Serum levels and urinary excretion of mequitazine after a single oral dose

Pharmacokinetics of mequitazine, a recently introduced peripheral H1-histamine receptor antagonist of phenothiazine type, was followed up to 72 h after the single oral dose of 5 mg of the drug to eight fasted healthy volunteers. Each subject was treated thrice with a dosing interval of 15 days or more. Thus all the results were triplicated. Serum mequitazine was measured by mass fragmentography using a gas-liquid chromatograph/mass spectrometer set in the electron impact mode. Urine phenothiazines were determined fluorometrically before and after cleaving phenothiazines from their glucuronide conjugates. Peak concentration of mequitazine in serum was 3.19 +/- 1.70 (s.d.) ng.ml-1, time to peak concentration 5.67 +/- 1.68 h, elimination half-life 45 +/- 26 h, and elimination rate constant 0.018 +/- 0.007 h-1. Only 10.9 +/- 3.3% of the dose appeared in urine in unconjugated plus the glucuronidated form during the first 72 h. About 46% of the urinary phenothiazines were glucuronide conjugates. The results suggested that after the oral administration only low mequitazine concentrations appeared in serum, most of the drug seemed to be deactivated by the extrarenal route, and the kinetic properties of the drug resembled those of several phenothiazines used for psychiatric therapy.     

Serum and urinary boron levels in rats after single administration of sodium tetraborate

The pharmacokinetics of boron was studied in rats by administering a 1 ml oral dose of sodium tetraborate solution to several groups of rats (n=20) at eleven different dose levels ranging from 0 to 0.4 mg/100 g body weight as boron. Twenty-four-hour urine samples were collected after boron administration. After 24 h the average urinary recovery rate for this element was 99.6 ± 7.9. The relationship between boron dose and excretion was linear (r=0.999) with a regression coefficient of 0.954. This result suggests that the oral bioavailability (F) of boron was complete. Another group of rats (n=10) was given a single oral injection of 2 ml of sodium tetraborate solution containing 0.4 mg of boron/100 g body wt. The serum decay of boron was followed and found to be monophasic. The data were interpreted according to a one-compartment open model. The appropriate pharmacokinetic parameters were estimated as follows: absorption half-life, t _1/2a=0.608±0.432 h; elimination half-life, t _1/2=4.64±1.19 h; volume of distribution, Vd=142.0±30.2 ml/100 g body wt.; total clearance, C _tot=0.359 ± 0.0285 ml/min per 100 g body wt. The maximum boron concentration in serum after administration (C _max) was 2.13 ± 0.270 mg/l, and the time needed to reach this maximum concentration (T _max) was 1.76 ± 0.887 h. Our results suggest that orally administered boric acid is rapidly and completely absorbed from the gastrointestinal tract into the blood stream. Boric acid in the intravascular space does not have a strong affinity to serum proteins, and rapidly diffuses to the extravascular space in proportion to blood flow without massive accumulation or binding in tissues. The main route of boron excretion from the body is via glomerular filtration. It may be inferred that there is partial tubular resorption at low plasma levels. The animal model is proposed as a useful tool to approach the problem of environmental or industrial exposure to boron or in cases of accidental acute boron intoxication. Received: 1 December 1997 / Accepted: 24 March 1998     

Evaluation of cytokine serum levels in patients with plaque-type psoriasis

Psoriasis is a chronic debilitating cutaneous disorder that affects both sexes and appears clinically as inflamed, edematous skin lesions covered with a silvery white scale. Strong evidence suggests that immune mechanisms are implicated in its pathogenesis, such as persistent activation of T-lymphocytes, excessive proliferation of keratinocytes and reactivation of proto-oncogenes and other elements. Additionally, several recent studies have demonstrated that cytokines play a significant role in the pathogenesis of the disease, as they can be found in the affected skin of psoriatic patients. In this study we evaluated levels of circulating cytokines in the serum of 45 Greek psoriatic patients before initiation of treatment and compared the results with those in 45 healthy volunteers. According to our findings interleukin (IL)-2, IL-10, IL-12 and tumor necrosis factor-alpha (TNF-alpha) levels were statistically significantly elevated in the serum of psoriatic patients before therapy compared with those of controls. IL-6 serum levels did not differ between psoriatic patients and healthy volunteers. Conversely, interferon-gammaserum levels of psoriatic patients were statistically significantly lower than those of healthy volunteers.     

