Which of the following is a univalent direct thrombin inhibitor?
Correct Answer: Argatroban
Description: Ans. is 'a' i.e., Argatroban Direct thrombin inhibitors (DTIs)o This is a class of medications that act as anticoagulants by directly inhibiting the thrombin (unlike heparin which inhibits thrombin indirectly through antithrombin - so, heparin is an indirect thrombin inhibitor),o Drugs in this class are :UnivalentBivalento Argatrobano Melagatrano Dabigatrano Hirudino Bivafirudino Lepirudino Desirudino Ximelagatran is prodrug of melagatran and can be given orally, all other drugs are used parenterally (IV, IM or SC), except for Dabigatran which can also be given orally,o All these drugs (except agratroban) are excreted by kidney - should be avoided in renal failure.o Agratroban is secreted in bile - safe in renal failure,o UsesThese are the anticoagulant of choice for heparin induced thrombocytopenia.Bivalent DTIs can be used in circumstances where heparin would be indicated but cannot be used, such as the acute coronary syndrome (unstable angina)Ximelagatran showed good efficacy in prevention and treatment of DVT and thromboprophylaxis in AF. However, development wras stopped by manufacturer because of reports of liver failure.Other anticoagulantso Danaparoid (mixture of 84% heparan sulfate, 12% dermatan sulfate and 4% chondrioitin sulfate) is approved for prophylaxis of DVT. It is also effective for HIT syndrome. It mainly promotes inhibition of factor Xa by antithrombin.o Rodenticides contain long acting anticoagulants like bromadiolone, brodifacoum, diphenadione, chlorphenacinone and pindone. Treatment is Vit. K.o Drotrecogin alfa is a recombinant form of human activated protein C that inhibits coagulation by proteolytic inactivation of factor Va and Villa. It also has anti-inflammatory activity. It decreases mortality in patients with severe sepsis.
Category:
Pharmacology
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