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1.
Beijing Da Xue Xue Bao Yi Xue Ban ; 56(2): 293-298, 2024 Apr 18.
Artículo en Zh | MEDLINE | ID: mdl-38595247

RESUMEN

OBJECTIVE: The pain-relieving effect and safety of compound aminopyrine phenacetin tablets, tramcontin (tramadol hydrochloride sustained-release tablets) and dolantin in the early stage of autologous tendon reconstruction of the anterior cruciate ligament (ACL) of the knee joint were compared. METHODS: Retrospective analysis of postoperative pain and drug analgesia in 45 patients performed by the same group from November 2018 to February 2019. The random area group design was divided into two groups according to whether ACL rupture was combined with meniscal injury, group A was 24 patients with ACL reconstruction of knee joint and group B was 21 patients with ACL fracture combined with meniscus injury. The two groups were divided into three subgroups respectively according to the actual treatment of postoperative analgesic drugs received by the patients, including 4 cases of compound aminopyrine phenacetin tablets, 11 cases of oral tramcontin, 9 cases of intramuscular dolantin combined with phenergan in group A; 3 cases of compound aminopyrine phenacetin tablets, 10 cases of oral tramcontin, and 8 cases of intramuscular dolantin combined with phenergan in group B. When the early postoperative patients complain about pain and actively ask for analgesia. When the patients complained about pain after the operation and actively asked for analgesia, they were randomly given painkillers, tramcontin or dolantin combined with phenergan to relieve pain. Pain visual analogue scale (VAS) was used to evaluate pain relief and observe the occurrence of adverse reactions. RESULTS: There were no significant dif-ferences in gender, age, body mass index, and time of hospital stay between the two groups of patients (P > 0.05). In the patients who used tramcontin and dolantin combined with phenergan to relieve pain judging by VAS score before and 1 h after taking the drug, it was found that the pain situation of the patient was significantly relieved, and the difference before and after taking the drug had statistical significance (P < 0.05). Pairwise comparisons of the three drugs applied in the two groups showed significantly greater pain relief in the dolantin combined with phenergan group than in the remaining two drugs. There was no significant difference (P > 0.05). Dolantin was prone to nausea and vomiting, but the application of phenergan was also used to reduce side effects. In terms of adverse reactions, only 1 case of nausea occurred in the tramcontin group for simple ACL reconstruction, and none of the patients in the other groups showed serious complications and allergic reactions. CONCLUSION: Whether in cruciate ligament reconstruction alone or combined with meniscus molding or suture, compound aminopyrine phenacetin tablets, tramcontin, dolantin combined with phenergan can effectively relieve pain. Among the three drugs, dolantin caused the largest pain relief. At the same time, the combination of phenergan effectively reduced the adverse reactions, such as vomiting and nausea, and increased the drug safety.


Asunto(s)
Lesiones del Ligamento Cruzado Anterior , Reconstrucción del Ligamento Cruzado Anterior , Humanos , Aminopirina , Analgésicos , Lesiones del Ligamento Cruzado Anterior/cirugía , Articulación de la Rodilla/cirugía , Meperidina , Náusea/cirugía , Dolor Postoperatorio/tratamiento farmacológico , Fenacetina , Prometazina , Estudios Retrospectivos , Resultado del Tratamiento , Vómitos/cirugía
2.
Sensors (Basel) ; 22(10)2022 May 12.
Artículo en Inglés | MEDLINE | ID: mdl-35632090

RESUMEN

Here, we describe 4-dimethylaminoantipyrine (4-DMAA)-mediated interfacing as a broad biochemical indicator to stabilize and promote the higher response of electrodes for immunological detection. We hypothesized that the improved biological interactions of 4-DMAA with electrodes and biological samples may be due to the interaction properties of the benzene and pyrazole chemical groups with graphite and proteins, respectively. In order to demonstrate that 4-DMAA could be used as a general indicator in electrochemical immunoassays, we used peptides as probes for the diagnosis of four neglected tropical infectious diseases Tegumentary leishmaniasis, Visceral leishmaniasis, Strongyloidiasis, and Leprosy on commercial graphite screen-printed electrodes. 4-DMAA oxidation was used to indicate specific biological recognition between the epitope-based peptide and serum immunoglobulin G (IgG) from infected patients. We demonstrated that 4-DMAA should be incorporated into the electrodes prior to serum application, which avoids interference with its sensitivity and specificity. In addition, 4-DMAA oxidizes at a low anodic potential, and the oxidation peak is useful for detecting proteins in biological fluids. In summary, we have successfully demonstrated the broad application of 4-DMAA as a general indicator for the specific diagnosis of four infectious diseases in electrochemical immunosensors. Such a strategy is quite advantageous for indirect detection of proteins that lack electrochemical activities or are spatially inaccessible on the electrode surface. This new indicator opens a new avenue for monitoring biological recognition, especially for immunosensors.


