bluuebunny/crossref_metadata_2025 huggingface dataset:
Analysis of normal fault populations in the Kumano Forearc Basin, Nankai Trough, Japan: 1. Multiple orientations and generations of faults from 3‐D coherency mapping
Authors: Moore G. F. , Boston B. B. , Sacks A. F. , Saffer D. M.
Published: March 2013

Analyses of normal faults in the Kumano forearc basin of the Nankai Trough reveal multiple normal fault populations in a region generally thought to be under compression. Most faults have offsets of less than 20 m and dips of 60–70° and show no growth structures, indicating that the faults were active for short periods of time. The oldest generation of faults is older than ~0.9 Ma and strikes ~50–60°. The next oldest faults strike ~160–170°, are older than 0.44 Ma, and are related to local uplift along the western edge of the region. The youngest faults cut the seafloor; shallow faults near the SE margin of the basin curve from ~100° in the middle of the survey area to ~145° at the SE corner of the area. The pattern of the two youngest fault populations is consistent with the regional stress pattern (maximum horizontal stress subparallel to the trench). Orientations of older fault populations are caused by uplift of the underlying accretionary prism, implying that the forearc basin region is not as stable as previously thought. Reconstruction of displacements on the youngest faults shows that the overall horizontal extension is less than 2%, concentrated near the seaward edge of the basin. The active normal faults distributed throughout the basin support the idea that the horizontal stress parallel to the plate convergence direction does not reach the critical stress to activate or form thrust faults and produce horizontal shortening within the shallow portion of the inner wedge.
Revised tectonic evolution of the Eastern Indian Ocean
Authors: Whittaker Joanne M. , Williams Simon E. , Müller R. Dietmar
Published: March 2013

Published plate tectonic models for the Australian‐Antarctic plate pair imply geologically improbable scenarios at either or both ends of the Cretaceous rift and spreading system. Controversy also exists around the location of and motion at the plate boundary extending west of Australia‐Antarctica, through the Kerguelen Plateau region. We present a plate tectonic model of relative motions among India, Australia, and Antarctica from the onset of continental rifting to the establishment of rapid seafloor spreading, at ~43 Ma. The model conforms to a wide range of geological/geophysical evidence and reconstructs the formation of both the western Kerguelen region and the eastern Tasman region. The incorporation of spatiotemporally continuous plate boundaries reveals the presence of a plate boundary beneath the contiguous Central Kerguelen Plateau and Broken Ridge for ~65 Ma. To investigate the relationship between the plate boundary system and the Kerguelen plume, we test three alternative absolute reference frames. Using a fixed hot spot reference frame, the Indian Ocean mid‐ocean ridge system remains within 500 km of the Kerguelen plume, while the proximity of the plate boundaries and the plume is more variable with a moving hot spot reference frame. Proximity between the plume, plate boundaries, and the Central Kerguelen Plateau/Broken Ridge for ~65 Myr suggests that these specific features were not formed by a single, short‐lived (5–10 Myr) pulse of magmatic activity, but rather by a ~25 Myr period of relatively high magma flux followed by ~40 Myr period of lower volume magmatic activity, an interpretation not excluded by the relatively sparse dredge and drill ages.
Properties of unipolar magnetic field pulse trains generated by lightning discharges
Authors: Kolmašová Ivana , Santolík Ondřej
Published: March 2013

We analyze and describe trains of regular unipolar microsecond‐scale magnetic field pulses produced by intracloud lightning discharges. Waveforms of the magnetic field are measured using a newly developed broadband analyzer with a sampling interval of 12.5 ns. The observed trains contained several tens of pulses, and the time interval between neighboring pulses typically varied between 1 and 10 µs. The amplitude of the pulses also varied by 1 order of magnitude. A systematic analysis of these variations is done for the first time. The interpulse interval is usually increasing (on average by 4.1 µs during a train), and the pulse amplitude is decreasing (on average by 15% of the maximum value within a given train). We propose a possible generation mechanism based on a hypothesis that periodical charge structures are present in the thundercloud. This mechanism can explain the observed evolution of peak amplitudes and interpulse intervals.
Future change of the potential landslide disasters as evaluated from precipitation data simulated by MRI‐AGCM3.1
Authors: Oku Yuichiro , Nakakita Eiichi
Published: March 2013

The purpose of this study is to evaluate the number of potential landslide disasters in the future due to the effect of climate change in Japan using atmospheric global atmospheric models. To achieve this, two indices of precipitation R1.5 and R72 were adopted for the evaluation of the number of occurrences in the near future and/or in the future. The potential of shallow landslide occurrence will increase 20% at the end of the 21st century compared with present‐day potential, and that of deep‐seated landslides will increase up to 30%. According to statistical analysis of future changes of precipitation indices, significant change to the number of shallow slides was to be found areas across most areas of Japan. As for deep‐seated landslides, however, changes are statistically significant only in western Japan and some areas of the Tohoku region. Copyright © 2013 John Wiley & Sons, Ltd.
Disposition of Intravenous Propylthiouracil
Authors: GILES H. G. , ROBERTS E. A. , ORREGO H. , SELLERS E. M.
Published: March 2013

