Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 293
Filter
1.
Arch. argent. pediatr ; 119(4): e357-e359, agosto 2021.
Article in Spanish | LILACS, BINACIS | ID: biblio-1281895

ABSTRACT

El montelukast se utiliza ampliamente en el tratamiento de sibilancias recurrentes y/o asma. Están descritas numerosas reacciones adversas medicamentosas (RAM) en niños relacionadas con montelukast; se destacan las neuropsiquiátricas. Realizamos un estudio observacional, retrospectivo, descriptivo, sobre RAM relacionadas con montelukast. Entre enero de 2012 y diciembre de 2017, en la Unidad de Neumonología Pediátrica se trataron con Montelukast 348 pacientes; de ellos, 20 presentaron RAM. Los síntomas más frecuentes fueron insomnio (n = 7), hiperactividad (n = 4), pesadillas (n = 3), dolor abdominal (n = 2) y parestesias en extremidades (n = 2). Se presentaron desde días hasta meses tras iniciar el tratamiento, y desaparecieron tras su suspensión. Se destacan dos pacientes con parestesias en extremidades, síntoma no descrito antes en niños. El 5,7 % de los pacientes tratados con montelukast presentaron RAM que requirieron suspender el tratamiento. Los trastornos del sueño fueron los más frecuentes.


Montelukast is widely used in recurrent wheezing and/or asthma treatment. Several adverse drug reactions (ADRs) have been described in children related to montelukast. Neuropsychiatric reactions are one of the most important. We designed an observational, retrospective, descriptive study on ADRs related to montelukast in the Pediatric Pulmonology Unit, Hospital Universitario Miguel Servet, Zaragoza, Spain. Between January 2012 and December 2017, in the Pediatric Pulmonology Unit, 348 patients were treated with Montelukast; of them, 20 presented RAM. The main symptoms described were insomnia (n = 7), hyperactivity (n = 4), nightmares (n = 3), abdominal pain (n = 2) and paraesthesia in extremities (n = 2). They appeared from the first days to months after the start of treatment and disappeared after stopping it. Two patients presented limb paresthesia, not described previously in children. The 5.7 % of our patients treated with montelukast had ADRs that required treatment discontinuation. Sleep disorders were the most frequent.


Subject(s)
Humans , Male , Female , Infant, Newborn , Infant , Child, Preschool , Child , Adolescent , Quinolines/adverse effects , Sulfides/adverse effects , Anti-Asthmatic Agents/adverse effects , Leukotriene Antagonists/adverse effects , Cyclopropanes/adverse effects , Acetates/adverse effects , Asthma/drug therapy , Sleep Wake Disorders/chemically induced , Retrospective Studies
2.
Rev. Soc. Bras. Med. Trop ; 54: e05362020, 2021. tab, graf
Article in English | LILACS | ID: biblio-1155593

ABSTRACT

Abstract INTRODUCTION: Artemisinin-based combination therapy (ACT), such as artemisinin-piperaquine (AP), dihydroartemisinin-piperaquine (DP), and artemether-lumefantrine (AL), is the first-line treatment for malaria in many malaria-endemic areas. However, we lack a detailed evaluation of the cardiotoxicity of these ACTs. This study aimed to analyze the electrocardiographic effects of these three ACTs in malaria patients. METHODS: We analyzed the clinical data of 89 hospitalized patients with falciparum malaria who had received oral doses of three different ACTs. According to the ACTs administered, these patients were divided into three treatment groups: 27 treated with AP (Artequick), 31 with DP (Artekin), and 31 with AL (Coartem). Electrocardiograms and other indicators were recorded before and after the treatment. The QT interval was calculated using Fridericia's formula (QTcF) and Bazett's formula (QTcB). RESULTS: Both QTcF and QTcB interval prolongation occurred in all three groups. The incidence of such prolongation between the three groups was not significantly different. The incidence of both moderate and severe prolongation was not significantly different between the three groups. The ΔQTcF and ΔQTcB of the three groups were not significantly different. The intra-group comparison showed significant prolongation of QTcF after AL treatment. CONCLUSIONS: Clinically recommended doses of DP, AL, and AP may cause QT prolongation in some malaria patients but do not cause torsades de pointes ventricular tachycardia or other arrhythmias.


Subject(s)
Humans , Malaria, Falciparum/drug therapy , Artemisinins/adverse effects , Malaria/drug therapy , Antimalarials/adverse effects , Quinolines , Drug Combinations , Electrocardiography , Artemether/therapeutic use , Artemether, Lumefantrine Drug Combination/therapeutic use
3.
Chinese Journal of Lung Cancer ; (12): 739-742, 2021.
Article in Chinese | WPRIM | ID: wpr-922241

ABSTRACT

45.7% of Chinese patients with advanced lung adenocarcinoma were reported to harbour sensitizing epidermal growth factor receptor (EGFR) mutations. Limited therapeutic options are left for non-small cell lung cancer (NSCLC) harbouring sensitizing EGFR mutations after failure of EGFR-tyrosine kinase inhibitor (TKI) therapy and chemotherapy, finding effective options for them is an unmet clinic need. Herein we reported a case that till January 12, 2021, an 82-year-old female with sensitizing EGFR-mutant advanced lung adenocarcinoma received a surprising progression-free survival (PFS) benefit of over 21 months from the combination therapy of pembrolizumab and anlotinib after her failure of treatments of osimertinib, chemotherapy and anlotinib-monotherapy.
.