Asunto(s)
Técnicas Biosensibles , Grafito , Aminopirina , Electrodos , Humanos , Inmunoensayo
3.
Mol Divers ; 25(3): 1701-1715, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-32862361

RESUMEN

The work presented in this paper aims toward the synthesis of aryl thiourea derivatives 4a-l of pyrazole based nonsteroidal anti-inflammatory drug named 4-aminophenazone, as potential inhibitors of intestinal alkaline phosphatase enzyme. The screening of synthesized target compounds 4a-l for unraveling the anti-inflammatory potential against calf intestinal alkaline phosphatase gives rise to lead member 4c possessing IC50 value 0.420 ± 0.012 µM, many folds better than reference standard used (KH2PO4 IC50 = 2.8 ± 0.06 µM and L-phenylalanine IC50 = 100 ± 3.1 µM). SAR for unfolding the active site binding pocket interaction along with the mode of enzyme inhibition based on kinetic studies is carried out which showed non-competitive binding mode. The enzyme inhibition studies were further supplemented by molecular dynamic simulations for predicting the protein behavior against active inhibitors 4c and 4g during docking analysis. The preliminary toxicity of the synthesized compounds was determined by using brine shrimp assay. This work also includes detailed biochemical analysis along with RO5 parameters for all the newly synthesized drug derivatives 4a-l.


Asunto(s)
Fosfatasa Alcalina/química , Aminopirina/química , Inhibidores Enzimáticos/química , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Tiourea/química , Aminopirina/análogos & derivados , Sitios de Unión , Fenómenos Químicos , Técnicas de Química Sintética , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacología , Humanos , Cinética , Estructura Molecular , Unión Proteica , Solventes , Análisis Espectral , Relación Estructura-Actividad , Tiourea/síntesis química , Tiourea/farmacología
4.
Liver Int ; 40(3): 530-538, 2020 03.
Artículo en Inglés | MEDLINE | ID: mdl-31507057

RESUMEN

BACKGROUND & AIMS: In patients with hepatitis C virus (HCV)-related advanced cirrhosis, the effects of sustained virological response (SVR) by direct antiviral agents (DAAs) on decompensation and liver deaths are less clearcut, since up to 30% of patients do not improve, and no predictors of outcome have been identified. We used 13 C-aminopyrine breath test (ABT) to assess whether its changes can predict liver-related outcomes after DAA treatment in patients with HCV cirrhosis. METHODS: Fifty consecutive patients with HCV cirrhosis were enrolled. Patients were included if they had Child A cirrhosis at risk for decompensation - defined as Child A6 (N = 22, 44%) or previous decompensation (N = 7, 14%) - or Child B cirrhosis (N = 21, 42%) eligible for DAA-based antiviral therapy. ABT was performed at baseline and 12 weeks after the end of antiviral therapy. Patients received sofosbuvir-based regimens. RESULTS: Aminopyrine breath test was available for all 50 patients at baseline. The 120' cumulative dose was directly associated at regression analysis only with albumin levels (P = .001). ABT was available at follow-up week 12 for 41 patients (FUW12), all with SVR, and followed for a median of 25.2 months (range 12.2-32.1 months). Lower Ʌ ABT - defined as changes of 120' cumulative dose from FUW12 to baseline - (HR 0.97, 95% CI 0.94-0.99; P = .02) and FUW12 hepatic encephalopathy (HR 19.0, 95% CI 1.16-310.3; P = .03) were the only independent predictors of liver events/death at multivariate Cox regression analysis. The AUC of Ʌ ABT was good (0.87, 95% CI 0.75-0.97), with a delta ≥0% well discriminating patients at lower vs patients at higher risk of liver-related events/death (P < .001). CONCLUSIONS: In patients with advanced HCV cirrhosis who achieve SVR with DAA, Ʌ ABT assists in assessing the residual likelihood of liver-related events and deaths after viral cure.


Asunto(s)
Hepatitis C Crónica , Hepatitis C , Aminopirina/uso terapéutico , Antivirales/uso terapéutico , Pruebas Respiratorias , Niño , Hepacivirus , Hepatitis C/complicaciones , Hepatitis C/diagnóstico , Hepatitis C/tratamiento farmacológico , Hepatitis C Crónica/complicaciones , Hepatitis C Crónica/tratamiento farmacológico , Humanos , Cirrosis Hepática/diagnóstico , Cirrosis Hepática/tratamiento farmacológico
5.
AAPS PharmSciTech ; 20(7): 264, 2019 Jul 24.
Artículo en Inglés | MEDLINE | ID: mdl-31342293