Serum lidocaine levels in patients undergoing fibrobronchoscopy

Serum lidocaine levels were determined in 29 patients undergoing fibrobronchoscopy after drug doses ranging from 180 to 400 mg. The results showed rapid absorption of the anaesthetic by the tracheobronchial mucosa with an average absorption constant of 4.77 +/- 1.99 h-1. Maximum lidocaine levels in serum averaged 1.21 +/- 0.64 microgram/ml, lower than the levels established as toxic for this anaesthetic. The serum half-life of lidocaine averaged 1.55 +/- 0.72 h. The percentage of dose absorbed in this kind of patient ranged between 20.89 and 60.88% of the dose administered.     

Serum levels of thioridazine in psychiatric patients and healthy volunteers

Summary The rate of absorption of thioridazine varied greatly in ten healthy volunteers who took 100 mg in the morning after an overnight fast. The peak level in blood was also variable and it was reached 1 1/4 to 4 h after dosing. Maximal concentrations in the blood varied widely from 0.13 µg/ml to 0.52 µg/ml. No relation was found between the weight or sex of the subjects and the pharmacokinetics of the drug. The serum half life of thioridazine in three healthy volunteers was 9, 10 and 10 h respectively. In a group of 22 patients receiving less than 5 mg/kg body weight a day, there was a strong correlation between the dose and the morning or evening concentration of thioridazine in the blood. A positive correlation was also observed between the age of the patient and the serum level in those who received doses of less than 5 mg/kg body weight.     

Some pharmacokinetic data on miocamycin. I: Serum, urinary and prostatic levels

The pharmacokinetics of miocamycin were studied in ten healthy male volunteers after three different administrations: the first group received 600 mg in a single oral dose; the second received 1200 mg divided into two administrations of 600 mg, each one every 12 h; the third received 1200 mg in a single oral dose. Prostatic levels of miocamycin were recorded after the administration of 1200 mg, divided into two administrations of 600 mg every 12 h. The pharmacokinetic analysis was carried out by applying a single-compartment kinetic model with zero-order absorption. The apparent duration of absorption (T) was about 0.55 h for all subjects. The area under the curve was 7.5767 +/- 0.2511 mg/h/l in the first group; 6.7333 +/- 0.6058 mg/h/l in the second group; and 18.6825 +/- 15.1555 mg/h/l in the third. The prostatic levels were five times higher than those in the serum at the same time.     

抗RA33抗体水平在类风湿关节炎和系统性红斑狼疮诊断中的意义

目的探讨抗RA33抗体水平在类风湿关节炎(RA)和系统性红斑狼疮(SLE)疾病诊断中的意义。方法采用定量ELISA双抗夹心法检测了140例RA患者、90例SLE患者、70例非SLE和非RA患者和40例正常人血清中抗RA33抗体的水平。结果SLE患者组与RA组抗RA33抗体水平分别为0～102.8U/ml和0～162.5U/ml,正常对照组为0～21.2U/ml。SLE患者组和RA患者组抗RA33抗体敏感性分别为21.1%(19/90)和34.3%(48/140),特异性分别为76.2%和86.9%。SLE患者组和RA患者组与正常对照组抗RA33抗体结果比较差异有显著性(P<0.01),SLE患者组血清抗RA33抗体结果与RA患者组比较差异有显著性(P<0.05)。结论抗RA33抗体检测在SLE和RA中具有良好的敏感性及特异性,可视为RA早期诊断新的血清学指标,抗RA33抗体阳性提示SLE患者已经有骨或关节的损害。     

