Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.979
Filtrar
1.
Environ Sci Technol ; 58(12): 5512-5523, 2024 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-38478581

RESUMO

The investigation of pharmaceuticals as emerging contaminants in marine biota has been insufficient. In this study, we examined the presence of 51 pharmaceuticals in edible oysters along the coasts of the East and South China Seas. Only nine pharmaceuticals were detected. The mean concentrations of all measured pharmaceuticals in oysters per site ranged from 0.804 to 15.1 ng g-1 of dry weight, with antihistamines being the most common. Brompheniramine and promethazine were identified in biota samples for the first time. Although no significant health risks to humans were identified through consumption of oysters, 100-1000 times higher health risks were observed for wildlife like water birds, seasnails, and starfishes. Specifically, sea snails that primarily feed on oysters were found to be at risk of exposure to ciprofloxacin, brompheniramine, and promethazine. These high risks could be attributed to the monotonous diet habits and relatively limited food sources of these organisms. Furthermore, taking chirality into consideration, chlorpheniramine in the oysters was enriched by the S-enantiomer, with a relative potency 1.1-1.3 times higher when chlorpheniramine was considered as a racemate. Overall, this study highlights the prevalence of antihistamines in seafood and underscores the importance of studying enantioselectivities of pharmaceuticals in health risk assessments.


Assuntos
Monitoramento Ambiental , Ostreidae , Preparações Farmacêuticas , Poluentes Químicos da Água , Animais , Humanos , Bromofeniramina/análise , China , Clorfeniramina/análise , Antagonistas dos Receptores Histamínicos/análise , Oceanos e Mares , Ostreidae/química , Preparações Farmacêuticas/análise , Prometazina/análise , Poluentes Químicos da Água/análise
2.
BMC Oral Health ; 23(1): 892, 2023 11 20.
Artigo em Inglês | MEDLINE | ID: mdl-37985984

RESUMO

BACKGROUND: The study objective was to examine the effect of arginine-sodium fluoride (Arg-NaF) varnish on preventing enamel erosion by acidic paediatric liquid medicaments (PLM). METHODS: The treatment groups were: 1) 2% Arg-NaF; 2) 4% Arg-NaF; 3) 8% Arg-NaF; 4) NaF; 5) MI (CPP-ACFP) varnishes; and 6) no varnish. The pH of PLM (paracetamol and chlorpheniramine) was measured at baseline and after immersing the Perspex® blocks coated with varnishes at 0 min, 30 min, 1 h, and 4 h. Seventy-two enamel specimens (n = 72) were randomly divided into 2 groups by PLM and further by treatment groups. Then, the specimens were pre-treated with varnishes and subjected to erosive cycles (5 min, 2×/day for 4 days) by PLM. After each erosive challenge, the specimens were stored in artificial saliva. At baseline and after 4 days, the specimens were assessed for surface roughness (Ra) using 2D-surface profilometric analysis (SPA) and atomic force microscopy (AFM). Additionally, the Ca/P ratio was determined using scanning electron microscopy with energy-dispersive X-ray spectroscopy. Paired samples dependent t-test, 1-way ANOVA and 2-way ANOVA with Bonferroni post-hoc tests were used to analyse data with the level of significance set at p < 0.05. RESULTS: The pH of PLM with 8% Arg-NaF was significantly higher than the other groups at 30 min and 4 h (p < 0.05). With paracetamol, no significant difference was observed between the baseline and post-erosive cycle measured enamel Ra (by SPA/AFM) and Ca/P ratio for all treatment groups (p > 0.05). The Ra determined by AFM, at the post-erosive cycle with chlorpheniramine, when treated with 4 and 8% Arg-NaF was significantly lower than the other groups (p < 0.05); except CPP-ACFP (p > 0.05). With the chlorpheniramine post-erosive cycle, the Ca/P ratio for 4, 8% Arg-NaF and CPP-ACFP treated specimens was significantly higher than the baseline Ca/P (p < 0.05). CONCLUSION: The 4%/8% Arg-NaF and MI varnish® application exhibit an enhanced preventive effect against low pH (pH < 3.0) PLM-mediated enamel erosive challenges compared to 5% NaF varnish.


Assuntos
Doenças Dentárias , Erosão Dentária , Criança , Humanos , Acetaminofen/farmacologia , Clorfeniramina/farmacologia , Esmalte Dentário , Fluoretos/farmacologia , Fluoretos Tópicos/uso terapêutico , Fluoretos Tópicos/farmacologia , Fluoreto de Sódio/uso terapêutico , Fluoreto de Sódio/química , Erosão Dentária/prevenção & controle
3.
Environ Sci Pollut Res Int ; 30(53): 113382-113393, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37848799

