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To compare the diagnostic value of dobutamine stress echocardiography with dipyridamole thallium-201 single-photon emission computed tomography (SPECT) in detecting coronary artery disease (CAD), we performed both tests on 54 patients who also underwent coronary arteriography. Dobutamine was infused at an incremental regimen of 5, 10, 20, 30 and 40 micrograms.kg-1.min-1. Dipyridamole was infused at a rate of 0.14 mg.kg-1.min-1 over 4 min. Dobutamine stress echocardiography detected 40 (93%) and SPECT 42 (98%, P = ns) of the 43 patients with significant CAD, defined as > or = 50% diameter stenosis. The specificity was 73% (8 of 11) for both tests. The sensitivity for detecting individual coronary artery stenosis with dobutamine stress echocardiography was 81% (30 of 37) for the left anterior descending artery, 75% (24 of 32) for the right coronary artery, and 61% (17 of 28) for the left circumflex artery. For SPECT it was 89%, 97% (P < 0.05 vs dobutamine stress echocardiography) and 75%, respectively. Among the 97 stenotic coronary arteries, 17 had mild to moderate stenosis (50%-69% diameter stenosis) and 80 had severe stenosis (> or = 70% diameter stenosis). With dobutamine stress echocardiography, 53% of the arteries with mild to moderate stenosis were identified vs 78% of those with severe stenosis (P < 0.05). With SPECT, the sensitivity was 82% (14 of 17) in mild to moderate stenosis and 89% (71 of 80) in severe stenosis (P = ns). No major side effects occurred during either test. Thus, both dobutamine stress and SPECT are highly sensitive for detection and localization of CAD.(ABSTRACT TRUNCATED AT 250 WORDS)
Exercise combined with dipyridamole during thallium stress testing in patients with coronary artery disease (CAD) increases the frequency of angina and ischemic ST changes in the electrocardiogram. Evidence for an increase in thallium abnormalities has been inconclusive. We prospectively examined 54 consecutive patients who underwent coronary angiography and tomographic thallium with dipyridamole (0.57 mg/kg) alone and combined with symptom-limited dynamic arm exercise. Most patients presented with a history of chest pain and 49 had angiographic evidence of significant coronary stenosis (50% diameter narrowing). Thallium abnormalities were scored blindly by consensus. The number of abnormal segments (total and ischemic) and indexes of left ventricular dysfunction, such as increased lung uptake or ischemic dilation, were compared in the 49 patients with CAD. During arm exercise more patients had evidence of ischemia (39 vs 30; p < 0.001), and the number of ischemic segments increased significantly from 1.3 +/- 1.5 to 2.5 +/- 2.2 (p < 0.001). There was also a significant increase in the indexes of left ventricular dysfunction, ischemic dilation (10 vs 4 patients; p < 0.03) and increased lung uptake (16 vs 5 patients; p < 0.001). Patients who exercised had increased thallium evidence of extent and severity of ischemia and more frequent indexes of left ventricular dysfunction. Thus, symptom-limited arm exercise improves detection of extent and severity of ischemia in patients with CAD undergoing dipyridamole thallium stress testing.
