Activities of Proscillaridin A in Thoracic Duct Lymph after Single Oral Doses in Man

Abstract In order to study the possibility that orally administered proscillaridin after absorption is transported by the lymph to the systemic circulation, the concentrations of the glycoside in thoracic duct lymph were analyzed in two patients with thoracic duct drainage. They received the drug as a single oral dose; plasma and lymph concentrations were measured by ⁸⁰Rb-technique. Lymph was collected at various intervals for 24 hrs. The proscillaridin activity in thoracic duct lymph was low and followed closely that in the plasma. During the sampling period, a total of 300 ng and 240 ng, respectively, was recovered in the lymph, corresponding to less than 0.03 %₀ of the administered dose. The results indicate that proscillaridin is not transported by the thoracic duct lymph.     

Withdrawal-like signs induced by a single administration of ethanol in mice that differ in ethanol sensitivity

These experiments studied changes produced by a hypnotic dose of ethanol in the LS and SS lines of mice, which differ in ethanol sensitivity. In the first experiment, animals were injected either with ethanol or saline, and activity and seizure susceptibility measured 7–9 h later when blood levels of ethanol would have reached zero. Ethanol-treated mice of both genetic lines were less active in an open field test and more susceptible to clonic convulsions induced by flurothyl than saline-injected controls. There was no difference in the magnitude of these changes in the two lines. In the control condition SS (short-sleep) mice were more active than LS (long-sleep) mice, and more susceptible than LS mice to myoclonic but not to clonic seizures. The effect of the ethanol injection on body temperature was evaluated in separate groups of animals. LS mice showed a more pronounced hypothermia than LS mice when temperature was measured 2 h after injection. Six hours after injection, SS mice exhibited a small but statistically significant overshoot in temperature, after which they again became hypothermic with respect to controls; hyperthermia was not observed in LS animals.     

Changes in the sensitivity to cholinomimetic drugs of smooth and cardiac muscle in the rat induced by subacute administration of di-isopropyl phosphorofluoridate

The effect of subacute administration to rats of di-isopropyl phosphorofluoridate (DFP) on the sensitivity of the cardiovascular system to carbachol and on the sensitivity of various isolated tissues to acetylcholine, methacholine and carbachol was investigated. Cholinesterase inhibition produced by DFP in the isolated tissues was also determined.In the cardiovascular experiments both the magnitude of responses and the slope of the dose-response curves for hypotension and bradycardia produced by carbachol in the anaesthetized rat were reduced in the DFP-treated group.In experiments with isolated tissuesfrom DFP-treated animals it was found that sensitivity to methacholine and acetylcholine increased in the bladder to a greater extent that in the atria or ileum. The sensitivity to carbachol decreased to a similar extent in all 3 tissues. Acetylcholinesterase and butyrylcholinesterase levels in the bladder were inhibited to a greater extent than in the other 2 tissues.The results show that the degree of enzyme inhibition produced by DFP in the tissues after subacute administration for 10 days does not correlate with the decrease in the sensitivity of the tissues to carbachol. It is suggested that the association between accumulation of transmitter and enzyme inhibition is a more important factor than the degree of enzyme inhibition itself in the development of subsensitivity to carbachol.The release of cholinergic transmitter from the electrically stimulated isolated rat bladder may also be impaired following subacute administration of DFP.     

622例外科病人抗菌药物使用调查分析

目的了解我院住院患者抗菌药物使用情况,为临床合理用药提供参考。方法抽取2004年1-6月间外科系统住院患者病历622份,将相关内容记入“抗菌药物使用调查表”并进行统计分析。结果抗菌药物使用率为86.5%.使用种类以头孢菌素类、青霉素类、喹诺酮类、硝基咪唑类和氨基糖苷类为主,给药途径以静脉注射占70.5%,DDDs排序列前3位分别为头孢曲松钠、甲硝唑和庆大霉素,大多数抗菌药的DUI≤1。结论抗菌药物使用基本合理,但存在着使用比例偏高,药敏试验率较低和不合理用药现象。     

Randomized trial comparing overnight preoperative fasting period Vs oral administration of apple juice at 06:00-06:30 am in pediatric orthopedic surgical patients

