Dixyrazine premedication for cataract surgery. A comparison with diazepam

Peroral dixyrazine (15–30 mg, n = 50) and diazepam (4–10 mg, n = 50) were used as premedicants for geriatric patients having cataract surgery under regional block. Compared to the diazepam patients, a larger number of the dixyrazine medicated patients appeared anxious, and there was a statistically significant difference between the groups, when summing up changes in anxiety throughout the study period. The dixyrazine patients needed more frequent supplementation with intravenous sedative drugs, compared with their diazepam counterparts. Peroral dixyrazine is an applicable choice for calm patients, when only slight sedation, or avoidance of somnolence are required.     

Zuclopenthixol,melperone and haloperidol/levomepromazine in the elderly. Meta-analysis of two double-blind trials at 15 nursing homes in Norway

Summary

A meta-analysis was carried out of the data from two double-blind. multi-centre studies with identical methodology which compared the effectiveness of treatment of elderly patients with zuclopenthixol and with other antipsychotic drugs. In one study, patients were treated for 4 weeks with either zuclopenthixol or melperone; in the other, with either zuclopenthixol or a combination of haloperidol and levomepromazine. The meta-analysis evaluated the results of 96 patients, 49 in the zuclopenthixol group and 47 in the comparison group. Doses, which were adjusted to individual patient's needs, were low as shown by the percentages of defined daily doses for each of the study drugs. The results indicated that all three treatment alternatives were effective in the treatment of elderly patients with symptoms of agitation and hostility/aggressiveness. There was a trend, however, for zuclopenthixol to have a more rapid onset of effect. Zuclopenthixol also has the advantage for both patients and nursing stuff that dosage is once daily. Only few and mild side-effects were reported with the three drug regimens.     

N10‐carbonyl‐substituted phenothiazines inhibiting lipid peroxidation and associated nitric oxide consumption powerfully protect brain tissue against oxidative stress

During some investigations into the mechanism of nitric oxide consumption by brain preparations, several potent inhibitors of this process were identified. Subsequent tests revealed the compounds act by inhibiting lipid peroxidation, a trigger for a form of regulated cell death known as ferroptosis. A quantitative structure–activity study together with XED (eXtended Electron Distributions) field analysis allowed a qualitative understanding of the structure–activity relationships. A representative compound N‐(3,5‐dimethyl‐4H‐1,2,4‐triazol‐4‐yl)‐10H‐phenothiazine‐10‐carboxamide (DT‐PTZ‐C) was able to inhibit completely oxidative damage brought about by two different procedures in organotypic hippocampal slice cultures, displaying a 30‐ to 100‐fold higher potency than the standard vitamin E analogue, Trolox or edaravone. The compounds are novel, small, drug‐like molecules of potential therapeutic use in neurodegenerative disorders and other conditions associated with oxidative stress.     

吩噻嗪衍生物的式电位、驱虫活性与分子结构间关系

目的：研究吩噻嗪式电位与驱虫活性关系的分子结构基础。方法：AMI半经验量子化学方法计算分子结构参数，主因子和多元线性回归分析寻找相关性。结果：吩噻嗪的式电位与总电子能量，Et(e)，总分子能量，Et(M),总偶极矩，μt,和分子z轴方向的偶极矩，μz,线性相关，E^0=1.1369-0.00966Et(e)-0.00052Et(M)-0.07602μz-0.06396μt(R=0.9665,SD=0.0336).吩噻嗪的驱虫活性与环上电荷，e(r)，分子生成热，Hf,总偶极矩，μt，和在分子z方向的偶极矩，μz，线性相关，a=3.8343-0.8832μz 0.671μt 2.781e(r)-0.00154Hf(R=0.7404,SD=0.5338).偶极矩不仅影响吩噻嗪的式电位而且影响其驱虫活性，是两的共同因子。结论：偶极矩可能是吩噻嗪驱虫活性与其式电位相关的分子结构因素。     

Psychotropic drugs and epilepsy

Psychotropic drug use in epileptics requires special considerations, since many such drugs lower the seizure threshold. Stress associated with epilepsy often produces psychiatric problems, so that psychotropic drug therapy may be required. Side-effects of the anticonvulsant drugs themselves must also be considered, as must psychotropic-anticonvulsant interactions. Other seizure risk factors must be taken into account, but nevertheless psychotropic drug therapy should not be denied to the epileptic when it is specifically indicated. This paper outlines the precautions that need to be taken under such circumstances.     

