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European Journal of Paediatric... Sep 2020Susceptibility to severe motion sickness has not been well described in the pediatric population, particularly in very young children. This study aimed to describe and...
INTRODUCTION
Susceptibility to severe motion sickness has not been well described in the pediatric population, particularly in very young children. This study aimed to describe and evaluate risk factors and treatment responses in a group of children with severe motion sickness, including infants and toddlers.
METHODS
We conducted a retrospective review of patients less than 18 years of age seen in our pediatric vestibular program for evaluation of motion sickness over a 6-year period.
RESULTS
A total of 23 patients with motion sickness were identified. Age of onset ranged from 0 to 15 years old, with a mean age of 6.6 ± 4.2 years. Eleven patients (47.8%) were diagnosed with a migraine variant. Vestibular deficits were identified in four out of 17 patients (23.5%) who underwent formal vestibular testing. Other frequent comorbid conditions included recurrent/chronic otitis media (n = 9; 39.1%) and a history of motor delay (n = 7; 30.4%). A high proportion of patients reported symptom improvement when treated with meclizine, ondansetron, cyproheptadine, or vestibular rehabilitation.
DISCUSSION
Motion sickness can impact children even in infancy. Common comorbid conditions that may contribute to pediatric motion sickness include migraine disorders, vestibular impairment, otitis media, and motor delay. Treatments such as cyproheptadine and vestibular rehabilitation may be helpful but require further study.
Topics: Adolescent; Child; Child, Preschool; Comorbidity; Female; Humans; Infant; Infant, Newborn; Male; Migraine Disorders; Motion Sickness; Otitis Media; Retrospective Studies; Risk Factors; Vestibular Diseases
PubMed: 32682672
DOI: 10.1016/j.ejpn.2020.06.010 -
EBioMedicine Sep 2015
Topics: Acute Kidney Injury; Animals; Kidney; Male; Meclizine; Mice; Reperfusion Injury
PubMed: 26501091
DOI: 10.1016/j.ebiom.2015.09.016 -
Otology & Neurotology : Official... Mar 2023To examine the risk factors for hip fracture in patients with vestibular disorders and the association between antihistamine use and hip fracture in patients with...
OBJECTIVES
To examine the risk factors for hip fracture in patients with vestibular disorders and the association between antihistamine use and hip fracture in patients with vestibular disorders.
STUDY DESIGN
Retrospective case series with chart review.
SETTING
Tertiary academic medical center.
METHODS
A retrospective review of adult patients with hip fracture based on International Classification of Diseases, Tenth Revision (ICD-10) code S72 from January 2013 to December 2019 who had previously been diagnosed with a vestibular disorder based on ICD-10 codes H81-83, A88.1, and R42.
RESULTS
A total of 201 patients were identified meeting the inclusion criteria. The average age at the time of hip fracture was 78.8 years and the majority were female (64.7%). Most patients were diagnosed with nonspecific dizziness (60.2%) or vertigo (23.9%). Those with a peripheral vestibular disorder included benign paroxysmal positional vertigo (BPPV) in 13.4% and Ménière's disease in 2.5%. Overall, meclizine was prescribed to 38.3% of patients, including 29.9% of patients before hip fracture. Meclizine was prescribed to 66.7% of patients with BPPV. Patients were seen for vestibular symptoms 0.67 ± 2.51 years before hip fracture, and 98 patients (48.8%) presented with vestibular concerns within 1 year prior.
CONCLUSION
Patients with vestibular disorders who sustain a ground level fall resulting in hip fracture are a vulnerable population of predominantly older adults with multiple comorbidities. Patients were frequently diagnosed with dizziness or vertigo rather than more specific causes being identified. Multifactorial interventions to prevent hip fractures in older adults have been recommended; however, this study suggests that meclizine use was common among patients diagnosed with dizziness, vertigo, or BPPV before hip fracture.
Topics: Humans; Female; Male; Aged; Dizziness; Meclizine; Retrospective Studies; Vestibular Diseases; Benign Paroxysmal Positional Vertigo; Hip Fractures
PubMed: 36728629
DOI: 10.1097/MAO.0000000000003792 -
Journal of AOAC International Mar 2022Noising is an undesirable phenomenon accompanying the development of widely used chemometric models such as partial least square regression (PLSR) and support vector...
BACKGROUND
Noising is an undesirable phenomenon accompanying the development of widely used chemometric models such as partial least square regression (PLSR) and support vector regression (SVR).
OBJECTIVE
Optimizations of these chemometric models by applying orthogonal projection to latent structures (OPLS) as a preprocessing step which is characterized by canceling noise is the purpose of this research study. Additionally, a comprehensive comparative study between the developed methods was undertaken highlighting pros and cons.