RESUMEN

The humidity was a well-known method to hydrate the skin; however, the published data were varied, and systemic experiments in the previous papers were few. Therefore, the in vitro permeation of excised porcine ear skin by drugs with different polarities [aminopyrine (AMP), antipyrine (ANP), methylparaben (MP), and ibuprofen (IP)] was analyzed under a constant skin surface temperature with different temperatures and humidities to reveal the effects of temperature and humidity on the skin permeation enhancement effects. Applied formulations were prepared by mixing the drug and a hydrophilic vehicle containing glycerin. The disposition-distance profiles of water and the humectant glycerin in the stratum corneum were also investigated using confocal Raman microscopy. High absolute humidity (AH) significantly contributed to the high skin penetration of the hydrophilic penetrants AMP, ANP, and MP but not the hydrophobic penetrant IP. An increase in the partition parameter and a decrease in the diffusivity parameter occurred with an increase in AH, independent of drug polarity. Moreover, we found that dew condensation induced by high AH on temperature-controlled skin surface may effectively increase water content and may provide higher glycerin distribution in the skin barrier, the stratum corneum. Increasing the amount of water and hydrophilic vehicles such as glycerin in the stratum corneum may enhance the permeation of hydrophilic penetrants AMP, ANP, and MP. These data suggested a dew condensation on the skin surface induced by high AH at a constant skin surface temperature would be important to enhance hydrophilic penetrants.


Asunto(s)
Absorción Cutánea , Piel/metabolismo , Temperatura , Aminopirina/farmacocinética , Animales , Antipirina/farmacocinética , Epidermis , Humedad , Interacciones Hidrofóbicas e Hidrofílicas , Ibuprofeno/farmacocinética , Parabenos/farmacocinética , Porcinos
6.
Drug Dev Res ; 79(6): 287-294, 2018 09.
Artículo en Inglés | MEDLINE | ID: mdl-30295945

RESUMEN

Preclinical Research & Development Pancreatic cancer is the third leading cause of death in the US with a poor 5-year survival rate of 8.5%. A novel anti-cancer drug, dimethylamino parthenolide (DMAPT), is the water-soluble analog of the natural sesquiterpene lactone, parthenolide. The putative modes of action of DMAPT are inhibition of the Nuclear chain factor kappa-light-chain enhancer of activated B cells (NFκB) pathway and depletion of glutathione levels; the latter causing cancer cells to be more susceptible to oxidative stress-induced cell death. Actinomycin-D (ActD) is a polypeptide antibiotic that binds to DNA, and inhibits RNA and protein synthesis by inhibiting RNA polymerase II. A phase 2 clinical trial indicated that ActD could be a potent drug against pancreatic cancer; however, it was not a favored drug due to toxicity issues. New drug entities and methods of drug delivery, used alone or in combination, are needed to treat pancreatic cancer more effectively. Thus, it was postulated that combining DMAPT and ActD would result in synergistic inhibition of Panc-1 pancreatic cancer cell growth because DMAPT's inhibition of NFκB would enhance induction of apoptosis by ActD, via phosphorylation of c-Jun, by minimizing NFκB inhibition of c-Jun phosphorylation. Combining these two drugs induced a higher level of cell death than each drug alone. A fixed drug ratio of DMAPT: ActD (1,200:1) was used. Data from metabolic (MTT) and colony formation assays were analyzed for synergism with CompuSyn software, which utilizes the Chou-Talalay equation. The analyses indicated synergism and moderate synergism at combination concentrations of DMAPT/ActD of 12/0.01 and 18/0.015 µM, respectively.


Asunto(s)
Aminopirina/administración & dosificación , Antibióticos Antineoplásicos/administración & dosificación , Dactinomicina/administración & dosificación , Inhibidores de Crecimiento/administración & dosificación , Neoplasias Pancreáticas/tratamiento farmacológico , Antibióticos Antineoplásicos/efectos adversos , Apoptosis/efectos de los fármacos , Dactinomicina/efectos adversos , Combinación de Medicamentos , Sinergismo Farmacológico , Inhibidores de Crecimiento/efectos adversos , Humanos , Neoplasias Pancreáticas/patología , Células Tumorales Cultivadas
7.
J Immunol ; 193(4): 1954-65, 2014 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-25024378

RESUMEN

Canonical neutrophil antimicrobial effector mechanisms, such as degranulation, production of reactive oxygen species, and release of neutrophil extracellular traps (NETs), can result in severe pathology. Activation of neutrophils through immune complexes (ICs) plays a central role in the pathogenesis of many autoimmune inflammatory diseases. In this study, we report that immobilized ICs (iICs), which are hallmarks of several autoimmune diseases, induce the release of NETs from primary human neutrophils. The iIC-induced NET formation was found to require production of reactive oxygen species by NADPH oxidase and myeloperoxidase and to be mediated by FcγRIIIb. Blocking of the ß2 integrin macrophage-1 Ag but not lymphocyte function-associated Ag-1 abolished iIC-induced NET formation. This suggests that FcγRIIIb signals in association with macrophage-1 Ag. As intracellular signaling pathways involved in iIC-induced NET formation we identified the tyrosine kinase Src/Syk pathway, which downstream regulates the PI3K/Akt, p38 MAPK, and ERK1/2 pathways. To our knowledge, the present study shows for the first time that iICs induce NET formation. Thus, we conclude that NETs contribute to pathology in autoimmune inflammatory disorders associated with surface-bound ICs.


