Binding of aprindine and moxaprindine to human serum, α1-acid glycoprotein and serum of healthy and diseased humans

Summary A comparison was made between the binding of the anti-arrhythmic agents aprindine and moxaprindine to human serum, to human serum albumin (HSA), to ₁-acid glycoprotein (₁-AGP) and to a mixture of HSA and ₁-AGP. In serum from healthy volunteers (n=4) the binding of aprindine-HCl 5 µg/ml (13.8 µM) was 93.8% (SD±1.0), and that of moxaprindine-HCl 5 µg/ml (12.8 µM) was 94.1% (SD±1.1). Their binding to the mixture of ₁-AGP and albumin approximated their binding to serum. For ₁-AGP, the binding was similar for both compounds, whereas for HSA the binding of aprindine was more pronounced than that of moxaprindine: for both products the affinity coefficient for binding to ₁-AGP was about 100 times greater than that for binding to albumin. In serum from rheumatoid patients and from patients with renal failure a small but significant increase in binding of aprindine and moxaprindine was observed, approximately 1%. Increased and decreased binding was seen in serum from cirrhotic patients; for example, for aprindine the range in cirrhosis was 96.7%–79.8%, and the range in controls was 95.0%–92.4%. Free drug fraction and ₁-AGP concentration were inversely correlated. The results show that ₁-AGP plays an important role in the binding of aprindine and moxaprindine, and that alteration in the binding of the two compounds in disease states to a large extent can be explained by changes in serum ₁-AGP concentration.     

Plasma protein binding of prednisolone in normal volunteers and arthritic patients

Summary The plasma binding of prednisolone was studied in twenty normal volunteers and twenty rheumatoid arthritis patients. An in vitro assessment of the binding following the addition of prednisolone, prednisone, and hydrocortisone to the plasmas obtained from the subjects showed significant differences in the percentage of prednisolone bound. However, the differences observed were regarded as clinically insignificant. The plasma protein binding was determined by an in vitro equilibrium dialysis of the individual plasma samples at 37° C. Prednisolone levels on both sides of the dialysis membrane were determined using radioactivity and HPLC analytical methodologies. The percentages of prednisolone bound calculated from the analytical results of either the radiochemical or HPLC method were not significantly different. The change in the percentage of prednisolone bound to plasma proteins was studied as a function of the total prednisolone plasma concentration in a normal volunteer and in a systemic lupus erythematosis patient. As a result of prednisolone binding to both transcortin and albumin, the binding of prednisolone changes as a function of prednisolone concentration. The binding data were fitted using nonlinear least squares regression, and the affinity constants for the binding of prednisolone to transcortin and albumin were estimated.     

试论肾虚痹证(类风湿性关节炎)发育生物学基础

类风湿性关节炎 (ＲｈｅｕｍａｔｏｉｄＡｒｔｈｒｉｔｉｓ ,ＲＡ)是一种常见的以关节组织慢性炎症病变为主要表现的难治性自身免疫性疾病 ,属于中医痹证范畴。现代医学对其病因尚未阐明 ,中医学认为痹证的病因以风寒湿为外因 ,肾虚为内因。随着现代科学的不断发展 ,运用现代科学的研究成果阐释肾虚痹证的发病机理 ,对于认识和治疗ＲＡ ,促进中西医结合的发展都具有重要的理论和现实意义。1　肾虚是痹证发生的重要原因中医学认为 ,肾藏精 ,主骨生髓 ,只有当肾气充盛时 ,方能“筋骨坚” ,“筋骨劲强 ,肌肉满状”。若肾精亏虚 ,或先天不足 ,则…     

右酮洛芬氨丁三醇对佐剂性关节炎大鼠的治疗作用及胃肠道损伤作用的研究

目的　研究右酮洛芬氨丁三醇 (D KPT)对佐剂性关节炎大鼠的治疗作用及胃肠道损伤作用。方法　采用大鼠佐剂性关节炎模型 ,观察D KPT对佐剂性关节炎大鼠原发和继发性症状的作用以及对前列腺素E2 和胃、十二指肠的影响。结果　D KPT(2 5、5、10mg·kg-1)不仅能抑制佐剂性关节炎大鼠的原发性炎症 ,而且对继发性炎症和多发性关节炎有抑制作用。D KPT(10 -8、10 -7、10 -6 、10 -5、10 -4 mol·L-1)体外对佐剂性关节炎大鼠腹腔巨噬细胞产生过高的PGE2 有抑制作用。D KPT(10mg·kg-1)对胃、十二指肠黏膜有损伤作用 ,但损伤程度小于酮洛芬 (KP) (10mg·kg-1)。结论　D KPT对佐剂性关节炎大鼠有治疗作用 ,同时对胃、十二指肠损伤小于KP。     

2种疗效判断标准对洛索洛芬治疗类风湿关节炎的评价

目的 :国内、美国风湿病学会 (ACR) 2种疗效判断标准评价洛索洛芬 (loxoprofen)治疗类风湿关节炎 (RA)的疗效及不良反应。方法 :选择 5 0例 ,年龄 (4 8±s 13)a ,4 0～ 69aRA活动期病人 (男女不限 ) ,口服洛索洛芬 60mg ,tid× 4wk ,比较用药前后关节压痛数、关节肿胀数、血沉、C反应蛋白等临床及实验室指标的变化 ,用国内、ACR不同疗效判断标准评价洛索洛芬治疗RA的疗效及不良反应。结果 :洛索洛芬治疗RA的总有效率达 74 %(国内标准 )和 80 % (ACR标准 ) ,2种疗效判断标准无显著差异 ,各项临床及实验室指标均有显著改善 ,不良反应发生率 10 % ,未出现危及生命的不良反应。结论 :洛索洛芬治疗RA安全、有效     

Maternal and perinatal outcome in rheumatic heart disease.