Abstract:Propylthiouracil was administered to 10 healthy, male volunteers by a short intravenous infusion. Plasma and urinary drug concentrations were determined by a specific high‐performance liquid chromatography assay, and protein binding was determined by equilibrium dialysis. After infusion, the plasma concentrations declined biexponentially, and the following median parameters (and ranges) were determined: clearance 273.5 ml/min (159.5–377.8 ml/min); free drug clearance, 1537.7 ml/min (985.9–1927.3 ml/min); apparent volume of distribution, 28.0 liters (22.7–44.4 liters); apparent elimination half‐life, 1.28 hr (0.88–2.05 hr);k21, 3.12 hr−1(1.06–5.36 hr−1); α 7.34 hr−1(1.94–25.03 hr−1);Vc9.40 liters (5.16–18.58 liters). In urine, only 1.28 per cent (0.03–2.01 per cent) of the administered dose was recovered over 24 hours as unchanged drug. The ratio (1.2 per cent) of urinary clearance (3.2 ml/min) to plasma clearance is far less (P< 0.001) than the free fraction in plasma (median 18.2 percent, range 16.2–20.2 per cent) and this suggests that there is significant renal tubular reabsorption of propylthiouracil. In healthy subjects, both intraindividual and interindividual variation in protein binding is modest, and free drug clearance can be predicted from total drug clearance (y= 257.6 + 4.56x, r= 0.95,P< 0.001).
Toxicologic Evaluation of Bumetanide, A Potent Diuretic Agent
Authors: McCLAIN R. M. , DAMMERS K. D.
Published: March 2013

Abstract: The studies reported represent the preclinical toxicologic evaluation of bumetanide. Toxicity testing in rats, rabbits, dogs, and baboons indicate that bumetanide is well tolerated in various species. The toxicity that was observed is, for the most part, the direct consequence of its potent diuretic activity and is similar to that produced by other“loop” diuretics. Bumetanide was fetotoxic at maternal toxic doses in the rabbit, but no evidence of teratogenic effects was observed in rabbits, rats, mice, or hamsters. The compound was devoid of mutagenic activity by the Ames test and was found to be noncarcinogenic in long‐term rat studies.
Pharmacokinetics and Bioavailability of Hydromorphone Following Intravenous and Oral Administration to Human Subjects
Authors: VALLNER J. J. , STEWART J. T. , KOTZAN J. A. , KIRSTEN E.B. , HONIGBERG I. L.
Published: March 2013

Abstract: In a relatively small pilot study, the half‐life of elimination of hydromorphone in six subjects was 2.64 ± 0.88 hours and the drug had a high volume of distribution, 1.22 1./kg. In addition, the drug was rapidly but incompletely absorbed after oral administration. An equation to predict the plasma concentration of hydromorphone on oral administration was developed from the data of these six subjects.
Pharmacokinetic Principles of Lidocaine Dosing in Relation to Disease State
Authors: WALLER ELAINE S.
Published: March 2013

Abstract: The pharmacokinetic parameters of lidocaine are pertinent to the determination of both appropriate loading doses and constant infusion rates that achieve a therapeutic plasma concentration while avoiding toxicity. Because lidocaine is used primarily in older patients who may have concurrent diseases, the effects of disease states on lidocaine disposition are important when calculating lidocaine doses. Patients with congestive heart failure and hepatic disease have pronounced changes in lidocaine clearance. Patients placed on prolonged lidocaine infusions have a change in disposition half‐life of the drug. Patients with renal disease do not have significant alterations in handling the parent compound but, because of the dependence of glycinexylidide elimination on renal function, may accumulate the metabolite and develop central nervous system toxicity. Even though there are differences in some of the pharmacokinetic variables for lidocaine in young and elderly patients, the clearance of the drug was not significantly different in the two patient groups. The effects of concurrently administered drugs on lidocaine pharmacokinetics remain to be more widely studied in patients.
Hydrochlorothiazide Pharmacokinetics and Pharmacologic Effect: The Influence of Indomethacin
Authors: WILLIAMS ROGER L. , DAVIES RICHARD O. , BERMAN RAYANNE S. , HOLMES GEOFFREY I. , HUBER PAUL , GEE WINNIE LIANG , LIN EMIL T. , BENET LESLIE Z.
Published: March 2013

Abstract:It is known that nonsteroidal antiinflammatory drugs such as indomethacin can attenuate the pharmacologic effect of loop diuretics such as furosemide and ethacrynic acid and that indomethacin may also reduce the pharmacologic response to chlorothiazide. To examine further this potential drug—drug interaction, we administered 50‐ and 100‐mg single oral doses of hydrochlorothiazide with and without indomethacin to 10 healthy, normal subjects. We observed no significant influence of indomethacin either on the pharmacokinetics of hydrochlorothiazide or the pharmacologic response to this diuretic. The absorption and disposition of hydrochlorothiazide demonstrate that this drug is rapidly absorbed and produces a diuretic and natriuretic response that peaks at approximately 2 hours after dosing and is essentially terminated 12 hours after dosing. There appeared to be no greater pharmacologic response to the 100‐mg than to the 50‐mg hydrochlorothiazide dose in the ten subjects in this study.
The Effects of Renal Function on the Disposition of Isradipine
Authors: Chandler Mary H. H. , Schran Horst F. , Cutler Ralph E. , Smith Albert J. , Gonasun Leonard M. , Blouin Robert A.
Published: March 2013

