Dirofilaria immitis is a parasitic nematode that survives in the circulatory system of suitable hosts for many years, causing the most severe thromboembolisms when simultaneous death of adult worms occurs. The two main mechanisms responsible for thrombus formation in mammals are the activation and aggregation of platelets and the generation of fibrin through the coagulation cascade. The aim of this work was to study the anticoagulant potential of excretory/secretory antigens from D. immitis adult worms (DiES) on the coagulation cascade of the host. Anticoagulant and inhibition assays respectively showed that DiES partially alter the coagulation cascade of the host and reduce the activity of the coagulation factor Xa, a key enzyme in the coagulation process. In addition, a D. immitis protein was identified by its similarity to the homologous serpin 6 from Brugia malayi as a possible candidate to form an inhibitory complex with FXa by sodium dodecyl sulfate polyacrylamide gel electrophoresis and mass spectrometry. These results indicate that D. immitis could use the anticoagulant properties of its excretory/secretory antigens to control the formation of blood clots in its immediate intravascular habitat as a survival mechanism.

X-ray powder diffraction data, unit-cell parameters, and space group for 17- hydroxy-16-methyl-9,11-epoxypregna-1,4,6-triene-3,20-dione, C22H26O4, are reported [ a = 18.435(1) Å, b = 12.269(3) Å, c = 8.251(5) Å, α = 90°, β = 90°, γ = 90°, unit-cell volume V = 1866.43 Å3, Z = 4, ρcal = 1.261 g cm−3 and space group P212121]. All measured lines were indexed and are consistent with the P212121 space group. No detectable impurities were observed.

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7- tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester is an important intermediate in the synthesis of the anticoagulant, apixaban. X-ray powder diffraction data for this compound are reported [a = 14.101(4) Å, b = 10.105(6) Å, c = 9.532(7) Å, α = 72.774(1)°, β = 97.356(3)°, γ = 108.237(3)°, unit-cell volume V = 1231.45 Å3, Z = 2, and space group P-1]. No detectable impurities were observed.

X-ray powder diffraction data, unit-cell parameters, and space group for Ethyl (Z)-2-chloro-2-[2-(4-methoxyphenyl)hydrazin-1-ylidene]acetate, C11H13ClN2O3, are reported [a = 13.308(4) Å, b = 9.908(5) Å, c = 4.753(4) Å, α = 90°, β = 91.510(8)°, γ = 90°, unit-cell volume V = 626.64 Å3, Z = 2, ρcal = 1.361 g cm−3, and space group P21]. All measured lines were indexed and are consistent with the P21 space group. No detectable impurities were observed.

X-ray powder diffraction data for 5,6-dihydro-3-(4-morpholinyl)-1-[4-(2-oxo-1-piperidinyl)phenyl]-2(1H)-pyridinone, C20H25N3O3, are reported [a = 5.989(2), b = 6.669(3), c = 24.605(5)Å, α = 84.466(7)°, β = 89.859(6)°, γ = 69.074(4)°, unit-cell volume V = 913.11 Å3, Z = 2, and space group P−1]. No detectable impurities were observed.

Introduction: Injured seniors visits are on the rise in the emergency department (ED) and up to 30 % are traumatic brain injury (TBI). Many patients suffer from comorbidities that require the use of anticoagulant drugs. The use of these drugs usually modify the trajectory patients will undergo in the ED. In the last decade, some authors suggested a systematic follow-up CT head scan 8 hours after the initial, while others didn’t see the need to scan, referring only to the clinical features. We sought to evaluate the presence of delayed intracranial bleeding, evolution and investigation at the ED of elderly patients presenting for a mild TBI, with or without anticoagulotherapy. Methods: A retrospective cohort was built with hospital administrative clinical data for year 2014 at a Canadian Level 1 trauma center. Patients 65 years and older with traumatic brain injury and residing in the trauma center catching area were included. Data were extracted from medical files using a standardized collection tool in a consecutive pattern. Patients were classified in three groups: use of anticoagulant drug, use of antiplatelet drug and no anticoagulotherapy. Clinico-administrative data, intervention delay, investigations, comorbidities, medication and physiological status were collected. Intra and extra-hospital data were collected for a period of 90 days and the use of imaging and trajectories were analysed. Univariate and multivariate analysis were conducted. Results: 93 of the 189 TBI injury were mild TBI. The 93 patients were divided in patients using anticoagulotherapy (n = 9, 10 %), using antiplatelet drug (n = 58, 62.4 %) and no use of drug (n = 29, 31.2 %). Each group respectively undergo an initial head CT scan in a proportion of 88.9 %, 93 % and 76 %. Follow-up head CT scan were seen in 43 %, 16 % and 10 %. Delayed intra-cranial hemorrhage were identified in respectively 0 %, 2 % and 0 %. Conclusion: With the increase in patients presenting at Canadian ED for head trauma, our study suggests that anticoagulated elderly patients suffering from a mild traumatic brain injury do not systematically require a follow up CT head scan or longer observation time at the ED. A future clinical decision rule to determine the need of follow-up CT could be of benefit to emergency physicians.

Apixaban (Eliquis®) is a novel oral pyrazole-based direct FXa inhibitor. The title compound is an intermediate in the synthesis of the anticoagulant, Apixaban. X-ray powder diffraction data for the title compound, are reported [a = 9.511(5) Å, b = 18.539(2) Å, c = 5.645(3) Å, α = 90°, β = 101.813(1)°, γ = 90°, unit-cell volume V = 974.28 Å3, Z = 2, ρcal = 1.336 g cm−3, and space group P2]. All measured lines were indexed and are consistent with the P2 space group. No detectable impurities were observed.