Asunto(s)
Complejo Antígeno-Anticuerpo/inmunología , Antígeno de Macrófago-1/inmunología , Activación Neutrófila/inmunología , Neutrófilos/inmunología , Receptores de IgG/inmunología , Aminopirina/farmacología , Antioxidantes/farmacología , Ácido Ascórbico/farmacología , Enfermedades Autoinmunes/inmunología , Butadienos/farmacología , Antígeno CD11a/metabolismo , Antígenos CD18/metabolismo , Degranulación de la Célula , Células Cultivadas , Quinasas MAP Reguladas por Señal Extracelular/antagonistas & inhibidores , Proteínas Ligadas a GPI/inmunología , Humanos , Imidazoles/farmacología , Inflamación/inmunología , Péptidos y Proteínas de Señalización Intracelular/antagonistas & inhibidores , Péptidos y Proteínas de Señalización Intracelular/inmunología , Antígeno-1 Asociado a Función de Linfocito/inmunología , Antígeno de Macrófago-1/metabolismo , Mesalamina/farmacología , Nitrilos/farmacología , Compuestos Onio/farmacología , Inhibidores de las Quinasa Fosfoinosítidos-3 , Proteínas Tirosina Quinasas/antagonistas & inhibidores , Proteínas Tirosina Quinasas/inmunología , Proteínas Proto-Oncogénicas c-akt/antagonistas & inhibidores , Piridinas/farmacología , Pirimidinas/farmacología , Especies Reactivas de Oxígeno/metabolismo , Receptores de IgG/antagonistas & inhibidores , Quinasa Syk , Proteínas Quinasas p38 Activadas por Mitógenos/antagonistas & inhibidores , Familia-src Quinasas/antagonistas & inhibidores , Familia-src Quinasas/inmunología
8.
J Pharm Pharm Sci ; 19(4): 423-429, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-28057172

RESUMEN

PURPOSE: The metabolic activities of aminopyrine N-demethylation and tolbutamide methylhydroxylation by the human hepatic cytochrome P450 (P450 or CYP) 2C subfamily were compared and the effects of azole antifungal agent on the drug-metabolizing activity of CYP2C8 were investigated. METHODS: Aminopyrine N-demethylation and tolbutamide methylhydroxylation by CYP2C8, CYP2C9, and CYP2C19 were determined by the previous reported methods. The effects of five azole antifungal agents, fluconazole, itraconazole, ketoconazole, miconazole, and voriconazole, on the aminopyrine N-demethylation activity by CYP2C8 were investigated. RESULTS: With regard to aminopyrine N-demethylation, CYP2C19 had the lowest Michaelis constant (Km) and CYP2C8 had the highest maximal velocity (Vmax) among the CYP2C subfamily members. The Vmax/Km values for CYP2C8 were the highest, followed by CYP2C19. For tolbutamide methylhydroxylation, the Km and Vmax for CYP2C19 were three and six times higher than the corresponding values for CYP2C9, and the Vmax/Km value for CYP2C19 was twice that for CYP2C9, whereas hydroxylated tolbutamide formed by CYP2C8 was not detected. Fluconazole, itraconazole, and voriconazole at a concentration of 2 or 10 µM neither inhibited nor stimulated CYP2C8-mediated aminopyrine N-demethylation activity at substrate concentrations around the Km (5 mM). However, ketoconazole and miconazole noncompetitively inhibited CYP2C8-mediated aminopyrine N-demethylation with the inhibitory constant values of 1.98 and 0.86 µM, respectively. CONCLUSION: These results suggest that ketoconazole and miconazole might inhibit CYP2C8 clinically. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.


Asunto(s)
Aminopirina/farmacología , Antifúngicos/farmacología , Azoles/farmacología , Inhibidores Enzimáticos del Citocromo P-450/farmacología , Sistema Enzimático del Citocromo P-450/metabolismo , Tolbutamida/farmacología , Aminopirina/química , Antifúngicos/química , Azoles/química , Inhibidores Enzimáticos del Citocromo P-450/química , Relación Dosis-Respuesta a Droga , Humanos , Relación Estructura-Actividad , Especificidad por Sustrato , Tolbutamida/química
9.
Chem Pharm Bull (Tokyo) ; 64(11): 1597-1606, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27803471

RESUMEN

This study investigated the effects of 25 kinds of esters that are used in cosmetics on the permeation of four model compounds with different polarities (caffeine [CF], aminopyrine [AMP], benzoic acid [BA], and flurbiprofen [FP]). The amount of each model compound that permeated through two types of artificial membrane (silicone and Strat-M®) was measured and correlated with the physicochemical properties of the esters, including their solubility, viscosity, wettability, surface tension, and uptake. The amount of each model compound that permeated through the silicone membrane was not significantly correlated with the solubility of the esters but was significantly correlated with all other measured physical properties of the esters. Similar correlations were observed for the amounts of AMP, BA, and FP that passed through the Strat-M® membrane. However, the amount of CF that permeated through the Strat-M® membrane also correlated with the solubility of the esters. There was a highly significant correlation between the amount permeating through the silicone and Strat-M® membranes because the model compounds had high lipophilicity. These findings demonstrated that to control the permeation of various chemicals through artificial membranes, it is important to consider the uptake of the esters and that the solubility of the esters is also an important consideration when using a more complex membrane.