Using an in vivo assay of tumor cytotoxicity (the subrenal capsule assay in nude mice), two therapeutic strategies for the treatment of advanced human transitional cell carcinoma have been evaluated: 1) the use of 5-fluorouracil in combination with cisplatin and 2) the ability of the chemosensitizer dipyridamole to augment the cytotoxicity of CDDP and 5FU. A moderate cytotoxic response of human TCC line DU-4284 to single agent CDDP was seen; it was dose dependent at minimally toxic doses [maximal cytotoxicity--27% tumor survival (%TS) relative to control]. Efficacy was further significantly enhanced by the addition of DP [11%TS (p = .008)]. 5FU at minimally toxic doses (100 and 150 mg./kg.) also demonstrated moderate dose-dependent cytotoxic activity (35 and 31%TS, respectively) which was further enhanced by DP [21%TS (p = .03) and 18%TS (p = .05)]. A constant dose ratio of CDDP/5FU when diluted showed dose-dependent cytotoxicity; at the highest dose dilution studied, substantial cytotoxic efficacy (17%TS) was attained. The cytotoxicity of 5FU/CDDP was order independent (p = .95). The addition of DP to this combination (5FU/CDDP) further enhanced efficacy; host toxicity was not substantially enhanced. A multiple regression analysis confirmed a statistically significant effect of DP with both CDDP and 5FU (p = .001 and 0.0001, respectively); tests for trend showed no significant interaction (p = 0.33 for all models). It is concluded that, in this preclinical in vivo model of human bladder cancer, 1) CDDP and 5FU show substantial enhanced efficacy when combined, and 2) DP serves as an in vivo chemosensitizer of both CDDP and 5FU; DP further augments the efficacy of this binary combination. These data would indicate the potential of this ternary (5FU/CDDP/DP) drug therapeutic regimen for clinical trial to treat advanced bladder cancer.
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Very low density lipoproteins (VLDL) and low density lipoproteins (LDL) were isolated from serum of hypercholesterolemic guinea-pigs, and the effect of these lipoproteins on guinea-pig platelets was studied. VLDL (greater than 100 microgram/ml) and LDL (greater than 400 microgram/ml) were found to cause aggregation of gel-filtered platelets (GFP), although the extent of GFP aggregation by LDL was smaller than that by VLDL. In platelet-rich plasma, however, lipoproteins could not induce platelet aggregation. VLDL and LDL even at the low concentrations at which lipoproteins alone could not induce aggregation potentiated ADP-induced aggregation of GFP. VLDL-induced aggregation of GFP was inhibited by apyrase (0.2--1.0 mg/ml) in a concentration-related manner. Prostaglandin E1, dipyridamole, potassium cyanide and ethylenediaminetetraacetic acid inhibited VLDL- and ADP-induced aggregation of GFP in the almost same degree. Inhibitions of VLDL-induced GFP aggregation by acetylsalicylic acid and albumin were slightly stronger than that of ADP-induced aggregation. These findings suggest that lipoproteins modulate platelets so that endogenous ADP can be released from platelets.
Atherosclerotic heart disease is the leading cause of death in patients with end stage renal disease, but its non invasive detection remains difficult because of a low efficacy of exercise testing. The aim of the study was to evaluate diagnostic accuracy of thallium myocardial imaging after dipyridamole combined with exercise. Forty two chronic dialysis patients (34 men, 8 women) aged 55 +/- 11 years (range: 36 to 75) without symptom of angina nor myocardial infarction were studied. In each patient, an echocardiography, a myocardial scintigraphy with dipyridamole combined with symptom-limited exercise, and coronarography were performed. A coronary heart disease was diagnosed by coronarography in 10 patients (4.5 and 1 respectively with 1, 2 and 3 vessels diseased). Echocardiography detected a left ventricular hypertrophy (LVH) in 26 patients and a regional asynergia in 14 patients. A positive scintigraphy was present in 11 patients. Three false-positive and 2 false-negative on scintigraphy were noted. Sensibility, specificity, positive predictive value and negative predictive value were respectively evaluated at 80, 73, 73 and 93%. All the five patients with either false-positive or false-negative scintigraphy exhibited a LVH. CONCLUSION. In chronic dialysis patients, coronary heart disease may be detected by thallium myocardial imaging after dipyridamole combined with exercise.
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Persantine combined with TNF-a enhances antiproliferative activity in human tumor cells. We hypothesized that the vasodilator persantine would ameliorate acute pancreatitis (AP) in vitro. Rat pancreatic ductal cells were cultured using standard techniques. Acute pancreatitis was induced by adding cerulein (10(-9) M) or TNF-a (200 ng/ml). AP was verified by increased amylase production. Persantine was added at concentrations from 0.1 uM to 100 uM post cerulein or TNF-a treatment. Statistical analysis was achieved by ANOVA. Amylase production was significantly increased (p < 0.05) compared with control upon stimulation with either cerulein or TNF-a. When persantine was added in graded concentrations from 0.1 uM to 100 uM to cerulein treated cells, it decreased amylase production significantly (p < 0.05) at 100 uM. However, when persantine was added to TNF-a treated cells, it decreased amylase production (p < 0.05) at the lower concentrations of 0.1 uM and 1 uM. We have shown for the first time that AP, resulting from either mild (cerulein) or severe (TNF-a) stimulation, is significantly improved by treatment with persantine.