METHODS
OPLS was conducted with PLSR and SVR for quantitative determination of pyridoxine HCl, cyclizine HCl, and meclizine HCl in the presence of their related impurities. The training set was formed from 25 mixtures as there were five mixtures for each compound at each concentration level. Additionally, to check the validity and predictive ability of the developed chemometric models, independent test set mixtures were prepared by repeating the preparation of four mixtures of the training set plus preparation of another four independent mixtures.
RESULTS
Upon application of the OPLS processing method, an upswing of the predictive abilities of PLSR and SVR was found. The root-mean-square error of prediction of the test set was the basic benchmark for comparison.
CONCLUSION
The major finding from the conducted research is that processing with OPLS reinforces the ability of models to anticipate the future samples.
HIGHLIGHTS
Novel optimizations of the widely used chemometric models; application of a comparative study between the suggested methods; application of OPLS preprocessing methods; quantitative determination of pyridoxine HCl, cyclizine HCl and meclizine HCl; checking the predictive power of developed chemometric models; analysis of active ingredients in their pharmaceutical dosage forms.
Topics: Chemometrics; Cyclizine; Least-Squares Analysis; Meclizine; Pyridoxine
PubMed: 34672335
DOI: 10.1093/jaoacint/qsab141 -
Biochemical and Biophysical Research... Feb 2022We screened pre-approved drugs for the survival of the Hu5/KD3 human myogenic progenitors. We found that meclozine, an anti-histamine drug that has long been used for...
We screened pre-approved drugs for the survival of the Hu5/KD3 human myogenic progenitors. We found that meclozine, an anti-histamine drug that has long been used for motion sickness, promoted the proliferation and survival of Hu5/KD3 cells. Meclozine increased expression of MyoD, but reduced expression of myosin heavy chain and suppressed myotube formation. Withdrawal of meclozine, however, resumed the ability of Hu5/KD3 cells to differentiate into myotubes. We examined the effects of meclozine on mdx mouse carrying a nonsense mutation in the dystrophin gene and modeling for Duchenne muscular dystrophy. Intragastric administration of meclozine in mdx mouse increased the body weight, the muscle mass in the lower limbs, the cross-sectional area of the paravertebral muscle, and improved exercise performances. Previous reports show that inhibition of phosphorylation of ERK1/2 improves muscle functions in mouse models for Emery-Dreifuss muscular dystrophy and cancer cachexia, as well as in mdx mice. We and others previously showed that meclozine blocks the phosphorylation of ERK1/2 in cultured cells. We currently showed that meclozine decreased phosphorylation of ERK1/2 in muscles in mdx mice but not in wild-type mice. This was likely to be one of the underlying mechanisms of the effects of meclozine on mdx mice.
Topics: Animals; Cell Differentiation; Cell Proliferation; Cell Survival; Extracellular Signal-Regulated MAP Kinases; Humans; Male; Meclizine; Mice, Inbred C57BL; Mice, Inbred mdx; Motor Activity; Muscle Development; Muscle Strength; Muscle, Skeletal; Muscular Dystrophy, Duchenne; Phosphorylation; Mice
PubMed: 35033871
DOI: 10.1016/j.bbrc.2022.01.003 -
In Silico Pharmacology 2023Cardiovascular diseases are the primary factor for increased mortality rates around the world. Atherosclerosis brought on by high serum cholesterol can result in...
Cardiovascular diseases are the primary factor for increased mortality rates around the world. Atherosclerosis brought on by high serum cholesterol can result in coronary heart disease (CHD). The risk of CHD is markedly reduced by lowering serum cholesterol levels. Scientists across the world are inventing new treatment regimens for lowering blood lipid levels. In this work, we repurposed the already established drugs, i.e., cyclizine derivatives as antihyperlipidemic agents. The repurposing was done based on the similarity of the selected cyclizine derivatives with the already established antihyperlipidemic drug, fenofibrate. Computational studies were performed and the 16 cyclizine derivatives docked against PPAR. alpha scored higher than fenofibrate. Lifarizine and medibazine outperform fenofibrate inmmgbsa. Fenofibrate, etodroxizine, meclizine, and cinnarizine had similar mmgbsa scores. The ADME properties of these compounds were performed and from that etodroxizine and levocetirizine were found to have better properties. The computational studies were performed using the Schrodinger software, maestro 12.8. The "Protein Preparation Wizard" module in the Maestro panel was used to create the protein structure and OPLS4 force field was used for energy minimization. The maestro builder panel's "Ligprep", "Receptor Grid Generation" and "Ligand Docking" modules were then used to prepare ligands, receptor grids and to perform docking respectively. MMGBSA was performed on the "prime MMGBSA" segment. Using the "Qikprop" setting in the maestro panel, a number of ADMET properties were predicted, and the program was run in default mode using vsgb as the solvation model.
