Torsades de pointes after intracoronary papaverine

Coronary blood flow velocity and coronary flow reserve can be assessed in humans using a coronary Doppler catheter and the vasodilator papaverine. Although it is a safe, elegant and reproducible technique, serious complications can occur. Coronary flow reserve assessment in a 49-year-old man with a critical stenosis in the proximal part of the circumflex artery was complicated by a papaverine-induced ventricular arrhythmia. Several features of the present case report support papaverine-induced disturbances of the repolarization phase as the pathophysiological mechanism: a 'torsade de pointes' pattern of the tachycardia, the lengthening of the QT-interval, the appearance of a new U-wave and the presence of additional risk factors (hypokalaemia and alcalosis). Patients presenting additional risk factors for this complication should be excluded from coronary flow reserve assessment.     

Effects of sympathetic stimulation on cerebral and ocular blood flow Modification by hypertension,hypercapnia, acetazolamide,PGI2 and papaverine

The effect of unilateral, electrical stimulatio of the cervical sympathetic chain in rabbits anesthetized with pentobarbital sodium and vasodilated by hypercapnia, acetazolamide, papaverine or PGI₂ was investigated to determine to what extent the sympathetic nerves to the brain and the eye cause vasoconstriction and prevent overperfusion in previously vasodilated animals. Evans blue was given as a tracer for protein leakage. Blood flow determinations were made with the labelled microsphere method during normotension and acute arterial hypertension. Hypertension was induced by ligation of the thoracic aorta and in some animals metaraminol or angiotensin was also used. Acetazolamide caused a two to threefold increase in cerebral blood flow (CBF) and hypercapnia resulted in a fivefold increase. CBF was not markedly affected by papaverine or PGI₂. In the choroid plexus, the ciliary body and choroid, papaverine and hypercapnia caused significant blood flow increases on the control side. Sympathetic stimulation induced a 12 % blood flow reduction in the brain in normotensive, hypercapnic animals. Marked effects of sympathetic stimulation at normotension were obtained under all conditions in the eye. In the hypertensive state the CBF reduction during sympathetic stimulation was moderate, but highly significant in hypercapnic or papaverine-treated animals as well as in controls. Leakage of Evans blue was more frequently seen on the nonstimulated side of the brain. In the eye there was leakage only on the control side except in PGI₂-treated animals where 2 rabbits had bilateral leakage. The effect of sympathetic stimulation on the blood flow in the cerebrum and cerebellum in vasodilated animals seems to be small or absent if the blood pressure is normal. In the eye pronounced vasoconstriction occurs under these conditions. In acute arterial hypertension sympathetic stimulation protects both the cerebral and ocular barriers even under conditions of marked vasodilation.     

Influence of propranolol and pindolol on the haemodynamic effects of papaverine,isoprenaline and noradrenaline in hypertensive patients

Summary The influence of two -adrenoceptor antagonists, propranolol and pindolol, on the haemodynamic effects of papaverine, isoprenaline and noradrenaline was investigated in 9 male patients with first degree essential hypertension. Propranolol and pindolol were given according to a doubleblind, crossover scheme. Heart rate and blood pressure were measured before and after each treatment. Propranolol 670 µg/kg i. v. reduced the supine and standing systolic blood pressures by 2.3% and 1.6%, respectively. Similarly, the intravenous administration of pindolol 35 µg/kg reduced supine and standing systolic blood pressure by 5.5% and 8.3% respectively (clinically insignificant). Neither drug affected diastolic blood pressure. Following propranolol, there were moderate reductions in supine and standing heart rates, respectively by 24% and 20% (p<0.001). Similarly, but to a lesser extent, pindolol reduced supine and standing heart rate by 12% and 17% (p<0.001). The effects of papaverine, which, at 1.5 mg/kg i. v. reduced systolic blood pressure by 5–10% and increased heart rate by 8–15%, were not significantly influenced by the -blockers. The blood pressure and heart rate responses to isoprenaline, on the other hand, were attenuated or inhibited by both -blockers. While the -blockers inhibited the -adrenoceptor component of noradrenaline, the pressor component of noradrenaline, which is mediated through the -adrenoceptors, was not influenced by propranolol, but was inhibited after pindolol. It is concluded that pindolol differs qualitatively from propranolol in that it inhibited both the -and -adrenoceptor effects of noradrenaline.Abbreviations BP blood pressure - ECG electrocardiogram - HR heart rate - ISA intrinsic sympathomimetic activity     