RESUMO

Chlorphenamine (CPA) adsorption onto three activated carbons (ACs), namely, Megapol M (MM), Micro 10 (M10), and GAMA B (GB), was studied in this work. The textural properties, concentrations of active sites, surface charge and point of zero charge of the ACs were assessed. The surface areas (SBET) of MM, GB and M10 were 1107, 812 and 766 m2/g, respectively. The MM surface had an acidic character, while the surfaces of M10 and GB were basic. The adsorption capacity of MM, M10, and GB towards CPA was studied at pH 7 and 11, and the adsorption capacity decreased in the order MM > M10 ≈ GB, which was ascribed to the magnitude of SBET and the concentration of acidic sites. The solution pH significantly increased the adsorption capacity of MM towards CPA by raising the solution pH from 5 to 9, and this behavior was attributed to the electrostatic attraction between the negatively charged surface of MM and the cationic species of CPA. The maximum uptake of CPA adsorbed on MM was 574.6 mg/g at pH = 11 and T = 25 °C. The adsorption capacity of MM was slightly raised by incrementing the temperature. Lastly, the zeta potential measurements of pristine MM and MM saturated with CPA confirmed that the electrostatic attraction predominated in the pH range of 5-9, and the π-π stacking interactions were the principal mechanism of CPA adsorption on MM at pH 11.


Assuntos
Carvão Vegetal , Clorfeniramina , Carvão Vegetal/química , Adsorção , Concentração de Íons de Hidrogênio , Temperatura , Propriedades de Superfície
4.
Environ Res ; 238(Pt 2): 117196, 2023 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-37778603

RESUMO

Chlorpheniramine (CPM) and Ciprofloxacin (CIP) adsorption onto a granular (GAC) and pelletized activated carbon (PAC) analyzing the physicochemical mechanisms involved using the carbon's characterization were studied. Adsorption isotherm studies were performed at temperatures of 25 °C at pH values of 4, 7 and 9 and at 45 °C at a pH of 7. The characterization demonstrated that GAC has a predominantly acid character due to its predominantly negative surface charge and acidic site concentration alongside the characteristic bands detected in the X-ray Photoemission Spectroscopy (XPS) study. On the other hand, PAC presented a mostly basic character due to its positive surface charge and basic site concentrations. The adsorption isotherm studies demonstrated that the Freundlich isotherm better described the equilibrium data with an average deviation percentage of 7.45 and 6.74 for GAC and PAC. The temperature and desorption studies demonstrated that the adsorption process occurs through a chemisorption mechanism, and the pH study alongside the GAC and PAC characterization demonstrated that the mechanisms involved are a combination of electrostatic interactions and pi-pi interactions between the CPM and CIP molecules and the carbon's surface. These results demonstrate that the adsorption process of these pharmaceutical compounds is done through a combination of physical and chemical interactions.


Assuntos
Ciprofloxacina , Poluentes Químicos da Água , Ciprofloxacina/química , Carvão Vegetal/química , Clorfeniramina , Poluentes Químicos da Água/química , Cinética , Adsorção
5.
Mol Psychiatry ; 28(9): 3648-3660, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37821573

RESUMO

Antipsychotic-induced sialorrhea carries a significant burden, but evidence-based treatment guidance is incomplete, warranting network meta-analysis (NMA) of pharmacological interventions for antipsychotic-related sialorrhea. PubMed Central/PsycInfo/Cochrane Central database/Clinicaltrials.gov/WHO-ICTRP and the Chinese Electronic Journal Database (Qikan.cqvip.com) were searched for published/unpublished RCTs of antipsychotic-induced sialorrhea (any definition) in adults, up to 06/12/2023. We assessed global/local inconsistencies, publication bias, risk of bias (RoB2), and confidence in the evidence, conducting subgroup/sensitivity analyses. Co-primary efficacy outcomes were changes in saliva production (standardized mean difference/SMD) and study-defined response (risk ratios/RRs). The acceptability outcome was all-cause discontinuation (RR). Primary nodes were molecules; the mechanism of action (MoA) was secondary. Thirty-four RCTs entered a systematic review, 33 NMA (n = 1958). All interventions were for clozapine-induced sialorrhea in subjects with mental disorders. Regarding individual agents and response, metoclopramide (RR = 3.11, 95% C.I. = 1.39-6.98), cyproheptadine, (RR = 2.76, 95% C.I. = 2.00-3.82), sulpiride (RR = 2.49, 95% C.I. = 1.65-3.77), propantheline (RR = 2.39, 95% C.I. = 1.97-2.90), diphenhydramine (RR = 2.32, 95% C.I. = 1.88-2.86), benzhexol (RR = 2.32, 95% C.I. = 1.59-3.38), doxepin (RR = 2.30, 95% C.I. = 1.85-2.88), amisulpride (RR = 2.23, 95% C.I. = 1.30-3.81), chlorpheniramine (RR = 2.20, 95% C.I. = 1.67-2.89), amitriptyline (RR = 2.09, 95% C.I. = 1.34-3.26), atropine, (RR = 2.03, 95% C.I. = 1.22-3.38), and astemizole, (RR = 1.70, 95% C.I. = 1.28-2.26) outperformed placebo, but not glycopyrrolate or ipratropium. Across secondary nodes (k = 28, n = 1821), antimuscarinics (RR = 2.26, 95% C.I. = 1.91-2.68), benzamides (RR = 2.23, 95% C.I. = 1.75-3.10), TCAs (RR = 2.23, 95% C.I. = 1.83-2.72), and antihistamines (RR = 2.18, 95% C.I. = 1.83-2.59) outperformed placebo. In head-to-head comparisons, astemizole and ipratropium were outperformed by several interventions. All secondary nodes, except benzamides, outperformed the placebo on the continuous efficacy outcome. For nocturnal sialorrhea, neither benzamides nor atropine outperformed the placebo. Active interventions did not differ significantly from placebo regarding constipation or sleepiness/drowsiness. Low-confidence findings prompt caution in the interpretation of the results. Considering primary nodes' co-primary efficacy outcomes and head-to-head comparisons, efficacy for sialorrhea is most consistent for the following agents, decreasing from metoclopramide through cyproheptadine, sulpiride, propantheline, diphenhydramine, benzhexol, doxepin, amisulpride, chlorpheniramine, to amitriptyline, and atropine (the latter not for nocturnal sialorrhea). Shared decision-making with the patient should guide treatment decisions regarding clozapine-related sialorrhea.


