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Update on novel anticoagulants
Update on novel anticoagulants

... Heparin was first discovered in 1916 by Jay Mc Lean and William Harry Howell Use of heparin in clinical practice was 20 years later Low molecular weight heparin was discovered in 1976 with clinical trials starting in the early 1980’s Sweet clover disease lead to the discovery of the first oral antic ...
Dabigatran - Surgical Critical Care. Net
Dabigatran - Surgical Critical Care. Net

... Prothrombin complex concentrates (PCC) are derived from human plasma and contain the vitamin Kdependent coagulation factors II, VII, IX, and X at varying concentrations. PCC is commonly used for vitamin K antagonist reversal and there have been trials using this therapy for reversal of non-vitamin K ...
Heparin May Be Hard to Beat - JACC: Cardiovascular Interventions
Heparin May Be Hard to Beat - JACC: Cardiovascular Interventions

... that the use of a continued (4 h) infusion of bivalir- ...
Objectives Aspirin Aspirin Kinetics
Objectives Aspirin Aspirin Kinetics

... STEMI patients with symptom onset within the prior 12 hours and 12-lead ECG findings consistent with a true posterior MI. In the absence of contraindications, it is reasonable to administer fibrinolytic therapy to patients with symptoms of STEMI beginning in the prior 12 to 24 hours who have continu ...
Blood Cancers
Blood Cancers

... Left and Middle Image from: http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cbc26e3c-aee9-4c0d-bdb1-bf350308fbce Right Image from: http://www.ismp.org/NAN/files/NAN-20130610.pdf ...
Antithrombotic agents: Implications in dentistry ORAL MEDICINE
Antithrombotic agents: Implications in dentistry ORAL MEDICINE

... patients having major surgery. LMWH is now the treatment of choice for patients undergoing total hip or knee replacement because of its superior efficacy compared with SC standard heparin in the prevention of thromboembolism (Table I). LMWH is prepared by depolymerization of unfractionated heparin c ...
OCR Document
OCR Document

... (blood in urine), abrupt decrease in hemoglobin/hematocrit III. Low molecular weight heparins (LMWH)---longer half-life therefore can be given QD-BID -less or no lab monitoring needed -slightly fewer bleeding complications 1. indications a. approved---hip, knee or abdominal surgery (prevent DVT), so ...
Newsletter
Newsletter

... concluded that apixaban was in fact not only safe but superior to warfarin in this regard. Apixaban is an oral, reversible, and selective inhibitor of factor Xa, and the recommended dose for most patients is 5mg by mouth twice a day. The dosing for apixaban does not need to be adjusted for renal imp ...
Pharmacy Updates in Cardiology
Pharmacy Updates in Cardiology

... • Currently in Phase III Clinical Trial – Approved in Japan ...
Factors that may cause Bleeding with Enoxaparin
Factors that may cause Bleeding with Enoxaparin

... • Enoxaparin is in a class of medications called low molecular ...
Reproducibility and Changes in Ejection Fraction (EF) Measured by
Reproducibility and Changes in Ejection Fraction (EF) Measured by

... p<.OOl). In both the VT and the control group changes were similar (differences NS): tQRS and LAS durations were prolonged by 282 11% vs 2 5 r 14% and by 66270% vs 102+58%, RMS40 voltage was reduced by 45234% vs 53+25%, respectively. Before F infusion, STM was abnormal in 8 VT pts and in 1 control. ...
Section: 2-1
Section: 2-1

... a. Prophylaxis of Deep Vein Thrombosis (DVT.) b. Treatment of acute DVT. c. Complications of unstable angina. d. Treatment of acute ST-segment elevation myocardial infarction. 2. Under normal circumstances, there is no need for daily monitoring of the effect of Lovenox in patients with normal baseli ...
Metrifonate
Metrifonate

... hour of oral administration  it undergoes little protein binding <15% • Metabolism:  It is a prodrug  biotransformation of mertifonate occurs independently of the hepatic cytochrome P450  It is slowly and non-enzymatically transformed to DDVP which is PH dependent  Serum t½ is 2 hours ...
Chapter 12 Section F: Blood and Hemostasis
Chapter 12 Section F: Blood and Hemostasis

... What is the abnormality in persons with sickle cell anemia? What causes the cells to assume a sickle shape and how does this interfere with blood flow? What is polycythemia and how does this affect blood viscosity and blood flow? How are the leukocytes visibly distinguishable based on cytoplasmic st ...
Anticaog_update_R_Maclean
Anticaog_update_R_Maclean

