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There are two general classes of anticoagulants.

  In vitro anticoagulants—in vitro means “in


glass”—are substances that can prevent coagulation after the blood is removed from the body
(e.g., in a test tube).  They work by preventing the activation of existing factors in the
blood.  These include Ca++ chelators like EDTA(ethylene diamine tetraacetate) and citrate, that
bind Ca++ and remove it from solution.  Reducing the Ca++concentration prevents activation of
the vitamin-K-dependent factors.  Calcium chelators cannot be used in the body, since reducing
extracellular Ca++ levels to a level sufficient to prevent coagulation would have dire
consequences:  the heart would cease to function (recall, electrical activity and excitation-
contraction coupling), synapses would cease to function (recall, the inward flow of Ca++ that
triggers synaptic release), etc.
 
Another in vitro anticoagulant is heparin.  Heparin is a mucopolysaccharide that is
normally made bymast cells (type of transformed leukocyte), and is found in particularly high
concentrations in lung tissue; presumably its function in the lungs is to maintain the blood in a
fluid state preventing blockage of small pulmonary vessels and capillaries.  Heparin prevents
coagulation (either in a test tube or in the body) principally by preventing activation of thrombin,
but it also (to a lesser extent) prevents the activation of other factors.  Heparin works in glass test
tubes, but it can also be used clinically in patients.  A problem, however, with the clinical use of
heparin is that it cannot be given orally—it is degraded by digestive enzymes prior to
absorption.  Thus, it must be given intravenously, and this can be problematic.  Namely, the
injection site itself is an injury with a tendency to bleed; injecting the heparin prevents clotting at
the injection site, and the patient usually develops a bruise (blood oozing out of the vein under
the skin).  Thus other drugs that can be administered orally are usually used for long-term
treatment of patients prone to thromboembolisms.
 
            The other class of anticoagulants are in vivo anticoagulants—in vivo means “in
life.”  These types of anticoagulands are ineffective in preventing clotting involving existing
clotting factors (i.e., the anticoagulants are not effective in vitro).  Rather, these factors act by
inhibiting the production of new clotting factors by the liver, and this is why they only work in
vivo.  An advantage to using these drugs is that they can be given orally, thereby avoiding the
unpleasant bruising when administering heparin intrevenously.  Thus, these drugs are clinically
referred to as oral anticoagulants.
 

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