PubMed: 37899967
DOI: 10.1007/s40203-023-00164-2 -
Lipids in Health and Disease Apr 2017Antiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination... (Comparative Study)
Comparative Study
BACKGROUND
Antiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated.
METHODS
Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol), Glyceryl palmitostearate (Precirol), Glyceryl behenate (Compritol) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5-1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found.
RESULTS
Sphericity indicated by shape factor (e) varied with type and concentration of lipids: Geleol (e = 0.891-0.997), Precirol (e = 0.611-0.743), Compritol (e = 0.665-0.729) and Carnauba wax (e = 0.499-0.551). Highly spherical pellets were obtained with Geleol (Aspect ratio = 1.005-1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153-1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol and Compritol, (ii) Geleol and Carnauba wax and (iii) Geleol, Compritol and Carnauba wax. Scanning electron microscopy of Compritol pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol and Compritol pellets, explained by Korsmeyer-Peppas (R = 0.978-0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol and Carnauba wax and (iii) Geleol, Compritol and Carnauba wax pellets followed Zero-order (R = 0.991-0.995). Similarity test was performed using combination of Geleol and Compritol (i) as a reference.
CONCLUSIONS
Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol, Compritol and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.
Topics: Administration, Oral; Antiemetics; Delayed-Action Preparations; Diglycerides; Drug Compounding; Drug Liberation; Drug Stability; Drug Storage; Fatty Acids; Glycerides; Humans; Hydrogen-Ion Concentration; Lipids; Meclizine; Microscopy, Electron, Scanning; Pharmaceutical Vehicles; Solubility; Spectroscopy, Fourier Transform Infrared; Water; Waxes
PubMed: 28403892
DOI: 10.1186/s12944-017-0466-x -
The Journal of Neuroscience : the... Apr 2024
Erratum: Shannonhouse et al., "Meclizine and Metabotropic Glutamate Receptor Agonists Attenuate Severe Pain and Ca Activity of Primary Sensory Neurons in Chemotherapy-Induced Peripheral Neuropathy".
PubMed: 38594070
DOI: 10.1523/JNEUROSCI.0541-24.2024 -
Stem Cell Reports Mar 2022Patients with coronavirus disease 2019 (COVID-19) commonly have manifestations of heart disease. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) genome...
Patients with coronavirus disease 2019 (COVID-19) commonly have manifestations of heart disease. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) genome encodes 27 proteins. Currently, SARS-CoV-2 gene-induced abnormalities of human heart muscle cells remain elusive. Here, we comprehensively characterized the detrimental effects of a SARS-CoV-2 gene, Orf9c, on human pluripotent stem cell-derived cardiomyocytes (hPSC-CMs) by preforming multi-omic analyses. Transcriptomic analyses of hPSC-CMs infected by SARS-CoV-2 with Orf9c overexpression (Orf9c) identified concordantly up-regulated genes enriched into stress-related apoptosis and inflammation signaling pathways, and down-regulated CM functional genes. Proteomic analysis revealed enhanced expressions of apoptotic factors, whereas reduced protein factors for ATP synthesis by Orf9c. Orf9c significantly reduced cellular ATP level, induced apoptosis, and caused electrical dysfunctions of hPSC-CMs. Finally, drugs approved by the U.S. Food and Drug Administration, namely, ivermectin and meclizine, restored ATP levels and ameliorated CM death and functional abnormalities of Orf9c hPSC-CMs. Overall, we defined the molecular mechanisms underlying the detrimental impacts of Orf9c on hPSC-CMs and explored potentially therapeutic approaches to ameliorate Orf9c-induced cardiac injury and abnormalities.
Topics: Action Potentials; Adenosine Triphosphate; Apoptosis; COVID-19; Coronavirus Nucleocapsid Proteins; Down-Regulation; Genome-Wide Association Study; Humans; Ivermectin; Meclizine; Myocytes, Cardiac; Phosphoproteins; Pluripotent Stem Cells; Protein Interaction Maps; RNA, Messenger; SARS-CoV-2; Signal Transduction; Transcriptome; Up-Regulation
PubMed: 35180394
DOI: 10.1016/j.stemcr.2022.01.014 -
The Medical Letter on Drugs and... Oct 2019
Review
Topics: Acetazolamide; Altitude Sickness; Antiemetics; Carbonic Anhydrase Inhibitors; Central Nervous System Stimulants; Dexamethasone; Humans; Jet Lag Syndrome; Modafinil; Motion Sickness
PubMed: 31599874
DOI: No ID Found