Direct and indirect antithrombins: Heparins, low molecular weight heparins, heparinoids, and hirudin

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

With the eclipse of UH by newer anticoagulants, the field has opened up to search for new and better drugs. Hirulog or bivalirudin is another direct antithrombin that has been used in initial trials. It is smaller than hirudin, at 20 amino acids. Currently under investigation, it seems to have a short half-life, a narrow therapeutic window, and a reverse dose effect, with lower levels achieving better cardiac post-thrombolysis patency than higher doses. Other antithrombins being examined are the hirudisins, where four amino acids of hirudin have been replaced by the RGDS integrin-binding sequence and thrombin receptor antagonist peptides. In addition, many other inhibitors of activated clotting factors are being studied for future therapeutic value. Tick anticoagulant protein studies are underway, as are studies on a group of benzamidine isoxazoline derivates, which are direct Xa inhibitors. We are truly at an age of discovery with the newer anticoagulants and it may take many years until we can distinguish the advantages and disadvantages of all the newer therapies. It looks like an ever more real possibility that medicine may find an antithrombotic regimen that is highly effective, highly reversible, and nontoxic.

Original languageEnglish (US)
Pages (from-to)15-29
Number of pages15
JournalClinics in Geriatric Medicine
Volume17
Issue number1
StatePublished - 2001

Fingerprint

Heparinoids
Hirudins
Antithrombins
Low Molecular Weight Heparin
Anticoagulants
Heparin
Arthropod Proteins
Thrombin Receptors
Amino Acids
Blood Coagulation Factors
Integrins
Half-Life
Therapeutics
Medicine
Peptides
Pharmaceutical Preparations
bivalirudin

ASJC Scopus subject areas

  • Geriatrics and Gerontology

Cite this

@article{04c6c49a892b48cf9eb985a49b13d960,
title = "Direct and indirect antithrombins: Heparins, low molecular weight heparins, heparinoids, and hirudin",
abstract = "With the eclipse of UH by newer anticoagulants, the field has opened up to search for new and better drugs. Hirulog or bivalirudin is another direct antithrombin that has been used in initial trials. It is smaller than hirudin, at 20 amino acids. Currently under investigation, it seems to have a short half-life, a narrow therapeutic window, and a reverse dose effect, with lower levels achieving better cardiac post-thrombolysis patency than higher doses. Other antithrombins being examined are the hirudisins, where four amino acids of hirudin have been replaced by the RGDS integrin-binding sequence and thrombin receptor antagonist peptides. In addition, many other inhibitors of activated clotting factors are being studied for future therapeutic value. Tick anticoagulant protein studies are underway, as are studies on a group of benzamidine isoxazoline derivates, which are direct Xa inhibitors. We are truly at an age of discovery with the newer anticoagulants and it may take many years until we can distinguish the advantages and disadvantages of all the newer therapies. It looks like an ever more real possibility that medicine may find an antithrombotic regimen that is highly effective, highly reversible, and nontoxic.",
author = "Billett, {Henny H.}",
year = "2001",
language = "English (US)",
volume = "17",
pages = "15--29",
journal = "Clinics in Geriatric Medicine",
issn = "0749-0690",
publisher = "W.B. Saunders Ltd",
number = "1",

}

TY - JOUR

T1 - Direct and indirect antithrombins

T2 - Heparins, low molecular weight heparins, heparinoids, and hirudin

AU - Billett, Henny H.

PY - 2001

Y1 - 2001

N2 - With the eclipse of UH by newer anticoagulants, the field has opened up to search for new and better drugs. Hirulog or bivalirudin is another direct antithrombin that has been used in initial trials. It is smaller than hirudin, at 20 amino acids. Currently under investigation, it seems to have a short half-life, a narrow therapeutic window, and a reverse dose effect, with lower levels achieving better cardiac post-thrombolysis patency than higher doses. Other antithrombins being examined are the hirudisins, where four amino acids of hirudin have been replaced by the RGDS integrin-binding sequence and thrombin receptor antagonist peptides. In addition, many other inhibitors of activated clotting factors are being studied for future therapeutic value. Tick anticoagulant protein studies are underway, as are studies on a group of benzamidine isoxazoline derivates, which are direct Xa inhibitors. We are truly at an age of discovery with the newer anticoagulants and it may take many years until we can distinguish the advantages and disadvantages of all the newer therapies. It looks like an ever more real possibility that medicine may find an antithrombotic regimen that is highly effective, highly reversible, and nontoxic.

AB - With the eclipse of UH by newer anticoagulants, the field has opened up to search for new and better drugs. Hirulog or bivalirudin is another direct antithrombin that has been used in initial trials. It is smaller than hirudin, at 20 amino acids. Currently under investigation, it seems to have a short half-life, a narrow therapeutic window, and a reverse dose effect, with lower levels achieving better cardiac post-thrombolysis patency than higher doses. Other antithrombins being examined are the hirudisins, where four amino acids of hirudin have been replaced by the RGDS integrin-binding sequence and thrombin receptor antagonist peptides. In addition, many other inhibitors of activated clotting factors are being studied for future therapeutic value. Tick anticoagulant protein studies are underway, as are studies on a group of benzamidine isoxazoline derivates, which are direct Xa inhibitors. We are truly at an age of discovery with the newer anticoagulants and it may take many years until we can distinguish the advantages and disadvantages of all the newer therapies. It looks like an ever more real possibility that medicine may find an antithrombotic regimen that is highly effective, highly reversible, and nontoxic.

UR - http://www.scopus.com/inward/record.url?scp=0035112907&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0035112907&partnerID=8YFLogxK

M3 - Article

C2 - 11270128

AN - SCOPUS:0035112907

VL - 17

SP - 15

EP - 29

JO - Clinics in Geriatric Medicine

JF - Clinics in Geriatric Medicine

SN - 0749-0690

IS - 1

ER -