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Thirty-six mongrel dogs were used. After systemic heparinization (150 U/kg), a 5 mm longitudinal coronary incision was made with looped non-elastic monofilament sutures or elastic sutures applied proximally and distally. The incised coronary artery was exposed to non-humidified carbon dioxide, humidified carbon dioxide with lactated Ringer solution, or humidified carbon dioxide with heparin and dipyridamole-added lactated Ringer solution for 10 or 20 min in each group. After gas insufflation, the incised coronary artery was repaired, then, the coronary was reperfused. Perfusion-fixation was done for observation of the coronary endothelium by scanning electron microscopy. The adverse effect on the endothelium was graded as follows: grade 1, appeared normal; grade 2, few blood cells deposited; grade 3, many blood cells deposited; grade 4, few endothelial cells delaminated with blood cells deposited; grade 5, many endothelial cells delaminated with blood cells deposited.
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370 questionnaires (222 private practices (PP), 117 hospitals (HO), 31 university hospitals (UH)) were evaluated.
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Mean Thrombolysis in Myocardial Infarction frame count significantly decreased after dipyridamole in both groups. At baseline, mean values of the single photon emission computed tomography score were 31.5 +/- 1.6 and 25.1 +/- 2.1 in groups A and B, respectively. After dipyridamole, they increased from 31.5 +/- 1.6 to 37.8 +/- 1.4 (P < 0.001) in group A, whereas a further decrease to 15.0 +/- 1.2 (P < 0.005) was observed in group B.
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RTPE demonstrated that cardiac tumors have greater microvascular blood volume and regional blood flow when compared with thrombi. Dipyridamole stress was useful in differentiating MT from BT.
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High-dose dobutamine-stress and high-dose dipyridamole-stress echocardiographies have comparable diagnostic accuracies, with a slightly higher sensitivity with dobutamine and a slightly higher specificity with dipyridamole.
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Evidence was obtained for the augmentation of cytotoxic effects of 5-fluorouracil (5-FU) when hyperthermia and dipyridamole (DP) were combined in vitro. Nontoxic levels of DP enhanced the combined cytotoxicity of 5-FU and heat against HeLa and B16 melanoma cells, and the 50% effective concentration of 5-FU decreased 7.3 fold for HeLa cells and 3.0 fold for B16 melanoma cells, when exposed to heat plus DP. This combined effect did not depend on intracellular increases in the concentrations of 5-FU. Thus hyperthermia together with DP seems to improve the sensitivity of tumor cells to 5-FU. As the sensitivity of colorectal cancer tissue to drugs is low, 5-FU plus hyperthermia and DP shows promise for the treatment of such patients.
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Ingestion of 1.2 g Bay g 6575 daily for 1 week by six healthy volunteers had no effect on blood-coagulation, fibrinolysis, or platelet aggregation in vitro, but it seemed to inhibit platelet aggregation in vivo (shown by a smaller reduction in the platelet aggregate ratio after venous occlusion). Plasma drawn from five volunteers after ingestion of a single dose of 1.2 g of the drug stimulated prostacyclin release from slices of rat aorta which had been washed until they stopped releasing anti-aggregating substances, whereas plasma from the same individuals before ingestion of the substance did not. Administration of either Bay g 6575 or dipyridamole alone had no effect on platelet aggregation in vitro, but combined administration resulted in a striking and prolonged inhibition of A.D.P.-induced platelet aggregation. It is proposed that the previously described antithrombotic properties of Bay g 6575 in animals are due to stimulation of prostacyclin release from the vessel wall, and that this effect is also demonstrable in man.