盐酸罂粟碱氯化钠注射液细菌内毒素检测法实验研究

目的：建立盐酸罂粟碱氯化钠注射液的细茵内毒素检查方法。方法：用两个生产厂的鲎试剂对盐酸罂粟碱氯化钠注射液进行干扰试验研究。结果：盐酸罂粟碱氯化钠注射液对细茵内毒素检查无干扰作用。结论：可以用细茵内毒素检查法(凝胶法)代替家兔热原检查法控制其热原。     

Renal fractional flow reserve: a hemodynamic evaluation of moderate renal artery stenoses.

The objective of this study was to perform a hemodynamic evaluation of moderate (50-90%) renal artery stenosis (RAS) under conditions of rest and maximum hyperemia. Identifying patients with RAS who have hemodynamically significant stenoses and are most likely to benefit from revascularization is clinically important. Current methods used to evaluate RAS, including angiography, have limitations. Physiologic evaluation of RAS may have a role in identifying patients with hemodynamically significant stenosis. Patients with suspected renovascular hypertension due to aorto-ostial RAS were included in the study. Hyperemia was induced by administration of intrarenal papavarine. Translesional pressure gradients were measured and renal fractional flow reserve (FFR) was calculated using a 0.014' pressure guidewire. Thirteen patients and 14 arteries with moderately severe (50-90%) RAS were studied. The mean translesional pressure gradient rose from a baseline of 6.3 +/- 3.9 to 17.5 +/- 10.8 mm Hg with maximal hyperemia. The renal FFR ranged from 0.58 to 0.95. There was a poor correlation between angiographic stenosis measurement and the renal FFR (r = -0.18; P = 0.54) and the hyperemic translesional mean pressure gradient (r = 0.22; P = 0.44). There was an excellent correlation between renal FFR and the resting mean translesional pressure gradient (r = -0.76; P = 0.0016) and the hyperemic mean translesional pressure gradient (r = -0.94; P < 0.0001). Selective renal arterial papavarine administration induces maximum hyperemia, permitting the calculation of renal FFR in renal arteries with aorto-ostial stenoses. The renal FFR correlates well with other hemodynamic parameters of lesion severity, but poorly with angiographic measures of lesion severity.     

Identification of embelin,a 3-undecyl-1,4-benzoquinone from Embelia ribes as a multitargeted anti-Alzheimer agent

Beta-secreatse (BACE-1) and cholinesterases are clinically validated targets of Alzheimer's disease (AD), for which natural products have provided immense contribution. The multifaceted nature of AD signifies the need of multitargeted agents to tackle this disease. In the search of new natural products as dual BACE-1/cholinesterase inhibitors, a library of pure natural products was screened for inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and BACE-1. The screening efforts have identified 1,4-benzoquinone “embelin,” a natural product derived from Embelia ribes displaying inhibition of all three enzymes, with IC₅₀ values of 2.5, 5.4, and 2.1 μM, respectively. This screen has also identified isoquinoline alkaloids papaverine and L-tetrahydropalmatine as AChE inhibitors. Kinetic study has shown that embelin inhibits EeAChE and EqBChE with ki values of 4.59 and 0.57 μM, in an uncompetitive and noncompetitive manner, respectively. The interactions of embelin with allosteric peripheral anionic site of cholinesterases, has further supported the results of kinetic study. Embelin has also enhanced the activity of P-gp in LS-180 cells, the efflux pump which is involved in the clearance of amyloid-β from AD brain. Further, the cell viability study in neuronal cell line has indicated the excellent therapeutic window of embelin. These results are indicative of the fact that embelin is a multitargeted agent playing role in stopping the formation of amyloid-β oligomers (via inhibition of BACE-1), improves cholinergic-transmission (via inhibition of AChE/BChE) and increases amyloid-β clearance (via P-gp induction).     

