Heparin and Its Low Molecular Weight Derivatives: Anticoagulant and Antithrombotic Properties

Holmer, E.; Söderberg, Karin; Bergqvist, David; Lindahl, Ulf

doi:10.1159/000215348

Cited by 33 publications

(22 citation statements)

References 15 publications

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“…For the heparin -antithrombin complex to create a bridge to thrombin, it takes a chain of at least 18 saccharides, while for factor Xa inactivation, just one pentasaccharide molecule is needed (Bjork and Lindahl, 1982;Olson and Shore, 1982;Turpie, 1998). Needless to say, dekaoctosaccharide (19 monomers) or a bigger molecule is present in all UFH preparations, but only in 25 to 50% of all LMWH's (Holmer et al, 1981;Lindahl et al, 1984;Holmer et al, 1986). For this reason LMWH's are more or less Xa-selective inhibitors, while the anticoagulant activity of UFH is approximately the same for both factors (anti IIa : anti Xa ~ 1 : 1) (Hirsh, 1991).…”

Section: Anticoagulation Properties Of Lmwh'smentioning

confidence: 99%

Heparin and its derivatives in the treatment of arterial thrombosis: a review

Dvořák¹,

Vlašín²,

Dvorakova³

et al. 2010

Vet. Med. - Czech

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Arterial occlusion due to thrombosis caused by ruptured atherosclerotic plaques (Baba et al., 1975) has been recognized as a major cause of morbidity and mortality in western populations. Thrombosis may occur in various sections of arterial circulation, peripheral arteries of the limbs, coronary arteries, brain arteries, or both major and minor vessels within the abdominal cavity. The ultimate consequence is varying degrees of organ failure, mostly of ischemic origin. Arterial thrombosis represents a continuous problem, debilitating patients and decreasing their quality of life. Moreover, along with chronic heart failure, it can significantly decrease patient life expectancy. Arterial thrombosis results in ischemia, with serious systemic consequences, such as metabolic breakdown. The major goal of treatment remains fast and efficient recanalization -surgical, interventional or thrombolytic. To be able to prevent acute reocclusion with severe consequences (rhabdomyolysis, compartment syndrome, excessive tissue necrosis leading to limb amputation, etc.), several adjunctive treatment regimens have been advocated. Among others, thrombin inhibitors and platelet inhibitors have been widely used for both prophylaxis and adjunctive treatment. Direct thrombin inhibitors and antithrombin stimulators have been recognized as typical antithrombotic drugs. Direct (antithrombin-independent) thrombin inhibitors can be divided into two main categories: monovalent, active site inhibitors (argatroban, efegatran, inovastan, melagatran) and bivalent (hirudin, hirugen, hirulog, bivalirudin), while antithrombin stimulators represent standard (unfractionated) heparin (UFH) and its depolymerizing products -low molecular weight heparins (LMWH's). Recently, a clear change in the main use of heparin, as well as low-molecular weight heparins has been advocated representing a shift from treatment and prophylaxis of deep vein thrombosis to prophylaxis of thromboembolic disease following vascular, cardiovascular or orthopedic surgery, treatment of unstable angina and prevention of acute myocardial infarction. The main effect of heparins lies in their anticoagulant activity. Heparins are involved in different pathways of the coagulation cascade with anticoagulant, antithrombotic, profibrinolytic, anti-aggregative, as well as anti-inflammatory effects. Moreover, there is a little doubt about their anti-proliferative and anti-ischemic activity (Penka and Bulikova, 2006). Unlike standard heparin, low-molecular weight heparins do not affect the patient's general coagulation profile. Obviously, the difference in molecular weight results in different pharmacokinetic and pharmacodynamic properties of the agents.Key words: coagulation; arterial thrombosis; standard heparin; low-molecular weight heparins List of abbreviations ABI = axillary/...index, t-PA = tissue-type plasminogen activator, ADP = adenosin diphosphate, AG = angiography, AMI = acute myocardial infarction, APSAC = acylated plasminogen streptokinase activator complex, APTT = acti...

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Section: Anticoagulation Properties Of Lmwh'smentioning

confidence: 99%

Heparin and its derivatives in the treatment of arterial thrombosis: a review

Dvořák¹,

Vlašín²,

Dvorakova³

et al. 2010

Vet. Med. - Czech

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show abstract

“…The explanation for the difference in anticoagulant profile between LMWH and heparin was elucidated in subsequent studies (Table 10). 29,30,[212][213][214][215][216] …”

Section: Low-molecular-weight Heparins Historical Perspectivementioning

confidence: 99%

“…In contrast, all LMWH chains containing the high-affinity pentasaccharide catalyze the inactivation of factor Xa (Figure 3). Because virtually all heparin molecules contain at least 18 saccharide units, 213,214 heparin has an anti-factor Xa to anti-factor IIa ratio of 1:1. In contrast, commercial LMWHs have anti-factor Xa to anti-IIa ratios between 2:1 and 4:1, depending on their molecular size distribution.…”

Section: Anticoagulant Effectsmentioning

confidence: 99%

Guide to Anticoagulant Therapy: Heparin

Hirsh¹,

Anand²,

Halperin³

et al. 2001

ATVB

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“…A ação anticoagulante é pró-pria das heparinas de alto peso molecular (HAPM > 15.000 Daltons). São características da heparina de elevada ação anticoagulante: 1) possuir alto peso molecular (16,17) ; 2) ter grande afinidade pela antitrombina (18) ; 3) conter alta densidade e homogeneidade de cargas aniônicas (15) .…”

Section: Introductionunclassified

“…As heparinas de baixo peso molecular (HBPM < 6.000 Daltons) têm atividade antitrombótica, aceleram a inibição do fator Xa (19) e interagem com as plaquetas (20) , sem atuarem na trombina (19) . Desde o modo original de se preparar fragmentos de heparina com ácido ascórbico, usando-se sulfato de cobre como catalizador (21) , muitos outros foram introduzidos.…”

Section: Introductionunclassified