Dabigatran

Class	Direct thrombin inhibitor
Chemistry	Small molecule polypeptide
Routes of administration	Oral only
Absorption	Available as dabigatran etexilate, which is a pro-drug; dabigatran on its own is mch too polar to be absorbed effectively. The exetilate is rapidly absorbed High oral bioavailablility (~ 100%) Maximum blood concentration ~ 90-180 minutes after intake.
Solubility	pKa 4.0, solubility in water is not very good
Distribution	VOD=1.0L/kg; 35% protein-bound
Metabolism	Mainly renally excreted as unchanged drug; but about 20% is conjugated with glucuronic acid to form acylglucuronides. These conjugates are pharmacologically active and demonstrate almost identical properties of free, unconjugated dabigatran.
Elimination	80% renal excretion of unchanged drug 20% biliary excretion of acylglucouronides
Time course of action	Half life = 12-14 hours
Target receptor	Thrombin
Mechanism of action	Dabigatran interacts with the active site of thrombin, and acts as a competitive inhibitor of thrombin. It inactivates thrombin, including fibrin-bound thrombin. This is a reversible reaction. Some thrombin remains active to produce haemostasis.
Clinical effects	Bleeding, insomnia, fever, periphral oedema
Literature reference	TGA PI document
CICM details of understanding	Level 2
Mentioned around Deranged Physiology	Warfarin and other oral anticoagulants
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