Pharmacodynamic Modeling for Change of Locomotor Activity by Methylphenidate in Rats

Purpose. The locomotive activity changes after intravenous (i.v.) administration of methylphenidate (MPD) in rats were pharmacodynamically analyzed. Methods. MPD concentration in plasma, MPD concentration and dopamine (DA) level in striatal dialysate collected by microdialysis method, and the locomotor activity after i.v. administration of MPD (2, 5 and 10 mg/kg doses) were used for the analysis. Results. The transport of MPD from plasma to the interstitial fluid in the brain could be expressed by the linear two-compartment model. The clockwise hysteresis between the MPD concentration and the DA level in the dialysate could be explained by the pharmacodynamic model considering Michaelis-Menten type reuptake process of the extracellular DA into the terminal of the dopaminergic nerve and its competitive inhibition by the extracellular MPD. The inhibition constant (K_i) of MPD for DA reuptake was estimated to be 41.3 ± 73.8 nM (mean ± SE), which was closely consistent with the in vitro value after correction with dialysis recovery. The relationship between DA level in dialysate and locomotor activity was expressed by the Emax model considering two contrary effects, hyperkinesia and stereotypy. The bi-phasic locomotor activity-time profiles after high dose of MPD could be represented by this model. Conclusions. The developed model made it possible to explain the tolerance in DA increase and the complicated locomotive change induced by MPD, and may be useful for other DA reuptake inhibitors, such as amphetamine and methamphetamine.     

茶色素对冠心病及高血压病病人血小板功能的影响

目的：探索茶色素对冠心病、高血压病病人血小板功能的影响。方法：冠心病病人３６例（男性２１例，女性１５例；年龄６４±ｓ４ａ）；高血压病病人３０例（男性１８例，女性１２例；年龄５８±８ａ）。采用茶色素２５０ｍｇ，ｐｏ，ｔｉｄ，３０ｄ为一个疗程。结果：治疗后ＴＸＢ２下降，６－ｋｅｔｏ－ＰＧＰ１α上升，ＴＸＢ２／６－ｋｅｔｏ－ＰＧＦ１α比值下降（Ｐ＜０．０１或Ｐ＜０．０５），ＧＭＰ－１４０下降（Ｐ＜０．０５），ＰａｇＴ，ＰａｄＴ下降（Ｐ＜０．０５）。结论：茶色素具有降低血小板表面活性作用，抑制血小板聚集和粘附，抗血栓形成，改善微循环，对冠心病和高血压病病人起到积极的防治作用。     

实验性大鼠液压分级颅脑损伤模型的建立与研究

用自制液压冲击颅脑损伤仪对大鼠的头部由轻到重的４种冲击力产生４级脑损伤。１级可以无明显病理生理变化；２～４级则随冲击力的加重病理生理变化亦加重。这些变化包括心率，呼吸，血压，颅内压，脑水份含量与伊文思蓝蓝染范围测定以及病理学的变化。     

Blood pressure lowering effect of the aqueous extract of the stem of Ipomoea acanthocarpa (convolvulaceae) in spontaneously and salt-loaded hypertensive rats

Spontaneously hypertensive (SHR) and salt-loaded hypertensive rats (SLHR) were submitted to a daily treatment by gavage of 2 mL/100 g body weight of the aqueous extract of the stem of Ipomoea acanthocarpa (30 mg/mL stock solution). A fall in blood pressure of nearly 13% was observed after two successive administrations of the aqueous extract. After 14 days of treatment, the blood pressure fell by more than 30±8%. The hypotensive effect might be due to a direct vascular smooth muscle effect or to its already observed high diuretic effects or might be acting by some other mechanism.     