Randomized trials of fractional flow reserve-guided percutaneous coronary interventions established an objective, quantitative, outcomes-driven standard of physiological stenosis severity. However, pressure-derived fractional flow reserve requires invasive coronary angiogram and was originally validated by comparison to noninvasive PET.
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Possible roles of dibutyryladenosine 3',5'-cyclic monophosphate (cAMP) and dibutyryl-guanosine 3',5'-cyclic monophosphate (cGMP) in regulation of hepatocyte DNA synthesis were examined using primary cultures of young-adult rat hepatocytes maintained in arginine-free medium. Throughout the experimental period, nonparenchymal cells were hardly observed in the selective medium. When epidermal growth factor (EGF) was added to the cultures, a transient increase in the intracellular cAMP level preceded the elevation of hepatocyte DNA synthesis. EGF-stimulated hepatocyte DNA synthesis was remarkably enhanced by the elevation of the intracellular cAMP level induced by treatment with cAMP alone or a combination of cAMP and theophylline, an inhibitor of cyclic nucleotide phosphodiesterase. Furthermore, the early elevation of intracellular cAMP alone, which was induced by treatment with the combination of cAMP and theophylline, caused a remarkable increase in hepatocyte DNA synthesis. On the other hand, addition of EGF to the cultures caused a rapid decrease in the intracellular cGMP level followed by an increase in hepatocyte DNA synthesis. EGF-stimulated hepatocyte DNA synthesis was severely suppressed or completely inhibited by the elevation of the intracellular cGMP level induced by treatment with cGMP alone or a combination of cGMP and dipyridamole, a specific inhibitor of cGMP phosphodiesterase. These findings indicate that cAMP and cGMP act oppositely on the regulation of DNA synthesis of young-adult rat hepatocytes in primary culture: cAMP plays a positive role, whereas cGMP plays a negative role. Also it is strongly suggested that an early elevation of the intracellular cAMP level is essential for the onset of DNA synthesis in hepatocyte primary cultures.
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We report an unselected series of eight patients younger than 6 months of age with Kawasaki disease evaluated between January 1982 and May 1984. The incidence of coronary artery aneurysms (six patients) and the mortality (two patients) were unusually high in this small series. Because of the confusing clinical presentation in three patients, diagnosis was delayed until pathologic or echocardiographic evidence of coronary vasculitis or aneurysm was discovered. The currently accepted clinical criteria for Kawasaki disease may not always identify patients with the pathologic findings of the syndrome who are younger than 6 months of age. The diagnosis of Kawasaki disease and echocardiographic evaluation of the coronary arteries should be considered in young infants with prolonged fever of unknown origin.
Loss of β-cell mass is a cardinal feature of diabetes. Consequently, developing medications to promote β-cell regeneration is a priority. cAMP is an intracellular second messenger that modulates β-cell replication. We investigated whether medications that increase cAMP stability or synthesis selectively stimulate β-cell growth. To identify cAMP-stabilizing medications that promote β-cell replication, we performed high-content screening of a phosphodiesterase (PDE) inhibitor library. PDE3, -4, and -10 inhibitors, including dipyridamole, were found to promote β-cell replication in an adenosine receptor-dependent manner. Dipyridamole's action is specific for β-cells and not α-cells. Next we demonstrated that norepinephrine (NE), a physiologic suppressor of cAMP synthesis in β-cells, impairs β-cell replication via activation of α(2)-adrenergic receptors. Accordingly, mirtazapine, an α(2)-adrenergic receptor antagonist and antidepressant, prevents NE-dependent suppression of β-cell replication. Interestingly, NE's growth-suppressive effect is modulated by endogenously expressed catecholamine-inactivating enzymes (catechol-O-methyltransferase and l-monoamine oxidase) and is dominant over the growth-promoting effects of PDE inhibitors. Treatment with dipyridamole and/or mirtazapine promote β-cell replication in mice, and treatment with dipyridamole is associated with reduced glucose levels in humans. This work provides new mechanistic insights into cAMP-dependent growth regulation of β-cells and highlights the potential of commonly prescribed medications to influence β-cell growth.