CSF concentrations and clinical effects following intravenous dixyrazine premedication

Single concurrent plasma and lumbar spinal fluid samples were collected from twenty-two patients given IV dixyrazine 0.15 mg/kg, 10–106 min earlier in an open study.Dixyrazine penetrated rapidly into the spinal fluid; the CSF/P ratio was 0.3 by 10 min after drug administration and persisted at that level during the study period. The uncontrolled sedative and anxiolytic effects assessed by the patients were slight, and were correlated with the CSF drug concentrations only during the first 30 min after medication.     

Effect of Ca+ on the photobactericidal efficacy of methylene blue and toluidine blue against gram-negative bacteria and the dye affinity for lipopolysaccharides

BACKGROUND AND OBJECTIVES: Methylene blue (MB) and toluidine blue (TB) form metachromatic complexes with lipopolysaccharides (LPS). The greater photobactericidal efficacy of TB may be explained by its affinity for LPS. This study aims to elucidate the difference in photobactericidal efficacies between the dyes using Ca(2+) as a competitor for dye-binding sites on the bacterial outer membrane. STUDY DESIGN/MATERIALS AND METHODS: Fixed dye concentration solutions with gram-negative bacteria and increasing concentrations of CaCl(2) were exposed to red laser light. Bacterial survival and spectrophotometry were used to describe the effect of Ca(2+) on dye interaction with bacteria and LPS. RESULTS: MB-mediated photokilling was inhibited more significantly than that of TB. CaCl(2) inhibited dye photobleaching and suppressed the metachromatic reaction between the dyes and LPS, in particular TB. CONCLUSIONS: CaCl(2) inhibits bacterial photokilling by binding with LPS, as well as other anionic polymers including outer membrane proteins. LPS is chiefly involved in TB-mediated photokilling, whereas outer membrane proteins probably are more involved in MB-mediated photokilling.     

The Effect of Thioridazine and Promazine in Reducing the Potassium Loss from Isolated Perfused Rat Hearts

Electrically stimulated isolated rat hearts were perfused with a Ringer solution containing a low concentration of K⁺. At the end of a control period of 20 min. the cumulative K⁺ loss from the hearts was approximately 30 meq./kg dry weight. This value was used in each experiment as reference (100 per cent) for the total loss found after a subsequent additional test period of 30 min. The addition of promazine and thioridazine to the perfusate at the end of the control period reduced the further K⁺ loss. The values found in the different groups at the end of the test period were: Control group (10 hearts): 154 ± 11.6 per cent; with promazine 10^-5 M added (8 hearts): 103 ± 5.6 per cent; with promazine 2.5 × 10^-5 M added (10 hearts): 74 ± 10.5 per cent and with thioridazine 10^-5 M added (8 hearts): 110 ± 5.8 per cent. In another type of experiments, ouabain 1.5 × 10^-6 M was added at the end of the control period. This drug caused an increased K⁺ loss (181 ± 14.2 per cent) and ventricular fibrillation in 6 out of 8 hearts. Promazine 2.5 × 10^-5 M added before ouabain, prevented the development of fibrillation in another group of 7 hearts, and also markedly reduced the K⁺ loss. It is concluded that phenothiazines reduce the K⁺ permeability of the heart muscle membranes.     

酚噻嗪类药物对血清载脂蛋白、脂蛋白含量的影响

目的探讨长期（平均６年）接受酚噻嗪类药物治疗的慢性精神分裂症患者血清载脂蛋白含量变化及其危险因素。方法采用酶法及火箭免疫电泳法对１５１例精神分裂症患者和１００名健康人血清胆固醇（ＴＣ）、甘油三酯（ＴＧ）、高密度脂蛋白胆固醇（ＨＤＬＣ）、载脂蛋白ＡⅠ（ａｐｏＡⅠ）、载脂蛋白Ｂ（ａｐｏＢ）的水平进行了对比分析。结果精神分裂症患者ａｐｏＡＩ，ａｐｏＡＩ／ａｐｏＢ，ＨＤＬＣ含量均低于正常对照组（Ｐ＜０．０１），ＴＧ、ａｐｏＢ水平却高于正常对照组（Ｐ＜０．０１），而ＴＣ浓度与正常对照组之间差异无显著性（Ｐ＞０．０５）。结论长期服用酚噻嗪类药物的精神分裂症患者存在载脂蛋白代谢紊乱，在治疗精神分裂症的同时应及早采取相应的预防措施，并定期测定血载脂蛋白等有关指标