Assuntos
Antipsicóticos , Clozapina , Sialorreia , Adulto , Humanos , Antipsicóticos/efeitos adversos , Clozapina/uso terapêutico , Sulpirida/efeitos adversos , Amissulprida/efeitos adversos , Sialorreia/induzido quimicamente , Sialorreia/tratamento farmacológico , Doxepina/efeitos adversos , Amitriptilina/efeitos adversos , Metanálise em Rede , Propantelina/efeitos adversos , Triexifenidil/efeitos adversos , Metoclopramida/efeitos adversos , Clorfeniramina/efeitos adversos , Astemizol/efeitos adversos , Ensaios Clínicos Controlados Aleatórios como Assunto , Ciproeptadina/efeitos adversos , Difenidramina/efeitos adversos , Ipratrópio/efeitos adversos , Derivados da Atropina/efeitos adversos
6.
Spectrochim Acta A Mol Biomol Spectrosc ; 303: 123274, 2023 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-37603975

RESUMO

The Keteling capsule (KC) is a traditional Chinese medicine (TCM) made from the dried extract of Ficus microphylla and an appropriate amount of chlorpheniramine maleate. It is widely used to treat cough and relieve asthma. Despite its extensive usage, a rapid and comprehensive quality evaluation strategy for KC remains a challenge. This study introduces an electrochemical fingerprint analysis technique, in addition to the commonly employed HPLC fingerprints, for efficient and convenient quality evaluation. Moreover, a cost-effective, rapid, and accurate multi-component quantification technique known as the "Multi-markers assay by the monolinear method (MAML)" and the "FT-IR quantitative model" were explored. The HPLC fingerprints were evaluated using a systematically quantified fingerprint method, while the electrochemical fingerprints, based on the Belousov-Zhabotinsky oscillation reaction principle, were effectively analyzed and characterized using oxidation induction times and oscillation lifetimes. Multi-component quantitative analysis was carried out through the MAML and FT-IR quantitative models. The HPLC fingerprint successfully classified the 22 samples into eight grades with excellent discrimination. Active ingredient content analysis was achieved using reliable parameters obtained from electrochemical fingerprinting. The no significant difference in the quantitative results proves the accuracy of the MAML method. Additionally, successful FT-IR quantitative prediction models were developed for chlorogenic acid, isovitexin, and chlorpheniramine maleate. This study offers a dependable and effective approach for enhancing the quality control of KC, and it can provide new insights for improving the quality analysis methods in the field of TCM.


Assuntos
Bioensaio , Clorfeniramina , Cápsulas , Espectroscopia de Infravermelho com Transformada de Fourier , Ácido Clorogênico
7.
Leg Med (Tokyo) ; 64: 102294, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37369168

RESUMO

A man in his forties was found dead in his friend's home, with moderate putrefaction. Quantitative toxicological analysis showed that concentrations of caffeine, chlorpheniramine, dihydrocodeine, and methylephedrine were 183.3 µg/mL, 0.533 µg/mL, 2.469 µg/mL and 8.336 µg/mL, respectively. Ephedrine, amitriptyline, nortriptyline, etizolam, fluvoxamine and 7-aminoflunitrazepam were detected in an aortic blood sample. Caffeine, chlorpheniramine, dihydrocodeine and methylephedrine are the main components of BRONTM, an over-the-counter antitussive sold in Japan. Those concentrations in blood were within fatal ranges. Caffeine is classified as a methylxanthine and is mainly metabolized by cytochrome P450 (CYP)1A2. Fluvoxamine is a potent CYP1A2 inhibitor. Blood fluvoxamine concentration was within the therapeutic range, but would have increased blood caffeine level by the inhibition of caffeine metabolism. The conclusion was that his death was caused by BRONTM overdose. Inhibition of caffeine metabolism may increase blood caffeine concentrations. This suggests that more attention should be paid to potential interactions between multiple drugs.