The effect of renal function on isradipine kinetics was examined in four groups of subjects (N = 55) who had normal or impaired renal function. Each subject received isradipine orally as a 10‐mg capsule. Serial blood samples were obtained from 0 to 48 hours postdose and the isradipine plasma concentrations determined by radioimmunoassay. Kinetic parameters, Cmax, Λ3, t1/2, AUC, CL'o (oral clearance), and CLo (oral clearance standardized to body weight) were determined. Marked intersubject variability of the pharmacokinetic parameters was observed. No statistically significant differences (P > .05) were found for AUC, CL'o, and CLo parameters when renal impairment groups were compared with controls. AUC values were lower (P < .05), however, for the group with severe renal function impairment than for groups with mild or moderate renal function impairment. No significant correlations (r = –.23, P > .05; and r = .13, P > .05, respectively) were found between creatinine clearance (CLCR) and CLo and between age and CLo. Considering the interpatient variability in isradipine disposition and the lack of significant differences in CLo between groups, no clear‐cut dosing regimen alterations, based on single‐dose data, are warranted in renal impairment.
Ranitidine Accumulation in Patients Undergoing Chronic Hemodialysis
Authors: Comstock Thomas J. , Sica Domenic A. , Stone Susan , Davis Judy , Garnett William R. , Karnes H. Thomas , Warner Christopher W.
Published: March 2013

Ranitidine accumulation was assessed in 20 patients undergoing chronic hemodialysis following oral daily doses of 150 mg ranitidine for 10 days. Serum ranitidine concentrations prior to dialysis were 191 ± 115 mcg/l and 207 ±172 mcg/l for patients dialyzed three and two times per week, respectively. The amount of ranitidine recovered in the dialysate during the final dialysis session of the study was negligible and ranged from 308–3036 mcg, representing less than 3% of the administered dose. Clearance by hemodialysis was 3.0 ± 1.1 1/hr. Once daily dosing of 150 mg ranitidine does not result in excessive accumulation, and drug loss during hemodialysis is small. These data suggest that supplemental dosing after hemodialysis is not indicated.
Pharmacodynamic Comparison ofl‐Bunolol with Propranolol, Metoprolol, and Placebo
Authors: Ochs Hermann R. , Bahrmann Heinrich , Greenblatt David J. , Labedzki Lothar
Published: March 2013

Twelve healthy volunteers received single oral doses of propranolol (80 mg), metoprolol (100 mg),l‐bunolol (2 mg), and placebo in a four‐way crossover study. Blood pressure, ventricular rate, and echocardiographically determined ejection fraction, ejection time, and mean rate of circumferential fiber shortening (mVcf) were measured before dosing and at multiple time points during 10 hours after each dose, with subjects maintained in the supine position. Reductions in systolic and diastolic blood pressure following administration of each of the beta blockers were greater than those observed with placebo, but differences among the four treatments were not significant. Heart rate reductions with the beta blockers differed significantly from placebo (P < .001), but differences among the three beta blockers were not significant. Differences among the four treatments in mVcf decrement did not attain significance at the 5% level (.05 < P < .1), and there were no significant differences in ejection‐time prolongation or ejection‐fraction reduction. Thus, reduced blood pressure, heart rate slowing, and reduced cardiac contractility may be associated with placebo treatment and may indicate the need for placebo controls in studies of the cardiovascular effects of beta blockers. Despite differing secondary pharmacologic properties, the three beta blockers reduced heart rate to a similar extent. Other effects of the beta blockers on blood pressure and cardiac contractility could not be consistently distinguished from those associated with placebo.
Lack of Effect of Cholestyramine on Phenytoin Bioavailability
Authors: Barzaghi N. , Monteleone M. , Amione C. , Lecchini S. , Perucca E. , Frigo G. M.
Published: March 2013

The effect of cholestyramine (4 g qid for 5 days) on the kinetics of phenytoin (400 mg orally) was investigated in normal subjects. Apart from a trend toward faster phenytoin absorption, the serum level profile of the drug during concurrent cholestyramine coadministration was similar to that observed in a control session. Areas under the serum phenytoin concentration curves were virtually identical in the two occasions. It is concluded that cholestyramine does not significantly affect the bioavailability of a single dose of phenytoin.
Comparative Bioavailability of Suprofen After Coadministration with Food or Milk
Authors: Chaikin Philip , Marriott Thomas B. , Simon David , Weintraub Howard S.
Published: March 2013

Suprofen is a nonsteroidal analgesic with demonstrated efficacy in the treatment of mild to moderate pain associated with a variety of clinical conditions. Because nonsteroidal analgesic agents may cause gastrointestinal side effects, they are frequently prescribed with food or milk. The purpose of this study was to evaluate the effects of a standard meal and milk alone on the rate and extent of absorption of suprofen. In a randomized three‐way cross‐over study, 24 healthy volunteers each received a single 200‐mg oral dose of suprofen in the fasted state half an hour after a standard meal or half an hour after an 8‐ounce glass of milk. The influence of food and milk was greater on the rate than on the extent of absorption of suprofen as illustrated by a more pronounced effect on Cmax than on AUC. In addition, food had a greater influence on the bioavailability of suprofen than milk. Food decreased the mean Cmax to 44% and the mean AUC to 81% relative to the fasted state, whereas milk decreased the mean Cmax to 74% and the mean AUC to only 87% of the respective parameters in the fasted state. Symmetrical confidence intervals demonstrated that the mean AUCmilk was within only 19% and the mean AUCfood was within only 25% of the mean AUC in the fasted state, with 95% confidence.
The Efficacy Results and Safety Profile of Imipenem/Cilastatin from the Clinical Research Trials
Authors: Calandra G. B. , Ricci F. M. , Wang C. , Brown K. R.
Published: March 2013