Subject(s)
Adenocarcinoma of Lung/genetics , Aged, 80 and over , Antibodies, Monoclonal, Humanized , Antineoplastic Combined Chemotherapy Protocols , Carcinoma, Non-Small-Cell Lung/genetics , ErbB Receptors/genetics , Female , Humans , Indoles , Lung Neoplasms/genetics , Mutation , Quinolines
4.
Chinese Medical Journal ; (24): 2954-2961, 2021.
Article in English | WPRIM | ID: wpr-921228

ABSTRACT

BACKGROUND@#Despite the recommendation of inhaled corticosteroids (ICSs) plus long-acting beta 2-agonist (LABA) and leukotriene receptor antagonist (LTRA) or ICS/LTRA as stepwise approaches in asthmatic children, there is a lack of published systematic review comparing the efficacy and safety of the two therapies in children and adolescents aged 4 to 18 years. This study aimed to compare the safety and efficacy of salmeterol/fluticasone (SFC) vs. montelukast (MON), or combination of montelukast and fluticasone (MFC) in children and adolescents aged 4 to 18 years with bronchial asthma.@*METHODS@#A systematic search was conducted in MEDLINE, EMBASE, the Cochrane Library, China BioMedical Literature Database, Chinese National Knowledge Infrastructure, VIP Database for Chinese Technical Periodical, and Wanfang for randomized controlled trials (RCTs) published from inception to May 24, 2021. Interventions are as follows: SFC vs. MON, or combination of MFC, with no limitation of dosage or duration. Primary and secondary outcome measures were as follows: the primary outcome of interest was the risk of asthma exacerbation. Secondary outcomes included risk of hospitalization, pulmonary function, asthma control level, quality of life, and adverse events (AEs). A random-effects (I2 ≥ 50%) or fixed-effects model (I2 < 50%) was used to calculate pooled effect estimates, comparing the outcomes between the intervention and control groups where feasible.@*RESULTS@#Of the 1006 articles identified, 21 studies met the inclusion criteria with 2643 individuals; two were at low risk of bias. As no primary outcomes were similar after an identical treatment duration in the included studies, meta-analysis could not be performed. However, more studies favored SFC, instead of MON, owing to a lower risk of asthma exacerbation in the SFC group. As for secondary outcome, SFC showed a significant improvement of peak expiratory flow (PEF)%pred after 4 weeks compared with MFC (mean difference [MD]: 5.45; 95% confidence interval [CI]: 1.57-9.34; I2 = 95%; P = 0.006). As for asthma control level, SFC also showed a higher full-controlled level (risk ratio [RR]: 1.51; 95% CI: 1.24-1.85; I2 = 0; P < 0.001) and higher childhood asthma control test score after 4 weeks of treatment (MD: 2.30; 95% CI: 1.39-3.21; I2 = 72%; P < 0.001) compared with MFC.@*CONCLUSIONS@#SFC may be more effective than MFC for the treatment of asthma in children and adolescents, especially in improving asthma control level. However, there is insufficient evidence to make firm conclusive statements on the use of SFC or MON in children and adolescents aged 4 to 18 years with asthma. Further research is needed, particularly a combination of good-quality long-term prospective studies and well-designed RCTs.@*PROSPERO REGISTRATION NUMBER@#CRD42019133156.


Subject(s)
Acetates , Administration, Inhalation , Adolescent , Adrenal Cortex Hormones/therapeutic use , Albuterol/therapeutic use , Anti-Asthmatic Agents/therapeutic use , Asthma/drug therapy , Child , Cyclopropanes , Drug Therapy, Combination , Fluticasone/therapeutic use , Humans , Quinolines , Salmeterol Xinafoate/therapeutic use , Sulfides
5.
Article in Chinese | WPRIM | ID: wpr-878889

ABSTRACT

Three compounds, including scolosprine C(1), uracil(2) and hypoxanthine(3), were isolated and purified from the ethyl acetate fraction of centipede by silica gel normal-phase column chromatography, reversed-phase medium pressure preparation chromatography, and high-pressure semi-preparative HPLC. The structure was elucidated through a combination of spectroscopic analyses [such as nuclear magnetic resonance(NMR) and mass spectrometry(MS)] and literature review. Among them, compound 1 was a new quinoline alkaloid. In previous reports, we have described the isolation and structure elucidation of one new and two known quinoline alkaloids. In this paper, we would report the isolation and structure elucidation of scolosprine C in detail.