Assuntos
Cafeína , Overdose de Drogas , Masculino , Humanos , Cafeína/metabolismo , Fluvoxamina , Clorfeniramina/farmacologia , Autopsia , Ingestão de Alimentos
8.
BMJ Open ; 13(2): e069733, 2023 02 17.
Artigo em Inglês | MEDLINE | ID: mdl-36806061

RESUMO

OBJECTIVE: To describe the price and affordability of key essential medicines for children in the private sector in Sri Lanka in 2017/2018, and compare the findings with 2009 data. DESIGN: National cross-sectional descriptive survey using the WHO/Health Action International medicine price methodology. SETTING AND PARTICIPANTS: Data were collected from a representative sample of 54 private sector pharmacies selected from all 9 provinces in Sri Lanka using a multistage clustered approach. MAIN OUTCOMES: Median price ratio (MPR) and affordability of originator brand (OB) and lowest priced generics (LPG) of 25 key essential medicines for children. RESULTS: The median MPR was 2.69 for OBs and 1.45 for LPGs compared with 3.7 and 1.35 in 2009. MPR of OB of all but one (chlorphenamine syrup) were higher than that of the LPG. MPR-OB>5 was observed for ceftriaxone injection, amoxicillin capsule, mebendazole chewable tablet and metronidazole tablet. This was documented in 2009 as well except for amoxicillin capsule. Prices of LPGs of seven medicines (amoxicillin capsule, amoxicillin suspension, clotrimazole cream, mebendazole chewable tablet, metronidazole tablet) were estimated as excessive (MPR ≥2.5) compared with chlorphenamine syrup, clotrimazole topical cream, ibuprofen syrup and paracetamol syrup in 2009. Compared with 2009, MPRs of OBs of 8 medicines and LPGs of 12 medicines were higher in 2017/2018. Compared with 2009, no change in affordability was noted except for asthma, which has been assessed as affordable in 2017/2018. Standard drug therapy for mild lower respiratory tract infections and acute gastroenteritis remained affordable, and treating epilepsy with carbamazepine syrup remained unaffordable. CONCLUSION: Economic access to key essential medicines for children has not improved in Sri Lanka in the 8 years' time since the initial survey in 2009.


Assuntos
Clorfeniramina , Medicamentos Essenciais , Humanos , Criança , Sri Lanka , Clotrimazol , Estudos Transversais , Países em Desenvolvimento , Mebendazol , Metronidazol , Amoxicilina , Medicamentos Genéricos
9.
Cells ; 12(3)2023 02 03.
Artigo em Inglês | MEDLINE | ID: mdl-36766852

RESUMO

Diabetic rat embryos have increased cortical neurogenesis and neuron maturation, and their offspring presented altered neuron polarity, lamination, and diminished neuron excitability. The FOXP2 overexpression results in higher cortical neurogenesis by increasing the transition of radial glia to the intermediate progenitor. Similarly, histamine through H1-receptor activation increases cortical neuron differentiation. Indeed, blocking the H1-receptor by the systemic administration of chlorpheniramine to diabetic pregnant rats prevents increased neurogenesis. Here, we explore the relationship between the H1-receptor and FOXP2 on embryo neurogenesis from diabetic dams. Through qRT-PCR, Western blot, immunohistofluorescence, and flow cytometry, we showed an increased FOXP2 expression and nuclear localization, a reduced Nestin expression and -positive cells number, and a higher PKCα expression in the cortical neuroepithelium of fourteen-day-old embryos from diabetic rats. Interestingly, this scenario was prevented by the chlorpheniramine systemic administration to diabetic pregnant rats at embryo day twelve. These data, together with the bioinformatic analysis, suggest that higher H1-receptor activity in embryos under high glucose increases FOXP2 nuclear translocation, presumably through PKCα phosphorylation, impairing the transition of radial glia to intermediate progenitor and increasing neuron differentiation in embryos of diabetic rats.


Assuntos
Diabetes Mellitus Experimental , Células-Tronco Neurais , Animais , Feminino , Gravidez , Ratos , Clorfeniramina/metabolismo , Diabetes Mellitus Experimental/metabolismo , Fatores de Transcrição Forkhead/metabolismo , Histamina/metabolismo , Células-Tronco Neurais/metabolismo , Neurogênese/fisiologia , Proteína Quinase C-alfa/metabolismo , Telencéfalo/metabolismo , Receptores Histamínicos H1
10.
Sci Total Environ ; 866: 161258, 2023 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-36587684