Imipenem/cilastatin is highly effective for infections in many body sites against a broad range of gram‐positive and gram‐negative aerobic and anaerobic bacteria. During therapy, development of resistance is uncommon except in the case of Pseudomonas aeruginosa in which the incidence appears similar to that for other beta‐lactam antibiotics. There appears to be a very low probability of cross‐resistance. The clinical and laboratory adverse reactions are similar in type to those for other beta‐lactam antibiotics. The frequency of colonization and superinfection during treatment with imipenem/cilastatin has been comparable to other antibiotics in comparative trials and to literature reports for other antibiotics for noncomparative trials.
Worsening of Ventricular Tachycardia by Amiodarone
Authors: Gallastegui Jose L. , Bauman Jerry L. , Anderson Jeffrey L. , Winkle Roger A. , Ezri Marilyn D. , Westveer Douglas C. , Swiryn Steven
Published: March 2013

The details of worsening of ventricular tachycardia in 8 (4.1%) of 194 patients receiving treatment with amiodarone are reported. Two forms of amiodarone‐induced tachycardia were recognized: first, the development of new tachycardias (three patients) and second, a change in the pattern of recurrence of clinical tachycardia (five patients). In retrospect, the time from the initiation of amiodarone to the initial documentation of worsening ranged from 1 to 23 days (mean ± SD, 9.4 ± 8.2 days) and the time from the initiation of therapy to the recognition of worsening ranged from 6 to 26 days (14.6 ± 10.1 days). Seven patients survived the worsening of tachycardia and one died. The total dose of amiodarone received and the duration of administration did not correlate with time to manifestation or time to resolution of worsening. This report emphasizes that worsening of ventricular tachycardia as a result of amiodarone is often difficult to differentiate from inadequate drug loading or early recurrence of 2 patient's clinical tachycardia. Further, because of the pharmacokinetics of the drug, the manifestations of worsening may be prolonged. In the cases reported, it ranged from 2 to 26 days (7.9 ± 8.3 days), which is longer than previously reported. Because of the potential for amiodarone to cause life‐threatening worsening of ventricular tachycardia and in accordance with current results, a period of in‐hospital monitoring of at least 10 days at the start of therapy with amiodarone is recommended.
Effects of Hetastarch and Albumin on Coagulation in Patients with Septic Shock
Authors: Falk Jay L. , Rackow Eric C. , Astiz Mark E. , Weil Max Harry
Published: March 2013

The effect of 6% hydroxyethyl starch (hetastarch) and 5% human serum albumin (albumin) infusion on coagulation in 12 patients with septic shock was evaluated. Patients were randomly assigned to receive either albumin (N = 6) or hetastarch (N = 6) infusion over a 24‐hour study interval. The prothrombin time (PT), partial thromboplastin time (PTT), and quantitative platelet count (PC) were obtained prior to and following 24 hours of fluid infusion. Hetastarch patients received 4934 ± 1354 mL and albumin patients received 3067 ± 256 mL over the study interval. After hetastarch infusion, the PT increased 2.2 ± 0.7 seconds, PTT increased 20.0 ± 4.1 seconds (P < .01), and PC decreased 158 ± 36 × 103/mm3 (P < .02). After albumin administration, the PT decreased 1.2 ± 1.7 seconds, PTT increased 20.5 ± 10.6 seconds and PC decreased 100 ± 34 × 103/mm3. There were no significant differences in the changes in PT, PTT, or PC between the groups. The authors conclude that hetastarch infusion does not result in increased bleeding in patients with septic shock compared with albumin infusion, despite moderate effects on the hemostatic coagulation profile.
Pharmacokinetics of Diltiazem in Patients Undergoing Continuous Ambulatory Peritoneal Dialysis
Authors: Grech‐Bélanger Odette , Langlois Serge , LeBoeuf Elizabeth
Published: March 2013

The disposition of a single oral dose of diltiazem hydrochloride was studied in six male patients treated by continuous ambulatory peritoneal dialysis. Peak concentrations were obtained 2 to 4 hours postdose. The mean absorption rate constant was 0.94 ± 0.21 (sd) hr‐1, and the mean elimination half‐life was 3.09 ± 1.16 hr. Serum levels of deacetyldiltiazem, a metabolite of diltiazem, were always below 10 ng/mL. The amounts of diltiazem and deacetyldiltiazem eliminated in dial ysate over 24 hours represent less than 0.1% of the administered dose. The pharmacokinetic parameters of diltiazem determined in these patients did not differ from those determined in healthy volunteers and in patients suffering from end‐stage renal disease.
Ethnicity and Ambulatory Blood Pressure Measurement: Relationship to Clinic and Laboratory Measurements
Authors: Schneiderman Neil
Published: March 2013

African Americans have a higher prevalence of hypertension than white Americans. Morbid consequences of hypertensive disease are greater in blacks than whites. For members of high‐risk groups such as blacks, ambulatory blood pressure monitoring may be useful in supplementing casual clinic measurements to prevent misdiagnosis, better characterize the temporal topography of blood pressure responses, and improve prediction of left ventricular hypertrophy, hypertensive complications, morbidity, and mortality. In conjunction with other data, laboratory experiments showing that African Americans as a group show greater peripheral resistance and slowed natriuretic responses to behavioral stressors than whites, appear to provide insights as to why blacks generally respond better to diuretics and calcium channel blockers than to β‐adrenergic antagonists or angiotensin‐converting enzyme inhibitors. It is suggested that ambulatory blood pressure monitoring and behavioral tasks in the laboratory may help predict individual responsiveness to antihypertensive agents.
The Effects of Estazolam on Sleep, Performance, and Memory: A Long‐Term Sleep Laboratory Study of Elderly Insomniacs
Authors: Vogel Gerald W. , Morris David
Published: March 2013