Subject(s)
Alkaloids , Animals , Arthropods , Chilopoda , Quinolines
6.
Braz. j. otorhinolaryngol. (Impr.) ; 86(1): 63-73, Jan.-Feb. 2020. tab, graf
Article in English | LILACS | ID: biblio-1089372

ABSTRACT

Abstract Introduction The types of allergic rhinitis are roughly classified based on the causative antigens, disease types, predilection time, and symptom severity. Objective To examine the clinical typing and individualized treatment approach for allergic rhinitis and to determine the optimal treatment method for this disease using various drug combination therapies. Methods A total of 108 participants with allergic rhinitis were divided into three groups based on symptoms. Subsequently, each group was further categorized into four subgroups based on the medications received. The efficacy of the treatments was evaluated using the visual analog scale VAS scores of the total and individual nasal symptoms, decline index of the symptom score, histamine and leukotriene levels, and mRNA and protein expression levels of histamine 1 and cysteinyl leukotriene 1 receptors. Results Loratadine + mometasone furoate and loratadine + mometasone furoate + montelukast significantly improved the sneezing symptom and reduced the histamine levels compared with the other combination therapies (p < 0.05). Meanwhile, montelukast + mometasone furoate and montelukast + mometasone furoate + loratadine considerably improved the nasal obstruction symptom and decreased the leukotriene D4 levels compared with the other combination therapies (p < 0.05). Conclusion Clinical symptom evaluation combined with experimental detection of histamine and leukotriene levels can be an objective and accurate method to clinically classify the allergic rhinitis types. Furthermore, individualized treatment based on allergic rhinitis classification can result in a good treatment efficacy.


Resumo Introdução A rinite alérgica é basicamente classificada de acordo com os antígenos causadores, tipos de doença, peridiocidade e gravidade dos sintomas. Objetivo Avaliar os tipos clínicos e a abordagem terapêutica individualizada para cada tipo de rinite alérgica e determinar o método de tratamento ideal utilizando várias terapias de combinação de fármacos. Método Um total de 108 participantes com rinite alérgica foram divididos em três grupos com base nos sintomas. Posteriormente, cada grupo foi subsequentemente categorizado em quatro subgrupos com base nos medicamentos recebidos. A eficácia dos tratamentos foi avaliada utilizando os escores da escala visual analógica EVA dos sintomas nasais totais e individualmente, índice de declínio do escore de sintomas, níveis de histamina e leucotrienos e níveis de expressão de mRNA e proteína dos receptores de histamina 1 e cisteinil-leucotrieno 1. Resultados As associações entre loratadina + furoato de mometasona, assim como a de loratadina + furoato de mometasona + montelucaste melhoraram significativamente o sintoma de espirros e reduziram os níveis de histamina em comparação às outras terapias combinadas (p < 0,05). Por outro lado, a associação montelucaste + furoato de mometasona, assim como a associação montelucaste + furoato de mometasone + loratadina melhoraram consideravelmente o sintoma de obstrução nasal e diminuíram os níveis de leucotrieno D4 em comparação com as outras combinações (p < 0,05). Conclusão A avaliação clínica dos sintomas combinada com a detecção experimental dos níveis de histamina e leucotrieno pode ser um método objetivo e preciso para classificar clinicamente os tipos de rinite alérgica. Além disso, o tratamento individualizado baseado na classificação da rinite alérgica pode resultar no aumento da eficácia do tratamento.


Subject(s)
Humans , Male , Female , Adolescent , Adult , Middle Aged , Aged , Young Adult , Histamine/blood , Leukotriene D4/blood , Drug Therapy, Combination/methods , Precision Medicine/methods , Rhinitis, Allergic/blood , Quinolines/therapeutic use , Sneezing , RNA, Messenger/genetics , Receptors, Histamine H1/genetics , Nasal Obstruction/drug therapy , Treatment Outcome , Loratadine/therapeutic use , Receptors, Leukotriene/genetics , Anti-Allergic Agents/therapeutic use , Rhinitis, Allergic/diagnosis , Rhinitis, Allergic/drug therapy , Mometasone Furoate/therapeutic use , Acetates/therapeutic use , Nasal Mucosa
7.
Acta cir. bras ; 35(9): e202000905, 2020. tab, graf
Article in English | LILACS | ID: biblio-1130676

ABSTRACT

Abstract Purpose To determine the nephroprotective effect of NAC and Montelukast Sodium administration against the development of renal damage associated with long warm renal ischemia. Methods Twenty-seven rats were randomly divided into 3 study groups, which received NAC, montelukast and placebo, and 3 rats were included in the sham-treated control group. Medications were given 3 days before the procedure. DMSA renal scintigraphy was performed before and after surgery. The right renal pedicle was occluded for 45 min to induce ischemia and then subjected to reperfusion for 6 h (I/R groups). Results On pathological examination, the mean pathological scores of the montelukast and NAC groups were significantly lower than those of the placebo group. (p <0.05). In biochemical examination, significant differences were found in all parameter levels between the placebo group and the montelukast and NAC groups. (p <0.05) When postoperative DMSA renal scintigraphy measurements and renal function levels were compared, significant differences were found between the montelukast and NAC groups and the placebo and sham groups. Conclusion The administration of NAC and montelukast sodium was seen to have a nephroprotective effect against the development of renal damage associated with warm renal ischemia.


