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Linköping University Post Print Effects of the oral, direct thrombin inhibitor
Linköping University Post Print Effects of the oral, direct thrombin inhibitor

... thrombosis. Millions of patients have been treated and the knowledge of pros and cons of this very efficient drug is well established, including effects on coagulation assays. One of the draw backs is the need for monitoring by measuring prothrombin time to achieve appropriate degree of anticoagulat ...
File - Doctorswriting
File - Doctorswriting

... Heparin binds to antithrombin and accelerates reactions between antithrombin and clotting factor proteases 100 fold. Heparin causes severe thrombocytopaenia in 10% of patients. Heparin crosses the placenta easily and thus should not be used in pregnancy. Long term use of heparin is associated with m ...
Cardiology ACCP PRN Journal Club: Hokusai
Cardiology ACCP PRN Journal Club: Hokusai

... The origin of this recommendation seems unclear. The edoxaban package insert refers to a section (14.2) that summarizes the Hokusai-VTE study results but does not explain the decision to recommend use in patients with CrCl 15-30 ml/min.2 The meeting minutes from the FDA Advisory Committee meeting ar ...
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... living thing invades the body. However, a disease is anything which affects the proper functioning of the body. It can be an infection, a genetic disorder, or the result of environmental conditions such ...
Inhibitors of Factor VIIa/Tissue Factor
Inhibitors of Factor VIIa/Tissue Factor

... inhibitors of the FVIIa/TF pathway in preclinical models and clinical trials1,2 has led to substantial interest in the development of orally active small molecule inhibitors of the enzyme active site that could be used for the long-term prevention or treatment of thrombosis. Vitamin K antagonists su ...
Department of Pharmacy
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Anticoagulation Guidelines for Reversal
Anticoagulation Guidelines for Reversal

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A low molecular weight, selective thrombin inhibitor, inogatran, vs
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... Unfractionated heparin-cont’d • Monitoring parameters – aPTT at 1.5-2.5 times control values – aPTT q6h after initiating therapy and after subsequent dosage adjustment – Once 2 consecutive aPPTs within the target, aPTT q24h – PLT, Hct/Hgb ...
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New Drugs Update from APC

... Recently there have been warnings relating to drug-induced QT prolongation for three commonly used drugs – citalopram, domperidone and ondansetron. This Medicines Q+A discusses the issues to be considered when assessing the risk of drug induced QT prolongation in individual patients. The American we ...
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Patients With a History of HIT Who Require Cardiac Surgery

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or S-warfarin
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... Inducers increase the metabolism of substrates  decreased efficacy For example, for CYP 2C9, both amiodarone and carvedilol will increase the efficacy of celecoxib, but barbiturates will reduce it ...
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VIOXX (ROFECOXIB)

... ROFETAB is a non-steroidal anti-inflammatory drug (NSAID) that exhibits antiinflammatory, analgesic and antipyretic activity. It acts by selectively inhibiting the enzyme cyclooxygenase-2 (COX-2), thus arresting the synthesis of inflammatory prostaglandins. At therapeutic concentrations, ROFETAB doe ...
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All of the following mechanism of action correctly match a drug
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... C. Sulfonylureas increase glucagons secretion. D.Sulfonylureas increase both the release of insulin and the insulin-sensitivity of target tissue. E. Sulfonylureas block the insulin receptors. 40. Which of the following is not true? A. one of the most common side effects of oral hypoglycemic agents i ...
mr-afib
mr-afib

... • apixaban was associated with lower risk (hazard ratio [HR] 0.67, 95% CI 0.46–0.98, P=0.04) • dabigatran and rivaroxaban were associated with a similar risk (dabigatran: HR 0.98, 95% CI 0.76– ...
PRODUCT MONOGRAPH ARGATROBAN (argatroban for injection
PRODUCT MONOGRAPH ARGATROBAN (argatroban for injection

... Argatroban to patients with hepatic disease, by starting with a lower dose and carefully titrating until the desired level of anticoagulation is achieved. Achievement of steady state aPTT levels may take longer and require more Argatroban dose adjustments in patients with moderate hepatic impairment ...
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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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