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Thrombin = anticoagulant
Thrombin = anticoagulant

... – After oral administration, the prodrug dabigatran etexilate is rapidly converted to dabigatran, a potent reversible Direct Thrombin Inhibitor (DTI) – Absolute bioavailability ~ 6.5 % – Fast onset of action (Cmax within 2h) – Not metabolized by CYP450 / Renal excretion ~80% – Half life 12-17 hours ...
Anticoagulants
Anticoagulants

... • Fast action intravenously or by injection (not absorbed through the stomach or intestinal wall) • peak after injection 2 - 4 hr • Complex metabolism (long chains broken up) • half life 1 - 5 hr; cleared by the reticuloendothelial system and some excreted in urine. • A few Drug-drug interactions • ...
Review: New oral anticoagulants reduced stroke and systemic
Review: New oral anticoagulants reduced stroke and systemic

... • AT + Heparin: conformational change in AT = 1000-4000 fold acceleration in inactivation • At high concentrations: Also binds to platelets and heparin co-factor II—which inhibits thrombin ...
Drugs Used in Coagulation Disorders
Drugs Used in Coagulation Disorders

... – To prevent restenosis after coronary angioplasty – In acute coronary syndromes (unstable angina and non-Qwave acute MI) ...
Preventing Anticoagulation Errors with Clinical Dashboards
Preventing Anticoagulation Errors with Clinical Dashboards

... Alert values for various drugs Concurrent monitoring of target drugs Focus on “at risk” patients when we cannot follow every patient • Resolve alerts and communicate information w. providers and other pharmacists ...
CVS 5
CVS 5

...  Can be used in hospital as well as out-patient ...
pharm 22 A [4-20
pharm 22 A [4-20

... [don’t FIB about being sick] i. used for ischemic events and during/after coronary intervention b. major bleeding c. abciximab binds GPIIb-IIIa site irreversibly (other 2 don't) so it can be reversed w/ admin of fresh platelets; with eptifibatide and tirofiban just have to wait it out 4 classes of a ...
oral direct thrombin inhibitors
oral direct thrombin inhibitors

... treated with UFH for a minimum of 7 days. Patients who develop HIT are treated by discontinuance of heparin and administration of a direct thrombin inhibitor. ...
Drugs Used in Coagulation Disorders
Drugs Used in Coagulation Disorders

... – To prevent restenosis after coronary angioplasty – In acute coronary syndromes (unstable angina and non-Qwave acute MI) ...
Thrombolytic Medications
Thrombolytic Medications

...  Protamine Sulfate: can be given in cases of life-threatening hemorrhage to reverse the effects of heparin (binds tightly and neutralizes it) ...
Drugs and Coagulation at Point of Care
Drugs and Coagulation at Point of Care

... UFH - monitoring • Activated partial thromboplastin time (aPTT) most commonly used test to monitor heparin ...
Factor Xa inhibitors
Factor Xa inhibitors

...  Mainly ...
< 1 ... 61 62 63 64 65

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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