Periarterial papaverine application improves intraoperative kidney function during laparoscopic donor nephrectomy

BACKGROUND: Laparoscopic donor nephrectomy decreases disincentives to donation frequently associated with the disadvantages of open surgery. However, concerns have been raised regarding graft quality, since the incidence of delayed graft function is higher when compared with open procedures. This may be caused by amelioration of kidney perfusion due to the elevated intraabdominal pressure and to a mechanically induced renal angiospasm during donation. This study was addressed to reveal whether the renal periarterial application of papaverine is able to enhance renal blood flow during laparoscopic nephrectomy. MATERIALS AND METHODS: Twelve male piglets underwent left laparoscopic donor nephrectomy after endoscopic occlusion of the right renal vessels and ureter. Urine output and creatinine clearance were determined as indicators of renal blood flow. In the treatment group (n = 6) papaverine hydrochloride was administered to the tissue surrounding the renal artery prior to preparation of the vessels and results were compared with those of controls (n = 6). Free sodium excretion was measured to preclude prerenal failure. RESULTS: In the control group the mean urine output was 0.015 ml/min/kg and the mean creatinine clearance was 0.95 ml/min/kg. In pigs treated with papaverine the mean urine output was 0.052 ml/min/kg and the mean creatinine clearance was 2.22 ml/min/kg. The differences were significant (urine output, P = 0.02; creatinine clearance, P = 0.038). CONCLUSIONS: Papaverine improves renal function during laparoscopic kidney harvest when applied in the vicinity of the renal artery prior to vascular preparation.     

野罂粟中野罂粟碱提取方法及其含量测定

目的考察野罂粟全草中野罂粟碱最佳提取方法以及确定HPLC含量测定方法学.方法用盐酸调pH 4酸水、70%乙醇、70%乙醇(2次) 酸水及95%乙醇作为提取溶剂,得到4种提取物并用HPLC法测定各提取物中野罂粟碱含量并以此为指标,确定最佳提取工艺.结果酸水提取物中野罂粟碱含量最高9.987%.结论野罂粟全草中野罂粟碱用pH 4酸水提取得率较高.     

阴茎海绵体注射血管活性药物治疗阳萎2150例

回顾性总结１２年间阴茎海绵体注射血管活性药物（ＩＣＩ）治疗阳萎２１５０例经验，对ＩＣＩ的疗效及随访、ＩＣＩ并发症及其预防、ＩＣＩ的应用前景进行了讨论，认为ＩＣＩ是治疗阳萎安全有效的方法。     

The actual incidence of papaverine-induced priapism in patients with erectile dysfunction following penile colour Doppler ultrasonography

Penile color Doppler sonography is a valuable method for evaluating erectile dysfunction. However, there are some concerns about the safety of this method due to the intracorporeal pharmacological injection, which may cause priapism as a complication, resulting in penile fibrosis. To evaluate the actual incidence of papaverine-induced priapism in patients with erectile dysfunction (ED) who underwent penile colour Doppler sonography and to determine the safety of this diagnostic tool, a retrospective study was conducted using the database of our institution. A total of 672 men with ED underwent penile color Doppler ultrasonography with the intracorporeal injection of 60 mg papaverine hydrochloride. The patient characteristics of priapism cases were retrospectively evaluated. Priapism in 18 of the 672 patients (2.68%) was successfully treated with blood aspiration, irrigation and injection of an α-agonist medication, when needed. Patients with priapism were younger compared with those without priapism; mean age 45 ± 12.51 (20–68) versus 50.93 ± 12.04 (17–78) ( P  < 0.001). Penile Doppler ultrasound is a safe procedure in evaluating erectile dysfunction. The incidence of priapism, which is the most important complication of this procedure, is low and can be managed successfully with conservative approaches.