新麻醉药静松灵生物转化的研究

静松灵[2-(2,4-二甲基苯胺基)-4,5-二氢噻唑,XT]是国内合成的麻醉物,经ip给药后,从大鼠尿中分离、纯化、鉴定了四个代谢产物。MB₁即XT原形;MB₃及MA₂互为异构体,分别为2位、4位甲基氧化为羧基的产物;MA₁则4位甲基氧化为羧基,二氢噻唑环中4¹位亚甲基氧化为羰基。初步实验表明:代谢产物MB₃,MA²,MA₁的药效与毒性均远低于原形药,大鼠与小鼠对XT的转化机制相近,但也存在种属的差异。     

Are single fractions of radiotherapy suitable for plantar fasciitis?

The use of radiotherapy for plantar fasciitis has never been reported in Australasia and is scarcely found in the English language medical literature, but it is commonly used in Europe, especially in Germany. In Europe, treatment courses consisting of multiple small fractions have been associated with high levels of pain relief. In the present report, the use of single fractions or radiotherapy was evaluated by reviewing seven consecutive patients referred for treatment and by applying objective and subjective criteria for pain relief. One patient died of unrelated causes soon after treatment and one declined to receive radiotherapy. Four patients each received a single dose of 8 Gy resulting in complete pain relief. One patient was treated with 8 Gy and 12 weeks later was retreated achieving partial pain relief. A follow‐up interview was conducted after a mean of 15.6 months, ranging from 1.5 to 30 months. No acute or late effects occurred; however, the possibility that delayed effects may yet occur, particularly carcinogenesis, cannot be excluded. Radiotherapy for this common condition should be investigated further as it might be safer and more effective than other methods currently in use.     

Meniscal injuries: detection using MR imaging

Both retrospective and blinded analyses of thin-section, high-resolution magnetic resonance (MR) images of the knee joint, produced using a solenoid surface coil, indicate that MR imaging is an effective technique for evaluating meniscal injuries. Images of 49 patients were evaluated, and the results were correlated with those of subsequent arthroscopy. A grading scale was developed to rate the index of suspicion of a meniscal tear based on the MR images. Overall, approximately 80% of menisci rated grade 4 (definite tear) or 3 (probable tear) were found to have corresponding tears at arthroscopy. In many other patients with a grade 4 or 3 meniscus in whom a corresponding tear was not found arthroscopically, meniscal tears at other sites or other abnormalities were correctly diagnosed using MR. A majority of the false-positive MR images involved the posterior horns of the menisci, the sites of most false-negative arthroscopic diagnoses. The predictive value of a negative MR image was almost 100%. Even in patients with moderate-to-large effusions, the menisci were accurately evaluated. The results imply that MR imaging is useful in the preoperative evaluation of suspected meniscal tears.     

Breast cancer detection: one versus two views

Mammographic examinations of 169 patients with 172 biopsy-proved carcinomas, and of 194 healthy subjects, were interpreted independently and retrospectively by three experienced mammographers, initially as single-view oblique examinations and 6 months later as two-view oblique-cephalocaudal examinations. For the single-view examinations of the cancer patients, 67% of the cancers were correctly recommended for biopsy, additional views were requested for 23%, and a "negative" interpretation was made for 10%. For the single-view examinations of healthy subjects, biopsy was recommended for 7% and additional views were recommended for 32%. For the two-view examinations of women with cancer, 80% of the cancers were correctly recommended for biopsy, additional views were requested for 4%, and a "negative" interpretation was made for 16%. For two-view examinations of healthy subjects, biopsy was recommended for 7% and additional views were requested for only 5%. The authors conclude that single-view screening should not be performed, because it would lead to an excessive number of "call-back" examinations of healthy patients, producing additional cost and anxiety that would outweigh any theoretical benefit.     

Valnoctamide as a valproate substitute with low teratogenic potential in mania: a double‐blind,controlled, add‐on clinical trial

Bersudsky Y, Applebaum J, Gaiduk Y, Sharony L, Mishory A, Podberezsky A, Agam G, Belmaker RH. Valnoctamide as a valproate substitute with low teratogenic potential in mania: a double‐blind, controlled, add‐on clinical trial.
Bipolar Disord 2010: 12: 376–382. © 2010 The Authors. Journal compilation © 2010 John Wiley & Sons A/S. Objectives: Valproic acid’s well‐known teratogenicity limits its use in women of childbearing age. Valnoctamide is an analog of valproate that does not undergo biotransformation to the corresponding free acid. In mice, valnoctamide has been shown to be distinctly less teratogenic than valproate. Valnoctamide is an anticonvulsant, and we hypothesized that valnoctamide is antimanic. Methods: We performed a double‐blind, five‐week, add‐on, controlled trial of valnoctamide in mania. Patients were treated with risperidone at doses of the physician’s discretion. Valnoctamide or placebo was begun at doses of 600 mg/day and increased to 1200 mg after four days. Weekly ratings by a psychiatrist blind to the study drug were conducted using the Brief Psychiatric Rating Scale (BPRS), the Young Mania Rating Scale (YMRS), and the Clinical Global Impression (CGI). Results: Fifteen valnoctamide patients and 17 placebo patients completed at least one post‐baseline week and were included in data analysis. In all efficacy measures valnoctamide was more effective than placebo as an add‐on to risperidone, using two‐way analysis of variance (ANOVA) with time as the within‐subject factor. Two‐way ANOVA showed a significant effect of time (p < 0.001) and significant interaction between treatment and time (YMRS: p = 0.012; BPRS: p = 0.007; CGI: p = 0.003). Differences between valnoctamide and placebo were significant from week 3 to week 5. Conclusion: Valnoctamide could be an important valproate substitute for women of childbearing age with bipolar disorder who may become pregnant.     

Perinatal outcomes in inflammatory bowel disease

Objective: To determine whether inflammatory bowel disease (IBD) is associated with increased risk for adverse perinatal outcome.

Methods: A case–control study of 116 singleton pregnancies with IBD compared to 56?398 singleton controls delivered between 1986 and 2001.

Results: Patients with IBD were slightly older (32.8 vs. 30.6 years, p <?0.001), more likely to be Caucasian or Asian than Black or Latino (92% vs. 57%, p <?0.001) and have private health insurance (33% vs. 3%, p <?0.001). IBD was associated with an increased risk for labor induction (32% vs. 24%, p?=?0.002), chorioamnionitis (7% vs. 3%, p?=?0.04) and Cesarean section (32% vs. 22%, p?=?0.007), but there were no differences in neonatal outcomes. Subgroup analysis demonstrated an increased risk for low birth weight (LBW) in the ulcerative colitis group vs. the Crohn's disease group (19% vs. 0%, p?=?0.002). Patients with prior surgery for IBD had a lower incidence of LBW (0% vs. 12%, p?=?0.03). Flares during pregnancy were associated with an increased risk for preterm delivery (27% vs. 8%, p?=?0.02) and LBW (32% vs. 3%, p?=?0.003).

Conclusion: IBD was an independent risk factor for Cesarean section but there was no increase in adverse perinatal outcome. Crohn's disease, prior IBD surgery and quiescent disease were associated with a lower risk for LBW.