Asunto(s)
Cosméticos/química , Ésteres/química , Ensayos Analíticos de Alto Rendimiento , Membranas Artificiales , Siliconas/química , Aminopirina/química , Ácido Benzoico/química , Cafeína/química , Difusión , Flurbiprofeno/química
10.
J Sep Sci ; 38(23): 4048-54, 2015 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-26434939

RESUMEN

The concentrations of residual aminopyrine and antipyrine in porcine muscle, milk, and egg samples were analyzed using liquid chromatography with tandem mass spectrometry after undergoing a series of sample pretreatment steps. Owing to an ion suppression effect, matrix-matched calibrations were used for analyte quantitation with determination coefficients (R(2) ) ≥ 0.9931. The recovery rates for aminopyrine and antipyrine in various matrices at two spiking levels (5 and 10 ng/g) fell in the range of 60.96-68.87 and 61.87-66.99%, respectively. Meanwhile, the intra- and inter-day precisions (expressed as relative standard deviation) were 1.02-12.95 and 1.71-5.50%, respectively. The method's detection limit (1 ng/g) was very low, thus enabling the detection of low residue levels. The applicability of the developed method was demonstrated with actual market samples and none of the tested analytes was detected in any of the samples.


Asunto(s)
Aminopirina/análisis , Antipirina/análisis , Cromatografía Liquida , Huevos/análisis , Análisis de los Alimentos/métodos , Leche/química , Músculos/química , Espectrometría de Masas en Tándem , Aminopirina/metabolismo , Animales , Antipirina/metabolismo , Límite de Detección , Estructura Molecular , Porcinos
11.
Z Gastroenterol ; 53(1): 21-7, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25594703

RESUMEN

BACKGROUND: Liver function and tumor staging are essential parameters for selection of treatment modalities in patients with hepatocellular carcinoma (HCC). Transarterial chemoembolization (TACE) is associated with a risk of deterioration of liver function. In clinical routine hepatic function in patients with liver cirrhosis is assessed by the Child-Pugh-classification. Dynamic breath tests allow the assessment of the hepatic functional mass and have the potential to give more accurate information on hepatic function periinterventionally. PATIENTS AND METHODS: A prospective clinical study was performed in 13 patients receiving a total of 18 TACE sessions. (13)C-aminopyrine breath test was performed the day before TACE, 2 days and 30 days after TACE and correlated with standard laboratory work-up of the patients. RESULTS: Fourteen TACE sessions were performed in Child A liver cirrhosis, 4 in Child B cirrhosis. All patients presented with impaired aminopyrine metabolism at baseline. No significant changes in the (13)C aminopyrine breath test following TACE were observed. Two patients treated in Child A cirrhosis decompensated to Child B, one of them recovered. No further decompensation was observed in patients treated in Child B cirrhosis. DISCUSSION AND CONCLUSION: Liver function assessment with (13)C-aminopyrine breath test and Child-Pugh-classification following TACE was discordant in a large proportion of patients. Whether a quantification of mitochondrial liver function in patients planned to undergo locoregional treatment of HCC in liver cirrhosis is helpful in the prediction of postprocedural liver decompensation needs to be addressed in larger prospective clinical trials.


Asunto(s)
Carcinoma Hepatocelular/patología , Carcinoma Hepatocelular/terapia , Quimioembolización Terapéutica/métodos , Pruebas de Función Hepática/métodos , Neoplasias Hepáticas/patología , Neoplasias Hepáticas/terapia , Anciano , Aminopirina/farmacocinética , Pruebas Respiratorias/métodos , Radioisótopos de Carbono/farmacocinética , Carcinoma Hepatocelular/metabolismo , Sistema Enzimático del Citocromo P-450/metabolismo , Monitoreo de Drogas/métodos , Femenino , Humanos , Neoplasias Hepáticas/metabolismo , Masculino , Estadificación de Neoplasias , Pronóstico , Reproducibilidad de los Resultados , Sensibilidad y Especificidad , Resultado del Tratamiento
12.
Liver Int ; 34(4): 487-94, 2014 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-24428683

RESUMEN

As liver diseases are a major health problem and especially the incidence of metabolic liver diseases like non-alcoholic fatty liver disease (NAFLD) is rising, the demand for non-invasive tests is growing to replace liver biopsy. Non-invasive tests such as carbon-labelled breath tests can provide a valuable contribution to the evaluation of metabolic liver function. This review aims to critically appraise the value of the (13) C-labelled microsomal breath tests for the evaluation of metabolic liver function, and to discuss the role of cytochrome P450 enzymes in the metabolism of the different probe drugs, especially of aminopyrine. Although a number of different probe drugs have been used in breath tests, the perfect drug to assess the functional metabolic capacity of the liver has not been found. Data suggest that both the (13) C(2) -aminopyrine and the (13) C-methacetin breath test can play a role in assessing the capacity of the microsomal liver function and may be useful in the follow-up of patients with chronic liver diseases. Furthermore, CYP2C19 seems to be an important enzyme in the N-demethylation of aminopyrine, and polymorphisms in this gene may influence breath test values, which should be kept in mind when performing the (13) C(2) -aminopyrine breath test in clinical practice.