X-ray powder diffraction data for 1-(4-aminophenyl)-5,6-dihydro-3-(4-morpholinyl)-2(1H)-pyridinone, C15H19N3O2, are reported [a = 14.877(4) Å, b = 5.893(6) Å, c = 18.984(3) Å, α = 90°, β = 122.298(3)°, γ = 90°, unit-cell volume V = 1406.86 Å3, Z = 4, and space group P21/c]. All measured lines were indexed and are consistent with the P21/c space group. No detectable impurities were observed.

X-ray powder diffraction data for 5-Chloro-N-(4-nitrophenyl)pentanamide, C11H13ClN2O3, are reported [a = 8.036(4) Å, b = 15.972(5) Å, c = 9.829(5) Å, α = 90°, β = 104.227(2)°, γ = 90°, V = 1222.98 Å3, Z = 4, ρx = 1.3941 g cm−3 and space group P21/c]. All measured lines were indexed and are consistent with the P21/c space group. No detectable impurities were observed.

X-ray powder diffraction data for 3-(4-Morpholinyl)-1-(4-nitrophenyl)-5,6-dihydro-2(1H)-pyridinone, C15H17N3O4, are reported [a = 7.112(1) Å, b = 33.360(2) Å, c = 6.265(1) Å, α = 90°, β = 94.037(1)°, γ = 90°, V = 1483.08 Å3, Z = 4, ρcal = 1.358 g cm−3 and space group P21]. All measured lines were indexed and are consistent with the P21 space group. No detectable impurities were observed.

X-ray powder diffraction data for 3,3-dichloro-1-(4-nitrophenyl)-2-piperidinone, C11H10Cl2N2O3, are reported [a = 11.088(4) Å, b = 11.594(5) Å, c = 12.689(3) Å, α = 118.456(1)°, β = 100.320(3)°, γ = 107.763(3)°, V = 1259.27 Å3, Z = 4 and space group P-1 ]. All measured lines were indexed and are consistent with the P-1 space group. No detectable impurities were observed.

Warfarin dosing for thromboprophylaxis in post-operative patients is time-consuming. Warfarin-dosing nomograms can be used in post-operative arthroplasty patients, but warfarin requirements are lower in frail older people. We modified an existing post-arthroplasty nomogram to a frail-friendly version and evaluated its performance in a frail elderly post-orthopaedic surgery on a geriatric rehabilitation ward to determine if it would improve quality indicators for oral anticoagulation. On a geriatric rehabilitation unit, post-operative orthopaedic patients were assigned to either physician-adjusted warfarin dosing or the nursing-administered nomogram. The proportion of days within target INR values was significantly higher in the nomogram group (77%, 95% CI 74% to 81%) compared to the physician-adjusted group (53%, 95% CI 46% to 60%), with no major bleeding or thromboembolic complications. The number of warfarin-related telephone calls to physicians was significantly reduced by tenfold. Use of a frail-friendly nomogram improved quality and efficiency of patient care on a geriatric rehabilitation unit.

The effects of larval stages of Ascaris lumbricoides on human blood clotting was studied in vitro. Extracts and excretory/secretory products of third-stage larvae (L3) and late third-stage larvae (LL3) cultured from ova obtained from infected patients were analysed for anti-coagulant activity. Prothrombin time (PT) was prolonged by the addition of either whole extract of L3/LL3 or ES products of L3/LL3 as compared to controls. Partial thromboplastin time with kaolin (PTTK) was also prolonged on the addition of either extracts of ES products of L3/LL3. The prolongation of PTTK was significantly higher with extracts/ES products of L3 when compared to the extracts/ES products of LL3 (p<0.005). Thrombin time (TT) was prolonged by extracts of L3/LL3 and their ES products.

Objectives: This assessment sought to evaluate the comparative benefit and adverse effect profile of ximelagatran, as well as the clinical issues surrounding its potential use.

Methods: We performed a Dialog OneSearch across BIOSIS Previews, EMBASE, MEDLINE, PASCAL, and ToxFile to identify published literature. PubMed and The Cochrane Library were also searched. Gray literature was identified by searching a variety of Web sites of health technology assessment and related agencies and their associated databases. The manufacturer's Canadian office, AstraZeneca, was invited to submit information.

Results: Ximelagatran is the first oral agent from a new class of anticoagulants called direct thrombin inhibitors. Other oral anticoagulants require routine blood monitoring; ximelagatran does not. Ximelagatran has been evaluated in the areas of venous thromboembolism management, particularly after orthopedic surgery, and stroke prevention in patients with atrial fibrillation. Overall, ximelagatran's efficacy appears comparable to other anticoagulants in these clinical settings. Also, bleeding rates were generally similar between ximelagatran and comparators but, as for warfarin, bleeding risk increases with higher ximelagatran doses. In addition, there is no specific antidote to help manage ximelagatran-induced bleeding. Finally, significantly more patients exposed to long-term ximelagatran developed elevated liver enzymes more than three times the upper normal limit, compared with patients on comparator anticoagulants.

Conclusions: Given its apparent simplicity of use, ximelagatran carries the potential to replace, at least in part, anticoagulants currently used in the management of venous thromboembolism or for preventing stroke in atrial fibrillation patients. However, the safety of ximelagatran will not be fully known without further evaluation and surveillance for potential liver toxicity. There is also a need to evaluate its use in special populations such as patients with renal failure and patients using several concurrent medications.