BIOCHEMICAL CORRECTION IN THE SYNDROME OF HYPERTENSION AND HYPERKALAEMIA BY SEVERE DIETARY SALT RESTRICTION SUGGESTS RENIN-ALDOSTERONE SUPPRESSION CRITICAL IN PATHOPHYSIOLOGY

1. Plasma potassium and chloride concentrations were raised and plasma renin activity, aldosterone, bicarbonate and arterial pH were reduced in two brothers with the syndrome of hypertension and hyperkalaemia with normal glomerular filtration rate (Gordon's syndrome), on unrestricted or moderately restricted sodium diets. 2. These abnormalities were corrected in both patients within 10 days of severe sodium restriction. 3. Pressor sensitivity to cold and angiotensin II decreased on low sodium diet, associated with a fall in blood pressure. 4. Increasing distal tubular sodium delivery by infusion of normal saline increased fractional excretion of potassium when aldosterone had been stimulated by severely restricted sodium diet, but not when aldosterone levels were low on unrestricted sodium diet. 5. These findings are consistent with excessive sodium reabsorption as the primary renal lesion in Gordon's syndrome, leading to volume expansion and suppression of renin and aldosterone. Severe dietary sodium restriction leading to volume contraction, by stimulating renin and aldosterone and promoting kaliuresis, corrects the abnormalities.     

Effects of carvedilol on renal function

A randomized, double-blind, placebo-controlled study was conducted to study the effects of acute and chronic administration of carvedilol in essential hypertension, with special emphasis on renal haemodynamics and function. Acute administration of a single dose of 50 mg carvedilol reduced systolic and diastolic blood pressure without inducing reflex tachycardia. Renal blood flow was preserved; accordingly, renal vascular resistance was significantly reduced. A significant reduction in the glomerular filtration rate and filtration fraction was observed. Plasma renin activity (PRA) and plasma aldosterone values were not changed. Chronic carvedilol treatment produced a significant fall in systolic and diastolic blood pressure, heart rate, PRA and plasma aldosterone. Renal blood flow, glomerular filtration rate and filtration fraction also remained unchanged; renal vascular resistance decreased significantly. It is concluded that carvedilol possesses definite antihypertensive and renal vasodilating properties, both acutely and after chronic treatment.     

Transjugular intrahepatic portosystemic shunting (TIPS) with balloon-expandable and self-expanding stents: Technical and clinical aspects after 3 1/2 years’ experience

Purpose To evaluate prospectively our experience with transjugular intrahepatic portosystemic shunt (TIPS) using four different metallic stents. Methods Between November 1991 and April 1995, 57 patients (41 men and 16 women; age 35–72 years, mean 54 years) underwent the TIPS procedure. Techniques for portal vein localization before and during TIPS were fluoroscopy, computed tomography (CT) studies, wedged hepatic venography, arterial portography, and ultrasound. After predilation we deployed balloon-expandable (n=48) and self-expanding (n=45) metallic stents. Fifteen patients underwent variceal embolization. Initial follow-up angiograms (mean 6.9 months, range 3–24 months) were obtained in 39 of these patients. Results Fifty-three patients (93%) had successful TIPS placement. The mean decrease in portal pressure was 42.7%. Besides fluoroscopy, the most helpful techniques for portal vein localization were venography and CT. Residual stenosis (n=1) and late shortening (n=4) of Wallstents resulted in shunt dysfunction. The technical problems encountered with the Palmaz stent resulted from its lack of flexibility. We combined balloon-expandable and self-expanding stents in 12 patients. The 30-day and late follow-up (mean 11.9 months) percutaneous reintervention rates were 11.3% and 64.2%, respectively. There were no clinically significant complications related to the TIPS insertions. Conclusion An ideal stent does not exist for TIPS, and the authors recommend combining a Palmaz stent with a flexible self-expanding stent.     

左心室舒张(充盈)功能的影响因素

本文用X线电影摄影方法评价了49例左室舒张(充盈)功能的影响因素。冠心病(CAD)组23例,高血压病组12例,正常对照组14例。左室充盈功能或顺应性主要受冠脉病变严重程度的影响。冠脉狭窄程度越重,并有陈旧性心肌梗塞、室壁运动异常、EF下降,则充盈功能受损愈明显。血压、年龄因素对舒张充盈功能的影响较小。在CAD组中,心率与1/3充盈分数呈负相关,与正常化高峰充盈率(NPFR)不相关,而EF则与NPFR相关良好。     

The prevalence of autonomic neuropathy in the primary glaucomas

The results of systemic autonomic nerve function studies in patients with closed-angle glaucoma and ocular hypertension are reviewed. Autonomic neuropathy has been demonstrated in 58% of patients with closed-angle glaucoma and 42% of ocular hypertensive subjects, with significantly increased prevalence in ocular hypertensives with narrow iridocorneal angles. The implications are discussed, with particular reference to the pathogenesis of raised intraocular pressure.