Serum immunoglobulin levels in paediatric patients with pneumonia

OBJECTIVE: To determine levels of serum immunoglobulins IgG, IgM and IgA in patients admitted with pneumonia to Harare Central Hospital paediatric wards. DESIGN: A cross sectional pilot study. SETTING: Harare Central Hospital, Department of Immunology, University of Zimbabwe; Department of Paediatrics, University of Zimbabwe; Immunology Laboratory, University of Utrecht (The Netherlands). SUBJECTS: 71 paediatric patients. MAIN OUTCOME MEASURES: Immunoglobulin profiles for children with pneumonia. RESULTS: Of the 71 children tested, 43 had high IgG levels of between two and half and five times the upper end of the normal age-matched reference range. While the same 43 children with high IgG had similarly elevated levels of IgM, only 25 of them had elevated IgA levels. Of this group of 43 children with hypergammaglobulinaemia, all but one, had antibodies to human immunodeficiency virus (HIV), 50% of whom had detectable levels of p24 antigen in their sera. A small minority, 4% of the 71 patients, had very low levels of total immunogloblins. CONCLUSIONS: High levels of total immunoglobulins occur frequently in children with pneumonia and are associated with the presence of HIV 1/2 antibodies and also p24 antigen.     

Serum angiotensin-converting enzyme levels in patients with silicosis

In a group of control subjects, the mean serum angiotensin-converting enzyme (ACE) level was 38.1 +/- 10.6 nmol/min X ml (n = 30), and in a group of silicosis patients the mean serum ACE level was 45.2 +/- 16.0 (n = 26). Thirteen of these patients were classified as having nodular silicosis, and their mean serum ACE level was 44.2; 10 of these patients were classified as having progressive massive fibrosis, and their mean serum ACE level was 39.4. Three of these patients had confirmed silicotuberculosis, and their serum ACE levels were 63, 67, and 77 (mean = 69); these serum ACE levels are somewhat higher than those having been reported for patients with acute sarcoidosis. Thus, when serum ACE levels are being used to assist in distinguishing between silicosis and sarcoidosis, the possibility of silicotuberculosis must be also considered when high serum ACE levels are encountered.     

度洛西汀对抑郁症患者血清microRNA和细胞因子水平的影响

目的探讨度洛西汀对抑郁症患者血清microRNA和细胞因子水平的影响。方法选取某院收治的抑郁症患者50例(抑郁症组),同期健康查体人群50例(对照组),采用real-time PCR及ELISA法检测两组人群血清miR-132、miR-182及细胞因子IL-1、IL-6、TNF-α水平。抑郁症患者给予度洛西汀治疗8周,比较治疗前后患者血清miR-132、miR-182及细胞因子水平有无差异。同时评价患者临床疗效,并分析临床疗效与血清miR-132、miR-182及细胞因子的相关性。结果 50例患者完成了8周治疗,其中痊愈22例,显效16例,好转8例,无效4例,显效率(痊愈+显效)为76.0%。抑郁症组患者血清miR-132、miR-182、IL-1、IL-6和TNF-α均显著高于对照组,且差异具有统计学意义(P<0.05);抑郁症组治疗后血清miR-132、miR-182和细胞因子IL-1、IL-6、TNF-α均显著降低(P<0.05)。分别以治疗前血清miR-132、miR-182、 IL-1、IL-6和TNF-α为预测度洛西汀显效的敏感性分别为78.2%、71.6%、75.3%、68.4%和66.9%,特异性分别为69.5%、65.8%、60.7%、66.5%和70.3%。诊断的ROC曲线下面积分别为0.73、0.68、0.66、0.64和0.69。结论抑郁症患者血清miR-132、miR-182、IL-1、IL-6和TNF-α显著高于健康人群。给予度洛西汀治疗后上述指标显著降低,并可作为判断度洛西汀疗效的生物学指标。     

Elevated urinary nitrite and citrulline levels in patients with rheumatoid arthritis

The objective of this research was to determine, if NO production, as measured in the serum and urine, is increased in patients with rheumatoid arthritis. Forty-seven patients with RA were recruited in the study and subdivided into inactive and active disease (24 and 23 patients, respectively). Twenty-eight healthy individuals served as controls and nine patients with gastroenteritis were studied to validate the technique of measurement of NO production. Nitrite and citrulline were measured by spectrophotometry, as surrogate markers of NO production. It was found that serum nitrite and citrulline levels of patients with gastroenteritis were not significantly different from controls and the two subgroups of RA. Urine nitrite and citrulline levels were significantly higher in patients with gastroenteritis as compared to the two subgroups of RA and controls (p; > 0.001). Serum and urine nitrite levels of patients with active RA were higher than controls and patients with inactive disease (p > 0.05). Serum citrulline levels were not significantly different among the two subgroups of patients with RA. However, they were significantly higher in patients with active disease as compared with controls (p > 0.05). Urinary citrulline levels were significantly higher among patients with active disease as compared to controls and patients with inactive RA (p > 0.05). It is therefore suggested that urinary nitrite and citrulline levels can be useful for the measurement of NO production and are associated with active disease in patients with RA.     