RESUMO

In Asian developing countries, undeveloped and ineffective sewer systems are causing surface water pollution by a lot of contaminants, especially pharmaceuticals and personal care products (PPCPs). Therefore, the risks for freshwater fauna need to be assessed. The present study aimed at: i) elucidating the contamination status; ii) evaluating the bioaccumulation; and iii) assessing the potential risks of PPCP residues in surface water and freshwater fish from three Asian countries. We measured 43 PPCPs in the plasma of several fish species as well as ambient water samples collected from India (Chennai and Bengaluru), Indonesia (Jakarta and Tangerang), and Vietnam (Hanoi and Hoa Binh). In addition, the validity of the existing fish blood-water partitioning model based solely on the lipophilicity of chemicals is assessed for ionizable and readily metabolizable PPCPs. When comparing bioaccumulation factors calculated from the PPCP concentrations measured in the fish and water (BAFmeasured) with bioconcentration factors predicted from their pH-dependent octanol-water partition coefficient (BCFpredicted), close values (within an order of magnitude) were observed for 58-91 % of the detected compounds. Nevertheless, up to 110 times higher plasma BAFmeasured than the BCFpredicted were found for the antihistamine chlorpheniramine in tilapia but not in other fish species. The plasma BAFmeasured values of the compound were significantly different in the three fish species (tilapia > carp > catfish), possibly due to species-specific differences in toxicokinetics (e.g., plasma protein binding and hepatic metabolism). Results of potential risk evaluation based on the PPCP concentrations measured in the fish plasma suggested that chlorpheniramine, triclosan, haloperidol, triclocarban, diclofenac, and diphenhydramine can pose potential adverse effects on wild fish. Results of potential risk evaluation based on the PPCP concentrations measured in the surface water indicated high ecological risks of carbamazepine, sulfamethoxazole, erythromycin, and triclosan on Asian freshwater ecosystems.


Assuntos
Carpas , Cosméticos , Triclosan , Poluentes Químicos da Água , Animais , Bioacumulação , Água , Clorfeniramina , Ecossistema , Índia , Cosméticos/análise , Carpas/metabolismo , Preparações Farmacêuticas , Poluentes Químicos da Água/análise , Monitoramento Ambiental
11.
Artigo em Inglês | MEDLINE | ID: mdl-36497913

RESUMO

In many parts of the world, water resources are scarce or even extremely scarce, and the reuse of water resources has become mainstream in today's world. Many regions use treated wastewater for agricultural irrigation, aquaculture, and other activities. However, in recent years, wastewater has been found to contain large amounts of pharmaceuticals and personal care products (PPCPs). Therefore, there is a potential risk of PPCPs being transported in the environment and affecting human health. In this study, we compared the uptake, transport, and accumulation of 27 PPCPs in three types of sprouts (radish, buckwheat, and okra).The bioaccumulation of amantadine, diphenhydramine, chlorpheniramine maleate, sibutramine, hemosibutramine, chlorosibutramine, N-monomethyl sibutramine, N, N-desmethyl sibutramine, and carbamazepine was found to be significantly higher in plants grown for 12 days in media containing 0.5, 5.0, and 50.0 ng/mL PPCPs. With increasing concentration of PPCPs in the culture solution, the amount of PPCPs absorbed by plants and the degree of accumulation also showed an increasing trend. At the same time, it was demonstrated that there was an obvious uptake transfer phenomenon of PPCPs by plants, and the trend of uptake transfer became more and more obvious as the concentration of external environmental pollutants increased. In addition, amantadine, chlorpheniramine maleate, carbamazepine, N, N-desmethyl sibutramine, hemosibutramine, and chlorosibutramine showed more active translocation in some plants (TF > 1.0).


Assuntos
Cosméticos , Poluentes do Solo , Poluentes Químicos da Água , Humanos , Verduras , Poluentes do Solo/análise , Clorfeniramina , Águas Residuárias , Irrigação Agrícola , Cosméticos/análise , Carbamazepina/análise , Plantas , Preparações Farmacêuticas , Poluentes Químicos da Água/análise , Monitoramento Ambiental
12.
Front Immunol ; 13: 930683, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36275732

RESUMO

Background: Systemic allergic reaction is characterized by vasodilation and vascular leakage, which causes a rapid, precipitous and sustained decrease in arterial blood pressure with a concomitant decrease of cardiac output. Histamine is a major mediator released by mast cells in allergic inflammation and response. It causes a cascade of inflammation and strongly increases vascular permeability within minutes through its four G-protein-coupled receptors (GPCRs) on endothelial cells. High mobility group box-1 (HMGB1), a nonhistone chromatin-binding nuclear protein, can be actively secreted into the extracellular space by endothelial cells. HMGB1 has been reported to exert pro-inflammatory effects on endothelial cells and to increase vascular endothelial permeability. However, the relationship between histamine and HMGB1-mediated signaling in vascular endothelial cells and the role of HMGB1 in anaphylactic-induced hypotension have never been studied. Methods and results: EA.hy 926 cells were treated with different concentrations of histamine for the indicated periods. The results showed that histamine induced HMGB1 translocation and release from the endothelial cells in a concentration- and time-dependent manner. These effects of histamine were concentration-dependently inhibited by d-chlorpheniramine, a specific H1 receptor antagonist, but not by H2 or H3/4 receptor antagonists. Moreover, an H1-specific agonist, 2-pyridylethylamine, mimicked the effects of histamine, whereas an H2-receptor agonist, 4-methylhistamine, did not. Adrenaline and noradrenaline, which are commonly used in the clinical treatment of anaphylactic shock, also inhibited the histamine-induced HMGB1 translocation in endothelial cells. We therefore established a rat model of allergic shock by i.v. injection of compound 48/80, a potent histamine-releasing agent. The plasma HMGB1 levels in compound 48/80-injected rats were higher than those in controls. Moreover, the treatment with anti-HMGB1 antibody successfully facilitated the recovery from compound 48/80-induced hypotension. Conclusion: Histamine induces HMGB1 release from vascular endothelial cells solely through H1 receptor stimulation. Anti-HMGB1 therapy may provide a novel treatment for life-threatening systemic anaphylaxis.


