopharmacology
Published in Expert Review of Clinical Pharmacology, 2021
Awais Aftab, Jeffrey A. Lam, Fred Liu, Anjan Ghosh, Martha Sajatovic
Eltoprazine is being developed as a medication to target aggression in Alzheimer’s disease. It is a 5-HT1A/5HT1B partial agonist and 5-HT2C full agonist activity that likely leads to decreased aggression by reducing serotonin release through the activation of pre-synaptic 5-HT1A and 5-HT1B auto-receptors [36–39]. Amarantus BioScience Holdings, Inc. announced that its phase 2 double-blind, randomized, placebo-controlled study conducted in elderly patients with Alzheimer’s disease and aggressive behavior showed that eltoprazine was reasonably well tolerated and showed significant improvement in aggression. Although some of the findings from the trial were reported in a press release in 2015 [40], these results have not been published in a peer reviewed journal as yet and no phase 3 trials are ongoing at the time of this writing, which suggests the need for caution with regards to the therapeutic potential of eltoprazine.
Emerging drugs for the treatment of L-DOPA-induced dyskinesia: an update
Published in Expert Opinion on Emerging Drugs, 2020
Sohaila AlShimemeri, Susan H Fox, Naomi P Visanji
Eltoprazine is a 5-HT1A/B receptor agonist licensed for anxiety. A phase I/IIa, dose-finding, DBRCT, was conducted using a single dose of eltoprazine (2.5 mg, 5 mg, or, 7.5 mg vs placebo) in combination with suprathreshold dose of L-Dopa (L-DOPA challenge), in 22 PD patients with LID. Significant reduction in LIDs based on Clinical Dyskinesia Rating Scale (CDRS) and Rush Dyskinesia Rating Scale (RDRS) scores was reported with 5 mg dose (15% for 5 mg dose vs 9% in 7.5 mg and 6% in 2.5 mg), with maximum reduction seen 3 h post dose. No change in UPDRS III score was seen. Mild but not serious adverse events occurred, with fatigue, nausea, and dizziness being the most frequent [131]. A phase II, multicenter, DBRCT in 60 PD patients with LID with dose escalation over 3 weeks is underway, but the status of which has not been recently updated (NCT02439125) [132].
Dyskinesia and Parkinson’s disease: animal model, drug targets, and agents in preclinical testing
Published in Expert Opinion on Therapeutic Targets, 2022
Valentina Cesaroni, Fabio Blandini, Silvia Cerri
Ghiglieri et al. (2016) [38] have demonstrated that anti-dyskinetic effect induced by eltoprazine activation of 5-HT1A/1B receptors is elicited through the regulation of striatal synaptic plasticity (LTP and depotentiation), the normalization of D1-related cAMP/PKA, ERK/mTOR signalling pathways and the rebalance of NMDA receptor subunits at the post-synaptic membrane. In addition to these mechanisms, recent findings suggest that eltoprazine treatment reduces theta activity in the dorsal striatum and substantia nigra pars reticulata as well as normalizes the flow of information between these brain structures [76].