A critical pentasaccharide sequence inheparin molecules is required for their binding to ATIII and for promoting the change in conformation of ATIII. In unfractionated heparin, which has a molecular size distribution of 5,000 to 30,000 d, with the majority of chains containing ≥ 18 saccharide units and LMWHs (CLEXANE), produced by chemical or enzymatic depolymerization of unfractionated heparin to yield molecular species that range from 1,000 to 10,000 d,only approximately 30% of the molecules present in heparin preparations contain the ATIII-binding sequence. The remainder is composed of polyanionic chains that may bind nonspecifically, through electrostatic interactions, to a large number of other plasma proteins. This phenomenon possibly accounts for some of the undesirable side effects of LMWH like HIT. well-defined pentasaccharides constitutes more potent, more selective, and consequently safer drugs. fondaparinux (ARIXTRA) is a synthetic pentasaccharide that selectively inhibits factor Xa.
Friday, June 12, 2009
enoxaparin & fondparinux
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