Subject(s)
Animals , Rats , Acetylcysteine/pharmacology , Quinolines/pharmacology , Reperfusion Injury/prevention & control , Acetates/pharmacology , Sulfides , Tomography, X-Ray Computed , Rats, Wistar , Succimer , Cyclopropanes , Kidney/blood supply
8.
Rev. Soc. Bras. Med. Trop ; 53: e20200091, 2020. graf
Article in English | LILACS, ColecionaSUS, SES-SP | ID: biblio-1136875

ABSTRACT

Abstract INTRODUCTION: The drugs currently available for leishmaniasis treatment have major limitations. METHODS: In vitro and in vivo studies were performed to evaluate the effect of a quinoline derivative, Hydraqui (7-chloro-4-(3-hydroxy-benzilidenehydrazo)quinoline, against Leishmania amazonensis. In silico analyses of absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters were performed. RESULTS: Hydraqui showed significant in vitro anti-amastigote activity. Also, Hydraqui-treated mice exhibited high efficacy in lesion size (48.3%) and parasitic load (93.8%) reduction, did not cause hepatic and renal toxicity, and showed appropriate ADMET properties. CONCLUSIONS: Hydraqui presents a set of satisfactory criteria for its application as an antileishmanial agent.


Subject(s)
Animals , Female , Quinolines/therapeutic use , Leishmania mexicana/drug effects , Leishmaniasis, Cutaneous/drug therapy , Antiprotozoal Agents/therapeutic use , Quinolines/chemistry , Leishmaniasis, Cutaneous/parasitology , Disease Models, Animal , Parasite Load , Mice , Mice, Inbred BALB C
9.
Braz. j. med. biol. res ; 53(7): e9271, 2020. tab, graf
Article in English | LILACS, ColecionaSUS | ID: biblio-1132527

ABSTRACT

Montelukast sodium is an effective and well-tolerated anti-asthmatic drug. Long non-coding RNAs (lncRNAs) are involved in the treatment of asthma. Therefore, this study aimed to investigate the effect of montelukast sodium on children with cough-variant asthma (CVA) and the role of lncRNA prostate cancer gene expression marker 1 (PCGEM1) in drug efficacy. The efficacy of montelukast sodium was evaluated by assessing the release of inflammatory factors and pulmonary function in CVA children after a 3-month treatment. An ovalbumin (OVA)-sensitized mouse model was developed to simulate asthmatic conditions. PCGEM1 expression in clinical peripheral blood samples and lung tissues of asthmatic mice was determined. Asthmatic mice experienced nasal inhalation of PCGEM1 overexpression with simultaneous montelukast sodium to investigate the roles of PCGEM1 in asthma treatment. The NF-κB axis after PCGEM1 overexpression was detected to explore the underling mechanisms. Consequently, montelukast sodium contributed to reduced levels of pro-inflammatory factors and improved pulmonary function in CVA children. PCGEM1 was poorly expressed in OVA-sensitized asthmatic mice and highly expressed in CVA children with response to the treatment. PCGEM1 overexpression enhanced the anti-inflammatory effects and promoted effects on pulmonary function of montelukast sodium in CVA children and OVA-sensitized asthmatic mice. Furthermore, PCGEM1 inhibited the activation of the NF-κB axis. This study demonstrated the anti-inflammatory and lung-protective effects of montelukast sodium on CVA, which was strengthened by overexpression of PCGEM1. Findings in this study highlighted a potential anti-asthmatic target of montelukast sodium.


Subject(s)
Quinolines/therapeutic use , Asthma/drug therapy , Anti-Asthmatic Agents/therapeutic use , Protective Agents/therapeutic use , Cough/drug therapy , RNA, Long Noncoding/metabolism , Acetates/therapeutic use , Asthma/blood , Cough/blood , Disease Models, Animal , Mice, Inbred BALB C
10.
Chinese Journal of Oncology ; (12): 807-816, 2020.
Article in Chinese | WPRIM | ID: wpr-877492

ABSTRACT

Anlotinib hydrochloride is the only anti-angiogenic, multi-targeted tyrosine kinase inhibitor, which has been approved for non-small cell lung cancer and small cell lung cancer in China. In order to provide guidance for clinical practitioners to use anlotinib hydrochloride safely and efficiently, the Chinese Association for Clinical Oncologists, the Expert Committee of Vascular Targeted Therapy of Chinese Society of Clincal Oncology and the Cancer Targeted Therapy Professional Committee of China Anti-Cancer Association co-organized experts and integrated multiple evidences of Anlotinib Hydrochloride, from both clinical trial, post-marketed clinical data and the associated experiences of experts accumulated in clinical practice, etc. The present consensus covers the clinical data of anlotinib hydrochloride applied in advanced non-small cell lung cancer and small cell lung cancer, and the safety management recommendations.