BACKGROUND: We aimed to evaluate the efficacy of clear liquids orally administered at 06:00-06:30 am on the morning of surgery to reduce prolonged preoperative fasting periods. METHODS: After obtaining informed parental consent, 100 children undergoing scheduled orthopedic surgical procedures, ASA I-II, were randomly allocated to two groups. In group 1, children underwent the typical overnight preoperative period and patients in group 2 received a commercial brand of apple juice (glucose 28 g in 250 ml) at 06:00-06:30 am on the day of surgery. Patients <3 years old received 15 ml.kg(-1) and older children 10 ml.kg(-1) to a maximum volume of 250 ml. All patients underwent overnight fasting for milk and solids. RESULTS: Fasting time was 4.8 +/- 2.1 h (ranging from 3 to 11 h) in the group receiving apple juice at 06:00-06:30 am and 13.2 +/- 3.3 h (ranging from 5 to 19 h) in the overnight-fasting group (P < 0.05; 95% CI: -9.6 to -7.4 h). More patients were irritable (odds ratio, OR 4.5; 95% CI: 1.9-10.8) and dehydrated (OR 21.6; 95% CI: 5.9-79.0) in the overnight-fasting group. Glucose levels <2.7 mmol.l(-1) (50 mg.dl(-1)) were not reported in any case. CONCLUSIONS: A 15 ml.kg(-1) of apple juice for patients of <3 years of age or 10 ml.kg(-1) for older children, at 06:00-06:30 am of the surgical morning is a simple procedure to prevent dehydration and to produce positive behavior in low-risk, pediatric surgical patients.     

Long-term intrathecal S(+)-ketamine in a patient with cancer-related neuropathic pain

Neuropathic pain sometimes needs invasive pain therapy. We presentthe case of a patient with cancer-related neuropathic pain untreatablewith conventional pain therapy after tumour-embolization. Thepatient was treated successfully with intrathecal (i.t.) administrationof S(+)-ketamine, in addition to morphine. Plasma concentrationsof S(+)-ketamine were measured regularly throughout the treatment.Continuous i.t. administration of S(+)-ketamine over a periodof 3 months demonstrated low plasma levels and no unwanted side-effects.     

A comparison of the discriminative stimulus properties of phencyclidine, given intraperitoneally or intraventricularly in rats

Rats trained to discriminate intraperitoneally injected phencyclidine (PCP) from saline in a two-lever operant procedure distributed most of their responses on the phencyclidine lever after administration of 150 or 300 μg of phencyclidine into a lateral ventricle. This demonstrated that the discriminative stimulus properties of phencyclidine were centrally mediated. On the other hand, the potency of phencyclidine was increased by no more than about 7-fold from intraperitoneal to intraventricular administration. This suggests that either periventricular sites are not involved in mediating the discriminative stimulus properties of phencyclidine or that absorption of phencyclidine to relevant sites in the brain is not markedly enhanced by intraventricular administration.     

Clinical studies of intrarectal administration of 5-FU emulsion as an adjunct to surgical treatment for rectal cancer

Preoperative intrarectal administration of 5-FU emulsion was attempted as an adjuvant chemotherapy to surgery for rectal cancer. The drug concentrations of resected specimens were determined and histological examinations of them were carried out in order to evaluate the effect of anticancer drugs on the metastatic lymph nodes as well as on the primary tumors. 5-FU levels both in the regional lymph nodes and primary tumors of 18 patients with rectal cancer, who were given with the 5-FU emulsion (emulsion group) or 5-FU suppository (suppository group) intrarectally two hours before surgery, was found to be much higher in emulsion group than in suppository group. 46 patients with rectal cancer were treated preoperatively with intrarectal administration of 5-FU emulsion (25 cases) or 5-FU suppositories (21 cases) for a period of 10 days before surgery, and the histological effect of this regimen on the metastatic lesion in the lymph nodes, as well as in the primary tumor was examined. No detectable difference was found in the primary lesions between the emulsion group and the suppository group. In the metastatic lesions, however, the rate of effectiveness was higher in the emulsion group than in the suppository (68 percent versus 33 percent).