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Titolo:
FACTOR XA VERSUS FACTOR IIA INHIBITORS
Autore:
KAISER B;
Indirizzi:
UNIV JENA,CTR VASC BIOL & MED ERFURT,FAC MED,NORDHAUSER STR 78 D-99089 ERFURT GERMANY
Titolo Testata:
Clinical and applied thrombosis/hemostasis
fascicolo: 1, volume: 3, anno: 1997,
pagine: 16 - 24
SICI:
1076-0296(1997)3:1<16:FXVFII>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
TICK ANTICOAGULANT PEPTIDE; COAGULATION FACTOR-XA; DISSEMINATED INTRAVASCULAR COAGULATION; SYNTHETIC THROMBIN INHIBITORS; ACTIVATOR-INDUCED REPERFUSION; FEMORAL ARTERIAL THROMBOSIS; BOVINE FACTOR-XA; RECOMBINANT HIRUDIN; CANINE MODEL; ANTITHROMBOTIC ACTION;
Keywords:
ANTICOAGULANTS; ANTITHROMBOTICS; FACTOR XA INHIBITORS; THROMBIN INHIBITORS;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
63
Recensione:
Indirizzi per estratti:
Citazione:
B. Kaiser, "FACTOR XA VERSUS FACTOR IIA INHIBITORS", Clinical and applied thrombosis/hemostasis, 3(1), 1997, pp. 16-24

Abstract

The development of specific inhibitors of blood coagulation enzymes has led to a number of new anticoagulant/antithrombotic agents that could be useful for prophylaxis and/or treatment of thromboembolic disorders. Because thrombin is the central bioregulatory enzyme in hemostasis, blocking of the active site of the enzyme by a fast reaction with an inhibitor may effectively prevent intravascular coagulation as well as other important biological effects of thrombin. For the direct inactivation of thrombin, several classes of compounds have been developedand characterized in vitro and in vivo as potential antithrombotic agents including natu rally occurring as well as synthetic thrombin inhibitors such:ls hirudin, hirulog, arginine (argatroban), and benzamidine (NAPAP) derivatives as well as tripeptide-type inhibitors (efegatran, D-Phe-Pro-Arg-CH2Cl, boroarginine derivatives). Experimental findings suggest that directly acting thrombin inhibitors may be effective ina wide range of arterial and venous thrombotic events. The important role of factor Xa in the coagulation cascade at the stage of the conversion of extrinsic and intrinsic pathways and the amplification of itsprocoagulant action by prothrombinase complex formation makes factor Xa a promising target also for antithrombotic drugs. Experimental studies on highly effective and selective factor Xa inhibitors (antistasin, tick anticoagulant peptide, yagin, DX-9065a) showed that inhibition of coagulation at a relatively early stage is a very effective way forthe prevention of thrombotic processes. Furthermore, it is assumed that factor Xa inhibitors selectively inhibit thrombus formation withoutcompromising hemostasis. In conclusion, both thrombin and factor Xa inhibitors are promising drugs for the management of thrombotic disorders. However, besides the strong inhibitory potency against the target enzyme, other pharmacological aspects such as pharmacodynamics, pharmacokinetics, and toxic side effects must be included in the evaluation of the potential usefulness of thrombin and factor Xa inhibitors for clinical indications.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/12/20 alle ore 14:23:53