Asunto(s)
Aminopirina/metabolismo , Pruebas Respiratorias/métodos , Isótopos de Carbono/análisis , Hepatopatías/diagnóstico , Hepatopatías/metabolismo , Microsomas Hepáticos/metabolismo , Acetamidas/metabolismo , Aminopirina/química , Hidrocarburo de Aril Hidroxilasas/metabolismo , Cafeína , Citocromo P-450 CYP2C19 , Sistema Enzimático del Citocromo P-450/metabolismo , Humanos , Marcaje Isotópico , Estructura Molecular
13.
J Clin Gastroenterol ; 48(1): 59-65, 2014 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-24335903

RESUMEN

GOALS: We investigated the utility of liver function breath tests [C-Aminopyrine Breath Test (C-ABT), C-Galactose Breath Test (C-GBT)], for the diagnosis of nonalcoholic steatohepatitis (NASH) among nonalcoholic fatty liver disease (NAFLD) patients. BACKGROUND: Liver biopsy is currently the gold standard for the differentiation between simple fatty liver (NAFL) and NASH in NAFLD patients. MATERIALS AND METHODS: Thirty-six patients with histologically proven NAFLD (NAFL:16, NASH:20) underwent C-ABT and C-GBT. The results were expressed as the percentage of administered C dose recovered per hour (%dose/h) and as cumulative percentage of administered C dose recovered over time (%cumulative dose). Histologic lesions were scored according to Brunt and Kleiner's classifications. RESULTS: C-ABT results correlated inversely with activity grade (r=-0.650, P=0.001), NAFLD activity score (r=-0.473, P=0.026), and fibrosis stage (r=-0.719, P=0.001). Compared with NAFL, NASH patients had significantly lower %dose/h and %cumulative dose at 60, 90, and 120 minutes (always P<0.04) by C-ABT. C-ABT %dose/h and %cumulative dose at 120 minutes could predict the presence of NASH (area under the receiver operating characteristic curve: 0.762 and 0.741, respectively). In contrast, there was no significant association between C-GBT results and any patient characteristic. CONCLUSIONS: In the NAFLD patients, decreased and delayed liver microsomal function, as assessed by C-ABT, is associated with more severe necroinflammation and fibrosis, whereas C-ABT results at 120 minutes may be helpful for the diagnosis of NASH.


Asunto(s)
Pruebas Respiratorias/métodos , Hígado Graso/diagnóstico , Pruebas de Función Hepática/métodos , Adulto , Anciano , Aminopirina/análisis , Isótopos de Carbono , Estudios Transversales , Hígado Graso/fisiopatología , Femenino , Galactosa/análisis , Humanos , Masculino , Persona de Mediana Edad , Enfermedad del Hígado Graso no Alcohólico , Curva ROC , Índice de Severidad de la Enfermedad , Factores de Tiempo
14.
Xenobiotica ; 44(7): 666-76, 2014 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-24779638

RESUMEN

1. It is inevitable that during some xenobiotic biotransformation studies, a certain metabolite or degradation product arises of which the identity is uncertain, the route of formation is ambiguous, or it is just a plain mystery. 2. The following communication draws attention to three drugs reported in the literature, chlorphentermine, phenothiazine and aminopyrine, where after many years of investigation there still exists uncertainty over some of their metabolites. Noticeably, these three examples probably involve (potential) interaction of a nitrogen centre within the drug molecule. 3. It is hoped that the resurrection and assemblage of these data will offer interesting reading and that these examples may prove sufficiently intriguing to motivate further exploration and some resolution of these lingering concerns.


Asunto(s)
Aminopirina/farmacocinética , Clorfentermina/farmacocinética , Fenotiazinas/farmacocinética , Aminopirina/metabolismo , Animales , Clorfentermina/metabolismo , Humanos , Inactivación Metabólica , Nitrógeno/química , Fenotiazinas/metabolismo , Xenobióticos/metabolismo , Xenobióticos/farmacocinética
15.
Fa Yi Xue Za Zhi ; 30(3): 188-90, 2014 Jun.
Artículo en Zh | MEDLINE | ID: mdl-25272873

RESUMEN

OBJECTIVE: To study DNA quantification and STR typing of samples pre-treated with pyramidon. METHODS: The blood samples of ten unrelated individuals were anticoagulated in EDTA. The blood stains were made on the filter paper. The experimental groups were divided into six groups in accordance with the storage time, 30 min, 1 h, 3 h, 6 h, 12 h and 24h after pre-treated with pyramidon. DNA was extracted by three methods: magnetic bead-based extraction, QIAcube DNA purification method and Chelex-100 method. The quantification of DNA was made by fluorescent quantitative PCR. STR typing was detected by PCR-STR fluorescent technology. RESULTS: In the same DNA extraction method, the sample DNA decreased gradually with times after pre-treatment with pyramidon. In the same storage time, the DNA quantification in different extraction methods had significant differences. Sixteen loci DNA typing were detected in 90.56% of samples. CONCLUSION: Pyramidon pre-treatment could cause DNA degradation, but effective STR typing can be achieved within 24 h. The magnetic bead-based extraction is the best method for STR profiling and DNA extraction.