Subject(s)
Carcinoma, Non-Small-Cell Lung/drug therapy , China , Consensus , Humans , Indoles/therapeutic use , Lung Neoplasms/drug therapy , Protein Kinase Inhibitors/therapeutic use , Quinolines/therapeutic use
11.
Rev. Soc. Bras. Med. Trop ; 52: e20180453, 2019. tab, graf
Article in English | LILACS | ID: biblio-1041531

ABSTRACT

Abstract INTRODUCTION: Concern regarding the cardiotoxicity of antimalarials has been renewed because of their potential to cause QT/QTc interval prolongation related to torsade de pointes (TdP). Artemisinin-piperaquine (AP) is considered an effective artemisinin-based combination therapy (ACT) for malaria. METHODS: This study involved a retrospective analysis of clinical data of 93 hospitalized malaria patients who had received AP orally. Electrocardiograms (ECGs) were obtained at specific time points in the original study. RESULTS: Some cases of QT prolongation were observed. However, no TdP was found. CONCLUSIONS: AP may cause QT interval prolongation in some malaria patients but may not lead to TdP.


Subject(s)
Humans , Male , Female , Adult , Quinolines/adverse effects , Long QT Syndrome/chemically induced , Malaria, Falciparum/drug therapy , Artemisinins/adverse effects , Antimalarials/adverse effects , Quinolines/therapeutic use , Long QT Syndrome/diagnosis , Retrospective Studies , Artemisinins/therapeutic use , Drug Therapy, Combination , Electrocardiography , Middle Aged , Antimalarials/therapeutic use
12.
Article in Chinese | WPRIM | ID: wpr-774111

ABSTRACT

OBJECTIVE@#To study the association of cytoplasmic phospholipase A2 (PLA2G4) rs932476 polymorphism with the development of bronchial asthma and the response to montelukast, a leukotriene receptor antagonist, in children.@*METHODS@#A total of 128 children with bronchial asthma were enrolled as case group, and 100 healthy children were enrolled as control group. The genotype and allele frequencies of PLA2G4 rs932476 were compared between the two groups. The children in the case group were administered with montelukast except routine treatment for 2 months, and the changes in serum levels of leukotriene B4 (LTB4), interleukin-4 (IL-4), immunoglobulin E (IgE), and interferon gamma (IFN-γ), pulmonary function and fractional exhaled nitric oxide (FeNO) after treatment were observed.@*RESULTS@#There were no significant differences in the genotype and allele frequencies of PLA2G4 rs932476 between the case and control groups, as well as between the groups with different severities of asthma (P>0.05). After treatment, the children with AA genotype had a significantly higher overall response rate than those with GG genotype. After treatment, the case group had significant reductions in the serum levels of IgE and IL-4 and a significant increase in the level of IFN-γ (P<0.05). After treatment, the children with GG genotype had a higher serum level of IL-4 and a lower level of IFN-γ than those with AA genotype. After treatment, the case group had significant increases in pulmonary function parameters, and the children with AA genotype had significantly higher parameters than those with GG genotype. The case group had a significant reduction in the level of FeNO, and the children with AA genotype had a significantly lower level than those with GG genotype after treatment. The case group had a significantly higher serum level of LTB4 than the control group before treatment (P<0.05). After treatment the case group had a significant reduction in the serum level of LTB4 (P<0.05). The children with GG genotype had a significantly higher level of LTB4 than those with AA genotype after treatment (P<0.05).@*CONCLUSIONS@#PLA2G4 rs932476 polymorphism is not associated with the susceptibility and severity of bronchial asthma in children, but it may has certain influence on children's response to the leukotriene receptor antagonist montelukast, possibly by affecting the level of LTB4.


Subject(s)
Acetates , Asthma , Child , Humans , Leukotriene Antagonists , Quinolines
13.
Article in Chinese | WPRIM | ID: wpr-774065