Assuntos
Anafilaxia , Histamina , Animais , Ratos , Anafilaxia/tratamento farmacológico , Clorfeniramina/farmacologia , Cromatina , Células Endoteliais , Epinefrina , Antagonistas dos Receptores Histamínicos H1/farmacologia , Antagonistas dos Receptores Histamínicos H1/uso terapêutico , Inflamação/tratamento farmacológico , Norepinefrina , p-Metoxi-N-metilfenetilamina , Receptores Acoplados a Proteínas G , Receptores Histamínicos H1/metabolismo
13.
Org Lett ; 24(41): 7677-7684, 2022 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-36214601

RESUMO

A general and mild strategy involving three-component carboarylation of unactivated alkenes with protic C(sp3)-H feedstocks via photoredox catalysis was reported. This catalytic system is compatible with a broad range of unactivated alkenes, cyano-substituted arenes, and diverse protic C(sp3)-H feedstocks. The synthetic value of this protocol was demonstrated by the late-stage functionalization of complex molecules and the synthesis of the antiallergies including pheniramine, chlorpheniramine, and brompheniramine.


Assuntos
Alcenos , Clorfeniramina , Catálise , Bromofeniramina
14.
Arch Razi Inst ; 77(1): 141-149, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-35891757

RESUMO

The current study was conducted to investigate the interaction between the central adrenergic and histaminergic systems and the broiler chick's feed intake. In the first experiment, the intracerebroventricular (ICV) injection of solutions was conducted which included 10 nmol of prazosin (an α1-receptor antagonist), 300 nmol of histamine, co-injection of prazosin and histamine. Experiments two to five were conducted similarly the same as the first experiment, in which chickens were ICV injected with 13 nmol of yohimbine (an α2-receptor antagonist), 24 nmol of metoprolol (a ß1 adrenergic receptor antagonist), 5 nmol of ICI 118,551 (a ß2 adrenergic receptor antagonist), and 20 nmol of SR 59230R (a ß3 adrenergic receptor antagonist). The injected solutions in the sixth experiment included 300 nmol of noradrenaline, 250 nmol of α-FMH (an alpha fluoromethyl histidine), noradrenaline, and α-FMH. Seventh to ninth experiments were similar to the sixth experiment, except that the chickens were ICV injected with 300 nmol of chlorpheniramine (a histamine H1 receptors antagonist), 82 nmol of famotidine (a histamine H2 receptors antagonist), and 300 nmol of thioperamide (a histamine H3 receptors antagonist), rather than α-FMH. Afterward, the cumulative food intake was measured 120 min after injection. Based on the obtained results, both histamine ICV injection and noradrenaline injection reduced food intake (P<0.05). Moreover, co-injection of histamine and ICI 118,551 (P<0.05), and co-injection of noradrenaline and Chlorpheniramine reduced food intake (P<0.05). In addition, noradrenaline and Thioperamide co-injection improved hypophagic effect of noradrenaline in neonatal chicken (P<0.05). These findings suggested the effect of interconnection between adrenergic and histaminergic systems, which may be mediated by H1 and H3 histaminergic and ß2 adrenergic receptors, on the regulation of food intake in the neonatal broiler chicken.


Assuntos
Apetite , Galinhas , Adrenérgicos/farmacologia , Antagonistas Adrenérgicos/farmacologia , Animais , Animais Recém-Nascidos , Clorfeniramina/farmacologia , Comportamento Alimentar/fisiologia , Histamina/farmacologia , Norepinefrina/farmacologia , Prazosina/farmacologia , Receptores Adrenérgicos , Receptores Histamínicos
15.
Molecules ; 27(12)2022 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-35744885

RESUMO

Non-destructive analysis of chlorpheniramine maleate (CPM), pharmaceutical tablets, and granules was conducted by chemometrics-assisted attenuated total reflectance infrared spectroscopy (ATR-IR). For tablets, an optimum PLSR model with eight latent factors was obtained from area-normalized and standard normal variate (SNV) pretreated ATR-IR spectral data with correlation coefficients (R2) of calibration and cross-validation of 0.9716 and 0.9602, respectively. The model capability for the 42 test set samples was proven with R2 between the reference and model prediction values of 0.9632, and a root-mean-square error of prediction (RMSEP) of 1.7786. The successive PLSR model for granules was constructed from SNV and first derivative pretreated ATR-IR spectral data with two latent factors and correlation coefficients (R2) of calibration and cross-validation of 0.9577 and 0.9450, respectively.