Insomnia, a common complaint among the elderly, is generally treated with benzodiazepines. Long‐acting benzodiazepines (e.g., Flurazepam) often produce daytime somnolence and performance deficits, whereas short‐acting drugs (e.g., triazolam) have been associated with marked rebound insomnia and anterograde memory loss. The authors designed a pilot study to evaluate the efficacy of an intermediate‐acting benzodiazepine, estazolam (e.g., ProSom), as well as its side effects. The parameters studied were sleep, daytime performance, and memory. Ten geriatric patients (>60 years of age) with insomnia participated in the study. They received placebo nightly for 2 weeks (baseline), estazolam 1 mg nightly for the next 4 weeks (treatment phase), and placebo again for 2 weeks (withdrawal period). Sleep was monitored by polysomnography the first two nights of each week in a sleep laboratory. Estazolam significantly decreased sleep latency, nocturnal awakenings, and wake time after sleep onset. Total sleep time increased an average of 63 minutes the first night of treatment. Significant improvements in wake time after sleep onset and total sleep time also were observed in the fourth week of estazolam treatment. Rebound insomnia occurred on the first withdrawal night only for wake time and total sleep time. By the next night, these sleep parameters returned to baseline. Neither daytime performance nor anterograde memory was adversely affected by estazolam treatment or its withdrawal. A 1‐mg dose of estazolam appears to be a safe and effective hypnotic for elderly patients with insomnia.
The Influence of Different Beta‐Blocking Drugs on the Peripheral Circulation in Raynaud's Phenomenon and in Hypertension
Authors: Franssen Casper , Wollersheim Hub , de Haan Anton , Thien Theo
Published: March 2013

In a double‐blind, randomized, placebo‐controlled study, the authors investigated the effects of different β‐adrenoceptor blocking drugs on the peripheral circulation. A single intravenous injection of the nonselective β‐blocker propranolol (0.20 mg/kg), the β1‐selective adrenoceptor blocker metoprolol (0.25 mg/kg), and the nonselective β‐blocker with partial agonistic activity (PAA) pindolol (0.04 mg/kg) and of placebo (saline) was given to eight patients with a primary Raynaud's phenomenon and to nine untreated patients with primary hypertension. The authors measured finger skin temperature (FST), and laser Doppler estimated finger skin blood flux (LDF) before, during, and after a standardized finger cooling test, performed 25 minutes after the administration of the drugs. In both patient groups propranolol, metoprolol, and pindolol had no significant effect on FST and LDF in the first 25 minutes after administration both in comparison to baseline value and to placebo. Also, no significant differences were found in the recoveries of FST and LDF after cold challenge between all drugs and placebo in both groups. The authors conclude that no adverse effect of any type of β‐adrenoceptor blocker in comparison to placebo could be detected after a single administration on both the baseline finger skin perfusion and the recovery after cold‐induced vasoconstriction. In addition, the authors could not demonstrate a favorable effect of β1‐selectivity or PAA in comparison to a nonselective β‐adrenoceptor blocker without PAA, in any group.
Effect of the Amount of Internal Standard on the Precision of an Analytical Method
Authors: Jemal Mohammed , Bergum James
Published: March 2013

In an earlier published paper,2 a confidence interval approach was used to show that the use of a large amount of internal standard (relative to the analyte) would adversely affect the precision of the analytical method. However, the confidence intervals were not calculated correctly. The authors recalculated the confidence intervals and found that there is no effect on the precision as measured by the confidence intervals.
Use of Angiotensin‐Converting Enzyme Inhibitors as Monotherapy and in Combination with Diuretics and Calcium Channel Blockers
Authors: Cheng Angela , Frishman William H.
Published: March 2013

Angiotensin‐converting enzyme (ACE) inhibitors have earned an important place in medical therapy since their discovery about two decades ago. This family of drug has grown tremendously since the introduction of captopril in 1981. There are currently more than 14 ACE inhibitors in the world and 9 are available in the United States. Although these agents share many similarities, they differ in their pharmacokinetic properties, approved indications, and cost. This paper provides guidance for selection of ACE inhibitors by examining the pharmacokinetics, pharmacodynamics, drug interactions, adverse effects, and cost of these agents. Combination products of ACE inhibitors with either diuretics or calcium channel blockers also are reviewed.
Effects of Oral and Intravenous Terazosin and Head‐up Tilt on Blood Pressure Responses in Patients with Hypertension
Authors: Achari Ramanuj , Hosmane Balakrishna , Linnen Paul , Cavanaugh John , Baroldi Paolo , Cohen Albert
Published: March 2013