ABSTRACT

OBJECTIVE@#To study the clinical effect of different combinations of fluticasone propionate (Flu), montelukast sodium (Mon) and ketotifen (Ket) in the treatment of children with cough variant asthma (CVA).@*METHODS@#A total of 280 children with CVA who were admitted to the department of respiratory medicine from June 2015 to January 2018 were randomly divided into Flu+Mon+Ket, Flu+Mon, Flu+Ket, Mon+Ket, Flu, Mon and Ket groups, with 40 children in each group. The children in each group were given corresponding drug(s), and the course of treatment was 3 months for all groups. The condition of cough, cough symptom score, pulmonary function and adverse drug reactions were evaluated after 2 and 3 months of treatment. The children were followed up to observe recurrence.@*RESULTS@#After treatment, cough symptom score tended to decrease in all 7 groups, with increases in percentage of forced expiratory volume in 1 second (FEV1%) and percentage of predicted peak expiratory flow (PEF%). After 2 months of treatment, the Flu+Mon+Ket group had a significantly lower cough symptom score and significantly higher FEV1% and PEF% than the other groups (P0.05). There was a low incidence rate of adverse events in all 7 groups, and there was no significant difference among the 7 groups (P>0.05). The Ket group had a significantly higher recurrence rate of cough than the other groups (P0.0024).@*CONCLUSIONS@#For children with CVA, a combination of Flu, Mon and Ket has a better clinical effect than a combination of two drugs and a single drug at 2 months of treatment and is safe. After 3 months of treatment, Flu or Mon alone has a similar effect to drug combination. Ket alone has a poor clinical effect and a high recurrence rate after drug withdrawal.


Subject(s)
Acetates , Androstadienes , Anti-Asthmatic Agents , Asthma , Drug Therapy , Child , Cough , Drug Therapy , Drug Combinations , Fluticasone , Humans , Ketotifen , Quinolines
14.
Arch. endocrinol. metab. (Online) ; 62(6): 636-640, Dec. 2018. tab, graf
Article in English | LILACS | ID: biblio-983805

ABSTRACT

ABSTRACT Objective: The advent of multikinase inhibitor (MKI) therapy has led to a radical change in the treatment of patients with advanced thyroid carcinoma. The aim of this manuscript is to communicate rare adverse events that occurred in less than 5% of patients in clinical trials in a subset of patients treated in our hospital. Subjects and methods: Out of 760 patients with thyroid cancer followed up with in our Division of Endocrinology, 29 (3.8%) received treatment with MKIs. The median age at diagnosis of these patients was 53 years (range 20-70), and 75.9% of them were women. Sorafenib was prescribed as first-line treatment to 23 patients with differentiated thyroid cancer and as second-line treatment to one patient with advanced medullary thyroid cancer (MTC). Vandetanib was indicated as first-line treatment in 6 patients with MTC and lenvatinib as second-line treatment in two patients with progressive disease under sorafenib treatment. Results: During the follow-up of treatment (mean 13.7 ± 7 months, median 12 months, range 6-32), 5/29 (17.2%) patients presented rare adverse events. These rare adverse effects were: heart failure, thrombocytopenia, and squamous cell carcinoma during sorafenib therapy and squamous cell carcinoma and oophoritis with intestinal perforation during vandetanib treatment. Conclusions: About 3 to 5 years after the approval of MKI therapy, we learned that MKIs usually lead to adverse effects in the majority of patients. Although most of them are manageable, we still need to be aware of potentially serious and rare or unreported adverse effects that can be life-threatening.


Subject(s)
Humans , Male , Female , Adult , Middle Aged , Aged , Young Adult , Piperidines/adverse effects , Quinazolines/adverse effects , Carcinoma/drug therapy , Carcinoma, Medullary/drug therapy , Protein Kinase Inhibitors/adverse effects , Antineoplastic Agents/adverse effects , Oophoritis/chemically induced , Phenylurea Compounds/adverse effects , Quinolines/adverse effects , Thrombocytopenia/chemically induced , Time Factors , Thyroid Neoplasms/drug therapy , Retrospective Studies , Risk Factors , Follow-Up Studies , Kaplan-Meier Estimate , Sorafenib/adverse effects , Heart Failure/chemically induced , Intestinal Perforation/chemically induced
15.
Biol. Res ; 51: 14, 2018. graf
Article in English | LILACS | ID: biblio-950900

ABSTRACT

BACKGROUND: Neurokinin1 (NK1) receptor has played a vital role in the development of tumor. However, NKP608 as a NK1 receptor antagonist whether has the effect of the resistance of colorectal cancer is still unclear. Thereby, in this study, we investigated the role of NKP608 on human colorectal cancer and explored the underlying mechanism. METHODS: The cell proliferation of colorectal cancer cells was detected by cell counting kit-8 (CCK8) assay, cell migration and invasion were assessed by transwell assay, the apoptotic ratio of cells was assessed by Annexin V-fluorescein isothiocyanate/propidium iodide stained and flow cytometry. The involvement of molecular mechanisms was examined by western blot. RESULTS: In this study, we found that NKP608 inhibited the proliferation, migration/invasion of HCT116 cells. In addition, NKP608 reduced expressions of Wnt-3a, ß-catenin, Cyclin D1, and (vascular endothelial growth factor) VEGF while induced expression of E-Cadherin. Furthermore, flow cytometry analyzed that NKP608 induced apoptosis of HCT116 cells, consistently, western blotting detecting of apoptosis-related proteins revealed that NKP608 downregulated Bcl-2 while upregulated Bax and Active-Caspase-3. CONCLUSIONS: Taken together, our results demonstrated that NKP608 inhibited colorectal cancer cell proliferation, migration and invasion via suppressing the Wnt/ß-catenin signaling pathway. Therefore, NKP608 might represent a promising therapeutic agent in the treatment of colorectal cancer.