Assuntos
Quimiometria , Clorfeniramina , Calibragem , Análise dos Mínimos Quadrados , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Comprimidos
16.
J Allergy Clin Immunol Pract ; 10(10): 2685-2692.e2, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35413472

RESUMO

BACKGROUND: An optimal strategy for choosing safe alternative low osmolar contrast media (LOCM) has not yet been established in patients with a history of LOCM-induced anaphylaxis. OBJECTIVES: To validate the practical pathway in patients with anaphylaxis to LOCMs and to compare 2 different doses of challenge testing with skin test-negative LOCM. METHODS: A retrospective cohort study was performed in patients with LOCM-induced anaphylaxis. Patients were challenged with intravenous LOCMs showing negativity in the skin test according to 2 different protocols: low-dose and high-dose (maximum dose 10 and 30 mL, respectively). Challenge-negative LOCMs were selected for use during computed tomography scans, and patients received intravenous pretreatment with 4 mg chlorpheniramine and 40 mg methylprednisolone. RESULTS: Of the 110 challenge tests, there were 4 (3.6%) positive challenges. Among 106 enhanced computed tomography scans performed using challenge-negative LOCMs, breakthrough reactions occurred in 8 (7.6%). Breakthrough reaction rates were not statistically different between the 2 protocols (8.9% and 6.0% in the low-dose challenge and the high-dose challenge, respectively). Compared with the low-dose protocol, the number needed to test of the high-dose challenge test decreased 2.5-fold. Moreover, none of the patients in the high-dose challenge group incurred severe reactions during computed tomography scans with challenge-negative LOCM, whereas 80% of reactions were severe in the low-dose challenge group. CONCLUSIONS: We validated a pathway consisting of a battery of skin testing to LOCMs and challenge with skin test-negative LOCM in patients with LOCM-induced anaphylaxis.


Assuntos
Anafilaxia , Meios de Contraste , Anafilaxia/induzido quimicamente , Anafilaxia/diagnóstico , Clorfeniramina , Meios de Contraste/efeitos adversos , Humanos , Metilprednisolona , Concentração Osmolar , Estudos Retrospectivos
17.
Am J Emerg Med ; 57: 236.e1-236.e3, 2022 07.
Artigo em Inglês | MEDLINE | ID: mdl-35459564

RESUMO

Chlorpheniramine is an H1 receptor antagonist of the alkylamine class. It is a widely used anti-allergy drug due to its strong antihistamine effect and mild adverse effects. In the case of chlorpheniramine overdose or poisoning, the primary manifestation is central nervous system symptoms. To date, no case of rhabdomyolysis induced by acute poisoning with chlorpheniramine has ever been reported. This study reports a case of acute chlorpheniramine poisoning at an oral dose of 4000 mg, which is the highest reported poisoning dose to date. The diagnosis of rhabdomyolysis (creatine kinase, 195,489 U/L) and acute kidney injury (serum creatinine, 150.1 umol/L) was confirmed based on laboratory results. After haemoperfusion and continuous renal replacement therapy, the patient's renal function fully recovered. This paper aims to analyse the clinical data of this patient and summarize its clinical characteristics. At the same time, the mechanism of chlorpheniramine-induced rhabdomyolysis is also explored in the context of the literature review.


Assuntos
Injúria Renal Aguda , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Rabdomiólise , Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/terapia , Clorfeniramina , Creatina Quinase , Creatinina , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/complicações , Antagonistas dos Receptores Histamínicos H1 , Humanos , Rabdomiólise/induzido quimicamente , Rabdomiólise/diagnóstico , Rabdomiólise/terapia
18.
Anal Methods ; 14(12): 1221-1231, 2022 03 24.
Artigo em Inglês | MEDLINE | ID: mdl-35237778

RESUMO

A chromatographic technique based on a chiral stationary phase (CSP) has been explored for enantioseparation. Herein, poly(glycidyl methacrylate) (poly(GMA)) brushes were grafted on the surface of silica gel via surface-initiated atom transfer radical polymerization (SI-ATRP), followed by the introduction of vancomycin as a chiral selector. The as-synthesized material was characterized by elemental analysis, scanning electron microscopy (SEM), Fourier transform infrared (FT-IR) and thermogravimetric analysis (TGA), proving the formation of vancomycin-immobilized brushes. Then the resulting CSP was explored to separate 7 racemic drugs (bicalutamide, 1-benzyl-5-phenylbarbituric acid, chlorpheniramine maleate, fluoxetine hydrochloride, verapamil hydrochloride, benzoxazocine hydrochloride and isoprenaline hydrochloride) in high performance liquid chromatography (HPLC). Several factors affecting the enantioseparation performance of the vancomycin-immobilized CSP, including the triethylamine (TEA) content in the buffer, pH value, content of organic solvent in the mobile phase, flow rate and injection volume, were mainly optimized. Under the optimal conditions, baseline separation of fluoxetine hydrochloride (RS = 2.52) was achieved, which was better than that on a commercial Chirobiotic V column, while enantioseparation of bicalutamide (RS = 1.01), chlorpheniramine maleate (RS = 0.77), 1-benzyl-5-phenylbarbituric acid (RS = 0.67), isoprenaline hydrochloride (RS = 0.73), verapamil hydrochloride (RS = 0.91) and benzoxazocine hydrochloride (RS = 1.03) was partly achieved. It was concluded that SI-ATRP is a robust way to fabricate vancomycin-based CSPs for enantioseparation.


