PMID- 19132170
OWN - NLM
STAT- MEDLINE
DCOM- 20090226
LR  - 20181201
IS  - 0720-9355 (Print)
IS  - 0720-9355 (Linking)
VI  - 28
IP  - 5
DP  - 2008 Dec
TI  - [Pharmacology of heparins and direct anticoagulants].
PG  - 400-20
AB  - For decades, the options for therapeutic anticoagulation were limited to 
      unfractionated heparin (UFH) and vitamin K antagonists (VKA), and their 
      well-known limitations had to be accepted. With the introduction of the various 
      LMWHs, the short- and medium-term anticoagulation could be much improved, but an 
      alternative to VKA is still missing The heparins provided the proof of concept 
      that FXa and thrombin represent suitable targets for therapeutic anticoagulation. 
      Consequently, the search for new anticoagulants focuses on inhibitors of thrombin 
      (DTI) or FXa (DXI). Apart from the VKA, the anticoagulants presently available or 
      in an advanced stage of development can thus be divided in two classes: One are 
      the glyco-anticoagulants with the natural sulfated glycosaminoglycans (GAGs) 
      (UFH, LMWHs, and danaparoid) and the synthetic oligosaccharides (OS) 
      (fondaparinux, idraparinux, and SR123781A). The other class are the xenobiotic 
      anticoagulants, i.e. proteins and synthetic chemical entities. Die 
      glyco-anticoagulants act partially (GAGs) or exclusively (oligosaccharides) by 
      catalysing antithrombin, whereas the xenobiotic anticoagulants are direct 
      inhibitors of either thrombin or FXa. At present, three parenteral DTI 
      (lepirudin, argatroban, and bivalirudin) and since March 2008 one oral DTI 
      (dabigatran etexilate) are clinically used for limited indications. In September 
      2008 rivaroxaban has been approved as the first oral DXI. This review describes 
      the development of the anticoagualants as well as the pharmacological profile of 
      the clinically used anticoagualants.
FAU - Alban, S
AU  - Alban S
AD  - Pharmazeutisches Institut, Christian-Albrechts-Universitat, Kiel. 
      salban@pharmazie.uni-kiel.de
LA  - ger
PT  - Journal Article
PT  - Review
TT  - Pharmakologie der Heparine und der direkten Antikoagulanzien.
PL  - Germany
TA  - Hamostaseologie
JT  - Hamostaseologie
JID - 8204531
RN  - 0 (Anticoagulants)
RN  - 0 (Antithrombins)
RN  - 0 (Glycosaminoglycans)
RN  - 0 (Oligosaccharides)
RN  - 0 (Polysaccharides)
RN  - 0 (Recombinant Proteins)
RN  - 6ADD3H8MFZ (idraparinux)
RN  - 9005-49-6 (Heparin)
RN  - J177FOW5JL (Fondaparinux)
SB  - IM
MH  - Anticoagulants/pharmacokinetics/pharmacology/*therapeutic use
MH  - Antithrombins/therapeutic use
MH  - Fondaparinux
MH  - Glycosaminoglycans/therapeutic use
MH  - Heparin/pharmacology/*therapeutic use
MH  - Humans
MH  - Oligosaccharides/pharmacokinetics/pharmacology/therapeutic use
MH  - Partial Thromboplastin Time
MH  - Polysaccharides/pharmacokinetics/therapeutic use
MH  - Recombinant Proteins/pharmacokinetics/pharmacology/therapeutic use
MH  - Structure-Activity Relationship
MH  - Thrombocytopenia/drug therapy
RF  - 161
EDAT- 2009/01/10 09:00
MHDA- 2009/02/27 09:00
CRDT- 2009/01/10 09:00
PHST- 2009/01/10 09:00 [entrez]
PHST- 2009/01/10 09:00 [pubmed]
PHST- 2009/02/27 09:00 [medline]
AID - 08050400 [pii]
PST - ppublish
SO  - Hamostaseologie. 2008 Dec;28(5):400-20.