Terazosin is a selective α1‐adrenoceptor antagonist. A double‐blind, randomized, placebo‐controlled, two‐period study evaluated the effects of posture and of oral and intravenous administration of terazosin on blood pressure and heart rate in patients with hypertension. At least one week after withdrawal of all antihypertensive medications, 31 patients with sitting diastolic blood pressure of 95 to 114 mmHg were enrolled in the study. After a 24‐hour, single‐blind, placebo lead‐in phase, the patients were randomized to receive either oral terazosin (1 mg on day 1, 2 mg on day 2, and 5 mg on days 3 and 4), a 12‐hour intravenous infusion of terazosin (2.5 mg, 5 mg, or 7.5 mg), or placebo for 4 consecutive days. Head‐up tilt (60° for 20 minutes) evaluations were performed before and 0.5, 1.5, 2.5, 6, 12, and 16 hours after start of administration during the placebo lead‐in phase and on each of the 4 days of the double‐blind treatment phase. Blood pressure and heart rate were monitored every 2 minutes during the 20‐minute tilt. Statistically significantly larger mean changes in blood pressure and heart rate were observed with the 7.5‐mg intravenous dose of terazosin compared with those after oral terazosin or placebo. With respect to intravenous terazosin, the orthostatic changes were maximal on the first day of the 4‐day treatment and increased with increasing doses of terazosin. Maximum orthostatic changes in blood pressure after oral administration of terazosin were not significantly different from those observed with placebo. The most common treatment‐emergent adverse events during tilt were dizziness and nausea. Dizziness occurred more frequently with intravenous terazosin than with oral terazosin. The results of this study indicate that oral dose titration of terazosin rather than a slower rate of terazosin infusion minimized the postural effects on blood pressure and associated symptoms during head‐up tilt.
Tramadol Hydrochloride: Analgesic Efficacy Compared with Codeine, Aspirin with Codeine, and Placebo after Dental Extraction
Authors: Moore Paul A. , Crout Richard J. , Jackson Douglass L. , Schneider Lawrence G. , Graves Robert W. , Bakos Lestor
Published: March 2013

Tramadol hydrochloride is a novel, centrally acting analgesic with two complementary mechanisms of action: opioid and aminergic. Relative to codeine, tramadol has similar analgesic properties but may have fewer constipating, euphoric, and respiratory depressant effects. A two‐center randomized double‐blind controlled clinical trial was performed to assess the analgesic efficacy and reported side effects of tramadol 100 mg, tramadol 50 mg, codeine 60 mg, aspirin (ASA) 650 mg with codeine 60 mg, and placebo. Using a third molar extraction pain model, 200 healthy subjects were enrolled in a 6‐hour evaluation after a single dose of drug. Of the 200 patients enrolled, seven provided incomplete efficacy data or discontinued prematurely and one was lost to follow‐up. Using standard measures of analgesia, including total pain relief score (TOTPAR), maximum pain relief score (MaxPAR), sum of pain intensity difference scores (SPID), peak pain intensity difference (Peak PID), remedication, and global evaluations, all active treatments were found to be numerically superior to placebo. ASA/codeine was found to be statistically superior to placebo for all measures of efficacy. Tramadol 100 mg was statistically superior to placebo for TOTPAR, SPID, and time of remedication, whereas tramadol 50 mg was statistically superior to placebo only for remedication time. Codeine was not found to be statistically superior to placebo for any efficacy measure. A greater TOTPAR response compared with all other active measures was seen for ASA/codeine during the first 3 hours of study. The 6‐hour TOTPAR scores for the tramadol groups and ASA/codeine group were not significantly different. Gastrointestinal side effects (nausea, dysphagia, vomiting) were reported more frequently with tramadol 100 mg, ASA/codeine, and codeine 60 mg than with placebo.
An Efficient Method for the Synthesis of 10‐Aminoartemisinin Derivative
Authors: Saha Pipas , Saikia Anil K.
Published: March 2013

An efficient method for the synthesis of 10‐aminoartemisinin derivative has been developed from 10‐acetoxyartemisinin and acetonitrile catalyzed by trimethylsilyltrifluoromethanesulfonate in good yield.
Redox‐ and pH‐Responsive Cysteamine‐Modified Poly(aspartic acid) Showing a Reversible Sol–Gel Transition
Authors: Gyarmati Benjámin , Vajna Balázs , Némethy Árpád , László Krisztina , Szilágyi András
Published: March 2013

Synthesis and characterization of a pH‐ and redox‐sensitive hydrogel of poly(aspartic acid) are reported. Reversible gelation and dissolution are achieved both in dimethylformamide and in aqueous medium via a thiol‐disulphide interconversion in the side chain of the polymers. Structural changes are confirmed by Raman microscopy and rheological measurements. Injectable aqueous solutions of thiolated poly(aspartic acid) can be converted into mechanically stable gels by oxidation, which can be useful for drug encapsulation and targeted delivery. Reduction‐facilitated release of an entrapped drug from disulphide cross‐linked hydrogels is studied.

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Fabrication of Mussel‐Inspired Highly Adhesive Honeycomb Films Containing Catechol Groups and Their Applications for Substrate‐Independent Porous Templates
Authors: Saito Yuta , Kawano Takahito , Shimomura Masatsugu , Yabu Hiroshi
Published: March 2013

Porous surface patterns are used in a wide variety of practical applications. Honeycomb‐patterned porous polymer films are good templates for preparing porous surfaces due to their simple fabrication and the arrangement of pores on the surface. Catechol groups include in adhesive protein of mussels have attracted much attention due to their highly and substrate‐independent adhesive properties. In this paper, highly and substrate‐independent adhesive honeycomb‐patterned porous polymer films are prepared by using amphiphilic copolymer having catechol moieties. Furthermore, porous surface patterns are transferred on various organic or inorganic substrates by wet etching with using adhesive honeycomb films as templates.