Assuntos
Clorfeniramina , Vancomicina , Cromatografia Líquida de Alta Pressão/métodos , Fluoxetina , Isoproterenol , Polimerização , Espectroscopia de Infravermelho com Transformada de Fourier , Estereoisomerismo , Vancomicina/química , Verapamil
19.
Eur J Clin Pharmacol ; 78(6): 897-906, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35218404

RESUMO

OBJECTIVE: Catheter-related bladder discomfort (CRBD) is a common complication of intraoperative urinary catheterization. Various studies have evaluated the efficacy of different interventions in postoperative CRBD. The present review was performed to assess the efficacy of these interventions. METHODS: PubMed, Embase, and CENTRAL (Cochrane Central Register of Controlled Trials) databases were systematically searched to identify randomized controlled trials (RCTs) investigating the efficacy of different drugs for the prevention of postoperative CRBD. This review evaluated the incidence and severity of CRBD after different interventions at 0, 1, 2, and 6 h postoperatively. RESULTS: Forty-five studies including 31 different drugs were analyzed. Eleven drugs were investigated in more than two RCTs, of which dexmedetomidine, gabapentin, tolterodine, tramadol, ketamine, nefopam, oxybutynin, pregabalin, and pudendal nerve block (PNB) generally showed significantly higher efficacy than controls postoperatively. Solifenacin only showed significant efficacy compared with the control at 0 h, and intravenous lidocaine only showed significant efficacy compared with the control at 6 h. There were insufficient trials to draw conclusions regarding atropine, butylscopolamine, chlorpheniramine, clonidine, darifenacin, diphenhydramine, glycopyrrolate, intravesical bupivacaine, ketamine-haloperidol, pethidine-haloperidol, ketorolac, lidocaine-prilocaine cream, magnesium, hyoscine n-butyl bromide, oxycodone, paracetamol, parecoxib, trospium, resiniferatoxin, or amikacin. However, all but pethidine-haloperidol and chlorpheniramine showed some efficacy at various time points compared with controls. CONCLUSION: This review suggests that dexmedetomidine, gabapentin, tolterodine, tramadol, ketamine, nefopam, oxybutynin, pregabalin, and PNB are effective in preventing postoperative CRBD. Considering the efficacy and adverse effects of all drugs, dexmedetomidine and gabapentin were ranked best.


Assuntos
Dexmedetomidina , Ketamina , Nefopam , Tramadol , Clorfeniramina/farmacologia , Clorfeniramina/uso terapêutico , Dexmedetomidina/uso terapêutico , Gabapentina/farmacologia , Gabapentina/uso terapêutico , Haloperidol/uso terapêutico , Humanos , Lidocaína , Meperidina/farmacologia , Meperidina/uso terapêutico , Nefopam/farmacologia , Nefopam/uso terapêutico , Dor Pós-Operatória/tratamento farmacológico , Dor Pós-Operatória/prevenção & controle , Pregabalina/farmacologia , Tartarato de Tolterodina/farmacologia , Tartarato de Tolterodina/uso terapêutico , Tramadol/uso terapêutico , Bexiga Urinária/cirurgia , Cateteres Urinários/efeitos adversos
20.
J AOAC Int ; 105(3): 703-716, 2022 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-35015880

RESUMO

BACKGROUND: A combination of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form is specified for the treatment of common cold and flu symptoms. OBJECTIVE: The functional role of this study is to develop a novel, reliable, and selective stability-indicating reversed-phase ultra-performance liquid chromatography (RP-UPLC) method for simultaneous identification of a quaternary mixture of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form. METHOD: The specific method is accomplished using an Acquity UPLC HSS T3 C18 column (2.1 mm × 100 mm), 1.8 µm particle size with pore size 100 Å, utilizing a mixture of purified water-methanol-trifluoroacetic acid (72.5:27.5:1.5, v/v) as the mobile phase at a flow rate of 0.3 mL/min. The column void volume is 1.15 min. UPLC detection is adjusted at 205 nm using a photodiode array detector. RESULTS: Calibration curves are obtained in the linearity ranges: 25-500 µg/mL for paracetamol, 10-50 µg/mL for pseudoephedrine, 0.5-5 µg/mL for chlorpheniramine, and 3-30 µg/mL for sodium benzoate with a correlation coefficient > 0.9992. The mean recovery of the developed method is tested and shows good recovery results between 99-101%; selectivity and forced degradation studies are investigated as per the International Council for Harmonisation Guidelines and no interference is detected due to degradation peaks. CONCLUSION: The proposed stability-indicating UPLC method for simultaneous determination of the three drugs, paracetamol, pseudoephedrine, and chlorpheniramine, with a preservative sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form is successfully accomplished, developed, and validated, and can be easily used in the analysis of drugs in pure or dosage form. HIGHLIGHTS: The novelty of the current research work lies in the development of the UPLC method for simultaneous determination of a quaternary mixture of paracetamol, pseudoephedrine, chlorpheniramine, and sodium benzoate in (Cold-Flu) 1,2,3 Syrup dosage form.


Assuntos
Clorfeniramina , Resfriado Comum , Acetaminofen/análise , Clorfeniramina/análise , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Pseudoefedrina/análise , Benzoato de Sódio/análise
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...