恙虫病患者检测三种细胞因子的临床意义

目的 探讨恙虫病患者检测血清白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、粒细胞集落刺激因子( G-CSF)的临床意义.方法 采用ELISA方法检测恙虫病51例(观察组)治疗前后血清IL-6、TNF-α、G-CSF的浓度,并与健康体检者(对照组)比较分析.结果 与对照组比较,观察组治疗前IL-6、TNF-...     

Serum sulphydryl levels in rheumatoid patients treated with alclofenac

Summary

Serum sulphydryl levels, which are decreased in rheumatoid patients, are increased to near normal during treatment with alclofenac. The biochemical function of the sulphydryl group and its possible pathogenic significance in rheumatoid and other auto-immune diseases are discussed.     

Serum IgG subclasses levels in paediatric patients with pneumonia

OBJECTIVES: To determine the IgG subclass levels of patients admitted to Harare Central Hospital paediatric wards with pneumonia. DESIGN: A cross sectional study. SETTING: Harare Central Hospital, Departments of Immunology and Paediatrics, University of Zimbabwe; Department of Paediatric Immunology, University of Utrecht, The Netherlands. SUBJECTS: 56 paediatric patients. MAIN OUTCOME MEASURES: IgG subclass profiles of children with pneumonia. RESULTS: Of the 56 children tested, 40 (71%) had antibodies to human immunodeficiency virus (HIV). The levels of IgG1 and IgG3 subclasses were significantly higher in HIV antibody positive children (p < 0.001, p < 0.01 respectively) than in those without detectable HIV antibodies in their sera. There was no significant relationship between IgG subclass levels and the presence of HIV p24 antigen. Furthermore, age and gender also had no significant influence on the levels of IgG subclasses in this population. CONCLUSION: High levels of IgG1 and IgG3, but not IgG2 and IgG4, occur frequently in children with pneumonia and are associated with the presence of HIV antibodies.     

Serum sialic acid levels in lung cancer patients.

The levels of N-acetyl neuraminic acid (sialic acid) in normal men and pre-and post-menopausal women were determined. Smoking post-menopausal estrogen therapy, oral contraceptives, and refreezing had no effects on sialic acid levels. Pre-treatment values from patients with lung carcinoma showed markedly elevated levels of sialic acid (0.697 +/- 0.149 muM/ml) as compared to those from normal controls (0.432 +/- 0.067 muM/ml). The potential usefulness of sialic acid as a biological marker is discussed.     

Serum adiponectin levels in patients with pollen-induced allergic rhinitis

BACKGROUND: Several studies have outlined a possible relationship between an increased body mass index and respiratory allergic diseases, such as asthma and rhinitis. OBJECTIVE: The aim of the study was to evaluate the serum adiponectin levels in a cohort of patients with pollen-induced allergic rhinitis, enrolled outside the pollen season, and in a group of healthy controls. METHODS: The study included 41 patients with moderate-severe persistent allergic rhinitis due to a pollen allergy and 34 normal subjects. All subjects were prospectively and consecutively evaluated. A skin prick test and blood sampling for assessing serum adiponectin levels were performed in all subjects. RESULTS: The comparison between allergic patients and normal subjects, globally considered without gender distinction, showed slightly higher values in the allergic population. After analysing genders separately, allergic patients show significantly higher levels than normal males (p = 0.0134), whereas the comparison between allergic and normal females was not significant (p = 0.1419). In addition, in normal males adiponectin serum levels are significantly related with age (p = 0.0123). CONCLUSION: This preliminary study provides the first evidence of significantly higher adiponectin serum levels in male patients with pollen-induced allergic rhinitis as compared to normal male subjects.     

