Intranasal Scopolamine for Motion Sickness

Stankovic, Aleksandra S.; Alvarenga, Donna L.; Daniels, Vernie; Simmons, Rita G.; Buckey, Jay C.; Putcha, Lakshmi

doi:10.3357/amhp.5456.2019

Cited by 6 publications

(4 citation statements)

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“…Intranasal orexin‐A delivery has been reported to be more effective than intravenous administration in terms of receptor binding in mouse brain (Hanson et al, 2004). Pharmacokinetics studies showed that intranasal scopolamine resulted in a rapid increase in plasma drug concentration for both animals and humans (Stankovic et al, 2019; Wei et al, 2016). In contrast, intranasal delivery of orexin‐A rapidly targets the brain with limited blood distribution (Dhuria et al, 2009).…”

Section: Discussionmentioning

confidence: 99%

Orexin‐A attenuated motion sickness through modulating neural activity in hypothalamus nuclei

Pan,

Xiao,

et al. 2024

British J Pharmacology

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BACKGROUND AND PURPOSEWe evaluated the hypothesis that central orexin application could counteract motion sickness (MS) responses through regulating neural activity in target brain area.EXPERIMENTAL APPROACHThe effects of intracerebroventricular (icv) administration of orexin‐A (OxA) and orexin 1 receptor (OX1R) antagonist (SB‐334867) on MS‐induced anorexia, nausea‐like behavior (conditioned gaping), hypoactivity and hypothermia were investigated in rats receiving Ferris wheel‐like rotation. OxA‐responsive brain areas were identified through Fos immunolabelling, and were verified via re‐evaluate MS responses after intra‐nucleus administration of OxA and orexin 1, 2 receptor antagonists (OX1R: SB‐334867, OX2R: TCS‐OX2‐29). Efficacy of intranasal application of OxA vs. scopolamine (SCOP) on MS symptoms in cats were also examined.KEY RESULTSOxA icv injection dose‐dependently attenuated MS‐related behavioral responses and hypothermia. Fos expression was inhibited in the dorsomedial hypothalamus ventral part (DMV) and the paraventricular nucleus (PVN), but was enhanced in the premammillary nucleus ventral part (PMV) by OxA (20 μg) in rotated animals. MS responses were differentially relieved by OxA injection into the DMV (anorexia and hypoactivity), the PVN (conditioned gaping) and the PMV (hypothermia). The behavioral and thermal effects of OxA were suppressed by SB‐334867 and TCS‐OX2‐29, respectively for both icv and intra‐nucleus injection experiment. Both OxA (60 μg/kg) and SCOP ameliorated rotation‐induced emesis and non‐retching/vomiting symptoms, while OxA also attenuated anorexia with mild salivation suppression effect in MS cats.CONCLUSION AND IMPLICATIONSOxA might relieve MS manifestations through acting on OX1R and OX2R in various hypothalamus nuclei. Intranasal OxA administration could be a potential strategy against MS.

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Section: Discussionmentioning

confidence: 99%

Orexin‐A attenuated motion sickness through modulating neural activity in hypothalamus nuclei

Pan,

Xiao,

et al. 2024

British J Pharmacology

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“…17,18 Scopolamine is a competitive antagonist of muscarinic acetylcholine receptors and has extensive clinical applications in the central nervous system, such as for curing motion sickness and depression, and for use as an anesthetic. [19][20][21][22][23] Datura extract containing scopolamine has broad-spectrum bacteriostatic effects, such as inhibiting the radial growth of fungi [Alternaria alternata (Fr.) Keissler and Curvularia lunata (Wakker) Boedijn] and bacteria (Pseudomonas marginalis, Stephylococcus aureus, and Pseudomona aeruginosa consecutive).…”

mentioning

confidence: 99%

“…The scopolamine content is high in genus Datura , up to 6980 μg g −1 , which is one of the best sources of scopolamine 17,18 . Scopolamine is a competitive antagonist of muscarinic acetylcholine receptors and has extensive clinical applications in the central nervous system, such as for curing motion sickness and depression, and for use as an anesthetic 19‐23 . Datura extract containing scopolamine has broad‐spectrum bacteriostatic effects, such as inhibiting the radial growth of fungi [ Alternaria alternata (Fr.)…”