Asunto(s)
Aminopirina/farmacología , ADN/aislamiento & purificación , Manchas de Sangre , Dermatoglifia del ADN , Medicina Legal , Humanos , Reacción en Cadena de la Polimerasa , Reproducibilidad de los Resultados , Manejo de Especímenes
16.
Dig Dis Sci ; 58(10): 3024-8, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-23817924

RESUMEN

BACKGROUND: (13)C-Aminopyrine breath test ((13)C-ABT) is a non-invasive, dynamic, quantitative liver function test, and the model for end-stage liver disease (MELD) is a recognised biochemical score used to predict survival in patients with cirrhosis. AIMS: The purpose of this study was to evaluate the relationship between the (13)C-ABT and MELD score in a cohort of cirrhotic patients and, moreover, to assess the prognostic value of (13)C-ABT results in the same group of patients. PATIENTS AND METHODS: Forty-six patients with cirrhosis and without hepatocellular carcinoma who underwent (13)C-ABT and who had at least 1-year follow-up were prospectively included in this study. MELD score was calculated at entry into the study in all patients. End-points of the study were 1-year liver-related death or liver transplantation. RESULTS: (13)C-ABT %dose/h at 30 min (%dose/h30) results showed significant, inverse correlation with MELD scores (r = -0.414, P = 0.004). During 1-year follow-up nine patients died (19.6 %) and two were transplanted (4.3 %). Median (13)C-ABT %dose/h30 results (3.2 vs. 1.8) were significantly higher in patients who survived as compared to those who died or underwent transplantation (P = 0.04). Receiver operating characteristics curves showed that a (13)C-ABT %dose/h30 cut-off of 2.0 had the best accuracy (c-index = 0.717) in assessing 1-year prognosis. CONCLUSIONS: We observed a correlation between a flow-independent quantitative liver function test and the MELD score, and found that the (13)C-ABT may accurately provide long-term prognostic information in cirrhotic patients.


Asunto(s)
Aminopirina , Pruebas Respiratorias/métodos , Enfermedad Hepática en Estado Terminal/fisiopatología , Cirrosis Hepática/diagnóstico , Cirrosis Hepática/mortalidad , Pruebas de Función Hepática/métodos , Aminopirina/metabolismo , Isótopos de Carbono , Estudios de Cohortes , Femenino , Estudios de Seguimiento , Humanos , Estimación de Kaplan-Meier , Cirrosis Hepática/cirugía , Trasplante de Hígado , Masculino , Persona de Mediana Edad , Valor Predictivo de las Pruebas , Pronóstico , Estudios Prospectivos , Curva ROC , Tasa de Supervivencia
17.
Ann Hepatol ; 13(1): 91-7, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-24378271

RESUMEN

BACKGROUND. In the management of chronic hepatitis C (CHC) patients, liver biopsy is the gold standard for liver fibrosis assessment despite some technical limits and risks. Non-invasive approaches have been proposed as alternative methods to evaluate structural liver damage. AIM. To investigate the diagnostic accuracy of transient elastography, 13C-aminopyrine breath test (13C-ABT), serum hyaluronic acid (HA) and cytokeratin 18 Asp396 fragment (CK-18) as non-invasive methods of liver fibrosis assessment ad their correlation to METAVIR score. MATERIAL AND METHODS. In a cohort of 57 CHC patients, liver stiffness, cumulative percentage of administered dose of 13C-aminopyrine at 120 min, serum HA and serum CK-18 concentration were determined. Diagnostic accuracy in detecting significant fibrosis (F ≥ 2), severe fibrosis (F ≥ 3) and cirrhosis (F = 4) was assessed by the area under the receiver operating characteristic curve. RESULTS. Liver fibrosis score showed a strong correlation with liver stiffness (r = 0.667; p < 0.0001) and a significant inverse correlation with 13C-ABT results (r = -0.418; p = 0.0012). A weaker correlation was found with CK18 (r = 0.329; p = 0.0126) and no correlation with HA. Areas under the curve of elastography, 13C-ABT, HA and CK18 were: 0.98, 0.75, 0.69, 0.64, respectively, for F ≥ 2; 0.97, 0.69, 0.80, 0.66, respectively, for F ≥ 3; 0.95, 0.64, 0.70, 0.56, respectively, for F = 4. CONCLUSION. Elastography has the best diagnostic accuracy for the assessment of the degree of liver fibrosis in CHC patients. Its application can provide an alternative useful tool for monitoring the disease evolution.