Subject(s)
Humans , Piperidines/pharmacology , Quinolines/pharmacology , Colorectal Neoplasms/pathology , Cell Movement/drug effects , Cell Proliferation/drug effects , Wnt Signaling Pathway/drug effects , Neurokinin-1 Receptor Antagonists/pharmacology , Down-Regulation/drug effects , Blotting, Western , Cell Line, Tumor , HCT116 Cells , Flow Cytometry
16.
Article in Chinese | WPRIM | ID: wpr-772604

ABSTRACT

OBJECTIVE@#: To determine the effects of cysteinyl leukotriene receptors (CysLTR and CysLTR) on phagocytosis of mouse BV2 microglial cells.@*METHODS@#: BV2 cells were stimulated with microglial activators lipopolysaccharide (LPS) or CysLT receptor agonists LTD. The phagocytosis of BV2 cells was observed by immunofluorescence analysis and flow cytometry. The intracellular distributions of CysLTR and CysLTR in BV2 cells were examined with immunofluorescence staining.@*RESULTS@#: Both LPS and LTD could significantly enhance the phagocytosis of BV2 cells, and such effect could be inhibited by CysLTR selective antagonist Montelukast and CysLTR selective antagonist HAMI 3379. The activation of BV2 cells induced by LTD or LPS resulted in changes in intracellular distributions of CysLTR and CysLTR. CysLTR and CysLTR was co-localization with a similar distribution.@*CONCLUSIONS@#: CysLTR and CysLTR regulate the phagocytosis of mouse BV2 microglial cells with a synergistic effect.


Subject(s)
Acetates , Pharmacology , Animals , Cell Line , Cyclohexanecarboxylic Acids , Pharmacology , Lipopolysaccharides , Pharmacology , Mice , Microglia , Cell Biology , Phagocytosis , Phthalic Acids , Pharmacology , Protein Binding , Quinolines , Pharmacology , Receptors, Leukotriene , Metabolism
17.
Chinese Journal of Lung Cancer ; (12): 428-430, 2018.
Article in Chinese | WPRIM | ID: wpr-772422

ABSTRACT

In recent years, the number of advanced non-small cell lung cancer (NSCLC) patients has gradually increased, and the treatment methods have also been significantly increased. However, there are no standard treatment plans at home and abroad for third-line and above patients who are refractory to targeted therapy epidermal growth factor receptor (EGFR)/anaplastic lymphoma kinase (ALK) or chemotherapy. The clinical treatment effect is also not satisfactory. Anlotinib is a novel TKI targeting the vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptor (PDGFR) and c-Kit. ALTER0303 trail, phase III study has demonstrated that Anlotinib significantly prolonged overall survival (OS) and progression-free survival (PFS) in advanced NSCLC patients as 3rd line treatment.Here we report a case of advanced lung adenocarcinoma harboring KRAS mutation treated with Anlotinib.
.


Subject(s)
Adenocarcinoma , Drug Therapy , Genetics , Pathology , Adenocarcinoma of Lung , Aged , Antineoplastic Agents , Therapeutic Uses , Humans , Indoles , Therapeutic Uses , Lung Neoplasms , Drug Therapy , Genetics , Pathology , Male , Mutation , Proto-Oncogene Proteins p21(ras) , Genetics , Metabolism , Quinolines , Therapeutic Uses
18.
Article in Chinese | WPRIM | ID: wpr-776666

ABSTRACT

OBJECTIVE@#To study the effect of montelukast sodium (MK), a leukotriene receptor antagonist, and bacterial lysates (OM-85BV), used alone or in combination, on airway remodeling and the expression of transforming growth factor-β1 (TGF-β1) and Smad7 in guinea pigs with bronchial asthma and their correlation.@*METHODS@#A total of 40 male Hartley guinea pigs were randomly divided into normal control group, asthma group, MK group, OM-85BV group, and MK+OM-85BV group, with 8 guinea pigs in each group. Intraperitoneal injection of 10% ovalbumin (OVA) for sensitization and aerosol inhalation of 1% OVA for challenge were performed to establish a model of airway remodeling of asthma in all of the groups apart from the normal control group, which were treated with normal saline. In the stage of challenge by aerosol inhalation, the guinea pigs in the MK, OM-85BV, and MK+OM-85BV groups were given corresponding suspension by gavage, and those in the normal control and asthma groups were given an equal volume of normal saline by gavage. Bronchoalveolar lavage fluid (BALF) of the guinea pigs was collected within 24 hours after challenge, and ELISA was used to measure the levels of TGF-β1 and Smad7 in BALF. The guinea pigs were sacrificed and the pathological section of lung tissue was prepared to observe the degree of airway remodeling. An image analysis technique was used to measure perimeter of the basement membrane (Pbm), total bronchial wall area (Wat), and airway bronchial smooth muscle area (Wam). Pearson linear regression was used to investigate the correlation between two variables.@*RESULTS@#According to the lung pathological section, compared with the normal control group, the asthma, MK, OM-85BV, and MK+OM-85BV groups had significant thickening of bronchial smooth muscle and alveolar wall, significantly higher Wat/Pbm and Wam/Pbm, a significantly higher level of TGF-β1, and a significantly lower level of Smad7 (P<0.05). Compared with the asthma group, the MK, OM-85BV, and MK+OM-85BV groups had a significant improvement in pathological injury, significantly lower Wat/Pbm and Wam/Pbm, a significantly lower level of TGF-β1, and a significantly higher level of Smad7 (P<0.05). The MK+OM-85BV group had significantly greater improvements than the MK group and the OM-85BV group (P<0.05). The expression of TGF-β1 was negatively correlated with that of Smad7 and positively correlated with Wat/Pbm and Wam/Pbm, and the expression of Smad7 was negatively correlated with Wat/Pbm and Wam/Pbm (P<0.01).@*CONCLUSIONS@#MK and OM-85BV, used alone or in combination, can reduce airway remodeling in guinea pigs with asthma, and MK combined with OM-85BV has the best effect, possibly by reducing TGF-β1 expression, increasing Smad7 expression, and improving the TGF-β1/Smad7 imbalance.