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confidence: 99%

Anti‐oomycete ability of scopolamine against Phytophthora infestans, a terrible pathogen of potato late blight

et al. 2023

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BACKGROUNDPhytophthora infestans causes late blight, threatening potato production. The tropane alkaloid scopolamine from some industrial plants (Datura, Atropa, etc.) has a broad‐spectrum bacteriostatic effect, but its effect on P. infestans is unknown.RESULTSIn the present study, scopolamine inhibited the mycelial growth of phytopathogenic oomycete P. infestans, and the half‐maximal inhibitory concentration (IC50) was 4.25 g L−1. The sporangia germination rates were 61.43%, 16.16%, and 3.99% at concentrations of zero (control), 0.5 IC50, and IC50, respectively. The sporangia viability of P. infestans was significantly reduced after scopolamine treatment through propidium iodide and fluorescein diacetate staining, speculating that scopolamine destroyed cell membrane integrity. The detached potato tuber experiment demonstrated that scopolamine lessened the pathogenicity of P. infestans in potato tubers. Under stress conditions, scopolamine showed good inhibition of P. infestans, indicating that scopolamine could be used in multiple adverse conditions. The combination effect of scopolamine and the chemical pesticide Infinito on P. infestans was more effective than the use of scopolamine or Infinito alone. Moreover, transcriptome analysis suggested that scopolamine leaded to a downregulation of most P. infestans genes, functioning in cell growth, cell metabolism, and pathogenicity.CONCLUSIONTo our knowledge, this is the first study to detect scopolamine inhibitory activity against P. infestans. Also, our findings highlight the potential of scopolamine as an eco‐friendly option for controlling late blight in the future. © 2023 Society of Chemical Industry.

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“…This study is consequently signi cant as it will be the rst RCT to date, to exclusively examine depressive episodes in bipolar disorder to ascertain if a rapid antidepressant effect is demonstrated. Scopolamine, also known as "hyoscine" is most commonly utilised for the management of post-operative nausea, motion sickness and hypersalivation secondary to psychotropic medications such as clozapine [14][15][16]. Scopolamine acts as an inhibitor at postganglionic muscarinic cholinergic receptor sites in the parasympathetic nervous system.…”

mentioning

confidence: 99%

Efficacy and Safety of Scopolamine Compared to Placebo in Individuals with Bipolar Disorder Who are Experiencing a Depressive Episode (SCOPE-BD): Study Protocol for a Randomized Double-Blind Placebo-Controlled Trial

Miravalles

Kane

McMahon

et al. 2022

Preprint

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Background: Current treatment options for the management of depressive episodes in bipolar disorder are often sub-optimal, with some treatments either noted to be only partially effective or to require long durations of treatment prior to a therapeutic response. Therefore, pharmaco-therapeutic options that reduce depressive symptoms in a more rapid manner, might provide a viable therapeutic option for some people. Intravenous (IV) Scopolamine, a pan muscarinic antagonist has been demonstrated in a number of studies to confer a rapid antidepressant effect, albeit no study to date has exclusively evaluated its potential therapeutic effect in a cohort consisting solely of individuals with bipolar disorder.Methods: Individuals with bipolar disorder who are currently experiencing a depressive episode of at least moderate severity will be included in this study. Eligible participants will undergo a screening and placebo-run in visit, and will be randomised at visit 3 to the treatment or placebo group. Participants will receive the three blinded infusions over the course of two weeks, with two subsequent follow-up visits, one and three weeks after the last infusion visit. The total duration of the study will be approximately six weeks. Patients will continue their regular treatment regime in addition to study medication. Objective and subjective mood questionnaires, cognitive assessments and other psychometric instruments will be administered and recorded.Discussion: To our knowledge, this is the first study to investigate the antidepressant effects of IV scopolamine in an exclusively bipolar disorder cohort. Trial findings will contribute to the evidence base regarding the cholinergic hypothesis of mood disorders and specifically might result in an additional safe therapeutic option for the management of depressive episodes in bipolar disorder.Trial registration: ClinicalTrials.gov: NCT04211961EudraCT Number: 2017-003112-39

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Intranasal Scopolamine for Motion Sickness

Cited by 6 publications

References 0 publications

Orexin‐A attenuated motion sickness through modulating neural activity in hypothalamus nuclei

Orexin‐A attenuated motion sickness through modulating neural activity in hypothalamus nuclei

Anti‐oomycete ability of scopolamine against Phytophthora infestans, a terrible pathogen of potato late blight

Efficacy and Safety of Scopolamine Compared to Placebo in Individuals with Bipolar Disorder Who are Experiencing a Depressive Episode (SCOPE-BD): Study Protocol for a Randomized Double-Blind Placebo-Controlled Trial

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