Asunto(s)
Diagnóstico por Imagen de Elasticidad/métodos , Hepatitis C Crónica/complicaciones , Cirrosis Hepática/diagnóstico , Hígado/diagnóstico por imagen , Adulto , Anciano , Aminopirina , Pruebas Respiratorias/métodos , Isótopos de Carbono , Estudios de Cohortes , Femenino , Humanos , Ácido Hialurónico/sangre , Queratina-18/sangre , Cirrosis Hepática/sangre , Cirrosis Hepática/etiología , Masculino , Persona de Mediana Edad , Curva ROC
18.
Yao Xue Xue Bao ; 48(1): 94-7, 2013 Jan.
Artículo en Zh | MEDLINE | ID: mdl-23600148

RESUMEN

This paper reports the establishment of a method for rapid identification 15 effective components of anti common cold medicine (paracetamol, aminophenazone, pseudoephedrine hydrochloride, methylephedrine hydrochloride, caffeine, amantadine hydrochloride, phenazone, guaifenesin, chlorphenamine maleate, dextromethorphen hydrobromide, diphenhydramine hydrochloride, promethazine hydrochloride, propyphenazone, benorilate and diclofenac sodium) with MRM by LC-MS/MS. The samples were extracted by methanol and were separated from a Altantis T3 column within 15 min with a gradient of acetonitrile-ammonium acetate (containing 0.25% glacial acetic acid), a tandem quadrupole mass spectrometer equipped with electrospray ionization source (ESI) was used in positive ion mode, and multiple reaction monitoring (MRM) was performed for qualitative analysis of these compounds. The minimum detectable quantity were 0.33-2.5 microg x kg(-1) of the 15 compounds. The method is simple, accurate and with good reproducibility for rapid identification many components in the same chromatographic condition, and provides a reference for qualitative analysis illegally added chemicals in anti common cold medicine.


Asunto(s)
Antiinflamatorios no Esteroideos/análisis , Antipiréticos/análisis , Acetaminofén/análisis , Acetanilidas/análisis , Amantadina/análisis , Aminopirina/análisis , Antipirina/análogos & derivados , Antipirina/análisis , Cafeína/análisis , Clorfeniramina/análisis , Cromatografía Liquida , Diclofenaco/análisis , Difenhidramina/análisis , Contaminación de Medicamentos , Estabilidad de Medicamentos , Efedrina/análogos & derivados , Efedrina/análisis , Guaifenesina/análisis , Prometazina/análisis , Seudoefedrina/análisis , Reproducibilidad de los Resultados , Salicilatos/análisis , Espectrometría de Masa por Ionización de Electrospray , Espectrometría de Masas en Tándem
19.
Vestn Otorinolaringol ; (6): 76-8, 2013.
Artículo en Ruso | MEDLINE | ID: mdl-24429865

RESUMEN

The objective of the present work was to study in vitro antimicrobial activity of the Candibiotic, ear drops used for the combined treatment of acute external ear otitis and acute otitis media Their anesthetic and anti-inflammatory action was compared with the effects of Otipax, and Anauran ear drops. The results of the study give a reason to recommend the application of Candibiotic ear drops as the highly effective medication for the endo-aural treatment of acute external ear otitis and acute otitis media.


Asunto(s)
Aminopirina/administración & dosificación , Antibacterianos/administración & dosificación , Lidocaína/administración & dosificación , Otitis Externa/tratamiento farmacológico , Otitis Media/tratamiento farmacológico , Enfermedad Aguda , Administración Tópica , Adolescente , Adulto , Anciano , Niño , Combinación de Medicamentos , Quimioterapia Combinada , Femenino , Humanos , Masculino , Persona de Mediana Edad , Resultado del Tratamiento , Adulto Joven
20.
Anal Methods ; 15(4): 529-536, 2023 01 26.
Artículo en Inglés | MEDLINE | ID: mdl-36628955

RESUMEN

With the popularity of herbal tea in China, many food fraudsters have added illegal drugs to herbal tea to enhance its functions, among which aminopyrine is widely abused as an antipyretic and analgesic. Presently, there is no immunoassays for aminopyrine, and it is difficult to achieve real-time detection in the field. Based on a polyclonal antibody of aminopyrine with high specificity and sensitivity, an optimal combination of coating antigen/antibody was obtained by screening different coating antigens. On this basis, a sensitive ic-ELISA method was established to detect aminopyrine in herbal tea. The detection limit of the ic-ELISA was 0.18 ng mL-1, which was much lower than the 100 ng mL-1 required as a standard. The method had good consistency with LC-MS in the detection of actual samples and could be used as a reliable method for the detection of aminopyrine in herbal tea.


Asunto(s)
Tés de Hierbas , Aminopirina , Inmunoensayo/métodos , Ensayo de Inmunoadsorción Enzimática/métodos , Anticuerpos
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