Lepirudin

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Image:Lepirudin.png
Lepirudin
Systematic (IUPAC) name
?
Identifiers
CAS number	120993-53-5
ATC code	B01AE02
PubChem	?
DrugBank	BTD00024
Chemical data
Formula	C288H448N80O110S6
Mol. mass	6983.5 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	~1.3 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Lepirudin (Refludan ®) is an anticoagulant which functions as a direct thrombin inhibitor. REFLUDAN was the first direct thrombin inhibitor (DTI) to be approved by the Food and Drug Administration (in 1998) for anticoagulation in patients with heparin-induced thrombocytopenia (HIT) and associated thromboembolic disease in order to prevent further thromboembolic complications (TECs). It is a recombinant hirudin, a derivative of the saliva of the medicinal leech Hirudo medicinalis.1 To date, nearly 60,000 patients have been treated with REFLUDAN worldwide.2

REFLUDAN is a bivalent, highly potent and specific direct inhibitor of both circulating and clot-bound thrombin, and has proved to be an effective and safe anticoagulant therapy for patients with HIT.1 It promotes rapid recovery of platelet counts, provides effective anticoagulation, and prevents further thromboembolic events.1, 3, 4

The principal trials for REFLUDAN were HAT-1 and HAT-2, two prospective, multicenter, historically controlled clinical studies in patients with serologically confirmed HIT. By Day 35 in the HAT-1 study, the REFLUDAN group showed a relative reduction of the cumulative risk for combined clinical endpoints (death, limb amputation, and new TECs) by 73% vs historical controls.1, 3 A meta-analysis of the HAT-1 and HAT-2 studies confirms a statistically significant difference in the combined incidence of death, new TECs, and amputations in favor of REFLUDAN vs historical control in patients with TECs. Relative risks for individual events also decreased.1, 4

The most frequently occurring adverse event in clinical trials was bleeding. With REFLUDAN, the most common adverse events were bleeding from puncture sites and wounds (14%), anemia (13%), and hematoma (11%). As with other anticoagulants, hemorrhage can occur at any site in patients receiving REFLUDAN. There have been reports of intracranial bleeding with REFLUDAN in the absence of concomitant thrombolytic therapy. Serious anaphylactic reactions that have resulted in shock or death have been reported during initial administration or upon second or subsequent re-exposure.1

[edit] External links

• DDB 30082
• Smythe M, Stephens J, Koerber J, Mattson J (2005). "A comparison of lepirudin and argatroban outcomes.". Clin Appl Thromb Hemost 11 (4): 371-4. PMID 16244762. 
• "Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin.". Blood. PMID 16690967. 
• Lubenow N, Eichler P, Lietz T, Greinacher A (2005). "Lepirudin in patients with heparin-induced thrombocytopenia - results of the third prospective study (HAT-3) and a combined analysis of HAT-1, HAT-2, and HAT-3.". J Thromb Haemost 3 (11): 2428-36. PMID 16241940. 

http://www.refludan.com/product/index.htm

v • d • e Antithrombotics (thrombolytics, anticoagulants, and antiplatelet drugs) (B01)
Vitamin K antagonists	Acenocoumarol, Clorindione, Dicumarol (Dicoumarol), Diphenadione, Ethyl biscoumacetate, Phenprocoumon, Phenindione, Tioclomarol, Warfarin
Heparin group (Platelet aggregation inhibitors)	Antithrombin III, Bemiparin, Dalteparin, Danaparoid, Enoxaparin, Heparin, Nadroparin, Parnaparin, Reviparin, Sulodexide, Tinzaparin
Other platelet aggregation inhibitors	Abciximab, Acetylsalicylic acid (Aspirin), Aloxiprin, Beraprost, Ditazole, Carbasalate calcium, Cloricromen, Clopidogrel, Dipyridamole,Eptifibatide, Indobufen, Iloprost, Picotamide, Prasugrel,Prostacyclin, Ticlopidine, Tirofiban, Treprostinil, Triflusal
Enzymes	Alteplase, Ancrod, Anistreplase, Brinase, Drotrecogin alfa, Fibrinolysin, Protein C, Reteplase, Saruplase, Streptokinase, Tenecteplase, Urokinase
Direct thrombin inhibitors	Argatroban, Bivalirudin,Dabigatran, Desirudin, Hirudin, Lepirudin, Melagatran, Ximelagatran
Other antithrombotics	Defibrotide, Dermatan sulfate, Fondaparinux, Rivaroxaban
Non-medicinal	Citrate, EDTA, Oxalate