Recent developments have permitted myocardial contrast echocardiography (MCE) to become a new method of noninvasively assessing myocardial perfusion in humans. Preliminary studies of myocardial perfusion imaging during adenosine, dipyridamole, and dobutamine stress echocardiography have shown excellent agreement with either radionuclide uptake or quantitative angiography. This article reviews the recent advances in microbubble technology, ultrasound imaging, and myocardial physiology that have made contrast echocardiography a potential new gold standard for perfusion imaging in the new millennium.
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The noninvasive identification of a high-risk subgroup among women with chest pain and unknown coronary artery disease is an unresolved task to date.
This study was undertaken to develop new dipyridamole (DP) formulations with acidic microenvironmental pH-modifiers for improving dissolution and absorption under hypochlorhydric conditions. Dipyridamole granules (DPG) with ten acidic pH-modifiers were prepared with conventional wet granulation, and their manufacturability, stability and dissolution behavior were characterized. Pharmacokinetic profiling of the optimized DPG with acid was carried out in omeprazole-treated rats as a hypochlorhydric model. On the basis of the manufacturability, stability and dissolution behavior of new DPG formulations, p-toluenesulfonic acid (TS) was found to be a suitable acidic pH-modifier for DPG formulation. Although DPG showed pH-dependent dissolution behavior, DPG with TS exhibited a high rate and extent of dissolution in both acidic and neutral media. After oral administration of DPG (10mg DP/kg) in omeprazole-treated hypochlorhydric rats, there was ca. 40% reduction of the area under the curve of plasma concentration vs. time from zero to 3h (AUC(0-3)) for DPG compared with that in normal rats. However, AUC(0-3) for DPG/TS under hypochlorhydria was almost identical to that of DPG in normal rats. From these findings, the addition of TS as a microenvironmental pH-modifier in DP formulation might be beneficial in expanding the therapeutic potential of DP in hypochlorhydric patients.
The tumor microenvironment plays a crucial role during tumor development. Integrated combination of drugs that target tumor microenvironment is a promising approach to anticancer therapy. Here, we report a multifunctional combination of low-cytotoxic drugs composed of dipyridamole, bestatin and dexamethasone (DBDx) which mainly acts on the tumor microenvironment shows highly potent antitumor efficacy in vivo. In mouse hepatoma H22 model, the triple drug combination showed synergistic and highly potent antitumor efficacy. The combination indices of various combinations of the triple drugs were between 0.2 and 0.5. DBDx inhibited the growth of a panel of human tumor xenografts and showed no obvious systemic toxicity. At tolerated doses, DBDx suppressed the growth of human hepatocellular carcinoma BEL-7402, HepG2, and lung adenocarcinoma A549 xenografts by 94.5%, 93.7% and 96.9%, respectively. Clonogenic assay demonstrated that DBDx showed weak cytotoxicity. Western blot showed that Flk1 and Nos3 were down-regulated in the DBDx-treated group. Proteomic analysis showed that DBDx mainly affected the metabolic process and immune system process; in addition, the angiogenesis and VEGF signaling pathway were also affected. Conclusively, DBDx, a multifunctional drug combination of three low-cytotoxic drugs, shows synergistic and highly potent antitumor efficacy evidently mediated by the modulation of tumor microenvironment. Based on its low-cytotoxic attributes and its broad-spectrum antitumor therapeutic efficacy, this multifunctional combination might be useful in the treatment of cancers, especially those refractory to conventional chemotherapeutics.
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Currently used methods for assessment of coronary flow reserve are invasive and require extensive laboratory equipment. Recently, noninvasive assessment of coronary flow reserve by transesophageal Doppler evaluation of coronary sinus (CS) or left anterior descending coronary artery (LAD) flow has been proposed. Direct comparison between these two techniques is lacking.