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In vivo effect of oat cereal β‐glucan on metabolic indexes and satiety‐related hormones in diet‐induced obesity C57‐Bl mice
Authors: Lin Ning , Li Yunming , Tang Lijun , Shi Jiaojiao , Chen Yi
Published: March 2013

This study explored the dose‐dependent effect of oat cereal β‐glucan on improving metabolic indexes of obesity mice. C57‐Bl mice were randomized to chow diet (N) group and high fat diet group and other three doses of oat β‐glucan groups (low β‐glucan, medium β‐glucan, and high β‐glucan). Energy intake, glucose, lipids, and appetite related hormones were tested. Dose‐dependent relation was observed on oat β‐glucan doses and body weight change, average energy intake, total cholesterol, HDL cholesterol, plasma neural peptide Y, arcuate neural peptide Y mRNA, and arcuate neural peptide Y receptor 2 mRNA level. Oat β‐glucan helped to increase plasma peptide Y‐Y and intestine peptide Y‐Y expression in obesity mice.
On best rank one approximation of tensors
Authors: Friedland S. , Mehrmann V. , Pajarola R. , Suter S.K.
Published: March 2013

Today, compact and reduced data representations using low rank data approximation are common to represent high‐dimensional data sets in many application areas as for example, genomics, multimedia, quantum chemistry, social networks, or visualization. To produce such low rank data representations, the input data is typically approximated by the so‐called alternating least squares (ALS) algorithms. However, not all of these ALS algorithms are guaranteed to converge. To address this issue, we suggest a new algorithm for the computation of a best rank one approximation of tensors, called alternating singular value decomposition. This method is based on the computation of maximal singular values and the corresponding singular vectors of matrices. We also introduce a modification for this method and the ALS method, which ensures that alternating iterations will always converge to a semi‐maximal point (a critical point in several vector variables is semi‐maximal if it is maximal with respect to each vector variable, while other vector variables are kept fixed). We present several numerical examples that illustrate the computational performance of the new method in comparison to the ALS method. Copyright © 2013 John Wiley & Sons, Ltd.
A revision of the quality of life‐breast cancer survivors (QOL‐BCS) instrument
Authors: Azuero Andres , Su Xiaogang , McNees Patrick , Meneses Karen
Published: March 2013

The importance of quality of life (QOL) measurement among breast cancer survivors (BCS) is well‐recognized by researchers and clinicians. With data from 427 rural BCS, the authors used a combination of clinical expertise and statistical analysis to revise a 48‐item measure of QOL specific to BCS. The revised 15‐item measure showed adequate psychometric properties and provides the basis for a brief yet comprehensive multidimensional measure of QOL applicable to most BCS. Future work includes fine‐tuning the measurement model and examining its generalizability among non‐rural BCS. © 2013 Wiley Periodicals, Inc. Res Nurs Health 36: 423–434, 2013
Lowering the dielectric constant of polyimide thin films by swelling with supercritical carbon dioxide
Authors: Ronova Inga A. , Bruma Maria , Kuznetsov Alexander A. , Nikolaev Alexander Yu.
Published: March 2013

The swelling with supercritical carbon dioxide (sc‐CO2) of thin films of polyimides having various structures was investigated. It was shown that the degree of swelling is significantly influenced by the solvent which was used for the synthesis of those polyimides, by the solvent which was used for the preparation of thin films and by the conformational rigidity of the polymers. The presence of hexafluoroisopropylidene groups in the main chain of a polymer prevents its swelling with sc‐CO2. The best results were obtained for polyimide film ULTEM, based on m‐phenylene‐diamine and isopropylidene‐diphenoxy‐bis(phthalic anhydride), synthesized in benzoic acid, whose free volume increased twice and its dielectric constant decreased from 3.15 to 2.45 by swelling with sc‐CO2. Copyright © 2013 John Wiley & Sons, Ltd.
Eco‐friendly conductive polymer nanocomposites (CPC) for solar absorbers design
Authors: Antar Zied , Feller Jean‐François , Vignaud Guillaume
Published: March 2013

To reduce both the cost and the environmental impact of copper‐based thermal solar absorbers, we have investigated their possible substitution by bio‐based conductive polymer nanocomposite (CPC) elements. Our results show that carbon nanotubes (CNT) have no significant influence on polymers’ calorimetric properties such as Tm and Tg but lead to a strong increase in crystallinity of poly(lactic acid) (PLA) and to a lesser extent of poly(amide 12) poly(amide 12) (PA12) for 2 and 3 CNT wt % respectively. Percolation thresholds as low as 0.5 and 0.58 were obtained for PA12 and PLA, respectively, and visco‐elastic properties such as η*, G’ and G” were found to increase exponentially with CNT content confirming the formation of a CNT network within the matrix. All CPC are absorbing more energy in the visible and infrared than in the ultraviolet wavelength ranges. Finally, the thermal conductivity k of PLA–CNT and PA12–CNT were increased, respectively, of 85% and 24%, to reach 0.28 W.m−1.K−1 and 0.26 W.m−1.K−1, for only 5 wt% CNT. The figure of merit suggests that PA12 is the polymer which satisfies at best all criteria, particularly combining a lower viscosity at almost equivalent thermal conductivity and absorptivity. Copyright © 2013 John Wiley & Sons, Ltd.
Guideline for the prevention of acute nausea and vomiting due to antineoplastic medication in pediatric cancer patients
Authors: Dupuis L. Lee , Boodhan Sabrina , Holdsworth Mark , Robinson Paula D. , Hain Richard , Portwine Carol , O'Shaughnessy Erin , Sung Lillian
Published: March 2013