OBJECTIVES: To study the maternal and perinatal outcome of pregnancies complicated by rheumatic heart disease. METHODS: A retrospective study was carried out in the cardio-obstetric clinic of the Postgraduate Institute of Medical Education and Research, Chandigarh (India) over a period of 13 years (1987-1999) involving 486 pregnant patients with rheumatic heart disease. Maternal and perinatal outcome was reviewed. RESULTS: Three hundred and four patients (63.3%) had single valve involvement and mitral stenosis was the most predominant lesion (89.2%). One hundred and seventy one (38.6%) patients had undergone surgical correction prior to the onset of pregnancy. One hundred and thirteen patients (22.6%) were identified as NYHA class III-IV. Mitral valvotomy was performed during pregnancy in 48 patients. The incidence of preterm birth and small for gestational age newborns was 12% and 18.2%, respectively. There were 10 maternal deaths, of which eight patients were NYHA III and IV. CONCLUSIONS: Rheumatic heart disease in pregnancy is associated with significant maternal and perinatal morbidity in NYHA class III-IV patients.     

Reiter's syndrome following intravesical BCG immunotherapy

A 71 year old woman developed conjunctivitis, asymmetrical oligoarthritis, and cystitis (Reiter's syndrome) secondary to intravesical BCG treatment for transitional cell carcinoma of the bladder. She received oral prednisolone, izoniazid, and pyridoxine and made a full recovery. Increasing use of BCG as immunotherapy will lead to an increase in the incidence of BCG associated reactive arthritis. Prompt recognition and early diagnosis will facilitate treatment and recovery.     

不确定风湿病患者人类白细胞抗原B27测定

目的调查临床诊断不确定风湿性疾病患者HLA—B27抗原的分布情况，探讨其在风湿性疾病中诊断及鉴别诊断的意义。方法采用标准NIH微量淋巴细胞毒实验方法对747例临床诊断不确定风湿性疾病患者做HLA—B27抗原检测。结果747例中，HLA—B27阳性196例，总阳性率26．24％。HLA—B27阳性者中16岁以下20例(男16例、女4例)，占10．21％；16～40岁162例(男126例，女36例)，占82．65％。大于40岁14例(男9例、女5例)，占7．14％。结论HLA-B27血清学检查对临床诊断不确定风湿性疾病的鉴别诊断具有重要意义．HLA—B27阳性提高了发现AS的可能性。对于诊断不确定的风湿病患者，HLA-B27可作为筛选指标。     

樱桃花青素对佐剂性关节炎大鼠自由基和炎症因子的影响

目的:观察樱桃花青素对佐剂性关节炎(AA)大鼠自由基和抗氧化功能以及炎症因子的影响.方法:将50只SD雄性大鼠随机分为5组即正常组、模型组、樱桃花青素高、中、低剂量组.对足爪肿胀进行测量,在光镜下观察各组组织形态学变化,用比色法检测了动物外周全血的谷胱甘肽过氧化物酶(GSH-PX)活性、血清超氧化物酶(SOD)活性、血清丙二醛(MDA)含量以及血清总抗氧化能力(T-AOC).用ELISA检测血清中TNF-α含量,用放射免疫法检测了足爪PGE2含量.结果:模型组和正常组相比GSH-PX,SOD活性和T-AOC能力下降,血清MDA含量升高,血清中TNF-α和足爪PGE2含量升高.樱桃花青素组能升高GSH-PX,SOD和T-AOC活力,降低血清MDA,TNF-α以及足爪PGE2含量.光镜下组织形态观察表明樱桃花青素各组能不同程度减轻滑膜增生,减少炎细胞浸润.结论:樱桃花青素能增强AA抗氧化能力,并能降低炎症细胞因子PGE2和TNF-α,从而减轻AA模型的关节炎损伤.     

Rheumatoid arthritis of the craniocervical region: assessment and characterization of inflammatory soft tissue proliferations with unenhanced and contrast-enhanced CT

The aim of this study was to depict and characterize inflammatory soft tissue proliferations caused by rheumatoid arthritis (RA) in the craniocervical region by unenhanced and contrast-enhanced CT. Computed tomography of the craniocervical region was performed in 35 patients in the axial plane before and after the i. v. administration of contrast material. According to the densities and contrast enhancement of the inflammatory soft tissue proliferations, four groups were classified. Ancillary findings, such as a compression of the dural sac or spinal cord, erosions of the bony structures, and atlantoaxial subluxation, were also evaluated. Inflammatory soft tissue proliferations were depicted in 28 of 35 patients and could be differentiated by unenhanced and contrast-enhanced CT according to the above defined criteria: effusion in 6 patients (17 %); hypervascular pannus in 8 (23 %); hypovascular pannus in 5 (14 %); and fibrous tissue in 9 patients (26 %). A compression of the dural sac was seen in 11 (31 %) patients; 3 of these had neurological symptoms. Erosions of the odontoid process were found in 20 (57 %) patients; 16 (80 %) of these also showed erosions of the atlas. Atlantoaxial subluxation was seen in 11 (31 %) patients. Inflammatory soft tissue proliferations in the craniocervical region caused by RA can be reliably demonstrated and classified by unenhanced and contrast-enhanced CT, which can differentiate between joint effusion and various forms of pannus and depict ancillary findings. Computed tomography is an alternative method for patients unable to undergo an MRI examination. Received: 4 October 1999; Revised: 7 March 2000; Accepted: 14 March 2000