Drug intelligence / Profile preview

unfractionated heparin + vitamin k antagonist

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Subcutaneous, Oral
01

Overview

This is a **combination of two anticoagulant drugs: unfractionated heparin and a vitamin K antagonist (such as warfarin)**. Both drugs are used to prevent and treat conditions related to abnormal blood clotting, such as atrial fibrillation, venous thromboembolism, and for perioperative anticoagulation management. - **Unfractionated heparin** is a parenteral anticoagulant that rapidly inhibits clotting by activating antithrombin, thereby inactivating thrombin and factor Xa, and other proteases involved in blood clotting. - **Vitamin K antagonists** (most commonly warfarin) are oral anticoagulants that inhibit the enzyme vitamin K epoxide reductase, which is necessary to recycle vitamin K required for the synthesis of active clotting factors II, VII, IX, and X, as well as proteins C and S. This combination is often used as “bridging” therapy: unfractionated heparin is started together with a vitamin K antagonist at therapy initiation because vitamin K antagonists have a slow onset of action and can paradoxically increase clotting risk at the start by lowering protein C and S before lowering circulating clotting factors. Heparin provides rapid anticoagulation until the vitamin K antagonist becomes fully effective, after which heparin is discontinued[1][3][4][5]. The combination is not available as a fixed-dose pharmaceutical product but rather is a clinical regimen where both agents are administered concomitantly.

02

Targets

F2 (Thrombin)F9 (Coagulation Factor IX)F10 (Factor Xa)F7 (Coagulation Factor VII)ATIII (Antithrombin III)VKORC1 (Vitamin K epoxide reductase complex subunit 1)PROC (Protein C)

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