Subject(s)
Acetates , Airway Remodeling , Animals , Asthma , Cell Extracts , Guinea Pigs , Lung , Male , Ovalbumin , Quinolines , Transforming Growth Factor beta1
19.
Article in Chinese | WPRIM | ID: wpr-775401

ABSTRACT

The root bark of Dictamnus dasycarpus is one of common traditional Chinese medicines (TCMs). Quinoline alkaloids are one of the main active substances in this TCM and possess many biological activities including anti-titumor, anti-inflammation, anti-bacteria, anti-oxidation, and anti-platelet aggregation activities. In this study, eight quinoline alkaloids 1-8 were firstly separated from the root barks of D. dasycarpus. It was difficult to isolate more quinoline alkaloids from the remaining fraction 8 in D. dasycarpus by this conventional chemical separation, so the target analysis method combined LC-MS guided-separation of quinoline alkaloids from fraction 8 was established. MS/MS fragmentation patterns of eight quinoline alkaloids reference standard compounds 1-8 were studied by ultra-performance liquid chromatography-electrospary ionization-mass spectrometry (UPLC-ESI-MS/MS). Based on the feature fragment ion 200, the parent ion scan mode was established for the target analysis of quinoline alkaloids in fraction 8. Finally, 8-methoxyflindersine (9) and N-metilatanina (10) were discovered and isolated quickly from fraction 8 guided by LC-MS, and their structures were identified by NMR and MS. Among them, compound 10 was isolated from the genus Dictamnus for the first time. These results indicated that this method is not only quick and sensitive for analyzing the quinoline alkaloids, but also to effectively guided-separate this kind of alkaloids in the root barks of D. dasycarpus.


Subject(s)
Alkaloids , Chromatography, High Pressure Liquid , Dictamnus , Chemistry , Ions , Phytochemicals , Plant Roots , Chemistry , Quinolines , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry
20.
Journal of Experimental Hematology ; (6): 1116-1121, 2018.
Article in Chinese | WPRIM | ID: wpr-689519

ABSTRACT

<p><b>OBJECTIVE</b>To study the effect of HDAC inhibitor Scriptaid on multiple myeloma IM9 cells and preliminarily clarify the mechanism of Scriptaid-induced cell apoptosis.</p><p><b>METHODS</b>The cell viability, cell cycle and cell apoptosis were measured by CCK8 assay and flow cytometry respectively, the relative target gene expression levels were detected by RT-PCR, the effect of Scriptaid on p21 promoter activity was detected by using luciferase reporter assay.</p><p><b>RESULTS</b>Scriptaid inhibited IM9 cell viability in a dose-dependent manner. Scriptaid induced IM9 cell cycle arrest at G/M phase in a dose-dependent manner. Scriptaid triggered IM9 cell apoptosis was obviously, the mRNA levels of apoptosis-related proteins Caspase 9, Caspase 3 and PARP1 were also activated. The apoptosis-associated factors BAD, PTEN and p21 increased following treatment with different dose of Scriptaid, meanwhile, p21 promoter activity was also activated significantly.</p><p><b>CONCLUSION</b>HDAC inhibitor Scriptaid can promote IM9 cell apoptosis by transcriptional activation of p21 promoter in concentration-dependent manner.</p>


Subject(s)
Apoptosis , Cell Cycle , Cell Line, Tumor , Cell Proliferation , Cyclin-Dependent Kinase Inhibitor p21 , Histone Deacetylase Inhibitors , Pharmacology , Humans , Hydroxylamines , Pharmacology , Quinolines , Pharmacology
SELECTION OF CITATIONS
SEARCH DETAIL