This guideline provides an approach to the prevention of acute antineoplastic‐induced nausea and vomiting (AINV) in children. It was developed by an international, inter‐professional panel using AGREE and CAN‐IMPLEMENT methods. Evidence‐based interventions that provide optimal AINV control in children receiving antineoplastic agents of high, moderate, low, and minimal emetogenicity are recommended. Recommendations are also made regarding selection of antiemetic agents for children who are unable to receive corticosteroids for AINV control, the role of aprepitant and optimal doses of antiemetic agents. Gaps in the evidence used to support the recommendations were identified. The contribution of this guideline to AINV control in children requires prospective evaluation. Pediatr Blood Cancer 2013; 60: 1073–1082. © 2013 Wiley Periodicals, Inc.
Quantitative Comparison of Multiple Components in Dioscorea nipponica and D. panthaica by Ultra‐High Performance Liquid Chromatography Coupled with Quadrupole Time‐of‐Flight Mass Spectrometry
Authors: Tang Yina , Yi Tao , Chen Homing , Zhao Zhongzhen , Liang Zhitao , Chen Hubiao
Published: March 2013

Introduction

Dioscorea nipponica (DN) and D. panthaica (DP) have been uniquely prepared as herbal medicinal products for treating coronary heart disease (CHD) in China. However, so far there has been little discussion and no work comparing the qualitative and quantitative differences between the two herbs nor assessing whether they have similarities in chemical composition that would support their common application for treating CHD.

Objective

To develop an efficient and reliable method based on UPLC–qTOF–MS for quantitative comparison of saponins in both DN and DP.

Methods

Using electrospray ionisation and atmospheric‐pressure chemical ionisation respectively, six steroidal glycosides and one aglycone were determined in 13 DN samples and 13 DP samples. The comparative analysis of chemical components in DN and DP was carried out by chromatographic fingerprint similarity evaluation, test of significance (t‐test) and principle component analysis (PCA).

Results

The UPLC–qTOF–MS method showed limit of detection and quantitation within the range 0.02–0.2 ng and 0.08–0.5 ng, respectively, for the seven saponins studied. The intra‐ and interday precision (RSD) were below 5%. The recoveries for the quantified compounds were within the range of 72.79–118.31%.

Conclusion

This UPLC–qTOF–MS assay provides a suitable method for the identification and determination of major bioactive constituents both in DN and DP. The chemical composition of all DN and DP samples studied exhibited a high level of global similarity. This chemical similarity validates their common application in the pharmaceutical industry as anti‐CHD herbal drugs. Copyright © 2013 John Wiley & Sons, Ltd.
Synthesis and properties of hyperbranched polyimides derived from novel triamine with prolonged chain segments
Authors: Shen Jie , Zhang Ying , Chen Wenqiu , Wang Wenhao , Xu Zushun , Yeung Kelvin W. K. , Yi Changfeng
Published: March 2013

Novel pyridine‐containing hyperbranched polyimides (HBPIs) were synthesized by using a new triamine 2,4,6‐tris[3‐(4‐aminophenoxy)phenyl]pyridine with prolonged chain segments, ether linkage and meta‐linked units as a BB′2‐like monomer, various commercial aromatic dianhydrides as A2 monomers. Most of the obtained HBPIs were readily soluble in common organic solvents such as N,N‐dimethylformamide, N,N‐dimethylacetamide, N‐methyl‐2‐pyrrolidone, m‐Cresol, and so forth. Meanwhile, they also had good thermal stability with the glass transition temperatures (Tgs) all above 210 °C, the temperature at 10% weight loss of 537.1–574.4 °C in nitrogen atmosphere. Strong and flexible HBPI films were obtained, which had good mechanical properties with tensile strengths of 83.3–95.8 MPa, tensile modulus of 1.82–2.43 GPa and elongations at break of 4.84–6.98%. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 2425–2437
Synthesis of block and end‐functionalized polyesters by triflimide‐catalyzed ring‐opening polymerization of ε‐caprolactone, 1,5‐dioxepan‐2‐one, and rac‐lactide
Authors: Makiguchi Kosuke , Kikuchi Seiya , Satoh Toshifumi , Kakuchi Toyoji
Published: March 2013

The ring‐opening polymerization (ROP) of cyclic esters, such as ε‐caprolactone, 1,5‐dioxepan‐2‐one, and racemic lactide using the combination of 3‐phenyl‐1‐propanol as the initiator and triflimide (HNTf2) as the catalyst at room temperature with the [monomer]0/[initiator]0 ratio of 50/1 was investigated. The polymerizations homogeneously proceeded to afford poly(ε‐caprolactone) (PCL), poly(1,5‐dioxepan‐2‐one) (PDXO), and polylactide (PLA) with controlled molecular weights and narrow polydispersity indices. The molecular weight determined from an 1H NMR analysis (PCL, Mn,NMR = 5380; PDXO, Mn,NMR = 5820; PLA, Mn,NMR = 6490) showed good agreement with the calculated values. The 1H NMR and matrix‐assisted laser desorption ionization time‐of‐flight mass spectrometry analyses strongly indicated that the obtained compounds were the desired polyesters. The kinetic measurements confirmed the controlled/living nature for the HNTf2‐catalyzed ROP of cyclic esters. A series of functional alcohols, such as propargyl alcohol, 6‐azido‐1‐hexanol, N‐(2‐hydroxyethyl)maleimide, 5‐hexen‐1‐ol, and 2‐hydroxyethyl methacrylate, successfully produced end‐functionalized polyesters. In addition, poly(ethylene glycol)‐block‐polyester, poly(δ‐valerolactone)‐block‐poly(ε‐caprolactone), and poly(ε‐caprolactone)‐block‐polylactide were synthesized using the HNTf2‐catalyzed ROP. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 2455–2463