右美托咪定对肝叶切除患者围术期肝功能及血浆细胞因子水平的影响

目的分析右美托咪定对肝叶切除患者围术期肝功能及血浆细胞因子水平的影响,从而为临床治疗提供依据。方法选取2012年1月至2015年1月承德医学院附属医院和承德市宽城县医院行肝叶切除术患者80例为研究对象,分为观察组与对照组,每组40例,观察组注射右美托咪定1μg/kg,注射时间为10min,然后以0.5μg·kg-1·h-1持续输注,对照组注射等量0.9%氯化钠注射液。结果 2组患者肝门阻断时间、手术时间以及术中输血量差异无统计学意义(P>0.05);2组患者在T0期,丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)差异无统计学意义,随着时间的延长,2组ALT与AST均显著升高,但对照组升高更加明显,差异有统计学意义(P<0.05);2组患者在T0期,肿瘤坏死因子(TNF)-α和白细胞介素(IL)-10差异无统计学意义,随着时间的延长,2组TNF-α和IL-10均显著升高,但对照组升高更加明显,差异有统计学意义(P<0.05)。结论右美托咪定可以抑制肝功能损伤和细胞因子的释放,有利于降低缺血再灌注损伤。     

急性脑梗死患者血清中Hey、NSE的临床研究

目的 研究急性脑梗死（ACI）患者治疗前、后血清同型半胱氨酸（Hcy）和神经元特异性烯醇化酶（NSE）水平的变化与意义.方法 应用化学发光法和双抗体夹心ELISA法对120例ACI患者治疗前、后进行血清Hcy和NSE水平测定.结果 ACI患者治疗后血清Hcy（5.6±1.5）μmol/L,明显低于治疗前的（18.8±3.2）μmol/L及对照组的（7.5±1.5）μmol/L,比较差异有显著性（P＜0.05）; ACI患者治疗后血清NSE（7.04±2.1）μg/L,明显低于治疗前的（21.06±4.6）μg/L,比较差异有显著性（P＜0.05）.结论 检测ACI患者血清Hcy和NSE水平对判断病情和预后有重要价值.     

腹膜透析患者血清基质金属蛋白酶水平变化的意义

目的 了解维持性腹膜透析(CAPD)患者血清基质金属蛋白酶-10(MMP-10)、基质金属蛋白酶-8(MMP-8)、基质金属蛋白酶组织抑制剂-1(TIMP-1)的水平及可能临床意义。方法 选取住院CAPD及临床符合诊断慢性肾脏病(CKD)患者135例,分为CKD3、CKD4、CKD5期组和CAPD组,其中CAPD组68例;记录患者年龄、腹透龄等临床资料,收集并记录患者的血红蛋白(HB)、血清清蛋白(ALB)、血钙、血磷、甲状旁腺激素(PTH)、血肌酐等指标;血清MMP-10、MMP-8、TIMP-1检测采用酶联免疫吸附试验。结果 CAPD患者血清MMP-10、MMP-8、TIMP-1、血磷、钙磷乘积水平明显高于CKD3、4、5期患者,CAPD组血钙水平较CKD5期组高,差异有统计学意义(P<0.05);Spearman直线相关分析结果提示MMP-10与血磷、钙磷乘积呈正相关,与ALB呈负相关,MMP-8与血磷、hs-CRP、血沉、钙磷乘积呈正相关,TIMP-1与血磷呈正相关;上述3项指标均与血钙、年龄、PTH、腹透龄、血肌酐、HB不具有相关性。CAPD组中的高磷组MMP-10、MMP-8、TIMP-1水平较正常血磷组升高,钙磷乘积增高组较钙磷乘积正常组MMP-10、MMP-8、TIMP-1浓度高,但组间比较仅MMP-10水平差异有统计学意义。结论 CAPD患者血清 MMP-10、MMP-8、TIMP-1、血磷、钙磷乘积水平较透析前CKD患者明显升高;CAPD患者血清MMP-10、MMP-8、TIMP-1水平可能与钙磷代谢有关。