... VTE prevention after elective hip or knee replacement surgery Stroke prevention in Atrial Fibrillation Deep Vein Thrombosis treatment and secondary prevention Pulmonary Embolism treatment and secondary prevention Acute coronary syndromes ...
05- Venous Thromboembolism
05- Venous Thromboembolism

... Management of Toxicity: • Patients with a mildly elevated INR (3.5 to 5) and no signs or symptoms of bleeding can usually be managed by either reducing the dose or holding one or two warfarin doses. • If rapid reduction of an elevated INR is required, oral or IV administration of vitamin K1 (phyton ...
Dabigatran
Dabigatran

... Stroke from Atrial Fibrillation • AF is the most preventable cause of stroke: – 12-16 million will be on warfarin treatment by 2050 in the US – Clinical trials have shown stroke can be reduced: ...
Anticoagulation Antidote Guide
Anticoagulation Antidote Guide

...  If ingested within 2 hours, administer activated charcoal  For life threatening bleed or emergency surgery, consider idarucizumab (Praxbind) 5 gm IV (non-formulary drug at Harris/Swain)  65% removed by HD NOTES: Plasma dabigatran concentrations can increase more than 12-24 hours after administra ...
Managing Atrial Fibrillation 2016: Anticoagulation, Pharma and
Managing Atrial Fibrillation 2016: Anticoagulation, Pharma and

... Small concern about myocardial infarction and arterial thromboembolism ...
Cardiovascular system pharmacology
Cardiovascular system pharmacology

... Heparin is not given orally because it will be destroyed by stomach acidity, so it must be given by IV or deep subcutaneous but not I.M because it will be produce hematoma LMW heparins have a longer half-life than standard heparin and a single dose by subcutaneous injection is as effective as IV hep ...
Anti-anemics
Anti-anemics

... following myocardial infarction), deep vein thrombosis. – MOA: Inhibits factor Xa, very little effect on factor IIa; aPPT is not used to measure its anticoagulant activity. Binds less to plasma proteins. – Pharmacokinetics: Administration: i.v. and s.c. outpatient basis for DVT patients. Immediate o ...
Warfarin (Coumadin®, Jantoven®) Considerations for Use*
Warfarin (Coumadin®, Jantoven®) Considerations for Use*

... Previously stabilized warfarin patients often have elevated INRs when admitted with decompensated heart failure. This often requires holding or reducing warfarin dose by ~50% for 1-2 days after admission, but as they diurese and improve, they often require their previous warfarin does. May take 3 to ...
Cardiopulmonary Bypass
Cardiopulmonary Bypass

... – Mainly membrane oxygenation replacing bubble and discs. – Oxygen flows along the microtubules and bloods. – Over time deposits accumulate and resistance increases, heparin coating of oxygenation surfaces might serve to reduce this effect. ...
Potent inhibition of thrombin with a monoclonal
Potent inhibition of thrombin with a monoclonal

... was observed with a dose-related pattern. Notably, the majority of spontaneous bleeding episodes were clinically consistent with platelet-mediated bleeding (e.g. gum, tongue) without thrombocytopenia. The median terminal half-life was 72.2 (25th, 75th: 28.4, 72.5) h. Conclusion Sunol-cH36 exhibited ...
Pharmacotheraputics
Pharmacotheraputics

... MOA: inhibits vitamin K epoxide reductase leading to inhibition of reduction of vitamin K, which is required for carboxylation (and activation) of factors II, VII, IX and X, as well as proteins C, S and Z o Inhibits the above factors o Inhibition of II, VII, IX, and X prevents extension and propagat ...
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Discovery and development of direct thrombin inhibitors



Direct thrombin inhibitors (DTIs) are a class of anticoagulant drugs that can be used to prevent and treat embolisms and blood clots caused by various diseases. They inhibit thrombin, a serine protease which affects the coagulation cascade in many ways. DTIs have undergone rapid development since the 90's. With technological advances in genetic engineering the production of recombinant hirudin was made possible which opened the door to this new group of drugs. Before the use of DTIs the therapy and prophylaxis for anticoagulation had stayed the same for over 50 years with the use of heparin derivatives and warfarin which have some well known disadvantages. DTIs are still under development, but the research focus has shifted towards factor Xa inhibitors, or even dual thrombin and fXa inhibitors that have a broader mechanism of action by both inhibiting factor IIa (thrombin) and Xa. A recent review of patents and literature on thrombin inhibitors has demonstrated that the development of allosteric and multi-mechanism inhibitors might lead the way to a more safer anticoagulant.
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